IV PERSANTINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for IV PERSANTINE (IV PERSANTINE).
Inhibits adenosine deaminase and phosphodiesterase, increasing intracellular cAMP and adenosine; causes coronary vasodilation and inhibits platelet aggregation.
| Metabolism | Hepatic metabolism via glucuronidation; not metabolized by cytochrome P450 enzymes. |
| Excretion | Primarily hepatic metabolism (glucuronidation) with enterohepatic recirculation; renal excretion of unchanged drug is minimal (<1%); biliary/fecal elimination accounts for approximately 90% of the dose. |
| Half-life | Terminal elimination half-life is approximately 10-12 hours in adults; may be prolonged in patients with hepatic impairment. |
| Protein binding | Approximately 91-99% bound to plasma proteins, primarily to alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 2-3 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Intravenous: 100% (administered IV only); oral bioavailability is low (~10-20%) due to extensive first-pass metabolism; not relevant for IV route. |
| Onset of Action | Intravenous: Onset of coronary vasodilation occurs within 2-5 minutes after start of infusion; peak effect at 5-10 minutes. |
| Duration of Action | Intravenous: Duration of pharmacodynamic effect (e.g., increased coronary blood flow) is approximately 30-45 minutes; clinical effects (e.g., thallium imaging) may persist up to 2 hours. |
0.14 mg/kg/min intravenous infusion over 4 minutes for myocardial perfusion imaging.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific dose adjustment guidelines available; use with caution in severe hepatic impairment. |
| Pediatric use | Not commonly used; safety and efficacy not established. Limited data: 0.14 mg/kg/min intravenous infusion over 4 minutes, as per some protocols. |
| Geriatric use | No specific dose adjustment; monitor for adverse effects due to potential age-related changes in renal and hepatic function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for IV PERSANTINE (IV PERSANTINE).
| Breastfeeding | Unknown if excreted in human milk. M/P ratio not available. Caution advised; limited data suggest potential for adverse effects in infant (e.g., apnea, hypotension). |
| Teratogenic Risk | FDA Category B. Animal studies show no fetal risk; no adequate human studies in first trimester. No known teratogenicity in second or third trimester. |
| Fetal Monitoring |
■ FDA Black Box Warning
Intravenous administration may cause severe adverse reactions including fatal and non-fatal myocardial infarction, ventricular fibrillation, symptomatic hypotension, and cardiac arrest. Resuscitative equipment and trained staff must be immediately available.
| Serious Effects |
["Known hypersensitivity to dipyridamole or any component of the formulation.","Active coronary ischemia or ongoing chest pain.","Unstable angina or acute myocardial infarction.","Severe hypotension (systolic blood pressure <90 mm Hg)."]
| Precautions | ["Risk of myocardial ischemia and infarction; avoid in patients with unstable angina or acute coronary syndrome.","May cause hypotension; use with caution in patients with hypotension or hemodynamic instability.","Contraindicated in patients with known hypersensitivity to dipyridamole.","Aminophylline should be available for reversal of adverse effects.","Use with caution in elderly patients and those with hepatic impairment."] |
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| Monitor maternal blood pressure, heart rate, ECG; fetal heart rate and uterine activity during infusion. Assess for signs of ischemia or arrhythmia. |
| Fertility Effects | No known effect on human fertility. Animal studies show no impairment at therapeutic doses. |