Carbamazepine is an anticonvulsant drug with a psychotropic, neurotropic, and antidiuretic effect.
Release form and composition
Available in the form of tablets - 10 pcs. in blisters, 1, 2, 3, 4 or 5 packs in a carton box.
The active ingredient of the drug is carbamazepine, in 1 tablet it contains 200 mg.
Auxiliary components: povidone (polyvinylpyrrolidone), potato starch, polysorbate (tween-80), talc, colloidal silicon dioxide (aerosil) and magnesium stearate.
Indications for use
- Epilepsy (as a single agent or as part of a complex therapy): generalized tonic-clonic seizures, complex and simple partial seizures (including loss of consciousness) with or without secondary generalization, mixed forms of epileptic seizures;
- Acute manic states;
- Preventing exacerbations or reducing the severity of clinical manifestations in the framework of maintenance therapy of bipolar affective disorders;
- Neuralgia of the trigeminal nerve (including idiopathic and multiple sclerosis), as well as idiopathic neuralgia of the glossopharyngeal nerve;
- Polydipsia and polyuria of neurohormonal nature with diabetes insipidus;
- Pain syndrome due to diabetic neuropathy;
- Alcohol withdrawal syndrome (as part of combination therapy).
- Hepatic porphyrias;
- The oppression of bone marrow hematopoiesis in history;
- AV blockade;
- The period of administration of MAO inhibitors, as well as within 2 weeks after their cancellation;
- Lactation period;
- Hypersensitivity to the drug or chemically similar drugs (tricyclic antidepressants).
Special supervision during treatment with carbamazepine necessary elderly, pregnant women, patients with benign prostatic hyperplasia, hypothyroidism, hyponatremia dilutions, elevated intraocular pressure, renal / hepatic / cardiac insufficiency, low platelets or leukocytes, mixed forms of epileptic seizures including absence.
Dosing and Administration
The drug should be taken orally with a small amount of liquid, regardless of the meal.
In epilepsy, carbamazepine is usually prescribed as a single agent. Treatment begins with a small dose, which is gradually increased until the optimal therapeutic effect is achieved. The initial dose for adults is 100-200 mg 1-2 times a day, the maximum allowable daily dose is 2000 mg. Children older than 5 years are prescribed 100 mg per day, if necessary, gradually (1 time per week), the dose is increased by 100 mg. The starting dose for children under 5 years old is 20-60 mg per day, then every 2 days it is increased by 20-60 mg. The supporting daily dose for children is 10-20 mg per kilogram of weight in 2-3 doses.
Treatment of trigeminal neuralgia or glossopharyngeal nerve begins with a daily dose of 200-400 mg. If necessary, it is increased daily, but not more than 200 mg until pain ceases (basically, 600–800 mg / day is enough), and then reduced to the minimum effective. The initial dose for elderly patients is 100 mg 2 times a day.
The average dose for alcohol withdrawal syndrome is 200 mg 3 times a day. In severe cases, the first few days are prescribed 400 mg 3 times a day and combine carbamazepine with detoxification therapy, sleeping pills and sedatives.
With polyuria and polydipsia with diabetes insipidus, the average dose for adults is 200 mg 2-3 times a day, the optimal dose for children is selected depending on body weight and age.
In the case of pain in diabetic neuropathy, 200 mg is prescribed 2 to 4 times a day.
In the framework of maintenance therapy of bipolar affective disorders and in acute manic conditions, the average daily dose is 200-600 mg in 2-3 doses, the maximum allowable is 1600 mg. Treatment begins with a low dose and then it is gradually increased. In acute cases, a rapid increase in dose is allowed.
