ITRACONAZOLE

Pharmacological action

Antifungal, triazole derivatives. The mechanism of action associated with the ability to inhibit cytochrome P 450-dependent enzymes of sensitive fungi, which leads to disruption of the synthesis of ergosterol of the cell wall of the fungus. It has a broader spectrum anti-fungal activity than ketoconazole. It is active against Aspergillus spp., Blastomyces dermatitidis, Candida, Coccidioides immitis, Cryptococcus neoformans, Epidermophyton, Microsporum, Trichophyton, Histoplasma capsulatum, Malassezia furfur, Paracoccidioides brasiliensis, Sporothrix schenckii.


Pharmacokinetics

Therapeutic concentrations in the skin persist for 2-4 weeks after the end of a 4-week course of treatment. Itraconazole is defined in the keratin of nails in a week after the start of treatment and lasts for 6 months after the end of the 3-month course of therapy.


Statement

Vulvovaginal candidiasis, mycoses of the skin, mouth, eyes, onychomycosis caused by dermatophytes and / or yeast, systemic mycosis (including systemic aspergillosis, candidiasis, cryptococcosis, histoplasmosis, sporotrichosis, parakoktsidioidoz, blastomycosis, and other rare tropical and systemic mycoses).


Dosage regimen

Inside of 100 mg 1 time / d or 200 mg 1-2 times / day, duration of treatment depends on the etiology of disease.


Side effect

Co of the digestive system: stomach aches, nausea, vomiting, constipation, increased activity of liver enzymes, cholestatic jaundice, and in some cases - hepatitis.

The part of the CNS and peripheral nervous system: headache, dizziness, and in some cases - peripheral neuropathy.

Since the cardiovascular system: in some cases - edema, congestive heart failure and pulmonary edema.

Allergic reactions: skin rash, itching, urticaria, angioedema, Stevens-Johnson syndrome.

Other: long-term use - dysmenorrhea, hair loss, hypokalemia.


Contraindications

Simultaneous ingestion terfenadina, astemizola, mizolastina, tsizaprida, dofetilida, quinidine, pimozida, simvastatin, lovastatin, midazolam, or triazolama; sensitivity to itraconazole.


Application of pregnancy and breastfeeding

Itraconazole is used during pregnancy only if systemic mycosis when the expected effect of therapy outweighs the potential risk to the fetus.

Women of childbearing age in the period of itraconazole is recommended to use contraceptives.

If necessary, use during lactation should decide on the termination of breastfeeding.

In experimental studies found that itraconazole has embryotoxicity and causes abnormal development of the fetus.


Cautions

Should not be used in patients with symptomatic ventricular dysfunction and indications in history to congestive heart failure.

You should not use itraconazole in patients with liver disease. However, in cases of extreme necessity in liver cirrhosis and / or breach of renal function itraconazole treatment is performed under the control of its level in plasma and with appropriate dose adjustment.

When the activity of liver transaminases Itraconazole is used in cases where the expected benefit of therapy exceeds the potential risk of liver damage.

In the case of itraconazole over 1 month is necessary to monitor liver function.

With the development during the treatment of symptoms of heart failure, abnormal liver function, peripheral neuropathy itraconazole should be abolished.

With careful use itraconazole sensitivity to other derivatives of Asola.

Use in Pediatrics

Currently, insufficient data on the use of itraconazole in children.


Drug Interactions

Vehicles causing an induction of liver enzymes (rifampicin, phenytoin) may decrease the concentration of itraconazole in plasma.

When applied simultaneously with drugs that reduce gastric acidity (including m-holinoblokatory, antacid, histamine blockers H 2-receptor), may decrease absorption of itraconazole.

With the simultaneous use of drugs, the metabolism of which involve the participation of isozymes 3A cytochrome P 450 may increase in intensity and / or duration of their effects. These drugs include terfenadin, astemizol, tsizaprid, midazolam, triazolam (Oral), indirect anticoagulants, cyclosporine, digoxin, calcium channel blockers, quinidine, vincristine.

Heparin sodium+Benzocaine+Benzonicotinic acid

International name:
Heparin sodium + benzocaine + Benzonikotinovaya acid (Heparin sodium + Benzocaine + Benzonicotinic acid)

Group Affiliation:
Anticoagulant line for local use

Description of the active substance (INN):
Heparin sodium + benzocaine + Benzonikotinovaya acid

Dosage form:
ointment for external use

Mode of action:
Combined preparation for external use, the effect is caused by properties of its constituent components. Anticoagulant of direct action. Eventually release of heparin sodium ointment reduces inflammation and has antithrombotic effects. Promotes the resorption of existing and prevents the formation of new clots. It blocks the synthesis of thrombin, reducing platelet aggregation. Inhibits the activity of hyaluronidase, activates the fibrinolytic properties of blood. Benzyl ester of nicotinic acid increases the surface blood vessels, promoting absorption of heparin. The local anesthetic benzocaine reduces the severity of pain. When applied to the skin has a local analgesic effect.

Indications:
Thrombophlebitis of superficial veins (prevention and treatment), and postinektsionny postinfuzionny phlebitis, external hemorrhoids, inflammation, postnatal hemorrhoids, sores leg, elephantiasis, surface periflebit, lymphangitis, mastitis superficial, localized infiltrates and edema, trauma and injuries (including muscle tissue, tendons, joints), subcutaneous hematoma.

Contraindications:
Hypersensitivity, ulcerous-necrotic processes, violating the integrity of skin pokrovov.C caution. Thrombocytopenia, increased bleeding.

Side effects:
Skin hyperemia, allergic reactions.

Dosage and administration:
Outwardly. The ointment is applied a thin layer to affected area (estimated at 0.5-1 g per plot with a diameter of 3-5 cm) and gently rubbed into the skin 2-3 times a day every day until the disappearance of inflammation, on average, from 3 to 7 days. The possibility of a longer course of treatment is determined by your doctor. Thrombosis of external hemorrhoids, rectal swabs are used, ointment is applied to calico or linen strip, which is imposed directly on the thrombosed parts and fix. The ointment should be applied daily until symptoms disappear, an average of 3-14 days. With the same purpose, you can use a swab soaked with grease, which is introduced into the anus.

Cautions:
Should not be applied to open wounds, in the presence of purulent processes. Application of the ointment is not recommended for deep venous thrombosis.

Interaction:
Do not appoint local concurrently with NSAIDs, tetracycline antibiotics, antihistamine drugs.

ALPHAREKIN

Pharmacological properties: Alfarekin similar natural leukocyte interferon, has three main types of biological activity: immunomodulating, antiviral and anticancer.
The mechanism of action Alfarekina based on the binding of IFN to specific receptors of cells of the body, resulting in triggered cascade of intracellular reactions, and synthesis of enzymes which depress viral replication, increased phagocytic activity of macrophages and lymphocytes specific cytotoxicity on target cells, inhibiting proliferation of metastatic cells.

INDICATIONS: in the complex therapy of children and adults with:
Viral hepatitis B and C;
acute viral, bacterial and mixed infections (including neonatal);
acute and chronic purulent diseases of viral and bacterial origin;
herpetic infections of different localization: (tinea, multiple cutaneous herpetic eruptions, genital herpes infection, herpetic keratoconjunctivitis and keratouveit, etc.);
chronic urogenital chlamydiosis;
lesions of the nervous system with mono-and poliradikulyarnym pain syndrome;
laryngeal papillomatosis;
multiple sclerosis;
malignancies: melanoma of skin and eye cancer, kidney, bladder, ovaries, breast cancer, Kaposi's sarcoma, myeloma;
hemoblastosis: chronic myeloid leukemia, volosatokletochnoy leukemia, non-Hodgkin's lymphoma.

APPLICATION: rr Alfarekina injected i / m, n / k / v, endolimfalno, intraperitoneal, intravesical, rectal, parabulbarno, intranasal. The dissolution of the contents of the vial in 1 ml of water as a solvent used for injection by dissolving the contents of the vial at a higher level using physiological pp.
Acute hepatitis B:
introduced on 1 million IU (in severe cases - by 2 million IU) in / m 2 twice daily for 10 days. The course of treatment may be extended to 2-3 weeks, depending on the patient's general condition, or extended by 1 million IU 2 times a week for several weeks.
Chronic viral hepatitis B:
injected i / m for 3-4 million IU 3 times a week for 2 months.
Chronic viral hepatitis C:
introduced into / m 3 million IU 3 times a week for 6 months as monotherapy or in combination with drugs-nucleoside analogues.
SARS in children (including newborns):
injected intranasally with 2-3 drops into each nasal passage 3-6 times a day for 3-5 days; dosage for newborns - 20-50 thousand IU / ml, for children of other age groups - 100 thousand IU / ml.
Acceptable introduction to the nasal passages (alternately) padded turundae wetted Alfarekinom, 10-15 min.
ARI (including influenza) in adults:
injected i / m by 1-3 million IU, beginning with 1-2 days of disease within 3 days;
intranasal imposed on 4-6 drops of p-ra Alfarekina (100 thousand IU / ml) in each nasal passage 6-8 times a day (to be entered using a dose Alfarekina should be heated in the syringe (use a syringe without the needle) to body temperature, the rest rr stored in the refrigerator, protected from bacterial contamination).
Acute and recurrent viral pneumonia and viral-bacterial etiology:
V / m at 1 million IU for 5-7 days in the complex treatment, including antibacterial, detoxication, anti-inflammatory therapy.
Acute diarrheal syndrome in infants:
rectally in the form of daily mikroklizmochek containing 100 thousand IU Alfarekina within 3-7 days.
Acute intestinal infections in young children with symptoms hypocoagulation:
injected rectally in a dose of 10 thousand IU / kg body weight 3 times with an interval of 48 h.
Purulent-septic disease, peritonitis, multiple abscesses of the abdominal cavity:
in / on 2-4 million IU 1 time per day, total dose: 12-16 million IU per course of treatment.
HSV infection:
zoster: daily / m - 1 million IU, and 2 million IU in 5 ml of physiological p-ra n / a at several points around the zone of the rash. Duration of treatment - 5-7 days.
cutaneous herpetic eruptions: 2 million IU / m or s / c (around lesion) daily; treatment can be combined with local application (applications) on herpetic papules.
Genital herpes infection: 2 million IU / m daily in combination with local application of the drug in the form of applications to the region of eruption.
herpetic keratoconjunctivitis: 1 million IU Alfarekina dissolved in 5 ml of physiological p-ra, injected conjunctiva with 2-3 drops every 2 h for 7-10 days, with decreasing severity of symptoms of a drug can enter every 4 hours
Chronic urogenital chlamydia:
Alfarekin used in complex therapy - to 1 million IU / m 1 times a day in the evening, on a course of treatment - 10 injections.
The defeat of the nervous system with mono-and poliradikulyarnym pain syndrome:
of 1 million IU / m for 5-10 days in the complex therapy.
Laryngeal papillomatosis:
in / m (if possible - in the perifocal area of the larynx) introduction Alfarekina a dose of 100-150 thousand IU / kg of body weight daily for 20-25 days. It is recommended to repeat this course of treatment with an interval of 1-1,5 months within 6 months, followed at intervals of 2-3 months for the next 6 months.
Multiple sclerosis:
V / m at 1 million IU 2-3 times a day for 10-15 days, then - by 1 million IU 1 times per week for 6 months.
Malignancies
Melanoma of the skin - by 3 million IU / m 1 times a day - 10 days with an interval of 1.5 months of repeating this course for 6 months;
or: by 3 million IU Alfarekina 4 times with an interval of 48 hours - endolimfalno followed lymphotropic drug administration for 1 million IU for 4 days every month.
Uveal melanoma: the 1 million IU parabulbarno daily for 10 days, 20 days later to repeat the course within 10 days, 2 times; dose of the drug on the general course of treatment is 30 million IU. Can not exclude the need for repeated courses in 45 days; treatment Alfarekinom combined with photodestruction of the tumor and beta applications.
Kidney cancer: by 3 million IU / m, daily for 10 days, the overall rate - 30 million IU, refresher courses held at intervals of 3-5 weeks for 6 months, and then at intervals of 1,5-2 months in within 1 year.
Bladder cancer: intravesical instillation in the form of, for 5-10 million IU per instillation, 3-6 times. The total course dose - 30 million IUs. The treatment is repeated every 2-3 months for 1 year-2 years.
Cancer of the ovary: 5 million IU injected intraperitoneally during surgery and in the next 5 days - in the drainage, then - at 3 million IU / m for 10 days between courses of chemotherapy, the total course dose Alfarekina of 90 million IU. Subsequent courses may be assigned at intervals of 2-3 months for 1-1,5 years: by 3 million IU / m every day - 10 days.
Breast Cancer: by 3 million IU per injection in / m, daily for 10 days. Repeated courses are held at intervals 1,5-2 months to 1 year and then every 2-3 months (depending on the clinical condition of the patient), appropriate alternate therapy Alfarekinom with courses of chemotherapy (or radiotherapy).
Kaposi's sarcoma: by 3 million IU per injection in / m, daily for 10 days; treatment combined with monohimioterapiey prospidin; repeated courses - 1 time per month for 6 months.
Multiple myeloma: by 3 million IU per injection in / m, daily for 10 days, a second course - 1 times 1,5-3 months (4-6 courses during the year).
Hemoblastosis
Chronic myeloid leukemia: 5 million IU / m daily.
Apply as in the form of mono-and chemotherapy in the complex. Duration of treatment - 6 months. When the phase of remission maintenance therapy Alfarekinom a dose of 5 million IU daily performed within 10-12 months.
Volosatokletochnaya leukemia: from 3 million IU 3 times a week / m (a day) for 4-6 weeks. When the phase of remission maintenance therapy is carried out: by 3 million IU a day - up to 12 months.
Non-Hodgkin's lymphoma: by 3 million IU 3 times a week / m over 12-18 months as maintenance therapy in achieving remission phase reached as a result of chemotherapy.

