Neurointin – official instructions for use and prices – Medicines | For everything.
Active substance: gabapentin Capsules contain 100 mg, 300 mg, 400 mg or 600 mg gabapentin; film-coated tablets contain 600 mg or 800 mg gabapentin.
Excipients: capsules contain lactose monohydrate, corn starch, magnesium hydrosilicate (talc) (capsules contain: gelatin, titanium dioxide, iron oxide yellow dye (caps. 300mg and 400 mg), iron dye oxide red (caps. 400 mg) sodium lauryl sulfate; inks contain: shellac, titanium dioxide, indigo carmine); film-coated tablets contain poloxamer 407, copovidone, corn starch, magnesium stearate, opadry white YS-1-18111 (contains talc, hyprolose), and herbal wax (candelica).
Capsules 100 mg: solid opaque gelatin capsules containing white or almost white powder, with a lid and body in white, blue printed on the lid of the Neurontin ® and 100 mg, on the body – "PD" in the form of a monogram in a circle . Size No. 3.
Capsules of 300 mg: hard opaque gelatin capsules containing white or almost white powder, with a lid and body in a light yellow color, marked in gray on the lid of "Neurontin ® " and "300 mg", on the body – "PD" in the form of a monogram in the circle. Size No. 1.
Capsules 400 mg:hard opaque gelatin capsules, containing white or almost white powder, with a lid and body of cream-orange color, gray on the lid "Neurontin" and "400 mg", on the body – "PD" in the form of a monogram in a circle. Size No. 0.
Dosage 600 mg: white, elliptical tablets, film-coated tablets, engraved with "NT" and "16", a risk between engraving on one side and a risk on the other side.
Dosage 800 mg: white elliptical tablets, film-coated tablets, engraved with "NT" and "26", a risk between engraving on one side and a risk on the other side.
Pharmacotherapeutic group : antiepileptic drug.
Gabapentin is structurally similar to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from that of some other drugs that interact with GABA receptors, including valproate, barbiturates, benzodiazepines, inhibitors of GABA-transaminase reuptake inhibitors GABA agonists, GABA and GABA prodrug forms: it does not possess GABA-ergic properties and does not affect the uptake and metabolism of GABA. Preliminary studies suggest that gabapentin binds to the α2-δ-subunit of voltage-dependent calcium channels and inhibits the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms involved in the action of gabapentin in neuropathic pain are: reduction of glutamate-dependent neuronal death, increased synthesis of GABA, suppressing the release of neurotransmitters of the monoamine group. At clinically relevant concentrations, gabapentin does not bind to receptors of other common drugs or neurotransmitters, including GABAH, GABAc, benzodiazepine, glutamate, glycine or N-methyl-d-aspartate receptors. Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels in vitro. Gabapentin has 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 μmol, which is not achieved in vivo. Gabapentin somewhat reduces the release of monoamine neurotransmitters in vitro. The use of gabapentin in rats led to an increase in the exchange of GABA in some areas of the brain; this effect was similar to that of sodium valproate, although it was observed in other parts of the brain. The significance of these effects of gabapentin for its anticonvulsant activity has not been established. In animals, gabapentin easily penetrates into the brain tissue and prevents seizures caused by maximum electroshock, chemicals, including inhibitors of GABA synthesis, as well as due to genetic factors.
The bioavailability of gabapentin is not proportional to the dose; so, with increasing dose, it decreases. After ingestion, the maximum concentration (Cmax) of gabapentin in plasma is reached in 2-3 hours. The absolute bioavailability of gabapentin in capsules is about 60%. Food, including those with a high fat content, does not affect the pharmacokinetics. Removal of gabapentin from plasma is best described using a linear model. The half-life (T1 / 2) of plasma does not depend on the dose and averages 5-7 hours. The pharmacokinetics do not change with repeated use; equilibrium plasma concentrations can be predicted based on the results of a single dose of the drug. Gabapentin is practically not bound to plasma proteins (<3%) and has a distribution volume of 57.7 l. Excreted exclusively by the kidneys unchanged, no signs of human metabolism were found. The drug does not induce mixed-function oxidative liver enzymes involved in drug metabolism. The clearance of gabapentin from plasma is reduced in the elderly and in patients with impaired renal function. The 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 patients receiving treatment with hemodialysis, dose adjustment is recommended (see Dosage and Administration, Table 1). It has been established that plasma concentrations of gabapentin in children aged 4 to 12 years are generally similar to those in adults. The clearance of gabapentin from plasma is reduced in the elderly and in patients with impaired renal function. The 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 patients receiving treatment with hemodialysis, dose adjustment is recommended (see Dosage and Administration, Table 1). It has been established that plasma concentrations of gabapentin in children aged 4 to 12 years are generally similar to those in adults. The clearance of gabapentin from plasma is reduced in the elderly and in patients with impaired renal function. The 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 patients receiving treatment with hemodialysis, dose adjustment is recommended (see Dosage and Administration, Table 1). It has been established that plasma concentrations of gabapentin in children aged 4 to 12 years are generally similar to those in adults. dose adjustment is recommended (see Dosage and Administration, Table 1). It has been established that plasma concentrations of gabapentin in children aged 4 to 12 years are generally similar to those in adults. dose adjustment is recommended (see Dosage and Administration, Table 1). It has been established that plasma concentrations of gabapentin in children aged 4 to 12 years are generally similar to those in adults.
Treatment of neuropathic pain in adults aged 18 years and older. Efficacy and safety in patients under the age of 18 years have not been established.
Monotherapy of partial seizures with secondary generalization and without it in adults and children over the age of 12 years. The efficacy and safety of monotherapy in children under the age of 12 years have not been established.
As an additional agent in the treatment of partial seizures with secondary generalization and without it in adults and children aged 3 years and older. The safety and efficacy of additional gabapentin therapy in children less than 3 years old have not been established.
Hypersensitivity to gabapentin or auxiliary components of the drug. These dosage forms are not intended for use in children under the age of 3 years.
Renal failure (see. "Dosage and administration").
There are no data on the use of the drug in pregnant women, so 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 the infant being fed is unknown, so during breastfeeding Neurontin should be prescribed only if the benefit to the mother clearly outweighs the risk to the infant.
Dosage and administration Neurontin is administered orally, regardless of the meal or with food. If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative means, this should be done gradually over at least one week.
Adults and children over the age of 12 years: 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 increased gradually to 900 mg according to the scheme described above (see the section "Neuropathic pain in adults"). Subsequently, the dose can be increased to a maximum of 3,600 mg / day (divided into 3 equal doses). There was a good tolerability of the drug in doses up to 4800 mg / day. The maximum interval between doses when taking the drug three times should not exceed 12 hours in order to avoid the resumption of seizures.
Children aged 3-12 years:The initial dose of the drug varies from 10 to 15 mg / kg / day, which is prescribed in equal doses 3 times a day and increased to an effective amount for approximately 3 days. The effective dose of gabapentin in children aged 5 years and older is 25-35 mg / kg / day in equal doses in 3 doses. The effective dose of gabapentin in children aged 3 to 5 years is 40 mg / kg / day in equal doses in 3 doses. A good tolerability of the drug in doses up to 50 mg / kg / day with prolonged use. The maximum interval between doses of the drug should not exceed 12 hours in order to avoid the resumption of seizures.
There is no need to control the concentration of gabapentin in plasma. It can be used in combination with other anticonvulsants without taking into account changes in its plasma concentration or the concentration of other anticonvulsant drugs in serum.
Selection of doses for renal failure.