Drug reference

Pregabalin

Antiepileptic

Also known as Lyrica, Pregabaline, PREGABALIN

START

75 mg BID (most indications); 50 mg TID (DPN/PHN); 7 mg/kg/day BID (pediatrics 1mo-4yr)

TYPICAL MAX

300 mg/day (neuropathic pain); 450 mg/day (fibromyalgia); 600 mg/day (GAD, epilepsy)

STOP IF

Angioedema (any facial/oral swelling), suicidal ideation, severe respiratory depression, DRESS syndrome (rash with eosinophilia/fever), rhabdomyolysis

WATCH

Renal function (dose MUST be adjusted for CrCl <60), peripheral edema/weight gain, mental status (suicidal ideation screen at baseline and periodically), respiratory rate (if on opioids or with COPD), signs of misuse/abuse

CDSCO approvedSchedule HJan AushadhiATC N03AX16

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · 1 h (Cmax); clinical effect days to weeks
PEAK: 1h · ~1 h (oral Cmax)
t½: 6.3h · 6.3 h (normal); ~52 h (CrCl <15)
DURATION: 12h · 8-12 h (BID-TID dosing)

EXCRETION

~90% renal unchanged · negligible hepatic metabolism (<2%)

route + CYP

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Risk cannot be ruled out. Animal studies have shown adverse effects on fetal development (skeletal malformations, decreased fetal weight). Use only if potential benefit justifies potential risk. Pregabalin is associated with an increased risk of major congenital malformations when used in the first trimester. Women of childbearing potential should use effective contraception.

FDA category + note

Top interactionssee all 12 →

AlcoholSevereDatabaseKimi deep-research + Cla
AlfentanilSevereDatabaseDDInter
BenzhydrocodoneSevereDatabaseDDInter
BuprenorphineSevereDatabaseDDInter

Available in India

307 branded formulations and 2,216 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Pregabalin binds with high affinity to the alpha-2-delta (α2-δ) auxiliary subunit of voltage-gated calcium channels (VGCC) on presynaptic neurons in the CNS and PNS. This binding reduces calcium influx into nerve terminals, thereby decreasing the release of several excitatory neurotransmitters including glutamate, norepinephrine, and substance P. The reduction in excitatory neurotransmission produces anticonvulsant, anxiolytic, and analgesic (neuropathic pain) effects. Pregabalin does not directly bind to GABA-A or GABA-B receptors, nor does it affect GABA uptake or degradation.

Indications

Neuropathic pain associated with diabetic peripheral neuropathy (DPN)Neuropathic pain associated with spinal cord injuryPostherpetic neuralgia (PHN)Adjunctive therapy for partial-onset seizures in adultsAdjunctive therapy for partial-onset seizures in pediatric patients 1 month of age and olderFibromyalgia in adultsGeneralized anxiety disorder (GAD) in adults

Dosing

Adult: Neuropathic pain (DPN/PHN): Initial 50 mg TID (150 mg/day); may increase to 100 mg TID (300 mg/day) within 1 week based on efficacy and tolerability. Max 300 mg/day. Spinal cord injury neuropathic pain: Initial 75 mg BID; may increase to 150 mg BID within 1 week. Max 300 mg/day. Fibromyalgia: Initial 75 mg BID (150 mg/day); may increase to 150 mg BID (300 mg/day) within 1 week, then to 225 mg BID (450 mg/day) if needed. GAD: Initial 75 mg BID (150 mg/day); may increase to 150 mg BID (300 mg/day) within 1 week, then to 225 mg BID (450 mg/day) or 300 mg BID (600 mg/day) if needed. Epilepsy: Initial 75 mg BID (150 mg/day); may increase to 150 mg BID (300 mg/day) based on response. Max 600 mg/day.
Pediatric: Partial-onset seizures (1 month to <4 years): Initial 7 mg/kg/day in 2 divided doses; may increase to 14 mg/kg/day in 2 divided doses. Partial-onset seizures (4-16 years): Initial 2.5 mg/kg BID (5 mg/kg/day); may increase to 5 mg/kg BID (10 mg/kg/day), then to 10 mg/kg BID (20 mg/kg/day) if needed. Max 10 mg/kg BID (600 mg/day whichever is less). Weight-based dosing uses a provided dosing chart.
Renal adjustment: CrCl ≥60 mL/min: No adjustment (max 600 mg/day). CrCl 30-59 mL/min: Max 300 mg/day (give BID or TID). CrCl 15-29 mL/min: Max 150 mg/day (give once daily or BID). CrCl <15 mL/min: Max 75 mg/day (single daily dose). Hemodialysis: Give supplemental dose of 25-100 mg after each 4-hour dialysis session (depending on indication and residual renal function).
Hepatic adjustment: No dosage adjustment is required for patients with hepatic impairment. Pregabalin undergoes negligible hepatic metabolism (<2%).
Geriatric: Dose adjustment may be needed due to age-related decrease in renal function. Start at the lower end of the dosing range (e.g., 25 mg BID or 25 mg TID) and titrate cautiously. Monitor renal function at baseline and periodically.
Max dose: 600 mg/day (neuropathic pain max 300 mg/day; fibromyalgia max 450 mg/day; GAD max 600 mg/day; epilepsy max 600 mg/day)

