Dipyridamole

Source: Wikipedia, the free encyclopedia.

Dipyridamole
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
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 checkY
  • Key:IZEKFCXSFNUWAM-UHFFFAOYSA-N checkY
  (verify)

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

Stroke

A combination of dipyridamole and

proton pump inhibitor) will inhibit the absorption of liquid and plain tablets.[7][8][9][10]

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.[11]

A triple therapy of aspirin, clopidogrel, and dipyridamole has been investigated, but this combination led to an increase in adverse bleeding events.[12]

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

endothelial cells.[13]

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

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:

Experimental studies

Dipyridamole is currently undergoing repurposing for treatment of ocular surface disorders. These include

pterygium and dry eye disease. The first report of topical dipyridamole's benefit in treating pterygium was published in 2014.[15] A subsequent report of outcomes in 25 patients using topical dipyridamole was presented in 2016.[16]

References

  1. .
  2. ^ a b "Aggrenox (aspirin/extended-release dipyridamole) Capsules. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Retrieved 1 December 2016.
  3. ^ "Dipyridamole" at Dorland's Medical Dictionary
  4. ^
    PMID 25486915
    .
  5. .
  6. .
  7. .
  8. .
  9. ^ "Persantin Retard 200mg - Summary of Product Characteristics (SPC)". Electronic Medicines Compendium (EMC). Archived from the original on 5 July 2009. Retrieved 6 February 2010.
  10. .
  11. .
  12. .
  13. .
  14. ^ AAGBI Guidelines Neuraxial and Coagulation June 2016
  15. PMID 24761148
    .
  16. ^ 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.