Pregabalin is indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy & management of post herpetic neuralgia. It is also indicated for the adjunctive therapy for adult patients with partial onset seizures. It can be used for the management of fibromyalgia & Neuropathic pain associated with spinal cord injury.
GABA Analogue; Anticonvulsant
Pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). It does not bind directly to GABAA, GABAB or benzodiazepine receptors. Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Although the mechanism of action of Pregabalin has not been fully elucidated, results in animal studies suggest that binding to the alpha2-delta subunit may be involved in Pregabalin's anti-nociceptive and antiseizure effects.
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) & may be increased to 300 mg/day within 1 week based on efficacy & 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) & may be increased to 300 mg/day within 1 week based on efficacy & tolerability. Adjunctive therapy for adult patients with partial onset seizures: Pregabalin at doses of 150 to 600 mg/day has been shown to be Effective as adjunctive therapy in the treatment of partial onset seizures in adults. The total daily dose should be divided & given either two or three times daily. 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 & 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) & may be increased to 150 mg two times a day (300 mg/day) within 1 week based on efficacy & tolerability. Patients who do not experience sufficient benefit with 300 mg/day may be further increased to 225 mg two times a day (450 mg/day). 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 & tolerability. Patients who do not experience sufficient pain relief after treatment with 300 mg/day & who tolerate Pregabalin may be treated with up to 300 mg two times a day.
Pregabalin is unlikely to be involved in significant pharmacokinetic drug interactions.
Pregabalin is contraindicated in patients with known hypersensitivity to Pregabalin or any of its components. Discontinuation of Pregabalin without tapering may produce insomnia, nausea, headache & 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.
The most common side Effects include dizziness, somnolence, dry mouth, edema, blurred vision, weight gain, & abnormal thinking.
Pregnancy: Pregnancy category C. Nursing mother: It is not known if pregabalin is excreted in human milk; it is, however, present in the milk of rats. So it should be used in nursing mother only if there is a clear benefit over the risk.
In case of overdose with pregabalin, sign and symptoms are reduced consciousness, depression/anxiety, confusional state, agitation and restlessness. Seizures and heart block have also been reported. There is no specific antidote. If indicated, elimination of unabsorbed drug may be attempted by emesis or gastric lavage; usual precautions should be observed to maintain the airway. General supportive care of the patient is indicated including monitoring of vital signs and observation of the clinical status of the patient.
Keep in a cool & dry place (below 30°C), protected from light & moisture. Keep out of the reach of children.
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