CONTRAINDICATIONS: Hypersensitivity to interferon alfa-2b or to other components of the drug during pregnancy (threatened miscarriage).

SIDE EFFECTS: Injecting Alfarekina in most cases accompanied by flu-like syndrome: fever, chills, headache and muscle pain, joint pain, general weakness. These side effects are dose-dependent, and usually occur only in the first days of treatment, then decrease and disappear. To treat or a significant reduction of symptoms used paracetamol 0,5-1 g for 30-40 min before injection.
Sometimes when long courses of treatment indicated leukopenia, thrombocytopenia, passing with a decrease in dose.

STORAGE: at 2-8 ° S.
Prepared pp preparation for injection used immediately; rr for intranasal administration can be stored for 1 day at 2-8 ° C (refrigerated).

VIAGRA

Pharmacological properties: oral chemotherapy in treating patients with erectile dysfunction, a selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE 5).

Sildenafil has no direct relaxing effect on isolated cavernous body, but significantly increases the relaxing effect of nitrous oxide (NO) by inhibition of the PDE 5, is responsible for the splitting of cGMP in the cavernous bodies. When you activate the pathway NO / cGMP, which occurs with sexual stimulation, inhibition of PDE 5 sildenafil increases the concentration of cGMP in the cavernous bodies. Therefore, for the manifestation of pharmacotherapeutic effect of sildenafil should be sexual stimulation.

In vitro found that sildenafil has a selectivity for PDE 5. His influence on the PDE 5 more pronounced than on other known phosphodiesterases (10 times stronger than for PDE 6, 80 times - compared to the PDE 1, 700 times - with PDE 2, 4, 7-11, 400 times - with PDE W, which is involved in the processes of regulation of heart rate).

In healthy volunteers in single dose of sildenafil 100 mg have been no reported clinically significant ECG changes. The use of sildenafil resulted in a slight or moderate blood pressure decrease, which usually does not affect the therapeutic effect. The mean maximum decrease in systolic blood pressure in the supine position after ingestion of 100 mg was 8.4 mmHg. Art. The corresponding change in diastolic blood pressure in the supine position was 5.5 mm Hg. Art. BP decrease is due to vasodilating action of sildenafil, which may be due to increased concentration of cGMP in smooth muscles of blood vessels. More pronounced decrease in blood pressure was noted in patients who are simultaneously taking nitrates.

Sildenafil is rapidly absorbed from the digestive tract. The maximum plasma concentration achieved after 30-120 min (mean 60 min) after oral administration on an empty stomach. Absolute oral bioavailability of 40% (within 25-63%). If the drug is taken with fatty foods, the rate of absorption is reduced and the time to reach maximum plasma concentrations increased by an average of 60 minutes, and the maximum plasma concentration is reduced by an average of 29%. Sildenafil inhibits PDE 5 in vitro by 50% at concentration of 3 5 nM. The average concentration in blood plasma after administration of sildenafil 100 mg is about 18 ng / ml or 38 nM.

The average volume of distribution of sildenafil in the equilibrium state is equal to 105 liters, indicating that its distribution in tissues. How to sildenafil and its main circulating in the blood of N-dismetilovy metabolite, by approximately 96% bound to plasma proteins of blood. Protein binding does not depend on the concentration of the drug.

In healthy volunteers who received sildenafil (single dose 100 mg), 90 min after drug administration in the ejaculate was determined less than 0.0002% sildenafil (mean 188 ng) on the accepted dose.

Sildenafil is metabolized primarily liver isoenzymes localized in microsomes, CYP3A4 (major route) and CYP2C9 (minor route). The main circulating in the blood metabolite formed by N-dimetilirovaniya sildenafil. This metabolite is characterized by selective action on the PDE 5, but the degree of selectivity on the PDE 5 is approximately 50% of the selectivity of sildenafil. The concentration of this metabolite in blood plasma is approximately 40% of the concentration of sildenafil. N-dismetilovy metabolite is metabolized, and subsequently during its half-life of approximately 4 hours

The total clearance of sildenafil is 41 l / h, half-life - 3-5 pm Sildenafil is excreted as metabolites, mainly in the faeces (approximately 80% of the applied dose) and to a lesser extent - in the urine (approximately 13% of the applied dose).

In healthy elderly volunteers (65 years and older) are marked decline in the clearance of sildenafil, and the concentration of sildenafil and its metabolite N-dismetilovogo approximately 40% higher than in healthy young volunteers (18-45 years).

In volunteers with mild and moderate (creatinine clearance - 30-80 ml / min) renal insufficiency Pharmacokinetics of sildenafil after oral administration of a single dose of 50 mg did not change. Volunteers with severe (creatinine clearance ≤ 30 mL / min) renal insufficiency decreased clearance of sildenafil, which led to an increase in AUC (100%) and increased the maximum concentration in blood (88%) compared with volunteers of similar age without disabilities function kidneys.

In volunteers with mild to moderate liver cirrhosis expressed (functional class A and B on the classification of Child-Pugh) decreased clearance of sildenafil, which led to an increase in AUC (84%) and increased the maximum plasma concentrations (47%) compared to c those of the volunteers of similar age without hepatic failure. Pharmacokinetics of sildenafil in patients with severely impaired liver function were studied.

INDICATIONS: Treatment of patients with impaired erection, which is defined as the inability to attain and maintain an erection of the penis, necessary to the sexual act.

APPLICATION: to develop the effect of the drug must be sexual stimulation. The recommended dose for persons older than 18 years is 50 mg, taken orally approximately 1 hour before sexual intercourse. Given the efficacy and tolerability, the dose is increased to 100 mg or decrease to 25 mg. The maximum recommended dose is 100 mg, the maximum frequency of intake - 1 times per day. The effect of Viagra while eating develops later than when receiving an empty stomach.

Patients with mild renal insufficiency and moderate (creatinine clearance of 30-80 ml / min), dosage regimen adjustment is not required. Because patients with severe renal insufficiency (creatinine clearance <30>

CIALIS

Pharmacological properties: tadalafil (pirazinol [1 ', 2': 1,6] pyrido (3,4-b) indole-1 ,4-dione, 6 - (1,3-benzodioksol-5-yl) -2,3 , 6,7,12,12 a-hexahydro-2-methyl-, (6R, 12aR)) - Means, used for erectile dysfunction. Tadalafil is a reversible selective inhibitor of specific phosphodiesterase type 5 (PDE-5), cyclic guanosine monophosphate (cGMP). When sexual stimulation causes local release of nitric oxide, inhibition of PDE-5 tadalafilom leads to increased levels of cGMP in the cavernous body of penis. The result is relaxation of smooth muscles of arteries and blood flow to the tissues of the penis that causes an erection. Tadalafil has no effect without sexual stimulation.

In in vitro studies found that Tadalafil is a selective inhibitor of PDE-5. PDE-5 is an enzyme found in smooth muscles of cavernous bodies in the vascular smooth muscles of internal organs, skeletal muscle, platelets, kidney, lung and cerebellum. Effects of tadalafil for PDE-5 is more pronounced than on other types of phosphodiesterase. Tadalafil is 10 000 times more active against PDE-5 than for FDE1, FDE2 and FDE4, which are located in the heart, brain, blood vessels, liver and other organs. Tadalafil 10 000 times more active blocks PDE-5 than FDE3 - enzyme that is detected in the heart and blood vessels. This selectivity for PDE-5 compared with FDE3 is important, because FDE3 is an enzyme involved in the reduction of the heart muscle. In addition, tadalafil about 700 times more active against PDE-5 than for FDE6 found in the retina and is responsible for fotoperedachu. Tadalafil is also shown in 9,000 times more powerful effect on PDE-5 compared with its effect on FDE8, FDE9 and FDE10, as well as 14-fold compared with FDE11.

The drug acts within 36 hours The effect is manifested as little as 16 minutes after taking the drug in the presence of sexual stimulation.

