Are gabapentin tablets psychotropic or not? Medicinal reference book geotar

Registration number:

Trade name: Gabapentin

International nonproprietary name: gabapentin

Dosage form: capsules

Compound: 1 capsule contains:
active substance: gabapentin - 300 mg;
excipients: calcium hydrogen phosphate dihydrate (Emcompress), potato starch, macrogol (polyethylene glycol 6000), magnesium stearate; capsule composition: body and cap - titanium dioxide, quinoline yellow dye, indigo carmine dye - FD&C Blue 2, gelatin.

Description:
Capsules No. 0 are green. The contents of the capsules are white or almost white powder. The presence of lumps is allowed, which, when pressed with a glass rod, easily turns into powder.

Pharmacotherapeutic group: antiepileptic drug.

ATX Code: .

PHARMACOLOGICAL PROPERTIES.
Pharmacodynamics:
Gabapentin is structurally similar to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from other drugs that interact with GABA receptors (valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, GABA agonists and prodrugs GABA). It does not have GABAergic properties and does not affect the uptake and metabolism of GABA. Preliminary studies have shown that gabapentin binds to the α2-σ subunit of voltage-gated calcium channels and reduces the flow of calcium ions, which plays an important role in neuropathic pain. Other mechanisms of action of gabapentin in neuropathic pain are a decrease in glutamate-dependent neuronal death, an increase in the synthesis of GABA, and a suppression of the release of monoamine neurotransmitters. Gabapentin at clinically significant concentrations does not bind to receptors sensitive to other drugs (drugs) or neurotransmitters, including GABAd, GABAb, 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 concentrations greater than 100 μM, 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 dose. So, as the dose increases, it decreases. After oral administration, the maximum concentration (Cmax) of gabapentin in plasma is achieved after 2-3 hours. The absolute bioavailability of gabapentin in capsules is about 60%. Food, including those high in fat, does not affect pharmacokinetics. The half-life (T1/2) from plasma does not depend on the dose and averages 5-7 hours. Pharmacokinetics does not change with repeated use; Steady-state plasma concentrations can be predicted from the results of a single dose of the drug. Gabapentin practically does not bind to plasma proteins (<3%) и имеет объем распределения 57,7 л. Выводится исключительно почками в неизмененном виде, метаболизму не подвергается. Препарат не индуцирует окислительные ферменты печени со смешанной функцией, участвующие в метаболизме лекарственных средств. Клиренс габапентина из плазмы снижается у пожилых людей и больных с нарушенной функцией почек. Константа скорости выведения, клиренс из плазмы и почечный клиренс прямо пропорциональны клиренсу креатинина. Габапентин удаляется из плазмы при гемодиализе. У больных с нарушенной функцией почек и пациентов, получающих лечение гемодиализом, рекомендуется коррекция дозы (см. Способ применения и дозы).

Indications for use:

epilepsy: partial seizures with and without secondary generalization in adults and children over 12 years of age (myotherapy); partial seizures with and without secondary generalization in adults (additional medicine); resistant form of epilepsy in children over 3 years of age (additional medicine).

