Karbaleks

Carballex is an anticonvulsant drug. Contains the component carbamazepine.

Indications Karbaleksa

It is used for such violations:

• various types of epileptic seizures and epilepsy, accompanied by mental disorders;
• various mania;
• preventing the development of manic-depressive disorders;
• neuralgia affecting the trigeminal nerve;
• diabetic neuropathy;
• withdrawal condition;
• central diabetes of non-sugar character.

Release form

The release of the drug is sold in tablet form - 10 pieces inside a blister pack. In a pack - 5 or 10 such packages.

Pharmacodynamics

As an anticonvulsant, Carballex can have an effect in the case of partial seizures (both complex and simple), against which generalization of a secondary nature is observed (or not), and besides this, in the tonic-clonic form of generalized seizures and .

Clinical tests with the use of drugs in monotherapy in people with epilepsy (especially for adolescents and children) found its psychotropic effects, which were partially manifested by positive effects on signs of depression and anxiety, and in addition weakening aggressiveness with irritability.

Information from individual tests showed that the effect of the drug on psychomotor data and cognitive activity depends on the size of the portion and is negative or doubtful. With other tests, a positive effect was observed regarding the data characterizing the ability to memorize with the training and attention of the patient.

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

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

In people with diabetes of a non-sugar type that has a central origin, it reduces the sensation of thirst and diuresis.

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

• manic state of acute nature;
• maintenance therapy for BAR manic-depressive type (and monotherapy, and complex use with lithium drugs, antidepressants or neuroleptics) or psychoses schizoaffective nature;
• manic psychosis (in combination with neuroleptics);
• acute stage of schizophrenia polymorphic nature.

The principle of the effect of carbamazepine was only partially determined. The substance normalizes the walls of excessively excited neural fibers, slows down the appearance of repeated nerve discharges and weakens the synaptic transport of excitatory impulses.

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

The anticonvulsant effect mainly develops with a decrease in the amount of glutamate released, as well as the normalization of the nerve walls; anti-mania influence 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 1-time use are noted after 12 hours.

Synthesis with blood protein is 70-80%. Inside the liquor, saliva forms values proportional to the proportion of the active element that is not synthesized with protein (20-30%). The drug passes into the mother's milk (25-60% of the plasma indicator) and through the placenta.

Distribution volumes are equal to 0.8-1.9 l / kg. After 1 single use, the half-life is 25-65 hours, and after prolonged use, it is 8-29 hours (this is due to the induction of metabolic enzymes). In people using such agents as phenobarbital or phenytoin (inducing the activity of the monooxygenase system), the half-life is 8-10 hours.

The exchange processes of carbamazepine are produced inside the liver, and it is excreted mainly through the kidneys.

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

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

Dosing and administration

Use for epilepsy.

Children from 10 years and adults need to start using the drug with a serving of 0.2 g (1 tablet) 2 times a day. Further, the dosage is slowly increased to achieve optimal indicators for the patient.

Infants up to 12 months: 0.1 g per day (0.5 tablets). Children of the age group of 1-5 years - 0.2-0.4 g per day (1-2 tablets). Children 6-10 years of age appoint 2-3 tablets per day (0.4-0.6 g).

Manic-depressive disorders and mania.

The portion size is often equal to 0.4-1.6 g (within 2-8 tablets) per day, divided into 2-3 applications. Standard portion - 2-3 tablets per day (0.4-0.6 g).

Affecting the trigeminal nerve neuralgia.

At the initial stage, you usually need to use 1-well tablet (0.2 g) 2 times a day. Later, the doctor must choose a personal dosage, determining the optimal size of servings. Often enough is about 3 tablets per day (0.6 g).

Diabetic form of neuropathy and diabetes of the central type, having a non-sugar character.

It is often required to consume 0.2 g of the drug (1 tablet) 3 times a day.

Withdrawal symptoms are acute.

For the first 4-5 days of the therapeutic cycle, it is required 3 times a day to use 2 tablets of drugs (0.4 g). Later they take 1 tablet (0.2 g) 3 times a day.

For disorders of renal activity, lower dosages are used.

Persons with low weight and elderly people need to start therapy with 2-fold use of 0.1 g of substance per day (0.5 tablets).

Tablets must be swallowed whole, while drinking water (it is forbidden to use grapefruit juice). Reception is carried out with food or after it.

When you skip the use of dosage, double serving is prohibited. Drug administration continues according to the standard scheme.

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Use Karbaleksa during pregnancy

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

Because carbamazepine is excreted with breast milk, breastfeeding should be abandoned during therapy.

Contraindications

Main contraindications:

• increased intolerance to carbamazepine and similar components (tricyclics - a certain form of drugs prescribed for depression) or one of the additional elements of drugs;
• AV blockade;
• combination with lithium or IMAO;
• severe stages of functional hepatic disorders;
• oppression of bone marrow work.

Side effects Karbaleksa

At the initial stage of treatment, vomiting, diarrhea, or obstipation may develop, and, in addition, dry mouth and loss of appetite.

Single side effects such as: dizziness, feeling tired or sleepy, headaches and visual disturbances or coordination; In addition, there is tingling or partial paralysis in the legs and speech disorder. In elderly people, clouding of consciousness or (single) the appearance of hallucinations is possible. These negative signs disappear after 8-14 days without any treatment or due to a temporary decrease in dosage prescribed by the attending doctor.

