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| {{drugbox
| | #REDIRECT [[Dipyridamole#Pharmacology]] |
| | IUPAC_name = 2-{[9-(bis(2-hydroxyethyl)amino)-2,7-bis(1-piperidyl)-<br>3,5,8,10-tetrazabicyclo[4.4.0]deca-2,4,7,9,11-pentaen-<br>4-yl]-(2-hydroxyethyl)amino}ethanol
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| | image = Dipyridamole_svg.png
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| | CAS_number = 58-32-2
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| | ATC_prefix = B01
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| | ATC_suffix = AC07
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| | PubChem = 3108
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| | DrugBank = APRD00360
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| | C = 24 |H = 40 |N = 8 |O = 4
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| | molecular_weight = 504.626 [[Gram|g]]/[[Mole (unit)|mol]]
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| | bioavailability =
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| | protein_bound = 99%
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| | metabolism =
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| | elimination_half-life = 40 minutes
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| | pregnancy_category = B
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| | legal_status =
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| | routes_of_administration = PO, IV
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| }}
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| __NOTOC__
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| {{CMG}}
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| ==[[Dipyridamole (patient information)|For patient information, click here]]==
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| ==Overview==
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| '''Dipyridamole''' is a [[medication|drug]] that inhibits thrombus formation when given chronically and causes [[vasodilation]] when given at high doses over short time.
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| * It inhibits the cellular reuptake of [[adenosine]] into platelets, [[red blood cell]]s and [[endothelial cell]]s leading to increased extracellular concentrations of adenosine.
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| * It also inhibits the [[enzyme]] [[adenosine deaminase]] which normally breaks down [[adenosine]] into [[inosine]]. This inhibition leads to further increased levels of extracellular adenosine.
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| * Dipyridamole also inhibits the enzyme [[phosphodiesterase]]- 5 (PDE 5) which normally breaks down [[cGMP]]. This results in added benefit when given together with NO or statins.
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| * Dipyridamole has shown to lower pulmonary hypertension without significant drop of systemic blood pressure
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| * Dipyridamole inhibits formation of pro-inflammatory cytokines (MCP-1, MMP-9) in vitro and results in reduction of hsCRP in patients.
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| * Dipyridamole inhibits proliferation of smooth muscle cells in vivo and has shown to prevent AV-shunt failure in dialysis patients.
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| * Dipyridamole increases release of t-PA from brain microvascular endothelial cells
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| * Dipyridamole treatment in vivo results in increase of 13 - HODE and decrease of 12 - HETE in the subendothelial matrix (SEM) and reduced thrombogenicity of the SEM.
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| * Dipyridamole pretreatment reduced reperfusion injury in volunteers.
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| * Dipyridamole treatment has shown to increase myocardial perfusion and left ventricular function in patients with ischemic cardiomyopathy.
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| * Dipyridamole treatment resulted in reduction of the number of thrombin and PECAM-1 receptors on platelets in stroke patients.
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| * Adenosine interacts with the adenosine receptors to cause increased cAMP via [[adenylate cyclase]].
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| * cAMP impairs platelet aggregation and also causes [[arteriole|arteriolar]] [[smooth muscle]] relaxation. Chronic therapy did not show significant drop of systemic blood pressure.
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| ==Use in individuals with a history of stroke==
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| Modified release dipyridamole is used in conjunction with [[aspirin]] (under the trade name '''Aggrenox'''®) in the secondary prevention of [[stroke]] and [[transient ischemic attack]]. Dipyridamole absorption is pH dependent and concomitant treatment with gastric acid suppressors will inhibit uptake significantly. The sustained formulation in '''Aggrenox'''® also corrects for this impairment.
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| <ref name="Diener-1996">{{cite journal | author=Diener HC, Cunha L, Forbes C, Sivenius J, Smets P, Lowenthal A. | title=European Stroke Prevention Study 2. Dipyridamole and acetylsalicylic acid in the secondary prevention of stroke. | journal=J Neurol Sci | year=1996 | volume=143 | issue=1-2 | pages=1-13 | id=PMID 8981292}}</ref> This practice is now confirmed by the ESPRIT trial.
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| It is not, however, licensed as monotherapy for stroke prophylaxis.
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| ==Use in nuclear stress testing==
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| Dipyridamole ('''Persantine''') is also used in pharmacological [[nuclear medicine|nuclear]] cardiac [[stress testing]] mediating coronary vasodilation.
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| * Via the mechanisms mentioned above, when given as 3 to 5 min infusion it rapidly increases the local concentration of adenosine in the coronary circulation which causes vasodilation .
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| * Vasodilation occurs in healthy arteries, whereas [[stenosis|stenosed]] arteries remain narrowed. This creates a "steal" phenomenon where the coronary blood supply will increase to the dilated healthy vessels compared to the stenosed arteries which can then be detected by clinical symptoms of chest pain, [[electrocardiogram]] and [[echocardiography]] when it causes ischemia.
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| * Flow heterogeneity (a necessary precursor to ischemia) can be detected with [[gamma camera]]s and [[SPECT]] using nuclear imaging agents such as [[Thallium]]-201 and [[Technetium-99m|Tc99m]]-[[Sestamibi]]. However relative differences in perfusion not necessarily imply absolute decrease in blood supply in the tissue supplied by a stenosed artery.
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| ==Other uses of dipyridamole==
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| Dipyridamole also has non-medicinal uses in a laboratory context, such as the inhibition of [[cardiovirus]] growth in [[cell culture]].
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| ==Overdose==
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| Dipyridamole [[overdose]] can be treated with [[aminophylline]]<ref>Aggrenox. RxList.com. URL: [http://www.rxlist.com/cgi/generic/aggrenox_od.htm http://www.rxlist.com/cgi/generic/aggrenox_od.htm]. Accessed on: May 1, 2007.</ref> and reverses its [[hemodynamics|hemodynamic]] effects (vasodilation).
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| ==References==
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| {{Reflist}}
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| ==External Link==
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| * Dipyridamole in the laboratory: {{cite web | last = Fata-Hartley | first = Cori L. | coauthors=Ann C. Palmenberg | title = Dipyridamole reversibly inhibits mengovirus RNA replication
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| | url=http://jvi.asm.org/cgi/content/full/79/17/11062?view=long&pmid=16103157 | doi=10.1128/JVI.79.17.11062-11070.2005 }}.
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| {{Antithrombotics}}
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| [[Category:Antiplatelet drugs]]
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