Arthrotec

Composition, structure and packing

Tablets are white or nearly white, round, biconvex, on one side and embossed in the form of arranged in a circle four characters "A", on the other - "Searle" and "1411".

1 tab. - Diclofenac sodium 50 mg - 200 micrograms misoprostol

Excipients: methylhydroxypropylcellulose, aerosil, microcrystalline cellulose, krospovidon, hydrogenated castor oil, lactose, corn starch, povidone (K-30), magnesium stearate, cellulose acetate phthalate, diethyl phthalate.

Tablets are white or nearly white, round, biconvex, on one side and embossed in the form of four characters "A" surrounding the number "75", on the other - "Searle" and "1421".

1 tab. - Diclofenac sodium -75 mg misoprostol 200 micrograms

Excipients: methylhydroxypropylcellulose, aerosil, microcrystalline cellulose, krospovidon, hydrogenated castor oil, lactose, corn starch, povidone (K-30), magnesium stearate, cellulose acetate phthalate, diethyl phthalate.

Clinico-pharmacological group

NSAIDs in combination with a synthetic analogue of prostaglandin E1.

Pharmacological action

Artrotek is a combination of diclofenac sodium - NSAID, which has anti-inflammatory and analgesic properties, and misoprostol - a synthetic analogue of prostaglandin E1, which protects the mucous membrane of the digestive tract. The mechanism of action of diclofenac sodium is linked to its ability to selectively inhibit COX-1 and COX-2.

Misoprostol is a synthetic analogue of prostaglandin E1, the reinforcing effect of factors involved in the protection of the mucous membrane of the stomach and duodenum. Misoprostol supports blood flow to the stomach, reduces the secretion of pepsin and hydrochloric acid in the stomach, promotes the formation of bicarbonate in the duodenum.

Pharmacokinetics

Pharmacokinetics of diclofenac and misoprostol in combination is similar to the pharmacokinetics of these drugs while taking in the form of individual tablets.

Pharmacokinetic interaction between these two substances was observed. After receiving multiple Artroteka cumulation of diclofenac, misoprostol, or misoprostol acid does not occur.

Indications for use of the drug

Expectant treatment
rheumatoid arthritis;
osteoarthritis;
ankylosing spondylitis;
acute joint-muscle pain.

Dosage regimen

Inside during the meal, not liquid, tablets can not crush or dissolve.

Artrotek recommended in the following doses:

Osteoarthritis, rheumatoid arthritis:

Tablets containing a dose of 50 mg/200 mg - 1 tablet 2-3; tablets containing a dose of 75 mg/200 mg - 1 tablet 2.

Ankylosing spondylitis:

Tablets containing a dose of 50 mg/200 mg - 1 tablet 2-3; tablets containing a dose of 75 mg/200 mg - 1 tablet 2.

Acute joint-muscle pain syndrome:

Tablets containing a dose of 50 mg/200 mg - 1 tablet 2-3; tablets containing a dose of 75 mg/200 mg - 1 tablet 2.

Side effect

Registered in major adverse reactions from the gastrointestinal tract, whose frequency is> 1%: abdominal pain, constipation, diarrhea, duodenitis, dyspepsia, eructation, esophagitis, flatulence, gastritis, nausea and vomiting.

Abdominal pain and diarrhea are usually transient in nature and are mild or moderate.

In addition, have been reported such side effects as dizziness, headache, insomnia, itchy skin, hemorrhagic rash, gastrointestinal bleeding and perforation. Also, changes in laboratory parameters were detected: elevated levels of alkaline phosphatase, decrease in hematocrit and increases in ALT.

Among women who received Artrotek, there have been adverse reactions from the breast and genital organs: breast pain, dysmenorrhea, intermenstrual bleeding in the period, menorrhagia, irregular menstruation, cramping abdominal pain, bloody discharge from the vagina (including bleeding in women postmenopausal), vaginitis.

During the observation period after the registration of the drug were additionally identified the following adverse reactions: Allergic reactions (including anaphylaxis and angioedema), skin reactions (including rash and bullous eruptions), mood changes, shortness of breath, hepatitis, interstitial nephritis, pancreatitis, acute renal failure, stomatitis , thrombocytopenia, rash, anemia, epidermal necrolysis.

In very rare cases, during therapy with diclofenac / misoprostol were reported blurred vision, heavy dreams, as well as reaction from the skin and mucous membranes.

In cases of administration of misoprostol by pregnant women revealed the following side effects: abnormal uterine contractions, uterine bleeding, uterine rupture / perforation, delay in separation of the placenta, amniotic fluid embolism, incomplete abortion, premature birth, fetal death, congenital malformations.

Contraindications to the use of the drug
active gastrointestinal bleeding;
pregnancy and lactation;
hypersensitivity to diclofenac sodium, misoprostol, or any other ingredients of the drug to other NSAIDs, including acetylsalicylic acid, as well as other prostaglandins;
"Aspirin" bronchial asthma, hemodyscrasia.

Data on the safety and efficacy Artroteka in children aged under 18 years of absence.

Precautions: anemia, asthma, congestive heart failure, hypertension, porphyria, old age, erosive and ulcerative lesions of the gastrointestinal tract of a history of liver or kidney failure, heart disease, fluid retention in the body, dehydration.

Pregnancy and lactation

Artrotek contraindicated in pregnant women, because misoprostol causes uterine contractions and may result in miscarriages, premature birth and fetal death. In the application of misoprostol may have malformations of the fetus. Diclofenac may cause premature closure of Botallova duct.

Misoprostol should not be prescribed for lactating mothers, since the possible allocation of misoprostol acid in milk can cause diarrhea in infants. It is not known whether this drug is released from the mother's milk. However, since many drugs are excreted with breast milk, as well as the fact that there is a possibility of development in infants adverse reactions to diclofenac / misoprostol, you should either give up breastfeeding or stop taking the drug.

Application for violations of liver function

With care apply in hepatic failure.

Application for violations of renal function

With caution used in renal insufficiency.

Cautions

In patients treated with NSAID therapy, including Artrotek were reported serious adverse reactions from the gastrointestinal tract, such as bleeding, sores and perforation.

Physicians and patients should be aware of a potential cause ulcers, even in the absence of symptoms from the gastrointestinal tract.

NSAIDs, including Artrotek should be used with caution in patients with diseases of the digestive tract in history or in the active stage, such as ulcers, bleeding, inflammatory bowel disease.

Women of childbearing age can not begin therapy until Artrotekom until pregnancy is excluded, and they should use reliable contraceptive measures during the entire period of therapy. If you are planning pregnancy, this medication should be abolished.

The therapy Artrotekom should periodically monitor liver function. If Artrotek be considered in patients with impaired liver function, the treatment should be carried out under constant medical supervision.

Patients with kidney, liver or heart diseases should also be careful, because the use of NSAIDs, including diclofenac / misoprostol, can lead to a breach of kidney function. Care must be taken in the early treatment of patients with dehydration. You should use the lowest possible dose and regular monitoring of renal function.

In patients treated with NSAIDs, including Artrotek were also marked fluid retention and swelling. Therefore, caution should be exercised in the appointment Artroteka patients with chronic heart failure in history, as well as conditions predisposing to fluid retention.

NSAIDs, including diclofenac, increase the time of platelet aggregation. Misoprostol does not strengthen the influence of diclofenac on platelet activity.

Artrotek reduces inflammation, it can reduce the severity of symptoms, allowing diagnosis of infectious diseases, such as fever.

Patients aged 65 years and older profile of side effects of diclofenac / misoprostol is similar to that in younger with only clinically significant difference is that patients age 65 and older are more susceptible to the adverse effects of diclofenac / misoprostol in the gastrointestinal tract.

Overdose

Toxic doses Artroteka not installed. However, describes the symptoms of overdose caused by components of the drug: nausea, vomiting, abdominal pain, bleeding, confusion, drowsiness, reduced muscle tone.

Clinical symptoms suggestive of an overdose of misoprostol are: tremors, convulsions, shortness of breath, abdominal pain, diarrhea, fever, palpitation, hypotension, bradycardia.

Treatment: acute overdose, gastric lavage is shown. It may also be effective in the forced diuresis, since metabolites of diclofenac and misoprostol is excreted with urine. Effect of dialysis on the elimination of diclofenac (the degree of binding is to plasma proteins is 99%) and misoprostol acid (the degree of plasma protein binding of less than 90%), while not determined. Ingestion of activated charcoal helps to reduce the absorption of diclofenac / misoprostol.

Drug Interactions

Diclofenac acetylsalicylic acid is displaced from its binding site from albumin, which reduces the concentration of diclofenac in plasma, as well as to reduce its maximum concentration in plasma and to decrease the value AUC. In this regard, it is not recommended the simultaneous use of diclofenac / misoprostol and acetylsalicylic acid.

In patients receiving both digoxin and diclofenac, recorded the highest levels of digoxin. Therefore, patients receiving both digoxin and diclofenac / misoprostol should be under medical supervision to identify the toxic effect of digoxin.

NSAIDs may reduce natriuretic effect of diuretics. Since the simultaneous use of potassium-sparing diuretics may increase potassium levels observed in the serum in such cases must monitor the level of this indicator. Be careful when appointing diclofenac / misoprostol in conjunction with the above mentioned drugs.

It is established that a number of NSAIDs interact with anticoagulants taken orally, although noted that diclofenac does not interact with anticoagulants such as warfarin. When you receive indirect anticoagulants (warfarin) with NPVC increases the risk of bleeding from the gastrointestinal tract. Therefore, patients receiving anticoagulants concurrently with this type of diclofenac / misoprostol should be monitored, so if necessary it was carried out adjusting the dose of anticoagulant

NPVC can reduce the effect of antihypertensive agents, including ACE inhibitors. In case of simultaneous appointment of diclofenac / misoprostol with ACE inhibitors may worsen renal function.

Diclofenac does not affect glucose metabolism in healthy people, in addition, while the use of diclofenac with antidiabetic means for oral action of the latter does not change. However, there are reports of change of such drugs at their reception at the same time NPVC. Therefore Artrotek be used with caution to patients receiving insulin or hypoglycemic means for oral administration.

Care should be exercised in the appointment while NPVC, including Artrotek, methotrexate, because NSAIDs can increase the level of methotrexate in plasma.

Diclofenac reduces the renal clearance of lithium and increase the concentration of lithium in plasma. Therefore, patients receiving lithium, Artrotek be used with caution.

Antacids may slow the absorption of diclofenac. Magnesium-containing antacids may provoke exacerbation of diarrhea associated with misoprostol.

Cyclooxygenase inhibitors, such as diclofenac, through their effects on renal prostaglandins, may increase the nephrotoxicity of cyclosporine.

