Dipyridamole
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Pharmacokinetic data | |
Bioavailability | 37–66%[1] |
Protein binding | ~99% |
Metabolism | Liver (glucuronidation)[2] |
Elimination half-life | α phase: 40 min, β phase: 10 hours |
Excretion | Biliary (95%), urine (negligible) |
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Dipyridamole (trademarked as Persantine and others) is a nucleoside transport inhibitor and a PDE3 inhibitor medication that inhibits blood clot formation[3][dead link] when given chronically and causes blood vessel dilation when given at high doses over a short time.
Medical uses
- Dipyridamole is used to dilate blood vessels in people with peripheral arterial disease and coronary artery disease.[4]
- Dipyridamole has been shown to lower pulmonary hypertension without significant drop of systemic blood pressure.
- It inhibits formation of pro-inflammatory cytokines (MMP-9) in vitro and results in reduction of hsCRP[clarification needed] in patients.
- It inhibits proliferation of smooth muscle cells in vivo and modestly increases unassisted patency of synthetic arteriovenous hemodialysis grafts.[5]
- It increases the release of tissue plasminogen activatorfrom brain microvascular endothelial cells.
- It results in an increase of 12-hydroxyeicosatetraenoic acidin the subendothelial matrix and reduced thrombogenicity of the subendothelial matrix.
- Pretreatment it reduced reperfusion injury in volunteers.
- It has been shown to increase myocardial perfusion and left ventricular function in patients with ischemic cardiomyopathy.
- It results in a reduction of the number of thrombin and PECAM-1 receptors on platelets in stroke patients.
- Cyclic adenosine monophosphate impairs platelet aggregation and also causes arteriolar smooth muscle relaxation. Chronic therapy did not show significant drop of systemic blood pressure.
- It inhibits the replication of mengovirus RNA.[6]
- It can be used for myocardial stress testing as an alternative to exercise-induced stress methods such as treadmills.
Stroke
A combination of dipyridamole and
However, it is not licensed as monotherapy for stroke prophylaxis, although a
A triple therapy of aspirin, clopidogrel, and dipyridamole has been investigated, but this combination led to an increase in adverse bleeding events.[12]
- Vasodilation occurs in healthy arteries, whereas electrocardiogram and echocardiographywhen it causes ischemia.
- Flow heterogeneity (a necessary precursor to ischemia) can be detected with Sestamibi. However, relative differences in perfusion do not necessarily imply any absolute decrease in blood supply in the tissue supplied by a stenosed artery.
Other uses
Dipyridamole also has non-medicinal uses in a laboratory context, such as the inhibition of cardiovirus growth in cell culture. [citation needed]
Drug interactions
Due to its action as a phosphodiesterase inhibitor, dipyridamole is likely to potentiate the effects of
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.[14]
Overdose
Dipyridamole
Mechanisms of action
Dipyridamole has two known effects, acting via different mechanisms of action:
- Dipyridamole inhibits the .
- Dipyridamole inhibits the cellular reuptake of endothelial cells, leading to increased extracellular concentrations of adenosine.
Experimental studies
Dipyridamole is currently undergoing repurposing for treatment of ocular surface disorders. These include
References
- PMID 474151.
- ^ a b "Aggrenox (aspirin/extended-release dipyridamole) Capsules. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Retrieved 1 December 2016.
- ^ "Dipyridamole" at Dorland's Medical Dictionary
- ^ PMID 25486915.
- PMID 19458364.
- PMID 16103157.
- S2CID 12877330.
- S2CID 36579161.
- ^ "Persantin Retard 200mg - Summary of Product Characteristics (SPC)". Electronic Medicines Compendium (EMC). Archived from the original on 5 July 2009. Retrieved 6 February 2010.
- ISBN 978-0-85369-424-3.
- PMID 17636684.
- PMID 18682741.
- S2CID 1877425.
- ^ AAGBI Guidelines Neuraxial and Coagulation June 2016
- PMID 24761148.
- ^ Rogosnitzky M, Bienstock CA, Issakov Y, Frenkel A (March 2016). Topical Dipyridamole for Treatment of Pterygium and Associated Dry Eye Symptoms: Analysis of User-Reported Outcomes. ISVER (Israeli Society for Vision and Eye Research) affiliate of ARVO (Association of Research in Vision and Ophthalmology). Kfar Maccabia, Israel. Retrieved 19 May 2019 – via ResearchGate.