化合物信息

Drug Groups

approved

Description

A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)

Indication

For as an adjunct to coumarin anticoagulants in the prevention of postoperative thromboembolic complications of cardiac valve replacement and also used in prevention of angina.

Pharmacology

Dipyridamole, a non-nitrate coronary vasodilator that also inhibits platelet aggregation, is combined with other anticoagulant drugs, such as warfarin, to prevent thrombosis in patients with valvular or vascular disorders. Dipyridamole is also used in myocardial perfusion imaging, as an antiplatelet agent, and in combination with aspirin for stroke prophylaxis.

Toxicity

Hypotension, if it occurs, is likely to be of short duration, but a vasopressor drug may be used if necessary. The oral LD₅₀ in rats is greater than 6,000 mg/kg while in the dogs, the oral LD₅₀ is approximately 400 mg/kg. LD₅₀=8.4g/kg (orally in rat)

Affected Organisms

Biotransformation

hepatic

Absorption

70%

Half Life

40 minutes

Protein Binding

99%

Elimination

Dipyridamole is metabolized in the liver to the glucuronic acid conjugate and excreted with the bile.

Distribution

* 1 to 2.5 L/kg

Clearance

* 2.3-3.5 mL/min/kg

References

External Links