- Central nervous system (CNS): drowsiness, ataxia, fatigue, dizziness, diplopia, headache, taste and accommodation disorders, tics, oculomotor disturbances, muscular dystonia, nystagmus, tremor, orofacial dyskinesia, peripheral neuropathy, irotetotoidoidnyy, iopathic dystrophy, orofacial dyskinesia, peripheral neuropathy, iodine disorder, tremor , paresis, neuroleptic malignant syndrome;
- Mind: auditory and visual hallucinations, anxiety, anorexia, aggressive behavior, disorientation, depression, agitation, increased psychosis;
- Skin and its appendages: allergic and exfoliative dermatitis, systemic lupus erythematosus, erythroderma, pruritus, urticaria, Stevens-Johnson syndrome, photosensitivity reactions, toxic epidermal necrolysis, erythema nodosum and multiforme, purpura, skin pigmentation disorders, acne, hair loss There are some isolated cases of hirsutism, but the causal relationship with taking carbamazepine has not been reliably established;
- Hemorrhaging system: eosinophilia
- Hepatobiliary system: hepatitis (hepatocellular, cholestatic or mixed type), jaundice, granulomatous hepatitis, increased gamma-glutamyl transferase, alkaline phosphatase and transaminase, hepatic insufficiency;
- Gastrointestinal (GI): dry mouth, abdominal pain, diarrhea or constipation, nausea and / or vomiting, stomatitis, glossitis, pancreatitis;
- Cardiovascular system (CVS): AV blockade with fainting, bradycardia, decrease or increase in blood pressure, intracardiac conduction disorders, arrhythmia, congestive heart failure, collapse, worsening of ischemic heart disease, thromboembolism, thrombophlebitis;
- Endocrine system and metabolism: fluid retention, edema, weight gain, increased prolactin levels (including accompanied by galactorrhea, gynecomastia), triglyceride concentrations, thyroid stimulating hormone and cholesterol (including high density lipoprotein cholesterol), reduced thyroxine and triiodothyronine concentrations, impaired bone tissue metabolism (which leads to osteomalacia), hyponatremia and reduced plasma osmolarity, which in some cases leads to water intoxication (dilution hyponatremia), rovozhdayuscheysya vomiting, disorientation, headache, and neurologic disorders up to lethargy;
- Urinary system: urinary retention or frequent urination, albuminuria, oliguria, hematuria, azotemia, renal failure, interstitial nephritis, impaired spermatogenesis, disorders of sexual function;
- The musculoskeletal system: muscle pain and weakness, arthralgia, convulsions;
- Sense organs: increased intraocular pressure, clouding of the lens, conjunctivitis, taste disturbances, hearing loss;
- Respiratory system: hypersensitivity reactions, manifested by shortness of breath, fever, pneumonia or pneumonitis;
- Hypersensitivity reactions: angioedema, anaphylactic reaction, aseptic meningitis with eosinopathy and myoclonus, multiorgan delayed-type hypersensitivity with skin rashes, fever, vasculitis, vasculitis, eosinophilia, leukopenia , other organs can also be involved - pancreas, kidneys, lungs, large intestine, myocardium;
- Laboratory indicators: hypogammaglobulinemia.
Symptoms of overdose:
- CNS: disorientation, hallucinations, agitation, feeling of mist before eyes, drowsiness, dysarthria, dyskinesia, ataxia, nystagmus, hyperreflexia, alternating hyporeflexia, psychomotor disorders, hypothermia, myoclonus, mydriasis, convulsions, depression of central nervous system, right up to
- SSS: decrease or increase in blood pressure, tachycardia, conduction disturbance and cardiac arrest;
- Gastrointestinal tract: delayed evacuation of food from the stomach or vomiting, decreased motility of the colon;
- Respiratory system: pulmonary edema, respiratory depression;
- Urinary system: oliguria or anuria, fluid and urine retention, dilution hyponatremia;
- Laboratory indicators: increased muscle fraction of CPK, hyperglycemia, hyponatremia, metabolic acidosis.
Specific antidote carbamazepine does not exist. In the event that the patient has taken too high a dose of the drug, it is necessary to do a gastric lavage, give activated charcoal and call a doctor, since required hospitalization and monitoring of vital functions. Hemodialysis, forced and peritoneal diuresis are ineffective (dialysis is indicated only when severe intoxication is combined with renal failure). Symptomatic treatment, including hemosorption on coal sorbents.
Before prescribing the drug, as well as periodically during the period of its use, clinical blood tests and general urine tests should be carried out, and blood urea should be determined. Patients with elevated intraocular pressure, in addition, require monitoring of this indicator.