neuropathic pain in adults (18 years and older). Contraindications:
Hypersensitivity to any of the components of the drug, age under 12 years (due to the impossibility of precise dosing). With caution
Renal failure (see "Method of administration and dosage"). Use during 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 expected benefit to the mother justifies the possible risk to the fetus.
Gabapentin is excreted in breast milk; its effect on a nursing baby is unknown, so breastfeeding should be avoided during treatment. Directions for use and doses:
Inside, swallow whole, regardless of food intake and drink plenty of liquid. If it is necessary to reduce the dose, discontinue the drug, or replace it with an alternative agent, this should be done gradually over a period of 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/day. Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days the dose can be gradually increased to 900 mg per day according to the following scheme:
Day 1: 300 mg once a day
Day 2: 300 mg 2 times a day
Day 3: 300 mg 3 times a day
Partial seizures
Adults and children over 12 years old: 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 regimen described above (see 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 when taking the drug three times should not exceed 12 hours to avoid resumption of seizures.
Dose selection for renal failure.
For patients with renal failure, it is recommended to reduce the dose of gabapentin according to the table: * prescribe 300 mg every other day. Recommendations for patients undergoing hemodialysis.
For patients on hemodialysis who have not previously taken gabalentin, it is recommended to prescribe the drug in a saturating dose of 300-400 mg, and then use it at 200-300 mg every 4 hours of hemodialysis. Side effects:
Cardiovascular system: symptoms of vasodilation or increased blood pressure, palpitations.
Digestive tract: flatulence, anorexia, gingivitis, abdominal pain, constipation, dental diseases (including discoloration of tooth enamel), diarrhea, dyspepsia, increased appetite, dry mouth or pharynx, nausea, vomiting, pancreatitis, increased activity of liver transaminases, hepatitis, jaundice.
Blood system, lymphatic system: purpura (most often described as bruising resulting from physical trauma), leukopenia, thrombocytopenia.
Musculoskeletal system: arthralgia, back pain, increased bone fragility, myalgia.
Nervous system: dizziness; headache; hyperkinesis; muscular dyskinesia and leafing; choreoathetosis; weakened or absent tendon reflexes; dysarthria; ataxia; nystagmus; paresthesia; convulsions; confusion; increased fatigue; asthenia; amnesia; depression; thinking disorder; 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, erythema multiforme (including Stevens-Johnson syndrome).
Genitourinary system: urinary tract infection, impotence, urinary incontinence, acute renal failure.
Sense organs: visual impairment, amblyopia, diplopia, tinnitus, otitis media.
Others: fever, viral infection, weight gain, lability of plasma glucose levels in patients with diabetes mellitus, pain of various localizations, gynecomastia, breast enlargement, generalized edema. Overdose:
Symptoms: dizziness, diplopia, speech impairment, drowsiness, lethargy, diarrhea and increased severity of other side effects.
Treatment: gastric lavage, taking activated carbon, symptomatic therapy. Hemodialysis may be indicated for patients with severe renal failure. Interaction with other drugs:
Morphine: When gabapentin and morphine were coadministered, when morphine was taken 2 hours before gabapentin, there was a 44% increase in the mean area under the gabapentin concentration-time curve (AUC) compared with gabapentin alone, which was associated with an increase in the drug threshold. (cold pressor test). The clinical significance of this change has not been established; the pharmacokinetic characteristics of morphine did not change. The side effects of morphine when taken together with gabapentin did not differ from those when morphine was taken together with placebo.
No interactions were observed between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine. The pharmacokinetics of gabapentin at steady state are similar in healthy subjects and patients receiving other anticonvulsants. Concomitant 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 the bioavailability of gabapentin by approximately 20%. It is recommended to take gabapentin approximately 2 hours after taking the antacid. Probenecid does not affect the renal excretion of gabapentin.
The slight decrease in renal excretion of gabapentin with concomitant use of cimetidine is probably not clinically significant. Special instructions:
Although withdrawal syndrome with the development of seizures has not been observed during treatment with gabapentin, abrupt cessation of therapy with antiepileptic drugs in patients with partial seizures may provoke the development of seizures (see Dosage and Administration).
Gabapentin is not considered an effective treatment for absence epilepsy. In patients requiring concomitant therapy with morphine, the dose of gabapentin may need to be increased. In this case, it is necessary to carefully monitor 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 is added to other anticonvulsants, false-positive results have been reported with urinary protein testing using Ames N-Multistix SG® test strips. To determine protein in urine, it is recommended to use the more specific precipitation method of sulfosalicylic acid.
Patients should avoid driving a car, as well as performing work that requires rapid psychomotor reactions. Release form:
Capsules 300 mg. 10 or 15 capsules in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.
3, 5, 10 blister packs of 10 capsules each or 2, 4, 6 blister packs of 15 capsules each, together with instructions for use, are placed in a cardboard pack for consumer packaging. Storage conditions:
Store in a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children. Best before date:
2 years. Do not use after expiration date. Conditions for dispensing from pharmacies:
According to the recipe. Manufacturer/organization accepting consumer complaints:
CJSC "Canonpharma Production"
Address: 141100, Shchelkovo, Moscow region, st. Zarechnaya, 105.

Gabapentin is similar in structure to GABA, that is, together with it it can transmit pain impulses, but without affecting specific receptors. The drug acts on specific protein targets, reducing pain of neuropathic origin at the central and peripheral level, and also causing an anticonvulsant effect. The main active substance does not settle in the tissues of the body, but is excreted in full through the kidneys. This medicine is mainly used in the treatment of epileptic conditions in adults and adolescents, as well as for pain symptoms of a neuropathic nature.

1. Pharmacological action

Drug group:

Anticonvulsant drug.

Therapeutic effects of Gabapentin:

Anticonvulsant;
Anesthetic.

Peculiarities:

The drug is able to penetrate the blood-brain barrier.

Binding to plasma proteins: absent.

Excretion: kidneys.

2. indications for use

The drug is used for:

Treatment of various forms of epilepsy in adults and adolescents;
Elimination of neuropathic pain of various origins.

3. Method of application

Recommended dosage of Gabapentin for adults and adolescents:

300 mg per day with a gradual increase in dose by 300 mg daily until a value of 900-1800 (3600) mg per day is reached.

Recommended dosage of the drug for children 8-12 years old (based on weight calculations):

10-15 mg per kg of weight per day with a gradual increase in dose to 35-30 mg per kg of weight per day.

Recommended dosage of Gabapentin for children 8-12 years old (based on actual weight):

900 mg per day;

1200 mg per day;

Over 50 kg:

1800 mg per day.

Features of application:

The received dose of the drug is divided into 2-3 doses;
According to the instructions, discontinuation of the drug is possible only by gradually reducing its dosage over a week;
The interval of 12 hours between two consecutive doses of the drug should not be exceeded.

4. Side effects

Cardiovascular system:

Relaxation of the vascular wall, drop in blood pressure;

Urinary system:

Urinary incontinence;

Blood system:

Decrease in the number of leukocytes;

Nervous system:

Fatigue, dizziness, nystagmus, asthenia, paresthesia, drowsiness, nervous excitability, trembling of limbs, headaches, thinking disorders;

Respiratory system:

Sense organs:

Diplopia, ringing in the ears;

Hypersensitivity reactions:

Exanthema, Stevens-Johnson syndrome.

5. Contraindications

Pregnancy and lactation;
Hypersensitivity and individual intolerance to Gabapentin or its components;
Age under 8 years.

Use with caution:

Driving vehicles or operating complex machinery.

6. During pregnancy and lactation

Pregnant women and nursing mothers should take the drug contraindicated.

7. Interaction with other drugs

Simultaneous use of Gabapentin with:

Morphine:

Increased pain threshold;

Cimetidine:

Suppression of drug excretion;

Antacid or astringent drugs:

Reduced bioavailability of Gabapentin.

