Egilok

Composition, structure and packing

Tablets are white or nearly white, round, biconvex, with a dividing line-cross and double-bevel on one side and engraved "E435" - on the other side, and odorless. 1 tab. metoprolol tartrate 25 mg. Excipients: microcrystalline cellulose, sodium karboksimetilkrahmal, silicon dioxide, colloidal anhydrous, povidone, magnesium stearate.

Tablet is white or nearly white, round, biconvex, with the risk to one side and engraved "E434" - on the other side, and odorless. 1 tab. metoprolol tartrate 50 mg. Excipients: microcrystalline cellulose, sodium karboksimetilkrahmal, silicon dioxide, colloidal anhydrous, povidone, magnesium stearate.

Tablets are white or nearly white, round, biconvex, with risks on the one side and engraved "E432" - on the other side, and odorless. 1 tab. metoprolol tartrate 100 mg. Excipients: microcrystalline cellulose, sodium karboksimetilkrahmal, silicon dioxide, colloidal anhydrous, povidone, magnesium stearate.

Clinico-pharmacological group: beta1-blocker.

Pharmacological action

Cardioselective β-adrenoceptor blocker, not having internal membranes and sympathomimetic activity. Has antihypertensive, antianginal and antiarrhythmic action. Blocking in low doses, β1-adrenergic receptors of the heart, reduces the formation of catecholamines stimulated cAMP from ATP, reduces the intracellular current is Ca2 +, has a negative chrono-, Drome, BATM-and inotropic effects (slows heart rate, depresses conduction and excitability, reduces myocardial contractility). TPVR at the beginning of the drug (in the first 24 h after oral administration) increases after 1-3 days of returning to its original level, while continuing to use - is reduced.

Antihypertensive effects were due to a decrease in cardiac output and renin synthesis, inhibition of renin-angiotensin system and central nervous system, restoring the sensitivity of baroreceptors of the aortic arch (not going to enhance their activity in response to BP decrease), and eventually decrease peripheral sympathetic influences.

Lowers high blood pressure at rest, on exertion and stress. BP reduced within 15 min, maximum - 2 hours; effect persists for 6 h. The steady decline is observed after several weeks of regular use. Antianginal effect is determined by the decrease in myocardial oxygen demand by decreasing heart rate (lengthening of diastole and improved myocardial perfusion) and contractility, and decreased sensitivity to the effects of myocardial sympathetic innervation.

Reduces frequency and severity of angina attacks and improves exercise tolerance. Antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, elevated levels of cAMP, hypertension), decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing AV-conduction (mainly in the antegrade and to a lesser extent in the retrograde direction through the AV-node) and on additional routes.
In supraventricular tachycardia, atrial fibrillation, sinus tachycardia with functional diseases of the heart and hyperthyroidism heart rate slows and may even lead to the restoration of sinus rhythm. Prevents the development of migraine.
With many years of taking reduces cholesterol.
When used in the medium therapeutic doses has a less pronounced effect on the organs that contain the β2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi, uterus) and carbohydrate metabolism.
When used in high doses (100 mg / day) has a blocking effect on both β-adrenoceptor subtype.

Pharmacokinetics

Absorption

Quickly and completely (95%) absorbed from the gastrointestinal tract. Cmax in plasma achieved by 1.5-2 h after ingestion. Bioavailability is 50%. In the course of treatment increases bioavailability of up to 70%. Eating increases the bioavailability by 20-40%.

Distribution

Vd is 5.6 L / kg. Linking to plasma proteins - 12%. Penetrates through the BBB and placental barrier. Excreted in breast milk in small amounts.

Metabolism

Metoprolol biotransformiruetsya in the liver. The metabolites have no pharmacological activity.

Withdrawal

T1 / 2 on average 3.5-7 hours Metoprolol almost completely excreted in urine over 72 h. About 5% of the dose was excreted unchanged.

Pharmacokinetics in special clinical situations
When expressed violations of liver function bioavailability and T1 / 2 of metoprolol increases, which may require correction dose.
In case of violation of renal function T1 / 2 and systemic clearance of metoprolol did not significantly change.

Statement
hypertension (as monotherapy or in combination with other antihypertensive drugs), including hyperkinetic type;
CHD (secondary prevention of myocardial infarction, prevention of angina attacks);
cardiac arrhythmias (Supraventricular arrhythmia, ventricular extrasystoles);
hyperthyroidism (in the complex therapy);
prevention of migraine.

Dosage regimen
When hypertension is prescribed in a daily dose 50-100 mg / day in 1 or 2 divided doses (morning and evening).
In case of insufficient therapeutic effect may be a gradual increase in daily dose to 100-200 mg.
In angina pectoris, supraventricular arrhythmias, for the prevention of migraine attacks is prescribed in doses of 100-200 mg / day in 2 divided doses (morning and evening). For secondary prevention of myocardial infarction in the prescribed average daily dose of 200 mg in 2 divided doses (morning and evening).

In functional disorders of cardiac activity, accompanied by tachycardia, prescribe a daily dose of 100 mg in 2 divided doses (morning and evening). In elderly patients, patients with impaired renal function, as well as the need for dialysis dosing regime change is not required.

In patients with severe disturbances of liver function should use the drug in smaller doses, due to slowing metabolism of metoprolol. Tablets, taken orally during or immediately after meals. The tablets can be divided in half, but do not chew.

Side effect
From the side of the central nervous system and peripheral nervous system: fatigue, weakness, headache, slow down the rate of mental and motor responses; rare - paresthesias in the extremities, depression, anxiety, reduced ability to concentrate, drowsiness, insomnia, nightmares, confusion, or transient memory impairment, asthenic syndrome, muscular weakness.
From the sense organs: rarely - reduced vision, reduced secretion of the lacrimal fluid, xerophthalmia, conjunctivitis, tinnitus.
Since the cardiovascular system: sinus bradycardia, palpitation, reduction in blood pressure, orthostatic hypotension, rarely - reduction of myocardial contractility, a temporary worsening of symptoms of chronic heart failure, arrhythmias, increased violations of the peripheral circulation (cooling of the lower extremities, Raynaud syndrome), conduction disorders infarction; in rare cases - AV-blockade cardiodynia.
On the part of the digestive system: nausea, vomiting, abdominal pain, diarrhea, constipation, xerostomia, changes in taste, increase in liver transaminases; rarely - hyperbilirubinemia. Dermatological reactions: urticaria, pruritus, rash, exacerbation of psoriasis, psoriazopodobnye changes in the skin, skin hyperemia, rash, photodermatosis, sweating, reversible alopecia.
On the part of the respiratory system: nasal congestion, difficulty exhaling (bronchospasm when administered high doses or in predisposed patients), shortness of breath.
From the Endocrine: hypoglycemia (in patients receiving insulin), rarely - hyperglycemia.
The part of the hemopoietic system: thrombocytopenia, agranulocytosis, leukopenia. Other: pain in the back or joints, slight weight gain, decreased libido and / or potency.

Contraindications
cardiogenic shock;
AV-block II and III degree;
sinoatrial block;
SSS;
pronounced bradycardia (HR <50 bpm);
heart failure in the stage of decompensation;
angiospastic angina (Prinzmetal angina);
marked hypotension (systolic BP <100 mm Hg);
lactation;
simultaneous reception of MAO inhibitors;
simultaneous in / introduction of verapamil;
Hypersensitivity to metoprolol and other ingredients.

Precautions should be prescribed medication for diabetes, metabolic disorders, bronchial asthma, chronic obstructive pulmonary disease (emphysema, chronic obstructive bronchitis), obliterating peripheral vascular disease (intermittent claudication, Raynaud syndrome), chronic liver disease, chronic renal insufficiency, myasthenia gravis, pheochromocytoma, AV-blockade of I degree, thyrotoxicosis, depression (including history), psoriasis, pregnancy, as well as children and adolescents under the age of 18 years, elderly patients.

Pregnancy and lactation

Application Egiloka during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. If necessary, the appointment of the drug in this period should be careful monitoring of the fetus and the newborn within 48-72 hours after birth, as intrauterine growth retardation, bradycardia, hypotension, respiratory depression, hypoglycemia.

Effect of metoprolol in the newborn during breast feeding has not been studied, and women receiving Egilok should stop breastfeeding.

Application for violations of liver function

In patients with severe disturbances of liver function should use the drug in smaller doses, due to slowing metabolism of metoprolol. Precautions should be prescribed the drug for chronic pechenochenoy failure.

Application for violations of renal function

Patients with impaired renal function, as well as the need for dialysis change the dosage required. Precautions should be prescribed the drug in patients with chronic renal failure.

Cautions
In appointing the drug Egilok should regularly monitor heart rate and blood pressure.

Patients should be warned that if HR <50 bpm is necessary to consult a doctor. Patients with diabetes should regularly monitor blood glucose levels and if necessary correction of insulin or oral hypoglycemic agents. Appointment Egiloka patients with chronic heart failure is possible only after reaching the stage of compensation.

Patients receiving Egilok may gain expression of hypersensitivity reactions (on the background of aggravated allergic history), and the lack of effect of the introduction of conventional doses of epinephrine (adrenaline). Against the background of Egiloka possible aggravation of symptoms of peripheral circulation. Egilok should be lifted gradually, consistently reducing the dose within 10 days.
With a sharp cessation of treatment may be withdrawal symptoms (increased angina attacks, increased blood pressure). During the withdrawal of the drug to patients with angina should be under close medical supervision.
When angina selected dose should provide heart rate at rest within 55-60 bpm, with a load - no more than 110 bpm.

Patients who use contact lenses should be aware that patients receiving beta-blockers may decrease production lacrimal fluid. Metoprolol may mask certain clinical signs of hyperthyroidism (tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since the symptoms can increase.
In diabetes reception Egiloka may mask symptoms of hypoglycemia (tachycardia, sweating, increased blood pressure).
In the appointment of metoprolol for patients with asthma should be the simultaneous use of beta 2-sympathomimetics.

In patients with pheochromocytoma Egilok should be used in combination with alpha-blockers. Prior to any surgical intervention is necessary to inform the anesthesiologist about the therapy Egilokom (drug choice for general anesthesia with minimal negative inotropic action); drug withdrawal is not required.
Administration of these drugs to elderly patients should regularly monitor liver function. Correction of dosage regimen is required only in case of elderly patients increasing bradycardia, BP decrease, AV-blockade, bronchospasm, ventricular arrhythmias, severe disturbances of liver function.

Sometimes it is necessary to stop treatment. There should be a special condition monitoring of patients with depressive disorders in history. In the case of depression Egilok should be abolished.
With simultaneous application of Egiloka with Clonidine in case of cancellation Egiloka Clonidine should be lifted in a few days (due to risk of cancellation syndrome).

Drugs that reduce the supply of catecholamines (eg reserpine) may enhance the action of beta-blockers, so patients taking these combinations of drugs should be under constant medical supervision in order to identify an excessive reduction of blood pressure or bradycardia.

