Gabapentin capsules 300mg, No. 50

Epilepsy:

• partial convulsions with and without secondary generalization in adults and children over 12 years of age (my therapy);

• partial seizures with and without secondary generalization in adults (additional drugs);

• resistant form of epilepsy in children over 3 years old (additional drug).

• Neuropathic pain in adults (18 years and older).

Inside, swallowing whole, regardless of food intake and drinking plenty of liquid.

If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative remedy, this should be done gradually over at least one week.

Neuropathic pain in adults

The initial daily dose is 900 mg, divided into three doses; if necessary, the dose is gradually increased to a maximum of 3600 mg / day. Treatment can be started immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days the dose can be gradually increased to 900 mg per day according to the following scheme:
1st day: 300 mg once a day
2nd day: 300 mg 2 times a day
3rd day: 300 mg 3 times a day

Partial seizures

Adults and children over 12 years old: The effective dose is from 900 to 3600 mg / day. Therapy can be started with a dose of 300 mg 3 times a day on the first day, or gradually increased to 900 mg according to the scheme described above (see section 'Neuropathic pain in adults'). Subsequently, the dose can be increased to a maximum of 3600 mg / day (divided into 3 equal doses). The maximum interval between doses when taking the drug three times should not exceed 12 hours in order to avoid the resumption of seizures.

Dose selection for renal failure.

A dose reduction of gabapentin is recommended for patients with renal insufficiency.

Recommendations for patients on hemodialysis.

Patients on hemodialysis who have not previously taken gabalentin are recommended to prescribe the drug in a saturating dose of 300-400 mg, and then use it at 200-300 mg every 4 hours of hemodialysis.

1 capsule contains:

active substance: gabapentin - 300 mg;

excipients: calcium hydrogen phosphate dihydrate (Emcompress), potato starch, macrogol (polyethylene glycol 6000), magnesium stearate; i capsule composition: body and cap - titanium dioxide, quinoline yellow dye, indigo carmine dye - FD&C Blue 2, gelatin.

• Hypersensitivity to any of the components of the drug,

• age up to 12 years (due to the impossibility of accurate dosing).

With caution
Renal failure (see 'Dosage and Administration').

Trade name : Gabapentin

International non-proprietary name : gabapentin

Dosage form : capsules

Ingredients :

1 capsule contains:

active substance: gabapentin - 300 mg;

excipients: calcium hydrogen phosphate dihydrate (Emcompress), potato starch, macrogol (polyethylene glycol 6000), magnesium stearate; i capsule composition: body and cap - titanium dioxide, quinoline yellow dye, indigo carmine dye - FD&C Blue 2, gelatin.

Description :

Capsules No. 0 are green. The contents of the capsules are white or almost white powder. Lumps are allowed, which, when pressed with a glass rod, easily turn into powder.

Pharmacotherapeutic group : antiepileptic drug.

ATX code : [N03AX12].

PHARMACOLOGICAL PROPERTIES .

Pharmacodynamics :

Gabapentin is structurally similar to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from other drugs that interact with GABA receptors (valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors and prodrugs of GABA GABA). It does not have GABAergic properties and does not affect the uptake and metabolism of GABA. Preliminary studies have shown that gabapentin binds to the ?2-?-subunit of voltage-dependent calcium channels and reduces calcium ion flux, which plays an important role in neuropathic pain. Other mechanisms of action of gabapentin in neuropathic pain are a decrease in glutamate-dependent neuronal death, an increase in GABA synthesis, and suppression of the release of monoamine neurotransmitters.Gabapentin at clinically significant concentrations does not bind to receptors that are sensitive to other drugs (MPs) or neurotransmitters, including receptors for GABA, GABA, benzodiazepine, glutamate, glycine, or N-methyl-d-aspartate. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuated the effects of the glutamate receptor agonist N-methyl-d-aspartate in some in vitro tests, but only at a concentration of more than 100 ?mol, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.glycine or N-methyl-d-aspartate. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuated the effects of the glutamate receptor agonist N-methyl-d-aspartate in some in vitro tests, but only at a concentration of more than 100 ?mol, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.glycine or N-methyl-d-aspartate. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin partially attenuated the effects of the glutamate receptor agonist N-methyl-d-aspartate in some in vitro tests, but only at a concentration of more than 100 ?mol, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.