8. Overdose

Symptoms:

Nervous system: drowsiness, dizziness;
Sense organs: diplopia;
Other: dysarthria.

Specific antidote: no.

Treatment of Gabapentin overdose:

Symptomatic.

Hemodialysis: in severe cases.

9. Release form

Capsules in packaging, 100, 300 or 400 mg - 30, 45, 50 or 100 pcs.

10. Storage conditions

Dry, dark place out of reach of children.

Varies, depends on the manufacturer, indicated on the packaging.

11. Composition

1 capsule:

gabapentin - 100, 300 or 400 mg;
Excipients: calcium stearate, sodium carboxymethyl starch (type A), microcrystalline cellulose.

12. Conditions for dispensing from pharmacies

The drug is dispensed according to the prescription of the attending physician.

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* Instructions for medical use of the drug Gabapentin are published in free translation. THERE ARE CONTRAINDICATIONS. BEFORE USE, YOU MUST CONSULT WITH A SPECIALIST

Dosage form: capsules Composition:

Each capsule contains:

active substance- gabapentin 100 mg, 300 mg or 400 mg;

excipients: corn starch 24.0 mg/72.0 mg/96.0 mg, talc 10 mg/30 mg/40 mg;

capsule composition: red iron oxide dye (for a dosage of 400 mg) 0.1167%, yellow iron oxide dye (for dosages 300 mg and 400 mg) 0.1500%/0.6667%, titanium dioxide 2.1119%/0.7795%/ 1.4062%, sodium lauryl sulfate 0.08%/0.08%/008%/, gelatin up to 100%/up to 100%/up to 100%.

ink composition: shellac 24-27%, anhydrous alcohol 23-26%, isoprapanol 1-3%, butanol 1-3%, propylene glycol 3-7%, black iron oxide dye 24-28%, potassium hydroxide 0.05-0.1% , concentrated ammonia solution 1-2%, purified water 151-218%.

Description: Dosage 100 mg. Hard gelatin capsules No. 3, white capsule body, white capsule wing, white capsule wing, with inscriptions printed in black ink: on the capsule body - “02”; there is a “D” on the capsule cap. The contents of the capsule are white or almost white crystalline powder.

Dosage 300 mg. Hard gelatin capsules No. 1, yellow capsule body, yellow capsule cap, with inscriptions written in black ink: on the capsule body - “03”; there is a “D” on the capsule cap. The contents of the capsule are white or almost white crystalline powder.

Dosage 400 mg. Hard gelatin capsules No. 0, orange capsule body, orange capsule cap, with inscriptions printed in black ink: on the capsule body - “04”; there is a “D” on the capsule cap. The contents of the capsule are white or almost white crystalline powder.

Pharmacotherapeutic group:Antiepileptic drug ATX:

N.03.A.X.12 Gabapentin

Pharmacodynamics:It is similar in structure to the neurotransmitter gamma-aminobutyric acid (GABA), but its mechanism of action differs from other drugs that interact with GABA receptors, including valproic acid, barbiturates, benzodiazepines, GABA transaminase inhibitors, GABA uptake inhibitors, GABA agonists and prodrugs GABA: It does not have GABAergic properties and does not affect the uptake of GABA metabolism. It is assumed that it binds to the α 2 -δ- subunit of voltage-gated calcium channels and suppresses the current of calcium ions, which plays an important role in the occurrence of neuropathic pain.

Gabapentin does not affect the reuptake of doamine, norepinephrine and sertonin.

Gabapentin at clinically relevant concentrations does not bind to receptors for other common drugs or transmitters, including GABA A, GABA B, benzodiazepine, glutamate, glycine, or N-methyl-D-aspartate receptors.

Unlike phenytoin and carbamazepine, it does not interact with sodium channels in vitro. partially attenuates the effects of the glutamate receptor antagonist N-methyl-D-aspartate in some in vitro tests, but only at concentrations greater than 100 µmol/L, which are not achieved in vivo. slightly reduces the release of monoamine neurotransmitters in vitro. The use of gabapentin in rats led to an increase in GABA metabolism in some areas of the brain; this effect was similar to that of valproic acid, although it was observed in other areas of the brain. The significance of these effects of gabapentin for its anticonvulsant activity has not been established. In animals, it easily penetrates into the brain tissue and prevents convulsions caused by maximum electric shock, chemicals, including inhibitors of GABA synthesis, and also caused by genetic factors.

Pharmacokinetics:

All pharmacological effects of gabapentin are associated with the activity of the unchanged compound. It is practically not metabolized in the human body.

Bioavailability when taken orally

The bioavailability of gabapentin is not proportional to dose. Thus, as the dose increases, it decreases and amounts to 60, 47, 34, 33 and 27% when taking 900, 1200, 2400, 3600 and 4800 mg/day, divided into 3 doses, respectively. Food intake has little effect on the rate and extent of gabapentin absorption (there is an increase in the maximum plasma concentration (Cmax) and the area under the concentration-time curve (AUC) by 14%).

Distribution

Gabapentin practically does not bind to plasma proteins (<3%) и имеет объем распределения 57,7 л.

Removal

It is excreted unchanged from the systemic circulation by the kidneys. It is practically not metabolized in the human body. The half-life (T 1/2) from blood plasma does not depend on the dose and averages 5-7 hours. The elimination rate is constant, plasma and renal clearances are directly proportional to creatinine clearance. In the elderly and patients with impaired renal function, the plasma clearance of gabapentin is reduced. Removed from plasma by hemodialysis. In patients with impaired renal function or on hemodialysis, dose adjustment is recommended (see section "Dosage and Administration").

