Tegretol CRS coated pills retard 400mg N30
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Carbamazepine
Release form
Pills
Composition
Active ingredient: Carbamazepine. Concentration of active ingredient (mg): 400 mg
Pharmacological effect
Antiepileptic agent, a derivative of tricyclic aminostilbene. It is believed that the anticonvulsant action is associated with a decrease in the ability of neurons to maintain a high frequency of development of repeated action potentials through inactivation of sodium channels. In addition, it seems to be important to inhibit the release of neurotransmitters by blocking presynaptic sodium channels and developing action potentials, which in turn reduces synaptic transmission. It shows a moderate anti-manic, antipsychotic effect, as well as an analgesic effect in neurogenic pain. gaba receptors that may be associated with calcium channels may be involved in the mechanisms of action; The effect of carbamazepine on the neurotransmission modulator systems also seems to be important. The antidiuretic effect of carbamazepine may be due to the hypothalamic effect on osmoreceptors, which is mediated through adg secretion, and also due to the direct effect on the renal tubules.
Pharmacokinetics
After oral administration, carbamazepine is almost completely absorbed from the gastrointestinal tract. Plasma protein binding is 75%. It is an inducer of liver enzymes and stimulates its own metabolism. T1 / 2 is 12-29 hours. 70% is excreted in the urine (as inactive metabolites) and 30% in feces.
Indications
Epilepsy Complicated or simple partial epileptic seizures (with loss or without loss of consciousness) with or without secondary generalization. Generalized tonic-clonic epileptic seizures. Mixed forms of epileptic seizures. Acute manic states and supportive therapy of bipolar affective disorders in order to prevent exacerbations or alleviate clinical manifestations of exacerbations Alcohol withdrawal syndrome. Idiopathic trigeminal neuralgia and trigeminal neuralgia in multiple sclerosis (typical and atypical). Idiopathic neuralgia of the glossopharyngeal nerve. Pain syndrome in diabetic neuropathy.Polyuria and polydipsia of neurohormonal nature with diabetes insipidus of central origin.
Contraindications
Hypersensitivity to carbamazepine or chemically similar drugs (for example, tricyclic antidepressants) or to any other component of the drug; atrioventricular block; history of episodes of suppression of bone marrow hematopoiesis; hepatic porphyria (for example, acute intermittent porphyria, late skin porphyria, variegated porphyria); use in combination with MAO inhibitors (structural similarity with tricyclic antidepressants).
Precautionary measures
Keep out of the reach of children.
Use during pregnancy and lactation
If necessary, use during pregnancy (especially in the first trimester) and during lactation should carefully weigh the expected benefits of treatment for the mother and the risk to the fetus or child. In this case, carbamazepine is recommended to be used only as a monotherapy in the minimum effective doses. Non-hormonal contraceptives are recommended for women of childbearing age during treatment with carbamazepine.
Dosage and administration
Inside The drug can be taken with meals, after meals or in between meals. Tablets should be taken with a small amount of liquid. The drug can be used as a monotherapy, and as part of combination therapy. Appointment of Tegretol in the form of a syrup (one measuring spoon = 5 ml = 100 mg) is advisable for patients in whom ingestion of pills is difficult or requiring careful dose selection. When taking Tegretol syrup, a large maximum concentration * is reached than when taking the same dose in tablet form, it is therefore recommended to start treatment with small doses and gradually increase them to avoid: adverse reactions. Syrup should be shaken before use. When transferring a patient from taking Tegretol in pill form to taking syrup, it is recommended to take the drug in the same daily dose, but in smaller doses and more often (for example, the syrup dosage regimen is three times a day, instead of two times a day for pills). Transfer of the patient from taking Tegretol in the form of conventional pills to taking Tegretol CR of long-acting pills.Clinical experience shows that in some patients using long-acting pills, it may be necessary to increase the dose of the drug. Considering drug interactions and pharmacokinetic features of antiepileptic drugs, elderly patients should be carefully selected. Epilepsy Whenever possible, the drug should be prescribed as monotherapy. The drug is usually ineffective with small attacks (petit mal, absans) and myoclonic seizures. Treatment begins with the use of a small daily dose, which is