Tadalafil in healthy individuals causes no significant change in systolic and diastolic blood pressure compared to placebo in supine position (mean maximum decrease of 1,6 / 0,8 mmHg. Cent.) And standing (mean maximum decrease of 0.2 / 4.6 mmHg. cent.). Tadalafil does not cause significant change in heart rate.

Tadalafil does not affect the perception of colors (blue / green), due to its low affinity to FDE6 compared with PDE-5. In addition, there is no influence of tadalafil on visual acuity, electroretinogram, intraocular pressure and pupil size.

Investigation of the effect on spermatogenesis receiving tadalafil for 6 months revealed no clinically significant effect of the drug on the number, mobility and structure of sperm. Receiving tadalafil had no effect on testosterone levels, LH and FSH in the blood.

After oral tadalafil is rapidly absorbed. The average maximum plasma concentration achieved after an average of 2 hours after ingestion.

The speed and extent of absorption of tadalafil is not dependent on food intake, so the drug can be taken irrespective of food intake. Hours (morning or evening) has no significant effect on the rate and extent of absorption.

The average volume of distribution is about 63 liters. At therapeutic concentrations, 94% of tadalafil is associated with plasma proteins.

In healthy persons less than 0.0005% of the administered dose is found in semen.

Tadalafil is mainly metabolized with the participation of isoenzyme (CYP) 3A4 cytochrome P450. The main circulating metabolite is metilkateholglyukuronid. This metabolite of at least 13,000 times less active against PDE-5 than tadalafil. Therefore, one can hardly assume that this metabolite at such concentrations is clinically significant.

In healthy individuals the average half-life - 17,5 hours Tadalafil appears mainly in the form of inactive metabolites, mainly with feces (about 61% of the dose) and to a lesser extent in the urine (about 36% of the dose).

In healthy elderly (65 years and older) were found lower clearance tadalafil while taking the drug by mouth, which was reflected in increased AUC by 25% compared with that in healthy individuals aged 19 to 45 years. This distinction is not clinically significant and does not require dose adjustment.

In individuals with renal failure (including patients on hemodialysis), tadalafil exposure (on the value of AUC) was greater than in healthy individuals.

Exposure tadalafil (by value AUC) in patients with mild and moderate hepatic insufficiency comparable to that in healthy individuals. Data on pharmacokinetics tadalafil with severe hepatic insufficiency is not.

Patients with diabetes mellitus during treatment with tadalafil AUC value was approximately 19% lower than in healthy individuals. This difference in exposure does not require dose adjustment.

INDICATIONS: Erectile dysfunction.

APPLICATION: The recommended dose is 20 mg. Cialis are inside before the alleged sexual activity regardless of the meal. The drug should be taken at least 16 minutes before the anticipated sexual activity.

The effectiveness of tadalafil may persist for 36 hours after taking the drug. The maximum recommended frequency of admission - once a day.

CONTRAINDICATIONS: Hypersensitivity to tadalafilu or other components of the preparation, the simultaneous application of organic nitrates.

SIDE EFFECTS: The most frequently noted headache (≥ 10% of cases). Other typical side effects (frequency ≥ 1% but <10%) are back pain, dyspepsia, dizziness, flushing, myalgia, nasal congestion. With a frequency of ≥ 0,1%, but <1% of the observed swelling of eyelids, pain in the eyes, hyperemia of the conjunctiva.

In postmarketing studies rarely observed such side effects:

hypersensitivity reactions: skin rash, hives and swelling of the person syndrome Stevens - Johnson, exfoliative dermatitis;

of the cardiovascular system: describes cases of serious reactions to the cardiovascular system, such as myocardial infarction, sudden cardiac death, stroke, angina, tachycardia, however, most patients had a history of guidance on the risk factors of the cardiovascular system . It is impossible to establish statistically significant association of these leaching reactions with cardiac risk factors, the reception tadalafil, sexual activity or with a combination of all these factors. It was also reported on the development of arterial hypotension (usually in the case of simultaneous reception of tadalafil with antihypertensive drugs), hypertension, collapse;

from the digestive system: abdominal pain, gastroesophageal reflux;

of the skin: hyperhidrosis;

from the organ of vision: blurring of vision, nearterialnaya anterior ischemic optic neuropathy, retinal vein occlusion, visual disturbances;

of the genitourinary system: a long erection priapism.

Cautions: sexual activity represents a potential risk for patients with diseases of the cardiovascular system. Therefore, treatment of erectile dysfunction, including the use of Cialis, you should not hold for men with heart disease, in which sexual activity is not recommended.

Keep in mind the potential risk of complications during sexual activity in patients with cardiovascular diseases such as myocardial infarction within the last 90 days, unstable angina or angina occurring during sexual intercourse, heart failure functional class II and higher NYHA, which developed in During the past 6 months, uncontrolled arrhythmias, hypotension (BP <90/50 mmHg. cent.) or hypertension, stroke, transferred within the last 6 months.

Safety and efficacy of a combination of Cialis with other treatments for erectile dysfunction have not been studied, so the use of such combinations is not recommended.

There are reports of occurrence of priapism when using PDE-5 inhibitors, including tadalafil. Patients should be alert for immediate access to medical care in case of erection continuing for 4 h or more. Delayed treatment leads to priapism damage the tissues of the penis with the onset of long-term impotence. Cialis should be used with caution in patients with predisposition to priapism (eg sickle cell anemia, multiple myeloma, or leukemia) or in patients with deformity of the penis (eg, angulation, cavernous fibrosis or Peyronie's disease).

Given the lack of data on the use of Cialis in patients with severely impaired liver function (class C according to Child-Pugh), patients of this group appoint Cialis with caution.

Like other inhibitors of PDE 5, tadalafil is able to provide a systemic vasodilator action, which can lead to a transient decrease in BP. Therefore, before the appointment Sialis physician should evaluate the likelihood of such an effect in patients with cardio-vascular system.

Cialis is not indicated for use in women.

Cialis does not affect or have little effect on the ability to drive vehicles and operate machinery.

INTERACTION: Cialis has no clinically significant effect on clearance of drugs, the metabolism of which proceeds with the participation of isoenzyme cytochrome P450. The study confirmed that tadalafil does not inhibit or induce CYP isoenzymes 3A4, CYP 1A2, CYP 2D6, CYP 2E1 and CYP 2C9.

Tadalafil is mainly metabolized with the participation of the enzyme CYP 3A4. The selective inhibitor of CYP 3A4 ketoconazole when receiving a dose of 400 mg / day increases the AUC tadalafil after a single administration of 312%, increases the maximum concentration in blood plasma by 107% and 200 mg / day - at 107 and 15% respectively.

Ritonavir (an inhibitor of CYP3A4, 2C9, 2S19, and 2D6) in a dose of 200 mg 2 times a day increases the AUC after a single dose of tadalafil in 124%, without changing the maximum concentration in the blood.

Although specific interactions have not been studied, it is likely that protease inhibitors such as saquinavir, as well as inhibitors of CYP 3A4 such as erythromycin and intrakonazol, raise the level of tadalafil in plasma.

Selective CYP3A4 inducer rifampicin 600 mg / day reduces the AUC after a single receiving tadalafil, 88%, and its maximum concentration in blood plasma increased by 46%. One can expect that the simultaneous use of other CYP3A4 inducers will also help to reduce the concentration of tadalafil in the blood plasma.

Tadalafil has no clinically significant effect on the pharmacokinetics of S-warfarin or R-warfarin and does not alter the effect of warfarin on prothrombin time.

Tadalafil does not increase the duration of bleeding in the intake of acetylsalicylic acid.

Tadalafil has a systemic vasodilating action, which may potentiate the hypotensive effect of antihypertensive drugs. In patients receiving multiple antihypertensive drugs may be a significant reduction in blood pressure. In most patients blood pressure reduction is not accompanied by symptoms of hypotension.

There were no significant BP reduction in patients taking both tadalafil and selective blocker of a 1-adrenoceptor tamsulosin.

In appointing tadalafil healthy volunteers who took a 1-blocker doxazosin adrenoceptor in a dose of 8 mg / day, marked enhancement of the hypotensive action. Some patients reported dizziness.

Tadalafil did not affect the concentration of ethanol, and ethanol did not affect the concentration of tadalafil. During the course of high doses of ethanol (0.7 g / kg), simultaneous reception of tadalafil did not cause a statistically significant decrease in blood pressure. Observed in some patients postural dizziness and orthostatic hypotension. Receiving tadalafil on the background of lower doses of ethanol (0.6 g / kg) did not cause the development of arterial hypotension, and dizziness was observed with the same frequency as the reception of only one alcohol.

Simultaneous reception of antacids (magnesium hydroxide / aluminum hydroxide) reduces the rate of absorption of tadalafil without altering AUC.

Raising the pH in the stomach as a result of receiving H 2-blocker receptor nizatidina had no effect on the pharmacokinetics of tadalafil.

OVERDOSE: If a single appointment healthy persons tadalafil at a dose of 500 mg and patients with erectile dysfunction - many times up to 100 mg / day - adverse effects were the same as in the appointment of lower doses. In case of overdose should be carried out standard symptomatic treatment.

Storage: Store in original container at temperatures below 30 ° C.

Tramadol+Paracetamol

Group Affiliation:
Analgesic (analgesic with a mixed mechanism of action of non-narcotic analgesic + vehicle)

Description of the active substance (INN):
Tramadol + Paracetamol

Dosage form:
coated tablets

Mode of action:
Combined analgesic containing tramadol and acetaminophen. Tramadol - has a central action and the action on the spinal cord (promotes opening of K + and Ca2 +-channels, causing hyperpolarization of the membrane and inhibits the conduct pain impulses), increases the effects of sedative drugs. Activates opioid receptors (mu, delta, kappa) on the pre-and postsynaptic membranes of nociceptive afferent fibers in the brain and GI tract, inhibits reverse neuronal capture of catecholamines in the CNS. Paracetamol - non-opioid analgesics, blocks COX mainly in the central nervous system, affecting pain centers and thermoregulation. Does not cause gastrointestinal irritation, no effect on water-salt metabolism, since no effect on the synthesis of Pg in the peripheral tissues. With paracetamol there is a rapid analgesia, whereas tramadol provides prolonged effect. Synergism analgesic effect of two active ingredients reduces the risk of side effects.

Indications:
Pain (moderate to severe intensity of various etiologies, including inflammatory, traumatic, vascular origin). Pain relief during painful diagnostic or therapeutic interventions.

Contraindications:
Hypersensitivity, acute alcohol intoxication or drugs depressing the central nervous system, hypnotics, narcotic analgesics and psychotropic drugs, simultaneous reception of MAO inhibitors (and within 2 weeks after withdrawal), severe hepatic and / or renal failure (CC <10 mL / min) uncontrolled epilepsy therapy, the syndrome of "cancellation" of narcotic drugs, children's age (14 years), pregnancy, laktatsii.C caution. Schoch, head injury, intracranial hypertension, susceptibility to convulsions (with controlled epilepsy drug may be used only emergencies), confusion of unknown etiology, respiratory failure, simultaneous reception of psychotropic and other analgesic drugs of the central action of local anesthetics, biliary tract disease, benign bilirubinemia, hepatitis, lack of glucose-6-phosphate dehydrogenase, alcoholic liver disease, alcoholism, drug addiction, symptoms of "acute" abdomen of unknown origin, advanced age (older than 75 years).