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Drug prescription.

Terms and Conditions of storage

List B. In dry, the reach of children, at a temperature not exceeding 25 ° C.

Shelf life - 3 years. Do not use later than the date specified on the package.

Artrosilen

Composition, structure and packing

Capsules are hard gelatin, oblong, with a white body and dark green cap, the contents of capsules - round granules of light yellow color.

1 capsule. ketoprofen lysine salt 320 mg.

Excipients: diethyl phthalate, karboksipolimetilen, magnesium stearate, povidone, acrylic and methacrylic acid polymers, talc. The composition of the shell capsules: titanium dioxide (E171), quinoline yellow (E104), indigo, titanium dioxide, gelatin.

Solution for in / and / m the introduction of transparent, colorless or slightly yellow.

1 ml of 1 amp. ketoprofen lysine salt 80 mg 160 mg.

Excipients: sodium hydroxide, citric acid, water d / and.

Rectal suppositories homogeneous, white to light yellow, torpedoobraznoy form.

A TIS. ketoprofen lysine salt 160 mg.

Excipients: semisynthetic glycerides.

Aerosol for external use only 15% in the form of a homogeneous foam after the release of gas - a transparent liquid of pale yellow color. 1 g of foam ketoprofen lysine salt 150 mg. Excipients: polysorbate, polypropylene, povidone, liquid nerolenovaya, benzyl alcohol, purified water, propellant - propane-butane.

Gel for external use only 5% transparent, thick with the smell of lavender. 1 g of ketoprofen lysine salt 50 mg Excipients: karboksipolimetilen, triethanolamine, polyoxyethylene sorbitan monooleate (vegetable oil), ethanol, metilparagidroksibenzoat, nerolenovaya liquid, distilled water.

Clinico-pharmacological group: NSAID.

Pharmacological action

NSAID. Has anti-inflammatory, analgesic and antipyretic effect. By inhibiting COX-1 and COX-2 inhibits the synthesis of prostaglandins. Has antibradikininovoy activity, stabilizes lysosomal membranes and prevents the release of these enzymes that contribute to tissue damage in chronic inflammation.

Reduces the allocation of cytokines, inhibits the activity of neutrophils. Reduces morning stiffness and swelling of the joints, increases range of motion. Ketoprofen lysine salt, in contrast to ketoprofen, an instant connection with a neutral pH, due to which almost does not irritate the digestive tract. Once inside the maximum therapeutic effect was observed for 4 to 24 hours when applied externally Artrozilen reduces the expression of inflammation and pain in damaged joints, tendons, ligaments and muscles.

When articular syndrome causes a weakening of joint pain at rest and in motion, decrease morning stiffness and swelling of the joints. Ketoprofen lysine salt does not have a catabolic effect on articular cartilage.

Pharmacokinetics

Absorption

After oral ketoprofen capsules quickly and adequately absorbed from the gastrointestinal tract, bioavailability exceeds 80%. Cmax of 3.9 mcg / ml and reached after 4-10 h, its value is directly dependent on the applied dose. Simultaneous food intake reduces the value of Cmax and an increase in Tmax, without changing the AUC. After rectal ketoprofen is also rapidly absorbed.

Time to reach Cmax following rectal 45-60 min. The concentration in plasma is linearly dependent on the applied dose. Time to reach Cmax for parenteral administration 45-60 min. The effective concentration remains 24 hours therapeutic concentrations in synovial fluid remain 18-20 h. epicutaneous application absorbed slowly; dose of 50-150 mg every 5-8 h creates a level of concentration in plasma of 0.08-0.15 mg / ml. Bioavailability of the drug - about 5%.

Distribution

Up to 99% ketoprofen bound to plasma proteins, primarily albumin. Vd - 0.1-0.2 L / kg. Easily penetrates through histohematogenous barriers and is distributed in the tissues and organs. Ketoprofen well into the synovial fluid and connective tissue. Although the concentration of ketoprofen in the synovial fluid is slightly lower than in plasma, it is more stable (save up to 30 h).

Metabolism

Ketoprofen is mainly metabolized in the liver, where it is glyukuronizatsii to form esters with glucuronic acid.

Withdrawal

T1 / 2 was 6.5 h. The metabolites are derived mainly from urine (up to 76% within 24 h). Since feces derived less than 1%. Drug is not cumulative in the body.

Statement

For oral and rectal pain docking weak to moderate intensity, including:
postoperative pain;
Post-traumatic pain;
inflammatory pain.

Symptomatic treatment of rheumatic and inflammatory diseases, including:
rheumatoid arthritis;
spondyloarthritis;
osteoarthritis;
gouty arthritis;
Inflammatory periarticular tissues.

For parenteral

Short-term treatment of acute pain:
in diseases of the musculoskeletal system of various origins;
in the postoperative period;
after injury and inflammatory processes.

For external use - acute and chronic inflammatory diseases of the musculoskeletal system (including rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, osteoarthritis of peripheral joints and spine, soft tissue rheumatism);
muscle pain and rheumatoid Non-rheumatic origin;
traumatic injuries of soft tissues.

Dosage regimen

Inside Artrozilen appoint 1 kaps. / day, during or after a meal. Duration of treatment may be 3-4 months. Rectal appoint 1 suppository 2-3 times / day. The maximum daily dose - 480 mg. Elderly patients should not appoint more than 2 suppositories per day.

If any function of the kidneys and liver need to reduce the dose. Parenteral (IM or IV) drug is administered in a dose of 160 mg (1 amp.) A day. The maximum daily dose is 320 mg (1 amp. 2 times / day). Elderly patients should be appointed not more than 1 amp. / day. Parenteral drug should be administered short duration (up to 3 days), then move on to taking the drug by mouth or by the use of suppositories. In / to the introduction of the drug is allowed only in the hospital.

To increase the duration of the drug recommended to carry out a slow i / v infusion. Duration / v infusion of at least 30 minutes. The solution for infusion is prepared on the basis of 50 ml or 500 ml of the following aqueous solutions: 0.9% sodium chloride, 10% aqueous solution of levulose 5% aqueous solution of dextrose, Ringer's acetate, Ringer Lactate Hartmann, colloidal solution of dextran in 0.9% sodium chloride or 5% dextrose.

When breeding Artrozilena in solutions of small volume (50 ml) the drug is introduced into / in the bolus. For exterior use single dose of gel is 5.3 g (large amount of cherries), Aerosol - 1-2 grams (size of a walnut). The product should be applied 2-3 times a day, rubbing gently until completely absorbed. Duration of treatment should not exceed 10 days (without consulting a doctor).

Side effect
On the part of the digestive system: abdominal pain, diarrhea, stomatitis, esophagitis, gastritis, duodenitis, erosive and ulcerative lesions gastrointestinal gematomezis, melena, increased bilirubin, increased liver enzymes, hepatitis, liver failure, enlarged liver.
From the central nervous system and peripheral nervous system: dizziness, hyperkinesia, tremor, vertigo, mood swings, anxiety, hallucinations, irritability, malaise, visual disturbances. Allergic reactions: urticaria, angioedema, erythema multiforme exudative (including Stevens-Johnson syndrome), anaphylactoid reaction (swelling of the oral mucosa, pharyngeal edema, periorbital edema). Dermatological reactions: erythematous rash, itching, Makulo-papular rash.
From the urinary system: painful urination, cystitis, edema, hematuria.
On the part of the hemopoietic system: leykotsitopeniya, leukocytosis, lymphangitis, a decrease prothrombin time, thrombocytopenia, thrombocytopenic purpura, an increase in the size of the spleen, vasculitis.
On the part of the respiratory system: bronchospasm, dyspnoea, sensation of spasm of the larynx, laryngism, larynx edema, rhinitis.
Since the cardiovascular system: hypertension, hypotension, tachycardia, chest pain, syncopal states, peripheral edema, pallor.

Other: conjunctivitis, menstrual disorders, increased sweating. Local reactions in rectal: burning, itching, heaviness in the anorectal region, exacerbation of hemorrhoids.

Local reactions when used externally: Skin manifestations of allergic reactions, photosensitivity. With prolonged use over large surface of the skin may develop systemic side effects. Ketoprofen lysine salt is much less common cause side effects compared with ketoprofenom.

Contraindications
"Aspirin triad";
III trimester of pregnancy;
lactation;
Hypersensitivity to ketoprofenu or other components of the drug, acetylsalicylic acid or other NSAIDs.

For regular use:
stomach ulcer and duodenal ulcer exacerbation;
Ulcerative colitis exacerbation;
Crohn's disease;
diverticulitis;
peptic ulcer;
blood coagulation disorders (including hemophilia);
chronic renal failure;
childhood and adolescence to 18 years.

For external use
weeping dermatitis;
eczema
violation of the integrity of the skin;
Children under 6 years.

Precautions should be prescribed the drug in I and II trimesters of pregnancy, as well as elderly patients.

The systems use caution should be exercised with anemia, asthma, alcoholism, smoking, alcoholic cirrhosis, hyperbilirubinemia, hepatic failure, diabetes, dehydration, sepsis, chronic heart failure, edema, hypertension, blood diseases (including leukopenia ), deficiency of glucose-6-phosphate dehydrogenase, stomatitis, when used externally - with acute hepatic porphyria, erosive and ulcerative lesions of the gastrointestinal tract, severe violations of liver and kidney function, congestive heart failure, asthma, and children under the age of 12 years.

Bermennost and lactation

Use of the drug Artrozilen in III trimester of pregnancy is contraindicated. In I and II trimesters of pregnancy should use the drug Artrozilen with caution and under medical supervision.

If necessary, use during lactation breastfeeding should be discontinued. Women planning pregnancy, should refrain from taking the drug Artrozilen, because against the background of their intake may decrease the probability of implantation of the embryo.

Application for violations of liver function

If abnormal liver function should reduce the dose.

Application for violations of renal function

In case of violation of renal function should reduce the dose.

Cautions

During treatment with Artrozilen necessary to carry out periodic monitoring of the pattern of peripheral blood and functional state of the liver and kidneys.

If necessary, determine the 17-ketosteroids drug should be abolished for 48 h before the study. Receiving Artrozilena may mask signs of infection.

Application Artrozilena bronchial asthma can provoke an attack of breathlessness.

For exterior use medication should be applied only to intact skin. Avoid contact with eyes and mucous membranes. To avoid reflections of the heightened sensitivity and photosensitivity, it is recommended to avoid skin damage the sun during the course of treatment.

Aqueous solutions of ketoprofen lysine salt, and gel for external use can be used for physiotherapy treatment (iontophoresis, mesotherapy): for iontophoresis drug is applied to the negative pole.

