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pregabalin LYRICA

Class: Gabapentinoid/​α2δ Ligand
FDA Indications: Postherpetic Neuralgia, Neuropathic Pain Associated With Diabetic Peripheral Neuropathy, Adjunctive Therapy For Adult Patients With Partial Onset Seizures , Fibromyalgia, Neuropathic Pain Associated With Spinal Cord Injury
Off-Label Use: GAD, Panic Disorder, Social Anxiety, Alcohol Dependence, Restless Leg Syndrome
Prescribing
Forms: 25, 50, 75, 100, 150, 200, 225, 300mg capsule
Dose Range: 150-600 mg/day
Starting: 75mg-300mg. Max: 600mg/d. May ↑ to 300 mg/d within 1 wk as tolerated. Start on a total daily dose no greater than 150 mg/d (75 mg b.i.d, or 50 mg t.i.d)
Stopping: ↑'d seizure frequency may occur in patients with seizure disorders if rapidly d/c'd ∴ taper gradually over a minimum of 1 week.

NAMI drug fact sheet

Precautions
Serious Side Effects: Angioedema and hypersensitivity reactions have occurred in patients receiving pregabalin
Side Effects: dizziness (30%), sedation/somnolence (22%), xerostomia, edema, visual changes, weight gain, difficulty concentrating
Pharmacodynamics
1° MOA: Binds to the α2δ subunit of presynaptic N and P/Q VGCCs, block the release of excitatory neurotransmitters such as glutamate when neurotransmission is excessive
Pharmacokinetics
t½: 6 (5-6.5)° TMAX: 1.5°
Substrate of: Renally cleared
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
  • - no pharmacokinetic DDIs; though pharmacodynamically, caution with co-prescribed CNS depressants
Misc
  • - a GABA analog with similarities in structure and effects to gabapentin 3-10 times more potent as an AED than is gabapentin
  • - it is the pharmacologically active S-enantiomer of 3-isobutyl GABA though no direct GABA-mimetic activity
  • - one of the few agents that ↑'s slow-wave δ sleep, which may be helpful in chronic neuropathic pain syndromes
  • - inform men who plan to father a child of the potential risk of male mediated teratogenicity
Special Populations

Category C—No reports describing the use in human pregnancy have been located. The animal reproduction data suggest moderate risk, but the absence of human pregnancy experience prevents an assessment of the embryo-fetal risk

RID 7%; No Human Data—Potential Toxicity


Clearance tends to ↓ with increasing age, c/w age-related ↓'s in CrCl ∴ ↓'d dose may be required in patients who have age-related compromised renal fcn

CrCl ≥60 mL/min: 300-1,200mg/d (divided BID or TID) CrCl >30-60 mL/min: 75-300mg/d (divided BID or TID) CrCl ≥15-30 mL/min: 25-150mg/d (given QD or divided BID) CrCl <15mL/min: 25-75mg/d QD (single dose)

No dose adjustment required in liver impairment

References
Package Insert
Drugs In Pregnancy And Lactation 11th Ed
Stahl's Essential Psychopharmacology 4th Ed
Foye's Principles Of Medicinal Chemistry

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Last updated August 14 2025 21:35:12. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.