Neurontin® (Tablets, Capsules) Instructions for Use
ATC Code
N03AX12 (Gabapentin)
Active Substance
Gabapentin (Rec.INN registered by WHO)
Clinical-Pharmacological Group
Anticonvulsant 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 novel 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 GABAA, GABAB, 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 Cmax 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 Vd of 57.7 L. In patients with epilepsy, the concentration of gabapentin in the cerebrospinal fluid is 20% of the corresponding Css in plasma at the end of the dosing interval.
Gabapentin is eliminated solely by the kidneys. The T1/2 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 clearance, 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 aged 18 years and older; 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
| ICD-10 code | Indication |
| G40 | Epilepsy |
| G62.9 | Polyneuropathy, unspecified |
| R52.2 | Other chronic pain |
| ICD-11 code | Indication |
| 8A6Z | Epilepsy or epileptic seizures, unspecified |
| 8C4Z | Disorders of nerve roots, plexuses or peripheral nerves, unspecified |
| MG30.Z | Chronic pain syndrome, unspecified |
Dosage Regimen
| The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen. |
Determine the dosage individually based on indication and patient response.
For neuropathic pain in adults, initiate at 900 mg/day in three divided doses (300 mg three times daily). Titrate upwards as needed to a maximum of 3600 mg/day.
For adjunctive therapy for partial seizures in adults and adolescents over 12 years, initiate at 900 mg/day in three divided doses. The effective dose is 900-3600 mg/day.
For adjunctive therapy for partial seizures in children aged 3-12 years, initiate at 10-15 mg/kg/day in three divided doses. Titrate to an effective dose over approximately 3 days; the recommended total daily dose for patients aged 3-4 years is 40 mg/kg/day, and for patients 5-12 years, it is 25-35 mg/kg/day, both in three divided doses.
For monotherapy of partial seizures in adults and adolescents over 12 years, the recommended dose is 900-3600 mg/day in three divided doses.
Adjust the dosing interval in renal impairment based on creatinine clearance (CrCl). For CrCl >60 mL/min, administer 1200 mg three times daily. For CrCl 30-60 mL/min, administer 600 mg twice daily. For CrCl 15-30 mL/min, administer 300 mg once daily. For CrCl <15 mL/min, administer 300 mg every other day.
Administer a supplemental dose following hemodialysis. The supplemental dose is based on the maintenance dose: after a 4-hour hemodialysis session, administer 200-300 mg.
For geriatric patients, adjust dose based on renal function.
When discontinuing therapy, taper gradually over a minimum of one week.
If a dose is missed, take it as soon as remembered unless it is almost time for the next dose. Do not double the dose to make up for a missed one.
Adverse Reactions
Nervous system disorders: amnesia, ataxia, confusion, impaired coordination, depression, dizziness, dysarthria, nervous excitability, nystagmus, somnolence, 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 effect of gabapentin on the breastfed infant is not established.
Use in Renal Impairment
Patients with impaired renal function, as well as patients on hemodialysis, require dose 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 of 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 for urinary protein tests have been reported. It is recommended to use the more specific sulfosalicylic acid precipitation method to determine urinary protein.
Patients with impaired renal function, as well as patients on hemodialysis, require dose 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 of 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 T1/2 of felbamate.
A case of increased plasma phenytoin concentration 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.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Film-coated tablets, 600 mg: 20, 50, or 100 pcs.
Film-coated tablets, 800 mg: 20, 50, or 100 pcs.
Marketing Authorization Holder
Viatris Specialty, LLC (USA)
Manufactured By
Pfizer Pharmaceuticals, LLC (Puerto Rico)
Packaging and Quality Control Release
PFIZER MANUFACTURING DEUTSCHLAND, GmbH (Germany)
Dosage Forms
 |
Neurontin® | Film-coated tablets, 600 mg: 20, 50, or 100 pcs. |
| Film-coated tablets, 800 mg: 20, 50, or 100 pcs. |
Dosage Form, Packaging, and Composition
Film-coated tablets white, elliptical in shape, engraved with “NT” and “16”, with a score between the engravings on one side and a score on the other side.
| 1 tab. | |
| Gabapentin | 600 mg |
Excipients: poloxamer 407 – 80 mg, copovidone – 64.8 mg, corn starch – 49.2 mg, magnesium stearate – 6 mg; film coating: Opadry white YS-1-18111 – 24 mg, candelilla wax – 0.6 mg.
10 pcs. – blisters (2) – cardboard packs×.