Side effects:
Allergic reactions: rash, itching, Quincke's edema, rash, bullous eruption. On the part of the nervous system: dizziness, headache, lethargy, paradoxical CNS stimulation (nervousness, agitation, anxiety, tremors, muscle spasms, euphoria, emotional lability, hallucinations), drowsiness, sleep disturbances, confusion, poor coordination of movements, spasms of central origin (while the appointment of antipsychotic drugs), depression, amnesia, violation of cognitive function, paresthesias, unsteadiness of gait. On the part of the digestive system: dry mouth, nausea, vomiting, flatulence , abdominal pain, constipation, diarrhea, difficulty swallowing, increased activity of "liver" enzymes, usually without the development of jaundice. On the part of the SSA: tachycardia, orthostatic hypotension, syncope, collapse. From the Endocrine: hypoglycemia, hypoglycemic coma until . mochevydelitelnoy the part of the system: difficulty urinating, dysuria, urinary retention. Chronic administration at doses considerably higher than recommended - Nephrotoxicity (interstitial nephritis, papillary necrosis). On the part of the senses: blurred vision, taste. The respiratory system: dyspnea. On the part of the skin: erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). From the side of hematopoiesis: sulfgemoglobinemiya. Chronic administration at doses considerably higher than recommended - aplastic anemia, pancytopenia, agranulocytosis. Other: Sweating, weakness, fatigue, menstrual disorders. When long-term use - the development of drug dependence (irritability, phobias, nervousness, sleep disturbances, psihotomotornaya activity tremor, discomfort in the stomach or intestine). In sharp end of reception may develop - syndrome "cancel." Overdose. Symptoms of overdose of tramadol: miosis, vomiting, collapse, coma, convulsions, depression of the respiratory center, sleep apnea. Symptoms of an overdose of paracetamol: (acute overdose develops within 6-14 h after administration of paracetamol, chronic - after 2-4 days in case of excess dose). Symptoms of acute overdose: diarrhea, loss of appetite. Symptoms of chronic overdose: cerebral edema, hypocoagulation, the development of DIC-syndrome, hypoglycemia, metabolic acidosis, arrhythmia, collapse; rare - abnormal liver function, which is developing at lightning speed and can be complicated by kidney failure (renal tubular necrosis). Treatment: gastric lavage and reception Enterosorbents (activated carbon, polyphepan), the maintenance functions of the SSA, to ensure the airway. When respiratory depression (symptom overdose tramadol) - naloxone, in convulsions - diazepam. Hemodialysis or hemofiltration during intoxication tramadol ineffective. If symptoms of overdosage of paracetamol: An Introduction donators of SH-groups and precursors of glutathione synthesis - through methionine 8-9 h after the overdose, and N-acetylcysteine have - after 12 pm The need for further introduction of methionine in / introduction N-acetylcysteine is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after the reception.

Dosage and administration:
Inside, regardless of the meal, swallow a whole (not crush or chew), washed down with liquid. Dosage regimen and duration of treatment are selected individually depending on the severity of pain. For adults and children over 14 years, the recommended initial single dose - 1-2 tablets with an interval between doses of the drug - at least 6 hours maximum daily dose - 8 tablets (300 mg tramadol and 2.6 g of paracetamol). In elderly patients (aged 75 years and older) can be used usual doses. However, with the possibility of a delayed launch, the interval between taking the drug may be increased. In patients with renal insufficiency (CC 10-30 ml / min) interval between doses must be at least 12 h. Since Tramadol very slowly excreted during hemodialysis or hemofiltration, the use of the drug after the dialysis session to maintain the analgesic effect is required. For a moderate abnormal liver function should be to increase the interval between doses of the drug.

Cautions:
Patients who are prone to abuse drugs or of drug addiction must be treated under close medical supervision in a short period. During drug treatment is recommended to avoid receiving ethanol. The risk of developing hepatotoxicity and overdose of paracetamol increases in patients with alcoholic hepatosis. During the long-term care necessary to monitor patterns of peripheral blood and liver functional state. At the time of treatment should refrain from driving motor vehicles and classes of potentially hazardous activities that require high concentration and quickness of psychomotor reactions.

Interaction:
The combined use of opioid agonist-antagonists (buprenorphine, nalbufinom, pentazocine), reduces the analgesic effect as a result of competing actions on the receptors, but also raises the risk of the syndrome of "cancel." Drugs, CNS depressants (including sleeping pills, tranquilizers), ethanol - increases the side effects characteristic of tramadol. Inductors microsomal oxidation (including carbamazepine, phenytoin, ethanol, barbiturates, rifampicin, fenilbutazon, tricyclic antidepressants) reduce the analgesic effect and its duration. naloxone activates respiration, eliminating the analgesia caused by taramadolom. Prolonged use of barbiturates reduce the effectiveness of paracetamol. Ethanol contributes to the development of acute pancreatitis. Prolonged joint use of paracetamol and other NSAIDs increases the risk of nephropathy and renal papillary necrosis, onset of end-stage renal failure. Simultaneous long-term assignment in high doses of paracetamol and salicylates increases the risk of kidney cancer or bladder. Diflunisal increases the plasma concentrations of paracetamol by 50% - the risk of hepatotoxicity. Concomitant use with drugs that reduce epileptic threshold (including selective inhibitors of reverse serotonin, tricyclic antidepressants, antipsychotics) - the risk of seizures. Drugs that inhibit CYP3A4 (ketoconazole and erythromycin) may slow the metabolism of tramadol (N-demethylation), and active O-demethylated metabolite. Quinidine increases the concentration in blood plasma tramadol and reduces the concentration of O demethylated metabolite due to competitive inhibition of isoenzyme CYP2D6. microsomal oxidation inhibitors (cimetidine) decrease the risk of hepatotoxicity. the rate of absorption of paracetamol is increased when taking metoclopramide or domperidone and decreases when receiving kolestiramina. preparation for admission to a long time increases the effect of indirect anticoagulants (warfarin, etc. coumarin), which increases the risk of bleeding.

Tramadol

Group Affiliation:
Analgetic opioid tool

Description of the active substance (INN):
Tramadol

Dosage form:
drops for oral administration, capsules, capsule-acting, injectable solution, a solution for oral, rectal suppositories, tablets, coated tablets, prolonged action tablets, tablets with prolonged action of

Mode of action:
Synthetic opioid analgesic with a central action and action on the spinal cord (promotes opening of K + and Ca2 +-channels, causing membrane hyperpolarization and inhibits the conduct pain impulses) increases the effects of sedative drugs. Activates opioid receptors (mu, delta, kappa) on the pre-and post-synaptic membranes of afferent nociceptive fibers of the brain and gastrointestinal tract. Slows destruction of catecholamines stabilize their concentrations in the CNS. It is a racemic mixture of two enantiomers - dextrorotatory (+) and levogyrate (-), each of which displays different from the other receptor affinity. (+) Tramadol is a selective agonist of mu-type opioid receptors and selectively inhibits the reverse neuronal serotonin. (-) Tramadol inhibits reverse neuronal capture noradrenaline. Mono-O-dezmetiltramadol (metabolite M1) also selectively stimulates the mu-opiate receptors. The affinity of tramadol to the opioid receptors is 10 times weaker than codeine and 6000 times weaker than morphine. Severity of analgesic effect is 5-10 times weaker than morphine. The analgesic effect is due to decreased activity of nociceptive and antinociceptive systems of the body increases. In therapeutic doses does not affect in a meaningful way on hemodynamics and respiration does not alter the pressure in the pulmonary artery, slightly slowing peristalsis, without causing This constipation. Has some antitussive and sedative effect. Inhibits the respiratory center, excites the launcher zone of the vomiting center, the nucleus of the oculomotor nerve. Prolonged use may develop tolerance. Analgesic effect develops within 15-30 minutes after ingestion and lasts till 6 pm

Indications:
Pain (strong and medium intensity, including inflammation, trauma, vascular disease). Analgesia during painful diagnostic or therapeutic interventions.

Contraindications:
Hypersensitivity, state, accompanied by respiratory depression or marked depression of the central nervous system (alcohol poisoning, sleeping drugs, narcotic analgesics and other psychoactive drugs), pregnancy, lactation period (in case of prolonged use), children's age (under 1 year - for parenteral administration; to 14 - Oral), receiving MAO inhibitors, severe hepatic and / or renal failure (CC <10 ml / min). C care. Drug addiction, mental confusion, intracranial hypertension TBI, epileptic syndrome (cerebral dysfunction), patients on a background of pain in the abdominal cavity of unknown origin.

Side effects:
On the part of the nervous system: increased sweating, dizziness, headache, weakness, fatigue, lethargy, paradoxical CNS stimulation (nervousness, agitation, anxiety, tremors, muscle spasms, euphoria, emotional lability, hallucinations), sleepiness, sleep disturbance, confusion , violation of motor coordination, seizures of central origin (with a / in the introduction of high-dose or while the appointment of antipsychotic drugs (neuroleptics), depression, amnesia, violation of cognitive function, paresthesias, unsteady gait. On the part of the digestive system: Dry mouth, nausea , vomiting, flatulence, abdominal pain, constipation or diarrhea, difficulty in swallowing. On the part of the SSA: manifestations of vasodilation - tachycardia, orthostatic hypotension, syncope, collapse. Allergic reactions: rash, itching, rash, bullous eruption. On the part of the urinary system: difficulty in urination, dysuria, urinary retention. On the part of the senses: blurred vision, taste. the respiratory system: dyspnea. Other: menstrual irregularities. With prolonged use - drug addiction. With a sharp lifting - syndrome "cancel." Overdose. Symptoms : miosis, vomiting, collapse, coma, convulsions, depression of the respiratory center, sleep apnea. Treatment: the provision of airway, breathing and maintenance of the SSA. opiate effects may be cropped naloxone, cramps - benzodiazepines.

Dosage and administration:
B / B, / m, n / a, mouth, rectum. Inside: For single use only in adults and children over 14 years - to 0.05 grams (tablets, capsules) with a small amount of liquid or 20 cap solution (or drops) for admission inside with a small number of liquid or on sugar. After 30-60 minutes you can repeat the method with the same dose, but no more than 8 doses per day. Retard Tablets - 100-200 mg every 12 hours daily dose - 0.4 grams (in exceptional cases, such as cancer patients, possibly reducing the interval Up to 6 h and an increase in daily dose). Rectal - 0.1, the multiplicity of reception - up to 4 times per day. / in slowly, s / c or i / m: 0.05-0.1 g. If the effect is insufficient, 20-30 minutes after i / v administration can continue infusion at 12 mg / h or additionally appoint inside. The total daily dose - 0.4, the kids over the age of 1 year - inside, only a drop or parenteral (IV, V / m, n / k), a dose of 1-2 mg / kg. Daily dose - 4-8 mg / kg (1 cap - 2.5 mg). Elderly and patients with renal insufficiency require individual dosage (possibly lengthening T1 / 2). When spacecraft less than 30 ml / min and in patients with liver failure required 12 h interval between doses of regular doses of the drug.