Use in pediatrics

Efficacy and safety of Egiloka in children and adolescents under the age of 18 are not defined.

Effects on ability to drive vehicles and management mechanisms

Patients whose work requires more attention, the appointment of an outpatient drug should be resolved only after the evaluation of individual patient response.

Overdose

Symptoms: pronounced sinus bradycardia, dizziness, nausea, vomiting, cyanosis, hypotension, arrhythmia, ventricular extrasystoles, bronchospasm, syncope, acute overdose - cardiogenic shock, unconsciousness, coma, AV-block until the full development of cross-blockade and heart failure , cardiodynia.

First signs of overdose appear within 20 min-2 h after administration. Treatment: gastric lavage, the appointment of adsorbents, symptomatic therapy: marked reduction in blood pressure - Trendelenburg position, in the case of severe hypotension, bradycardia, and threatening heart failure - in / in (with an interval of 2-5 minutes) introduction of beta-adrenostimulyatorov or in / introduction of 0.5-2 mg of atropine sulfate, in the absence of a positive effect - dopamine, dobutamine, or norepinephrine.

As a follow up appointment may be 1-10 mg of glucagon, staging transvenous intracardial electrostimulator. If bronchospasm - to / at the introduction of beta2-adrenostimulyatorov, in convulsions - slow to / in the introduction of diazepam. Metoprolol poorly displayed with hemodialysis.

Drug Interactions
With simultaneous application Egiloka with MAO inhibitors may significantly increased the hypotensive actions. The interval between admission and MAO inhibitors Egiloka must be at least 14 days. At the same time / in the introduction of verapamil can trigger heart failure, co-administration of nifedipine leads to a significant decrease in BP. Means for inhalation anesthesia (derivatives of hydrocarbons), while applying to Egilokom increase the risk of myocardial depression and arterial hypotension.
With simultaneous use of beta-adrenostimulyatorov, theophylline, cocaine, estrogens, indomethacin and other NSAIDs reduce the hypotensive effect Egiloka.
With simultaneous application Egiloka and ethanol has increased, inhibitory action on the CNS. With simultaneous application Egiloka with ergot alkaloids increases the risk of peripheral circulatory disorders.
With simultaneous application Egilok increases the effect of oral hypoglycemic agents and insulin and increases the risk of hypoglycemia.
With simultaneous application Egiloka with antihypertensive diuretics, nitrates, calcium channel blockers increased risk of arterial hypotension.
With simultaneous application of Egiloka with verapamil, diltiazem, antiarrhythmics (amiodarone), reserpine, methyldopa, clonidine, guanfatsinom, means for general anesthesia and cardiac glycosides may be a manifestation of shortening increased heart rate and inhibition of AV-conduction.

Inductors microsomal liver enzymes (rifampicin, barbiturates) accelerate the metabolism of metoprolol, which reduces the concentration of metoprolol in plasma and reduce the effect Egiloka.

Inhibitors of microsomal liver enzymes (cimetidine, oral contraceptives, phenothiazines) increase the concentration of metoprolol in plasma. The allergens used for immunotherapy, or allergen extracts for skin tests or combined with Egilokom, increase the risk of systemic allergic reactions or anaphylaxis.

Iodine radiopaque substances for in / in the introduction, while the use of Egilokom increase the risk of anaphylactic reactions. Egilok while applying reduced clearance of xanthine, especially in patients with initially increased clearance of theophylline under the influence of smoking.
At simultaneous application with Egilokom reduced clearance of lidocaine and increases the concentration of lidocaine in plasma.
With simultaneous application Egilok strengthens and extends the effect of nondepolarizing muscle relaxants, prolongs the action of indirect anticoagulants.
When combined with the use of ethanol increases the risk of significant decrease of BP.

Terms and Conditions of storage

List B. The drug should be stored out of reach of small children at a temperature of 15 ° to 25 ° C. Shelf life - 5 years.

Celascon Vitamin C

Composition, structure and packing

Effervescent tablets tasteful red orange round, smooth, marble-pale pink, hygroscopic.
1 tab. ascorbic acid 500 mg

Excipients: anhydrous citric acid, sodium bicarbonate, lactose anhydrous, orange flavor type Bolexo, macrogol 6000, acesulfame potassium, dye Allura Red AC, sorbitol.

Clinico-pharmacological group: Vitamin

Pharmacological action and pharmacokinetics

To cover the shortage of vitamin C, the metabolic regulating the redox processes, antioxidant.

Absorbed in the small intestine (duodenum, partly - in the ileum).

Excreted in the urine, faeces, sweat, breast milk. Smoking and the use of ethanol accelerated the destruction, dramatically reducing the reserves in the body.

It has antioxidative properties.

Regulates the transport of hydrogen in many biochemical reactions, and improves utilization of glucose in the citric acid cycle, participates in the formation of tetrahydrofolic acid and regeneration of tissues, the synthesis of steroid hormones, collagen and procollagen.

Supports normal capillary permeability. Activates proteolytic enzymes involved in the exchange of aromatic amino acid, pigments, and cholesterol, promotes the accumulation of glycogen in the liver.

Improves bile secretion, restores the function of exocrine pancreas and endocrine - Thyroid.

Regulates immunological reactions, promotes phagocytosis, increases resistance to infection.

Inflammatory and antiallergic action.

Statement
hypovitaminosis C
hemorrhagic diathesis,
kapillyarotoksikoz,
hemorrhagic stroke
haemorrhages (nasal, lung, uterine, etc.)
infectious diseases
intoxication
alcohol and infectious delirium,
acute radiation sickness,
posttranfuzionnye complications
liver disease (infectious hepatitis, chronic hepatitis and cirrhosis),
GI (Akhil, peptic ulcer, especially after the bleeding, enteritis, colitis, helminthic),
cholecystitis
adrenal insufficiency (Addison disease),
sluggishly healing wounds,
ulcers
fractures,
dystrophy,
physical and mental overload
pregnancy and lactation,
hemosiderosis,
melanoderma,
erythroderma,
psoriasis
common chronic dermatosis.

As an antioxidant
Atherosclerosis
asthma,
diffuse connective tissue disease (rheumatoid artirit,
systemic lupus erythematosus,
scleroderma) and others;
overdose of anticoagulants,
aconite poisoning, Anaesthesinum, aniline, antabusom, barbiturates, benzene, dichloroethane, potassium permanganate, methyl alcohol, arsenic, carbon monoxide, hydrocyanic acid, sulfanilamide, thallium, phenols, and quinine.

Dosage regimen

Adults: prophylactically - 500 mg.

In therapeutic purposes - on 1000mg.

Before taking tablets dissolve in about 150 ml of water.

Side effect

Gastrointestinal irritation (nausea, vomiting, diarrhea), hypertension, metabolic disorders, depression function insular apparatus of the pancreas (hyperglycemia, Glycosuria) and glycogen synthesis, reduces capillary permeability and deterioration of trophic tissue, thrombocytosis, giperprotrombinemiya, blood clots, erythropenia, neutrophilic leukocytosis, myocardial degeneration, damage to glomerular apparatus of the kidneys, allergic reactions (including anaphylactic shock); Propafenone formation of urinary stones, metabolic zinc, copper, increased excitability of the CNS, sleep disorders, the development of microangiopathies.

Contraindications
hypersensitivity
thrombophlebitis
propensity to thrombosis,
diabetes.

Pregnancy and lactation

No data are presented.

Cautions

During long-term treatment requires monitoring of renal function, blood pressure and glucose level (especially in the appointment of high-dose).

Ascorbic acid as a reducing agent, can distort the results of various laboratory tests (blood levels of glucose, bilirubin, transaminase activity, LDH).

Overdose

Data on predozirovke not represented.

Drug Interactions

Improves concentration in the blood to salicylates (increases the risk of crystalluria), ethinyl estradiol, benzylpenicillin and tetracycline, reduces oral contraceptives.

Decreases the anticoagulant effect of coumarin derivatives.

It improves the absorption in the intestine of iron preparations.

Increases total Cl of ethanol.

Preparations quinolinic series, calcium chloride, salicylates, corticosteroids for prolonged use deplete reserves of vitamin C.

Terms and Conditions of storage

In a dry place protected from light at room temperature.

Shelf life - 2 years.

Haes-Steril

Composition, structure and packing

Solution for infusion of 6% 1 l starch 200/0.5 60 g osmolarity of 308 mOsm / l pH 3.5-6.0. Excipients: sodium chloride, water, d / and.

Solution for infusion 10% 1 l starch 200/0.5 100 g osmolarity 308 mOsm / l pH 3.5-6.0. Excipients: sodium chloride, water, d / and.

Clinico-pharmacological group: Plazmozameschayuschy drug.

Mechanism of action Plazmozameschayuschy drug. It is a 6% or 10% isotonic solution of starch (derived from amylopectin) with an average molecular weight of 200,000 daltons and the degree of substitution of about 0.5, which means that 10 glucose residues of amylopectin are 5 gidroksietilovyh groups.

The action of the drug due to the ability to bind and retain water in the intravascular space, thus decreasing swelling of tissues. The drug improves blood rheology and microcirculation, and cerebral and utero-placental blood flow (including through the reduction in the hematocrit). This leads to improved blood supply to tissues, reduce plasma viscosity, platelet aggregation and prevents the aggregation of red blood cells. Starch structurally related glycogen, which explains its high tolerance and a low risk of anaphylactoid reactions.

Infusion Haese-ters (500 ml per 15 min), volunteers with hypovolemia leads to increased plasma volume by approximately 100% of the administered volume (for infusion of 6% solution) or 145% (with the infusion of 10% solution) for 3-4 PM Haese-ters is highly stable solution and does not give flocculation temperature fluctuations.

Pharmacokinetics

Metabolism and excretion

Hydrolyzed serum amylase. About 47% incorporated into starch excreted in the urine within 24 h and only 10% continued to circulate in the blood serum.

Statement
treatment and prevention of hypovolemia and shock in surgical interventions (hemorrhagic shock), traumatic injuries (traumatic shock), infections (septic shock), burns (burn shock);
normovolemicheskaya acute hemodilution to reduce the introduction of donor blood during surgery;
therapeutic hemodilution.

Dosage regimen

For the treatment and prevention of hypovolemia and shock, the maximum daily dose of 6% solution for infusion is 33 ml / kg body weight (2500 ml/75 kg body weight) (1.2 g starch / kg body weight). Maximum speed in / infusion - 20 ml / kg body weight / h (1500 ml/75 kg body weight / h) (2 g starch / kg body weight / h). The maximum daily dose of 10% solution for infusion of 20 ml / kg body weight (1500 ml/75 kg body weight) (2 g starch / kg body weight). Maximum speed in / infusion - 20 ml / kg body weight / h (1500 ml/75 kg body weight / h) (2 g starch / kg body weight / h).