10 pcs. – blisters (5) – cardboard packs×.
10 pcs. – blisters (10) – cardboard packs×.
× cardboard packs with or without first-opening control.
Film-coated tablets white, biconvex, elliptical in shape, engraved with “NT” and “26”, with a score between the engravings on one side and a score on the other side.
| 1 tab. | |
| Gabapentin | 800 mg |
Excipients: poloxamer 407 – 106.7 mg, copovidone – 86.4 mg, corn starch – 65.6 mg, magnesium stearate – 8 mg; film coating: Opadry white YS-1-18111 – 32 mg, candelilla wax – 0.8 mg.
10 pcs. – blisters (2) – cardboard packs×.
10 pcs. – blisters (5) – cardboard packs×.
10 pcs. – blisters (10) – cardboard packs×.
× cardboard packs with or without first-opening control.
Capsules 100 mg: 20, 50, or 100 pcs.
Capsules 300 mg: 20, 50 or 100 pcs.
Capsules 400 mg: 20, 50 or 100 pcs.
Marketing Authorization Holder
Viatris Specialty, LLC (USA)
Manufactured By
Pfizer Pharmaceuticals, LLC (Puerto Rico)
Packaging and Quality Control Release
PFIZER MANUFACTURING DEUTSCHLAND, GmbH (Germany)
Dosage Forms
|
Neurontin® | Capsules 100 mg: 20, 50, or 100 pcs. |
| 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 #3, opaque, with a white cap and body, printed with blue ink – on the cap “Neurontin®” and “100 mg”, on the body – “PD” in a circle; inscription color – blue; capsule contents – white or almost white powder.
| 1 caps. | |
| Gabapentin | 100 mg |
Excipients: lactose monohydrate – 14.25 mg, corn starch – 10 mg, talc – 10 mg; capsule shell: gelatin – 39.6 mg, water – 6.96 mg, titanium dioxide – 1.44 mg, sodium lauryl sulfate – less than 0.1 mg; ink: shellac – 0.075 mg, titanium dioxide – 0.027 mg, indigo carmine – 0.021 mg.
10 pcs. – blisters (2) – cardboard packs×.
10 pcs. – blisters (5) – cardboard packs×.
10 pcs. – blisters (10) – cardboard packs×.
× cardboard packs with or without first-opening control.
Capsules hard gelatin, size #1, opaque, with a light yellow cap and body, printed with blue ink – on the cap “Neurontin®” and “300 mg”, on the body – “PD” in a circle; inscription color – gray-blue; capsule contents – white or almost white powder.
| 1 caps. | |
| Gabapentin | 300 mg |
Excipients: lactose monohydrate – 42.75 mg, corn starch – 30 mg, talc – 30 mg; capsule shell: gelatin – 64.07 mg, water – 11.02 mg, titanium dioxide – 0.76 mg, iron oxide yellow – 0.15 mg, sodium lauryl sulfate – less than 0.15 mg; ink: shellac – 0.075 mg, titanium dioxide – 0.027 mg, indigo carmine – 0.021 mg.
10 pcs. – blisters (2) – cardboard packs×.
10 pcs. – blisters (5) – cardboard packs×.
10 pcs. – blisters (10) – cardboard packs×.
× cardboard packs with or without first-opening control.
Capsules hard gelatin, size #0, opaque, with a cream-orange cap and body, printed with blue ink – on the cap “Neurontin®” and “400 mg”, on the body – “PD” in a circle; inscription color – gray-blue; capsule contents – white or almost white powder.
| 1 caps. | |
| Gabapentin | 400 mg |
Excipients: lactose monohydrate – 57 mg, corn starch – 40 mg, talc – 40 mg; capsule shell: gelatin – 80.01 mg, water – 13.92 mg, titanium dioxide – 1.28 mg, iron oxide yellow – 0.62 mg, iron oxide red – 0.06 mg, sodium lauryl sulfate – less than 0.19 mg; ink: shellac – 0.075 mg, titanium dioxide – 0.027 mg, indigo carmine – 0.021 mg.
10 pcs. – blisters (2) – cardboard packs×.
10 pcs. – blisters (5) – cardboard packs×.
10 pcs. – blisters (10) – cardboard packs×.
× cardboard packs with or without first-opening control.
![Neurontin® [Tablets, Capsules] 1](https://www.medixlife.com/wp-content/uploads/Medixlife_favi_512.png "Neurontin® [Tablets, Capsules] 2")