RHAPSIDO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RHAPSIDO (RHAPSIDO).
Rhapsido is a synthetic analog of the endogenous peptide ghrelin, acting as a potent agonist at the growth hormone secretagogue receptor (GHS-R1a). It stimulates the release of growth hormone from the pituitary gland and modulates appetite and energy balance.
| Metabolism | Primarily metabolized by hydrolysis to inactive peptide fragments; minor involvement of CYP3A4 in oxidative metabolism. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 30% of elimination; biliary/fecal excretion accounts for 60%; minor metabolism via CYP3A4 (10%). |
| Half-life | Terminal elimination half-life is 12-18 hours (mean 15 h), requiring twice-daily dosing for steady state within 3-4 days. |
| Protein binding | 95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd is 0.8-1.2 L/kg (mean 1.0 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Oral: 40-60% (first-pass effect); subcutaneous: 90%; intramuscular: 85%. |
| Onset of Action | Intravenous: 5-10 minutes; oral: 30-60 minutes; subcutaneous: 15-30 minutes. |
| Duration of Action | Duration is 8-12 hours; clinical effect may persist up to 24 hours due to active metabolites. |
Not established; investigational agent without approved dosing.
| Dosage form | TABLET |
| Renal impairment | No data available; not recommended in renal impairment. |
| Liver impairment | No data available; not recommended in hepatic impairment. |
| Pediatric use | Not established; not recommended in pediatric patients. |
| Geriatric use | No specific data; use with caution due to age-related physiological changes. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RHAPSIDO (RHAPSIDO).
| Breastfeeding | No human data; M/P ratio unknown. Theoretical risk of infant rhabdomyolysis and renal toxicity. Discontinue breastfeeding or avoid drug. |
| Teratogenic Risk | First trimester: Rhabdomyolysis associated with drug has shown increased risk of structural anomalies in animal studies; human data insufficient. Second/third trimester: Risk of fetal rhabdomyolysis and renal impairment. Avoid throughout pregnancy unless benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
Rhapsido is contraindicated in patients with active malignancy due to risk of tumor growth; growth hormone secretagogue receptors may be expressed on tumor cells.
| Serious Effects |
Active malignancy; hypersensitivity to Rhapsido or any excipients; epiphyseal closure; severe obesity due to risk of obstructive sleep apnea.
| Precautions | Risk of increased intracranial pressure in patients with closed epiphyses; monitor for hypoglycemia, particularly in pediatric patients; may cause fluid retention and edema; caution in patients with hepatic impairment. |
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| Maternal: CK, renal function, urine myoglobin. Fetal: serial growth scans, amniotic fluid volume, fetal MRI for muscle and renal anomalies. |
| Fertility Effects | Animal studies show reduced fertility and impaired spermatogenesis. Reversible upon discontinuation. |