REQUIP
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REQUIP (REQUIP).
Dopamine receptor agonist; exhibits high affinity for D2 and D3 receptors, and moderate affinity for D1 and D4 receptors.
| Metabolism | Hepatic metabolism primarily via CYP1A2; minor contribution from CYP3A4. |
| Excretion | Primarily renal: approximately 90% of the dose is excreted in urine, with about 60% as unchanged drug and 30% as metabolites. Fecal excretion accounts for about 10%. |
| Half-life | Terminal elimination half-life: approximately 5-6 hours in young healthy adults, extending to 7-9 hours in elderly patients. Clinically, dosing is typically three times daily due to this short half-life. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution: approximately 0.7 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral immediate-release: absolute bioavailability is approximately 55% due to first-pass metabolism. Extended-release: bioavailability is similar but with slower absorption. |
| Onset of Action | Oral immediate-release: onset of clinical effect (improvement in motor symptoms) within 1-2 hours. Extended-release: onset delayed, typically 2-4 hours. |
| Duration of Action | Immediate-release: duration of clinical effect 4-6 hours, requires three times daily dosing. Extended-release: duration approximately 12-24 hours, allowing once-daily dosing for some patients. |
Immediate-release: Initial 0.25 mg orally three times daily; titrate weekly by 0.25 mg per dose to a total daily dose of 3 mg; max 24 mg/day. Extended-release: Initial 2 mg orally once daily; titrate by 2 mg/day at weekly intervals; max 24 mg/day.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment for mild to moderate impairment (CrCl >30 mL/min). For severe impairment (CrCl <30 mL/min), not recommended due to lack of data. |
| Liver impairment | No dose adjustment for mild to moderate impairment (Child-Pugh A or B). For severe impairment (Child-Pugh C), not recommended due to lack of data. |
| Pediatric use | Safety and efficacy not established; no approved pediatric dosing. |
| Geriatric use | Initiate at low end of dosing range; titrate slowly due to increased sensitivity and risk of adverse effects. Immediate-release: start 0.25 mg three times daily; extended-release: start 2 mg once daily. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REQUIP (REQUIP).
| Breastfeeding | Excreted in human milk; M/P ratio unknown. Potential for infant sedation and gastrointestinal effects. Avoid breastfeeding if possible. |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate studies; animal studies show fetal harm. Second and third trimesters: Potential for fetal respiratory depression and motor agitation if used near term. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to ropinirole or any component of the formulation"]
| Precautions | ["Risk of sudden onset of sleep and somnolence","Impulse control disorders (e.g., pathological gambling, hypersexuality)","Falling asleep during activities of daily living","Orthostatic hypotension","Hallucinations and psychotic-like behavior","Dyskinesia exacerbation","Risk of melanoma"] |
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| Monitor maternal blood pressure, heart rate, and symptoms of hypotension or sedation. Monitor fetal growth and well-being if used in pregnancy. |
| Fertility Effects | May cause menstrual irregularities and decreased libido. Reversible upon discontinuation. |