Index of drugs

Epilepsy. Supplementary treatment of partial seizures, also secondary generalized, in adults and children aged 6 years and older. Monotherapy of partial seizures, also secondary generalized, in adults and adolescents aged 12 years and older.Treatment of peripheral neuropathic pain. Treatment of peripheral neuropathic pain, e.g. painful diabetic neuropathy and post-herpetic neuralgia in adults.

One capsule contains 100 mg, 300 mg or 400 mg of gabapentin.

Gabapentin has a structural similarity to gamma-aminobutyric acid (GABA), but its mechanism of action is different from that of other substances that affect the GABA synapse. Gabapentin binds with high affinity to binding sites in the brain that are associated with alpha subunits₂- a delta of Calcium channels dependent on the electrical potential. It does not bind in the brain to other common receptors for drugs or neurotransmitters, such as the GABA receptor_AND, GABA_B, benzodiazepine, for glutamate, Glycine or N-methyl-D-aspartate. After oral administration, gabapentin achieves a peak plasma concentration after 2-3 hours. Bioavailability is about 60%. The presence of a meal does not affect the absorption of the preparation. It does not bind to plasma proteins. In patients with epilepsy, the concentration of gabapentin in the cerebrospinal fluid accounts for approximately 20% of the steady-state concentration achieved in the plasma. Gabapanthin is excreted in breast milk. T_0,5 in the blood is 5-7 h. Gabapentin is not metabolised in the human body; it is excreted in urine in unchanged form.

Hypersensitivity to the components of the preparation.

Gabapentin is usually considered ineffective in the treatment of seizures of the unconscious and may exacerbate this type of epilepsy in some patients. Therefore, gabapentin should be used with caution in patients with mixed seizures, including seizures of the unconscious. Use with caution in patients with impaired renal function. If acute pancreatitis develops during treatment, gabapentin should be discontinued. Some patients may experience an increase in the frequency of seizures or the appearance of new types of seizures.

The safety of the preparation in pregnant women has not been established. In general, the use of anti-epileptic preparations during pregnancy increases 2-3 times the risk of malformations in comparison to children of women without epilepsy. If a woman plans to become pregnant, the need for anti-epileptic treatment should be considered. Taking several antiepileptic drugs at the same time may be associated with a higher risk of congenital malformations than monotherapy. Gabapentin should be used during pregnancy only if the benefits outweigh the potential risk. Do not suddenly stop your antiepileptic treatment because you may experience a seizure breakthrough that can have serious consequences for your mother and baby. It passes into breast milk and can only be used in breastfeeding women when the benefits clearly outweigh the risks to the baby.

Very common (≥1 / 10): viral infections, drowsiness, dizziness, ataxia, fatigue, fever. Common (≥ 1/100, <1/10): pneumonia, respiratory infection, urinary tract infection, infection, otitis media, leukopenia, anorexia, increased appetite, hostility, confusion and emotional lability, depression, anxiety, nervousness, thinking disorders, convulsions, hyperkinesia, dysarthria, insomnia, headache, sensory disturbances (paraesthesia, hypoesthesia), coordination disorders, nystagmus, increased, weakened or suppressed reflexes, visual disturbances (amblyopia, double vision), dizziness, hypertension, enlargement vasodilation, dyspnoea, bronchitis, pharyngitis, cough, rhinitis, vomiting, nausea, tooth disorders, gingivitis, diarrhea, abdominal pain, indigestion, constipation, dry mouth or throat, bloating, swelling of the face,purpura most often described as occurrence of bruising due to physical injuries, rash, pruritus, acne, joint, muscle or back pain, muscle twitching, impotence, peripheral or generalized edema, gait disturbances, weakness, pain, malaise, flu syndrome, reduction of leukocytes in blood, weight gain, accidental injuries, fractures, abrasions of the epidermis. Uncommon: reduced mobility, palpitations, generalized edema, increased SGOT liver function tests (AST), SGPT (ALT) and bilirubin. Rare (≥1 / 10,000, <1/1000): hypersensitivity reactions (eg urticaria). Not known: thrombocytopenia, hypersensitivity syndrome, generalized reactions with variable symptoms that may include fever, rash, hepatitis, lymphadenopathy, eosinophilia and sometimes other signs and symptoms, hallucinations, movement disorders (eg choreoathetosis, dyskinesias, dystonia ), tinnitus, pancreatitis, hepatitis, jaundice, Stevens-Johnson syndrome, angioedema, erythema multiforme, alopecia, drug eruption with oesinophilia and systemic signs, myoclonic convulsions, acute renal failure, myalgia and back pain, acute renal failure , incontinence, breast hypertrophy, gynecomastia, withdrawal symptoms (mainly anxiety, insomnia, nausea, pain, sweating), chest pain, changes in blood Glucose in patients with diabetes. Respiratory tract infections, otitis media, seizures and bronchitis, aggressive behavior, dyskinesias were found only in children.