Cautions:
Do not use for the treatment of the syndrome of "cancellation" of drugs. It should not be used simultaneously to ethanol. In the case of single dose is not necessary to interrupt breast-feeding. In the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and the rapidity psychomotor reactions.

Interaction:
Pharmaceutical incompatible with solutions of diclofenac, indomethacin, fenilbutazona, diazepam, flunitrazepam, nitroglycerin. Enhances the action of drugs which depress the central nervous system, and ethanol. Inductors microsomal oxidation (including carbamazepine, barbiturates) reduce the severity of analgesic effect and duration of action. Prolonged use of opioid analgesics, or barbiturates stimulate the development of cross-tolerance. generalized anxiety increases the expression of analgesic effect, duration of anesthesia increases in combination with barbiturates. naloxone activates respiration, analgesia after eliminating the use of opioid analgesics. MAO inhibitors, furazolidone, procarbazine, antipsychotic drugs (neuroleptics) increase the risk of convulsions ( decrease the convulsive threshold). Quinidine increases the plasma concentration of tramadol and metabolite M1 reduces the expense of competitive inhibition of isoenzyme CYP2D6.

Paclitaxel

International name:
Paclitaxel (Paclitaxel)

Group Affiliation:
Antitumor agents, alkaloid

Description of the active substance (INN):
Paclitaxel

Dosage form:
Concentrate for solution for infusion

Mode of action:
Antitumor agents of plant origin. Does the process of cell division, changes the process of formation and stabilization of the mitotic spindle microtubules and prevents depolymerization. As a result, suppressed the dynamic reorganization mikrotubulyarnoy network in the interphase of mitosis, causes the appearance of abnormal bundles of microtubules throughout the cell cycle and multiple condensations of star (Astaire) during mitosis.

Indications:
Ovarian cancer (first-line treatment of patients with common form of the disease or residual tumor (more than 1 cm) after laparotomy (in combination with cisplatin) and second-line therapy for metastases after conventional therapy, which gave no positive result.) Breast cancer (presence of affected lymph nodes after standard combination therapy (adjuvant therapy) after disease recurrence within 6 months after the start of adjuvant therapy - first-line therapy, metastatic breast cancer after standard therapy is ineffective - for second-line therapy). non small cell lung lung cancer (first-line treatment of patients which is not planned for surgical treatment and / or radiation therapy (in combination with cisplatin). Kaposi's sarcoma in AIDS patients: secondary treatment. Squamous cell carcinoma of the head and neck; transitorial bladder cancer, esophagus cancer, leukemia (lymphocytic, nelimfotsitarnaya).

Contraindications:
Hypersensitivity (including to polioksolu castor oil), neutropenia (less than 1.5 thousand / ml), thrombocytopenia (less than 100 thousand / ml), pregnancy, lactation, liver failure, infectious diseases (including herpes shingles, chickenpox, herpes), arrhythmias, myocardial infarction (history), myocardial ischemia, inhibition of bone marrow hematopoiesis after chemotherapy or radiotherapy.

Side effects:
From the side of hematopoiesis and hemostasis system: inhibition of bone marrow hematopoiesis (neutropenia, thrombocytopenia, anemia). The nervous system: ataxia, seizures, encephalopathy, peripheral neuropathy, paresthesia. On the part of the SSA: lowering blood pressure, rarely - increased BP, bradycardia, and or tachycardia, AV block, ventricular bigeminy, mesenteric thrombosis. On the part of the digestive system: nausea, vomiting, diarrhea, decreased appetite, constipation, obstruction and intestinal perforation, ischemic colitis. On the part of the skin and subcutaneous fat: peripheral edema , alopecia (reversible), not heavy defeat of the skin and nails. From a musculoskeletal: arthralgia, myalgia. On the part of the sense organs: reduced visual acuity. Allergic reactions: skin rash, "tides" of blood to the skin of the face and upper chest cells, angioedema, bronchospasm, generalized urticaria. Other: reduced tolerance to infections (any etiology). Laboratory indicators: increase in activity of "liver" transaminases and alkaline phosphatase, hyperbilirubinemia. Local reaction: flushing, tromboflebit.Peredozirovka. Symptoms: aplasia of the bone marrow, peripheral neuropathy, mucositis. Treatment: symptomatic.

Dosage and administration:
V / a drip for 3 hours 1 time in 3 weeks. Solution before injection diluted to a concentration of 0.3-1.2 mg / ml 0.9% NaCl solution or 5% dextrose. When ovarian cancer - 135-175 mg / sq.m. When breast cancer, non small cell lung lung cancer - 175 mg / m (subject to prolonged infusion of up to 24 h at a dose of 135 mg / m² every 3 weeks). In KS - 135 mg / m or 100 mg / sqm for 3 h, 1 every 2 weeks. Repeated course should be conducted when the number of neutrophils in peripheral blood of more than 1.5 thousand / microliter and platelets - more than 100 thousand / ml. Patients with profound neutropenia (less than 500 cells / mm) or significant peripheral neuropathy, which was developed during the treatment, with repeated treatments should be reduce the dose by 20%. To prevent the development of pronounced allergic reactions in all patients before the introduction of - 20 mg dexamethasone by mouth or IM - for 6-12 h, 50 mg diphenhydramine in / in and 300 mg of cimetidine / v - 30 - 60 min.

Cautions:
During treatment, you should regularly monitor the pattern of peripheral blood, blood pressure, heart rate and the number of breaths (especially during the first hour of infusion), ECG monitoring (and before treatment). In cases of violations of AV conduction after repeated administration is necessary to conduct continuous cardiac monitoring. Has embryo-and fetotoxicity. During treatment, you must use a reliable contraceptive measures. Paclitaxel should be administered under the supervision of a physician hospital or clinic that has experience with anticancer drugs, and if the conditions necessary for coping with complications. In order to introduce is not recommended infusion of polyvinyl chloride. Solutions should be prepared and stored in glass, polypropylene or polyolefin systems and enter through the infusion system with the inner surface of polyethylene, and connects to the system through a membrane filter with pore size of less than 0.22 microns. During the period of treatment must be careful when driving and lesson other potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Interaction:
Cisplatin decreases the total clearance of paclitaxel by 20% (with more pronounced myelosuppression observed when paclitaxel is introduced after cisplatin). Inhibitors of microsomal oxidation (including ketoconazole, cimetidine, verapamil, diazepam, quinidine, cyclosporine, etc.) inhibit metabolism of paclitaxel.

Abciximab

International name:
Abtsiksimab (Abciximab)

Group Affiliation:
Antiplatelet tool

Description of the active substance (INN):
Abtsiksimab

Dosage form:
intravenous

Mode of action:
Antiplatelet tool, is also fibrinolytic action. Connect to glycoprotein receptors (GP IIb / IIIa) platelet, inhibits their aggregation and subsequent formation of thrombus. It prevents the binding of fibrinogen, von Willebrand factor with receptor sites on activated platelets. Calling the conformational changes of receptors, reduces access to large molecules. Platelet function recovers within 48 h; in / bolus 0.15-0.3 mg / kg dose-dependent manner inhibits platelet function and increase bleeding time. After 2 h after a dose of 0.25-0.3 mg / kg blocks more than 80% receptor GP IIb / IIIa, with the bleeding time increased to 30 min. V / a bolus 0.25-0.3 mg / kg followed by continuous in / infusion at 10 micrograms / min for 12-96 h is stable blockade expressed GP IIb / IIIa receptors and inhibition of platelet function throughout the infusion. After graduating in / infusion partial blockade of GP IIb / IIIa retained for 10 days.

Indications:
Prevention of myocardial ischemia in patients with high-risk groups, which planned percutaneous coronary balloon angioplasty, stent implantation or atherectomy (consisting of combined therapy on the background of heparin and ASA). The state of the coronary arteries after angioplasty or atherectomy to prevent acute cardiac ischemic complications in patients with high risk of reocclusion of the operated vessel (the presence of intracoronary thrombus, extent of damage> 20 mm). A tendency to thrombosis, including acute myocardial infarction with Q Wave for 12 hours after it began, postinfarction angina. Unstable angina (patients with no effect on conventional therapy), if coronary angioplasty is planned within the next 24 hours

Contraindications:
Hypersensitivity; aneurysm of large vessels, malformations of the arteries, veins, internal bleeding, recent (within 6 weeks), clinically significant bleeding in the gastrointestinal tract or urinary system; ischemic attacks (in the history of the past 2 years), the residual effects of the cerebral circulation with neurological deficit, bleeding diathesis, hypertension (hypertensive crises within), intracranial neoplasm, extensive surgery or trauma (including recent - up to 6 weeks), thrombocytopenia (less than 100 thousand / ml), vasculitis, lactation, children vozrast.C caution. Diseases of the digestive tract (in history), receiving oral anticoagulants within the past 7 days with a decrease in prothrombin time 1.2 times more compared to baseline; in / dextran before the introduction of coronary angioplasty, pregnancy, body weight less than 75 kg, age over 65 years, percutaneous coronary intervention (not A successful, lasting more than 70 minutes, within 12 hours after the development of acute myocardial infarction).

Side effects:
From the side of hematopoiesis and hemostasis system: bleeding (in place of arterial access in the groin, gastrointestinal tract, urinary tract, retroperitoneal, intracranial), thrombocytopenia, anemia, leukopenia, petechiae. On the part of the SSA: lowering blood pressure, bradycardia, pulmonary edema, AV block III Art., supraventricular tachycardia, ventricular tachycardia, "intermittent" claudication, pericardial effusion, peripheral vascular thromboembolism, pulmonary embolism. On the part of the digestive system: nausea, vomiting, constipation, or diarrhea paralytic ileus. the nervous system: confusion, dizziness, insomnia, cerebral ischemia, hyperesthesia. On the part of the urinary system: kidney failure (worsening or development), urinary retention. Allergic reactions: itching, anaphylactic shock. Other: myopathy, myalgia, phlegmon, dysphonia, impairment, pleural effusion, pneumonia, leykotsitoz.Peredozirovka. Symptoms: profuse bleeding, vascular collapse, and thrombocytopenia. Treatment: removal of the drug, platelet transfusion.