The first 10-20 ml of solution should pour slowly, with careful monitoring of the patient in connection with the risk of anaphylactoid reactions. Duration of Haese-ters determined by the degree and duration of hypovolemia.

To minimize the introduction of donor blood during surgery before the surgery recommended single dose of 6% solution Haese-ters in the ratio 1:1 (to target hematocrit not lower than 30%). Producing 2-3-fold selection of 500 ml of his own blood and 2-3 injections of 500 ml 6% solution Haese sr. Speed of blood collection - 1000 ml for 15-30 min, the rate of introduction of 6% solution Haese ste - 1000 ml for 15-30 min. Repeated administration of the drug is possible with normal values of hematocrit (not below 30%).

In the conduct of therapeutic hemodilution criterion for selection of doses is a reduction in the hematocrit, determined for each patient. Infusion Haese-ters can be Isovolemic (with simultaneous selection of his own blood), or hypervolemic (without selection of his own blood) in small (250 ml for 0.5-2 h), medium (500 ml for 4-6 h) or high doses (twice at 500 ml for 8-24 h). The maximum daily dose is 1.2 g / kg body weight. The drug is introduced within 10 days.

Side effect

Allergic reactions: skin rash, bronchospasm, anaphylactoid reactions (tachycardia, hypotension, dizziness, nausea, vomiting), the shock until the cessation of breathing and cardiac activity. Skin reactions: with prolonged daily use in middle and high doses often - itchy skin, are difficult to therapy (reduction in the maximum recommended daily dose of up to 250 ml). Other: rarely - pain in the kidneys when used in high doses - increase in bleeding time, increased concentration of serum amylase.

Contraindications
Chronic heart failure stage IIB-III;
renal insufficiency (serum creatinine> 2 mg / dl or more than 177 mmol / l);
expressed disorders of blood coagulation (except for life threatening conditions);
hyperhydration;
marked dehydration;
intracranial bleeding
sensitivity to starch.

Pregnancy and lactation

Data on the feasibility and safety of the drug Haese-ters during pregnancy and lactation no. Use of the drug in early pregnancy is only possible to survive.

Application for violations of renal function

Contraindicated in renal insufficiency (serum creatinine> 2 mg / dl or more than 177 mmol / l). Before therapy with Haese-ters needed to control the content of creatinine in serum. In terms creatinine 1.2-2 mg / dL (106-177 micromol / l) should be conducted daily monitoring of fluid balance and renal excretory function.

Cautions

Before therapy with Haese-ters necessary to control the content of creatinine in serum.
In terms creatinine 1.2-2 mg / dL (106-177 micromol / l) should be conducted daily monitoring of fluid balance and renal excretory function.
If you have allergic reactions during infusion Haese-ters of the drug should be stopped immediately and initiate an Antiallergic therapy (antihistamines, prednisolone 120 mg IV); during resuscitation prescribe adrenaline 0.05-0.1 mg / in the SCS in / in 5% albumin solution.
If you experience pain in the kidneys infusion of the drug should be discontinued to ensure plenty of fluids and frequent monitoring of serum creatinine.
If you want to mix with other drugs should comply with the rules of asepsis and ensure interoperability of solutions.

Overdose

Cases of overdose are not currently registered.

Drug Interactions

Currently, drug interactions drug Haese-ters not described.

Terms and Conditions of storage

The drug should be stored at a temperature not above 25 ° C; not freeze. Shelf life - 5 years.

Factive

Composition, structure and packing

Tablets, coated in white or almost white, oblong shape.

1 tab. gemifloksatsin (in the form mesylate seskvigidrata) 160 mg.

Excipients: microcrystalline cellulose, polyvinylpyrrolidone (povidone), krospovidon (poliplasdon X EL-10), magnesium stearate.

Tablets, coated in white or almost white, oblong, with the risk from two sides.

1 tab. gemifloksatsin (in the form seskvigidrata mesylate) 320 mg.

Excipients: microcrystalline cellulose, polyvinylpyrrolidone (povidone), krospovidon (poliplasdon X EL-10), magnesium stearate.

Clinico-pharmacological group: antibacterial fluoroquinolone group.

Pharmacological action

Antibacterial fluoroquinolone group. Bactericidal action. Interferes with the replication, repair and transcription of bacterial DNA by inhibiting the enzymes DNA gyrase (topoisomerase II) and topoisomerase IV, essential for the growth of bacteria. Gemifloksatsin has high affinity with bacterial topoisomerase II and IV. The mechanism of action of fluoroquinolones, including gemifloksatsin differs from that of beta-lactam antibiotics, macrolides, aminoglycosides and tetracyclines. There was no cross-resistance between gemifloksatsinom and these groups of antibiotics. The main mechanism of resistance to fluoroquinolones are mutations in the genes of DNA gyrase and DNA topoisomerase IV, the frequency of occurrence of which is 10-7-10-10.

Strains of Streptococcus pneumonia, with mutations in the genes encoding these enzymes, resistant to most fluoroquinolones. However, in a therapeutically relevant concentrations gemifloksatsin able to inhibit the modified enzymes. Thus, some strains of Streptococcus pneumonia, resistant to fluoroquinolones may be susceptible to gemifloksatsinu.

The drug is active against a broad spectrum of microorganisms, both in conditions in vitro, and in vivo: Gram-positive aerobic bacteria: Streptococcus spp., Including Streptococcus pneumoniae (including strains resistant to penicillin and macrolides and the most resistant to ofloxacin / levofloxacin strains, including strains of group Streptococcus pneumoniae, including subspecies, previously known as PRSP (Streptococcus pneumoniae resistant to penicillin), and combining strains resistant to two or more of the following antibiotics: penicillin, cephalosporins II generation, macrolides, tetracyclines and trimethoprim / sulfamethoxazole), Streptococcus pyogenes (including macrolide-resistant), Streptococcus viridans, Streptococcus agalactiae, Streptococcus milleri, Streptococcus anginosius, Streptococcus constellatus, Streptococcus mitis; Staphylococcus spp. (Including Staphylococcus aureus / methicillin sensitive to /, Staphylococcus epidermidis, Staphylococcus saprophyticus, Staphylococcus haemolyticus), Enterococcus spp. (Including Enterococcus faecalis, Enterococcus faecium); Gram-negative aerobic bacteria: Haemophilus spp. (Including Haemophilus influenzae, including strains producing β-lactamases, Haemophilus parainluenzae), Moraxella spp. (Including Moraxella catarrhalis, and producing β-lactamase neprodutsiruyuschie), Klebsiella spp. (Including Klebsiella pneumoniae, Klebsiella oxytoca), Escherichia coli, Neisseria gonorrhoeae, Acinetobacter spp. (Including Acinetobacter lwoffii, Acinetobacter anitartus, Acinetobacter calcoaceticus, Acinetobacter haemolyticus), Citrobaster spp. (Including Citrobaster freundii, Citrobaster koseri), Salmonella spp., Shigella spp., Enterobacter spp. (Including Enterobacter aerogenes), Serratia spp. (Including Serratia marcescens), Proteus spp. (Including Proteus mirabilis, Proteus vulgaris), Providencia spp., Morganella spp. (Including Morganella morganii), Yersinia spp., Pseudomonas spp. (Including Pseudomonas aeruginosa), Bordetella spp. (Including Bordetella pertrussis); as well as atypical bacteria: Coxiella spp. (Including Coxiella burnetti), Mycoplasma spp. (Including Mycoplasma pneumoniae), Legionella spp. (Including Legionella pneumophila), Chlamydia spp. (Including Chlamydia pneumoniae); anaerobic bacteria: Peptostreptococcus spp., Clostridium spp. (Including Clostridium non-perfringes, Clostridium perfringes), Fusobacterium spp., Porphyromonas spp., Prevotella spp.

Pharmacokinetics

Absorption

Once inside gemifloksatsin rapidly absorbed from the gastrointestinal tract. After a single dose of the drug at a dose of 320 mg Cmax plasma levels achieved during 0.5-2 hours after re-admission 320 mg Cmax in plasma was 1.61 ± 0.51 pg / ml (0.70-2.62 / ug / ml), and AUC - 9.93 ± 3.07 mg x h / ml (4.71-20.1 mg x h / ml). Eating virtually no effect on the pharmacokinetics gemifloksatsina, so the drug can be taken without regard to meals. Pharmacokinetics gemifloksatsina is linear in the dose range 40-640 mg. Drug is not cumulative (less than 30% at a dose of 640 mg for 7 days in advance).

Distribution

In exchange you receive 320 mg gemifloksatsina 1 time / Cmax is achieved on the third day. If readmission 55-73% of the drug bound to plasma proteins, the proportion of bound fraction does not depend on age.

Gemifloksatsin well into the lung tissue. The concentration gemifloksatsina in bronchoalveolar lavage above that of plasma.

Metabolism

In a small number gemifloksatsin metabolized in the liver. After 4 h after administration of unmodified gemifloksatsin prevails among the metabolites of the drug (65%) in blood plasma.

Gemifloksatsin not Biotransformation microsomal hepatic enzyme cytochrome P450.

Withdrawal

In healthy individuals 61.0 ± 9.5% dose gemifloksatsina eliminated through the intestines, and 36.0 ± 9.3% in the urine as unchanged drug and metabolic products. In hemodialysis the plasma displays 20-30% of the dose gemifloksatsina.

Pharmacokinetics in special clinical situations

The pharmacokinetics of the drug in children has not been studied.

In adult patients age does not affect the pharmacokinetics gemifloksatsina.

When liver failure possibly a slight increase in Cmax gemifloksatsina in blood plasma, which does not require dose adjustment.

In renal failure has been a slight increase in the time of elimination from the plasma gemifloksatsina unchanged Cmax.

Statement

Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
exacerbation of chronic bronchitis;
community-acquired pneumonia (including those caused by multiresistant strains);
Acute sinusitis.

Dosage regimen

Assign to 320 mg 1 time / day. With exacerbation of chronic bronchitis treatment is 5 days, with community-acquired pneumonia - 7 days for acute sinusitis - 5 days.

In mild and moderate renal dysfunction (QA more than 40 ml / min) dose correction is required. When expressed renal dysfunction (CC less than 40 ml / min), as well as patients who are on hemodialysis and continuous ambulatory peritoneal dialysis, long-term, the recommended dose is 160 mg 1 time / day.

Elderly patients, patients with impaired hepatic function changes dose regimen is not required.

The tablets should be taken by mouth, without chewing, drinking a small amount of water, regardless of the meal.

Side effect

Allergic reactions: sometimes - itching, rash, and in some cases - Stevens-Johnson syndrome (malignant exudative erythema multiforme), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, allergic pneumonitis.

On the part of the digestive system: nausea, diarrhea, and sometimes - vomiting, abdominal pain, flatulence, anorexia, rarely - acute liver failure, hepatitis, increase in liver transaminases, total bilirubin level.