Pharmacokinetics :

The bioavailability of gabapentin is not dose proportional. So, with an increase in the dose, it decreases. After oral administration, the maximum concentration (Cmax) of gabapentin in plasma is achieved after 2-3 hours. The absolute bioavailability of gabapentin in capsules is about 60%. Foods, including those with a high fat content, have no effect on pharmacokinetics. The half-life (T1 / 2) from plasma does not depend on the dose and averages 5-7 hours. Pharmacokinetics does not change with repeated use; equilibrium plasma concentrations can be predicted from the results of a single dose of the drug. Gabapentin practically does not bind to plasma proteins (<3%) and has a volume of distribution of 57.7 liters. It is excreted exclusively by the kidneys in unchanged form, it is not metabolized. The drug does not induce oxidative liver enzymes with mixed function,involved in the metabolism of drugs. The clearance of gabapentin from plasma is reduced in the elderly and in patients with impaired renal function. Elimination rate constant, plasma clearance and renal clearance are directly proportional to creatinine clearance. Gabapentin is removed from plasma by hemodialysis. In patients with impaired renal function and in patients receiving hemodialysis treatment, dose adjustment is recommended (see Dosage and Administration).dose adjustment is recommended (see Dosage and Administration).dose adjustment is recommended (see. Dosage and Administration).

Indications for use :

Epilepsy:

• partial convulsions with and without secondary generalization in adults and children over 12 years of age (my therapy);

• partial seizures with and without secondary generalization in adults (additional drugs);

• resistant form of epilepsy in children over 3 years old (additional drug).

• Neuropathic pain in adults (18 years and older).

Contraindications :

• Hypersensitivity to any of the components of the drug,

• age up to 12 years (due to the impossibility of accurate dosing).

With caution
Renal failure (see 'Dosage and Administration').

Application during pregnancy and lactation :

There is no data on the use of the drug in pregnant women, therefore, gabapentin should be used during pregnancy only if the intended benefit to the mother justifies the possible risk to the fetus.
Gabapentin is excreted in breast milk, its effect on a breast-fed child is unknown, so breastfeeding should be avoided during treatment.

Method of administration and dosage :

Inside, swallowing whole, regardless of food intake and drinking plenty of liquid.

If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative remedy, this should be done gradually over at least one week.

Neuropathic pain in adults

The initial daily dose is 900 mg, divided into three doses; if necessary, the dose is gradually increased to a maximum of 3600 mg / day. Treatment can be started immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days the dose can be gradually increased to 900 mg per day according to the following scheme:
1st day: 300 mg once a day
2nd day: 300 mg 2 times a day
3rd day: 300 mg 3 times a day

Partial seizures

Adults and children over 12 years old: The effective dose is from 900 to 3600 mg / day. Therapy can be started with a dose of 300 mg 3 times a day on the first day, or gradually increased to 900 mg according to the scheme described above (see section 'Neuropathic pain in adults'). Subsequently, the dose can be increased to a maximum of 3600 mg / day (divided into 3 equal doses). The maximum interval between doses when taking the drug three times should not exceed 12 hours in order to avoid the resumption of seizures.

Dose selection for renal failure.

A dose reduction of gabapentin is recommended for patients with renal insufficiency.

Recommendations for patients on hemodialysis.

Patients on hemodialysis who have not previously taken gabalentin are recommended to prescribe the drug in a saturating dose of 300-400 mg, and then use it at 200-300 mg every 4 hours of hemodialysis.

Side effects :

Cardiovascular system: symptoms of vasodilation or increased blood pressure, palpitations.

Digestive tract: flatulence, anorexia, gingivitis, abdominal pain, constipation, dental diseases (including discoloration of the enamel of the teeth), diarrhea, dyspepsia, increased appetite, dry mouth or throat, nausea, vomiting, pancreatitis, increased liver activity їTransaminases, hepatitis, jaundice.

Blood system, lymphatic system: purpura (most often described as bruising resulting from physical injury), leukopenia, thrombocytopenia.