Among other violations:

• Disorders of the PNS and CNS: often develop a violation of consciousness or its depression and cerebellar ataxia; seniors may have a feeling of anxiety or confusion. Occasionally, there are involuntary movements (muscle contraction and large-size tremor); in elderly persons (also with cerebral lesions), choreoathetosis or dyskinesias affecting the rototraline region is possible. Aggression in behavior, depressive mood, mental retardation, decreased activity, speech disorders, hallucinations and, moreover, paresthesia, ear noise, muscle weakness, paresis, peripheral neuritis, and gustatory disorder are singled out. Possible activation of proceeding latent psychosis. Basically, such manifestations occur independently after 8-14 days or after a temporary reduction of the portion;
• lesions of the visual organs: sometimes temporary visual disturbances occur (ocular accommodation disorder, blurring or double vision). A single clouding of the eye lens or conjunctivitis develops;
• dysfunction of the musculoskeletal structure: myalgia with arthralgia and muscle spasms occur spontaneously after stopping drug use;
• signs of allergy: occasionally rash, TEN, itching or urticaria, as well as Stevens-Johnson syndrome;
• epidermal manifestations: development of exfoliative dermatitis is possible, IEE, purpura, photosensitivity, vasculitis, nodular erythema, and in addition alopecia, hyperhidrosis and disseminated lupus erythematosus;
• disorders of hematopoietic processes: thrombocyto or leukopenia, leukocytosis or eosinophilia, as well as agranulocytosis or anemia;
• digestive disorders: dry mouth, vomiting, loss of appetite and nausea. Occasionally, constipation or diarrhea occurs, and liver transaminase activity increases. Perhaps the development of pancreatitis, glossitis, jaundice, stomatitis, hepatitis or gingivitis;
• problems with respiratory function: dyspnea or pneumonia may appear;
• lesions of the urinary system: rarely develop hematuria, pollakiuria, proteinuria, and in addition dysuria or oliguria. Renal failure may occur;
• disorders of the cardiovascular system: arrhythmia, AV-blockade, bradycardia, as well as worsening of the course of stenocardia. Occasionally, there is an increase or decrease in blood pressure. Thromboembolism or thrombophlebitis is singled out individually;
• others: occasionally, puffiness or hyponatremia appear, as well as weight gain. Galactorrhea, sexual dysfunction, lymphadenopathy or gynecomastia may occur;
• signs that appear when using large portions: upset heart rate, tremors, and changes in blood pressure.

If there are negative symptoms that are not described in the list above, you should consult a doctor.

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Overdose

Signs of acute poisoning include vomiting, cramping, dizziness, agitation, ataxia, tremor, nausea, and movements that are involuntary. In addition, tachycardia, problems with the respiratory process, convulsions that have a tonic-clonic nature, AV blockade and changes in blood pressure values. In case of severe disturbances, clouding of consciousness or its loss, as well as the arrest of the respiratory process, are noted. Immediate medical attention is required.

There is no antidote to the drug. Gastric irrigation, artificial induction of vomiting, intake of activated carbon and laxatives are performed. After that, symptomatic measures are held to support the work of the respiratory system and the cardiovascular system. In the event of seizures, convulsions use other anticonvulsants (excluding barbiturates, because they suppress the respiratory activity). Hemodialysis, forced diuresis or peritoneal dialysis procedures do not have the desired effect.

Interactions with other drugs

Combining medication and other antconvulsants (for example, phenobarbital or difenina) can mutually reduce the anticonvulsant effect (sometimes, on the contrary, potentiates it).

The drug is able to reduce the effect of drugs that slow down blood coagulation (anticoagulants), certain antibiotics (for example, doxycycline), anti-arrhythmic drugs (quinidine), as well as hormonal OK.

Other drugs (and grapefruit juice) can increase the blood values of carbamazepine, changing in a similar way the effect of individual antibiotics (for example, isoniacid with erythrimycin and troleandomycin), remedies for treating diseases of the CAS (for example, diltiazem with verapamil), analgesics (dextropropropofyrophympathy). (viloxazine), as well as substances that lower the gastric pH (cimetidine), and some antiepileptic drugs (primidone with phenytoin and valproic acid).

Combination with certain medications used for mental disorders (lithium) may provoke a feeling of confusion or anxiety.

It is necessary to withstand at least a 2-week period between the completion of the use of MAOI and the initiation of therapy with Carbalex.

The drug may affect the testimony of laboratory tests showing thyroid function.

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Storage conditions

Carballex is required to be kept in a dark place at temperature elevations constituting a maximum of 25 ° C.

Shelf life

Carballex can be used within the 5-year term from the moment of release of the pharmaceutical agent.

Application for children

Faster removal of the drug in children may require the use of higher dosages in comparison with an adult (mg / kg recalculation).

For infants up to 12 months of age, the drug is used only with the appointment of a doctor and under his control.

Children are prescribed Carballex extremely carefully, after the doctor carefully weighs all the risks and positive aspects of the use of drugs. Monotherapeutic use is recommended.

Analogs

Analogues of the substance are drugs Carballex retard, Zeptol, Finlepsin retard with carbamazepine, and Finlepsin.