Gabapentin - instructions for use, reviews, analogs and forms of release (capsules or tablets 100 mg, 300 mg and 400 mg) drugs for the treatment of epilepsy and partial seizures, pain in neuralgia in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Gabapentin. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Gabapentin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of gabapentin in the presence of existing structural analogues.Use for the treatment of epilepsy and partial seizures, pain in neuralgia in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Gabapentin - similar in structure to a neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from other drugs interacting with GABA receptors (valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA capture inhibitors, GABA agonists and prodrug forms GABA). It does not possess GABA-ergic properties and does not affect the capture and metabolism of GABA.

Preliminary studies have shown that gabapentin binds to the alpha2-omega subunit of voltage-dependent calcium channels and reduces the flow of calcium ions, which plays an important role in the occurrence of neuropathic pain. Other mechanisms of action of gabapentin in neuropathic pain are a decrease in glutamate-dependent neuronal death, an increase in GABA synthesis, suppression, release of the neurotransmitters of the monoamine group. Gabapentin in clinically significant concentrations does not bind to the receptors of other common drugs or neurotransmitters,including GABA, GABAA, benzodiazepine, glutamate, glycine, or N-methyl-D-aspartate receptors.

Unlike phenytoin and carbamazepine, gabapentin does not interact with sodium channels. 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 μmol, which is not achieved in vivo. Gabapentin somewhat reduces the release of monoamine neurotransmitters.

Composition

Gabapentin + auxiliary substances.

Pharmacokinetics

The bioavailability of gabapentin is not proportional to the dose. So, with an increase in the dose, it decreases. Absolute bioavailability of gabapentin in capsules is about 60%. Food, incl. with a high fat content, does not affect the pharmacokinetics. The elimination of gabapentin from plasma is best described using a linear model. Pharmacokinetics does not change with repeated application; equilibrium concentrations in plasma can be predicted based on the results of a single dose of the drug. The drug does not induce oxidative liver enzymes with a mixed function involved in the metabolism of drugs.It is excreted exclusively by the kidneys in unchanged form, it is not metabolized.

The clearance of gabapentin from plasma decreases in elderly people and in patients with impaired renal function. Gabapentin is removed from the plasma during hemodialysis. In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended.

Indications

• monotherapy or as an additional agent for the treatment of partial seizures or epileptic seizures with secondary generalization or without it in adults and children with 12 years of age with epilepsy;
• Neuropathic pain in adults (18 years and older) with postherpetic neuralgia and other diseases.

Forms of release

Capsules 100 mg, 300 mg and 400 mg (sometimes mistakenly called tablets).

Instructions for use and dosage

Inside, swallowing whole, regardless of the reception of food and drink plenty of liquids. If it is necessary to reduce the dose, cancel the drug or replace it with an alternative remedy, this should be done gradually for 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 per day.Treatment can begin immediately with a dose of 900 mg per day (300 mg 3 times a day) or within the first 3 days the dose can be increased gradually to 900 mg per day according to the following scheme:

• 1st day: 300 mg once a day;
• Day 2: 300 mg twice daily;
• Day 3: 300 mg 3 times a day.

Partial cramps

Adults and children from 12 years: effective dose - from 900 to 2400 mg per day. Therapy can begin with a dose of 300 mg 3 times a day on the first day or increase gradually to 900 mg according to the scheme described above. Subsequently, the dose can be increased to a maximum of 3600 mg per day (divided into 3 equal receptions). The maximum interval between doses with a triple take of the drug should not exceed 12 hours in order to avoid the resumption of seizures.

Recommendations for patients on hemodialysis

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

Side effect

In the treatment of neuropathic pain

• accidental injury;
• asthenia;
• backache;
• influenza-like syndrome;
• headache;
• infection;
• pain of different localization;
• peripheral edema;
• increase in body weight;
• alcohol intolerance;
• constipation, diarrhea;
• dry mouth;
• dyspepsia;
• flatulence;
• nausea, vomiting;
• abdominal pain;
• violation of gait;
• amnesia;
• ataxia;
• confusion of consciousness;
• dizziness;
• drowsiness;
• violation of thinking;
• tremor;
• dyspnea;
• pharyngitis;
• skin rash.

