Tegretol CR pills retard 200mg N50
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Active ingredients
Carbamazepine
Release form
Pills
Composition
Active ingredient: Carbamazepine (Carbamazepinum) Active ingredient concentration (mg): 2000
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: complex 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 the 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 in non-diabetes mellitus of central genesis.
Contraindications
AV-blockade; - history of episodes of suppression of bone marrow hematopoiesis or information about acute intermittent porphyria; - combination with MAO inhibitors (structural similarity with tricyclic antidepressants); or to other components of the drug.
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
The drug can be taken during, after a meal or in between meals with a small amount of liquid. The drug can be used both as monotherapy and as part of combination therapy. Tablets of prolonged action (whole tablet or half, if so prescribed by a doctor) swallow whole, without chewing, with a small amount of liquid. Since the active substance is released from the prolonged-action pills slowly and gradually, they are prescribed 2 times / day. Considering that Tegretol CR is prescribed 2 times / day, the doctor determines the optimal treatment regimen based on the recommendations given. When transferring a patient from taking regular pills to taking prolonged pills action, clinical experience shows that in some patients with long-acting pills, it may be necessary to increase the dose of the drug. Considering the drug interaction Wie and different antiepileptic drug pharmacokinetics, elderly patients a dose of Tegretol should be selected with ostorozhnostyu.Pri epilepsy in cases where this is possible, Tegretol CR should be administered in the form of monoterapii.Lechenie begin with the application of a small daily dose,which is then slowly increased to achieve the optimal effect. To select the optimal dose of the drug, it is recommended to determine the level 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 adjustment of the doses of drugs taken. For adults, the initial dose of Tegretol CR is 100-200 mg 1 or 2 times / day. Then the dose is slowly increased to achieve the optimal therapeutic effect; it is usually achieved at a dose of 400 mg / day, 2–3 times / day. Some patients may require a dose of Tegretol CR, which is 1.6 g / day or 2 g / day. In children over 4 years of age, treatment can be started with the use of the drug at a dose of 100 mg / day; the dose is increased gradually - every week by 100 mg. In children younger than 3 years old, carbamazepine is preferably used in the form of a syrup due to the difficulty of applying solid dosage forms in this age group. The maintenance doses for children are 10–20 mg / kg / day (in several doses):
Side effects
When assessing the frequency of occurrence of various adverse reactions, the following gradations were used: very often - ≥10%; often from ≥1% to <10%; sometimes from ≥0.1% to <1%; rarely from ≥0.01% to <0.1%; very rarely - <0.01%. Certain types of side effects, for example, from the CNS (dizziness, headache, ataxia, drowsiness, general weakness, diplopia), gastrointestinal tract (nausea, vomiting) or allergic skin reactions, occur more or less frequently, at the beginning of treatment with Tehretol CR, when using too much of the initial dose of the drug or in the treatment of elderly patients. Dose-dependent side effects usually disappear within a few days, both spontaneously and after a temporary reduction in the dose of the drug. The development of side effects from the central nervous system can 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 level of the active substance in the blood plasma. From the mental sphere: rarely - hallucinations (visual or auditory), depression, loss of appetite, anxiety, aggressive behavior, arousal,disorientation; very rarely - activation of psychosis. For the central nervous system and peripheral nervous system: very often - dizziness, ataxia, drowsiness, general weakness; often - headache, diplopia, accommodation accommodation disturbances (for example, blurring of vision); sometimes - abnormal involuntary movements (eg, tremor, fluttering tremor / asterixis /, dystonia, tics), nystagmus; rarely, orofacial dyskinesia, oculomotor disturbances, speech disorders (eg, dysarthria), choreoathetoid disorders, peripheral neuritis, paresthesias, muscle weakness and paresis symptoms. , remains unexplained. Dermatological reactions: very rarely - photosensitivity, erythema multiforme and nodosum, disorders of skin pigmentation , Purpura, acne, sweating, hair loss. Rare cases of hirsutism have been reported, but the causal relationship of this complication with the use of Tegretol CR remains unclear. Allergic reactions: very often allergic skin reactions, urticaria, which can be significantly pronounced; sometimes exfoliative dermatitis, erythroderma; rarely, lupus-like syndrome, pruritus; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). From the hematopoietic system: very often - leukopenia; often - thrombocytopenia, eosinophilia; rarely - leukocytosis, lymphadenopathy, folic acid deficiency; very rarely - agranulocytosis, aplastic anemia, true erythrocyte aplasia, megaloblastic anemia, acute intermittent porphyria, reticulocytosis, hemolytic anemia. While taking the drug, agranulocytosis and aplastic anemia may develop. 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. From the liver: very often - an increase in gamma levels - glutamyltransferase (due to the induction of this enzyme in the liver),which usually has no clinical significance; often - increase in alkaline phosphatase sometimes - increased transaminase levels; rarely - cholestatic, parenchymal (hepatocellular) or mixed hepatitis, jaundice; very rarely - granulomatous hepatitis, liver failure. From the side of the digestive tract: very often - nausea, vomiting; often - dry mouth; sometimes - diarrhea or constipation, abdominal pain; very rarely - glossitis, stomatitis, pankreatit.Reaktsii hypersensitivity seldom - multiorgan delayed type hypersensitivity with fever, skin rashes, vasculitis, lymphadenopathy, symptoms resembling lymphoma, arthralgia, leukopenia, eosinophilia, hepatosplenomegaly and altered liver function (indicated manifestations occur in various combinations). Other organs can also be involved (for example, lungs, kidneys, pancreas, heart, colon); very rarely, aseptic meningitis with myoclonus and peripheral eosinophilia; anaphylactic reaction, angioedema. When the above-mentioned hypersensitivity reactions occur, use of the drug should be discontinued. On the cardiovascular system: rarely, intracardiac conduction disorders, arterial hypertension or hypotension; very rarely - bradycardia, arrhythmias, AV blockade with fainting, collapse, congestive heart failure, exacerbation of ischemic heart disease, thrombophlebitis, thromboembolism. From the endocrine system and metabolism: often - edema, fluid retention, weight gain, hyponatremia and reduced osmolar plasma due to an effect similar to the action of antidiuretic hormone, which in rare cases leads to dilution hyponatremia, accompanied by lethargy, vomiting, headache, disorientation and neurological disorders; very rarely - an increase in prolactin level, accompanied or not accompanied by such manifestations as galactorrhea, gynecomastia; changes in thyroid function parameters - a decrease in the level of L-thyroxin (FT4, T4, T3) and an increase in the level of thyroid-stimulating hormone, which is usually not accompanied by clinical manifestations; disorders of bone tissue metabolism (reduction of calcium and 25-OH-colecalciferol in the blood plasma),leading to osteomalacia; in some cases - an increase in cholesterol (Xc) concentration, including Xc-HDL, and triglycerides. From the urogenital system: very rarely - interstitial nephritis, renal failure, impaired renal function (for example, albuminuria, hematuria, oliguria, urea / azotemia increase) , frequent urination, urinary retention, disorders of sexual function / impotence. On the part of the sense organs: very rarely - disorders of taste, clouding of the lens, conjunctivitis; hearing disorders, incl. tinnitus, hyperacusia, hypoacusia, changes in perception of pitch. From the musculoskeletal system: very rarely - arthralgia, muscle aches or cramps. From the respiratory system: very rarely - hypersensitivity reactions of the lungs, characterized by fever, shortness of breath, pneumonitis or pneumonia.
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 - it is possible to 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.