Dipyridamole

Anticoagulant drug From Wikipedia, the free encyclopedia

Dipyridamole

Dipyridamole, sold under the brand name Persantine among others, is an antiplatelet drug of the nucleoside transport inhibitor and PDE3 inhibitor class that inhibits blood clot formation when given chronically and causes blood vessel dilation when given at high doses over a short time.

Quick Facts Clinical data, Trade names ...
Dipyridamole
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Clinical data
Trade namesPersantine, others
AHFS/Drugs.comMonograph
MedlinePlusa682830
Routes of
administration
By mouth, intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability37–66%[1]
Protein binding~99%
MetabolismLiver (glucuronidation)[2]
Elimination half-lifeα phase: 40 min,
β phase: 10 hours
ExcretionBiliary (95%), urine (negligible)
Identifiers
  • 2,2',2'',2'''-(4,8-di(piperidin-1-yl)pyrimido[5,4-d]pyrimidine-2,6-diyl)bis(azanetriyl)tetraethanol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.000.340
Chemical and physical data
FormulaC24H40N8O4
Molar mass504.636 g·mol−1
3D model (JSmol)
  • C1CCN(CC1)C2=NC(=NC3=C2N=C(N=C3N4CCCCC4)N(CCO)CCO)N(CCO)CCO
  • InChI=1S/C24H40N8O4/c33-15-11-31(12-16-34)23-26-20-19(21(27-23)29-7-3-1-4-8-29)25-24(32(13-17-35)14-18-36)28-22(20)30-9-5-2-6-10-30/h33-36H,1-18H2 Y
  • Key:IZEKFCXSFNUWAM-UHFFFAOYSA-N Y
  (verify)
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Medical uses

Summarize
Perspective

Stroke

A combination of dipyridamole and aspirin (acetylsalicylic acid/dipyridamole) is FDA-approved for the secondary prevention of stroke and has a bleeding risk equal to that of aspirin use alone.[3] Dipyridamole absorption is pH-dependent and concomitant treatment with gastric acid suppressors (such as a proton pump inhibitor) will inhibit the absorption of liquid and plain tablets.[6][7][8][9]

However, it is not licensed as monotherapy for stroke prophylaxis, although a Cochrane review suggested that dipyridamole may reduce the risk of further vascular events in patients presenting after cerebral ischemia.[10]

A triple therapy of aspirin, clopidogrel, and dipyridamole has been investigated, but this combination led to an increase in adverse bleeding events.[11]

Interactions

Due to its action as a phosphodiesterase inhibitor, dipyridamole is likely to potentiate the effects of adenosine. This occurs by blocking the nucleoside transporter (ENT1) through which adenosine enters erythrocyte and endothelial cells.[12]

According to Association of Anaesthetists of Great Britain and Ireland 2016 guidelines, dipyridamole is considered to not cause risk of bleeding when receiving neuroaxial anaesthesia and deep nerve blocks. It does not therefore require cessation prior to anaesthesia with these techniques, and can continue to be taken with nerve block catheters in place.[13]

Overdose

Dipyridamole overdose can be treated with aminophylline[2]:6 or caffeine which reverses its dilating effect on the blood vessels. Symptomatic treatment is recommended, possibly including a vasopressor drug. Gastric lavage should be considered. Since dipyridamole is highly protein bound, dialysis is not likely to be of benefit.

Mechanisms of action

Dipyridamole has two known effects, acting via different mechanisms of action:

References

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