Carbamazepine - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Antiepileptic drug, a derivative of dibenzazepine. It blocks sodium channels, inhibits the release of neurotransmitters. Has anticonvulsant, normotimichesky, antipsychotic, antidiuretic and analgesic effect.

Pharmacokinetics:Bioavailability more than 70%. In the gastrointestinal tract is absorbed slowly, but almost completely. The connection with plasma proteins is 76%, in children it is slightly less, up to 59%. Biotransformation is exposed in the liver with the help of the enzyme CYP3A4. It induces its own metabolism by the mechanism of positive feedback. The half-life at the introduction of a single dose to volunteers 25-65 years is 8-29 hours. The clearance is 0.025-0.54 l / h × kg. Elimination of the kidneys by 72%, in the unchanged form, only 3% is excreted; with feces stand out the remaining 28%.

Indications:Epilepsy (excluding petit mal): partial forms of seizures with complex and simple symptoms, primary and secondary generalized forms of seizures with a tonic-clonic component, mixed forms of seizures. Acute manic states.Affective and schizoaffective psychoses. Pain syndrome of mainly neurogenic genesis: trigeminal neuralgia, essential glossopharyngeal neuralgia, diabetic polyneuropathy accompanied by pain. Abstinence syndrome - for the treatment of symptoms of alcohol withdrawal, dependence and for the prevention of seizures. Non-diabetes mellitus (of any origin). Polydipsia (used because of its antidiuretic effect).

ICD-10

V.F00-F09.F06.3 Organic mood disorders [affective]

V.F00-F09.F07.2 Postcontasia syndrome

V.F10-F19.F10.3 Mental and behavioral disorders caused by alcohol use - withdrawal symptoms

V.F20-F29.F20 Schizophrenia

V.F20-F29.F25 Schizoaffective disorder

V.F20-F29.F29 Inorganic psychosis, unspecified

V.F30-F39.F30 Manic episode

V.F30-F39.F32 Depressive episode

V.F30-F39.F34.0 Cyclothemia

V.F40-F48.F40.0 Agoraphobia

V.F40-F48.F41.0 Panic disorder [episodic paroxysmal anxiety]

V.F40-F48.F41.1 Generalized anxiety disorder

V.F40-F48.F43.0 Acute stress reaction

V.F40-F48.F43.1 Post-Traumatic Stress Disorder

V.F40-F48.F43.2 Disorder of adaptive reactions

V.F40-F48.F44 Dissociative [conversion] disorders

V.F40-F48.F45 Somatoform disorders

V.F60-F69.F60 Specific personality disorders

V.F60-F69.F63 Disorders of habits and drives

V.F70-F79.F79 Mental retardation, unspecified

VI.G40-G47.G40 Epilepsy

VI.G50-G59.G50.0 Neuralgia of the trigeminal nerve

VI.G50-G59.G52.1 Lesions of the glossopharyngeal nerve

XIII.M70-M79.M79.2 Neuralgia and neuritis, unspecified

XVIII.R25-R29.R25.2 Cramp and spasm

XVIII.R50-R69.R52 Pain, not elsewhere classified

Contraindications:Hypersensitivity (including tricyclic antidepressants), simultaneous administration of MAO inhibitors, disturbance of bone marrow hematopoiesis, anemia, leukopenia, acute porphyria in history, AV blockade, cardiac and / or liver failure, chronic renal failure, hyponatremia of dilution (inadequate secretion syndrome antidiuretic hormone, hypopituitarism, hypothyroidism, insufficiency of the adrenal cortex), angle-closure glaucoma or increased intraocular pressure, prostatic hyperplasia, diabetes mellitus, pregnancy, breast-feeding.

Carefully:Diseases of the cardiovascular system, old age.

