PERSANTINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PERSANTINE (PERSANTINE).
Dipyridamole inhibits platelet phosphodiesterase and blocks adenosine uptake, leading to increased intracellular cAMP and potentiation of prostacyclin, resulting in inhibition of platelet aggregation. It also causes coronary vasodilation via adenosine-mediated effects.
| Metabolism | Hepatic metabolism via glucuronidation; no significant CYP involvement. |
| Excretion | Primarily hepatobiliary excretion into feces (approximately 80-90% as unchanged drug and metabolites). Renal excretion accounts for less than 10% of the dose, mainly as metabolites. |
| Half-life | Terminal elimination half-life is approximately 11-12 hours in healthy adults; may be prolonged in patients with hepatic impairment. |
| Protein binding | Approximately 91-99% bound to plasma proteins, primarily to alpha-1-acid glycoprotein (orosomucoid) and albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.7-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 40-60% due to first-pass metabolism. Not typically administered via other routes. |
| Onset of Action | Intravenous: immediate (within 2-3 minutes) for coronary vasodilation. Oral: peak effect occurs within 1-2 hours for antiplatelet effect. |
| Duration of Action | Intravenous: coronary vasodilation lasts about 30 minutes; oral: antiplatelet effects persist for 24 hours with regular dosing. |
75-100 mg orally four times daily as an adjunct to warfarin in prevention of thromboembolism; for cardiac stress testing, 0.57 mg/kg intravenously over 4 minutes (max 60 mg).
| Dosage form | TABLET |
| Renal impairment | No dosage adjustment necessary for GFR ≥10 mL/min; for GFR <10 mL/min, reduce dose or increase interval as accumulation may occur, but specific guidelines not established. |
| Liver impairment | No specific Child-Pugh based recommendations; use with caution in severe hepatic impairment due to potential for reduced metabolism and increased risk of adverse effects. |
| Pediatric use | For prevention of thromboembolism: 3-6 mg/kg/day orally in divided doses; for cardiac stress testing: 0.57 mg/kg intravenously over 4 minutes (max 60 mg). |
| Geriatric use | No specific dose adjustment required; monitor for hypotension and orthostatic effects due to increased sensitivity in elderly patients. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PERSANTINE (PERSANTINE).
| Breastfeeding | Dipyridamole is excreted in human breast milk. The milk-to-plasma ratio is approximately 0.5. Limited data suggest low risk to the nursing infant, but caution is advised. Consider the benefits of breastfeeding and the potential for adverse effects in the infant. |
| Teratogenic Risk | PERSANTINE (dipyridamole) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated fetal harm, but adequate studies in pregnant women are lacking. No specific teratogenic effects have been consistently reported in limited human data. Use only if clearly needed. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to dipyridamole or any component","Hypotension","Unstable angina or acute myocardial infarction (for stress testing)"]
| Precautions | ["May cause hypotension; use with caution in patients with hypotension or unstable angina","Can exacerbate angina or precipitate myocardial infarction due to coronary steal","Risk of bleeding when used with anticoagulants or antiplatelet agents","Use with caution in patients with aortic stenosis, left ventricular outflow obstruction, or severe coronary artery disease"] |
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| Fetal Monitoring |
| Monitor maternal blood pressure and heart rate during infusion. Observe for signs of hypotension or angina exacerbation. Fetal heart rate monitoring is recommended during intravenous administration for cardiac stress testing. |
| Fertility Effects | No specific studies on fertility effects in humans. Animal studies have not shown impaired fertility at clinically relevant doses. |