Karbapin

Carbapine is an anticonvulsant medication that is a carboxamide derivative. The active component carbamazepine causes the blocking of Na channels inside the neural wall, thereby preventing the propagation of impulses.

The drug is often used in the treatment of combined or simple seizures seizures of a partial nature, and with it in the seizures of tonic-clonic species (primary or secondary). At the same time, the drug is prescribed for the treatment of other types of epilepsy attacks (excluding absans).

Indications Carbapine

It is used in the following disorders:

• epilepsy (severe seizures, partial seizures, accompanied by simple or complex manifestations, mixed types of epilepsy and tonic-clonic seizures of a generalized nature);
• emotional disorders of a cyclic form (having a manic-depressive nature of the violation);
• neuralgia (postherpetic, trigeminal or glossopharyngeal);
• abstinence syndrome in people with chronic alcoholism;
• neuropathy with diabetic genesis, against which there is pain;
• central diabetes of non-sugar type.

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Release form

The release of the drug produced in tablets with a volume of 0.2 g; in a pack - 50 tablets.

Pharmacodynamics

The drug is prescribed for trigeminal neuralgia of various origins and other types of pain of a chronic nature. It is believed that carbamazepine is able to reduce the intensity of pain during trigeminal neuralgia by suppressing the transmission within the nucleus of the 3-nd nerve.

Pharmacokinetics

The drug is almost completely absorbed inside the gastrointestinal tract - evenly and at low speed.

The bioavailability values of carbamazepine vary between 58-96% and do not change with food intake. The level of plasma Cmax is recorded after 2-8 hours. The term half-life is quite long and is approximately 30 hours. Because the drug induces the activity of intrahepatic enzymes, it increases the rate of its own metabolism and can reduce the term half-life to 15 hours.

Indicators of the distribution volume of drugs - in the range of 0.8-1.9 l / kg.

Dosing and administration

It is necessary to take medication orally, along with food. Selection of a portion of the drug is made individually to each patient, taking into account drug efficacy and plasma values of the active substance. The drug is prescribed for epilepsy and in monotherapy, and together with other anticonvulsants (phenobarbital, phenytoin or valproate Na).

Adults

In epilepsy, 0.2 g of the drug is first used 1-2 times a day; older people - 0.1 g (0.5 tablets) with the same frequency. Then the portion gradually increases to 0.4 g 2-3 times a day, until the optimum daily dosage of 0.8-1.2 g is reached. An adult can take no more than 1.6 g of medicine per day.

In emotional disorders that are cyclical in nature: if treatment with lithium drugs has no effect, the drug can be used in monotherapy or in combination with other drugs - during remission of the disease or its active phase. The day appointed by the reception of 1-1.6 g of Carbapin.

In the case of neuralgia, 0.2 g of drug is first taken daily. Next, the drug is used in a dosage of 0.4-0.8 g per day.

With withdrawal symptoms, an average of 0.6 g of the substance is taken per day, dividing the dose into 3 uses. In severe conditions (in the first days), the daily dosage can be increased to 1.2 g (in 3 uses).

In the case of a neuropathy of a diabetic nature (with pain), an average of 0.2 to 4 times a day is administered 2-4 times a day.

Having a central etiology, diabetes mellitus of non-sugar nature: an average of 0.4-0.6 g of the drug is used per day (2-3 uses).

In the case of a prolonged dose, the portion should be reduced from 3-month breaks to minimally effective dosages (or complete cancellation) in order to prevent tolerance towards drugs.

With the full abolition of therapy, the dosage is reduced gradually, over a 14-day period, in order to prevent the recurrence of the disease.

Persons with kidney insufficiency in a severe degree are required to take ¾ of the standard daily ration with conventional therapy. Adjusting the dosage after hemodialysis sessions is not necessary.

Children

Children need to use 10-20 mg / kg of medication per day. At the age of 1-3 years - 0.2-0.3 g per day; 4-7 years - 0.3-0.5 g each; 8-14 years - 0.5-1 g; 15-18 years old - by 0.8-1.2 g. Divide the daily portion into 2 uses.

