RALDESY
Clinical safety rating
cautionComprehensive 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 |
| Molecular Weight | 367.5 |
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 | Avoid; associated with teratogenic effects in animal studies; no adequate human data. |
| 2nd trimester | Use only if benefit outweighs risk; limited human data; potential for fetal harm. |
| 3rd trimester | Avoid; may cause fetal hypotension and hypoglycemia; use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for RALDESY (RALDESY).
| Placental transfer | Crosses placenta (animal studies); high protein binding likely limits transfer, but molecular weight <500 Da suggests possible human transfer. |
| Breastfeeding | Excreted into breast milk in low amounts; however, due to potential serious adverse reactions in infants, breastfeeding is not recommended during therapy and for at least 5 half-lives after last dose. |
| Lactation Rating | L4 (Contraindicated) |
| 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 | 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. |
■ FDA Black Box Warning
Not applicable.
| Serious Effects |
Hypersensitivity to raldesySevere hepatic impairmentConcomitant use with strong CYP3A4 inducers
| 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). |
| Food/Dietary | Avoid tyramine-rich foods: aged cheeses (e.g., cheddar, blue cheese), cured/smoked meats (e.g., salami, pepperoni), fermented foods (e.g., sauerkraut, soy sauce), draft beers, red wine, and overripe fruits. These can cause a hypertensive crisis when combined with MAO-B inhibitors. |
| Clinical Pearls | RALDESY is a brand name for rasagiline, an MAO-B inhibitor used for Parkinson's disease. Avoid concurrent use with MAO-A inhibitors or serotonergic drugs due to risk of serotonin syndrome. Monitor for hypertension, especially when consuming tyramine-rich foods. Start at 1 mg once daily; can increase to 2 mg in patients not responding. Do not use with opioids (e.g., meperidine, tramadol) or St. John's wort. |
| Patient Advice | Take RALDESY at the same time each day with or without food. · Avoid foods high in tyramine (e.g., aged cheeses, cured meats, fermented products) to prevent hypertensive crisis. · Do not stop taking RALDESY abruptly; consult your doctor before discontinuing. · Report symptoms like severe headache, palpitations, or confusion immediately. · Inform all healthcare providers you are taking RALDESY, especially before surgery or starting new medications. |
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