Carbalex

Carbalex is an anticonvulsant drug. Contains the component carbamazepine.

Indications Carbalexa

It is used for the following disorders:

• various types of epileptic seizures and epilepsy, accompanied by mental disorders;
• various manias;
• prevention of the development of manic-depressive disorders;
• neuralgia affecting the trigeminal nerve;
• diabetic neuropathy;
• withdrawal state;
• central form of diabetes insipidus.

Release form

The release of the medicinal product is realized in tablet form - 10 pieces inside a blister package. In a pack - 5 or 10 such packages.

Pharmacodynamics

As an anticonvulsant, Carbalex can have an effect in case of partial seizures (both complex and simple), against the background of which generalization of a secondary nature is observed (or not), and in addition to this, in the tonic-clonic form of seizures of a generalized type and in case of a combination of the described forms of seizures.

Clinical tests using the drug in monotherapy in people with epilepsy (especially in adolescents and children) have found its psychotropic effect, which was partially manifested by a positive effect on signs of depression and anxiety, and in addition to this, a decrease in aggression and irritability.

Data from individual tests showed that the effect of the drug on psychomotor data and cognitive activity depends on the portion size and is negative or questionable. In other tests, a positive effect was observed with respect to data characterizing the patient's ability to memorize with learning and attention.

In the form of a neurotropic substance, the drug is active in certain neurological pathologies: for example, it prevents attacks of pain in neuralgia affecting the trigeminal nerve and having a secondary or idiopathic nature. At the same time, the drug is used to reduce neurogenic pain in such disorders as spinal tabes, paresthesia caused by injuries, and postherpetic neuralgia.

In the case of alcohol withdrawal, the drug increases the seizure threshold (in this state it is lowered) and reduces the strength of the clinical symptoms of the disorder (tremor, excitability and gait disorder).

In people with central diabetes insipidus, it reduces the sensation of thirst and diuresis.

Tests confirm that in the form of a psychotropic substance, Carbalex demonstrates effectiveness in the case of such disorders:

• acute manic states;
• maintenance therapy for bipolar disorder of the manic-depressive type (both monotherapy and combination use with lithium agents, antidepressants or neuroleptics) or schizoaffective psychoses;
• psychoses of a manic nature (in combination with neuroleptics);
• acute stage of schizophrenia of a polymorphic nature.

The principle of action of carbamazepine has only been partially determined. The substance normalizes the walls of overexcited neural fibers, slows down the occurrence of repeated nerve discharges and weakens the synaptic transport of excitatory impulses.

It was revealed that the main mechanism of action of the drug is the prevention of repeated formation of sodium-dependent influence potentials in the area of depolarized neurons (blocks Na channels).

The anticonvulsant effect mainly develops with a decrease in the amount of released glutamate, as well as normalization of the nerve walls; the antimanic effect is provided by the suppression of metabolic processes of norepinephrine with dopamine.

Pharmacokinetics

When administered orally, carbamazepine is almost completely absorbed from the gastrointestinal tract; Cmax values after a single dose are noted after 12 hours.

Synthesis with blood protein is 70-80%. In the cerebrospinal fluid with saliva, values proportional to the share of the active element not synthesized with protein are formed (20-30%). The drug passes into mother's milk (25-60% of the plasma indicator) and through the placenta.

Distribution volumes are 0.8-1.9 l/kg. After a single use, the half-life is 25-65 hours, and after prolonged use - 8-29 hours (this is due to the induction of metabolic enzymes). In people using such drugs as phenobarbital or phenytoin (inducing the activity of the monooxygenase system), the half-life is 8-10 hours.

Metabolic processes of carbamazepine occur within the liver, and it is excreted mainly through the kidneys.

The prolonged effect of the drug is not tied to food intake. It is allowed to dissolve the tablets in any liquid (tea, milk, plain water or orange juice) without risking losing their effectiveness. By inhibiting enzyme activity (CYP-450-IIIA4) in the liver and stomach, grapefruit juice significantly increases the level of bioavailability of carbamazepine.