Dosage and administration:
V / a bolus, 0.25 mg / kg for 10-60 min before coronary angioplasty (the duration of bolus injections - not less than 1 min) followed by continuous i / v infusion at 10 micrograms / min for 12 h (with a pump for continuous infusion with a built in sterile, apyrogenic weakly binding proteins by a filter with pores of 0.2 or 0.22 microns). Unstable angina in a similar bolus dose (followed by infusion for 12 h) starting 24 hours before planned angioplasty. The rules of preparation and administration solution for injection: for the introduction of a bolus recruit the required number abtsiksimaba (2 mg / ml) into a syringe through a sterile, pyrogen-free, low protein binding filter with pores of 0.2 or 0.22 microns for the preparation of infusion solution required for continuous infusion of abtsiksimaba injected into a sterile 0.9% NaCl solution or 5% dextrose. The prepared infusion solution can store up to 12 h at 2-8 grad.S. At the end of 12 h infusion of the unused portion of the solution destroyed.

Cautions:
Must be used only by doctors with sufficient diagnostic and therapeutic possibilities, and only in patients with high risk of acute coronary. Abtsiksimab should enter through a separate infusion system. During pregnancy and lactation are used only if the intended benefits to the mother outweigh the risks to the fetus and child. The risk of bleeding increased in patients weighing less than 75 kg, in patients older than 65 years, coronary angioplasty, which was conducted during 12 weeks after the onset of symptoms of acute myocardial infarction, coronary angioplasty during long (over 70 min), an unsuccessful coronary angioplasty. Before the introduction of the drug should be the definition of platelets, prothrombin time, APTT. Determination of Hb and hematocrit, and ECG done before the introduction, after 12 h and 24 h after a bolus injection. Blood pressure and heart rate monitor every hour during the first 4 h after bolus injection and then at 6, 12, 18, 24 h after it. In case of serious bleeding, which did not stop clamping, injection should be discontinued. Increases the likelihood of bleeding at the site of arterial access sheath femoral artery. For vascular access punktired only the front wall of an artery or vein. Using the method of cross-cutting approaches to determine the vascular structure is not recommended. Should be avoided without the need to puncture the arteries, veins, i / m injections, urinary catheterization, nazotrahealnoy intubation, the introduction of nasogastric tube, overlap cuff for automatic blood pressure measurement. Upon receipt of venous access should be avoided incompressible sites (subclavian or jugular vein). Vascular puncture site should be recorded and kept under observation. When removing the bandages to be especially cautious. In order to prevent spontaneous bleeding from the gastrointestinal tract - the appointment of H2-blockers, histamine receptors or liquid antacids, vomiting - antiemetic drugs.

Interaction:
Anticoagulants, thrombolytics, antiplatelet drugs (ASA, ticlopidine, dipyridamole, low molecular weight dextran) increases the risk of bleeding. The introduction of other monoclonal antibodies increases the risk of allergic reactions.

Vaccine hepatitis A

International name:
The vaccine for the prevention of hepatitis A (Vaccine hepatitis A)

Group Affiliation:
MIBP vaccine

Description for commercial items:
AWACS

Mode of action:
Inactivated vaccine for the prevention of viral hepatitis A, containing the hepatitis A virus, inactivated with formaldehyde.

Indications:
Viral hepatitis A (prevention) in adults and children older than 2 years, especially among risk groups: Unvaccinated persons traveling to endemic regions (with a high incidence of hepatitis A), persons exposed to occupational risk of infection (doctors, nursing staff for patients, including care for adults and children, moved to a wheelchair, the staff of sewer and water services, food industry workers and catering), hemophiliacs, patients with multiple blood transfusions, drug addicts who use drugs / c, homosexuals.

Contraindications:
Hypersensitivity (to any component of the vaccine), allergic reactions to previous vaccinations, hyperthermia or acute (or exacerbation of chronic) disease (vaccination is desirable to defer to the normalization condition), pregnancy, laktatsii.C caution. Liver disease, hypersensitivity to neomycin (each dose of vaccine contains trace amounts of neomycin).

Side effects:
Local: pain and hyperemia at the injection site, it is very rare - the seal in the injection site. Common: mild hyperthermia, fatigue, headache, myalgia, arthralgia, and impaired function of the gastrointestinal tract, is rarely - a small reversible increase in activity of "liver" transaminases.

Dosage and administration:
V / m (in the deltoid muscle). Primary vaccination - single 0.5 ml of vaccine. Revaccination - single 0.5 ml after 6-18 months. Subsequent revaccination is recommended that every 10 years.

Cautions:
In / in the introduction is not allowed. When you enter you must make sure that the needle does not penetrate into the blood vessel. To reduce the likelihood of local reactions to the vaccine should enter / m in the deltoid muscle (shoulder muscle). The vaccine should not be used in the gluteal muscles (due to variability in the thickness of the fat layer) or w / c, since in these cases may decrease the immune response. In special cases - patients suffering from thrombocytopenia or bleeding - the vaccine can be administered n / c. The study of this drug during lactation and the effect on embryo or fetus was carried out. However, as for any other inactivated viral vaccines, it seems unlikely that the ability of this drug have side effects on the embryo or fetus. A decision on vaccination of pregnant or lactating women should only be taken on the basis of assessment of real risk of contamination of hepatitis A. Immunosuppressive therapy or immunodeficiency condition can cause a weak immune response to the vaccine. Vaccination is carried out in an incubation period of hepatitis A, may be ineffective. Vaccination with this drug does not prevent viral hepatitis other etiologies, as well as infections caused by other known hepatotropic microorganisms.

Interaction:
The vaccine can be administered simultaneously with Ig under the condition of different parts of the body to inject the vaccine and Ig. Because the vaccine is inactivated, its combination with other inactivated vaccines does not affect the effectiveness of vaccination, provided the introduction of vaccines in different parts of the body (in particular, with recombinant vaccine to prevent hepatitis B, typhoid vaccine, live vaccine for the prevention of yellow fever). The vaccine can be used for revaccination, and in cases where the previous vaccination is carried out other inactivated vaccines for the prevention of hepatitis A.

AVAMIS

Pharmacological properties: Pharmacodynamics. Flyutikazona furoate - a synthetic fluorinated corticosteroid with a very high affinity for glucocorticoid receptors and a strong anti-inflammatory action.
Pharmacokinetics. Flyutikazona furoate undergoes extensive first pass metabolism and incomplete absorption in the liver and intestines, resulting in very little systemic effects of the drug. Typically, intranasal application of 110 mg 1 time per day achieved this concentration of the drug in plasma, which can not be measured (≤ 10 pg / ml). Absolute bioavailability flyutikazona furoate applying 880 mg 3 times daily (total daily dose - 2640 mg) is 0,5%.
Level flyutikazona furoate binding to proteins in blood plasma of 99%. The drug is widely distributed, volume of distribution is approximately 608 liters.
Flyutikazona furoate is rapidly excreted (total plasmatic clearance - 58 l / h) from the systemic circulation, mainly through hepatic metabolism involving CYP 3A4 enzyme cytochrome P450 to the inactive carboxyl metabolite (GW694301X). The primary mechanism of metabolism is the hydrolysis of S-flyuorometilkarbotionata to metabolite 17β-carboxylic acid. Is derived after oral and / in use, mainly in the faeces with signs of excretion flyutikazona furoate and its metabolites with bile. After i / v use half-life - 15,1 hours Excretion in the urine is approximately 1 and 2% after oral and / in the application accordingly.

INDICATIONS: Allergic rhinitis (as a symptomatic therapy).

APPLICATION: Avamis intranasal use only.
Adults and children over the age of 12 years: The recommended starting dose - 2 injection (27.5 micrograms per 1 injection) in each nasal passage 1 time per day (total daily dose - 110 micrograms).
After achieving control of symptoms of rhinitis maintenance dose can be reduced to 1 injection into each nasal passage 1 time per day (total daily dose - 55 micrograms).
Children aged 6-11 years: The recommended starting dose - 1 injection each nasal passage 1 time per day (total daily dose - 55 micrograms). In case of inadequate control of symptoms of rhinitis when injected into each nasal passage 1 time per day (total daily dose - 55 mg) dose may be increased to 2 injections into each nasal passage 1 time per day (total daily dose - 110 micrograms). After achieving control of symptoms of rhinitis dose reduced to 1 injection into each nasal passage 1 time per day (total daily dose - 55 micrograms).
Elderly patients using the same dose as in adults.
In renal insufficiency, dosage adjustment is not needed.
Hepatic insufficiency of mild to moderate severity does not require dose adjustment. Data on severe liver failure there.
To achieve the full therapeutic effect of the drug should be used regularly, that should inform the patient. Onset of action occurs within 8 h after the first application, maximum therapeutic effect after a few days of starting treatment. Duration of treatment should be limited to the period of influence allergen.
Terms of Use nasal sprays
Nasal metered dose spray consists of a glass bottle, placed in a plastic housing with a protective cap, which closes the tip of the sprayer (a special device at the upper end of the spray). In the lower part of the body are small holes through which the visible presence of the drug in a glass vial. At one of the sides of the plastic casing is a large dosing button, when clicked, which is fed through spray atomizer.
Before the first application (and if the drug is not used within 1 month) should check the device:
Shake the closed bottle (without removing the protective cap);
remove the cap, pulling it up, lightly pressing his fingers on both sides;
strongly press the dispensing button (not less than 6 times) for the release of a sufficient number of spray into the air.
Before each application must clear nasal passages, a little shake and spray the following steps:
slightly tilt your head forward;
holding the spray upright and gently place the dispenser in one nasal passage;
send a spray nozzle in the opposite direction from the nose to the drug is uniformly distributed in the nasal cavity;
inhale nose and simultaneously press the dispensing button on a plastic housing for spraying a spray in the nasal cavity;
Avoid getting spray into the eyes, and if this happens, rinse eyes with water;
, remove the spray from the nose and exhale mouth.
For the introduction of spray in the other nasal passage procedure is repeated in the same sequence.
Always close the device after the application of a protective cap.
After each use of a spray nozzle and cap is wiped clean, dry cloth.

CONTRAINDICATIONS: Hypersensitivity to the drug's components.

SIDE EFFECTS: very often (≥ 1 / 10), often (≥ 1 / 100 and ≤ 1 / 10), rare (≥ 1 / 1000 ≤ 1 / 100), sometimes (≥ 1 / 10 000 and ≤ 1 / 1000 ), isolated cases (≤ 1 / 10 000).
On the part of the respiratory system: very often - nosebleeds, often - sores on the mucous membrane of the nose. Epistaxis were usually mild or moderate degree. In adults and adolescents nasal bleeding occurred more frequently with prolonged use (6 weeks) than in the application of up to 6 weeks. In the pediatric clinical trials of up to 12 weeks, cases of nasal bleeding were similar in the group, which applied flyutikazona furoate and placebo.
On the part of the immune system: sometimes - hypersensitivity reactions, including anaphylaxis, angioedema, rash, and urticaria.