subsequently slowly increased to achieve the optimal effect. To select the optimal dose of the drug, it is recommended to determine the concentration of the active substance in the blood plasma. When Tegretol is added to other antiepileptic drugs taken, the dose of Tegretol is increased gradually. If necessary, carry out the appropriate correction of doses of drugs taken. For adults, the initial dose of carbamazepine is 100-200 mg 1 or 2 times a day. Then the dose is slowly increased to achieve the optimal therapeutic effect; it is usually achieved at a dose of 400 mg 2-3 times a day. Some patients may need to increase the daily dose to 1600 mg or 2000 mg. In children aged 4 years and under, the recommended starting dose is 20–60 mg per day; further, the dose is increased by 20-60 mg every other day. In children over the age of 4 years, treatment can be started with the use of 100 mg / day; the dose is increased gradually, by 100 mg per week. In children under three years old, it is preferable to use the drug in the form of a syrup due to the difficulties of applying solid dosage forms in this age group. Maintenance doses: for children set at the rate of 10-20 mg / kg of body weight per day (in several doses). Age of child Daily dose 4–5 years 200–400 mg 6–10 years 400–600 mg 11–15 years 600–1000 mg Neuralgia of the trigeminal nerve The initial dose is 200–400 mg per day. It is slowly increased to the disappearance of pain (usually to a dose of 200 mg 3-4 times a day). Then the dose is gradually reduced to the minimum maintenance. The recommended initial dose for elderly patients is 100 mg 2 times a day. Alcohol withdrawal syndrome The average dose is 200 mg 3 times a day. In severe cases, during the first few days, the dose may be increased (for example, up to a dose of 400 mg 3 times a day).In severe manifestations of alcohol withdrawal, treatment begins with the use of the drug in combination with drugs that have sedative and hypnotic effects (for example, with clometiazole, chlordiazepoxide). After the resolution of the acute phase, treatment with the drug can be continued as monotherapy. Polyuria and polydipsia of a neurohormonal nature with diabetes insipidus of central origin The average dose for adults is 200 mg 2-3 times per day. In children, the dose of the drug should be reduced in accordance with the age and weight of the child. Pain in diabetic neuropathy The average dose is 200 mg 2-4 times a day. Acute manic states and maintenance treatment of affective (bipolar) disorders. The daily dose is 400-1600 mg. The average daily dose is 400-600 mg (in 2-3 doses). In the acute manic state, the dose should be increased rather quickly. With maintenance therapy of bipolar disorders in order to ensure optimal tolerability, each subsequent dose increase should be small, the daily dose increases gradually.
Side effects
Certain types of adverse reactions, for example, on the part of the CNS (dizziness, headache, ataxia, drowsiness, fatigue, diplopia), on the part of the digestive system (nausea, vomiting), as well as allergic skin reactions, are very common or the beginning of drug treatment, or when using an excessively high initial dose of the drug or in the treatment of elderly patients. Dose-dependent adverse reactions usually disappear within a few days, both spontaneously and after a temporary reduction in the dose of the drug. The development of adverse reactions on the part of the central nervous system may be a consequence of the relative overdose of the drug or significant fluctuations in the concentration of the active substance in the blood plasma. In such cases it is recommended to monitor the concentration of the active substance in the blood plasma. When assessing the frequency of occurrence of various adverse reactions, the following gradations were used: very often - more than 1/10, often - more than 1/100 - less than 1/10, sometimes - more than 1/1000 - less than 1/100 rarely - more than 1 / 10,000 - less than 1/1000, very rarely - less than 1 / 10,000, including individual messages.Mental disorders: rarely hallucinations (visual or auditory), depression, anorexia, anxiety, aggression, agitation, disorientation; very rarely - activation of psychosis. On the part of the nervous system: very often - dizziness, ataxia, drowsiness, fatigue; often - headache, diplopia, accommodation accommodation disturbances (for example, blurring of vision); sometimes abnormal involuntary movements (for example, tremor, fluttering tremor / asterixis /, muscular dystonia, tics); nystagmus; rarely, orofacial dyskinesia, oculomotor disorders, speech disorders (for example, dysarthria), choreoathetosis, peripheral neuropathy, paresthesias, paresis; very rarely - taste disorders, malignant neuroleptic syndrome. On the