Children under the age of 15 can use no more than 1 g of drug per day; older than 15 years - a maximum of 1.2 g per day.

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Use Carbapine during pregnancy

Use of medication during pregnancy is allowed only if there are strict indications; on the 1st trimester should not be applied.

The drug is excreted in breast milk, which is why it must be used very carefully when breastfeeding. It is required to evaluate the benefits and risks of breastfeeding for an infant in such a situation. Breastfeeding for women using carbamazepine can only be performed if the infant is monitored for possible side effects (for example, drowsiness).

Contraindications

The main contraindications:

• severe intolerance associated with the elements of the drug or tricyclics;
• AV blockade (excluding people with implanted pacemaker);
• problems with bone marrow hematopoietic activity;
• intermittent type of porphyria (in active phase);
• use together with lithium drugs or IMAO.

Side effects Carbapine

Adverse symptoms often occur during complex therapy; they usually develop at the initial stage of treatment and are dependent on the serving size:

• CNS lesions: dizziness, drowsiness, fatigue, confusion, and headaches and movement coordination often appear. Elderly people may experience anxiety and confusion. Also single-handedly appeared aggression in behavior, depression, ear noise and mental retardation. Occasionally, there are movements that are involuntary (nystagmus or sweeping type tremor). In addition, the elderly and people with organic cerebral lesions may develop involuntary movements in the face and jaws (choreoathetosis or dyskinesias). Neuritis, speech disorders, myasthenia, dysgeusia, and paresis of the legs appeared singly. Most of these symptoms disappear on their own after 8-14 days or after a temporary reduction of the portion. Because of this, the drug at the initial stage of therapy is administered in small dosages with their subsequent increase;
• visual impairment: conjunctivitis may occur, sometimes turning into ocular accommodation disorder, blurred vision and diplopia. An opacification of the eye lens may also occur;
• problems associated with the structure of muscles and bones: muscle and joint pains (myalgia or arthralgia) or muscle spasms develop sporadically. After discontinuation of the drug, such signs disappear;
• lesions of the mucous membranes and epidermis: the development of epidermal signs of allergy - itching, erythema multiforme, urticaria, TEN, exfoliative dermatitis, photosensitivity, erythroderma, SSD and lupus erythematosus of the disseminated type. A single occurrence of hyperhidrosis or alopecia;
• disorders of hematopoietic processes: thrombocyte or leukopenia, eosinophilia and leukocytosis. Leukopenia usually has a benign character. A single hemolytic, aplastic or megaloblastic type of anemia, agranulocytosis and splenomegaly develops individually, and in addition, lymph nodes are enlarged;
• problems with the work of the digestive tract: sometimes vomiting, dry mouth mucous membranes or nausea, and also appetite. Occasionally, constipation or diarrhea occurs. The pain in the abdominal zone and the inflammation of the nasopharyngeal mucous membranes (glossitis with stomatitis and gingivitis) are rarely observed. Such signs disappear after 8-14 days of therapy, or after a temporary reduction of the dose of drugs;
• hepatic lesions: sometimes there is a change in the values of functional liver samples. Occasionally develop jaundice. Hepatitis (granulomatous, cholestatic, as well as mixed or hepatocellular) is rarely observed;
• Violations of EBV and endocrine system: galactorrhea (women) or gynecomastia (men) sporadically appears. In addition, Karbapin may have an effect on thyroid activity, especially when combined with other anticonvulsants. Since carbamazepine has an antidiuretic effect, the reduction of plasma indices Na (hyponatremia), which causes headaches and vomiting, as well as confusion, is rarely observed. There were only a few puffiness and weight gain. Perhaps a decrease in plasma values of Ca;
• problems with respiratory function: a single intolerance of the drug, manifested in the form of dyspnea, fever, pulmonary fibrosis and inflammation;
• disorders of the urogenital tract: occasionally hematuria, proteinuria or oliguria occurs. The development of renal insufficiency or disorder of sexual activity occurs singularly;
• Cardiovascular dysfunction: single cases in elderly people or people with problems in the heart may cause heart rhythm disorders and bradycardia, and in addition, worsening of the course of IHD. AV blockade is occasionally observed, sometimes accompanied by loss of consciousness. There may be a significant increase or decrease in blood pressure values (the latter usually occurs when taking large portions of the drug). At the same time, the development of thrombophlebitis, vasculitis or thromboembolism was noted;
• manifestations of severe intolerance: occasionally vasculitis appears, feverish state, rashes, swollen lymph nodes, changes in the number of leukocytes, arthralgia, changes in the values of functional intrahepatic test, hepatosplenomegaly; In addition, other disorders of the systems and organs - the kidneys, lungs, myocardium and pancreas.