Cautions: flyutikazona furoate undergoes extensive first pass metabolism in the liver, so systemic effects intranasal flyutikazona furoate with severe liver disease may increase, which in turn may increase the risk of systemic side effects. Therefore, use in patients with severe hepatic insufficiency should be cautious.
Do not recommend the use of the drug combined with ritonavir due to the increased risk of systemic effects flyutikazona furoate.
Exceeding the recommended dose of intranasal GCS can cause clinically significant adrenal suppression. In times of stress or elective surgical intervention need to take into account the additional use of systemic GCS in the presence of signs of exceeding the recommended dose of GCS. Application of 110 mg / day flyutikazona furoate is not associated with the suppression of the hypothalamic-pituitary-adrenal system in adults and children. However, the dose intranasal flyutikazona furoate reduced to the minimum effective. As with the application of other intranasal GCS in the case of concomitant use of any other types of corticosteroid therapy take into account their overall systemic impact.
When treating children intranasal GCS in recommended doses, there were instances of stunted growth. Therefore, we recommend regularly measuring the growth of children with long-term therapy intranasal GCS. If you delay your child grows, treatment should be reviewed to reduce the dose, if possible - to the minimum effective.
In the case of signs of adrenal suppression function to transfer a patient with systemic use of steroids on the intranasal application flyutikazona furoate should be cautious.
Avamis contains benzalkonium chloride, which can cause irritation of the nasal mucosa.
During pregnancy and lactation. Flyutikazona furoate is used in this period, if the expected benefit to the mother exceeds potential risk to the fetus / child.
For children aged under 6 years old to apply Avamis not recommended, since the experience of the drug in pediatric practice is not enough.
Ability to influence the reaction rate on driving or using machinery is unlikely.

INTERACTION: flyutikazona furoate is rapidly excreted by the extensive first pass metabolism in the liver by cytochrome P450 3A4.
According to the results of other SCS - flyutikazona propionate, which is also metabolized by CYP 3A4, is not recommended the combined use with ritonavir due to increased systemic impact flyutikazona furoate.
Apply flyutikazona furoate in combination with strong CYP 3A4 inhibitors should be cautious due to the increasing influence of systemic flyutikazona furoate. In a clinical study drug interaction flyutikazona furoate with strong CYP 3A4 inhibitor ketoconazole number of persons whose concentration flyutikazona furoate in plasma can be measured, it was greater in the group using ketoconazole (6 to 20) compared with placebo (1 to 20). This is a slight strengthening of systemic effects caused no statistically significant difference in 24-hour levels of cortisol in the blood plasma in these 2 groups.
Data for the study of enzyme induction and inhibition suggest that there is no reason to expect the metabolic interaction between flyutikazona furoate and other neurotransmitters metabolism of cytochrome P450 in the relevant intranasal dosages for clinical application. Therefore, clinical studies on the interaction flyutikazona furoate and other drugs was not performed.

OVERDOSE: According to clinical studies with intranasal application of up to 2,640 micrograms of the drug per day for 3 days, side effects were observed. In applying the drug in high doses necessary to monitor the condition of the patient. In case of overdose Treatment is symptomatic.

Storage conditions: at temperatures below 30 ° C. Do not store in the refrigerator. Do not freeze. Before use, stir.

Abies sibirici extract

Trade name:
ALIS

International name:
Fir extract (Abies sibirici extract)

Group Affiliation:
Antiphlogistic

Description for commercial items:
ALIS

Dosage form:
solution for local and external use [oil]

Mode of action:
It has wound-healing, anti-inflammatory and bactericidal action. When applied topically does not irritate action.

Indications:
In Surgery: pyo-inflammatory diseases of skin and soft tissue (wounds, burns, frostbite, ulcers, pressure sores, abscesses, cellulitis, including maxillo-facial region). In dentistry: stomatitis, periodontal disease, complications of prosthetic teeth. In Otorhinolaryngology: pyo-inflammatory diseases of the ear, throat, nose and paranasal sinuses. In dermatology: bullosa necrotic forms of erysipelas, pyoderma.

Contraindications:
Hypersensitivity.

Side effects:
Burn, allergic reactions.

Dosage and administration:
Local. Prior to the surgical treatment of the wound surface and then applied 1-2 times a day uniform thin layer. Duration of treatment depends on the severity of the disease (usually 5-10 days) and ends with the appearance of fresh granulation, islands of epithelium or complete epithelialization. In inflammatory processes in the maxillofacial region (after the autopsy and surgical treatment of abscesses and phlegmon) in his pockets and postoperative wound introduce tampons soaked in a solution of ALIS. The procedure is repeated daily for 5-7 days. When external otitis instilled into the ear canal for 2-3 cap 3-4 times daily or enter tampons. When treating rhinitis instilled in each nasal passage 1-2 cap 3-4 times a day. If sinusitis is introduced into the sinus after their preliminary remediation.

Cautions:
Do not combine with other external drugs. Keep the drug at the conjunctiva, by ingestion - rinse eyes with water.

Abacavir+Lamivudine+Zidovudine

Trade name:
Trizivir

International name:
Abacavir + Lamivudine + Zidovudine (Abacavir + Lamivudine + Zidovudine)

Group Affiliation:
Antiviral agent

Description of the active substance (INN):
Abacavir + Lamivudine + Zidovudine

Dosage form:
coated tablets

Mode of action:
Combination antiviral drug. Abacavir, Lamivudine and Zidovudine - nucleoside analogues, inhibitors of the enzyme reverse transcriptase. Consistently metabolized by intracellular kinases to 5 "-triphosphate. Lamivudine triphosphate, abacavir and zidovudine triphosphate triphosphate are substrates and competitive inhibitors of HIV reverse transcriptase. The main mechanism of their antiviral activity is to introduce monofosfatnyh forms of these drugs in the chain of viral DNA, with subsequent rupture. Lamivudine, zidovudine and abacavir show a much lower affinity to the DNA polymerase of the host cells. Lamivudine and zidovudine have a high synergistic action and inhibit HIV replication in cell culture. Abacavir in vitro also showed a synergistic action with zidovudine and an additional effect in combination with lamivudine. In vitro derived strains HIV-1 resistant to abacavir. genotypic resistance due to specific changes in certain codons reverse transcriptase (codons M184V, K65R, L74V and Y115F) and evolves relatively slowly, due to multiple mutations of the virus, resulting in up to 8-fold increase in IC50 compared with a wild strain of HIV. In strains that are resistant to abacavir, there is a reduction in sensitivity to lamivudine, zalcitabine and / or didanosine, but sensitivity to zidovudine, and stavudine is maintained. Reduction of sensitivity to abacavir were noted in hospital strains of HIV isolated from patients with uncontrolled viral replication previously treated with other nucleoside inhibitors, or resistant to them. ineffectiveness of initial combination therapy of abacavir, lamivudine and zidovudine is mainly due to mutations in one codon M184V, which supports the view of the need for second-line treatments. The development of cross-resistance between abacavir, zidovudine and lamivudine and protease inhibitors or non-nucleoside reverse transcriptase inhibitors is unlikely.

Indications:
HIV infection.

Contraindications:
Hypersensitivity, hepatic failure, neutropenia (less than 750/mkl), decreased Hb (less than 75 g / l or 4.65 mmol / l), children's age (12 years), body weight less than 40 kg, during laktatsii.C caution. Pregnancy.

Side effects:
From the CCC: cardiomyopathy. On the part of the digestive tract: nausea, vomiting, diarrhea, pain in upper abdominal, anorexia, pigmentation of oral mucosa, bloating, transient increase in activity of "liver" transaminase (ACT, ALT), serum amylase, hyperbilirubinemia, pancreatitis, marked hepatomegaly with steatosis. From the side of blood: anemia, erythrocytic germ cell aplasia of the bone marrow, neutropenia, thrombocytopenia, leukopenia, pancytopenia. From the Metabolic: lactic acidosis. From the musculoskeletal system: the defeat of the muscles rarely - rhabdomyolysis, myalgia, myopathy, arthralgia. the nervous system: headache, insomnia, peripheral neuropathy, paresthesia, dizziness, drowsiness, convulsions, anxiety, depression, reduced speed of thinking. On the part of the respiratory system: cough, shortness of breath. On the part of the skin: skin rash (without systemic symptoms), alopecia, pigmentation of nails and skin rash, itching, sweating, rarely - exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome). allergic reactions. Other: fever , lethargy, fatigue, malaise, anorexia, frequent urination, taste perversion, pain, chills, chest pain, flu-like syndrome, gynecomastia, asteniya.Peredozirovka. Treatment: observation of a doctor, if necessary - supportive therapy. Because lamivudine excreted by dialysis, the overdose could be applied long hemodialysis. At the same time, the effectiveness of hemodialysis and peritoneal dialysis is inadequate for the elimination of zidovudine, but its metabolite glucuronide excretion increases. The effectiveness of hemodialysis and peritoneal dialysis in overdose abacavir is not known.

Dosage and administration:
Inside, regardless of the meal. Adults and children over 12 years - 1 tablet 2 times a day. In renal insufficiency (CC less than 50 ml / min) required dose reduction of lamivudine and zidovudine, it would be preferable to appoint abacavir, lamivudine and zidovudine separately. When Hb value of less than 90 g / l (5.59 mmol / l) or neutrophil count below 1 thousand / ml abacavir, zidovudine and lamivudine should be nominated separately.

Cautions:
Treatment should be under the supervision of a physician with experience in management of HIV infected patients. In appointing the elderly patients should pay particular attention to the possible age decline of renal function and changes in blood indices. HIV-infected patients, more frequently in women, with the use of antiretroviral nucleoside analogs including abacavir, lamivudine, zidovudine, were observed lactic acidosis and severe hepatomegaly with steatosis, leading to death. The drug should be used with caution in the presence of risk factors for liver disease and cancel in the case of lactic acidosis or signs of hepatotoxicity. Zidovudine, particularly in the high dose (1200-1500 mg / day) can cause anemia, neutropenia and leukopenia in patients with signs suppression of bone marrow function prior to treatment, especially when deployed clinical picture of HIV infection with the concentration of CD4 cells less 100/mkl. The risk of neutropenia increases in the case of source reduction in the number of neutrophils, Hb, and cyanocobalamin. During the period of treatment should be carefully monitored blood parameters. Gematotoksichnost usually develops within 4-6 weeks of therapy. For patients with a comprehensive clinical picture of HIV infection is recommended to perform blood tests every 2 weeks during the first 3 months of therapy and then monthly. In the early stage of HIV infection - every 1-3 months. Patients with severe anemia and bone marrow suppression (Hb less than 90 g / l or neutrophil count less than 1 thousand / ml) required dosage adjustment of zidovudine, it would be preferable to abacavir, lamivudine and zidovudine separately. Pancreatitis is rare in the abacavir, zidovudine and lamivudine, and it is not clear is whether his development with their drug use or HIV infection. In case of clinical and laboratory signs of pancreatitis drug overturned. Some patients with chronic hepatitis B with lamivudine cancellation can appear clinical and laboratory signs of recurrence of hepatitis. If you remove the drug in patients coinfected with hepatitis B virus must be monitored to determine liver function and serological markers of viral replication. During the period of treatment may develop opportunistic infections and other complications of HIV infection, so patients should be under the supervision of a physician with experience treating these diseases. Patients should be informed that current antiretroviral therapy does not prevent HIV infection through sexual contact or through infected blood to them. It should comply with the relevant precautions. Abacavir, lamivudine and zidovudine should be used separately if necessary, dose adjustment of one of the components.

