Egipentin (Tablets, Capsules) Instructions for Use

ATC Code

N03AX12 (Gabapentin)

Active Substance

Gabapentin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Anticonvulsant drug

Pharmacotherapeutic Group

Anticonvulsant agent

Pharmacological Action

Antiepileptic drug. In its chemical structure, it is similar to GABA, which functions as an inhibitory neurotransmitter in the CNS. It is believed that the mechanism of action of gabapentin differs from other anticonvulsants acting through GABA synapses (including valproate, barbiturates, benzodiazepines, GABA-transaminase inhibitors, GABA uptake inhibitors, GABA agonists, and GABA prodrugs).

In vitro studies have shown that Gabapentin is characterized by the presence of a new peptide binding site in rat brain tissues, including the hippocampus and cerebral cortex, which may be related to the anticonvulsant activity of gabapentin and its derivatives.

Gabapentin at clinically relevant concentrations does not bind to other common drugs and neurotransmitter receptors in the brain, including GABA_A-, GABA_B-, benzodiazepine receptors, and NMDA receptors.

The mechanism of action of gabapentin has not been definitively established.

Pharmacokinetics

Gabapentin is absorbed from the gastrointestinal tract. After oral administration, the C_max of gabapentin in plasma is reached in 2-3 hours. The absolute bioavailability is about 60%.

Concomitant administration with food (including high-fat food) does not affect the pharmacokinetics of gabapentin.

Gabapentin does not bind to plasma proteins and has a V_d of 57.7 L. In patients with epilepsy, the concentration of gabapentin in the cerebrospinal fluid is 20% of the corresponding C_ss in plasma at the end of the dosing interval.

Gabapentin is excreted solely by the kidneys. The T_1/2 is dose-independent and averages 5-7 hours.

The clearance of gabapentin is reduced in the elderly and in patients with impaired renal function. The elimination rate constant, plasma and renal clearance of gabapentin are directly proportional to creatinine clearance.

Gabapentin is removed from plasma by hemodialysis.

Plasma gabapentin concentrations in children were similar to those in adults.

Indications

Treatment of neuropathic pain in adults over 18 years of age; monotherapy of partial seizures with or without secondary generalization in adults and children over 12 years of age; as an adjunctive therapy in the treatment of partial seizures with or without secondary generalization in adults and children aged 3 years and older.

ICD codes

Dosage Regimen

Determine the dosage individually based on indication, renal function, and patient response.

For neuropathic pain in adults, initiate at 900 mg/day, divided into three 300 mg doses on day one. Increase to 1800 mg/day on day two, divided into three doses. The maximum maintenance dose is 3600 mg/day, administered in three divided doses.

For adjunctive therapy of partial seizures in patients over 12 years, initiate at 900 mg/day in three divided doses. Titrate upwards to a maximum of 3600 mg/day based on clinical response and tolerability.

For adjunctive therapy in children aged 3 to 12 years, initiate at 10-15 mg/kg/day in three divided doses. Titrate to a maintenance dose of 25-35 mg/kg/day over three days. The maximum dose is 50 mg/kg/day, administered in three divided doses.

For monotherapy of partial seizures in patients over 12 years, initiate at 900 mg/day in three divided doses. Titrate to a maximum of 3600 mg/day.

Adjust the dose in patients with renal impairment. For creatinine clearance (CLcr) 60-89 mL/min, use 800-2400 mg/day. For CLcr 30-59 mL/min, use 400-1400 mg/day. For CLcr 15-29 mL/min, use 200-700 mg/day. For CLcr less than 15 mL/min, use 100-300 mg/day.

Administer a supplemental dose of 125-350 mg following each 4-hour hemodialysis session, based on the maintenance dose.

Administer the final dose at bedtime.

Take tablets and capsules with a full glass of water, with or without food.

When discontinuing therapy, reduce the dose gradually over a minimum of one week to minimize the risk of increased seizure frequency.