Effects on ability to drive vehicles and management mechanisms

During the period of the drug should avoid potentially hazardous activities that require high concentration and quickness of psychomotor reactions.

Overdose

Currently, cases of drug overdose Artrozilen not reported. In case of overdose should be symptomatic therapy, monitoring of respiratory and cardiovascular activity. Specific antidote exists. Hemodialysis is ineffective.

Drug Interactions

Inductors microsomal oxidation in the liver (including phenytoin, ethanol, barbiturates, flumetsinol, rifampicin, fenilbutazon, tricyclic antidepressants), while the use of the drug Artrozilen increase metabolism ketoprofen (increase production of hydroxylated active metabolites). Against the background of the simultaneous application of the drug reduced the effectiveness Artrozilen urikozuricheskih drugs, increases the effects of anticoagulants, antiplatelet agents, fibrinolytics, ethanol, side effects mineralokortikoidov, glucocorticoids, estrogen, decreases the effectiveness of antihypertensive drugs and diuretics.

The simultaneous use of the drug Artrozilen with other NSAIDs, SCS, ethanol, corticotropin may lead to ulceration and the development of gastrointestinal bleeding, increased risk of renal dysfunction.

The simultaneous appointment Artrozilena with oral anticoagulants, heparin, thrombolytics, antiagregantami, cefoperazone, and tsefamandolom tsefotetanom increases the risk of bleeding.

The drug Artrozilen while the application increases the hypoglycemic effect of insulin and oral hypoglycemic agents (requires recalculation of dose).

Joint appointment Artrozilena with sodium valproate causes a disturbance of platelet aggregation. Ketoprofen in odnovremennnom application increases plasma concentration of nifedipine and verapamil, lithium, methotrexate. Antacids and kolestiramin while ingestion of the drug reduces the absorption of ketoprofen Artrozilen.

Terms and Conditions of storage

The drug should be kept in the dark, away from children below 25 ° C. The container with the aerosol can overheat! Expiration capsules and suppositories rectal - 5 years, a solution for in / and / m the introduction, gel and aerosol for external use - 3 years.

Artrosan

Composition, structure and packing

The tablets from light yellow to yellow, ploskotsilindricheskie, with beveled and risk tolerance of marbling.

1 tab. Meloxicam 7.5 mg - - 15 mg.

Excipients: potato starch, lactose monohydrate, povidone, trisodium citrate, magnesium stearate, colloidal silicon dioxide.

Clinico-pharmacological group: NSAID. Selective COX-2 inhibitor.

Pharmacological action

NSAIDs. Has anti-inflammatory, analgesic and antipyretic effect. Anti-inflammatory effect associated with inhibition of COX-2 - specific enzyme involved in the biosynthesis of prostaglandins in inflammation. To a lesser extent Meloxicam blocks the COX-1 involved in the synthesis of prostaglandin that protects the mucous membrane of the gastrointestinal tract and taking part in the regulation of blood flow in the kidneys.

Pharmacokinetics

Absorption

It is well absorbed from the gastrointestinal tract. The absolute bioavailability of meloxicam - 89%. Simultaneous ingestion does not alter absorption. When using the drug inside at doses 7.5 mg and 15 mg doses are proportional to its concentration.

Distribution

Css achieved in techenie3-5 days. With long-term use (more than 1 year) concentrations are similar to those that have been observed after the first reach a steady state pharmacokinetics. Binding to plasma proteins - more than 99%.

The vast differences between the maximum and basal concentrations of the drug after receiving a once a day is relatively small and at a dose of 7.5 mg of 0.4-1 mg / ml, a dose of 15 mg - 0.8-2 mg / ml. Meloxicam penetrates histohematogenous barriers, concentration in the synovial fluid reaches 50% Cmax plasma.

Metabolism

Meloxicam is almost completely metabolized in the liver with the formation of four pharmacologically inactive metabolites. The major metabolite, 5'-karboksimeloksikam (60% of the dose), formed by oxidation of the intermediate metabolite - 5'-gidroksimetilmeloksikama (9% of the dose).

In in vitro studies revealed that biotransformation occurs with the participation CYP2S9, the added value is isoenzyme CYP3A4. In the formation of two other metabolites (representing respectively 16% and 4% of the dose) is involved peroxidase activity which is likely to vary individually.

Withdrawal

We derive equally from the feces and urine, mostly as metabolites. With the feces as unchanged output of less than 5% of the daily dose in the urine as unchanged drug is found only in trace amounts. T1 / 2 - 15-20 h. The plasma clearance is approximately 8 ml / min.

Pharmacokinetics in special clinical situations

In the elderly clearance of the drug decreases. Vd is low and amounts to an average of 11 liters. In patients with hepatic or renal insufficiency moderately pharmacokinetics of meloxicam did not significantly change.

Statement

Cimptomaticheskaya therapy:
osteoarthritis;
rheumatoid arthritis;
ankylosing spondyloarthritis (Bechterew's disease);
other inflammatory and degenerative diseases associated with pain syndrome.

Dosage regimen

In rheumatoid arthritis the recommended dose is 15 mg / day, and after a therapeutic effect the dose can be reduced to 7.5 mg / day. In osteoarthrosis the drug administered in a dose of 7.5 mg / day, with no effect of the dose can be increased to 15 mg / day.

In ankylosing spondylitis daily dose is 15 mg. The maximum daily dose should not exceed 15 mg. Drugs are taken by mouth 1 time per day during meals.

In patients with increased risk of side effects, as well as in patients with severe impaired renal function who are on hemodialysis, the dose should not exceed 7.5 mg / day. Patients with impaired renal function (CC> 25 ml / min), dosage regimen adjustment is not required.

Side effect
On the part of the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, flatulence, erosive and ulcerative lesions gastrointestinal tract, perforation of stomach or intestinal bleeding from the gastrointestinal tract (implicit or explicit), increase in liver enzymes, hepatitis, colitis, stomatitis, dry mouth, esophagitis.
Since the cardiovascular system: tachycardia, increased blood pressure, feeling the tides.
On the part of the respiratory system: exacerbation of bronchial asthma, cough.
From the CNS: headache, dizziness, tinnitus, disorientation, confusion of thoughts, sleep disturbance.
From the urinary system: edema, interstitial nephritis, renal medullary necrosis, urinary tract infection, proteinuria, hematuria, renal insufficiency.
From the side of the organ of vision: conjunctivitis, blurred vision.

Dermatological reactions: increased photosensitivity.
On the part of the hemopoietic system: anemia, leukopenia, thrombocytopenia. Allergic reactions: anaphylactoid reactions (including anaphylactic shock), swelling of the lips and tongue, allergic vasculitis, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), itching, skin rash or urticaria.

Other: fever.

Contraindications
stomach ulcer and duodenal ulcer exacerbation;
renal failure, severe (without dialysis);
severe hepatic insufficiency,
"Aspirin" bronchial asthma;
Children under 15 years
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to the drug's components.

Precautions should be used drug in the elderly and in patients with erosive-ulcerative lesions of the gastrointestinal tract in history.

Pregnancy and lactation

The drug is contraindicated in pregnancy. If necessary, the appointment during lactation should resolve the issue of termination of breastfeeding.

Application for violations of liver function

Patients with hepatic insufficiency moderately pharmacokinetics of meloxicam did not significantly change. Should exercise caution and monitor indicators of renal function in the application of the drug in patients with cirrhosis.

Application for violations of renal function

In patients with renal insufficiency moderately pharmacokinetics of meloxicam did not significantly change. in patients with severe impaired renal function who are on hemodialysis, the dose should not exceed 7.5 mg / day. Patients with impaired renal function (spacecraft more than 25 ml / min), dosage regimen adjustment is not required.

Should exercise caution and monitor indicators of kidney function in the application of the drug in elderly patients, patients with chronic heart failure in patients with cirrhosis, as well as in patients with hypovolemia in surgical care.

Cautions

Caution must be exercised when applying the drug in patients with a history of ulcers of the stomach and duodenum, and patients receiving anticoagulant therapy. In these patients at increased risk of erosive and ulcerative lesions of the gastrointestinal tract.

Should exercise caution and monitor indicators of kidney function in the application of the drug in elderly patients, patients with chronic heart failure in patients with cirrhosis, as well as in patients with hypovolemia in surgical care.

Patients taking both diuretics and meloxicam, should receive plenty of fluids. Patients should be informed that, in allergic reactions (including itching, skin rash, urticaria, photosensitivity) should seek medical advice to address the issue of stopping.

Effects on ability to drive vehicles and management mechanisms

Use of the drug can cause the development of undesirable effects (including headaches, dizziness, drowsiness). Therefore should be abandoned vehicle management and maintenance arrangements that require concentration.

Overdose

Symptoms: impaired consciousness, nausea, vomiting, epigastric pain, bleeding from the gastrointestinal tract, acute renal failure, liver failure, respiratory arrest, asystole.

Treatment: gastric lavage, activated charcoal method (within 1 h after drug administration), if necessary, carry symptomatically. Kolestiramin accelerates the elimination of meloxicam from the body. Forced diuresis, alkalization of urine, hemodialysis is ineffective because of the high degree of binding of meloxicam with blood proteins. No specific antidote.

Drug Interactions

With simultaneous use of other NSAIDs (including with acetylsalicylic acid) increases the risk of erosive-ulcerative lesions and bleeding from the gastrointestinal tract. With the simultaneous use of antihypertensive drugs may reduce the effectiveness of the latter.

When applied simultaneously with the preparations of lithium may develop accumulation of lithium and increase its toxic action (recommended monitoring the concentration of lithium in the blood).

When applied simultaneously with methotrexate increases the risk of anemia and leukopenia (shown periodically, an overall analysis of blood). At simultaneous application with diuretics and cyclosporine increases the risk of renal failure.

With the simultaneous use of intrauterine contraceptive devices may reduce the effectiveness of the latter.

With the simultaneous use of anticoagulants (including those with heparin, ticlopidine, warfarin), as well as with thrombolytic drugs (including with streptokinase, fibrinolysin), an increased risk of bleeding (requires periodic monitoring of indicators of blood coagulation).

At simultaneous application with kolestiraminom increased excretion of meloxicam in the gastrointestinal tract.

Terms and Conditions of storage

The drug should be stored out of reach of children, dry, dark place. Shelf life - 2 years.

Artrodarin

Hard gelatin capsules, the size № 1, consisting of white opaque body and green opaque lids, the contents of capsules - granules are yellow and odorless.

1 capsule. diatserein 50 mg

Excipients: lactose monohydrate, croscarmellose sodium, povidone K30, colloidal silicon dioxide, magnesium stearate, indigotine (E132), iron oxide yellow (E172), titanium oxide (E171), gelatin.

Clinico-pharmacological group

The drug used in inflammatory and inflammatory-dystrophic diseases of the locomotor system.