Special patient groups

Kidney failure Patients (n = 60) with renal failure (mean creatinine clearance 13-114 ml/min) took 400 mg gabapentin. The average T1/2 ranged from 6.5 hours (creatinine clearance >60 ml/min) to 52 hours (creatinine clearance<30 мл/мин), а почечный клиренс габапентина от 90 мл/мин (клиренс креатинина >60 ml/min) to 10 ml/min (creatinine clearance<30 мл/мин). Средний плазменный клиренс (С1/F) снижался с 190 мл/мин до 20 мл/мин. ц взрослых пациентов с почечной недостаточностью необходимо проводить коррекцию дозы (см. раздел "Способ применения и дозы"). Дети с почечной недостаточностью не исследовались.

Hemodialysis

Gabapentin is removed from blood plasma during hemodialysis. In anuric patients, hemodialysis has a significant effect on the elimination of gabapentin.

Liver failure

Since it is not metabolized in the liver, its use in patients with impaired liver function has not been studied.

Plasma clearance of gabapentin is reduced in the elderly and patients with impaired renal function.

Age

Gabapentin clearance decreases with increasing age. In patients under the age of 30 years, the clearance of gabapentin is 225 ml/min, and in patients over the age of 70 years, it is 125 ml/min. Renal clearance and clearance per unit body surface area of the subject also decrease with age. The decrease in renal clearance with age may be explained by a decrease in renal function.

Children

It has been established that plasma concentrations of gabapentin in children aged 1 month to 12 years are generally similar. Cmax was reached in 2-3 hours.

In children aged 1 month to 5 years, the AUC of gabapentin was 30% lower than in children aged 5 years and older. Clearance in terms of body weight is higher in children of the younger group. The apparent clearance of gabapentin is proportional to creatinine clearance. The average T1/2 is about 4.7 hours and is similar between the indicated age groups.

According to pharmacokinetic data, the effective daily dose in children with epilepsy aged 3-4 years is 40 mg/kg/day, with plasma concentrations similar to plasma concentrations in children 5 years of age and older when the latter take 30 mg/kg/day (see section " Method of administration and dosage").

Floor

Although the pharmacokinetics of gabapentin have not been compared in men and women, it is assumed that the pharmacokinetic parameters are not significantly different.

Race

Differences in the pharmacokinetics of gabapentin among representatives of different races have not been studied. Since it is predominantly excreted by the kidneys, and there are no differences in renal function in patients of different races, differences in pharmacokinetic parameters are not expected.

Indications:

Treatment of neuropathic pain in adults aged 18 years and older. Efficacy and safety in patients under 18 years of age have not been established.

Monotherapy for partial seizures with and without secondary generalization in adult children over 12 years of age. The effectiveness and safety of monotherapy in children under 12 years of age have not been established.

As an additional remedy in the treatment of partial seizures with and without secondary generalization in adults and children aged 3 years and older. The safety and effectiveness of adjunctive gabapentin therapy in children less than 3 years of age have not been established.

Contraindications:Hypersensitivity to gabapentin or auxiliary components of the drug.

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

With caution:Renal failure (see section "Method of administration and dosage"). Pregnancy and lactation:There are no data on the use of the drug in pregnant women, so it should be used during pregnancy only if the expected benefit to the mother justifies the possible risk to the fetus. is excreted in breast milk, its effect on a nursing baby is unknown, so breastfeeding should be discontinued during treatment. Directions for use and dosage:

Gabapentin is prescribed orally regardless of meals. If it is necessary to reduce the dose, discontinue the drug or replace it with an alternative drug, this should be done gradually over a period of 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/day. Treatment can begin immediately with a dose of 900 mg / day (300 mg 3 times a day) or during the first 3 days the dose can be gradually increased to 900 mg per day according to the following scheme:

Day 1: 300 mg 1 time per day;

Day 2: 300 mg 2 times a day;

Day 3: 300 mg 3 times a day.

Partial seizures

Adults and children over 12 years old: effective dose is from 900 to 2400 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 regimen described above (see section "Neuropathic pain in adults"). Subsequently, the dose can be increased to a maximum of 3600 mg/day (divided into 3 equal doses). The drug was well tolerated in doses up to 4800 mg/day. The maximum interval between doses when taking the drug three times should not exceed 12 hours to avoid 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 dose over 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 divided doses. The effective dose of gabapentin in children aged 3 to 5 years is 40 mg/kg/day in equal doses in 3 divided doses. The drug was well tolerated in doses up to 50 mg/kg/day with long-term use. The maximum interval between doses of the drug should not exceed 12 hours to avoid resumption of seizures.

There is no need to monitor the concentration of gabapentin in the blood plasma. It may be used in combination with other anticonvulsants without regard to changes in plasma concentrations or serum concentrations of other anticonvulsants.

Dose selection for renal failure

Creatinine clearance	Daily dose (mg/day) A

A The daily dose should be prescribed in three doses

B Prescribe 300 mg every other day

For patients on hemodialysis who have not previously taken the drug, it is recommended to prescribe the drug in a saturating dose of 300-400 mg, and then use it at 200-300 mg every 4 hours of hemodialysis.

Side effects:

In the treatment of neuropathic pain

Major adverse reactions that occurred during treatment in at least 1% of patients:

constipation, diarrhea, dry oral mucosa, dyspepsia, flatulence, nausea, vomiting, abdominal pain.

