Pregabalin is a structural analogue of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). It is a potent, centrally-acting analgesic and anticonvulsant used primarily for neuropathic pain, fibromyalgia, and as an adjunctive therapy for partial-onset seizures. It binds to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing the release of several excitatory neurotransmitters.
Adult: Neuropathic Pain/Fibromyalgia: Start at 75 mg twice daily (150 mg/day). May increase to 150 mg twice daily (300 mg/day) within 1 week based on efficacy and tolerability. Max 300 mg/day for PHN/DPN. Fibromyalgia: Max 225 mg twice daily (450 mg/day). Partial Seizures: Start at 75 mg twice daily (150 mg/day). Max 600 mg/day in 2-3 divided doses.
Note: Can be taken with or without food. Swallow the capsule whole with water. Do not crush, chew, or break. 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. For discontinuation, taper gradually over a minimum of 1 week to avoid withdrawal symptoms.
Pregabalin binds with high affinity to the alpha2-delta (α2-δ) subunit of presynaptic voltage-gated calcium channels in the central nervous system. This binding is thought to modulate channel function, reducing the influx of calcium into nerve terminals.
Pregnancy: Pregnancy Category C (US FDA). Limited human data. Animal studies showed developmental toxicity. Use only if potential benefit justifies potential risk to the fetus. Indian guidelines recommend avoidance unless absolutely necessary. Pregabalin is present in breast milk; avoid during pregnancy and lactation unless essential.
Driving: WARNING: May cause dizziness, somnolence, blurred vision, and reduced alertness. Patients should not drive, operate complex machinery, or engage in hazardous activities until they know how the medication affects them.
| CNS Depressants (e.g., Alcohol, Benzodiazepines, Opioids) | Additive CNS depression (sedation, dizziness, respiratory depression). | Major |
| Thiazolidinediones (e.g., Pioglitazone, Rosiglitazone) | May potentiate pregabalin-induced peripheral edema and weight gain. | Moderate |
| Angiotensin-Converting Enzyme (ACE) Inhibitors | May increase risk and severity of angioedema. | Moderate |
| Oral Contraceptives (Ethinyl Estradiol/Levonorgestrel) | No clinically significant pharmacokinetic interaction. | Minor |