Pharmacological action

Anti-inflammatory drug, an inhibitor of the synthesis and activity of interleukin-1 (IL-1). IL-1 plays an important role in the development of inflammation, degradation and the subsequent destruction of cartilage in osteoarthrosis.

In addition, diatserein inhibits the action of other cytokines that cause inflammation, including IL-6, TNF. Diatserein also slows down the formation of metalloproteases (collagenase, elastase), which are involved in the process of damaged cartilage. With prolonged use diatserein stimulates the synthesis of proteoglycans and does not affect the synthesis of prostaglandins.

Pharmacokinetics

Absorption and metabolism

After taking the drug inside diatserein rapidly absorbed from the gastrointestinal tract and fully deatsetiliruetsya to Reina. Acceptance of the drug simultaneously with food increases bioavailability by 25%. Reina Cmax in plasma is achieved through 144 min. In single dose of the drug in a dose of 50 mg Cmax reached 3.15 mg / liter. Repeatedly taking the drug Cmax Reina increases in relation to cumulation.

Distribution and excretion

Linking Reina albumin reaches almost 100%. Reina penetrates through the BBB and placental barrier. T1 / 2 is 255 min. Reina derived kidneys unchanged (20%) and glucuronide (60%) and sulfate (20%).

Indications for use of the drug
primary and secondary osteoarthritis.

Dosage regimen

The drug is usually prescribed 1 capsule 2 (morning and evening after meals).

The capsules should be swallowed whole without chewing, and wash down with water.

Effect of treatment should be expected in 2-4 weeks. Artrodarin designed for continuous long-term use or for the exchange rate of the duration of the course at least four months.

Side effect

If you are sensitive to the components of the drug possible allergic reactions of varying severity.

On the part of the digestive system: the initial period of therapy may include diarrhea, nausea, vomiting, abdominal pain. In this case the dose can be reduced to 1 capsule.

During the administration of the drug may be an intense staining of urine from yellow to brown (depending on pH), which does not require dose reduction (cancellation) of the drug.

Contraindications to the use of the drug
Pregnancy
lactation (breastfeeding);
childhood and adolescence (18 years);
individual intolerance to the components of the drug or hypersensitivity to antrahionovym drugs (such as a laxative).

Precautions designate patients with irritation of the lower intestine, chronic renal insufficiency.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

Application for violations of liver function

With caution is prescribed for chronic renal failure. With the deterioration of renal function the physician should reduce the dose of the drug.

Cautions

The duration of therapy depending on the result achieved can be lengthy.

To achieve the therapeutic effect Artrodarin ® should be administered in conjunction with analgesics and NSAIDs.

Against the background of the drug requires periodic monitoring of the pattern of peripheral blood and liver enzymes.

With the deterioration of renal function the physician should reduce the dose of the drug.

Overdose

Symptoms: diarrhea, weakness.

Treatment: symptomatic. Patients should be warned about the need to see a doctor in case of overdose.

Drug Interactions

Artrodarin should not be taken concurrently with substances that affect the quality of the intestinal contents and its rate of discharge (including a lot of fiber).

Antacids reduce the absorption of the drug.

With the simultaneous use of antibiotics or chemotherapy drugs that affect the intestinal microflora may increase the frequency of adverse reactions from the intestine.

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Drug prescription.

Terms and Conditions of storage

The drug should be stored protected from light and away from children at or above 25 ° C. Shelf life - 3 years.

Artra Chondroitin

Composition, structure and packing

Capsules are hard gelatin, opaque, from white to almost white; the contents of capsules - powder from white to almost white; exception of specific smell.

1 capsule. chondroitin sulfate sodium 250 mg - 500 mg - 750 mg.

Excipients: rice flour, silicon dioxide, magnesium stearate. The composition of the shell capsules: gelatin, titanium dioxide.

Clinico-pharmacological group: The drug that stimulates the regeneration of cartilage tissue.

Pharmacological action

Stimulator of regeneration of cartilage tissue. Influences on exchange processes in hyaline and fibrous cartilage, stimulates the biosynthesis of glycosaminoglycans. Slows bone resorption and reduces calcium loss, accelerates restoration of bone tissue.

Reduces degenerative changes and promotes the restoration of cartilage of joints, relieves pain in joints and spine, increases joint mobility, is involved in the formation of bone, ligament, maintaining firmness and elasticity of the vascular wall.

In the treatment of osteoarthritis relieves symptoms of the disease and reduces the need for NSAIDs. Slows bone resorption and reduces calcium loss, accelerates restoration of bone tissue. The therapeutic effect persists for a long time after treatment.

Pharmacokinetics

Absorption and distribution

Once inside more than 70% of chondroitin sulfate is absorbed from the gastrointestinal tract. Bioavailability is 13%. For a single ingestion of high therapeutic dose Cmax in plasma observed after 3-4 h, in the synovial fluid after 4-5 hours absorbed from the gastrointestinal tract drug accumulates in the synovial fluid.

Withdrawal

We derive the kidneys.

Statement
osteoarthritis of peripheral joints;
osteochondrosis of the spine.

Dosage regimen

The drug is prescribed into adults. Capsules 250 mg - 2 capsules. 2 times / day.

Capsules 500 mg - 1 capsule. 2 times / day.

Capsules 750 mg - 1-2 kaps. / day. The recommended duration of the initial course of treatment - 6 months. The period of the drug after its cancellation - 3-5 months.

Duration of repeated courses of treatment is established by a doctor individually.

Side effect

Rare: allergic reaction.

Contraindications
Hypersensitivity to the drug's components.

Pregnancy and lactation

Not advisable to appoint during pregnancy and lactation (breastfeeding) in the absence of clinical experience in this patient.

Cautions

Precautions should be prescribed to patients with bleeding, as well as patients with a tendency to bleeding.

Overdose

Cases of overdose are unknown.

Treatment: gastric lavage, the holding of symptomatic therapy.

Drug Interactions

With simultaneous application may gain indirect action of anticoagulants, antiplatelet agents, fibrinolytics. The product is compatible with NSAIDs and SCS.

Terms and Conditions of storage

The drug should be stored out of reach of children, dry place at temperatures from 10 ° to 30 ° C. Shelf life - 3 years.

Artra

Composition, structure and packing

Tablets, film-coated white to white with a yellowish tint, with splashes, oval, biconvex, engraved with "ARTRA" on the one hand, with a specific smell.

1 tab. chondroitin sulfate sodium 500 mg of glucosamine hydrochloride 500 mg.

Excipients: calcium sulfate, disodium, microcrystalline cellulose, sodium croscarmellose, stearic acid, magnesium stearate.

The composition of the shell: hydroxypropylmethylcellulose, titanium dioxide (E171), triacetin.

Clinico-pharmacological group: The drug that stimulates the regeneration of cartilage tissue.

Pharmacological action

Stimulator of regeneration of cartilage tissue. Glucosamine and chondroitin sulfate sodium involved in the biosynthesis of connective tissue, helping to prevent the destruction processes of cartilage, stimulating the regeneration of tissue. Introduction of exogenous glucosamine increases production of cartilage matrix and provides nonspecific protection, including of NSAIDs and the SCS.

The drug has mild anti-inflammatory action. Chondroitin sulfate sodium, regardless of whether it is absorbed in intact form or as individual components, serves as an additional substrate for the formation of healthy cartilage matrix.

It stimulates the formation of proteoglycans and collagen type II, and also protects the cartilage matrix by enzymatic cleavage (by suppressing the activity of hyaluronidase) and from the damaging effect of free radicals, maintains the viscosity of synovial fluid, stimulates cartilage repair mechanisms and inhibits the activity of those enzymes (elastase, hyaluronidase), which break down cartilage.

In the treatment of osteoarthritis relieves symptoms of the disease and reduces the need for NSAIDs.

Pharmacokinetics

Absorption

Bioavailability of glucosamine ingestion - 25% (due to the effect of "first pass" through the liver). Bioavailability of chondroitin sulfate - 13%.

Distribution

Distributed in the tissues: highest concentrations of glucosamine found in the liver, kidneys and articular cartilage. About 30% of applied dose long persist in bone and muscle tissue.

Withdrawal

Glucosamine is derived mainly from the urine in unchanged form, in part - with the feces. T1 / 2 of glucosamine - 68 pm

Statement
osteoarthritis of peripheral joints and spine.

Dosage regimen

Into adults and children over 15 years appoint 1 tab. 2 times / day during the first three weeks of 1 tablet. 1 time per day over the next weeks and months. Sustained therapeutic effect is achieved while taking the drug for at least 6 months.

Side effect
On the part of the digestive system: lung dysfunction GIT - epigastric pain, flatulence, diarrhea, constipation (due to the action of glucosamine).
From the side of the central nervous system: dizziness (due to the action of glucosamine).
Other: allergic reactions (caused by the action of glucosamine and chondroitin sulfate).

Contraindications
marked impairment of renal function;
Hypersensitivity to the drug's components.

Precautions are used for bleeding or bleeding tendency, bronchial asthma, diabetes.

Pregnancy and lactation

Artro drug is not recommended during pregnancy and during lactation.

Application for violations of renal function

The drug is contraindicated in disturbancies renal function.

Cautions

Use in Pediatrics

Clinical data on efficacy and safety of the drug arthritis in children aged under 15 years of absence.

Overdose

So far, cases of overdosing Artro not reported.

Treatment: gastric lavage, symptomatic therapy.

Drug Interactions

When applied simultaneously increases the effects of anticoagulants and antiplatelet agents. Increases absorption of tetracycline reduces the effect of semisynthetic penicillins. The product is compatible with the SCS.

Terms and Conditions of storage

The drug should be stored out of reach of children, dry place at temperatures from 10 ° to 30 ° C. Shelf life - 5 years.

Artezine

Composition, structure and packing

Tablets are white or white with kremovatym color ploskotsilindricheskie, with bevel.

1 tab. doxazosin mesilate 1.22 mg, which corresponds to the content of doxazosin 1 mg.

Excipients: potato starch, lactose, microcrystalline cellulose, povidone (kollidon 25), colloidal silicon dioxide (aerosil), sodium lauryl sulfate, magnesium stearate.

Tablets are white or white with kremovatym color ploskotsilindricheskoy form.

1 tab. doxazosin mesilate 2.44 mg, which corresponds to the content of doxazosin 2 mg.

Excipients: potato starch, lactose, microcrystalline cellulose, povidone, colloidal silicon dioxide (aerosil), sodium lauryl sulfate (sodium dodecyl sulphate), magnesium stearate.

Tablets are white or white with kremovatym color.

1 tab. doxazosin (via mesylate) 4 mg.