From the nervous system: gait disturbance, loss of coordination, amnesia, ataxia, confusion, dizziness, hypoesthesia, drowsiness, thinking, tremor, headache.

shortness of breath, pharyngitis.

From the skin: skin rash.

From the senses: amblyopia, vertigo, conjunctivitis, otitis media.

Others: accidental injuries, asthenia, back pain, flu-like syndrome, infections, pain of various localizations, peripheral edema, weight gain, hyperglycemia.

In the treatment of partial seizures

The safety of gabapentin as an adjunctive agent has been studied in more than 200 patients; its tolerability was satisfactory. Most often it is used in combination with other anticonvulsants, so it is impossible to determine which drug causes the adverse reaction (if there is such a connection at all). Major adverse reactions that occurred during treatment in at least 1% of patients:

From the cardiovascular system: symptoms of vasodilation or hypertension.

From the digestive system: constipation, dental disease, diarrhea, dyspepsia, increased appetite, dry mucous membrane of the mouth or pharynx, nausea and/or vomiting, abdominal pain, flatulence, anorexia, gingivitis.

From the hematopoietic organs: leukopenia, decreased concentration of white blood cells, purpura (most often described as bruising resulting from physical trauma).

From the musculoskeletal system: fractures, myalgia, arthralgia.

From the nervous system: amnesia, ataxia, confusion, incoordination, depression, dysarthria, emotional lability, insomnia, nervousness, nystagmus, drowsiness, impaired thinking, tremor, muscle twitching, dizziness, hyperkinesis, increased, weakened or absent reflexes, paresthesia, restlessness, hostility, headache pain. From the respiratory system: cough, pharyngitis, rhinitis, pneumonia, bronchial respiratory tract infections.

From the skin: abrasions, acne, itchy skin, skin rash.

From the senses: amblyopia, diplopia, visual impairment, vertigo. From the genitourinary system: urinary tract infection, impotence. Others: back pain, fatigue, fever, viral infection, peripheral edema, weight gain, asthenia, general malaise, facial swelling, erectile dysfunction.

These adverse reactions were mild or moderate. Adverse reactions observed in older patients were no different from those in younger patients. No new or unexpected adverse reactions were observed during monotherapy.

When comparing the tolerability of the drug at doses of 300 and 360 mg/day, there is a dose dependence of such phenomena as dizziness, ataxia, drowsiness, paresthesia and nystagmus.

Children

Listed below are side effects observed with adjunctive therapy in children 3-12 years of age with an incidence of approximately 2% or higher than with placebo.

From the digestive system: nausea and/or vomiting.

From the nervous system: drowsiness, hostility, emotional lability, dizziness, hyperkinesia.

From the respiratory system: bronchitis, respiratory infection.

Others: viral infection, fever, weight gain, fatigue. Other adverse events observed in more than 2% of children, the incidence of which was similar or higher than the placebo group: pharyngitis, upper respiratory tract infections, headache, rhinitis, cramps, diarrhea, anorexia, cough and otitis media.

Discontinuation of treatment due to adverse events

Adverse reactions that most often led to discontinuation of the drug used as adjuvant therapy: drowsiness, ataxia, dizziness, fatigue, nausea and (or) vomiting; as monotherapy: dizziness, nervousness, weight gain, nausea and/or vomiting and drowsiness.

Adverse events that most often led to drug discontinuation in children: drowsiness, hyperkinesia and hostility.

Post-registration experience of use

There have been cases of sudden unexplained death, the connection of which with gabanentine treatment has not been established. Other adverse events recorded during post-marketing use of the drug included acute renal failure, allergic reactions including urticaria, alopecia, angioedema, generalized edema; fluctuations in blood glucose concentrations in diabetic patients, chest pain, enlargement of the mammary glands, drug rash, including zosinophilia and systemic reactions; gynecomastia, increased liver function tests, hepatitis, jaundice, erythema multiforme, including Stevens-Johnson syndrome, hallucinations, hypersensitivity, including systemic reactions, movement disorders such as choreoathetosis, dyskinesia and dystopia, myoclonus, palpitations, pancreatitis, thrombocytopenia, noise in the ears, urinary incontinence.

Cancellation of therapy

After abrupt discontinuation of gabapentin therapy, the following adverse reactions were most often observed: anxiety, insomnia, nausea, pain of various localizations and increased sweating.

Overdose:

With a single dose of 49 g of gabapentin, the following symptoms were observed: dizziness, double vision, speech impairment, drowsiness, lethargy and mild diarrhea, which completely disappeared with symptomatic therapy.

Hemodialysis may be indicated for patients with severe renal failure.

Interaction:

When 600 mg of gabapentin was administered 2 hours after administration of morphine 60 mg extended-release capsules, there was a 44% increase in the mean area under the gabapentin concentration-time curve (AUC) compared with gabapentin monotherapy, which was associated with an increase in pain threshold (cold pressor test). The clinical significance of this change has not been established; the pharmacokinetic characteristics of morphine did not change. Adverse reactions of morphine when administered concomitantly with gabapentin were no different from those when morphine was taken concomitantly with placebo. The extent to which these drugs interact at other doses is unknown. No interactions were observed between gabapentin and phenobarbital, phenytoin, valproic acid and carbamazepine. The pharmacokinetics of gabapentin at steady state are similar in healthy subjects and patients receiving other anticonvulsants. The simultaneous use of gabapentin with oral contraceptives containing and (or) is 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% (see section "Special instructions").

Probenecid does not affect the renal excretion of gabapentin.

The small decrease (14%) in renal excretion of gabapentin with concomitant use of cimetidine is probably not clinically significant.