Adverse Reactions

Nervous system disorders amnesia, ataxia, confusion, impaired coordination, depression, dizziness, dysarthria, increased nervous excitability, nystagmus, drowsiness, thinking impaired, tremor, convulsions, amblyopia, diplopia, hyperkinesia, increased, decreased or absent reflexes, paresthesia, anxiety, hostility, abnormal gait.

Digestive system disorders tooth discoloration, diarrhea, increased appetite, dry mouth, nausea, vomiting, flatulence, anorexia, gingivitis, abdominal pain, pancreatitis, abnormal liver function tests.

Hematopoietic system disorders leukopenia, decreased white blood cell count, thrombocytopenic purpura.

Respiratory system disorders rhinitis, pharyngitis, cough, pneumonia.

Musculoskeletal system disorders myalgia, arthralgia, bone fractures.

Cardiovascular system disorders arterial hypertension, manifestations of vasodilation.

Urinary system disorders urinary tract infections, urinary incontinence.

Allergic reactions erythema multiforme, Stevens-Johnson syndrome.

Dermatological reactions skin maceration, acne, pruritus, rash.

Other back pain, fatigue, peripheral edema, impotence, asthenia, malaise, facial edema, weight gain, accidental injury, asthenia, flu-like syndrome, fluctuations in blood glucose levels, in children – viral infection, otitis media.

Contraindications

Hypersensitivity to gabapentin.

Use in Pregnancy and Lactation

There are no adequate and well-controlled studies on the safety of gabapentin use during pregnancy and lactation in humans. If use during pregnancy and lactation is necessary, the expected therapeutic benefit for the mother should be carefully weighed against the potential risk to the fetus or infant.

Gabapentin is excreted in breast milk. The nature of the effect of gabapentin on the breastfed infant has not been established.

Use in Renal Impairment

Patients with impaired renal function, as well as patients on hemodialysis, require dose regimen adjustment.

Pediatric Use

The efficacy and safety of neuropathic pain therapy in patients under 18 years of age have not been established.

The efficacy and safety of gabapentin monotherapy for the treatment of partial seizures in children under 12 years of age and adjunctive therapy with gabapentin for the treatment of partial seizures in children under 3 years of age have not been established.

Geriatric Use

Elderly patients may require adjustment of the gabapentin dosage regimen due to a possible decrease in renal clearance in this category of patients.

Special Precautions

Abrupt discontinuation of anticonvulsant therapy in patients with partial seizures may provoke status epilepticus. If it is necessary to reduce the dose, discontinue Gabapentin or replace it with an alternative agent, this should be done gradually over a minimum of 1 week.

Gabapentin is not an effective treatment for absence seizures.

When used concomitantly with other anticonvulsants, false-positive results of the urine protein test have been reported. The more specific sulfosalicylic acid precipitation method is recommended for determining urine protein.

Patients with impaired renal function, as well as patients on hemodialysis, require dose regimen adjustment.

Elderly patients may require adjustment of the gabapentin dosage regimen due to a possible decrease in renal clearance in this category of patients.

The efficacy and safety of neuropathic pain therapy in patients under 18 years of age have not been established.

The efficacy and safety of gabapentin monotherapy for the treatment of partial seizures in children under 12 years of age and adjunctive therapy with gabapentin for the treatment of partial seizures in children under 3 years of age have not been established.

If symptoms of an allergic reaction or skin reactions that occur during the use of gabapentin are not treated, more serious disorders may develop.

Avoid alcohol consumption during treatment.

It should be borne in mind that some gabapentin preparations contain dyes as excipients: sunset yellow FCF (E110), which may cause allergic reactions; erythrosine (E127), which should not be used in thyroid diseases.

Effect on ability to drive vehicles and operate machinery

Until the individual response to treatment is determined, the patient should refrain from potentially hazardous activities requiring concentration and increased speed of psychomotor reactions.

Drug Interactions

Concomitant use with antacids reduces the absorption of gabapentin from the gastrointestinal tract.

Concomitant use with felbamate may increase the T_1/2 of felbamate.

A case of increased plasma concentration of phenytoin has been described with concomitant use.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.