TaperCommunitypregabalin
Boxed Warning
Respiratory depression risk when used with CNS depressants, particularly opioids. Increased risk of suicidal thoughts and behavior (anticonvulsant class warning).
Pregabalin is a gabapentinoid approved for neuropathic pain (diabetic peripheral neuropathy, postherpetic neuralgia), fibromyalgia, partial-onset seizures (adjunctive), and spinal cord injury neuropathic pain. It is a Schedule V controlled substance due to abuse potential.
25mg, 50mg, 75mg, 150mg, 300mg
Capsules: 25mg, 50mg, 75mg, 100mg, 150mg, 200mg, 225mg, 300mg; Oral solution: 20mg/mL; Extended-release tablets (Lyrica CR): 82.5mg, 165mg, 330mg
Category C (risk cannot be ruled out)
Binds potently to the alpha-2-delta subunit of voltage-gated calcium channels, reducing excitatory neurotransmitter release. Similar mechanism to gabapentin but with 6-fold higher binding affinity. Does not bind GABA receptors.
Linear absorption unlike gabapentin. Short half-life requires slow taper. Capsules can be opened for precise dosing.
Linear pharmacokinetics but short half-life. Gradual reduction essential. Capsule contents can be weighed for precise reductions.
Toxicity
Dizziness and somnolence most common. Respiratory depression with CNS depressants/opioids. Physical dependence with chronic use. Euphoria/misuse potential (Schedule V). Suicidal ideation (anticonvulsant class warning). Angioedema rarely reported.
Pharmacokinetics
Rapidly absorbed with linear, dose-proportional pharmacokinetics (unlike gabapentin). Bioavailability ≥90%. Tmax ~1.5 hours. Food decreases Cmax by ~25% and delays Tmax but does not reduce total absorption.
~0.5 L/kg
Negligible metabolism in humans (<2% of dose). No CYP involvement. N-methylated metabolite is the only identified metabolite.
Renal (~90% excreted unchanged). Clearance proportional to creatinine clearance.
Not significantly bound to plasma proteins
~67–80 mL/min (renal clearance)
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