Interaction:
Clinically significant interactions between abacavir, zidovudine and lamivudine were observed. Abacavir: did not inhibit the metabolism associated with ZA4 isoenzymes, CYP3A4, CYP2C9, CYP2D6 cytochrome P450 and does not increase hepatic metabolism, so the probability of interaction with antiretroviral protease inhibitors and drugs, is metabolized with the participation of isoenzymes of cytochrome P450 is low. The metabolism of abacavir is violated or combined with ethanol, which is accompanied by an increase in AUC by 41% and has no clinical significance. Abacavir has no effect on the metabolism of ethanol. With simultaneous use of abacavir at a dose of 600 mg 2 times a day and methadone C max of abacavir snizhalaetsya 35%, a TCmax increased by 1 h the AUC does not change. These data have clinical significance. Abacavir increases the systemic clearance of methadone by 22%, so sometimes you may need dosage adjustment of methadone. Retinoids are derived from the body by the enzyme alcohol dehydrogenase, so there may be interactions with abacavir. Lamivudine: appointment of trimethoprim / sulfamethoxazole at a dose of 160 mg/800 mg causes an increase in exposure to lamivudine 40% In the absence of renal insufficiency, dose adjustment of lamivudine is not required. Lamivudine has no effect on the pharmacokinetics of trimethoprim or sulfamethoxazole. Lamivudine may inhibit the intracellular phosphorylation zalitsitabina. The drug is not recommended for use in conjunction with zalcitabine. Zidovudine: the combined use of zidovudine and lamivudine leads to an increase of 13% of zidovudine exposure and a 28% increase Cmax in the plasma, but the total exposure (AUC) was not significantly disturbed and does not require dose adjustment. Zidovudine does not affect the pharmacokinetics of lamivudine. The concentration of phenytoin in the blood of patients receiving zidovudine, usually low, but in some cases it may be increased, so the concentration of phenytoin when combined it with the drug should be monitored. Drugs that block tubular secretion increases T1 / 2 and AUC of zidovudine by reducing glyukuronirovaniya, with renal excretion of glucuronide (and possibly zidovudine itself) is reduced. Because the nucleoside analogue ribavirin is an antagonist of zidovudine, should avoid this combination of drugs. Rifampicin reduces the AUC of zidovudine by 48 * 34%, but the clinical significance of this change is not known. Zidovudine may inhibit the intracellular phosphorylation of stavudine, stavudine therefore should not be mixed with the drug. The combination with potentially nephrotoxic and mielosupressivnymi drugs (pentamidine, dapsone, pyrimethamine, sulfamethoxazole / trimethoprim, amphotericin B, flutsitozin, ganciclovir, interferon, vincristine, vinblastine, doxorubicin) increases the risk of adverse reactions to zidovudine. In cases where such treatment is necessary, carefully monitor renal function and blood parameters, if necessary - dose was reduced. With extreme caution the drug should be used in combination with ASA, codeine, morphine, methadone, indomethacin, ketoprofenom, naproksenom, oksazepamom, lorazepam, cimetidine , clofibrate, dapsone, inosine pranobeksom because they violate its metabolism through competitive inhibition glyukuronirovaniya or direct suppression of microsomal oxidation in the liver.

TRIAMCINOLONE ACETONIDE

Pharmacological action

SCS. Inhibits the function of leukocytes and tissue macrophages. The migration of leukocytes in the area of inflammation. Impair the capacity of macrophages to phagocytosis and the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the field of inflammation. Decreases capillary permeability due to histamine release. Inhibits activity of fibroblasts and collagen formation.

Inhibits the activity of phospholipase A 2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce production of prostaglandins.

Reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the vascular bed to lymphoid tissue, suppresses the formation of antibodies.

Suppresses the release of pituitary ACTH and β-lipotropina, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

With direct application of the receptacles has a vasoconstrictor effect.

It has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the capture of amino acids by the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, increases glycogen deposition by stimulating the activity glikogensintetazy and synthesis of glucose from the products of protein metabolism. Increased blood glucose activates the secretion of insulin.

Suppresses the seizure of glucose by fat cells that leads to activation of lipolysis. However, due to increased secretion of insulin is stimulation of lipogenesis, which contributes to the accumulation of fat.

Has catabolic effect in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue.

Osteoporosis and Cushing's syndrome Itsenko-are the main factors limiting the long-term therapy of GCS. As a result of catabolic actions may suppress growth in children.

In high doses may increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. It stimulates the excessive production of hydrochloric acid and pepsin in the stomach that promotes the development of peptic ulcers.

The systems use therapeutic activity due to anti-inflammatory, anti-allergic, immunosuppressive and antiproliferative action.

When external and local application of therapeutic activity triamtsinolona acetonide caused by anti-inflammatory, anti-allergic and antiexudative (due to vasoconstrictor effect) action.

For anti-inflammatory activity triamtsinolona acetonide in 6 times more active than hydrocortisone. Mineralocorticoid activity in triamtsinolona acetonide is virtually absent.


Pharmacokinetics

When the system application is metabolized primarily in the liver and partially - in the kidneys. The main route of metabolism is a 6-β-hydroxylation. T 1 / 2 - 3.5 hours is derived by the kidneys.


Statement

For regular use: asthma, chronic bronchitis with bronchoobstructive syndrome, pemphigoid, psoriasis, dermatitis.

Intraarticular injection: chronic inflammatory disease of the joints, exudative arthritis, gout, dropsy of the joints, the blockade of the shoulder joint, chronic inflammation of the inner layer of articular capsule.

For external use: eczema, psoriasis, atopic dermatitis, various types of dermatitis and other inflammatory and allergic skin diseases non-microbial etiology (combined therapy).


Dosage regimen

Solo, depending on the evidence and applied dosage form.


Side effect

On the part of the endocrine system: the redistribution of body fat, menstrual irregularities, increased blood glucose, adrenal suppression, moon face, striae, hirsutism, acne.

From the Metabolic: edema, electrolyte imbalance, negative nitrogen balance, growth retardation in children.

On the part of the digestive system: steroid ulcer, erosive and ulcerative lesions gastrointestinal acute pancreatitis.

From the CNS: convulsions, sleep disorders, mental disorders, headaches and dizziness, weakness.

On the part of the musculoskeletal system: myopathy, osteoporosis.

Since the cardiovascular system: hypertension.

From the blood coagulation system: thromboembolism.

On the part of the organ of vision: visual impairment, back subcapsular cataracts, increased intraocular pressure, or exophthalmos, anaphylactic reactions.

Reactions due to immunosuppressive effect: intensification of infectious diseases.

With intraarticular injection: possible joint pain, irritation at the injection site, hyperpigmentation, sterile abscess, atrophy of the skin, with the introduction of doses over 40 mg resorptive possible side effects.

For exterior use: possible itching, skin irritation, the late reaction of the type of eczema, steroid acne, purpura. Prolonged use of the ointment may develop secondary infectious lesions and atrophic changes of the skin.


Contraindications

Acute psychosis, a history of active TB disease, myasthenia gravis, tumor metastases, diverticulitis, stomach ulcer and duodenal ulcer, hypertension, Cushing's syndrome Itsenko-, renal failure, thrombosis and embolism in history, osteoporosis, diabetes, latent foci of infection, amyloidosis, syphilis, fungal diseases, viral infections (including those caused by Herpes simplex and Varicella zoster), amoebic infections, polio (except bulbar encephalitis-form), gonococcal or tuberculous arthritis, the period of vaccination lymphadenitis after BCG vaccination, glaucoma infected skin lesions.


Application of pregnancy and breastfeeding

If necessary, use during pregnancy (especially in the I trimester) and during lactation should assess the perceived benefit to the mother and the risk of side effects in the fetus or child.


Cautions

Not designed for to / in the introduction.

With caution and under strict medical supervision is used in edema, obesity, mental illness and gastrointestinal diseases. In the period of treatment is recommended to take vitamin D supplements and consume foods rich in calcium.

When applied externally to prevent local infectious complications is recommended in combination with antimicrobials.

Parenteral use in children under 6 years not recommended; aged 6-12 years - according to strict indications.

Should avoid prolonged outdoor use in children regardless of age.


Drug Interactions

With the simultaneous use of anabolic steroids, androgens increase the risk of peripheral edema, acne.

At simultaneous application with antithyroid drugs and thyroid hormones may change thyroid function.

With simultaneous application of histamine H 1 blocker receptors decreases action triamtsinolona; with hormonal contraception - potentsiruet triamtsinolona.

Hypocalcemia associated with the use of triamtsinolona may lead to an increase in the duration of neuromuscular blockade caused by the action of the depolarizing muscle relaxants in their simultaneous application.

With the simultaneous use of immunosuppressants increases the risk of bacterial and viral infections.

With the simultaneous use of potassium-sparing diuretics can hypokalaemia.

With the simultaneous use may decrease the effectiveness of indirect anticoagulants, heparin, streptokinase, urokinase, increasing the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract.

With the simultaneous use of NSAIDs (including with acetylsalicylic acid) increases the risk of erosive-ulcerative lesions and bleeding from the gastrointestinal tract.

With simultaneous application of attenuated effect of oral hypoglycemic funds insulin; with laxatives - can hypokalaemia; with cardiac glycosides - increase the risk of cardiac arrhythmias and other toxic effects of glycosides.

With the simultaneous use of tricyclic antidepressants may gain mental disorders associated with the reception triamtsinolona.



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SODIUM AMIDOTRIZOATE

Pharmacological action

Radiocontrast diagnostic tool that contains iodine. Increases contrast of the image by x-ray absorption of iodine.


Statement

Apply for / v and retrograde urography, for angiokoronarografii, as well as for the image contrast of the cavities of the body (CT imaging, hysterosalpingography).


Dosage regimen

The dose depends on the evidence and the applicable dosage form.


Side effect

On the part of the digestive system: nausea, vomiting.

Allergic reactions: urticaria, Quincke's edema, asthma, anaphylactic reactions up to shock and collapse (especially in predisposed patients).

Other: dizziness, erythema, cyanosis, a feeling of heat and pain during injection.


Contraindications

Absolute: severe hyperthyroidism, circulatory failure with signs of decompensation, hypersensitivity to iodine-containing drugs, marked renal and hepatic failure, active tuberculosis and pulmonary emphysema, cardiomyopathy, arterial hypertension, heavy flow, a state of shock and collapse. In acute forms of phlebitis venography is contraindicated.

Relative: cerebral arteriosclerosis, decompensated diabetes mellitus, increased blood clotting, nodular goiter easy flow plasmacytoma, pregnancy, severe general condition of the patient.


Cautions

For coronary use only 76% solution.