With simultaneous use of naproxen (250 mg) and gabapentin (125 mg), an increase in gabapentin absorption from 12% to 15% was observed. does not affect the pharmacokinetic parameters of naproxen. The indicated doses of drugs are less than the minimum therapeutic ones. The simultaneous use of these drugs in large doses has not been studied.

With the simultaneous use of gabapentin and hydrocodone, a dose-dependent decrease in Cmax and AUC of hydrocodone is observed compared with hydrocodone monotherapy.

Special instructions:

Antiepileptic drugs, including, may increase the risk of suicidal thoughts or behavior. Therefore, patients receiving these drugs should be closely monitored for new or worsening depression, the emergence of suicidal thoughts or behavior, and any changes in behavior.

If acute pancreatitis develops while taking gabapentin, the possibility of discontinuing the drug should be assessed.

Although withdrawal syndrome accompanied by the development of seizures has not been observed during treatment with gabapentin, abrupt cessation of anticonvulsant therapy in patients with epilepsy can provoke the development of status epilepticus (see section "Dosage and Administration"). is not considered as an effective treatment for absence epilepsy.

When used simultaneously with morphine, an increase in the concentration of gabapentin in the blood plasma may be observed. In this regard, the patient needs to be carefully monitored for the development of signs of central nervous system (CNS) depression, such as drowsiness. The dose of gabapentin or morphine should be adequately reduced (see section "Interactions with other drugs").

Severe, life-threatening hypersensitivity reactions, such as drug rash with associated eosinophilia and systemic symptoms, have been reported while taking antiepileptic drugs, including gabapentin. It must be remembered that early signs of a hypersensitivity reaction, such as fever, lymphadenopathy, can develop even in the absence of a skin rash. If such symptoms occur, immediate examination of the patient is necessary. If no other reason is found other than the use of gabapentin, the use of the drug should be discontinued.

It is recommended to take gabapentin approximately 2 hours after taking the antacid. The effect of long-term therapy (more than 36 weeks) with gabapentin on the learning ability, intelligence and development of the child has not been sufficiently studied. The ratio of possible risks and benefits should be assessed when prescribing long-term therapy.

As with other antiepileptic drugs, gabapentin may cause an increase in the frequency of seizures or the appearance of a different type of seizure.

When gabapentin was used concomitantly with other anticonvulsants, false-positive results were reported when determining protein in urine using Ames N-Multistix SG® test strips. To determine protein in urine, use the more specific method of precipitation with sulfosalicylic acid.

Impact on the ability to drive vehicles. Wed and fur.:While taking the drug, patients are not recommended to drive a car or use potentially dangerous equipment until it is confirmed that the drug does not have a negative effect on the performance of these functions. Release form/dosage:Capsules 100, 300, 400 mg. Package: 10 capsules per blister A1/A1.

3 or 10 blisters along with instructions for use are placed in a cardboard box.

Storage conditions:In a dry place, protected from light, at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Best before date: 2 years.

Do not use after expiration date.

Conditions for dispensing from pharmacies: By prescription Registration number: LP-002191 Registration date: 21.08.2013 Expiration date: 21.08.2018 Owner of the Registration Certificate:Aurobindo Pharma Ltd. India Manufacturer: Representative office: Aurobindo Pharma, JSC Information update date: 11.03.2017 Illustrated instructions

The drug is actively used as an analgesic and anticonvulsant. It was originally developed to effectively treat epilepsy and is now used in neuropathic therapy to relieve pain and restless leg syndrome. Gabapentin tablets are indicated for diabetic neuropathy, central neuropathic pain and postherpetic neuralgia. Taking the pills helps improve the patient’s overall well-being, helps normalize the functioning of the nervous system, and actively combat the symptoms of pathologies.

Composition of Gabapentin

The drug is available in the form of hard capsules filled with white or yellowish powder. The main active ingredient of the drug is gabapentin, the content of which is 300 mg in one capsule. The substance has an anticonvulsant effect and helps relieve neuropathic pain. Other components that make up the medicine:

Pharmacodynamics and pharmacokinetics

The anticonvulsant is structurally similar to gamma-aminobutyric acid, but is not a GABA mimetic, since it is not bound by GABA receptors. It does not interact with glutamate, benzodiazepine, opiate and strychnine-insensitive receptors. When it enters the body, the active ingredient of the drug combines with the α2-σ subunit, which leads to a decrease in the flow of calcium ions.

Gabapentin is a drug that has a direct effect on highly specific centers of the central nervous system that do not have an affinity for many other anti-epileptic drugs. It blocks the entry of calcium into the cell, thereby preventing the occurrence of neuropathological pain and effectively relieving it. Under the influence of the drug, the synthesis of GABA significantly increases and glutamate-dependent neuronal death decreases.

The maximum concentration of Gabapentin in the body is achieved after taking the capsule only after 120–180 minutes. The bioavailability of the drug is disproportionate to the dose and decreases as it increases. Food does not affect the pharmacokinetics of the drug. It is excreted from the body by the kidneys after 6–7 hours. The active components of the drug do not bind to blood proteins. A decrease in the excretion of Gabapentin is observed in elderly patients and with kidney pathologies, so dose adjustment is required for this group of people.

