Overview
Pregabalin is a gabapentinoid anticonvulsant and analgesic agent used for neuropathic pain conditions, fibromyalgia, and as adjunctive therapy for partial-onset seizures. It binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing neurotransmitter release. The drug requires careful dose titration and monitoring due to risks of CNS depression, edema, and potential for misuse.
Mechanism of Action
Pregabalin binds with high affinity to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing calcium influx at nerve terminals. This decreases the release of several neurotransmitters including glutamate, norepinephrine, and substance P, resulting in analgesic, anticonvulsant, and anxiolytic effects.
Indications
- Management of neuropathic pain associated with diabetic peripheral neuropathy
- Management of postherpetic neuralgia
- Adjunctive therapy for partial-onset seizures in patients 1 month and older
- Management of fibromyalgia
- Management of neuropathic pain associated with spinal cord injury
Common Doses
- 25 mg
- 50 mg
- 75 mg
- 100 mg
- 150 mg
- 200 mg
- 225 mg
- 300 mg
Dosage
Dosing varies by indication, typically starting at 75-150 mg/day in divided doses and titrated based on efficacy and tolerability to maximum 600 mg/day. For neuropathic pain: start 150 mg/day, may increase to 300 mg/day within 1 week, maximum 600 mg/day. For fibromyalgia: start 150 mg/day, increase to 300 mg/day within 1 week, may increase to 450 mg/day. Renal impairment requires dose adjustment.
Contraindications
- Known hypersensitivity to pregabalin or any of its components
Side Effects
- Dizziness
- Somnolence
- Peripheral edema
- Weight gain
- Dry mouth
- Blurred vision
- Balance difficulties
- Fatigue
- Euphoria
- Confusion
- Angioedema
- Hypersensitivity reactions
- Suicidal thoughts or behavior
- Respiratory depression
Interactions
- Additive CNS depression with opioids, benzodiazepines, alcohol, and other CNS depressants
- No significant pharmacokinetic interactions with most antiepileptic drugs including carbamazepine, valproic acid, lamotrigine, phenytoin, phenobarbital, and topiramate
Counseling Points
- Take exactly as prescribed; do not stop abruptly
- May cause dizziness, drowsiness, blurred vision - avoid driving until effects known
- Report swelling, weight gain, mood changes, or suicidal thoughts
- Avoid alcohol and other CNS depressants
- Rise slowly to prevent dizziness
- Notify provider if pregnant or planning pregnancy