Excipients: lactose, potato starch, povidone (kollidon 25), magnesium stearate, krospovidon.

Clinico-pharmacological group: alpha 1-blocker. Antihypertensives.

The drug, used in violation of urination in benign prostatic hyperplasia.

Pharmacological action

Selective competitive antagonist of postsynaptic α1-adrenergic receptors. By reducing the muscle tone of vessels doxazosin reduces TPVR, which leads to a decrease in blood pressure. After a single dose of the drug the maximum reduction in blood pressure observed during the 2-6 hours hypotensive effect persists for 24 hours

During treatment with Artezin hypertensive patients with no difference between the values of BP in the standing position and lying. Effective with hypertension, including accompanied by metabolic disorders (obesity, reduced glucose tolerance). Reduces the risk of CHD. Acceptance of the drug in "normotensive" not accompanied by a reduction in BP. With prolonged use Artezina patients no change of tolerance to the therapeutic antihypertensive effect. During treatment Artezinom decrease triglycerides and total cholesterol in blood plasma. At the same time has been an increase (at 4-13%) ratio of HDL / total cholesterol.

Prolonged use of the drug observed regression of left ventricular hypertrophy, the suppression of platelet aggregation and increased content in the tissues of active plasminogen.

Due to the fact that doxazosin blocks α1-adrenergic receptors located in the stroma and capsule of the prostate and bladder neck, a decrease in resistance and pressure in the urethra, reducing the resistance of internal sphincter, which in turn leads to significant improvement in urodynamic parameters and reduce the symptoms of benign prostatic hyperplasia. The drug is effective in 66-71% of patients, stable clinical effect develops after 1-2 weeks of treatment, the maximum effect - in 14 weeks. The effect persists for a long time.

Pharmacokinetics

Absorption and distribution

After oral administration in therapeutic doses of doxazosin is well absorbed from the gastrointestinal tract. Absorption - 80-90%. Simultaneous food intake delays absorption. Time to reach Cmax - 3 hours, at the Gala Dinner - 5 pm Bioavailability - 60-70%. Linking to plasma proteins - about 98%.

Metabolism

Actively metabolized in the liver by O-demethylation and hydroxylation.

Withdrawal

Withdrawal of blood plasma occurs in 2 phases with the final T1 / 2 - 19-22 h, which allows you to assign a drug once a day. Eliminated through the intestines, primarily in the form of metabolites. Urinary recovery of about 10%, 5% - unchanged.

Pharmacokinetics in special clinical situations

In patients with impaired liver function, as well as when taking drugs that affect liver metabolism, may be in breach of the biotransformation doxazosin. Pharmacokinetic studies with doxazosin in elderly patients and patients with kidney disease did not reveal any significant pharmacokinetic characteristics.

Statement
hypertension (as monotherapy or in combination with other antihypertensive therapy / thiazide diuretics, beta-blockers, calcium channel blockers slow or ACE inhibitors /).
benign prostate hyperplasia (as in the presence of arterial hypertension and normal blood pressure).

Dosage regimen

The drug is prescribed inside 1 time / day (morning or evening), regardless of the meal, without chewing, and drinking plenty of water. When hypertension initial daily dose is 1 mg at bedtime. After the first dose the patient should be in bed for 6-8 hours is necessary due to the possibility of "first dose phenomenon", especially against the background of previous diuretic usage.

In case of insufficient therapeutic effect after 1-2 weeks the daily dose can be increased to 2 mg. Thereafter every 1-2 weeks can increase the dose of 2 mg. In most patients the optimal therapeutic effect is achieved at a daily dose of 8 mg. The maximum daily dose - 16 mg. After reaching a stable therapeutic effect of the dose is usually lower (average therapeutic dose for maintenance therapy is usually equal to 4.2 mg / day).

In benign prostatic hyperplasia Artezin appointed at the initial dose of 1 mg / day.

If necessary, dose increased to 2.4 mg / day. The maximum daily dose - 8 mg. The duration of treatment determines the physician.

Side effect
Since the cardiovascular system: orthostatic hypotension, fainting - a phenomenon first dose, edema, tachycardia, arrhythmia.
From the central nervous system and peripheral nervous system: dizziness, headache, insomnia, asthenia, abnormal sleepiness, impaired cerebral circulation.
On the part of the digestive system: dry mouth, dyspepsia, increased activity of hepatic transaminases, cholestasis, hepatitis, jaundice, constipation.
On the part of the respiratory system: dyspnea, rhinitis, nasal bleeding.
From the senses: blurred vision.
The part of the hemopoietic system: thrombocytopenia, thrombocytopenic purpura, leukopenia.
From the urinary system: polyuria, haematuria, rarely - urinary incontinence. Allergic reactions: skin rash, hives, itching.

Other: weakness, chest pain and / or back, seldom - priapism.

Contraindications
Hypersensitivity to the drug's components;
Hypersensitivity to derivatives quinazolone;
tablet 2 mg and 4 mg: children's age (efficacy and safety have not been established).

With care use in patients with aortic and mitral stenosis, orthostatic hypotension, abnormal liver function (including with liver failure), pregnancy and during breastfeeding, in the form of tablets 1 mg - in children and adolescents under age 18 years.

Pregnancy and lactation

The drug can be given during pregnancy and during breast-feeding only after careful assessment of the expected benefit of therapy for the mother and the possible risk to the fetus or infant.

Application for violations of liver function

With care use in patients with disorders of liver function.

Application for violations of renal function

Pharmacokinetic studies with doxazosin in patients with kidney disease did not reveal any significant pharmacokinetic differences.

Cautions

"The phenomenon of the first dose, especially pronounced on the background of the previous admission of diuretics and diet with restriction of sodium. Particular caution should be exercised in the appointment of the drug to patients with hepatic impairment, especially in those cases when they are used drugs that can adversely affect liver function. In cases of deterioration of functional liver drug should be abolished.

In order to prevent orthostatic reactions patients should avoid sudden and sharp changes in body position (the transition from the supine position to standing position). Before starting therapy it is necessary to exclude malignant tumor of the prostate.

Using alcohol can increase adverse reactions. Effects on ability to drive vehicles and management mechanisms

Due to the fact that the drug can cause orthostatic response at the beginning of treatment or during the period of increasing doses of appropriate patients to refrain from any potentially dangerous activities, in particular from management and other motor vehicles and machinery. Overdose Symptoms: marked reduction of blood pressure, sometimes accompanied by fainting.

Treatment: the patient should be given a horizontal position with legs elevated. Spend symptomatically. Hemodialysis is ineffective.

Drug Interactions

Doxazosin enhances the hypotensive effect of antihypertensive agents (when used in combination require dosage adjustment). There was no adverse interaction with the simultaneous use of doxazosin and antibiotics, oral hypoglycemic means of indirect anticoagulants and urikozuricheskih funds. The drug has no effect on the degree of plasma protein binding of digoxin and phenytoin.

When applied simultaneously with inducers of microsomal oxidation enzymes in the liver may reduce the effectiveness of doxazosin, with inhibitors - improvement.

Cimetidine increases the AUC doxazosin. NSAIDs (especially indomethacin), estrogens (fluid retention), and sympathomimetic drugs can reduce the hypotensive effect of doxazosin. By eliminating the alpha-adrenostimuliruyuschie effects of epinephrine, doxazosin can cause tachycardia and arterial hypotension.

Terms and Conditions of storage

List B. The drug should be stored in a dry, protected from light and away from children at or above 25 ° C. Shelf life - 3 years.

Arpenal tablets 0.05 g

Method of production - tablets (banks) 50 mg

Pharmacotherapeutic group - antispasmodic

Pharmacological action
m-and n-anticholinergic
spasmolytic

Ingredients - arpenal 50 mg, excipients (lactose, starch, talc, calcium stearate)

Statement
Gastrojejunal ulcer
Pain in the abdomen and pelvis
Pain localized in the upper abdomen
Pain localized to other areas of the lower abdomen
Secondary parkinsonism
Pilorospazm, not elsewhere classified
Renal colic, unspecified
Peptic ulcer unspecified localization
Other diseases of stomach and duodenum
Other and unspecified abdominal pain
Cholelithiasis
Duodenal ulcer
Gastric ulcer

The composition of the components
arpenal
lactose
calcium stearate
starch
talc

Description

White crystalline powder. Very easily soluble in water, soluble in alcohol. Aqueous solutions of hydrolyzed during storage. The structure is very close to spazmolitinu.

Pharmacodynamics

Is an antagonist of M-cholinergic receptors and a little more N-cholinergic receptors. Along with the peripheral has a moderate central holinoliticheskoe action. Also has direct spasmolytic (papaverinopodobnoe) effect on smooth muscles.

Application

Applied pilorospazme, gastric ulcer and duodenal ulcer, hepatic and renal colic. In connection with the central cholinolytic effect can be used in parkinsonism. Applied also to decrease the muscle tone in spastic paresis pyramid of different origin (in the recovery period).

Dosage regimen

Assign inside (after eating) for 0,05-0,1 g 2-4 times a day. The course of treatment an average of 3-4 weeks.

Side effects

In case of overdose can appear dizziness, headache, feeling of intoxication (in conjunction with central action), dry mouth (due to peripheral cholinolytic action), breach of accommodation. By providing an irritating effect on the gastric mucosa, spazmolitin may cause dyspeptic symptoms. The feeling of intoxication and dizziness can prevent or reduce the appointment of caffeine (0,1-0,2 g kofeinbenzoata sodium inward or 1 ml of 20% solution under the skin).

Contraindications

Glaucoma.

Aronar

Composition, structure and packing

Tablets are white or white with kremovatym color ploskotsilindricheskie, with beveled and risks.

1 tab. amlodipine (in the form bezilata) 5 mg.

Excipients: microcrystalline cellulose, potato starch, lactose monohydrate, calcium hydrogen phosphate dihydrate, croscarmellose sodium, magnesium stearate, aerosil (colloidal silicon dioxide).

Clinico-pharmacological group: Calcium channel blockers.

Pharmacological action

Blocker "slow" calcium channels from the group dihydropyridine derivatives. Antihypertensive and antianginal effects. Blocks the flow of calcium ions across cell membranes in smooth muscle cells of blood vessels and myocardium.

Mechanism of antihypertensive action is due to the direct relaxing effect on smooth muscles of blood vessels. Antianginal effect of the drug due to its ability to expand the peripheral arterioles, which leads to a decrease in TPVR, a reduction in afterload leads to a decrease in myocardial oxygen demand. In addition, amlodipine increases coronary arteries and arterioles, which leads to an increase in the supply of oxygen to the myocardium (the mechanism is particularly important when angiospastic angina). Amlodipine has no adverse effect on metabolism and lipid content of blood plasma, has antiateroskleroticheskoy, antithrombotic activity, increases the glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria.

