Gabapentin - instructions for use, dose, side effects, contraindications

Description:Capsules number 0 green. The contents of capsules are white or almost white powder.Allowed the presence of lumps, which, when pressed with a glass rod, easily turn into a powder.

Pharmacotherapeutic group:Antiepileptic remedy

ATX: & nbsp

N.03.A.X.12 Gabapentin

Pharmacodynamics:Gabapentin structurally similar to a neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action is different from other drugs that interact with GABA receptors (valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA capture inhibitors, GABA agonists and prodrugs of GABA). It does not possess GABA-ergic properties and does not affect the capture and metabolism of GABA. Preliminary studies have shown that gabapentin is associated with α₂-δ-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, a suppression of the release of neurotransmitters of the monoamine group. Gabapentin at clinically significant concentrations, does not bind to receptors that are sensitive to other drugs (LS) or neurotransmitters, including GABA, HAMIB, benzodiazepine, glutamate, glycine or N-methyl-d-aspartate receptors. 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 μmol, which is not achieved in vivo. Gabapentin slightly reduces the release of monoamine neurotransmitters in vitro.

Pharmacokinetics:The bioavailability of gabapentin is not proportional to the dose. So, with an increase in the dose, it decreases. After oral administration, the maximum concentration (C_max) gabapentin in plasma is achieved after 2-3 hours. Absolute bioavailability of gabapentin in capsules is about 60%. Food, including those with a high fat content, does not affect the pharmacokinetics. Half-life (T_1/2) from the plasma does not depend on the dose and averages 5-7 hours. 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: Gabapentin practically does not bind to plasma proteins (<3%) and has a volume 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 a mixed function involved in the metabolism of drugs. The clearance of gabapentin from plasma decreases in elderly people and in patients with impaired renal function. The rate of elimination constant, clearance from plasma and renal clearance are directly proportional to the creatinine clearance. Gabapentin is removed from the plasma during hemodialysis. In patients with impaired renal function and patients receiving hemodialysis treatment, dose adjustment is recommended (see Dosage and Administration).

Indications:

- Epilepsy: partial seizures with secondary generalization and without it in adults and children over 12 years of age (monotherapy); partial seizures with secondary generalization and without it in adults (additional drugs); resistant form of epilepsy in children older than 3 years (additional drugs).

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

Contraindications:Hypersensitivity to any of the components of the drug,age to 12 years (due to the impossibility of accurate dosing).

Carefully:Renal failure (see "Method of administration and dose").

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.

Dosing and Administration:

Inside, swallowing whole, regardless of food intake and 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.

NeuropamAdult pain

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 begin immediately with a dose of 900 mg / 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:

Day 1: 300 mg once a day

Day 2: 300 mg twice a day

Day 3: 300 mg 3 times a day

Partial cramps

Adults and children from 12 years: The effective dose is from 900 to 3600 mg / 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 (see the 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 with a three-time intake of the drug should not exceed 12 hours in order to avoid the resumption of seizures.

Selection of a dose for renal failure.

Patients with renal failure are recommended to reduce the dose of gabapentin according to the table:

Creatinine clearance (ml / min)	Daily dose (mg / day)
>80	900-2400
50-79	600-1200
30-49	300-600
15-29	150*-300
<15	150*

* Assign 300 mg every other day.

Recommendations for patients on hemodialysis.

Patients on hemodialysis who had not previously taken gabapentin, the drug is recommended to be prescribed in a saturating dose of 300-400 mg, and then apply it to 200-300 mg every 4 hours of hemodialysis.

Side effects:

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

The 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 activity of "hepatic" trances inases, hepatitis, jaundice.

System of blood, lymphatic system: purpura (most often it is described as bruising that occurs during physical trauma), leukopenia, thrombocytopenia.

Musculoskeletal system: arthralgia, back pain, increased brittle bones, myalgia.

Nervous system: dizziness; headache; hyperkinesis; muscular dyskinesia and dysthia; 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: tremor; tics; malaise.

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

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

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

Sense organs: impaired vision, amblyopia, diplopia, tinnitus, otitis media.

Other: fever, viral infection, weight gain, lability of the glucose level in plasma of blood in patients with diabetes mellitus, pain of different localization, gynecomastia, enlargement of mammary glands, generalized edema.

Overdose:Symptoms: dizziness, diplopia, speech impairment, drowsiness, lethargy, diarrhea and increased severity of other side effects. Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy. Patients with severe renal insufficiency can be shown hemodialysis.

Interaction:Morphine: with the joint administration of gabapentin and morphine, when morphine was taken 2 hours prior to administration of gabapentin, an increase in the average area under the faq-macokinetic concentration-time curve (AUC) of gabapentin by 44% compared to gabapentin monotherapy 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 the 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 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 bioavailability of gabapentin by approximately 20%. Gabapentin it is recommended to take about 2 hours after taking an antacid. Probenecid does not affect renal excretion of gabapentin.

A small decrease in renal excretion of gabapentin with simultaneous administration of cimetidine is probably of no clinical significance.

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 seizures (see Dosage and Administration).

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 (see "Interaction-with other drugs").

Laboratory research

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

Effect on the ability to drive transp. cf. and fur:Patients should avoid driving, as well as performing work that requires quickness in performing psychomotor reactions.

Form release / dosage:

Capsules 300 mg.

Packaging:

For 10 or 15 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 3, 5, 10 contour cell packs of 10 capsules or 2, 4, 6 contour cell packs of 15 capsules together with the instruction for use are placed in a pack of cardboard for consumer containers.

Storage conditions:Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003736/09

Date of registration:15.05.2009

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp11.03.2017

Illustrated instructions

Instructions

Gabapentin (Gabapentin)