Indications for use

Gabapentin tablets can be prescribed for monotherapy and adjunctive treatment. They relieve pain, make you feel better, and help normalize the functioning of the nervous system.. Gabapentin is no less effective for osteochondrosis. The drug has not only analgesic, but also anti-inflammatory and relaxing effects. Pathological conditions for which the drug Gabapentin is prescribed are the following:

neuralgic manifestations that occur after herpes zoster;
epileptic syndromes accompanied by seizures;
symptomatic focal epilepsy, accompanied by partial seizures and convulsions;
resistant epilepsy;
migraines;
neuropathic pain in diabetic, HIV-related, postherpetic, alcoholic neuralgia, spinal canal stenosis;
menopause (prescribed to women for whom estrogens are contraindicated).

Directions for use and dosage

Gabapentin Vidal should be used carefully and strictly following the instructions of your doctor. Drinking capsules without first consulting a specialist is not recommended, since the medicine has many contraindications and side effects that can only aggravate the situation and worsen the patient’s condition. Instructions for using Gabapentin before taking capsules are required to be studied.

The medicine is taken orally. The daily dose depends on the patient’s age, the pathology that worries him, and the presence of concomitant diseases. The dosage and method of administration of the drug are as follows:

For epilepsy:

adults, children over 12 years of age: 1 capsule of 300 mg 3 times a day;
maximum daily dose – 3600 mg, effective – from 900 to 3600 mg;
the intervals between each dose of the drug are no more than 12 hours;
It is possible to select the dose on an individual basis (the first day of treatment - 1 capsule of 300 mg, the second - 2 capsules of 300 mg in 2 doses, the third - 3 capsules of 300 mg in 3 doses);
children from 3 to 12 years: 25–35 mg/kg 3 times a day.

For neuralgia:

adults, children: 1 capsule of 300 mg 3 times a day;
then the dose is increased to 3600 mg;
exceeding a dose of 3600 mg is prohibited.

Special instructions

For patients treated with Gabapentin, experts recommend following these simple rules:

If you need to stop taking the drug, you cannot do this right away. The dose of medication taken should be reduced gradually over 1 to 2 weeks, otherwise a sudden cessation of treatment may cause epistatus (a condition in which epileptic seizures follow one after another, and in the intervals between them the patient does not regain consciousness).
During the period of bearing a baby, tablets should be used only in cases of extreme necessity, according to the testimony of the attending physician, when the benefits to the mother outweigh the existing risks to the fetus.
If, during treatment with the drug, patients experience ataxia, dizziness, drowsiness, or a sharp increase in body weight (excitability in children), taking the tablets should be gradually stopped.
During treatment with Gabapentin, it is advisable to refrain from driving.

Drug interactions

It is allowed to take oral contraceptives and other antiepileptic drugs simultaneously with the medicine: Carbamazepine, Phenobarbital, Phenytoin. These drugs do not affect the pharmacokinetics of the tablets. It is better to minimize the intake of antacids and sorbents, as they reduce the bioavailability of Gabapentin. If antacids and sorbents are indispensable during treatment, then they and the main drug should be taken with a time difference of 2 to 3 hours.

Myelotoxic drugs, like antacids, are used with the drug carefully, as they increase its hematotoxicity. If you take the drug together with morphine, the pharmacokinetics of morphine does not change, but you need to strictly monitor adverse reactions that may occur in the nervous system. Alcohol while taking Gabapentin increases adverse reactions, so drinking alcohol during treatment is not recommended.

Side effects of Gabapentin

The instructions indicate that when using the drug, patients may experience the following pathological conditions:

tachycardia, high blood pressure;
nausea, dyspepsia, dry mouth, abdominal pain;
anorexia, constipation or diarrhea, flatulence;
pancreatitis, gingivitis;
back pain, myalgia;
dizziness, drowsiness, nystagmus;
excitability, increased fatigue;
headache, depression;
dysarthria, confusion;
anxiety, insomnia, hyperkinesia;
cough, pharyngitis, rhinitis;
ringing in the ears, blurred vision;
impaired potency, urinary incontinence;
weight gain, edema;
exudative erythema, skin rash.

Overdose

Exceeding the daily dose of the drug is indicated by the following symptoms:

speech disorders;
drowsiness;
dizziness;
double vision;
lethargy;
bowel disorder.

Treatment for overdose is symptomatic. In other words, doctors provide care based on the symptoms that are presenting. The following events are expected to take place:

gastric lavage;
hemodialysis;
reception of sorbents.

Contraindications

Gabapentin capsules are prescribed for pancreatitis and other pathologies of the gastrointestinal tract in the acute stage, if the patient has allergic reactions to the components of the drug. Other contraindications.

Gabapentin is a potent drug that is available strictly with a prescription. The main active ingredient, gabapentin, has a direct effect on highly specific centers of the central nervous system, stopping seizures and blocking neuropathic pain.

But sometimes the patient has to pay for such relief with depression and even obsessive suicidal thoughts. So what is more – benefit or harm?

How does Gabapentin work?

The structure of the gabapentin molecule resembles gamma-aminobutyric acid (GABA), which is the main inhibitory neurotransmitter of the human central nervous system. Moreover, gabapentin was originally synthesized precisely to imitate the chemical structure of GABA. However, it turned out that, despite the structural similarities, gabapentin and GABA drugs act differently.

Unlike GAM acid, gabapentin does not directly affect brain receptors. It interacts with calcium channels in cortical neurons and prevents calcium from entering the cell, thereby relieving neuropathic pain. On the other hand, under the influence of the drug, glutamate-dependent neuronal death decreases, and GABA synthesis, on the contrary, increases.

Indications

The main indications for treatment with Gabapentin are epilepsy and neuropathic pain, but not everything is as simple as it might seem at first glance.

