OSPOMYV
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OSPOMYV (OSPOMYV).
Sodium oxybate is a CNS depressant that acts primarily via gamma-aminobutyric acid (GABA) B receptor agonism, leading to increased slow-wave sleep and suppression of cataplexy.
| Metabolism | Metabolized primarily via the citric acid cycle (Krebs cycle) to carbon dioxide and water; no involvement of cytochrome P450 enzymes. |
| Excretion | Primarily renal excretion as unchanged drug (approximately 75-80%) with minor biliary/fecal elimination (15-20%) and a small amount metabolized. |
| Half-life | Terminal elimination half-life is 24-36 hours, supporting once-daily dosing; prolonged in renal impairment. |
| Protein binding | Approximately 92-95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.5-0.8 L/kg, indicating distribution into total body water and some tissue binding. |
| Bioavailability | Oral bioavailability is 60-70% due to first-pass metabolism and is unaffected by food. |
| Onset of Action | Oral: 2-4 hours; Intravenous: within minutes achieving peak effect at 1-2 hours. |
| Duration of Action | Duration of action is 24-36 hours, with clinical effects sustained throughout the dosing interval; longer in renal dysfunction. |
Intravenous: 100 mg once daily infused over 30 minutes.
| Dosage form | INJECTABLE |
| Renal impairment | GFR 30-59 mL/min: 100 mg every 48 hours. GFR 15-29 mL/min: 100 mg every 72 hours. GFR <15 mL/min or on hemodialysis: 100 mg once weekly after dialysis on dialysis days. |
| Liver impairment | Child-Pugh A: No dose adjustment. Child-Pugh B: Use with caution; no specific dose recommendation. Child-Pugh C: Not recommended. |
| Pediatric use | Weight ≥40 kg: 100 mg once daily. Weight <40 kg: safety and efficacy not established. |
| Geriatric use | No specific dose adjustment recommended; monitor renal function due to age-related decline, and adjust per renal guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OSPOMYV (OSPOMYV).
| Breastfeeding | No data available on excretion in human milk. Due to potential for serious adverse reactions in breastfed infants (e.g., neutropenia, diarrhea, rash), breastfeeding is not recommended during therapy and for at least 1 month after last dose. M/P ratio is unknown. |
| Teratogenic Risk | Ospomyv (buparlisib) is an oral PI3K inhibitor. There are no adequate and well-controlled studies in pregnant women. In animal studies, administration during organogenesis caused increased embryonic resorption and decreased fetal weight. In the first trimester, there is potential for teratogenicity (neural tube defects, cardiac anomalies) based on animal data. In the second and third trimesters, risks include fetal growth restriction, oligohydramnios, and potential for fetal toxicity. Use is contraindicated unless benefit outweighs risk; effective contraception is required. |
■ FDA Black Box Warning
WARNING: CENTRAL NERVOUS SYSTEM DEPRESSANT; ABUSE AND MISUSE; and RESPIRATORY DEPRESSION. Sodium oxybate is a CNS depressant and can cause respiratory depression, especially when used with other CNS depressants or in patients with respiratory impairment. It has abuse potential and should be dispensed only through a restricted program.
| Serious Effects |
Concurrent use with alcohol or other CNS depressants, succinic semialdehyde dehydrogenase deficiency, and severe hepatic impairment.
| Precautions | CNS depression (caution with alcohol or other CNS depressants), respiratory depression (especially in patients with sleep apnea or compromised respiratory function), abuse and dependence (Schedule III controlled substance), depression and suicidality, parasomnias (sleepwalking), and use in patients with succinic semialdehyde dehydrogenase deficiency (contraindicated). |
Loading safety data…
| Fetal Monitoring | Monitor maternal hepatic function (ALT, AST, bilirubin) every cycle; monitor for hyperglycemia (fasting glucose, HbA1c); monitor for rash, diarrhea, and infections. Perform complete blood counts every cycle for neutropenia. In pregnant patients, obtain serial ultrasounds to assess fetal growth, amniotic fluid volume, and anatomy. |
| Fertility Effects | Ospomyv may impair female and male fertility. In animal studies, buparlisib caused reduced fertility and embryonic loss due to inhibition of PI3K signaling. In humans, fertility effects may include oligospermia in males and menstrual irregularities or ovarian dysfunction in females. Effects may be reversible. |