| Treatment of moderate-to-severe primary restless legs syndrome; postherpetic neuralgia (label). View labelExact | RLS: 600 mg once daily taken at about 5 PM with food (label). | Prodrug of gabapentin (alpha-2-delta ligand) used for moderate-to-severe primary restless legs syndrome and postherpetic neuralgia; converted by esterases to gabapentin (not CYP-mediated) with renal elimination of released gabapentin. | Extensive first-pass hydrolysis to gabapentin (non-CYP; carboxylesterases) (label)., Released gabapentin is not appreciably metabolized (label). | Single-dose range 5.1–6 h | No | | - Next-day sedation and driving/falls risk monitoring (label/clinical).
- Kidney function and renal-dose adjustment review (label).
- Mood and suicidality monitoring when baseline risk is elevated (label/class).
- Edema and weight monitoring during longer courses (label/clinical).
- Review of concurrent sedatives/substances (alcohol, opioids, benzodiazepines) to reduce additive CNS depression risk (label/clinical).
| No | 2025-12-30 |
|---|
pregabalinAdjunctive therapyBrands: LYRICA, LYRICA CR | Neuropathic pain (diabetic peripheral neuropathy, postherpetic neuralgia, spinal cord injury); fibromyalgia; adjunctive therapy for partial-onset seizures (label). Off-label psychiatry use includes anxiety symptoms and insomnia adjuncts. View labelExact | For off-label anxiety/sleep use, start low and titrate slowly over days to weeks based on sedation, dizziness, and functional impact.
Avoid rapid escalation or “chasing tolerance,” especially in patients with substance use risk; reassess diagnosis and first-line therapies instead. | Alpha-2-delta (α2δ) ligand that modulates voltage-gated calcium channels and reduces excitatory neurotransmitter release. | Negligible metabolism; eliminated primarily unchanged (label). | Single-dose mean 6.3 h | No | | - Check renal function (eGFR/CrCl) before starting and after clinical changes that may reduce clearance.
- Monitor sedation, dizziness, and driving/fall risk during titration.
- Track weight and assess peripheral edema; reassess if dyspnea or rapid weight change occurs.
- Screen for misuse/diversion signals (early refills, escalating doses, co-use with opioids/alcohol).
- Taper rather than stopping abruptly after sustained use.
| No | 2025-12-29 |
|---|
| Parkinson’s disease (PD) and moderate-to-severe primary restless legs syndrome (RLS) (label). View labelExact | RLS: start 0.125 mg once daily 2 to 3 hours before bedtime; dose may be increased every 4 to 7 days based on response and tolerability (label). | Non-ergoline dopamine agonist (D2/D3-preferring) indicated for Parkinson’s disease and moderate-to-severe primary restless legs syndrome; largely renally eliminated as unchanged drug with clinically important somnolence, impulse- control, hallucination/psychosis, and RLS augmentation considerations. | Negligible metabolism (<10%); not CYP-mediated (label). | Single-dose range 8–12 h | No | | - Somnolence and sudden sleep onset monitoring; driving safety review (label).
- Orthostatic blood pressure and dizziness/falls risk monitoring (label/clinical).
- Hallucinations/psychosis and mood destabilization monitoring, especially in serious mental illness (label/clinical).
- Impulse-control symptom monitoring (new compulsive behaviors) (label/clinical).
- RLS symptom timing tracking to detect augmentation (earlier onset, increased severity, spread) (guideline/clinical).
- Renal function review and renal-dose adjustment as needed (label).
| No | 2025-12-30 |
|---|
| Parkinson’s disease (PD) and moderate-to-severe primary restless legs syndrome (RLS) (label). View labelExact | RLS: start 0.25 mg once daily 1 to 3 hours before bedtime; titrate based on response/tolerability up to a maximum recommended dose of 4 mg once daily (label). | Non-ergoline dopamine agonist (D2/D3) indicated for Parkinson’s disease and moderate-to-severe primary restless legs syndrome; metabolized primarily by CYP1A2 with ~6 hour half-life and clinically important somnolence, impulse- control, hallucination/psychosis, and RLS augmentation considerations. | CYP1A2 (major) | Single-dose mean 6 h | No | | - Somnolence and sudden sleep onset monitoring; driving safety review (label).
- Orthostatic blood pressure and dizziness/falls risk monitoring (label/clinical).
- Hallucinations/psychosis and mood destabilization monitoring, especially in serious mental illness (label/clinical).
- Impulse-control symptom monitoring (new compulsive behaviors) (label/clinical).
- RLS symptom timing tracking to detect augmentation (earlier onset, increased severity, spread) (guideline/clinical).
- CYP1A2 interaction review, including smoking status changes (label/clinical).
| No | 2025-12-30 |
|---|