part of the skin and its appendages: very often - allergic dermatitis, urticaria, which can be significantly pronounced; sometimes exfoliative dermatitis, erythroderma; rarely, systemic lupus erythematosus, pruritus; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, photosensitivity reactions, erythema multiforme and nodosum, skin pigmentation disorders, purpura, acne, sweating, hair loss. Rare cases of hirsutism have been reported, but the causal relationship of this complication with the drug intake remains unclear. From the hemopoietic system: very often - leukopenia; often thrombocytopenia, eosinophilia; rarely, leukocytosis, lymphadenopathy, folic acid deficiency; very rarely agranulocytosis; aplastic anemia, pancytopenia, anemia, true red cell aplasia, megaloblastic anemia, variegated porphyria, late skin porphyria, acute intermittent porphyria, reticulocytosis, and possibly hemolytic anemia. While taking the drug may develop agranulocytosis and aplastic anemia. However, due to the fact that these conditions occur very rarely, it is difficult to quantify the risk of their occurrence. It is known that the total risk of agranulocytosis in the general population that did not receive treatment is 4.7 Cases per 1 million population per year, and aplastic anemia - 2.0 cases per 1 million population per year. On the part of the digestive system: very often - nausea, vomiting; often, dry mouth; sometimes - diarrhea, constipation; rarely - abdominal pain; very rarely -glossitestomatitis, pancreatitis. From the hepatobiliary system: very often - an increase in the level of gamma-glutamine transferase (due to induction of this enzyme in the liver), which usually has no clinical significance; often - increased blood alkaline phosphatase; sometimes - increased transaminase levels; rarely - cholestatic, parenchymal (hepatocellular) or mixed hepatitis, jaundice; very rarely granulomatous hepatitis, liver failure. Hypersensitivity reactions: rarely - multiorgan hypersensitivity of a delayed type with fever, skin rashes, vasculitis, lymphadenopathy, signs resembling lymphoma, arthralgia, leukopenia, eosinophilia, hepatosplenomegaly and altered indicators of liver function (these symptoms occur in various combinations). Other organs may also be involved (for example, lungs, kidneys, pancreas, myocardium, large intestine); very rarely, aseptic meningitis with myoclonus and peripheral eosinophilia; anaphylactic reactions to angioedema. When the above reactions of hypersensitivity occur, the use of the drug should be discontinued. Since the cardiovascular system: rarely - violations of intracardiac conduction; increase or decrease in blood pressure; very rarely - bradycardia, arrhythmias, AV blockade with syncope, vascular collapse, congestive heart failure, exacerbation of coronary heart disease, thrombophlebitis, thromboembolism (for example, pulmonary embolism). On the part of the endocrine system: often - edema, fluid retention, weight gain, hyponatremia and decrease in blood osmolarity due to the effect similar to the action of antidiuretic hormone, which in rare cases leads to water intoxication (hyponatremia dilution), accompanied by lethargy, vomiting, headache , disorientation and neurological disorders; very rarely - an increase in the level of blood prolactin, accompanied or not accompanied by such manifestations as galactorrhea, gynecomastia; changes in thyroid function parameters, a decrease in the level of L-thyroxin (free thyroxin, thyroxin, triiodothyronine) and an increase in the level of thyroid stimulating hormone,that is usually not accompanied by clinical manifestations; disorders of bone tissue metabolism (decrease in calcium and 25-hydroxy-colecalciferol in the blood), which leads to osteomalacia / osteoporosis; increasing cholesterol concentrations, including high-density lipoprotein cholesterol, and triglycerides. On the part of the urogenital system: very rarely - interstitial nephritis, renal failure, impaired renal function (eg, albuminuria, hematuria, oliguria, increased urea / azotemia), frequent urination, urinary retention, disorders of sexual function / impotence, impaired spermatogenesis (reduced sperm count) and their mobility). On the part of the senses: very rarely, violations of taste sensations, clouding of the lens, conjunctivitis, increased intraocular pressure; hearing disorders, incl. tinnitus, hyperacusia, hypoacusia, changes in perception of pitch. On the part of the musculoskeletal system: rarely muscular weakness, very rarely - arthralgia, muscle pain or cramps. On the part of the respiratory system: very rarely - hypersensitivity reactions characterized by fever, shortness of breath, pneumonitis or pneumonia. Changes in laboratory results: very rarely hypogammaglobulinemia.
