OLPRUVA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OLPRUVA (OLPRUVA).
Olprinone is a selective phosphodiesterase III (PDE3) inhibitor, which increases intracellular cyclic adenosine monophosphate (cAMP) levels in cardiac and vascular smooth muscle cells, leading to positive inotropic and vasodilatory effects.
| Metabolism | Primarily hepatic via CYP3A4 and other unspecified pathways; metabolites include inactive forms excreted renally. |
| Excretion | Primarily renal excretion as unchanged drug (approximately 70%) and glucuronide conjugate (approximately 15%); biliary/fecal excretion accounts for less than 10%. |
| Half-life | Terminal elimination half-life is approximately 18-22 hours in patients with normal renal function; prolonged in renal impairment (up to 40 hours in severe impairment). |
| Protein binding | Highly protein bound (>99%), primarily to albumin; also binds to alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 0.2-0.3 L/kg, indicating distribution mainly in extracellular fluid; minimal tissue binding. |
| Bioavailability | Oral bioavailability is approximately 85-90% (range 80-95%), not significantly affected by food. |
| Onset of Action | Oral: 2-4 hours after single dose for measurable clinical effect; maximal effect after multiple doses within 1-2 weeks. |
| Duration of Action | Duration of clinical effect is 24 hours with once-daily dosing; steady-state achieved after 5-7 days. |
2 mg orally three times daily with meals or as directed by physician
| Dosage form | FOR SUSPENSION |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not recommended in severe renal impairment (CrCl <30 mL/min) or dialysis. |
| Liver impairment | Contraindicated in Child-Pugh class B or C. For class A, use with caution; no specific dose adjustment established. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no dosing recommendations available. |
| Geriatric use | No specific dose adjustment recommended, but monitor renal function and consider increased sensitivity; use cautiously. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OLPRUVA (OLPRUVA).
| Breastfeeding | No human lactation data available. Olprinone is likely excreted into breast milk given its low molecular weight and protein binding. M/P ratio unknown. Use only if potential benefit outweighs risk; consider alternatives. |
| Teratogenic Risk | Olprinone (OLPRUVA) is a phosphodiesterase III inhibitor with limited human pregnancy data. In animal studies, no teratogenic effects were observed at clinically relevant doses. However, potential risks include reduced uteroplacental blood flow due to vasodilation. First trimester: insufficient data; avoid unless clearly needed. Second/third trimester: monitor fetal heart rate due to possible maternal hypotension and reflex tachycardia. Avoid near term due to risk of uterine relaxation and postpartum hemorrhage. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to olprinone or any component","Severe aortic or mitral valvular stenosis","Hypertrophic cardiomyopathy with outflow tract obstruction","Severe hypotension (systolic blood pressure < 90 mmHg)"]
| Precautions | ["May cause ventricular arrhythmias, including ventricular tachycardia and fibrillation, especially in patients with pre-existing arrhythmias or electrolyte imbalances","Monitor blood pressure and heart rate closely during infusion; risk of hypotension","Use with caution in patients with hepatic or renal impairment"] |
Loading safety data…
| Fetal Monitoring | Maternal: blood pressure, heart rate, electrocardiogram (QTc interval), signs of hypotension or arrhythmia. Fetal: heart rate monitoring (non-stress test or biophysical profile) if used in pregnancy for extended duration or at high doses. |
| Fertility Effects | No human data. In animal studies, no adverse effects on fertility at therapeutic doses. Theoretical risk of reduced sperm motility or oocyte quality due to PDE3 inhibition, but clinical significance unknown. |