From the side of the central nervous system and peripheral nervous system: Rarely - tremor, restlessness, anxiety, confusion, hallucinations, paranoid syndrome, depression, drowsiness (with symptoms of CNS lesions reception gemifloksatsina stop), in some cases - sensory or sensorimotor axonal polyneuropathy, manifested by paresthesias , hypoesthesia and other violations of sensitivity, weakness.

From the sensory organs: rarely - violations of taste and smell, visual disturbances (diplopia, changes in color vision), tinnitus, vertigo, hearing loss.

On the part of the hematopoietic system: sometimes - leukopenia; rarely - thrombocytopenia, in some cases - pancytopenia, thrombocytopenic purpura, agranulocytosis, anemia (including hemolytic and aplastic).

On the part of the urinary tract: rare - crystalluria, in some cases - interstitial nephritis, acute renal failure.

On the part of the musculoskeletal system: rarely - arthralgia, arthritis, abscess, myalgia, tendon rupture shoulder, hand, Achilles tendon or other tendons.

From the laboratory tests: rarely - to improve the content of sodium, potassium reduction, reduction of calcium levels, changes in hematocrit, increased activity of CK.

Other: rarely - vasculitis, superinfection (candidiasis, a pseudomembranous colitis).

Contraindications
Pregnancy
Lactation (breastfeeding);
childhood and adolescence to 18 years;
lengthening of the QT interval on ECG (including congenital);
tendon injury, previously deferred due to the use of fluoroquinolones;
individual intolerance gemifloksatsina and other fluoroquinolones.

Precautions should be prescribed the drug at an increased risk of arrhythmias (including clinically significant bradycardia, and acute myocardial ischemia), and deficiency of glucose-6-phosphate dehydrogenase (the risk of hemolytic reactions), patients, especially elderly receiving SCS (because of their increased risk of injury to tendons) , epilepsy and a tendency to seizures, while receiving chemotherapy, prolong the interval QT (antiarrhythmics class I A (quinidine, procainamide) and class III (amiodarone, sotalol), for violations of water-electrolyte imbalance (hypokalemia, gipomagniemiya).

Pregnancy and lactation

Drug is contraindicated in pregnancy. If necessary, use during lactation should stop breastfeeding.

Application for violations of liver function

Patients with impaired liver function changes in dosage regimen is not required.

Application for violations of renal function

In mild and moderate renal dysfunction (QA more than 40 ml / min) doses of correction is required.

When expressed renal dysfunction (CC less than 40 ml / min), as well as patients who are on continuous hemodialysis and long-term ambulatory peritoneal dialysis, the recommended dose is 160 mg 1 time / day.

Cautions

During treatment gemifloksatsinom need to supply a sufficient amount of fluid subject to normal diuresis.

When receiving the drug (as the use of other fluoroquinolones), photosensitivity reactions may occur, it is recommended to avoid contact with direct sunlight. Treatment should be discontinued if symptoms of photosensitivity (eg, change skin like sunburn).

The risk of tendon injury may increase in patients receiving SCS, especially in elderly patients. At the first sign of tendonitis (pain and swelling in the tendons) to use the drug should be stopped, deleted exercise and consult your doctor.

In patients with diarrhea developed after the start of treatment Factiva, we can assume the development of pseudomembranous colitis. The most frequent causative agent of colitis is Clostridium difficile. In most cases, stopping treatment is sufficient for the disappearance of symptoms of colitis (in rare cases may require the appointment of antibacterial drugs active against Slostridium difficile).

Effects on ability to drive vehicles and management mechanisms

Be careful when driving or busy with other potentially hazardous activities that require high concentration and speed of psychomotor reactions, especially with simultaneous use of ethanol.

Overdose

Treatment: gastric lavage, artificial vomiting, excessive drinking, if necessary, carry symptomatically. The specific antidote is known. In hemodialysis of blood plasma displays 20-30% of the dose gemifloksatsina.

Drug Interactions

At the same time appointing Factiva c antacids containing aluminum and magnesium sulfate or iron bioavailability gemifloksatsina reduced. Antacids should be taken not less than 3 hours before or not earlier than 2 h after administration gemifloksatsina.

Sukralfat while applying reduced bioavailability gemifloksatsina. Sukralfat should be taken no earlier than 2 h after administration gemifloksatsina.

Estrogen-gestagen oral contraceptives significantly reduces the bioavailability gemifloksatsina.

Course reception gemifloksatsina not affect the pharmacokinetics of oral contraceptive preparations containing ethinylestradiol / levonorgestrel.

Terms and Conditions of storage

The drug should be stored in a dry, protected from light and away from children at or above 25 ° C.

Shelf life - 3 years.

Ultop

Composition, structure and packing

Capsules two colors: body capsule pale pink cover - white; the contents of capsules - pellets from white to white with a slightly yellowish or until white with a slightly pinkish tint.
1 capsule.
omeprazole 10 mg



Excipients: granules of sugar, sucrose, corn starch, gidroksipropiltsellyuloza (giproloza), heavy magnesium carbonate, sodium lauryl sulphate, methacrylic acid copolymer and etakrilovoy, talc, macrogol 6000, titanium dioxide.

The composition of the shell capsules: titanium dioxide (E171), iron oxide (E172), gelatin.

7 pcs. - Blisters (2) - bundles of cardboard.

7 pcs. - Blisters (4) - bundle pasteboard.

14 pcs. - Plastic pencil cases with polypropylene lid and the capsule gidrosorbenta (1) - packs cardboard.

28 pieces. - Plastic pencil cases with polypropylene lid and the capsule gidrosorbenta (1) - packs cardboard.

Capsules two colors: body capsule pale pink cap - brown-pink color, the contents of capsules - pellets from white to slightly yellowish or slightly pink color.
1 capsule.
omeprazole 20 mg


Excipients: granules of sugar, sucrose, corn starch, gidroksipropiltsellyuloza (giproloza), heavy magnesium carbonate, sodium lauryl sulfate, methacrylic acid copolymer and etakrilovoy, talc, macrogol 6000 and titanium dioxide.

The composition of the shell capsules: titanium dioxide (E171), iron oxide (E172), gelatin.

7 pcs. - Blisters (2) - bundles of cardboard.

7 pcs. - Blisters (4) - bundle pasteboard.

14 pcs. - Plastic pencil cases with polypropylene lid and the capsule gidrosorbenta (1) - packs cardboard.

28 pieces. - Plastic pencil cases with polypropylene lid and the capsule gidrosorbenta (1) - packs cardboard.

Capsules two colors: body capsule pale pink color, cover - a brownish-pink color, the contents of capsules - pellets from white to white with a slightly yellowish or white up with a slightly pinkish tint.
A capsule.
omeprazole 40 mg



Excipients: granules of sugar, sucrose, corn starch, gidroksipropiltsellyuloza (giproloza), heavy magnesium carbonate, sodium lauryl sulfate, methacrylic acid copolymer and etakrilovoy, talc, macrogol 6000, titanium dioxide.

The composition of the shell capsules: titanium dioxide (E171), iron oxide (E172), gelatin.

7 pcs. - Blisters (2) - bundles of cardboard.

7 pcs. - Blisters (4) - bundle pasteboard.

14 pcs. - Plastic pencil cases with polypropylene lid and the capsule gidrosorbenta (1) - packs cardboard.

28 pieces. - Plastic pencil cases with polypropylene lid and the capsule gidrosorbenta (1) - packs cardboard.

Clinico-pharmacological group: an inhibitor of H +-K +-ATPase. Antiulcer drug

Registration № №:
cps. 20 mg: 14 or 28 pieces. - P № 014514/01, 22.10.08
cps. 10 mg: 14 or 28 pieces. - LS-000 695, 31.08.07
cps. 40 mg: 14 or 28 pieces. - LS-000 695, 31.08.07

Pharmacological action

Antiulcer drug, an inhibitor of H +-K +-ATPase. Inhibits the activity of H +-K + ATPase in gastric parietal cells and thus blocks the final stage of formation of hydrochloric acid, which lowers the level of basal and stimulated secretion, irrespective of the nature of the stimulus.

After a single dose of the drug into the effect of omeprazole occurs within the first hour and continues for 24 h, the maximum effect is achieved within 2 hours after stopping the secretory activity was fully restored within 3-5 days.

Pharmacokinetics

Absorption and distribution

After taking the drug inside omeprazole is rapidly absorbed from the gastrointestinal tract, Cmax in the plasma is achieved through 0.5-1 hours

Bioavailability is 30-40%. Binding to plasma proteins - 90%.

Metabolism and excretion

Omeprazole virtually biotransformiruetsya in the liver with the formation of six pharmacologically inactive metabolites (gidroksiomeprazol, sulfide and sulfonic derivatives). Write mainly by the kidneys (70-80%) and bile (20-30%).

Omeprazole is an inhibitor of isoenzyme CYPS19.

Pharmacokinetics in special clinical situations

In chronic renal failure, excretion decreased proportionally reduced creatinine clearance.

In the elderly excretion of omeprazole decreases bioavailability increases.

When liver failure bioavailability increases to 100%, T 1 / 2 - 3 hours

Statement
stomach ulcer and duodenal ulcer (in the exacerbation and anti-treatment), including associated with Helicobacter pylori (in the combined therapy)
reflux esophagitis
erosive and ulcerative lesions of the stomach and duodenal ulcers associated with NSAID intake, stress ulcer
Zollinger-Ellison syndrome

Dosage regimen

In duodenal ulcer in acute Ultop prescribe 20 mg 1 time / day for 2-4 weeks. In resistant cases, may increase the dose to 40 mg / day.

In gastric ulcer in acute and erosive-ulcerative esophagitis - from 20-40 mg / day for 4-8 weeks.

For the eradication of Helicobacter pylori - 20 mg 2 times / day for 7 or 14 days (depending on the applied treatment regimen) in combination with antibacterial drugs.

To prevent worsening of gastric ulcer and duodenal ulcer Ultop administered in doses of 10-20 mg / day.

In order to prevent aggravation of reflux esophagitis - 20 mg / day for a long time. Chance of receiving the drug on demand.

When erosive and ulcerative lesions of the gastrointestinal tract, caused by taking NSAIDs, - 20 mg / day for 4-8 weeks.

In Zollinger-Ellison syndrome the dose selected individually depending on the initial level of gastric secretion, usually from 60 mg / day. If necessary, the dose is increased to 80-120 mg / day in 2 divided doses.

In patients with severe hepatic insufficiency Ultopa daily dose should not exceed 20 mg.

The drug, taken orally, before eating, not liquid, squeezed a small amount of water.

Side effect

In rare cases, may experience the following, usually reversible adverse reactions:

On the part of the digestive system: nausea, diarrhea, constipation, abdominal pain, flatulence, dry mouth, breach of taste, stomatitis, transient increase in liver enzymes in blood plasma. Patients with previous severe liver disease - hepatitis (including those with jaundice), abnormal liver function.