The anticonvulsant effect begins to manifest itself after several hours or several days (but sometimes this period reaches 1 month).

Dosing and administration

Use in epilepsy.

Children aged 10 years and over and adults should start taking the drug with a dose of 0.2 g (1 tablet) 2 times a day. Then the dosage is slowly increased until the patient reaches the optimal level.

Infants up to 12 months: 0.1 g per day (0.5 tablets). Children aged 1-5 years – 0.2-0.4 g per day (1-2 tablets). Children aged 6-10 years are prescribed 2-3 tablets per day (0.4-0.6 g).

Manic-depressive disorders and mania.

The serving size is often 0.4-1.6 g (2-8 tablets) per day, divided into 2-3 applications. The standard serving is 2-3 tablets per day (0.4-0.6 g).

Neuralgia affecting the trigeminal nerve.

At the initial stage, you usually need to take 1 tablet (0.2 g) 2 times a day. Later, the doctor should select a personal dosage, determining the optimal portion size. Often, about 3 tablets per day (0.6 g) are enough.

Diabetic form of neuropathy and central diabetes insipidus.

Often it is necessary to take 0.2 g of the drug (1 tablet) 3 times a day.

Abstinence of an acute nature.

During the first 4-5 days of the therapeutic cycle, it is necessary to take 2 tablets of the drug (0.4 g) 3 times a day. Later, take 1 tablet (0.2 g) 3 times a day.

In case of renal dysfunction, reduced dosages are used.

People with low weight and the elderly need to start therapy with 2 doses of 0.1 g of the substance per day (0.5 tablets).

The tablets must be swallowed whole with water (do not drink grapefruit juice). They can be taken with or after food.

If you miss a dose, do not take a double dose. Continue taking the medicine as usual.

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Use Carbalexa during pregnancy

The decision to use Carbalex in a pregnant woman can only be made by a doctor.

Because carbamazepine is excreted in breast milk, breastfeeding should be discontinued during therapy.

Contraindications

Main contraindications:

• increased intolerance to carbamazepine and similar components (tricyclics - a certain form of drugs prescribed for depression) or any of the additional elements of the drug;
• AV block;
• combination with lithium agents or MAOIs;
• severe stages of functional liver disorders;
• suppression of bone marrow function.

Side effects Carbalexa

At the initial stage of treatment, vomiting, diarrhea or constipation may develop, as well as dry mouth and loss of appetite.

The following side effects may occasionally occur: dizziness, fatigue or drowsiness, headaches, and visual or coordination disorders; in addition, tingling or partial paralysis in the legs and speech disorders may occur. In elderly people, clouding of consciousness or (in rare cases) hallucinations may occur. These negative symptoms disappear after 8-14 days without any treatment or due to a temporary reduction in dosage prescribed by the attending physician.

Among other violations:

• Disorders of the PNS and CNS: often develop impaired consciousness or its depression and cerebellar ataxia; in the elderly, a feeling of anxiety or confusion may develop. Involuntary movements (muscle contractions and large-scale tremor) are occasionally observed; in the elderly (also with cerebral lesions), choreoathetosis or dyskinesia affecting the orofacial region is possible. Aggression in behavior, depressive mood, mental retardation, decreased activity, speech disorders, hallucinations, as well as paresthesia, tinnitus, muscle weakness, paresis, peripheral neuritis and taste disorders are observed isolatedly. Activation of latent psychoses is possible. Basically, such manifestations pass on their own after 8-14 days or after a temporary reduction in the portion;
• visual organ damage: sometimes temporary visual disturbances occur (disorder of ocular accommodation, blurring or double vision). Clouding of the lens of the eye or conjunctivitis develops occasionally;
• disorders of the musculoskeletal system: myalgia with arthralgia and muscle spasms appear occasionally, passing after stopping the use of the drug;
• signs of allergy: occasionally rashes, TEN, itching or urticaria, as well as Stevens-Johnson syndrome may occur;
• epidermal manifestations: possible development of exfoliative dermatitis, MEE, purpura, photosensitivity, vasculitis, nodular erythema, and in addition alopecia, hyperhidrosis and disseminated lupus erythematosus;
• disorders of hematopoiesis: thrombocytopenia or leukopenia, leukocytosis or eosinophilia, as well as agranulocytosis or anemia;
• digestive disorders: dry mouth mucous membranes, vomiting, loss of appetite and nausea. Occasionally, constipation or diarrhea occurs, and the activity of liver transaminases increases. Pancreatitis, glossitis, jaundice, stomatitis, hepatitis or gingivitis may develop;
• problems with respiratory function: dyspnea or pneumonia may occur;
• urinary tract lesions: hematuria, pollakiuria, proteinuria, and also dysuria or oliguria occasionally develop. Renal failure may occur;
• disorders of the cardiovascular system: arrhythmia, AV block, bradycardia, and worsening of angina. Rarely, an increase or decrease in blood pressure is observed. Thromboembolism or thrombophlebitis is observed sporadically;
• Others: Occasionally, edema or hyponatremia may occur, and weight may increase. Galactorrhea, sexual dysfunction, lymphadenopathy, or gynecomastia may occur;
• Signs that appear when using large portions: irregular heartbeat, tremors and changes in blood pressure.

If you experience any negative symptoms not listed above, you should consult a doctor.

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Overdose

Signs of acute poisoning: vomiting, spasms, dizziness, agitation, ataxia, tremor, nausea and involuntary movements. In addition, tachycardia, breathing problems, tonic-clonic seizures, AV block and changes in blood pressure. In severe cases, clouding of consciousness or loss of consciousness, as well as respiratory arrest are noted. Immediate medical attention is required.

The drug has no antidote. Gastric lavage, artificial induction of vomiting, administration of activated carbon and laxatives are performed. After this, symptomatic measures are taken to support the respiratory system and cardiovascular system. In the event of seizures, other anticonvulsants are used (excluding barbiturates, because they suppress respiratory activity). Hemodialysis, forced diuresis or peritoneal dialysis procedures do not have the desired effect.

Interactions with other drugs

The combination of the drug and other anticonvulsants (for example, phenobarbital or diphenin) can mutually reduce the anticonvulsant effect (rarely, on the contrary, it potentiates it).

The drug can reduce the effect of medications that slow blood clotting (anticoagulants), certain antibiotics (for example, doxycycline), antiarrhythmic drugs (quinidine), and hormonal contraceptives.

Other medications (and grapefruit juice) can increase blood levels of carbamazepine, similarly altering the effects of certain antibiotics (eg, isoniazid with erythromycin and troleandomycin), cardiovascular drugs (eg, diltiazem with verapamil), analgesics (dextropropoxyphene) with antidepressants (viloxazine), as well as substances that lower gastric pH (cimetidine), and some antiepileptic drugs (primidone with phenytoin and valproic acid).

Combination with certain medications used for mental disorders (lithium) may cause feelings of confusion or anxiety.

A minimum of 2 weeks must be observed between the end of MAOI use and the start of therapy with Carbalex.

The medicine may affect the results of laboratory tests that show how well your thyroid gland is working.

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Storage conditions

Carbalex must be stored in a dark place at a temperature of no more than 25°C.

Shelf life

Carbalex can be used within a 5-year period from the date of release of the pharmaceutical product.

Application for children

Faster elimination of the drug in children may require the use of higher dosages compared to adults (mg/kg recalculation).

For infants under 12 months of age, the drug is used only with a doctor's prescription and under his supervision.

Carbalex is prescribed to children with extreme caution, after the doctor has carefully weighed all the risks and positive aspects of using the drug. Monotherapeutic use is recommended.

Analogues

Analogues of the substance are the drugs Carbalex retard, Zeptol, Finlepsin retard with Carbamazepine, and also Finlepsin.