Class: Analgesic, Anticonvulsant. C-V
Dosage Forms. Capsule: 25 mg, 50 mg, 75 mg, 100 mg, 150 mg, 200 mg, 225 mg, 300 mg; Solution: 20 mg/mL
Common FDA Label Indication, Dosing, and Titration.
1. Diabetic peripheral neuropathy: 50-100 mg po tid
2. Fibromyalgia: 75-150 mg po bid; max 225 mg bid
3. Partial seizure, adjunct: 25-75 mg po bid; may titrate to max 600 mg/d in 2-3 divided doses
4. Postherpetic neuralgia: Initial, 75 mg po bid; may titrate to 300 mg/d; maintenance 75-150 mg bid or 50-100 mg tid may titrate to max 600 mg/d
1. Generalized anxiety disorder: 150-600 mg/d in 3 divided doses
MOA. Pregabalin is a GABA analog that strongly binds to the α 2-delta site (a subunit of voltage-gated calcium channels) in central nervous system tissues. Binding to the α2-delta subunit may be involved in pregabalin’s effects on neuropathic pain and seizure control. Pregabalin reduces the calcium-dependent release of several neurotransmitters; however, the exact mechanism of action is unknown.
Drug Characteristics: Pregabalin
Medication Safety Issues: Pregabalin
Drug Interactions: Pregabalin
Adverse Reactions: Pregabalin
Efficacy Monitoring Parameters. Reduction in seizure frequency, improvement in pain, reduced symptoms of fibromyalgia.
Toxicity Monitoring Parameters. Creatine kinase, emergence or worsening of depression, suicidal behavior or ideation, or unusual changes in behavior, symptoms of angioedema, during initial and chronic therapy.
Key Patient Counseling Points. Solution must be used within 45 d of first opening the bottle. Avoid activities requiring mental alertness or coordination until drug effects are realized. Avoid sudden discontinuation of drug, as adverse effects are enhanced including increased seizure frequency. Avoid drinking alcohol.
Clinical Pearls. Safety and efficacy have not been established in children. Data suggest an increased risk of suicidal behavior or ideation may exist in patients receiving therapy with antiepileptic drugs (AEDs). Dose of solution should be written in mg and pharmacist should calculate volume of dose.