Pharmacokinetics

Absorption

If ingestion is absorbed from the gastrointestinal tract, slowly and almost completely (90%). Cmax plasma levels achieved within 6-12 hours Bioavailability - 60-65%.

Distribution

Css achieved after 7-8 days of continuous use. Relationship to plasma proteins - more than 95%. Vd - about 20 l / kg. It penetrates through the blood-brain barrier, is excreted in breast milk. Metabolism Biotransformiruetsya mainly in the liver with the formation of inactive metabolites.

Withdrawal

T1 / 2 - 35-45 hours, which allows you to assign it 1 time / day. Less than 10% accepted oral dose excreted unchanged in about 60% excreted in the urine as inactive metabolites, 20-25% of output in the form of metabolites with bile and feces.

Pharmacokinetics in special clinical situations

T1 / 2 in arterial hypertension can increase up to 48 hours in elderly patients - up to 65 h, with liver problems - up to 60 hours in case of breach of kidney function - does not change.

Statement
hypertension (as monotherapy and as part of combination therapy);
Stable angina;
angiospastic angina (Prinzmetal angina).

Dosage regimen

When hypertension Aronar administered in an initial dose of 2.5 mg / d for the prevention of angina attacks - 5 mg / day. The recommended maintenance dose in arterial hypertension and angina - 5 mg / day. If necessary, the daily dose may be increased to 10 mg. Do not exceed the recommended initial daily dose in patients with impaired liver function, elderly patients and patients with reduced body weight. The maximum daily dose - 10 mg.

With simultaneous use of thiazide diuretics, beta-blockers or ACE inhibitors correct dosing regimen Aronara not required. Patients with impaired renal function correct dosing regimen is also not required.

Side effect
Since the cardiovascular system: heart rate, shortness of breath, excessive lowering of blood pressure, syncope, vasculitis, edema ankles and feet, facial flush, rarely, cardiac arrhythmias - (bradycardia, ventricular tachycardia, atrial flutter), chest pain, orthostatic hypotension, in rare cases - the development or worsening symptoms of heart failure, arrythmia, migraines.
From the central nervous system and peripheral nervous system: dizziness, headache, drowsiness, fatigue, rarely - asthenia, mood changes, seizures, visual disturbances, paresthesia, tinnitus.
On the part of the musculoskeletal system: rarely - arthralgia, arthrosis, myalgia (with prolonged use), in isolated cases - myasthenia gravis.
On the part of the digestive system: dyspepsia, nausea, abdominal pain, rarely - increased activity of hepatic transaminases, jaundice (caused by cholestasis), gingival hyperplasia, pancreatitis, taste perversion, dry mouth, changes in bowel movements.
Dermatological reactions: skin rash, itching, rarely - erythema multiforme, skin discoloration, dermatitis.
From the urinary system: rarely - thamuria, tenesmus, nocturia, in rare cases - dysuria, polyuria.
On the part of the hemopoietic system: rarely - thrombocytopenia, leukopenia.
Other: rarely - gynecomastia, violation of sexual function (including reduction of potency), the increase / decrease in body weight, hyperglycemia, conjunctivitis, eye pain, nosebleeds, increased sweating, thirst.

Contraindications
hypotension;
tachycardia
collapse;
cardiogenic shock;
aortic stenosis;
mitral stenosis;
childhood and adolescence to 18 years;
Hypersensitivity to amlodipine and other derivatives of dihydropyridine.

Precautions should be prescribed drug in violation of liver and kidney function, chronic heart failure, III and IV functional class (classification NYHA), SSS, and mild to moderate hypotension, hypertrophic obstructive cardiomyopathy during the acute phase of myocardial infarction, diabetes, disorders lipid metabolism, in elderly patients.

Pregnancy and lactation

Application Aronara during pregnancy and lactation is possible only when the intended benefits to the mother outweighs the potential risk to the fetus or baby (due to lack of reliable clinical data supporting the safety of the drug in these periods).

If necessary, the appointment Aronara during lactation should decide the issue of termination of breastfeeding.

Application for violations of liver function

Precautions should be prescribed the drug in violation of liver function.

Application for violations of renal function

Precautions should be prescribed the drug in violation of renal function.

Cautions

During the administration of the drug requires monitoring of body weight, diet (especially limiting sodium intake), the maintenance of oral hygiene and regular dental visits (to prevent soreness, bleeding and gingival hyperplasia). Care should be exercised in appointing Aronara elderly patients, especially with increasing dose. Despite the absence of a drug withdrawal syndrome upon termination of treatment Aronarom recommend a gradual reduction in dose. Appointment Aronara not affect the plasma concentrations of potassium, glucose, triglycerides, total cholesterol, LDL, uric acid, creatinine and urea nitrogen.

Possible joint use Aronara with thiazide diuretics, alpha-and beta-blockers, ACE inhibitors, nitrates (including prolonged), NSAIDs, antibiotics, oral hypoglycemic drugs.

Use in Pediatrics

Safety and effectiveness in pediatric practice Aronara not installed. Effects on ability to drive vehicles and management mechanisms have been no reports on the impact Aronara on ability to drive a car or operate machinery.

Nevertheless, some patients, mainly at the beginning of treatment, there may be drowsiness and dizziness. When they occur, the patient must observe special precautionary measures while driving and using machinery.

Overdose

Symptoms: marked reduction of blood pressure, tachycardia, excessive peripheral vasodilatation.

Treatment: gastric lavage, activated charcoal appointment, the patient should be given to a horizontal position with legs raised, hold the control performance of the heart and lungs, BCC, diuresis, carry out activities aimed at maintaining the function of the cardiovascular system. To restore the tone of the vessels used vasoconstrictive drugs (in the absence of contraindications to their use) to eliminate the effects of calcium channel blockade in / injected calcium gluconate. Hemodialysis is ineffective.

Drug Interactions

With simultaneous use of thiazide and loop "diuretics, beta-blockers, verapamil, ACE inhibitors and nitrates increase antianginal and antihypertensive effects Aronara.

At simultaneous application with Aronarom inhibitors of microsomal liver enzymes increase the concentration of amlodipine in plasma, increasing the risk of side effects, and inducers of microsomal liver enzymes - reduce its concentration. The simultaneous use of Aronara and digoxin did not change the concentration in serum and renal clearance of digoxin.

Joint application Aronara and cimetidine does not alter the pharmacokinetics of amlodipine.

The simultaneous use Aronara not significantly modify the effect of warfarin on prothrombin time in healthy male volunteers. Antihypertensive effect Aronara weaken NSAIDs, especially indomethacin (there is a delay of sodium and blocking the synthesis of prostaglandins by the kidneys), as well as sympathomimetic and estrogens (cause sodium retention). When the joint application of funds for inhalation anesthesia (derivatives of hydrocarbons), amiodarone, quinidine may increase the hypotensive effect Aronara.

When combined with the use of lithium therapy may be a manifestation of neurotoxicity.

Terms and Conditions of storage

List of BN drug should be stored in a dry place protected from light, out of reach of children. Shelf life - 2 years.

Aromasin

Composition, structure and packing

Tablets are coated with sugar coat white or white with a grayish tint, round, biconvex, marked "7663" on one side, executed in black paint.

1 tab. eksemestan 25 mg.

Excipients: mannitol, gipromelloza, polysorbate 80, krospovidon, silicon dioxide colloidal hydrated, microcrystalline cellulose, sodium karboksimetilkrahmal, magnesium stearate. Composition of sugar-shell: gipromelloza, simetikonovaya emulsion, macrogol 6000, magnesium carbonate, titanium dioxide, methyl-p-hydroxybenzoate, polyvinyl alcohol, sucrose.

Clinico-pharmacological group: The antitumor drug. Aromatase inhibitors.

Pharmacological action

The irreversible steroidal aromatase inhibitor, similar in structure to the natural substance androstenedione. In postmenopausal women estrogens are produced mainly by converting androgens to estrogens under the action of the enzyme aromatase in peripheral tissues.

Blocking formation of estrogens by inhibiting aromatase is an effective and selective treatment for hormone breast cancer in postmenopausal women. The mechanism of action of the drug Aromazin due to the fact that it irreversibly binds to the active fragment of the enzyme, causing its inactivation.

In postmenopausal women Aromazin significantly reduces the concentration of estrogen in the blood serum, starting with a dose of 5 mg, with the maximum reduction (> 90%) is achieved at doses of 10-25 mg. Patients diagnosed with postmenopausal breast cancer, treated with 25 mg of the drug on a daily basis, the overall level of the enzyme aromatase in the body decreased by 98%. Eksemestan not possess progestogenic and estrogenic activity. Showed only a slight androgenic activity, mainly when used in high doses. Aromazin no effect on the biosynthesis of cortisol and aldosterone in the adrenal glands, which confirms the selectivity of the drug.

In this regard, there is no need for substitution treatment of glucocorticoid and mineralocorticoid. In applying the drug, even at low doses there is a slight increase in levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in serum, which is characteristic of drugs of this pharmacological group, and probably developed on the basis of feedback at the level of the pituitary: decrease the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland and also in postmenopausal women.

Pharmacokinetics

Absorption

Once inside eksemestan rapidly absorbed, mainly from the gastrointestinal tract. Absolute bioavailability is not installed. It is believed that it is limited by extensive first-pass effect through the liver. In single dose of the drug in a dose of 25 mg Cmax in plasma was 17 ng / ml achieved after 2 h. Simultaneous ingestion increases bioavailability by 40%. Pharmacokinetic parameters eksemestana are linear.

Distribution

Relationship to plasma proteins - approximately 90%. Eksemestan and its metabolites do not bind to erythrocytes. If readmission unpredictable cumulation eksemestana not observed.

Metabolism

The process of biotransformation eksemestana effected by oxidation of methylene groups in position 6 under the action of isoenzyme SYR3A4 and / or restoration of 17-keto group under the action of aldoketoreduktazy with subsequent conjugation. Products of metabolism eksemestana either inactive or less active in respect of inhibition of aromatase than the parent compound.

Withdrawal

Final T1 / 2 approximately 24 hours approximately equal amounts of eksemestana (40%) excreted in the urine and feces for a week. From 0.1 to 1% excreted in the urine in unchanged form.

Pharmacokinetics in special clinical situations

Relation between the systemic impact of the drug and the age is not established. In patients with renal failure severe (CC <30 ml / min) systemic exposure eksemestana 2 times higher, but dose adjustment is required. In patients with moderate or severe hepatic insufficiency systemic exposure eksemestana 2-3 times higher, but dose adjustment is required.