From the side of the central nervous system and peripheral nervous system: headache, dizziness, agitation, drowsiness, insomnia, paresthesia, depression, hallucinations, blurred vision, patients with severe concomitant somatic diseases, patients with prior severe liver disease - encephalopathy.

On the part of the musculoskeletal system: muscle weakness, myalgia, arthralgia.

On the part of the hemopoietic system: leucopenia, thrombocytopenia, and in certain cases - agranulocytosis, pancytopenia.

Dermatological reactions: skin rash, itching, and in some cases - photosensitivity, erythema multiforme exudative, alopecia.

Allergic reactions: urticaria, angioedema, bronchospasm, interstitial nephritis, anaphylactic shock, fever.

Other: peripheral edema, increased sweating, gynaecomastia, rarely - the formation of gastric glandulyarnyh cysts during long-term treatment (result from the inhibition of secretion of hydrochloric acid and are benign and reversible).

Contraindications
childhood
pregnancy
lactation (breastfeeding)
Hypersensitivity to the drug's components

Precautions should be prescribed the drug in renal or hepatic insufficiency.

Application of pregnancy and breastfeeding

Do not use Ultop pregnancy. If necessary, the appointment during lactation is necessary to solve the issue of termination of breastfeeding.

Application for violations of liver function

Precautions should be prescribed the drug for hepatic failure.

In patients with severe hepatic insufficiency Ultopa daily dose should not exceed 20 mg.

Application for violations of renal function

Precautions should be prescribed the drug in renal failure.

Cautions

Before treatment is necessary to exclude the presence of malignant process in the upper GI tract (since treatment can mask symptoms and complicate diagnosis).

Under special circumstances, if you have trouble swallowing the whole capsule can be swallowed its contents after opening or dissolving the capsule, and you can mix the contents of a capsule with slightly acidified liquid (juice, yogurt), and use the suspension for 30 min.

Overdose

Symptoms: visual disturbances, drowsiness, agitation, confusion, headache, increased sweating, dry mouth, nausea, arrhythmia.

Treatment: perform symptomatically. Specific antidote exists.

Drug Interactions

Long-term use of omeprazole 20 mg 1 time / day in combination with caffeine, theophylline, piroxicam, diclofenac, naproksenom, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, chinidin and estradiol did not lead to a change in their concentrations in plasma.

There was no interaction with omeprazole simultaneously take antacids.

Omeprazole can decrease the absorption of ampicillin esters, iron salts, itraconazole, and ketoconazole (because omeprazole increases the pH of the stomach).

As an inhibitor of cytochrome P450, omeprazole may increase concentration and reduce the excretion of diazepam, indirect anticoagulants, phenytoin, in some cases may require a reduction of doses of these medicines.

At the same time receiving increased absorption of omeprazole and clarithromycin.

To the top

Drug prescription.

Terms and Conditions of storage

List B. The drug should be stored protected from moisture away from children at a temperature of 25 ° C. Shelf life - 2 years (when stored in a blister pack), 3 years (when stored in a plastic pencil box).

Tavanic

Composition, structure and packing

Coated tablets pale yellowish-pink, oblong, biconvex, with a dividing groove.

1 tab.

levofloxacin gemigidrat 256.23 mg

which corresponds to the content of levofloxacin 250 mg.

Excipients: krospovidon, methylhydroxypropylcellulose, microcrystalline cellulose, sodium stearyl fumarate, macrogol 8000, talc, titanium dioxide (E171), iron oxide red (E172), iron oxide yellow (E172).

Coated tablets pale yellowish-pink, oblong, biconvex, with a dividing groove.

1 tab.

levofloxacin gemigidrat 512.46 mg

which corresponds to the content of levofloxacin 500 mg.

Excipients: krospovidon, methylhydroxypropylcellulose, microcrystalline cellulose, sodium stearyl fumarate, macrogol 8000, talc, titanium dioxide (E171), iron oxide red (E172), iron oxide yellow (E172).

Solution for infusion transparent, greenish-yellow.

1 ml of levofloxacin gemigidrat 5.12 mg.

which corresponds to the content of levofloxacin 5 mg.


1 vial. levofloxacin gemigidrat 512.46 mg

which corresponds to the content of levofloxacin 500 mg.

Excipients: sodium chloride, concentrated hydrochloric acid, sodium hydroxide, water d / and.

Clinico-pharmacological group: antibacterial fluoroquinolone group.

Pharmacological action

Antimicrobial group of fluoroquinolones, ofloxacin isomer levogyrate. It has a wide spectrum of antimicrobial action. Levofloxacin blocks DNA-gyrase (topoisomerase II) and topoisomerase IV, and crosslinking violates supercoiling of DNA, inhibits DNA synthesis, causes profound morphological changes in the cytoplasm, cell wall and membranes.

Levofloxacin is active against most strains of microorganisms in the conditions in vitro, and in vivo. In vitro sensitive (IPC ≤ 2mg/ml) aerobic Gram-positive microorganisms: Corynebacterium diphtheriae, Enterococcus spp. (Including Enterococcus faecalis), Listeria monocytogenes, Staphylococcus spp. (Coagulase metitsillin-chuvstvitelnye/metitsillin-umerenno sensitive strains), Staphylococcus aureus (methicillin-sensitive strains), Staphylococcus epidermidis (methicillin-chuvstvitelnye strains), Staphylococcus spp. (CNS), Streptococcus spp. Group C and G (including Streptococcus agalactiae, Streptococcus pneumoniae (penitsillin-chuvstvitelnye/umerenno sensitive / resistant strains), Streptococcus pyogenes, Streptococcus viridans (penitsillin-chuvstvitelnye/rezistentnye strains), aerobic gram-negative microorganisms: Acinetobacter baumannii, Acinetobacter spp ., Actinobacillus actinimycetemcomitans, Citrobacter freundii, Eikenella corrodens, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter spp. (including Enterobacter cloacae), Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae (ampitsillin-chuvstvitelnye/rezistentnye strains), Haemophilus parainfluenzae, Helicobacter pylori, Klebsiella spp. (including Klebsiella oxytoca, Klebsiella pneumoniae), Moraxella cattaralis (producing strains and β-lactamase neprodutsiruyuschie), Morganella morganii, Neisseria gonnorrhoeae (producing strains and neprodutsiruyuschie penicillinase), Neisseria meningitidis, Pasteurella spp. (including Pasteurella conis, Pasteurella dagmatis, Pasteurella multocida), Proteus mirabilis, Proteus vulgaris, Providencia spp. (including Providencia rettgeri, Providencia stuartii), Pseudomonas spp. (in t. h. Pseudomonas aeruginosa), Salmonella spp., Serratia spp. (Serratia marcescens); anaerobic microorganisms: Bacteroides fragilis, Bifidobacterium spp., Clostridium perfringens, Fusobacterium spp., Peptostreptococcus spp., Propionibacterum spp., Veilonella spp.; other microorganisms: Bartonella spp., Chlamydia pneumoniae, Chlamydia psittaci, Chlamydia trachomatis, Legionella pneumophila, Legionella spp., Mycobacterium spp. (including Mycobacterium leprae, Mycobacterium tuberculosis), Mycoplasma hominis, Mycoplasma pneumoniae, Rickettsia spp., Ureaplasma urealyticum.

Levofloxacin is moderately active (IPC ≥ 4 mg / L) against aerobic gram-positive microorganisms: Corynebacterium urealiticum, Corynebacterium xerosis, Enterococcus faecium, Staphylococcus epidermidis (methicillin-resistant strains), Staphylococcus haemolyticus (methicillin-resistant strains), aerobic gram-negative organisms: Burkholderia cepacia , Campilobacter jejuni, Campilobacter coli; anaerobic microorganisms: Bacteroides thetaiotaomicron, Bacteroides vulgatus, Bacteroides ovaius, Prevotella spp., Porphyromonas spp. By levofoloksatsinu resistant (IPC ≥ 8 mg / l) aerobic Gram-positive microorganisms: Corynebacterium jeikeium, Staphylococcus aureus (methicillin-resistant strains), Staphylococcus spp. (Coagulase-negative methicillin-resistant strains), aerobic gram-negative bacteria: Alcaligenes xylosoxidans; other microorganisms: Mycobacterium avium.

Pharmacokinetics

Absorption

After oral levofloxacin rapidly and almost completely absorbed from the gastrointestinal tract. Eating little effect on the speed and completeness of absorption.

When a single dose of 500 mg C max in plasma is achieved through 1.3 h and is 5.2-6.9 mg / ml. Bioavailability - 100%.

After i / in the 60-minute infusion of levofloxacin 500 mg healthy volunteers the mean C max in plasma was 6.2 ± 1.0 pg / ml, Tmax - 1.0 ± 0.1 h. The pharmacokinetics of levofloxacin is linear and predictable after a single and multiple injections of the drug. Plasma concentration profile of levofloxacin following to / in the introduction is similar to that in the pill.

Therefore, oral and / in route of administration may be interchanged.

Distribution

Binding to plasma proteins - 30-40%.

Well into the organs and tissues: lungs, bronchial mucosa, sputum, organs and urinary system, reproductive organs, bone, cerebrospinal fluid, prostate gland, polymorphonuclear leukocytes, alveolar macrophages.

The average Vd levofloxacin ranges from 89 to 112 l after single and multiple in / at a dose of 500 mg.

Metabolism

In the liver, a small part of levofloxacin is oxidized and / or dezatsetiliruetsya.

Withdrawal

When you receive a single dose of 500 mg of T1 / 2 is 6-8 hours

After a single in / in a dose of 500 mg of T1 / 2 - 6.4 ± 0.7 h.

Write mainly by the kidneys by glomerular filtration and tubular secretion.

The mean final T1 / 2 from 6 to 8 h after single and repeated administration.

About 87% of the dose excreted in the urine unchanged within 48 hours Less than 4% found in feces for the period 72 hours

Pharmacokinetics in special clinical situations

In renal insufficiency, reducing clearance of the drug and its excretion by the kidneys depends on the degree of reduction of QA.

Statement

Infectious-inflammatory diseases of mild to moderate severity caused by microorganisms sensitive to the drug:
Acute sinusitis (Oral);
exacerbation of chronic bronchitis (Oral);
infections of skin and soft tissues (for oral);
in the complex therapy of drug-resistant tuberculosis (Oral);
community-acquired pneumonia (for both dosage forms);
Complicated infections of the kidneys and urinary tract infections, including pyelonephritis (for both dosage forms);
uncomplicated urinary tract infections (for both dosage forms);
prostatitis (for both dosage forms);
septicemia / bacteremia associated with the above readings (for both dosage forms);
intra-abdominal infection (for both dosage forms). .

Dosage regimen

The drug taken by mouth or injected i / v at 250-500 mg 1-2 times / day.

