Gabapentin

The analogues of this drug are: Gabagama 100, Gabagama 300, Gabagama 400, Gabalept, Gabantin 100, Gabastadine, Grimodin, Lamitril, Neurontin, Topilepsin, Tebantinum, Epileptal, etc.

[1], [2],

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 for adults and children over 12 years of age with local (partial or focal) unregulated convulsions due to primary (idiopathic) epilepsy, as well as tonic-clonic seizures and somatosensory paroxysms in secondary (symptomatic) epilepsy (temporal, mesial and etc.)

Also indications for the use of gabapentin is children's partial epilepsy with a pronounced delay in psychomotor development, in which drug treatment is ineffective (so-called resistant epilepsy).

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

[3], [4]

Release form

Form release - capsules; one capsule contains 300 mg of active substance gabapentin.

[5], [6], [7]

Pharmacodynamics

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

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

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 excitation of the central nervous system. As a result, the exciting and inhibitory processes come to equilibrium.

[8], [9], [10], [11], [12]

Pharmacokinetics

The maximum concentration of gabapentin in the blood plasma is noted 2-3 hours after taking the drug inside. With plasma proteins, no more than 3-5% of the active substance binds.

Absolute bioavailability of the drug in the form of capsules does not exceed 60%, with increasing dose bioavailability decreases. The average half-life of gabapentin from plasma is between five and seven hours and does not depend on the dose taken.

Gabapentin is not metabolized and unchanged is excreted from the body by the kidneys. The drug does not promote the production of liver oxidative enzymes involved in the metabolism of drugs. In elderly patients and patients with impaired renal function, the rate of purification of blood plasma from gabapentin is reduced, so dosage should be adjusted.

[13], [14], [15]

Dosing and administration

Capsules of gabapentin are taken orally regardless of food intake, with plenty of water. The dosage of the drug is determined by the attending physician. With epileptic seizures, treatment starts 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 way of using gabapentin: one capsule (300 mg) three times a day. To prevent the resumption of seizures, the drug should be taken at intervals not exceeding 12 hours.

The maximum daily dose of this drug is 3600 mg, which is divided into three equal in volume reception. Selection of a dose for renal insufficiency is made on the basis of the data of tests on the effectiveness of the kidneys on the purification of blood from metabolic products - creatinine clearance.

[19], [20], [21], [22], [23], [24]

Use Gabapentin during pregnancy

Since there are 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 benefits of the expectant mother exceed the possible risk to the fetus.
Gabapentin penetrates into breast milk, but the effect of this drug on the infant is not studied. For this reason, if taking gabapentin coincides with the period of lactation, it is recommended to stop breastfeeding.

Contraindications

Contraindications to the use of antiepileptic drugs Gabapentin and its analogues are hypersensitivity to the components that make up the drug, as well as age to 12 years. The administration of this drug to patients with renal insufficiency requires caution.

[16],

Side effects Gabapentin

The undesirable side effects of gabapentin and all its analogues from the cardiovascular system are manifested in the form of tachycardia (rapid heartbeat), increased blood pressure and an increase in the lumen of the blood vessels (vasodilation), which arises from the temporary decrease in muscle tone of the vascular wall.

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

Taking this medication can also cause abdominal pain, diarrhea, flatulence, dry mouth, nausea and vomiting, jaundice. Possible edema and allergic skin reactions (pruritus, rash, exudative erythema). Often there are muscle pains, painful sensations in the back and joints, fragility of bones increases.

Among the possible side effects of gabapentin are also noted an increase in body weight and fluctuations in blood glucose levels in patients with diabetes mellitus.

[17], [18]

Overdose

Excess dosage of gabapentin and its analogues is manifested by symptoms such as dizziness, drowsiness, frequent loose stools (diarrhea), diplopia (double image), speech impairment, and a more intense manifestation of side effects of this drug.

In case of an overdose of Gabapentin, gastric lavage should be performed, activated charcoal should be taken and the prescriber's appointments directed to symptomatic therapy should be performed. In the case of severe renal failure, patients can undergo extrarenal blood purification (hemodialysis).

[25], [26]

Interactions with other drugs

The use of gabapentin along with other antiepileptic drugs is considered possible, but this combination reduces the effectiveness of oral hormonal contraceptives. Alcohol and sedatives can enhance all of the above side effects of gabapentin.

Bioavailability of gabapentin significantly reduces some antacids containing magnesium and aluminum (used in the treatment of acid-dependent gastrointestinal diseases). Therefore, it is recommended to take gabapentin not less than two hours after taking an antacid.

Used with gastric ulcer and duodenal ulcer antihistamine cimetidine reduces the output of gabapentin by the kidneys.

[27], [28]

Storage conditions

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

[29], [30], [31], [32]

Shelf life

Shelf life of the drug is 24 months.