Musculoskeletal system: arthralgia, back pain, increased fragility of bones, myalgia.

Nervous system: dizziness; headache; hyperkinesis; muscle dyskinesia and paging; choreoathetosis; weakening or absence of tendon reflexes; dysarthria; ataxia; nystagmus; paresthesia; convulsions; confusion of consciousness; increased fatigue; asthenia; amnesia; depression; violation of thinking; hostility; emotional lability; insomnia; anxiety; drowsiness; hallucinations: tremors; tics; malaise.

Respiratory system: rhinitis, pharyngitis, bronchitis, pneumonia, cough, shortness of breath, respiratory infections.

Skin and subcutaneous tissues: acne, peripheral edema, allergic reactions: itching of the skin, skin rash, exudative erythema multiforme (including Stevens-Johnson syndrome).

Genitourinary system: urinary tract infection, impotence, urinary incontinence, acute renal failure.

Sense organs: visual impairment, amblyopia, diplopia, tinnitus, otitis media.

Others: fever, viral infection, weight gain, lability of plasma glucose levels in patients with diabetes mellitus, pain of various localization, gynecomastia, breast enlargement, generalized edema.

Overdose :

Symptoms: dizziness, diplopia, speech impairment, drowsiness, lethargy, diarrhea and increased severity of other side effects.

Treatment: gastric lavage, intake of activated charcoal, symptomatic therapy. Patients with severe renal insufficiency may be indicated for hemodialysis.

Interaction with other medicinal products :

Morphine: with the combined administration of gabapentin and morphine, when morphine was taken 2 hours before taking gabapentin, there was an increase in the mean area under the concentration-time pharmacokinetic curve (AUC) of gabapentin by 44% compared with gabapentin monotherapy, which was associated with an increase in the brachial threshold (cold pressor test). The clinical significance of this change has not been established, and the pharmacokinetic characteristics of morphine did not change. The side effects of morphine when taken together with gabapentin did not differ from those when taking morphine together with placebo.
Interactions between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine have not been observed. The steady state pharmacokinetics of gabapentin are similar in healthy individuals and in patients receiving other anticonvulsants. The simultaneous use of gabapentin with oral contraceptives containing norethisterone and / or ethinyl estradiol was not accompanied by changes in the pharmacokinetics of both components.
The simultaneous use of gabapentin with antacids containing aluminum and magnesium is accompanied by a decrease in the bioavailability of gabapentin by about 20%. It is recommended to take gabapentin approximately 2 hours after taking the antacid. Probenecid does not affect the renal excretion of gabapentin.
The slight decrease in renal excretion of gabapentin while taking cimetidine is probably not of clinical significance.

Special instructions :

Although withdrawal syndrome with the development of seizures during treatment with gabapentin was not noted, nevertheless, abrupt cessation of antiepileptic therapy in patients with partial seizures can provoke the development of seizures (see Dosage and Administration).
Gabapentin is not considered to be an effective treatment for absence epilepsy. In patients requiring concomitant morphine therapy, an increase in the gabapentin dose may be required. At the same time, it is necessary to ensure careful monitoring of patients for the development of such a sign of depression of the central nervous system (CNS), such as drowsiness. In this case, the dose of gabapentin or morphine should be adequately reduced (see 'Interaction with other medicinal products').

Laboratory Tests
When gabapentin has been added to other anticonvulsants, false positive results have been reported for urine protein with Ames N-Multistix SGЃ Test Strips. For the determination of protein in urine, it is recommended to use a more specific precipitation method with sulfosalicylic acid.
Patients should avoid driving a car, as well as performing work that requires the speed of performance of psychomotor reactions.

Release form :

Capsules 300 mg. On 10 or 15 capsules in a blister strip packaging from a film of polyvinyl chloride and printed aluminum foil varnished.
3, 5, 10 blister packs of 10 capsules or 2, 4, 6 blister packs of 15 capsules, together with instructions for use, are placed in a cardboard box for consumer packaging.

Storage conditions :

Store in a dry, dark place at a temperature not exceeding 25 ? C. Keep out of the reach of children.

Expiration date :

2 years. Do not use after the expiration date.

Terms of dispensing from pharmacies :

On prescription.