Product Description




Europe delivered time is 8 — 12 business days.

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Australia/Asia delivered time 15-26 business days.

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dosage form
gabapentin (in recalculation on 100% basis) of 300.0 mg;

Excipients: 4.2 mg calcium stearate, sodium carboxymethyl Type A 4.2 mg microcrystalline cellulose 111.6 mg;
pharmachologic effect
Gabapentin is structurally similar to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action is different from other drugs that interact with GABA-receptors (valproate, barbiturates, benzodiazepines, inhibitors of GABA-transaminase reuptake inhibitors GABA agonists, GABA prodrugs GABA). It has no GABA-ergic and does not affect the properties of grip and GABA metabolism. Preliminary studies showed that gabapentin binds to alpha2-gamma subunit of the voltage-dependent calcium channels and reduces the flow of calcium ions, which plays an important role in the onset of neuropathic pain. Other mechanisms of action of gabapentin for neuropathic pain is a decrease in glutamate-dependent neuronal death, increasing the synthesis of GABA, inhibition of monoamine neurotransmitter release group. Gabapentin at clinically relevant concentrations, does not bind to receptors or other drugs common neurotransmitters, including GABA receptors, GABAB, benzodiazepine, glutamate, glycine, or

N-methyl-D-aspartate. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuated effects glutamate receptor agonist N-methyl-D-aspartate in some tests in vitro, but only at a concentration of more than 100 micromoles, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.
The bioavailability of gabapentin is not proportional to dose. Thus, by increasing the dose is reduced. After oral administration, maximum concentration (C max) of gabapentin in plasma achieved in 2-3 hours. The absolute bioavailability of gabapentin capsules is approximately 60%. Food, including a high content of fat, has no effect on pharmacokinetics. Excretion of gabapentin plasma is best described by a linear model. The half-life (T1 / 2) in plasma is independent of dose and averages 5-7 hours Pharmacokinetics does not change with repeated use.; equilibrium plasma concentration can be predicted based on the results of single receiving drug. Gabapentin is almost bound to plasma proteins (<3%) and has a volume of distribution of 57.7 liters. Displays only the kidneys in an unmodified form, does not undergo metabolism. The drug does not induce liver oxidative enzymes mixed function involved in the metabolism of drugs. Clearance from plasma gabapentin reduced in the elderly and patients with impaired renal function. The constant rate of excretion, clearance from the plasma and renal clearance are directly proportional to creatinine clearance. Gabapentin is removed from plasma by hemodialysis. In patients with impaired renal function and patients receiving hemodialysis, dose adjustment is recommended (see. «Dosage and Administration» section).
Side effects
In the treatment of neuropathic pain

Body as a whole: accidental injury, asthenia, back pain, flu syndrome, headache, infection, pain of various localization, peripheral edema, weight gain;

Digestive tract: constipation, diarrhea, dry mouth, dyspepsia, flatulence, nausea, vomiting, abdominal pain;

Nervous System: gait disturbance, amnesia, ataxia, confusion, dizziness, hypesthesia, somnolence, abnormal thinking, tremor;

Respiratory: shortness of breath, sore throat;

Skin and subcutaneous tissue: skin rash;

Special Senses: amblyopia.

In the treatment of partial seizures

Body as a whole: back pain, fatigue, fever, headache, viral infection, peripheral edema, weight gain, fatigue, — malaise, swelling of the face;

Cardiovascular system: symptoms of vasodilation or hypertension;

Digestive tract: constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea and / or vomiting, abdominal pain, flatulence, anorexia, gingivitis;

blood system, lymphatic system: leukopenia, purpura (often described as her bruises, occurred when a physical injury);

Musculo-mshechnaya system: fractures, myalgia, arthralgia;

Nervous system: amnesia, ataxia, confusion, impaired coordination, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, abnormal thinking, tremor, muscle twitching, dizziness, giperk
sale Properties
Special conditions
Although the syndrome with the development of seizures in the treatment of gabapentin is not checked, however, the abrupt discontinuation of therapy with antiepileptic drugs in patients with partial seizures can induce seizures.

Gabapentin is not considered effective in the treatment of absence-epilepsy

In patients who require combination therapy with morphine, may require increased doses of gabapentin. It is necessary to ensure thorough monitoring of patients for the development of such a sign of oppression of the central nervous system (CNS) such as drowsiness. In this case the dose of gabapentin or morphine must be adequately reduced.

Laboratory research

When adding gabapentin to other anticonvulsants, it has been reported false positive results in the determination of protein in urine using test strips Ames N-Multistix SG®. For the determination of protein in urine it is recommended to use more specific sulfosalicylic acid precipitation method. Patients should avoid driving, as well as the performance of work requiring speed of psychomotor reactions.
monotherapy or as an adjunct in the treatment of partial seizures with secondary generalization and without adults and children 12 years of age;
Inside, swallowing a whole, regardless of the meal and abundantly with some liquid. If you need to reduce the dose, stop the drug or replace it with an alternative means, it should be done gradually over a minimum of one week. Neuropathic pain in adults The initial daily dose is 900 mg, divided into three stages; if necessary, the dose is gradually increased to the maximum — 3600 mg / day. Treatment can be started immediately with a dose of 900 mg / day (300 mg 3 times daily) or within the first 3 days the dose may be increased gradually to 900 mg a day as follows: 1st day: 300 mg 1 time per day ; Day 2: 300mg 2 times a day; Day 3: 300 mg 3 times a day. Partial seizures Adults and children from 12 years: effective dose — from 900 to 2400 mg / day. Therapy can be started with a dose of 300 mg three times a day on the first day and increased gradually to 900 mg according to the scheme described above (see., «Neuropathic pain in adults» section). Subsequently, the dose may be increased to a maximum of 3600 mg / day (divided into 3 equal Hour). The maximum interval between doses with three-time taking the drug should not exceed 12 hours in order to avoid the resumption of seizures. Selection of doses in renal failure patients with renal insufficiency is recommended to decrease the dose of gabapentin according to the table: Creatinine clearance (ml / min) daily dose (mg / day)> 80 900-2400 50-79 600-1200 30-49 300-600 15-29 150 * -300 <15 150 * * appoint 300 mg every other day recommendations for patients on hemodialysis patients on hemodialysis who had not previously received gabapentin, a drug is recommended to be administered in a saturating dose of 300-400 mg, and then apply it on 200-300 mg every 4 hours of hemodialysis