When treating partial seizures

• backache;
• fatigue;
• fever;
• headache;
• viral infection;
• peripheral edema;
• increase in body weight;
• asthenia;
• alcohol intolerance;
• general malaise;
• swelling of the face;
• symptoms of vasodilation or hypertension;
• constipation, diarrhea;
• dyspepsia;
• increased appetite;
• dry mouth or throat;
• nausea, vomiting;
• abdominal pain;
• flatulence;
• anorexia;
• gingivitis;
• leukopenia, purpura;
• fractures;
• myalgia;
• arthralgia;
• amnesia;
• ataxia;
• confusion of consciousness;
• lack of coordination;
• depression;
• dysarthria;
• emotional lability;
• insomnia;
• nervousness;
• drowsiness;
• violation of thinking;
• muscle twitching;
• dizziness;
• hyperkinesis;
• amplification, attenuation or absence of reflexes;
• paresthesia;
• anxiety;
• hostility;
• cough;
• pharyngitis;
• rhinitis;
• pneumonia;
• abrasions;
• itching of the skin;
• skin rash;
• urinary tract infection;
• impaired vision;
• impotence.

Contraindications

• hypersensitivity to any of the components of the drug;
• age up to 12 years with partial seizures.

Application in pregnancy and lactation

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 influence on the infant is unknown, so during treatment should abandon breastfeeding.

Use in children

Contraindicated at the age of 12 years with partial seizures. To treat neuropathic pain, do not prescribe to children and adolescents under 18 years of age.

special instructions

Although withdrawal syndrome with the development of seizures in the treatment of gabapentin is not noted, nevertheless, a sharp cessation of therapy with antiepileptic drugs in patients with partial seizures can provoke the development of convulsions.

GABAPENTIN is not considered an effective treatment for absence-epilepsy.

Patients who require co-therapy with morphine may require an increase in the dose of gabapentin.In this case, it is necessary to ensure close monitoring of patients for the development of such a sign of central nervous system (CNS) depression as drowsiness. In this case, the dose of gabapentin or morphine should be adequately reduced.

Laboratory research

When Gabapentin was added to other anticonvulsants, false-positive results were detected when determining the protein in the urine using Ames N-Multistix SG test strips. To determine the protein in the urine it is recommended to use a more specific method of precipitation with sulfosalicylic acid.

Impact on the ability to drive vehicles and manage mechanisms

Patients should avoid driving, as well as performing work requiring quickness of psychomotor reactions.

Drug Interactions

Morphine: when combined with gabapentin and morphine, when morphine was taken 2 hours before taking gabapentin, the mean area under the pharmacokinetic AUC of gabapentin increased by 44% compared to gabapentin alone, which was associated with an increase in the pain threshold (cold pressor test).The clinical significance of this change has not been established, the pharmacokinetic characteristics of morphine remain unchanged. 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 pharmacokinetics of gabapentin in an equilibrium state is the same in healthy people and patients receiving other anticonvulsants.

The simultaneous use of gabapentin with oral contraceptives containing norethisterone and / or ethinylestradiol 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 approximately 20%. It is recommended to take gabapentin approximately 2 hours after taking an antacid.

Probenecid does not affect the renal excretion of gabapentin.

A slight decrease in gabapentin's renal excretion with concurrent administration of cimetidine is probably of no clinical significance.

Analogues of the drug Gabapentin

Structural analogs for the active substance:

• Gabagamma;
• Gabantine;
• Gapentec;
• Caten;
• Convalis;
• Neuronthin;
• Tebantin;
• Egipentin;
• Eplorontin.

Analogues on the curative effect (antiepileptic drugs):

• Algerian;
• Acetazolamide;
• Benzobarbital;
• Benzon;
• Valopixime;
• Valparin;
• Valproic acid;
• Wimpat;
• Habitryl;
• Hexamidine;
• Depakin;
• Depakin chrono;
• Depamid;
• Diazepam;
• Diakarb;
• Diphenine;
• Zagreton;
• Zenicetam;
• Zeptol;
• Zonegran;
• Inovevelon;
• Carbaleptin retard;
• Carbamazepine;
• Clonazepam;
• Convalis;
• Convulex;
• Convulsant;
• Convulsofin;
• Lamyctal;
• Lamitor;
• Lamotrigine;
• Levetinol;
• Levetiracetam;
• Lyrics;
• Mysolin;
• Paglyuferal;
• Pregabalin;
• Prigabilon;
• Primidone;
• Relium;
• Replica;
• Sibazon;
• Suxilep;
• Tegretol;
• Topamax;
• Topiramate;
• Trobult;
• Phenobarbital;
• Finlepsin;
• Finlepsin retard;
• Chloracon;
• Exalieff;
• Enkorat;
• Epimax;
• Eplorontin.

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