Doses are determined by the nature and severity of infection, as well as the sensitivity of the parasite.

Patients with normal or slightly impaired renal function (CC> 50 ml / min) the drug is recommended to appoint the following doses.

Sinusitis: inside 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1 times / day. The treatment course - 10-14 days.

Exacerbation of chronic bronchitis: the interior of a tablet of 250 mg (250 mg levofloxacin), or 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1 times / day. The treatment course - 7-10 days.

Community-acquired pneumonia: the interior of 2 tablets of 250 mg or 1 tablet of 500 mg 1-2 times / day. (500-1000 mg of levofloxacin /) or in / - 500 mg 1-2 times / sut.Kurs treatment - 7 -14 days.

Uncomplicated urinary tract infection: the interior of a tablet 250 mg (250 mg levofloxacin) 1 times / day., Or a / c - 250 mg 1 time / sut.Kurs treatment - 3 days.

Complicated urinary tract infections (including pyelonephritis): inside of a 250-mg tablets (250 mg levofloxacin) 1 times / day., Or a / c - 250 mg 1 time / day. In severe infections dosage for i / v administration may be increased. The treatment course - 7-10 days.

Prostatitis: mouth 2 tablets of 250 mg or 500 mg 1 tablet (500 mg levofloxacin) 1 times / day., Or a / c - 500 mg 1 time / day. The course of treatment - 28 days.

Septicemia / bacteremia: inside of 2 tablets of 250 mg or 1 tablet of 500 mg 1-2 times / day. (500-1000 mg of levofloxacin /) or in / - 500 mg 1-2 times / sut.Kurs treatment - 10-14 days.

Intra-abdominal infection: inside the 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1 times / day., Or in / in - 500 mg 1 time / day. The treatment course - 7-14 days in combination with antibacterial drugs, acting on the anaerobic flora.

Infections of skin and soft tissue: the interior of a 250-mg tablets (250 mg levofloxacin) 1 times / day. Or 2 tablets of 250 mg or 1 tablet of 500 mg (500 mg levofloxacin) 1-2 times a day. (Respectively 500 -1000 mg of levofloxacin in the day). The treatment course - 7-14 days.

In the combined therapy of drug-resistant forms of tuberculosis tavanic designate the interior of 1-2 tablets 500 mg 1-2 times / day. (500-1000 mg of levofloxacin /) up to 3 months.

For elderly patients with normal renal function correct dosing regimen is not required.

If abnormal liver function does not require a special selection of doses, since tavanic metabolized in the liver in a very limited degree.

Tablets should be taken without chewing and drinking plenty of fluids (from 0.5 to 1 cup). In the selection of doses of the pills can be broken on the separation groove. The drug can be taken before meals or at any time between meals.

Tavanic drug in solution is introduced into / in drip slowly.

Duration of drug administration in a dose of 500 mg (100 ml infusion rastvora/500 mg levofloxacin) should be at least 60 minutes. The solution of the drug tavanic 500 mg/100 ml, compatible with the following infusion solutions: 0.9% sodium chloride, 5% dextrose, 2.5% Ringer's solution with dextrose, Combined Solution for parenteral nutrition (amino acid, carbohydrates, electrolytes). The solution of the drug should not be mixed with heparin or solutions with an alkaline reaction (eg, with a solution of sodium bicarbonate).

When the positive dynamics of the clinical condition of the patient within a few days of treatment to move from the i / v drip to oral medication tavanic in the same dose.

Duration of treatment with a / in the introduction, depending on the course of the disease is not more than 14 days. As the use of other antibiotics, treatment for drug tavanic for oral or in / infusion should continue for at least 48-72 h after normalization of body temperature or after the eradication of reliable agent.

If you missed taking the drug should be as soon as possible to resume the reception and then continue to take tavanic on the recommended scheme.

Patients should be cautioned against self-interruption or early termination of therapy without a doctor's instructions.

Side effect

The frequency of side effects is determined according to the following table:

often in patients 1-10 out of 100

sometimes less than 1 patient out of 100

rarely less than 1 patient in 1000

rarely less than 1 patient out of 10 000

in some cases even less

Allergic reactions: sometimes - itching and redness of the skin; rare - anaphylactic and anaphylactoid reactions (manifesting symptoms such as urticaria, bronchospasm and the possibility of severe asthma) are very rare - swelling of the skin and mucous membranes (eg, in the face, throat), sudden fall in blood pressure, shock, allergic pneumonitis, vasculitis, and in some cases - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) and erythema multiforme exudative.

Dermatologic reactions: very rare - photosensitization.

On the part of the digestive system: common - nausea and diarrhea, increased ALT, AST, and sometimes - loss of appetite, vomiting, abdominal pain, digestive disorders, rarely - increase of bilirubin in the blood serum, diarrhea with blood (in very rare cases it may be a sign of inflammation of the intestine or pseudomembranous colitis); very rarely - hepatitis.

On the part of metabolism: very rarely - hypoglycemia (manifested by a sharp increase in appetite, nervousness, sweating, trembling). Experience with other quinolones suggests that they can exacerbate existing porphyria, in some cases, this effect is not excluded the application of the drug tavanic.

From the side of the central nervous system and peripheral nervous system: sometimes - headache, dizziness and / or stiffness, drowsiness and sleep disorders are rarely - depression, anxiety, psychotic reactions such as hallucinations, paresthesias in the hands, trembling, excited state, seizures and confusion; very rare - and hearing impairment, violation taste and smell sensitivity, reduction of tactile sensitivity.

Since the cardiovascular system: rarely - tachycardia, falling blood pressure, very rarely - vascular collapse, and in some cases - lengthening the interval QT.

From the Musculoskeletal System: rare - the defeat of the tendons (including tendonitis), joint and muscle pain, very seldom - tendon rupture, such as Achilles tendon (may be bilateral in nature and occur within 48 h after treatment), muscle weakness ( is of particular importance for patients suffering from asthenic bulbar paralysis), in some cases - rhabdomyolysis.

From the urinary system: rarely - increases in serum creatinine in serum, very rarely - the deterioration of renal function until the acute renal failure (eg, due to allergic reactions - interstitial nephritis).

On the part of the hemopoietic system: sometimes - eosinophilia, leucopenia, rarely - neutropenia, thrombocytopenia (increased tendency to hemorrhage or bleeding) is very rare - agranulocytosis and the development of severe infection (accompanied by persistent or recurrent fever, inflammation of the tonsils and persistent deterioration of the well-being, in individual cases - hemolytic anemia, pancytopenia.

Other: sometimes - asthenia, very rarely - fever, allergic pneumonitis. Any antibiotic can cause changes in the microflora (bacteria and fungi), which is normally present in humans.

Local reactions: often - pain at the injection site, redness, phlebitis.

Contraindications
epilepsy;
tendon injury associated with hosting quinolones in history;
childhood and adolescence to 18 years;
Pregnancy
lactation (breastfeeding);
hypersensitivity to levofloxacin or other quinolones.

Precautions should use the drug in elderly patients due to high likelihood of concomitant reduction of renal function, with deficit of glucose-6-phosphate dehydrogenase.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Application for violations of liver function

If abnormal liver function does not require a special selection of doses, since tavanic metabolized in the liver in a very limited degree.

Cautions

In appointing the drug elderly patients should be borne in mind that this group of patients often have renal dysfunction. During treatment with tavanic possible development of an attack of convulsions in patients with previous brain damage (including stroke or severe brain injuries). Cramping may increase readiness and while applying fenbufena similar with NSAIDs or theophylline.

In applying the drug in patients with diabetes should be borne in mind that tavanic can cause hypoglycemia.

In severe pneumonia caused by pneumococcus, the use of the drug tavanic may be insufficiently effective. Nosocomial infections caused by Pseudomonas aeruginosa, may require the use of combination therapy. Despite the fact that photosensitization observed in the application of levofloxacin is very rare, to prevent its development patients must avoid exposure to sunlight or UV-irradiation.

Suspicion of pseudomembranous colitis should be lifted immediately tavanic and start appropriate treatment. In such cases, can not be applied drugs, which suppress motility.

Elderly patients when using the drug tavanic likely to develop tendonitis increases. In the application of SCS, apparently, increases the risk of tendon rupture. If you suspect tendonitis should be lifted immediately tavanic and start appropriate treatment, providing a quiescent state in defeat.

Precautions should be administered simultaneously with tavanic probenecid and cimetidine, which block the tubular secretion; under their influence excretion of levofloxacin slightly slower. This interaction has little clinical significance and may focus mainly on patients with impaired renal function.

With simultaneous application tavanic and vitamin K antagonists should monitor the status of the blood coagulation system.

If an antibiotic can be observed changes in the microflora (bacteria, fungi), which is normally present in humans. For this reason, perhaps increased multiplication of bacteria and fungi that are resistant to antibiotics (secondary infection and superinfection), which in rare cases may require additional treatment.

Experience with other quinolones suggests that they can exacerbate porphyria. Such an effect is not excluded in the application of the drug tavanic.

In the application of quinolones in patients with deficiency of glucose-6-phosphate dehydrogenase possible hemolysis. Given this, treatment tavanic this category of patients should be conducted with extreme caution.

It should strictly adhere to the recommended duration of administration, which must be at least 60 minutes for 100 ml infusion solution. Experience with levofloxacin shows that during the infusion may experience tachycardia and transient drop in blood pressure. In rare cases it may be vascular collapse. If during infusion observed pronounced decrease in BP, the introduction of an immediate cease.

Use in pediatrics

Tavanic contraindicated for the treatment of children and adolescents because of the probability of destruction of articular cartilage.

Effects on ability to drive vehicles and management mechanisms

Tavanic may cause dizziness or stiffness, drowsiness, visual disturbances, and reduce ability to concentrate attention and psychomotor speed of reaction that should be considered in need of the drug in patients whose activities are related to driving, maintenance of machinery, the performance of work in unstable situation. This is especially true cases of drug interaction with alcohol.

Overdose

Symptoms: confusion, dizziness, impaired consciousness and seizures seizures by type of epileptic seizures, nausea, erosive lesions of mucous membranes. In clinical pharmacological studies with the use of levofloxacin at doses higher than average therapeutic, was observed lengthening of the interval QT.

Treatment: perform symptomatically. Levofloxacin is not displayed by dialysis. Specific antidote exists. The erroneous admission of one extra tablet of 250 mg tavanic no negative actions.

Drug Interactions

Quinolone can enhance the ability of drugs (including fenbufena and similarities with NSAIDs, theophylline), lower the threshold of convulsive readiness. The action of the drug tavanic significantly reduced, while the use of sukralfatom, magnesium or aluminum containing antacid, as well as salts of iron (the interval between doses tavanic and these drugs should be at least 2 h). Since calcium carbonate interaction was not detected.

