• Code CAS
Most popular brand: Tegretol
Active ingredient: Carbamazepine
Available dosage forms: 100, 200, 400 mg
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Carbamazepine general information
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Carbamazepine (Carbamazepine): instruction, and the use of a formula
Feature substance carbamazepine
A white or almost white crystalline powder. Practically insoluble in water, soluble in ethanol and acetone. Molecular weight 236,27.
Mode of action – an anticonvulsant, antiepileptic, antipsychotic, timolepticheskoe, normotimicheskoe, analgesic.
Does sodium channels of membranes hyperactive nerve cells, reduces the effect of excitatory amino acid neurotransmitter (glutamate, aspartate), enhances brake (GABAergic) processes and the interaction with the central adenosine receptors. Antimanic properties are due to inhibition of metabolism of dopamine and norepinephrine. Anticonvulsant action is manifested in the partial and generalized seizures (grand mal) . Effective (especially in children and adolescents) for the relief of symptoms of anxiety and depression, as well as reduce irritability and aggression (epilepsy). Prevents attacks of trigeminal neuralgia, reduces the severity of the clinical manifestations of alcohol withdrawal (including agitation, tremor, gait disturbance) and reduces seizure activity. When diabetes insipidus reduces urine output and thirst.
In the digestive tract is absorbed, albeit slowly, but almost completely; Food does not affect the rate and extent of absorption. C max at a single dose of conventional tablets is achieved after 12 hours. For a single or reappointment retard tablets C max (25% less than after the usual pill) indicated within 24 . h retard form reduces daily fluctuations in the plasma level (determined in 1 – 2 weeks) without changing the minimum value of the equilibrium concentration. Bioavailability retard tablets received in a 15% lower than that after applying al. Dosage forms. Linking blood protein is 70 – 80%. The cerebrospinal fluid and saliva concentrations are proportionately disconnected protein active ingredient (20 – 30%). Penetrates into breast milk (25 – 60% of plasma levels) and the placental barrier. The apparent volume of distribution is 0,8 – 1,9 l / kg. Biotransformed in the liver (mainly epoxy path) to form several metabolites ; 10,11 – trans – diol derivative conjugates and glucuronic acid monogidroksilirovannye derivatives, and N – glucuronide. T 1/2 ; 25 – 65 hours, with a long reception ; 8 – 29 hours (due to induction of metabolism enzymes); in patients taking inducers monoksigenaznoy system (phenytoin, phenobarbital), T 1/2 is 8 – 10 hours after a single oral administration of 400 mg 72% of the dose is excreted by the kidneys and 28% through the intestines.. 2 is determined in the urine unchanged carbamazepine% 1% active (10,11 – epoxy derivative) and about 30% other metabolites.. In children, excretion accelerated (may be required in terms of higher doses of body weight). Starting anticonvulsant action ranging from several hours to several days (sometimes up to 1 month). Antinevralgichesky effect develops after 8 – 72 h, antimanic ; after 7 – 10 days.
Application of the substance carbamazepine
Epilepsy (excluding the petit mal ), mania, prophylaxis of manic – depressive disorders, alcohol withdrawal syndrome, trigeminal neuralgia and language – pharyngeal nerves, diabetic neuropathy.
Hypersensitivity (including the tricyclic antidepressants), AV blockade, myelosuppression or acute porphyria history.
Application of pregnancy and breastfeeding
Category effects on the fetus by FDA ; D.
Side effects of substance carbamazepine
dizziness, agitation, hallucinations, depression, aggressive behavior, activation of psychosis, headache, diplopia, accommodation disturbances, cataract, nystagmus, conjunctivitis, tinnitus, change in taste, speech (dysarthria, slurred speech) disorders, abnormal involuntary movements, peripheral neuritis, paresthesia, muscle weakness and paresis symptoms, AV block, congestive heart failure, hyper – or hypotension, thromboembolism, renal dysfunction, interstitial nephritis, nausea, vomiting, increased liver enzymes, jaundice, hepatitis, osteomalacia, violation sexual function, mild leukopenia, thrombocytopenia, disorders of hematopoiesis, hyponatremia, multiorgan delayed-type hypersensitivity, exfoliative dermatitis, lupus-like syndrome (skin rash, urticaria, pyrexia, sore throat, joint pain, weakness), Stevens – Johnson syndrome, toxic epidermal necrolysis, anaphylaxis .
Incompatible with MAO inhibitors. Increases isoniazid hepatotoxicity. It reduces the effects of anticoagulants, anticonvulsants (hydantoin derivatives or succinimides), barbiturates, clonazepam, primidone, valproic acid. Phenothiazines, pimozide, thioxanthenes enhance CNS depression; cimetidine, clarithromycin, diltiazem, verapamil, erythromycin, propoxyphene reduce metabolism (increased risk of toxicity). Decreases activity of corticosteroids, estrogens and estrogensoderjath oral contraceptives, quinidine, cardiac glycosides (induction of metabolism). Against the background of carbonic anhydrase inhibitors increases the risk of osteopenia.
Symptoms: disorientation, drowsiness, agitation, hallucinations, and coma, blurred vision, dysarthria, nystagmus, ataxia, dyskinesia, hyper – / hyporeflexia, convulsions, myoclonus, hypothermia; respiratory depression, pulmonary edema; tachycardia, hypo – / hypertension, heart failure, accompanied by loss of consciousness; vomiting, decreased motility of the colon; fluid retention, oliguria or anuria, changes in laboratory parameters: hyponatremia, possible metabolic acidosis, hyperglycemia, increased muscle creatinine phosphokinase fraction.
Treatment: induction of vomiting or gastric lavage, the appointment of activated charcoal and saline laxatives, forced diuresis. To maintain airway patency ; tracheal intubation, artificial respiration, and (or) the use of oxygen. If hypotension or shock ; plasma expanders, dopamine or dobutamine, with the appearance of seizures ; the introduction of benzodiazepines (diazepam) or other anticonvulsants (in children may increase the respiratory depression, the development of hyponatremia ;.. fluid restriction, cautious intravenouslyfusion of isotonic sodium chloride solution When combined with severe poisoning with renal insufficiency shows kidney dialysis specific antidote is available. . it is necessary to foresee the re-strengthening of the symptoms of overdose for 2 – and 3 – days after it began, due to the slow absorption of the drug.
Dosing and Administration
Inside, adult ; 100 – 1600 mg per day (depending on the indication and the severity of the disease), children ; 10 – 20 mg / kg per day in divided doses.
Precautions substance carbamazepine
Before and during therapy recommended regular blood tests (cell elements) and urine tests, monitoring of liver function. Be wary appointed with a history of heart disease, liver or kidneys, hematological disorders, elevated intraocular pressure, latent psychoses, inadequate response to external stimuli, excitement, diseases characterized by spasms of mixed character, in old age, the drivers of vehicles and persons, exploiting mechanisms. Do not suddenly stop treatment. Women are recommended folic acid supplementation (prior to pregnancy or during her); in order to prevent excessive bleeding during the last weeks of pregnancy and the newborn possible use of vitamin K.
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