Pharmacokinetics

Onset

Analgesic and anxiolytic effects may be observed within days of starting therapy; full therapeutic effect may take 1-2 weeks.

Peak effect

Approximately 1 hour post-dose (Cmax for immediate-release formulation).

Duration

Approximately 8-12 hours (supports BID or TID dosing).

Half-life

Approximately 6.3 hours in healthy adults (range 4.6-6.7 hours); prolonged in renal impairment (up to ~52 hours in patients with CrCl <15 mL/min).

Bioavailability

≥90% (oral); dose-independent and not affected by food.

Protein binding

Negligible (<1%); pregabalin is essentially unbound in plasma.

Metabolism

Negligible hepatic metabolism in humans. Less than 2% of a dose is metabolized, primarily to N-methylated derivative. Not metabolized by CYP450 enzymes. No clinically significant drug-drug interactions via metabolic pathways.

Excretion

Primarily renal: approximately 90% excreted unchanged in urine via glomerular filtration. Negligible fecal excretion. Renal clearance is directly proportional to creatinine clearance.

Contraindications

Hypersensitivity to pregabalin or any component of the formulation
Angioedema (has been reported with pregabalin; discontinue immediately if facial, perioral, or upper airway swelling occurs)

Side effects

Common

Dizziness (most common; ~20-30%)Somnolence/drowsiness (~15-20%)Peripheral edema (~5-10%)Weight gain (~5-10%; dose-dependent)Dry mouth (~5%)Blurred vision (~5%)Constipation (~4%)Difficulty concentrating (~3%)Euphoria (~2-5%; may be misused)HeadacheFatigue

Serious

Angioedema (swelling of face, lips, tongue, throat — may be life-threatening; discontinue immediately)
Suicidal ideation and behavior (FDA boxed warning for all antiepileptic drugs)
Respiratory depression (especially with concomitant opioid use or in patients with underlying respiratory impairment)
Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) / multiorgan hypersensitivity (discontinue if suspected)
Rhabdomyolysis (rare; discontinue if markedly elevated CK with muscle symptoms)
Thrombocytopenia
PR interval prolongation (dose-related; clinical significance uncertain)
Withdrawal symptoms upon abrupt discontinuation (insomnia, nausea, headache, diarrhea, anxiety, sweating, seizures in epileptic patients)

Pregnancy & lactation

Pregnancy

Lactation

Pregabalin is excreted into human breast milk (estimated relative infant dose ~7% of maternal dose). Potential for adverse effects in breastfed infants (sedation, poor feeding, inadequate weight gain). A decision should be made whether to discontinue nursing or discontinue pregabalin, taking into account the importance of the drug to the mother. If breastfeeding continues, monitor infant for excessive sedation and adequate weight gain.

Drug interactions

Alcohol

Severe

Database

Additive CNS depression. Alcohol enhances the sedative and cognitive-impairing effects of pregabalin, increasing risk of excessive drowsiness, impaired judgment, respiratory depression, and accidents.

Advise complete abstinence from alcohol while taking pregabalin. If alcohol use occurs, limit strictly and avoid driving or operating machinery. Monitor for signs of excessive CNS depression.

Source: Kimi deep-research + Cla

Alfentanil

Severe

Database

Drug interaction classified as: absorption

Source: DDInter

Benzhydrocodone

Severe

Database

Drug interaction classified as: synergy

Source: DDInter

Buprenorphine