RALDESY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RALDESY (RALDESY).
Selective beta-3 adrenergic receptor agonist; relaxes detrusor smooth muscle during storage phase of urinary bladder fill cycle, increasing bladder capacity and reducing urgency.
| Metabolism | Extensively metabolized by multiple enzymes including CYP2D6, CYP3A4, butyrylcholinesterase, and UDP-glucuronosyltransferases (UGTs). |
| Excretion | Primarily renal (85-90%) with 60% unchanged; biliary/fecal (10-15%) |
| Half-life | 4-6 hours in adults; prolonged to 8-12 hours in elderly or renal impairment (CrCl <30 mL/min) |
| Protein binding | 99% bound primarily to albumin |
| Volume of Distribution | 0.15-0.25 L/kg, indicating limited extravascular distribution |
| Bioavailability | Oral: 85-90% |
| Onset of Action | Oral: 30-60 minutes; intravenous: 2-5 minutes |
| Duration of Action | 4-6 hours for analgesic effect; 6-8 hours for antipyretic effect |
Intravenous: 1 mg/kg every 8 hours; maximum single dose 100 mg.
| Dosage form | SOLUTION |
| Renal impairment | GFR ≥60 mL/min: no adjustment. GFR 30-59 mL/min: 1 mg/kg every 12 hours. GFR <30 mL/min: 1 mg/kg every 24 hours. Hemodialysis: administer after dialysis. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: not recommended. |
| Pediatric use | Children 1 month to 12 years: 1.5 mg/kg IV every 8 hours (max 100 mg per dose). Children ≥12 years: same as adult dosing. |
| Geriatric use | No specific age-based adjustment; use caution due to age-related renal decline; follow renal function-based dosing. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RALDESY (RALDESY).
| Breastfeeding | Contraindicated during breastfeeding. M/P ratio unknown; drug is excreted in human milk and may cause severe adverse effects in nursing infants. |
| Teratogenic Risk | FDA Pregnancy Category D. First trimester: known teratogen causing craniofacial defects, neural tube defects, and cardiovascular malformations. Second and third trimesters: risk of oligohydramnios, fetal renal impairment, and premature closure of ductus arteriosus. |
| Fetal Monitoring |
■ FDA Black Box Warning
Not applicable.
| Serious Effects |
["Hypersensitivity to mirabegron or any excipient.","Severe uncontrolled hypertension."]
| Precautions | ["May cause urinary retention, especially in patients with bladder outlet obstruction or taking anticholinergic medications.","Avoid use in patients with severe uncontrolled hypertension (systolic >180 mm Hg or diastolic >110 mm Hg).","Angioedema reported; discontinue if occurs.","Use with caution in patients with hepatic impairment (Child-Pugh class C: not recommended)."] |
Loading safety data…
| Monitor maternal blood pressure, renal function (serum creatinine, BUN), and liver enzymes (AST, ALT). Serial fetal ultrasound for growth, amniotic fluid index, and ductus arteriosus patency. Nonstress test or biophysical profile after 32 weeks. |
| Fertility Effects | May impair female fertility through disruption of ovarian function and endometrial receptivity. Use effective contraception during therapy and for at least 6 months after discontinuation. |