Pregabalin
Indications
Pregabalin is indicated for:
- Management of neuropathic pain associated with diabetic peripheral neuropathy
- Management of post-herpetic neuralgia
- Adjunctive therapy for adult patients with partial onset seizures
- Management of fibromyalgia
- Neuropathic pain associated with spinal cord injury.
Pharmacology
Pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-amino butyric acid (GABA). It does not bind directly to GABAA, GABAB, or benzodiazepine receptor. Pregabalin binds with high affinity to the alpha-2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Oral bioavailability of Pregabalin is ≥90% and is independent of dose. It is eliminated from the systemic circulation primarily by renal excretion as unchanged drug with a mean elimination half-life of 6.3 hours in subjects with normal renal function.
Dosage And Administration
Neuropathic pain associated with diabetic peripheral neuropathy: The maximum recommended dose of Pregabalin is 100 mg three times a day (300 mg/day) in patients with creatinine clearance of at least 60 mL/min. Dosing should begin at 50 mg three times a day (150 mg/day) and may be increased to 300 mg/day within 1 week based on efficacy and tolerability.
Post-herpetic neuralgia: The recommended dose of Pregabalin is 75 to 150 mg two times a day, or 50 to 100 mg three times a day (150 to 300 mg/day) in patients with creatinine clearance of at least 60 mL/min. Dosing should begin at 75 mg two times a day, or 50 mg three times a day (150 mg/day) and may be increased to 300 mg/day within 1 week based on efficacy and tolerability.
Adjunctive therapy for adult patients with partial onset seizures: In general, it is recommended that patients be started on a total daily dose no greater than 150 mg/day (75 mg two times a day, or 50 mg three times a day). Based on individual patient response and tolerability, the dose may be increased to a maximum dose of 600 mg/day.
Management of Fibromyalgia: The recommended dose of Pregabalin for fibromyalgia is 300 to 450 mg/day. Dosing should begin at 75 mg two times a day (150 mg/day) and may be increased to 150 mg two times a day (300 mg/day) within 1 week based on efficacy and tolerability.
Neuropathic pain associated with spinal cord injury: The recommended dose range is 150 to 600 mg/day. The recommended starting dose is 75 mg two times a day (150 mg/day). The dose may be increased to 150 mg two times a day (300 mg/day) within 1 week based on efficacy and tolerability.
Pregabalin capsules can be taken without regards to meals.
Interaction
There are no significant interactions between Pregabalin with other antiepileptic drugs & oral contraceptive. Pregabalin may potentiate the effects of ethanol and lorazepam.
Contraindications
Pregabalin is contraindicated in patients with known hypersensitivity to Pregabalin or any of its components.
Side Effects
The most common side effects include dizziness, somnolence, dry mouth, edema, blurred vision, weight gain and abnormal thinking.
Pregnancy And Lactation
Pregnancy category of Pregabalin is C. So it should only used if potential benefit justifies the potential risks to the fetus.
Pregabalin may be secreted through the breast milk like other drugs, so it should be used in nursing women only if the benefits clearly overweigh the risk.
Precautions And Warnings
Discontinuation of Pregabalin without tapering may produce insomnia, nausea, headache and diarrhea. So it should be tapered gradually over a minimum of 1 week rather than discontinued abruptly. Creatinine kinase may be elevated if treated with Pregabalin. It should be discontinued rapidly if myopathy is diagnosed or suspected or if creatinine kinase is elevated markedly.
Therapeutic Class
Adjunct anti-epileptic drugs.
Use in special populations
The safety and efficacy of Pregabalin in paediatric patients have not been established.
Storage Conditions
Keep in a cool & dry place (below 30° C), protected from light & moisture. Keep out of the reach of children.
