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Persantine (DIPYRIDAMOLE)

Boehringer Ingelheim · FDA-approved approved Small molecule Verified Quality 80/100

Persantine works by inhibiting platelet activation and aggregation by blocking the equilibrative nucleoside transporter 1.

Persantine (Dipyridamole) is a small molecule platelet aggregation inhibitor developed by Boehringer Ingelheim, targeting the equilibrative nucleoside transporter 1. It was first approved by the FDA in 1961 for various indications, including atrial fibrillation, chronic heart failure, and myocardial perfusion imaging adjunct. Persantine is now off-patent, with 17 generic manufacturers available. Key safety considerations include its potential to cause vasodilation and myocardial ischemia. As a platelet aggregation inhibitor, Persantine works by inhibiting platelet activation and aggregation, thereby reducing the risk of thrombosis.

At a glance

Generic nameDIPYRIDAMOLE
SponsorBoehringer Ingelheim
Drug classPlatelet Aggregation Inhibitor [EPC]
TargetEquilibrative nucleoside transporter 1
ModalitySmall molecule
Therapeutic areaCardiovascular
PhaseFDA-approved
First approval1961

Mechanism of action

Mechanism of Action. Dipyridamole inhibits the uptake of adenosine into platelets, endothelial cells and erythrocytes in vitro and in vivo; the inhibition occurs in dose-dependent manner at therapeutic concentrations (0.5-1.9 ug/mL). This inhibition results in an increase in local concentrations of adenosine which acts on the platelet 2-receptor thereby stimulating platelet adenylate cyclase and increasing platelet cyclic-3,5- adenosine monophosphate (cAMP) levels. Via this mechanism, platelet aggregation is inhibited in response to various stimuli such as platelet activating factor (PAF), collagen and adenosine diphosphate (ADP). Dipyridamole inhibits phosphodiesterase (PDE) in various tissues. While the inhibition of cAMP-PDE is weak, therapeutic levels of dipyridamole inhibit cyclic-3,5-guanosine monophosphate-PDE (cGMP- PDE), thereby augmenting the increase in cGMP produced by EDRF (endothelium-derived relaxing factor, now identified as nitric oxide).

Approved indications

Common side effects

Drug interactions

Key clinical trials

Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results

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