Gabapentin

Analogues of this drug are: Gabagama 100, Gabagama 300, Gabagama 400, Gabalept, Gabantin 100, Gabastadin, Grimodin, Lamitril, Neurontin, Topilepsin, Tebantin, Epileptal, etc.

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Indications Gabapentin

The main use of this drug is the treatment of epilepsy, which is one of the most common chronic neurological diseases. As a monotherapeutic agent, Gabapentin is prescribed to adults and children over 12 years of age for local (partial or focal) non-generalized seizures caused by primary (idiopathic) epilepsy, as well as tonic-clonic seizures and somatosensory paroxysms in secondary (symptomatic) epilepsy (temporal, mesial, etc.)

Another indication for the use of Gabapentin is childhood partial epilepsy with severe delay in psychomotor development, in which drug treatment is ineffective (the so-called resistant epilepsy).

In addition, Gabapentin is used as an adjunctive treatment in adults with peripheral neuropathy of various etiologies ( diabetic, postherpetic), as well as neuralgia caused by shingles.

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Release form

Release form: capsules; one capsule contains 300 mg of the active substance gabapentin.

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Pharmacodynamics

The therapeutic neuroprotective properties of the drug Gabapentin and its analogues are based on their active substance - gabapentin, which is 1-aminomethyl-cyclohexaneacetic acid and is structurally an analogue of the endogenous neurotransmitter - gamma-aminobutyric acid (GABA).

The function that GABA performs in the central nervous system is to change the activity of neurons, slowing down (inhibiting) synaptic transmission of impulses, as well as the transmission of signals from neurons to muscle tissue. Thus, Gabapentin - similar to GABA - acts as an inhibitory mediator (mediator) between the membrane receptors of neurons and special sections of the central nervous system located in the cerebral cortex.

In addition, the biologically active substance of the drug Gabapentin helps to increase the level of gamma-aminobutyric acid in the blood plasma, which reduces the concentration of excitatory monoamine neurotransmitters and the pathological activity of CNS excitation. As a result, excitatory and inhibitory processes come into balance.

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Pharmacokinetics

The maximum concentration of Gabapentin in blood plasma is observed 2-3 hours after oral administration. No more than 3-5% of the active substance binds to plasma proteins.

The absolute bioavailability of the drug in capsule form does not exceed 60%, with an increase in the dose, bioavailability decreases. The average half-life of Gabapentin from plasma is from five to seven hours and does not depend on the dose taken.

Gabapentin is not metabolized and is excreted unchanged by the kidneys. The drug does not promote the liver's production of oxidative enzymes involved in drug metabolism. In elderly patients and patients with impaired renal function, the rate of plasma clearance of gabapentin is reduced, so the dosage must be adjusted.

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Dosing and administration

Gabapentin capsules are taken orally, regardless of food intake, with plenty of water. The dosage of the drug is determined by the attending physician. For epileptic seizures, treatment begins with taking one capsule (300 mg) on the first day; two capsules - twice during the second day; three capsules - three times during the third day.

The second acceptable method of using Gabapentin is one capsule (300 mg) three times a day. To prevent the recurrence of seizures, the drug should be taken at intervals of no more than 12 hours.

The maximum daily dose of this drug is 3600 mg, which is divided into three equal doses. The dose for renal failure is selected based on the data from tests on the effectiveness of the kidneys in cleansing the blood of metabolic products - creatinine clearance.

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Use Gabapentin during pregnancy

Since there is no data on the use of Gabapentin during pregnancy, the use of this drug (and its analogues) for the treatment of pregnant women is justified only if the expected health benefit to the expectant mother outweighs the possible risk to the fetus.
Gabapentin penetrates into breast milk, but the effect of this drug on a breastfed baby has not been studied. For this reason, if taking gabapentin coincides with the lactation period, it is recommended to stop breastfeeding.

Contraindications

Contraindications to the use of the antiepileptic drug Gabapentin and its analogues are hypersensitivity to the components included in the drug, as well as age under 12 years. Prescribing this drug to patients with renal insufficiency requires caution.

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Side effects Gabapentin

Undesirable side effects of Gabapentin and all its analogues from the cardiovascular system are manifested in the form of tachycardia (increased heart rate), increased blood pressure and an increase in the lumen of blood vessels (vasodilation), which occurs due to a temporary decrease in the tone of the muscles of the vascular wall.

From the side of the central nervous system, dizziness and headache, tinnitus, increased fatigue, sleep disturbances, anxiety, confusion and hallucinations, amnesia, depression, as well as visual impairment - reversible decreased vision (amblyopia) and double vision (diplopia) are observed.

Taking this drug may also cause abdominal pain, diarrhea, flatulence, dry mouth, nausea and vomiting, jaundice. Edema and allergic skin reactions (itching, rash, exudative erythema) are possible. Muscle pain, pain in the back and joints, and increased bone fragility often occur.

Possible side effects of Gabapentin also include weight gain and fluctuations in blood glucose levels in patients with diabetes.

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Overdose

Exceeding the dosage of the drug Gabapentin and its analogues is manifested by symptoms such as dizziness, drowsiness, frequent loose stools (diarrhea), diplopia (double vision), speech impairment, as well as more intense manifestation of the side effects of this drug.

In case of overdose of Gabapentin, gastric lavage should be performed, activated charcoal should be taken, and the attending physician's instructions for symptomatic therapy should be followed. In case of severe renal failure, patients may undergo extrarenal blood purification (hemodialysis).

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Interactions with other drugs

The use of Gabapentin together with other antiepileptic drugs is considered possible, but such a combination reduces the effectiveness of oral hormonal contraceptives. Alcohol and sedatives can increase all of the above side effects of Gabapentin.

The bioavailability of Gabapentin is significantly reduced by some antacid drugs containing magnesium and aluminum (used in the treatment of acid-dependent gastrointestinal diseases). Therefore, it is recommended to take Gabapentin at least two hours after taking an antacid.

The antihistamine drug cimetidine, used for gastric ulcer and duodenal ulcer, reduces the excretion of Gabapentin by the kidneys.

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Storage conditions

Gabapentin and all its analogues should be stored at a temperature not exceeding +24-25°C - in a dry place, protected from light and inaccessible to children.

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Shelf life

The shelf life of the drug is 24 months.