When prescribing the drug to pregnant women, children, if used as part of combination therapy, if the frequency of epileptic seizures increases or the development of pronounced side effects occurs, the concentration of carbamazepine in plasma should be regularly determined during the entire treatment period.
At the time of treatment should refuse to take alcoholic beverages, occupations of potentially dangerous activities and driving.
Cross-reactions of hypersensitivity may occur between carbamazepine and oxcarbazepine or phenytoin.
The concentration of carbamazepine in plasma can increase inhibitors of the isoenzyme CYP 3A4. And inducers of the isoenzyme CYP 3A4 can lead to an acceleration of its metabolism and, possibly, a decrease in plasma concentration, however, the abolition of these drugs can cause a decrease in the rate of biotransformation of carbamazepine, which will lead to an increase in its level in the blood plasma.
With simultaneous use with drugs that are metabolized by the isoenzyme CYP 3A4, there is a possibility of induction of metabolism and a decrease in their concentration in plasma.
The following drugs can increase the concentration of carbamazepine and carbamazepine-10,11-epoxide in plasma: azoles (e.g., ketoconazole, itraconazole, fluconazole and voriconazole), ibuprofen, dextropropoxyphene, danazol, nefazodone, fluvoxamine, paroxetine, viloksazin, trazodone, stiripentol, fluoxetine, vigabatrin, olanzapine, loxapapine, quetiapine, terfenadine, isoniazid, loratadine, macrolide antibiotics (for example, troleandomycin, erythromycin, clarithromycin and josamycin), viral protease inhibitors for treating HIV infection (for example, ritonavi p), diltiazem, verapamil, omeprazole, dantrolene, oxybutynin, ticlopidine, acetazolamide, nicotinamide (in adults and only in high doses), and also presumably - valproic acid, desipramine, cimetidine, primidone.
The following drugs can reduce the concentration of carbamazepine in plasma: vegetable products containing St. John's wort, phenobarbital, oxcarbazepine, fensuksimid, metsuksimid, phenytoin, felbamate, fosphenytoin, aminophylline, theophylline, isotretinoin, progabid, rifampicin, primidone, cisplatin, doxorubicin.
Carbamazepine can reduce the concentration in the plasma, reduce or even completely neutralize the effects of the following drugs: tricyclic antidepressants (amitriptyline, imipramine, clomipramine, nortriptilin), oral anticoagulants (fenprocoumon, warfarin, acenokumarol, dicouleol), and the optics to help with the movement of pain, to treat the effects of the following drugs; trazodone, clobazam, doxycycline, clonazepam, tramadol, ethosuximide, oxcarbazepine, lamotrigine, primidone, felbamate, tiagabine, valproic acid, topiramate, zonisamide, praziquantel, clozapine, imatinib, halopermolde for example, dexamethasone and prednisone), levothyroxine sodium, everolimus, cyclosporine, estrogens and / or progesterone, as well as oral contraceptives (an alternative method of contraception must be selected).
In some cases, carbamazepine may increase the plasma concentration of mephenytoin.
There is evidence that during the administration of carbamazepine, the plasma phenytoin content can either increase or decrease.
Combinations to be taken into account:
- Grapefruit juice increases plasma carbamazepine;
- Carbamazepine may enhance isoniazid-induced hepatotoxicity;
- The toxic effect of carbamazepine may enhance levetiracetam;
- When used concurrently with metoclopramide, lithium, or neuroleptic agents, it is possible to increase the frequency of unwanted neurological reactions;
- The simultaneous administration of certain diuretics (furosemide, hydrochlorothiazide) can lead to the development of hyponatremia, accompanied by clinical manifestations;
- Carbamazepine may be antagonistic to the action of non-depolarizing muscle relaxants, therefore, an increase in their dose may be required, and during the period of treatment, special monitoring of the patients is necessary, because perhaps a faster than expected cessation of muscle relaxants.
Terms and conditions of storage
Store in a dark, dry place inaccessible to children at temperature up to 25 ºC.
Shelf life - 3 years.