Interaction with other drugs
With simultaneous use of CYP3A4 isoenzyme inhibitors, plasma concentrations of carbamazepine can be increased. With simultaneous use of the CYP3A4 system isoenzyme inducers, carbamazepine metabolism can be accelerated, its plasma concentrations can be reduced, and therapeutic effects can be reduced. use of valproic acid may reduce the concentration of carbamazepine and significantly reduce valproic acid concentration in plasma. This increases the concentration of the metabolite carbamazepine - carbamazepine-epoxide (probably due to inhibition of its conversion to carbamazepine-10,11-trans-diol), which also has anticonvulsant activity, therefore the effects of this interaction can be leveled, but more often side reactions occur - blurred vision, dizziness, vomiting, weakness, nystagmus.With simultaneous use of valproic acid and carbamazepine, a hepatotoxic effect may develop (presumably due to the formation of a secondary metabolite of valproic acid, which has a hepatotoxic effect). With simultaneous use of valpromid, metabolism in the liver of carbamazepine and its metabolite carbamazepine-epoxy decreases inhibition of the epoxide inhibition enzyme. Said metabolite possesses anticonvulsant activity but with a significant increase in plasma concentrations may be toxic deystvie.Pri simultaneous use of verapamil, diltiazem, isoniazid, dextropropoxyphene, viloksazinom, fluoxetine, fluvoxamine, cimetidine, acetazolamide, danazol, desipramine, nicotinamide (in adults, only in high doses), erythromycin, troleandomycin, josamycin, clarithromycin; with azoles (including with itraconazole, ketoconazole, fluconazole), terfenadine, loratadine, plasma concentrations of carbamazepine may be elevated with the risk of side effects (dizziness, drowsiness, ataxia, diplopia). When used simultaneously with hexamidine, the anti-convulsant effect of carbamases decreases. ; with hydrochlorothiazide, furosemide - possible reduction of sodium in the blood; with hormonal contraceptives - possible weakening of the action of contraceptives and the development of acyclic bleeding. With simultaneous use of thyroid gland hormones may increase the elimination of thyroid hormones; with clonazepam - possible increase in clearance of clonazepam and a decrease in clearance of carbamazepine; with lithium preparations - mutual enhancement of neurotoxic action is possible. With simultaneous use with primidone, a decrease in plasma plasma concentration of carbamazepine is possible. There are reports that primidone may increase the plasma concentration of a pharmacologically active metabolite, carbamazepine-10,11-epoxide. If used simultaneously with ritonavir, the side effects of carbamazepine may be enhanced; with sertraline - a decrease in sertraline concentration is possible; with theophylline, rifampicin, cisplatin,doxorubicin - may decrease the concentration of carbamazepine in the blood plasma; with tetracycline - the effects of carbamazepine may be reduced. When used simultaneously with felbamate, plasma concentrations of carbamazepine may decrease, but the concentration of the active metabolite carbamazepine-epoxide may increase, while the concentration of carbamazepine in plasma may decrease. blood plasma. Perhaps the mutual weakening of the anticonvulsant action, and in rare cases - its strengthening.
special instructions
Carbamazepine is not used for atypical or generalized minor epileptic seizures, myoclonic or atonic epileptic seizures. It should not be used to relieve ordinary pain; as a prophylactic during prolonged periods of remission of the trigeminal neuralgia. It is used with caution in case of concomitant diseases of the cardiovascular system, marked disorders of the liver and / or kidneys, diabetes mellitus, increased intraocular pressure, with a history of hematological reactions to the use other drugs, hyponatremia, urinary retention, increased sensitivity to tricyclic antidepressants, with indications of a history of interruption of treatment arbamazepinom, as well as children and elderly patients vozrasta.Lechenie should be under the supervision of a physician. With long-term treatment, it is necessary to monitor the blood picture, the functional state of the liver and kidneys, the concentration of electrolytes in the blood plasma, and an ophthalmologic examination. Periodic determination of the level of carbamazepine in the blood plasma is recommended to monitor the efficacy and safety of treatment. Not less than 2 weeks before starting therapy with carbamazepine, it is necessary to discontinue treatment with MAO inhibitors. Avoid alcohol consumption during the treatment period. Influence on the ability to drive motor vehicles and control mechanisms should refrain from engaging in potentially hazardous activities that require increased attention, speed of psychomotor reactions.