Oskela
Get started

Drug Reference

pregabalin

Gabapentinoid· Brands: Lyrica, AlzainPO

Mechanism of action
Pregabalin binds to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing calcium influx and thereby decreasing the release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P. This modulation of neurotransmitter release underlies its anticonvulsant, analgesic, and anxiolytic effects.
Pharmacokinetics
Pregabalin is well absorbed orally with a bioavailability of about 90%, and peak plasma concentrations occur within 1 hour. It does not bind to plasma proteins and is excreted unchanged in the urine. The elimination half-life is approximately 6 hours, and it is removed by haemodialysis. Dose adjustment is required in renal impairment.
Indications & dosing

Neuropathic pain (e.g., diabetic peripheral neuropathy, postherpetic neuralgia)

Titrate gradually; reduce dose in renal impairment. Abrupt discontinuation may cause withdrawal symptoms.

  • adult · PO: 75–300 mg twice daily · Titrate gradually; reduce dose in renal impairment. Abrupt discontinuation may cause withdrawal symptoms.

Fibromyalgiaoff-label

Licensed in some regions (e.g., US); off-label in others. Titrate gradually; reduce dose in renal impairment. Abrupt discontinuation may cause withdrawal symptoms.

  • adult · PO: 75–225 mg twice daily · Licensed in some regions (e.g., US); off-label in others. Titrate gradually; reduce dose in renal impairment. Abrupt discontinuation may cause withdrawal symptoms.

Epilepsy (adjunctive therapy for partial-onset seizures)

Adjunctive therapy for partial-onset seizures. May be given two or three times daily. Titrate gradually; reduce dose in renal impairment.

  • adult · PO: 75–300 mg twice daily · Adjunctive therapy for partial-onset seizures. May be given two or three times daily. Titrate gradually; reduce dose in renal impairment.

Generalized anxiety disorderoff-label

Licensed in some regions (e.g., Europe); off-label in others. Titrate gradually; reduce dose in renal impairment. Abrupt discontinuation may cause withdrawal symptoms.

  • adult · PO: 75–300 mg twice daily · Licensed in some regions (e.g., Europe); off-label in others. Titrate gradually; reduce dose in renal impairment. Abrupt discontinuation may cause withdrawal symptoms.
Contraindications & precautions
  • Hypersensitivity to pregabalin or any excipient · Can cause angioedema or other allergic reactions.
  • Pregnancy · Animal studies show harm; avoid unless benefit clearly outweighs risk.
  • Breastfeeding · Excreted in breast milk; consider alternatives or monitor infant.
  • Abrupt discontinuation may cause withdrawal symptoms; taper gradually over at least 1 week.
  • Use with caution in patients with renal impairment; adjust dose based on creatinine clearance.
  • May cause dizziness and somnolence; advise caution when driving or operating machinery.
  • Concomitant use with opioids or CNS depressants increases risk of respiratory depression; monitor closely.
  • Monitor for signs of angioedema or hypersensitivity; discontinue therapy immediately if they occur.
  • Advise patients and carers to seek medical advice if mood changes or suicidal thoughts occur.
Adverse effects
  • Dizziness
  • Somnolence
  • Peripheral oedema
  • Weight gain
  • Dry mouth
  • Blurred vision
  • Ataxia
  • Angioedemaserious
  • Respiratory depressionserious
  • Suicidal ideationserious
Renal & hepatic adjustment
  • eGFR 60+: Usual dose, 150–300 mg/day in 2–3 divided doses.
  • eGFR 30–60: 75–150 mg/day in 2–3 divided doses.
  • eGFR 15–30: 25–75 mg/day in 1–2 divided doses.
  • eGFR 0–15: 25 mg once daily; for haemodialysis, give 25 mg after each dialysis session.
Monitoring, pregnancy & toxicity
  • Dizziness and somnolence · At each visit and during dose titration
  • Visual disturbance · At each visit
  • Peripheral oedema and weight gain · At each visit
  • Renal function · Baseline and periodically, especially in renal impairment
  • Mood and behaviour changes (including suicidal ideation) · At each visit
  • Pregnancy: Not recommended unless clearly necessary. Animal studies have shown teratogenicity; there is limited human data. Women of childbearing potential should use effective contraception while taking pregabalin.
  • Toxicity: CNS depression, including somnolence, confusion, and coma · Supportive care; monitor respiratory and cardiac function; consider activated charcoal if recent ingestion, and haemodialysis in severe cases (pregabalin is dialysable).
  • Toxicity: Seizures · Standard management of seizures; consider benzodiazepines.
  • Toxicity: Respiratory depression · Supportive care, including oxygen and ventilation if needed.
  • Toxicity: Cardiac conduction abnormalities · ECG monitoring and supportive care.
Clinical notes
Pregabalin is used for neuropathic pain, fibromyalgia, partial-onset seizures, and generalised anxiety disorder. It should be tapered off gradually to avoid withdrawal symptoms such as insomnia, headache, and anxiety. Dizziness and somnolence are common dose-related adverse effects. Caution is needed in patients with renal impairment, and it is not recommended in pregnancy unless clearly necessary. The misuse potential should be considered; it is a controlled drug in some regions.

Log in to read the full pregabalin monograph

A free account unlocks the complete drug reference, the interaction checker, prescription practice and every other learning tool.

Log inCreate a free account

BNF; local formulary