Stain (renal clearance) levofloxacin slightly slower under the influence of cimetidine and probenecid, which has virtually no clinical significance. Tavanic causes a slight increase in T1 / 2 cyclosporine from plasma.

Simultaneous reception from the SCS increases the risk of tendon rupture.

Terms and Conditions of storage

The drug in the form of coated tablets should be stored in a dry place at temperatures not above 25 ° C.

Shelf life - 5 years

Do not use the drug after the expiration date stated on the packaging.

The drug in the form of solution for injection should be stored in a dry, dark place at temperatures not above 25 ° C.

Shelf life - 3 years.

When room lighting solution can be stored without svetozaschity no more than 3 days.

The drug should be stored out of reach of children.

Sagenit

Composition, structure and packing

Tablets are white, ploskotsilindricheskie.
1 tab.
dikalievaya salt of meso-3 ,4-di (para-sulfofenil)-hexane 100 mg



Excipients: microcrystalline cellulose, starch, stearic acid.

10 pcs. - Packaging of cellular outline (1) - packs cardboard.

10 pcs. - Packaging of cellular contour (2) - bundles of cardboard.

Clinico-pharmacological group: Protivoklimakterichesky drug

Registration № №:
Tab. 100 mg: 10 or 20 pieces. - P № 002222/01-2003, 25.02.03 outage

Pharmacological action

Protivoklimakterichesky drug.

Saguenay inhibits the gonadotrophic function of the adrenal glands. It has no estrogenic effects, but also participates in the positive and negative feedback in the hypothalamic-pituitary-ovarian system, affects the gonadotrophic function of the pituitary and hypothalamic center.

Pharmacokinetics

Data on the pharmacokinetics Saguenay is not available.

Statement

climacteric syndrome, manifested by hot flashes, sweating, sleep disturbances, irritability, depression, forgetfulness, degenerative changes in the skin and mucous membranes (brittle nails, thinning of the skin, wrinkles, dryness of mucous membranes of the urinary tract).

Dosage regimen

In climacteric syndrome Saguenay designate the interior of 50-100 mg, regardless of the meal. The daily dose is 100-200 mg, the treatment course - 30-40 days.

Side effect

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

From the central nervous system: dizziness.

On the part of the reproductive system: long-term use - metrorrhagia.

Allergic reactions: rash, edema of the eyelids.

Contraindications
metrorrhagia
Hypersensitivity to the drug's components

Precautions should be prescribed a drug for kidney failure, abnormal liver function, hyperlipoproteinaemia.

Application of pregnancy and breastfeeding

Saguenay in tablet form is not intended for use in pregnancy.

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 renal failure.

Overdose

Symptoms: metrorrhagia, hemorrhagic shock.

Treatment: removal of the drug, blood transfusions, parenteral administration of blood products.

Drug Interactions

Folic acid and thyroid medications increase the efficiency Sagenita.

Saguenay intensifies the effect of diuretics, anticoagulants, antiarrhythmics, antihypertensive drugs, reduces the effects of drugs of male sex hormones.

Terms and Conditions of storage

List B. The drug should be stored in a dry place. Shelf life - 3 years.

To the top

Drug prescription.

Rapten Rapid

Composition, structure and packing

Tablets are coated with sugar coat red, with small splashes of lighter-colored, round, biconvex.

1 tab. diclofenac potassium 12.5 mg.

Excipients: calcium hydrophosphate, corn starch, karboksimetilkrahmal sodium (Type A), colloidal silicon dioxide (anhydrous), povidone 30, magnesium stearate.

The composition of the shell: sucrose, talc, dye, crimson Ponceau E124, acacia gum, povidone 25, titanium dioxide E171, macrogol 6000.

Tablets, coated in red, with small splashes of lighter-colored, round, biconvex.

1 tab. Diclofenac Potassium 50 mg.

Other ingredients: colloidal silicon dioxide (anhydrous), calcium hydrophosphate (anhydrous), starch maize, povidone K30, magnesium stearate, sodium karboksimetilkrahmal, gum arabic, sucrose, talc, cochineal red lacquer E124, povidone K25, macrogol 6000.

Clinico-pharmacological group: NSAID.

Pharmacological action

NSAIDs. Has a marked anti-inflammatory, analgesic and antipyretic effect.

Indiscriminately inhibiting cyclooxygenase 1 and 2 (COX-1 and COX-2), diclofenac potassium violates the metabolism of arachidonic acid and inhibits the synthesis of prostaglandins (mediators, which play a major role in the pathogenesis of inflammation, pain and fever).

Analgesic and antipyretic effect Rapten Rapida tablets 12.5 mg manifested during the first 30 min after administration, but the effect lasts for 4-6 hours

Pharmacokinetics

Absorption

After oral administration the drug is rapidly and completely absorbed. Absorption of diclofenac is reduced when taking it with food. Absorption begins in the stomach, Cmax of diclofenac in plasma is reached after about 40 minutes after ingestion. The concentration in plasma is in a linear dose-dependent administration. Cmax in blood plasma after administration of 50 mg tablets of 1.3 ug / ml.

Distribution

The binding with plasma proteins (mainly albumin) is high - up to 99%. Rapidly distributed in tissues and body fluids. Penetrates the synovial fluid. At the same time Cmax of diclofenac potassium in the synovial fluid observed by 2-4 h later than in plasma. T1 / 2 of diclofenac potassium from the synovial fluid is 3-6 hours, and its concentration in the synovial fluid within 4-6 hours after taking the drug remain higher than in plasma as early as within 12 hours

Under the recommended interval between meals is no accumulation of the drug.

Metabolism

Diclofenac is metabolized in the liver. 50% of the active substance undergoes metabolism during the "first pass" through the liver. Metabolism occurs by multiple or single-hydroxylation and conjugation. Participates in the metabolism of isoenzyme CYP2C9. Pharmacological activity of metabolites is lower than that of diclofenac potassium.

Withdrawal

T1 / 2 from plasma is 1-2 hours is derived mainly kidneys: about 60% - in the form of metabolites, less than 1% - unchanged. The remainder of the drug is excreted in the bile as metabolites.

Systemic clearance is 260 ml / min.

Pharmacokinetics in special clinical situations

Pharmacokinetics does not change depending on the age of the patient.

In patients with severe renal dysfunction (CC <10 ml / min) during removal of metabolites with bile increases. At the same time increasing their concentration in the blood is not observed.

In patients with chronic hepatitis or compensated cirrhosis pharmacokinetic parameters of diclofenac are the same as that of patients without liver disease.

Changes in the pharmacokinetics of diclofenac on the background of repeated administration does not occur.

Statement

Tablets 12.5 mg pain syndrome of different origin:
sharp pains in muscles and joints (including pain in various parts of the spine);
severe headache;
severe toothache;
Primary tuberculosis,.

Addressing symptoms of colds and flu:
Acute pain in muscles and joints;
headache
sore throat;
sharp rise in body temperature.

Tablets 50 mg are used for short-term treatment (up to 7 days) of pain that accompanies the following conditions:
inflammatory diseases of the musculoskeletal system (including abscess, bursitis, myalgia);
post-traumatic pain syndromes accompanied by inflammation;
postoperative pain;
lumbago;
sciatica;
neuralgia;
toothache;
migraine;
inflammatory disease of the pelvic organs;
Primary tuberculosis,;
proctitis;
renal colic;
biliary colic;
infectious and inflammatory diseases of ENT organs with marked pain syndrome, v.t.ch pharyngitis, tonsillitis, otitis media (in the complex therapy);
fever.

Dosage regimen

12.5 mg Tablets Adults and children over 14 years, the drug is prescribed in an initial dose of 2 tabs. Next to reach the required therapeutic effect recommended to take 1-2 pills. every 4-6 hours maximum daily dose of 6 tab. (75 mg).

Patients should be aware that, without consulting a doctor, the drug should not take more than 3 days for fever and more than 5 days to treat pain. If deadlines are not achieved the desired effect, you must consult a doctor.

Tablets should be taken as a whole, without chewing, drinking water. To achieve maximum therapeutic effect of the drug should be taken before meals.

Tablets 50 mg

Dosage is determined individually according to the severity of the disease.

Adults medication prescribed in a daily dose of 100-150 mg, divided into 2-3 reception.

The maximum dose - 200 mg / day.

Adolescents over 15 years of drug administered in a daily dose of 100 mg, divided into 2 admission.

Elderly patients, particularly exhausted and debilitated patients should be prescribed the drug in the lowest effective dose.

Tablets should be taken as a whole, without chewing, drinking water. To achieve maximum therapeutic effect of the drug should be taken before meals.

Side effect

The frequency of side effects: frequent (> 1 / 100), sometimes (<1> 1 / 1000), rarely (<1> 1 / 10 000), very rarely - <1 / 10 000.

12.5 mg Tablets

On the part of the hemopoietic system: very rarely - thrombocytopenia, leukopenia, anemia (including hemolytic and aplastic anemia), agranulocytosis.

From the side of the central nervous system and peripheral nervous systems: common - headache, dizziness, rarely - drowsiness, disorientation, depression, insomnia, nightmares, irritability, psychotic disorders, very rare - paresthesia, memory loss, convulsions, anxiety, tremor, aseptic meningitis , taste disorders, cerebrovascular disorders.

From the sensory organs: often - dizziness, very rarely - tinnitus, hearing impairment, blurred vision, diplopia.

Since the cardiovascular system: very rarely - a feeling the heartbeat, pain behind the sternum, heart failure, myocardial infarction, hypertension, vasculitis.

On the part of the respiratory system: rarely - bronchial asthma (including dyspnoea); very rarely - pneumonia.

On the part of the digestive system: frequent - nausea, vomiting, diarrhea, dyspepsia, abdominal pain, flatulence, anorexia, increase in liver transaminases; rarely - gastritis, gastrointestinal bleeding, vomiting blood, diarrhea, melena, stomach ulcer or intestine (with with or without bleeding or perforation), hepatitis, jaundice, very rarely - colitis (including the blood, worsening of ulcerative colitis or Crohn's disease), constipation, stomatitis, glossitis, pathology of the esophagus, esophageal stricture orifice, pancreatitis, fulminant ( fulminant) hepatitis.

From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

Dermatological reactions: often - a rash, very rarely - as a blistering rash, eczema, erythroderma (exfoliative dermatitis), alopecia, photosensitivity, purpura.

Allergic reactions: rare - rash, anaphylactic and anaphylactoid reactions (including hypotension and shock) are very rare - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis syndrome (toxic epidermal necrolysis), allergic purpura, angioedema (including edema person).

Other: rarely - swelling.

Tablets 50 mg

On the part of the digestive system: often - NSAID-gastropathy (gastralgia and discomfort in the epigastric region, nausea, feeling of repletion, regurgitation, heartburn, diarrhea, abdominal pain, flatulence), erosive and ulcerative lesions gastrointestinal tract, perforation of the intestinal wall, bleeding from the gastrointestinal tract , dry mouth, constipation, pancreatitis, toxic hepatitis, sometimes - vomiting, decreased appetite, anorexia, stomatitis, glossitis.