Epilepsy. Adults and adolescents: On the first day 300 mg is administered, on the second day - 600 mg in two divided doses, on the third day - 900 mg in three divided doses; alternatively, the first day can be given 900 mg in three divided doses, and then depending on the patient's response to the drug and tolerability can be increased by 300 mg / day every 2-3 days up to a maximum dose of 3600 mg / day. Some patients may need to increase their dose more slowly. The minimum time to reach a dose of 1800 mg / day is 1 week, for a dose of 2400 mg / day - a total of 2 weeks, and up to a dose of 3600 mg / day - a total of 3 weeks. The total daily dose should be divided into three single doses, with the maximum interval between doses should not be longer than 12 hours to prevent breakthroughs.Children 6 years and older: the starting dose is 10-15 mg / kg / day. The effective dose is achieved by gradually increasing the dose over a period of approximately 3 days and amounts to 25-35 mg / kg / day. Doses up to 50 mg / kg / day were well tolerated in a long-term clinical study. The total daily dose should be divided into three single doses, the maximum interval between doses should not be longer than 12 hours.Peripheral neuropathic pain. On the 1st day, 300 mg are given, on the second day - 600 mg in two divided doses, on the third day - 900 mg in three divided doses; alternatively, the first day can be given 900 mg in three divided doses, and then depending on the patient's response to the drug and tolerability can be increased by 300 mg / day every 2-3 days up to a maximum dose of 3600 mg / day. Some patients may need to increase their dose more slowly. The minimum time to reach a dose of 1800 mg / day is 1 week, for a dose of 2400 mg / day - a total of 2 weeks, and up to a dose of 3600 mg / day - a total of 3 weeks. If it is necessary to use the preparation for more than 5 months, the patient's clinical condition and the need for additional treatment. In patients with poor overall condition, i.e. low body weight, transplant patients, etc., the dose should be increased more slowly - by lower doses or by increasing the interval between subsequent increases in the daily dose.Elderly patients: Dose reduction may be necessary due to deteriorating renal function.Patients with impaired renal function: the daily dose of gabapentin is determined by the creatinine clearance: for clearance ≥ 80 ml / min, the daily dose is 900-3600 mg / day; for 50-79 ml / min - 600-1800 mg / day; for 30-49 ml / min - 300-900 mg / day; for 15-29 ml / min - 150-600 mg / day (300 mg administered every other day); for clearance <15 ml / min - 150-300 mg / day (the daily dose should be reduced in proportion to the creatinine clearance value, i.e. patients with a creatinine clearance of 7.5 ml / min should receive half the daily dose used in patients with creatinine clearance of 15 ml / min).Patients undergoing hemodialysis: For patients with anuria undergoing hemodialysis who have never received Gabapentin, a loading dose of 300-400 mg is recommended, followed by 200-300 mg of gabapentin after every 4 h of hemodialysis. In the days between hemodialysis, gabapentin should not be given.