Gabagamma^® (Capsules) Instructions for Use

Marketing Authorization Holder

Woerwag Pharma GmbH & Co. KG (Germany)

Manufactured By

Dragenopharm Apotheker Pueschl, GmbH (Germany)

Packaging and Quality Control Release

MEDIS INTERNATIONAL, a.s. (Czech Republic)

ATC Code

N03AX12 (Gabapentin)

Active Substance

Gabapentin (Rec.INN registered by WHO)

Dosage Forms

	Gabagamma®	Capsules 300 mg: 20, 50, or 100 pcs.
		Capsules 400 mg: 20, 50, or 100 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size No. 1, yellow, opaque; capsule contents – white powder.

Excipients: lactose, corn starch, talc, gelatin, titanium dioxide, iron oxide yellow.

10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (5) – cardboard packs.
10 pcs. – blisters (10) – cardboard packs.

Capsules hard gelatin, size No. 0, orange, opaque; capsule contents – white powder.

Excipients: lactose, corn starch, talc, gelatin, titanium dioxide, iron oxide yellow, iron oxide red.

10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (5) – cardboard packs.
10 pcs. – blisters (10) – cardboard packs.

Clinical-Pharmacological Group

Antiepileptic drug

Pharmacotherapeutic Group

Antiepileptic agent

Pharmacological Action

Antiepileptic agent. 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 significant 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%. Concurrent 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 eliminated only by the kidneys. T_1/2 is dose-independent and averages 5-7 hours.

The clearance of gabapentin decreases in elderly individuals 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 concentration values of gabapentin 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 with 300 mg once daily on Day 1. Increase to 300 mg twice daily on Day 2. Increase to 300 mg three times daily on Day 3. Titrate further as needed for pain relief up to a maximum daily dose of 3600 mg administered in three divided doses.

For epilepsy monotherapy in patients over 12 years: Initiate with 300 mg three times daily. Titrate upwards to an effective dose; the recommended maintenance dose is 900 mg to 1200 mg three times daily.

For adjunctive epilepsy therapy in patients aged 3 years and older: Initiate with 10-15 mg/kg/day in three divided doses. Titrate to the effective dose over three days. The maintenance dose for patients aged 3-12 years is 25-35 mg/kg/day in three divided doses. For patients over 12 years, the maintenance dose is 900 mg to 1200 mg three times daily.

Adjust the dosage in patients with renal impairment based on creatinine clearance (CrCl). For CrCl 30-59 mL/min: maximum 400 mg twice daily. For CrCl 15-29 mL/min: maximum 300 mg twice daily. For CrCl <15 mL/min: maximum 300 mg once daily. For patients on hemodialysis: administer a loading dose of 300-400 mg, then a maintenance dose of 200-300 mg after each 4-hour hemodialysis session.

Administer doses three times daily. Do not exceed 12 hours between doses in a t.i.d. schedule.

When discontinuing therapy or switching to another anticonvulsant, 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 impairment, tremor, convulsions, amblyopia, diplopia, hyperkinesia, increased, decreased or absent reflexes, paresthesia, anxiety, hostility, gait disturbance.

Digestive system disorders tooth discoloration, diarrhea, increased appetite, dry mouth, nausea, vomiting, flatulence, anorexia, gingivitis, abdominal pain, pancreatitis, changes in 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

Adequate and strictly controlled studies on the safety of gabapentin use during pregnancy and lactation in humans have not been conducted. If use during pregnancy and lactation is necessary, the expected therapeutic benefit for the mother and the potential risk to the fetus or infant should be carefully weighed.

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 dosage 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 gabapentin therapy 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 dosage 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 gabapentin therapy 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 noted that some gabapentin preparations contain the following dyes as excipients: sunset yellow (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.