From the side of the central nervous system and peripheral nervous systems: common - headache, dizziness, and sometimes - convulsions, aseptic meningitis, memory decline, depression, psychotic reactions, peripheral polyneuropathy (hypoesthesia, tremor, pain or weakness in the muscles of the arms and legs), lethargy, irritability and nervousness, anxiety, insomnia, weakness and fatigue.

From the senses: sometimes - a toxic lesion of the optic nerve, reduction of visual acuity, diplopia, scotoma, hearing loss, ringing, and tinnitus.

On the part of the urinary system: often - fluid retention, sometimes - hematuria, cystitis, thamuria, proteinuria, interstitial nephritis, nephrotic syndrome, oliguria, anuria, acute renal failure, peripheral edema.

On the part of the reproductive system: dysmenorrhea.

From the side of hematopoiesis: sometimes - agranulocytosis, hemolytic anemia, aplastic anemia, anemia associated with internal bleeding, leukopenia, neutropenia, thrombocytopenia purpura with or without her.

The respiratory system: sometimes - shortness of breath.

Dermatological reactions: often - itching, skin rash (predominantly erythematous and urticaria), ecchymosis, hyperemia of the skin, sometimes - photodermatitis.

Allergic reactions: sometimes - erythema multiforme exudative, including Stevens-Johnson syndrome, Lyell syndrome (toxic epidermal necrolysis).

Contraindications

12.5 mg Tablets
bronchial asthma;
urticaria or acute rhinitis in history in response to receiving aspirin or other NSAID (eg ibuprofen);
Since the aorto-coronary bypass surgery;
ulcer;
inflammatory bowel disease exacerbation (UC, Crohn's disease);
ulcer bleeding or perforation;
III trimester of pregnancy;
severe hepatic impairment;
renal failure severe (CC less than 30 ml / min);
heart failure, severe;
progressive renal disease;
confirmed hyperkalaemia;
hemodyscrasia;
various violations of hemostasis;
damage to bone marrow;
Children under 14 years
Hypersensitivity to the drug's components.

Tablets 50 mg
"Aspirin" asthma;
erosive-ulcerative lesions GIT (exacerbation);
bleeding from the gastrointestinal tract;
hemodyscrasia;
Various hemostatic disorders (including hemophilia);
Pregnancy
Lactation (breastfeeding);
childhood and adolescence (15 years);
hypersensitivity to NSAIDs (including aspirin).

Precautions to apply Rapten Rapid patients with severely impaired liver and kidney function in history, with QA <60 ml / min, hepatic porphyria, anemic, suffering from bronchial asthma, hypertension, ischemic heart disease, congestive heart failure, edema, erosions and ulcerative lesions GIT without exacerbation, diverticulitis, dyslipidemia, or hyperlipidemia, diabetes, severe somatic diseases, patients receiving long-term NSAIDs, elderly patients and patients in the postoperative period in chronic alcoholism and smoking.

Pregnancy and lactation

12.5 mg Tablets

In I and II trimesters of pregnancy drug prescribed only when the intended use of therapy to the mother outweighs the potential risk to the fetus and child. The use of diclofenac, like other NSAIDs, is contraindicated in the III trimester of pregnancy because of possible uterine atony and / or premature closure of ductus arteriosus.

As with other NSAIDs, diclofenac in small amounts excreted in breast milk. Therefore, to prevent adverse effects in the child Rapten Rapid is not recommended during lactation (breastfeeding).

Tablets 50 mg

Use during pregnancy and lactation (breastfeeding) is contraindicated.

Diclofenac may have a negative impact on female fertility, and therefore not advisable to appoint Rapten Rapid women planning pregnancy.

Application for violations of liver function

Precautions appoint Rapten Rapid disorders of liver function.

Application for violations of renal function

Precautions appoint Rapten Rapid disorders of kidney function.

Cautions

In the application of NSAIDs is likely the development of gastrointestinal bleeding and ulcers of the digestive tract, sometimes complicating perforation, without prior symptoms or the presence of similar attacks in the history of the patient. These complications can have serious consequences especially for the elderly. If you have similar symptoms the drug should be lifted immediately.

The risk of gastrointestinal bleeding increases with increasing doses of NSAIDs in patients with peptic ulcer history, especially in case of complications of the disease bleeding and perforation, as well as elderly patients. To reduce the risk of complications of therapy should be initiated and maintained at the minimum effective dose for the possibility of combined therapy and the use of protective equipment (eg, proton pump inhibitors or misoprostol). In the appointment of diclofenac in patients with available pathology of the gastrointestinal tract (ulcers, hemorrhage, perforation) history, it is necessary to conduct therapy with careful medical supervision and compliance with particular caution. Caution should be observed while the appointment of drugs that may increase the risk of erosive and ulcerative lesions or bleeding from the gastrointestinal tract (such as systemic corticosteroids, anticoagulants, platelet aggregation inhibitors or selective serotonin reuptake inhibitors).

Patients suffering from ulcerative colitis or Crohn's disease, therapy should be administered under close medical supervision, because as a result of taking diclofenac can occur exacerbation of these diseases.

The use of diclofenac should be discontinued at the first sign of the emergence of skin rashes, lesions of the mucous membranes, and when you have other signs of hypersensitivity to the drug's components.

In patients who previously did not use diclofenac during treatment may occur allergy, including anaphylactic / anaphylactoid reactions.

It should be remembered that in connection with their pharmacological properties diclofenac may mask the symptoms associated with infectious diseases.

Avoid the simultaneous application of diclofenac with systemic NSAID (including a selective inhibitor of COX-2), since there is no evidence of a beneficial effect as a result of synergy, and there are no data on possible side effects.

Caution must be exercised in the appointment of the drug in elderly patients. Debilitated elderly patients and elderly patients with low body weight should appoint a drug in the lowest effective dose.

In patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (nasal polyps), COPD, or chronic infection of the respiratory tract (especially related to allergic rhinitis-like symptoms), reactions to drugs from the group of NSAIDs in the form of asthma attacks, Quincke's edema or hives develop more often than usual. In the appointment of the drug in such patients should be very careful (readiness for urgent medical intervention).

In the appointment of diclofenac in patients with impaired liver function should involve careful monitoring, because the state of such patients may deteriorate. During the application Rapten Rapida can increase the activity of one or more liver enzymes. Therefore, long-term therapy the drug showed regular study of indicators of liver function. If violations of the functional parameters of liver persist or intensify, or if you develop complaints or symptoms suggestive of liver disease, and if there are other side effects (eg, eosinophilia, rash etc.), the drug should be cancel. It must be borne in mind that hepatitis on a background of taking diclofenac can occur without prodrome. Caution must be exercised in the appointment of the drug to patients with hepatic porphyria, since receiving diclofenac can provoke attacks.

As has been reported that during treatment with NSAIDs may be fluid retention and edema should be very careful when appointing Rapten Rapida patients with impaired renal function and heart failure, arterial hypertension, a history of elderly patients, while taking diuretics or drugs that have a significant impact on renal function, as well as patients that have a significant decrease in BCC of any etiology, eg, in the period before or after major surgery. In such cases, the use of diclofenac as a precaution it is recommended to monitor kidney function. After the cessation of therapy is usually restored the original settings. Rapten Rapid recommended for use within a few days.

In the appointment of the drug for a long time shows a systematic pattern control peripheral blood, liver, kidneys, study stool test for blood.

Rapten Rapid may temporarily inhibit platelet aggregation. Therefore, in patients with disorders of hemostasis requires careful control of the laboratory parameters.

During the reception Rapten Rapid should avoid alcohol.

Effects on ability to drive vehicles and management mechanisms

In the period of treatment there may be some reduction of speed of psychomotor reactions. Therefore, patients taking the drug, must refrain from activities requiring attention and rapid psychomotor reactions.

Overdose

Symptoms: disorders of the digestive system, hypotension, nephrotoxicity (up to acute renal failure), dizziness, headache, hyperventilation lungs, clouding of consciousness in children - Myoclonic seizures, nausea, vomiting, abdominal pain, bleeding, abnormal liver function and kidney.

Treatment: gastric lavage, followed by the appointment of activated charcoal, symptomatic therapy. Forced diuresis, hemodialysis ineffective.

Drug Interactions

Tablets 12.5 mg and 50 mg tablets

With simultaneous application of diclofenac may increase the concentration of lithium and digoxin in the blood plasma.

At the same time taking a diuretic or other antihypertensive drugs (eg, beta-blockers, ACE inhibitors), diclofenac can reduce the severity of antihypertensive action.

The simultaneous use potassium-sparing diuretics may increase potassium levels in blood serum.

Simultaneous use of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of adverse events from the gastrointestinal tract.

Take special care is required when a joint appointment with anticoagulants or platelet aggregation inhibitor, because, while taking diclofenac with these drugs increases the risk of bleeding.

In clinical studies revealed that the simultaneous application of diclofenac and oral hypoglycemic agents is possible and thus the effectiveness of the latter does not change. However, we know of individual cases, as hypoglycemia and hyperglycemia, which required dose change hypoglycemic drugs during the application of diclofenac.

Caution must be exercised in the appointment of NSAIDs for less than 24 hours before or after taking methotrexate, as in such cases may increase the concentration of methotrexate in blood and increase its toxic effects.

Effect of NSAIDs on the synthesis of prostaglandins in the kidney may increase the nephrotoxicity of cyclosporine.

There are some reports on the development of seizures in patients treated with both antibacterial drugs quinolone derivatives and NSAIDs.

Antacids, such as aluminum hydroxide and magnesium hydroxide, can slow the absorption of diclofenac, but not affect the total amount of absorbed drug.

Concomitant therapy selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline) accompanied by increased risk of gastrointestinal bleeding.

Tablets 50 mg

The drug reduces the effectiveness of hypnotic drugs.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

At simultaneous application with paracetamol increases the risk of nephrotoxic effects of diclofenac.

Tsefamandol, cefoperazone, tsefotetan, valproic acid and plikamitsin increase the incidence of gipoprotrombinemii.

Preparation of gold increases the influence of diclofenac on the synthesis of prostaglandins in the kidneys that increases the nephrotoxicity.

Simultaneous with the appointment of ethanol, colchicine, corticotrophin, and St. John's wort preparations increases the risk of bleeding from the gastrointestinal tract.

Diclofenac increases the effects of drugs causing photosensitivity.

Drugs that block tubular secretion, increase plasma concentration of diclofenac, thereby increasing its toxicity.

Terms and Conditions of storage

The product should be stored out of reach of children, dry, dark place at a temperature of 15 ° to 25 ° C.

Expiration pills 12.5 mg - 2 years.

Expiration tablets 50 mg - 3 years.