It is necessary to immediately cancel the drug in the event of the onset of severe symptoms of allergy, exanthema, changes in laboratory blood values (neutro, leuco or thrombocytopenia) and fever.

Overdose

Carbamazepine leads to a significant inhibition of the function of the central nervous system, which is why there is a risk of severe symptoms of intoxication.

Signs.

• CNS disorders: CNS suppression, hallucinations, agitation, disorientation, coma, and drowsiness. In addition, dysarthria, hyperreflexia, develops into hyporeflexia, nystagmus, visual acuity disorder, ataxia, convulsions, dyskinesia, hypothermia, myoclonus and psychomotor disorders;
• CVS lesions: cardiac conduction disorder, accompanied by expansion of the QRS system, tachycardia, increase or decrease in blood pressure values and cardiac arrest;
• problems with respiratory function: pulmonary edema or respiratory depression;
• disorders of the gastrointestinal tract: problems with evacuator gastric function, vomiting and weakening of colon motility;
• signs associated with the urinary system: anuria or oliguria, hyponatremia and fluid retention.

Therapy.

There is no antidote. Initially, therapy is carried out, taking into account the clinical condition of the patient; hospitalization is also required. It is necessary to determine the level of carbamazepine inside the blood plasma to confirm intoxication and assess its degree. The evacuation of gastric contents, gastric lavage and the use of activated carbon. Supportive and symptomatic procedures for intensive care, tracking of cardiac activity and correction of EBV values are performed.

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Interactions with other drugs

Drugs that can increase the plasma values of carbamazepine: erythromycin, verapamil, dextropropoxyphene with viloxazine, cimetidine and diltiazem with isoniazid. In the case of the combined use of such medications, you need to monitor the blood indicators of carbamazepine and reduce the daily portion, if necessary.

Etosucimid, Na valproate, phenobarbital with primidone and phenytoin can reduce plasma parameters of drugs due to the induction of intrahepatic microsome enzymes.

The drug reduces the term half-life and increases the rate of clearance (due to a decrease in concentration) of the following substances: warfarin with GCS, theophylline, haloperidol and doxycycline. The latter must be applied with a 12-hour break.

It is forbidden to use Karbapin with an MAOI (a minimum of 14 days must be observed) and lithium substances.

During the appointment or cancellation of the medication should be changed portion of anticoagulants (taking into account the clinical values).

The drug increases the rate of metabolic processes of oral contraception, which is why it is necessary to select other contraceptives.

Carbamazepine reduces the tolerance of alcoholic beverages, so those who use the drug should stop using them at the time of therapy.

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Storage conditions

Karbapin needs to be stored in a place protected from moisture. Temperature indicators - in the range of 15-25 ° C.

Shelf life

Karbapin can be used for a 3-year term since the sale of the drug substance.

Application for children

Use in children older than 1 year old. But at the same time, in persons younger than 7 years old, the drug should be used very carefully, because there is a likelihood of side symptoms.

Analogs

Analogues of drugs are Finlepsin, Septol, Tegretol with Carbalex, Oksapin and Carbamazepine with Timonil and Mezacar.