Pregnancy and lactation:The action category for the fetus is FDA-D. The drug has been shown to have a teratogenic and embryotoxic effect.If necessary, use during pregnancy (especially in the first trimester) and during lactation should carefully weigh the expected benefit of treatment for the mother and the risk to the fetus or child. Wherein carbamazepine it is recommended to use only in the form of monotherapy in the lowest effective doses. Women of childbearing age during the treatment with carbamazepine are recommended to use non-hormonal contraceptives. Breast milk penetrates up to 60% of the mother's dose. Do not use during breastfeeding.

Dosing and Administration:The drug is taken inwards, while eating.

The minimum single dose is 400 mg.

Maximum daily doses: when ingested by adults and adolescents 15 years and older - 1.2 grams per day, children - 1 g per day. The average dose of 400 mg 2-3 times a day.

Treatment begins with small doses, gradually increased at an interval of a week to an adequate response of the patient. The daily dose is taken with a meal in 3-4 divided doses. Cancel slowly (abrupt cancellation can cause status epilepticus!)

The daily dose in children is not more than 1 g. Assign in a dosage of 10-20 mg / kg per day in several doses. In children, it is especially effective for relieving the symptoms of anxiety and depression, as well as reducing irritability and aggressiveness (epilepsy).

In the treatment of elderly patients and patients with hypersensitivity, the initial dose is 100 mg twice a day.

Side effects:Blurred vision or double vision, nystagmus, impaired coordination of movements, tremor, confusion, dizziness, drowsiness, headache, behavior change.

Allergic reactions - rash, Stevens-Johnson syndrome.

Lupus-like syndrome: skin rash, fever, arthralgia, myalgia.

Severe diarrhea, nausea.

Aplastic anemia, agranulocytosis, eosinophilia, leukopenia, pancytopenia, thrombocytopenia, adenopathy and lymphadenopathy.

Overdose:Symptoms: athetia, athetoid limb movements and hyperkinesis, dysmetry, hyper and hyporeflexia, motor anxiety, convulsions, muscle twitching, trembling, dizziness, drowsiness, mydriasis, tachycardia, hyper- or hypotension, opisthotonus, respiratory depression, shock, oliguria or ishuria, anuria .

Treatment symptomatic, artificial ventilation.

Interaction:Anticoagulants (coumarin and indanedione derivatives), other anticonvulsants (clonazepam, primidon, phenytoin, barbiturates, succinamides, preparations of valproic acid), estrogen-containing drugs (including contraceptives), quinidine, glucocorticoids, tricyclic antidepressants - a decrease in their effectiveness due to increased metabolism.

Valproic acid is an increase in the concentration of carbamazepine metabolite, and accordingly the toxicity of carbamazepine.

Verapamil, diltiazem, isoniazid, clarithromycin, propoxyphene, cimetidine, erythromycin - an increase in the toxicity of carbamazepine due to an increase in its concentration.

Halothane, isoniazid, methoxyflurane, paracetamol, enflurane - an increase in hepatotoxicity.

Inhibitors of carbonic anhydrase - an increased risk of osteogenesis disorders.

MAO inhibitors, including furazolidone and procarbazine - hyperpyrexia, hypertensive crisis, convulsions, death. Between taking these medications, a break of at least 14 days is mandatory.

Methoxyflurane, lithium preparations - increased risk of nephrotoxicity.

Oral contraceptives - a decrease in the effectiveness of oral contraceptives, which requires an additional appointment of non-hormonal contraceptives.

Special instructions:Abrupt cancellation of carbamazepine can cause an epileptic status!

Monitoring: hepatic transaminases, bilirubin, urea, ionized calcium, peripheral blood (including platelets, reticulocytes) - before treatment, weekly 1 month, then monthly.

Drinking alcoholic beverages during treatment is prohibited.

Carbamazepine is not used in atypical or generalized small epileptic seizures, myoclonic or atonic epileptic seizures.

Do not use to relieve normal pain; as a preventive agent during long periods of remission of trigeminal neuralgia.

Antiepileptic drugs can increase folate deficiency during pregnancy (one of the possible causes of fetal development disorders), therefore, during the treatment period an additional intake of folic acid is recommended.

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Instructions

Carbamazepine (Carbamazepinum)