Statement
common breast cancer in women with natural or induced postmenopausal women with disease progression on a background Antiestrogenic therapy, as well as with the progression of the disease after repeated application of different types of hormone replacement therapy;
adjuvant therapy for early breast cancer in postmenopausal women with estrogen-receptor positive or unknown receptor status, after 2 or 3 years of initial adjuvant therapy with tamoxifen, to reduce the risk of recurrence (distant or regional), as well as contralateral breast cancer .

Dosage regimen

Assign inside. For adults and elderly patients the recommended dose is 25 mg 1 time / day, preferably after a meal. In early breast cancer treatment drug is recommended to continue for as long as the total duration of sequential adjuvant hormonal therapy did not reach 5 years.

Treatment of patients with advanced cancer of the breast long. If signs of progression of a tumor or when the contralateral breast cancer treatment Aromazinom should be discontinued. When hepatic or renal failure dose adjustment is required. Do not use the drug in children.

Side effect

Adverse effects associated with use of the drug in a dose of 25 mg / day were minor to moderate. The following adverse reactions, divided by the body's systems and frequency: very frequent (> 10%), frequent (> 1%, <10%),> 0.1%, <1%),> 0.01%, <0 , 1%).

On the part of the digestive system: very often - nausea, often - anorexia, abdominal pain, vomiting, constipation, indigestion and diarrhea.

From the central and peripheral nervous system: very often - insomnia, headache, and often - depression, dizziness, carpal tunnel syndrome.

Since the cardiovascular system: very often - the tides. Dermatological reactions: very often - sweating, often - a rash, alopecia.

On the part of the musculoskeletal system: very often - articular and musculoskeletal pain.

Other: very often - fatigue, often - the pain of unspecified location, peripheral edema, or swelling feet. Approximately 20% of patients (especially patients with an initial lymphopenia) were observed periodically reduce the number of lymphocytes.

However, the average number of lymphocytes in these patients over time has not significantly changed, and the concomitant increase in the incidence of viral infections were observed. Sometimes the observed increase in liver enzymes and alkaline phosphatase, primarily in patients with liver metastases and the bone, as well as the presence of other hepatic lesions (not determined whether these changes to the drug intake or not).

Contraindications
premenopauzny endocrine status;
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to eksemestanu or to any other component of the drug.

With care use in patients with abnormal liver function or kidney.

Pregnancy and lactation

Aromazin contraindicated during pregnancy and lactation.

Application for violations of liver function

When liver failure dose adjustment is required. With care use in patients with abnormal liver function.

Application for violations of renal function

In renal insufficiency, dose adjustment is required. Precautions should be used drug in violation of renal function.

Cautions

Aromazin should not be given to women with premenopauznym endocrine status, therefore, in those cases where it is clinically justified, postmenopauzny status should be acknowledged definition of the level of LH, FSH and estradiol. Aromazin should not be given concurrently with any medication containing estrogen.

Effects on ability to drive vehicles and management mechanisms

Patients should be warned of the emergence during treatment Aromazinom somnolence, asthenia and dizziness. If you experience these symptoms for patients to refrain from driving lessons and other potentially hazardous activities that require high concentration and speed of psychomotor reactions.

Overdose

A single dose of the drug, which could cause a life-threatening symptoms that are not installed. Application eksemestana a single dose of 800 mg in healthy women and in a daily dose of 600 mg in postmenopausal women with advanced breast cancer is well tolerated.

Treatment: No specific antidotes. If necessary, carry out palliative care, as well as regular monitoring of vital functions and closely monitored.

Drug Interactions

Preparations containing estrogens, while the use of Aromazinom completely negate its pharmacological action. Eksemestan undergoes metabolism under the influence of CYP3A4 and aldoketoreduktaz and did not inhibit any of the major isoenzymes of CYP.

Specific inhibition of CYP3A4 ketoconazole had no significant effect on the pharmacokinetics eksemestana. Despite the established pharmacokinetic interaction eksemestana with rifampicin, a strong inducer of CYP3A4, pharmacological activity Aromazina (suppression of estrogen) remains unchanged, so dose adjustment is required.

Terms and Conditions of storage

List B. The drug should be stored at temperatures not above 30 ° C in the reach of children. Shelf life - 3 years. The drug should not be used beyond the expiration date indicated on the package.

Armanor

Composition, structure and packing

Tablets, coated in white, oblong, with notches on both sides.

1 tab. almitrina bismezilat 50 mg.

Excipients: corn starch, corn starch, gelled, lactose monohydrate, sodium lauryl sulfate, titanium dioxide, macrogol 6000, povidone, magnesium stearate, talc, white beeswax, glycerol, gipromelloza.

Clinico-pharmacological group: Respiratory analeptic.

Pharmacological action

Peripherals respiratory analeptic. Due to stimulation of peripheral chemoreceptors located in the aorta and carotid arteries, the leveling of ventilation-perfusion ratio, ie increase in oxygen pressure in the blood and decrease carbon dioxide tension (increase in SaO2 and PaO2, decrease PaCO2). These effects combined with the improvement of alveolar ventilation, observed during long-term use of the drug, which contributes to a general improvement in gas exchange function.

In applying the drug in doses of 50-100 mg / day observed effects do not depend on any change of ventilation in general, at that point: the absence of any change of indicators defined in the standard functional tests (vital capacity, respiratory rate, O2 consumption), reduction hypoxemia after taking into Armanora in patients with acute decompensation of respiratory function, located on the prolonged mechanical ventilation.

Pharmacokinetics

Absorption

When administered almitrin rapidly absorbed, Cmax in plasma obtained after 3 h after administration.

Distribution

The degree of binding to proteins in blood almitrina high - over 99%. Metabolism is mainly metabolized in the liver.

Withdrawal

Withdrawal of the drug occurs mainly in the faeces, to a lesser extent - in the urine in the form of inactive metabolites. After receiving a single T1 / 2 of 40-80 h, when re-admission - 30 days.

Statement
respiratory failure with hypoxemia with chronic obstructive pulmonary disease (COPD).

Dosage regimen

The drug is intended only for the treatment of adults. Assign inside of 1-2 tab. / day (50-100 mg / day) in 2 divided doses during the main meal. For a single ingestion Armanora in doses exceeding 100 mg may be transient moderate increase in overall ventilation, which can cause poor tolerance to the drug. Patients weighing 50 kg should be administered for 1 tab. / day.

After an initial period of treatment for 3 months at a dose of 50-100 mg switching to maintenance therapy on the scheme: 1 month break - 2 months of treatment.

If necessary, may require dosage adjustment based on patient weight, tolerance to the drug and the severity of the disorder of gas exchange. Due to the fact that almitrin not displayed by the kidneys, patients with renal insufficiency does not require correction of dosing regimen.

Side effect
On the part of metabolism: rarely - weight loss.
From the side of the central nervous system and peripheral nervous system: rarely - sleep disturbance (insomnia), sleepiness, agitation, anxiety, dizziness, prolonged use (over 1 year and over) - peripheral neuropathy with paresthesias of the lower extremities.
On the part of the digestive system: rarely - nausea, heartburn, feeling of heaviness in the epigastrium, indigestion, disorders of the chair.
Since the cardiovascular system: rarely - heartbeat.
On the part of the respiratory system: rarely - a subjective feeling of conscious breathing movements.

Contraindications
severe liver disease;
peripheral neuropathy or peripheral neuropathy cases in history;
Pregnancy
breastfeeding;
Hypersensitivity to the drug.

Pregnancy and lactation

Contraindicated during pregnancy and during breastfeeding.

Application for violations of liver function

If you have severe liver disease in the case of the need for drug therapy Armanor requires careful monitoring of clinical and laboratory parameters. The drug is contraindicated in hepatic failure.

Application for violations of renal function

Due to the fact that almitrin not displayed by the kidneys, patients with renal insufficiency does not require correction of dosing regimen.

Cautions

Armanor can be assigned in conjunction with oxygen therapy. Armanor should not be taken with other medications containing almitrin. Dosage regimen and treatment should be reviewed every 6 months. Therapeutic drug Armanor should be terminated in the following cases:
with a decrease in body weight by more than 5% of the original;
in the presence of sustained lower extremity paresthesias (sensation of tingling, numbness).

If you have severe liver disease in the case of the need for drug therapy Armanor requires careful monitoring of clinical and laboratory parameters. In connection with the presence of lactose drug is not recommended for patients taking the drug with congenital galactosemia, glucose and galactose malabsorption syndrome and lactase deficiency.

Use in Pediatrics

Due to the lack of sufficient clinical data to use the drug Armanor patients under the age of 18 years is not recommended.

Overdose

There have been no cases of overdose.

Symptoms: When you receive a random almitrina in excessive doses may cause hypocapnia with the development of respiratory alkalosis.

Treatment: symptomatic therapy under the control of lung function, heart and blood gases.

Drug Interactions

Armanor should not be taken with other medications containing almitrin.

Terms and Conditions of storage

Special storage conditions required. Keep out of reach of children. Shelf life - 4 years.

Arlet

Composition, structure and packing

Tablets, film-coated white or almost white, oblong.

1 tab. amoxicillin (in the form of trihydrate) 250 mg Clavulanic acid (in the form of potassium salt) 125 mg.

Excipients: povidone (polyvinylpyrrolidone), talc, starch 1500, calcium stearate, colloidal silicon dioxide (aerosil), microcrystalline cellulose.

The composition of the shell: gipromelloza (oksipropilmetiltsellyuloza), propylene glycol, titanium dioxide, macrogol 4000 (polyethylene 4000).

Tablets, film-coated white or almost white, oblong.

1 tab. amoxicillin (in the form of trihydrate) 500 mg Clavulanic acid (in the form of potassium salt) 125 mg.

Excipients: povidone (polyvinylpyrrolidone), talc, starch 1500, calcium stearate, colloidal silicon dioxide (aerosil), microcrystalline cellulose. The composition of the shell: gipromelloza (oksipropilmetiltsellyuloza), propylene glycol, titanium dioxide, macrogol 4000 (polyethylene 4000).

Tablets, film-coated white or almost white, oblong.

1 tab. amoxicillin (in the form of trihydrate) 875 mg Clavulanic acid (in the form of potassium salt) 125 mg.

Excipients: povidone (polyvinylpyrrolidone), talc, starch 1500, calcium stearate, colloidal silicon dioxide (aerosil), microcrystalline cellulose. The composition of the shell: gipromelloza (oksipropilmetiltsellyuloza), propylene glycol, titanium dioxide, macrogol 4000 (polyethylene 4000).

Clinico-pharmacological group: Antibiotic penicillin group broad-spectrum beta-lactamase inhibitor.