Gabapentin is only really effective in treating focal (partial) seizures, which are localized to one part of the brain.

For generalized attacks (those that cover the entire brain, cause complete loss of consciousness and massive muscle spasms), the drug is not used.

It turns out that the indications for the use of Gabapentin for epilepsy are limited:

Treatment of focal seizures in children over 12 years of age;
Adjunctive therapy for focal seizures in adults;
Additional therapy for resistant (particularly severe, uncontrollable) forms of epilepsy in children over 3 years of age.

In other words, you can fight focal seizures in children with Gabapentin alone.

In the treatment of adults, this drug is used only as an additional measure as part of complex therapy.

Another reason to start taking Gabapentin is neuropathic pain. That is, those that arise not as a result of a reaction to any physical damage, but on their own, for no apparent reason. This occurs due to the voluntary excitation of neurons responsible for pain sensations. Such pain can torment diabetics, HIV patients, alcoholics, as well as those whose medical history includes spinal stenosis or herpes zoster.

However, only patients over 18 years of age can take Gabapentin to relieve neuropathic pain.

Gynecologists are also aware of the mechanism of action of Gabapentin. Some of them prescribe the drug to patients who are seriously experiencing menopause. Especially those who, for one reason or another, cannot be treated with estrogens. It has been noted that Gabapentin can significantly reduce the intensity of hot flashes, calm you down and put you to sleep.

Instructions for use

The drug is sold in tablets and capsules, each of which contains 300 mg of the active substance. You can take them regardless of meals, with a small amount of water. The tablet does not begin to act immediately; the maximum effect is achieved only after 2-3 hours.

The dosage and schedule for taking the drug should be determined by a doctor. Often the dosage regimen for epilepsy looks like this:

Adults and children over 12 years of age are prescribed 300 mg of gabapentin 3 times a day.
The dose can be increased gradually, for example: 1 day – 300 mg, 2 days – 600 mg, 3 days – 900 mg, that is, 3 tablets 3 times a day.
When treating children from 3 to 12 years of age, the daily dose is calculated individually, based on the body weight of the small patient - 25/35 mg of gabapentin per kilogram of weight. For example, if a child weighs 20 kg, then he needs about 600 mg of active substance per day. This amount should be divided into 3 doses.

To get rid of pain due to neuropathy, a very large dose of the drug is often required - 3600 mg per day. Increase the number of tablets in stages, starting with 300 mg at a time.

Gabapentin does not bind to blood proteins and is excreted by the kidneys 6-7 hours after administration. In older people and those who suffer from renal failure, the elimination of the drug is delayed, so they should be especially careful in selecting doses to avoid overdose.

You need to stop taking the medicine, just like starting it, gradually. If you abruptly stop using Gabapentin, as well as any other anticonvulsant drug, the risk of convulsive status (when the intervals between seizures are reduced so much that the patient does not even have time to regain consciousness) will significantly increase.

When changing treatment tactics and prescribing another drug instead of Gabapentin, the doctor must warn the patient that he should not switch from one tablet to another at a time

It is necessary to reduce the daily dose of gabapentin for 7 days and only after that begin a course of treatment with another active substance.

Possible adverse reactions

Gabapentin is a potent drug that affects not only the central nervous system, but also the entire body as a whole. Exceeding the maximum daily dose (3600 mg) is fraught with dizziness, drowsiness, and diarrhea. The patient may complain that he often sees double vision. He becomes tired, apathetic and even risks falling into lethargy, when all mental reactions slow down to a critical level.

The fact that you cannot independently experiment with doses of Gabapentin is convincingly demonstrated by the fact of the trial that took place in 2009 in the USA.

The drug's manufacturer is facing trial over a link between the drug and a sharp increase in suicide rates among patients found by the Federal Food and Drug Administration.

It has been proven that taking the medication significantly increases the tendency to depression and suicidal thoughts. Now these properties of the drug are listed among the possible side effects set out in the official instructions for Gabapentin.

In addition, the drug may cause:

Increased blood pressure, tachycardia;
Nausea, various digestive system disorders (constipation, diarrhea, flatulence);
Back pain;
Confusion, increased excitability and anxiety;
Urinary incontinence, problems with potency;
Runny nose, cough, pharyngitis;
Tinnitus;
Rash, itching, acne;
Swelling of the face;
General increase in body weight (less commonly, provoke anorexia).

In the course of numerous experiments on rats, it was found that Gabapentin is also capable of causing pancreatic cell cancer. That is why the drug is strictly contraindicated in patients with pancreatitis.

After taking the drug, you should not drive.

Gabapentin can affect consciousness and sharply reduce concentration. Driving a car in a state where the processes of the central nervous system are so inhibited is dangerous. However, just like performing any responsible work that requires maximum mental concentration.

Gabapentin and alcohol should not be combined.

Both ethyl alcohol and gabapentin have a direct effect on the central nervous system. Therefore, they are capable of enhancing each other’s side effects and putting the patient into severe conditions in which he will be completely disoriented in space and will not be able to coordinate his movements.

Another side effect from the combined use of alcohol and Gabapentin tablets is impaired consciousness, even stunning.

If symptoms of overdose appear, you should immediately consult a doctor.

As soon as the patient notices that he begins to see double, his stool is disrupted, he cannot form and express his thoughts normally, he needs to immediately seek help. These are the first symptoms of an overdose of the active substance, which can be eliminated by gastric lavage and taking sorbents. Severe renal failure, which is one of the likely side effects of the drug, will require hemodialysis.