Pharmacological action

Broad-spectrum antibiotic, contains a semisynthetic penicillin, amoxicillin and irreversible inhibitor of β-lactamases clavulanic acid. Clavulanic acid provides a stable inactivated complex with these enzymes and provides stability to the effects of amoxicillin β-lactamase produced by microorganisms. Clavulanic acid, similar to the structure of β-lactam antibiotics, has its own weak antibacterial activity.

The drug has broad spectrum antibacterial action. Active against susceptible to amoxicillin strains, including strains producing β-lactamases: aerobic Gram-positive bacteria - Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus bovis, Staphylococcus aureus (except methicillin-resistant strains), Staphylococcus epidermidis (except methicillin-resistant strains ), Staphylococcus saprophyticus, Listeria spp., Enterococcus spp.; aerobic gram-negative bacteria - Bordetella pertussis, Brucella spp., Campylobacter jejuni, Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae, Haemophilus ducreyi, Klebsiella spp., Moraxella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella multocida, Proteus spp., Salmonella spp., Shigella spp., Vibrio cholerae, Yersinia enterocolitica, Helicobacter pylori, Eikenella corrodens; anaerobic Gram-positive bacteria - Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Actinomyces israelii, Fusobacterium spp ., Prevotella spp.; anaerobic Gram-negative bacteria - Bacteroides spp.

Pharmacokinetics

The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar.

Absorption

After taking the drug inside the two components are well absorbed from the gastrointestinal tract, food intake does not affect the degree of suction. Cmax in plasma obtained 1 h after drug administration and is (depending on dose) for amoxicillin 3-12 ug / ml for clavulanic acid - about 2 ug / ml.

Distribution

Both components are characterized by good volume distribution in body fluids and tissues (including lungs, middle ear, pleural and peritoneal fluid, uterus, ovaries). Amoxycillin penetrates well into synovial fluid, liver, prostate gland, palatine tonsils, muscle, gall bladder, the secret of the paranasal sinuses, saliva, bronchial secretion. Amoxicillin and Clavulanic acid does not penetrate the BBB under nevospalennyh mater.

The active substances penetrate the placenta and in trace concentrations excreted with breast milk. The degree of binding to plasma proteins is low. Metabolism Amoxicillin partially metabolized Clavulanic acid is exposed, apparently, metabolic rate.

Withdrawal

Amoxicillin is displayed by the kidneys virtually unchanged by tubular secretion and glomerular filtration. Clavulanic acid is obtained by glomerular filtration and partly in the form of metabolites. Smaller quantities can be displayed through the intestines and lungs. T1 / 2 of amoxicillin and clavulanic acid - 1-1.5 hours

Pharmacokinetics in special clinical situations

In severe renal insufficiency T1 / 2 increases to 7.5 h for amoxicillin and up to 4.5 h for clavulanic acid. Both components are removed by hemodialysis and small amounts - peritoneal dialysis.

Statement

Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
infections of the upper respiratory tract and ENT-organs (including acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis);
Infection of lower respiratory tract (including acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia);
urinary tract infections;
gynecological infections;
infections of skin and soft tissues;
infection of bone and connective tissue;
biliary tract infections (cholecystitis, cholangitis);
odontogenic infection.

Dosage regimen

Adults and children over 12 years (or c-weight 40 kg) with mild to moderate infections or appoint 1 tab. 250/125 mg every 8 hours or 1 tab. 500/125 mg every 12 hours, in severe cases, infection and respiratory infections - 1 pi. 500/125 mg every 8 hours or 1 tab. 875/125 mg every 12 hours

Children under 12 years old with body weight below 40 kg dose was selected individually on the basis of the recommended dosing schemes (for amoxicillin) - 45 mg / kg / day in 2 divided doses or 40 mg / kg / day in 3 divided doses. Optimum dosage forms of the drug for children from 6 to 12 years are tablets 500/125 mg in the appointment of two times a day. The maximum daily dose of clavulanic acid (in the form of potassium salt) is for adults - 600 mg for children - 10 mg / kg body weight. The maximum daily dose of amoxicillin for adults - 6 g, for children - 45 mg / kg body weight. The course of treatment is 5-14 days. The duration of treatment is determined by your doctor.

Treatment should not last more than 14 days without re-medical examination. In odontogenic infections appoint 1 tab. 250/125 mg every 8 h or 1 tab. 500/125 mg every 12 h for 5 days. In renal insufficiency, moderate (CC 10-30 ml / min) appoint 1 tab. 500/125 mg every 12 hours for adults and 15/3.75 mg / kg body weight 2 times / day for children under 12 years. In renal insufficiency, severe (CC <10 ml / min) - 1 tab. 500/125 mg every 24 hours for adults, children under 12 years - 15/3.75 mg / kg of body weight one time per day. When anuria interval between administration of a single dose should be increased to 48 hours or more.

Adults who are on hemodialysis, should appoint a drug in a dose of 1 tablet. 500/125 mg or 2 tab. 250/125 mg every 24 hours to compensate for the reduction of the concentration of amoxicillin and clavulanic acid in the blood serum during dialysis should be added to a dose of the drug during the dialysis session and another dose at the end of the session. Children who are on hemodialysis, should appoint a drug in a dose of 15/3.75 mg / kg of body weight one time per day. To compensate for the reduction of the concentration of amoxicillin and clavulanic acid in the blood during dialysis should additionally take a dose before the dialysis session and another dose after the dialysis session.

Side effect
On the part of the digestive system: loss of appetite, nausea, vomiting, diarrhea, rarely - liver problems, increased activity of ALT and AST, and in rare cases - cholestatic jaundice, hepatitis, pseudomembranous colitis.
From the side of the central nervous system: dizziness, headache, reversible hyperactivity, and convulsions.
On the part of the hemopoietic system: a reversible increase in prothrombin time, leukopenia, reversible agranulocytosis and hemolytic anemia.
On the part of the genitourinary system: interstitial nephritis, crystalluria. Allergic reactions: itching, rash, erythematous rash, rarely - exudative erythema multiforme, angioedema, anaphylactic shock, in rare cases - exfoliative dermatitis, Stevens-Johnson syndrome. Other: the development of superinfection (including candidiasis).

Contraindications
infectious mononucleosis (also in the appearance of korepodobnoy rash);
Children under 3 years;
increased sensitivity to antibiotics of penicillin, cephalosporins;
hypersensitivity to amoxicillin or clavulanic acid.

Be wary prescribers for patients with liver failure severe, gastrointestinal diseases (including colitis associated with antibiotic penicillin group in history), chronic renal insufficiency.

Pregnancy and lactation

The drug prescribed with caution during pregnancy and lactation (breastfeeding). Arlette can be used during pregnancy if the expected benefit to the mother outweighs the potential risk to the fetus. Amoxicillin and Clavulanic acid in small amounts are excreted with breast milk, so if you need to appoint during lactation must decide whether termination of breastfeeding.

Application for violations of liver function

The drug should be considered in patients with otsrozhnostyu with hepatic insufficiency.

Application for violations of renal function

Prapart should be cautious to use in violation of the kidney. In renal insufficiency, moderate (CC 10-30 ml / min) appoint 1 tab. 500/125 mg every 12 hours for adults and 15/3.75 mg / kg body weight 2 times / sutdetyam to 12 years, with renal failure, severe (CC <10 ml / min) - 1 tab. 500/125 mg every 24 hours for adults, children under 12 years - 15/3.75 mg / kg of body weight one time per day. When anuria Interval doses should be increased to 48 hours or more.

Adults located at gemodialeze should appoint a drug in a dose of 1 tablet. 500/125 mg or 2 tab. 250/125 mg every 24 hours to compensate for the reduction of the concentration of amoxicillin and klavuronovoy acid in the blood serum during dialysis should be further understood one dose of the drug during the dialysis session and another dose at the end of the session.

Children under 12 years located on gemodialeze should appoint a drug in a dose of 15/3.75 mg / kg of body weight one time per day. To compensate for the reduction of the concentration of amoxicillin and klavuronovoy acid in the blood serum during dialysis should be further understood one dose prior to dialysis session and another dose after the dialysis session.

Cautions

With careful use the drug in patients with impaired liver function during treatment regularly monitor liver function.

In exchange therapy should be monitored blood function, liver and kidneys. In patients with severely impaired renal function requires adequate correction of dosing regimen or increased intervals between doses of the drug. To reduce the risk of adverse reactions from the gastrointestinal tract should take the drug with food.

Because the tablets of the drug combination 250 mg/125 mg and 500 mg/125 mg contain the same amount of clavulanic acid (125 mg), then 2 tablets of 250 mg/125 mg are not equivalent to 1 tablet 500 mg/125 mg.

High concentrations of amoxicillin give false-positive reaction in the determination of glucose in urine using Benedict's reagent or solution Felling (recommend the use of enzymatic reaction with glycosidase).

Effects on ability to drive vehicles and management mechanisms

The drug at recommended doses does not affect the ability to drive transport and management of complex mechanisms.

Overdose

Symptoms: abdominal pain, diarrhea, vomiting, possibly as agitation, insomnia, dizziness, and in some cases - seizures.

Treatment: In the case of the recent treatment (less than 4 hours) is necessary to gastric lavage and activated charcoal to appoint to reduce the absorption of the drug, the patient must remain under medical supervision, if necessary, carry out palliative care. Effective hemodialysis.

Drug Interactions

With simultaneous application of Arlette enhances the toxicity of methotrexate. With simultaneous application of Arleta with allopurinol increases the risk of exanthema. With simultaneous application of Arleta with antacids, glucosamine, laxatives, aminoglycoside absorption slows down, with ascorbic acid - increases.

With simultaneous application of Arleta with bactericidal antibiotics (including aminoglycosides, tsefalosproriny, cycloserine, vancomycin, rifampicin) shows synergistic effects; with antibiotics with bacteriostatic mechanism of action (including macrolides, chloramphenicol, Lincosamides, tetracyclines, sulfonamides) - antagonism.

With simultaneous application of Arlette increases the efficiency of the indirect anticoagulants due to suppression of intestinal microflora, reducing the synthesis of vitamin K and a decrease in prothrombin index. In the appointment of this combination should be dynamic control of blood tests.

With simultaneous application of Arlette reduces the effectiveness of oral contraceptives.

In case of simultaneous appointment of Arleta with drugs in the process of metabolism which is formed of para-aminobenzoic acid, ethinylestradiol increased the risk of breakthrough bleeding. Diuretics, allopurinol, fenilbutazon, NSAIDs and other drugs that block tubular secretion, increase the concentration of amoxicillin (Clavulanic acid is derived mainly by glomerular filtration).

Terms and Conditions of storage

The drug should be stored in a dry place protected from light, away from children at or above 25 ° C. Shelf life - 2 years. The drug should not be used after the expiration date.