Cilostazol drug interactions: Difference between revisions

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__NOTOC__
#REDIRECT [[Cilostazol#Drug Interactions]]
{{Cilostazol}}
 
{{CMG}}; {{AE}} {{AK}}
 
==Cilostazol Drug Interactions==
 
===Aspirin===
 
Short-term (≤4 days) coadministration of [[aspirin ]]with PLETAL increased the inhibition of ADP-induced ex vivo platelet aggregation by 22%-37% when compared to either aspirin or PLETAL alone. Short-term (≤4 days) coadministration of [[aspirin ]]with PLETAL increased the inhibition of [[arachidonic acid]]-induced [[ex vivo]] platelet aggregation by 20% compared to PLETAL alone and by 48% compared to aspirin alone. However, short-term coadministration of aspirin with PLETAL had no clinically significant impact on [[PT]], [[aPTT]], or bleeding time compared to [[aspirin ]]alone. Effects of long-term coadministration in the general population are unknown. In eight randomized, placebo-controlled, double-blind clinical trials, aspirin was coadministered with cilostazol to 201 patients. The most frequent doses and mean durations of aspirin therapy were 75-81 mg daily for 137 days (107 patients) and 325 mg daily for 54 days (85 patients). There was no apparent increase in incidence of hemorrhagic adverse effects in patients taking cilostazol and [[aspirin ]]compared to patients taking placebo and equivalent doses of [[aspirin]].
 
===Warfarin===
 
The cytochrome P-450 isoenzymes involved in the metabolism of R-[[warfarin ]]are [[CYP3A4]], [[CYP1A2]], and [[CYP2C19]], and in the metabolism of S-warfarin, [[CYP2C9]]. Cilostazol did not inhibit either the metabolism or the pharmacologic effects (PT, aPTT, bleeding time, or platelet aggregation) of R- and S-warfarin after a single 25-mg dose of [[warfarin]]. The effect of concomitant multiple dosing of warfarin and PLETAL on the pharmacokinetics and pharmacodynamics of both drugs is unknown.
 
===Clopidogrel===
 
Multiple doses of [[clopidogrel ]]do not significantly increase steady state plasma concentrations of cilostazol.
 
===Inhibitors of CYP3A4===
 
====Strong Inhibitors of CYP3A4====
 
A priming dose of [[ketoconazole ]]400 mg (a strong inhibitor of CYP3A4), was given one day prior to coadministration of single doses of [[ketoconazole]]400 mg and cilostazol 100 mg. This regimen increased cilostazol Cmax by 94% and AUC by 117%. Other strong inhibitors of CYP3A4, such as [[itraconazole]], [[fluconazole]], [[miconazole]], [[fluvoxamine]], [[fluoxetine]], [[nefazodone]], and [[sertraline]], would be expected to have a similar effect (see DOSAGE AND ADMINISTRATION).
 
====Moderate Inhibitors of CYP3A4====
 
[[Erythromycin ]]and other[[ macrolide antibiotics]]: [[Erythromycin ]]is a moderately strong inhibitor of CYP3A4. Coadministration of [[erythromycin]]500 mg q 8h with a single dose of cilostazol 100 mg increased cilostazol Cmax by 47% and AUC by 73%. Inhibition of cilostazol metabolism by erythromycin increased the AUC of 4´-trans-hydroxy-cilostazol by 141%. Other macrolide antibiotics (e.g., [[clarithromycin]]), but not all (e.g., [[azithromycin]]), would be expected to have a similar effect (see [[Cilostazol dosage and administration|DOSAGE AND ADMINISTRATION]]).
[[Diltiazem]]: [[Diltiazem ]]180 mg decreased the clearance of cilostazol by ~30%. Cilostazol Cmax increased ~30% and AUC increased ~40% (see DOSAGE AND ADMINISTRATION).
Grapefruit Juice: [[Grapefruit juice]] increased the Cmax of cilostazol by ~50%, but had no effect on AUC.
 
====Inhibitors of CYP2C19====
 
''Omeprazole''
 
Coadministration of [[omeprazole ]]did not significantly affect the metabolism of cilostazol, but the systemic exposure to 3,4-dehydro-cilostazol was increased by 69%, probably the result of omeprazole's potent inhibition of CYP2C19 (see [[Cilostazol dosage and administration|DOSAGE AND ADMINISTRATION]]).
 
''Quinidine''
 
Concomitant administration of [[quinidine ]]with a single dose of cilostazol 100 mg did not alter cilostazol pharmacokinetics.
 
''Lovastatin''
 
The concomitant administration of [[lovastatin ]]with cilostazol decreases cilostazol Css, max and AUCτ by 15%. There is also a decrease, although nonsignificant, in cilostazol metabolite concentrations. Coadministration of cilostazol with [[lovastatin]] increases lovastatin and β-hydroxi lovastatin AUC approximately 70%. This is most likely clinically insignificant.
 
===Major Interactions===
{{refbegin|3}}
* [[Aptivus]]
* [[ardeparin]]
* [[Arixtra]]
* [[Arixtra 10 mg/dose]]
* [[Arixtra 5 mg/dose]]
* [[Arixtra 7.5 mg/dose]]
* [[Bexxar Dosimetric]]
* [[Bexxar I 131 Dosimetric]]
* [[Bexxar I 131 Therapeutic]]
* [[BexxarTherapeutic]]
* [[Clexane]]
* [[Clexane Forte]]
* [[dalteparin]]
* [[danaparoid]]
* [[dasatinib]]
* [[drotrecogin]]
* [[drotrecogin alfa]]
* [[enoxaparin]]
* [[fondaparinux]]
* [[Fragmin]]
* [[ibritumomab]]
* [[In-111 Zevalin]]
* [[Innohep]]
* [[iodine I 131 tositumomab]]
* [[Lovenox]]
* [[Lovenox HP]]
* [[Normiflo]]
* [[Orgaran]]
* [[Sprycel]]
* [[tinzaparin]]
* [[tipranavir]]
* [[tositumomab]]
* [[Xigris]]
* [[Y-90 Zevalin]]
 
{{refend}}
 
===Moderate Interactions===
{{refbegin|3}}
* [[abciximab]]
* [[Accolate]]
* [[Acetylsalicylic Acid]]
* [[Actron]]
* [[Acular]]
* [[Acular LS]]
* [[Acular PF]]
* [[Acuprin 81]]
* [[Adalat]]
* [[Adalat CC]]
* [[Advil]]
* [[Advil Childrens]]
* [[Advil Junior Strength]]
* [[Advil Liquigel]]
* [[Advil Migraine]]
* [[Advil Pediatric]]
* [[Afeditab CR]]
* [[Aflaxen]]
* [[Agenerase]]
* [[Aggrastat]]
* [[Agrylin]]
* [[Aleve]]
* [[Aleve Caplet]]
* [[Aleve Easy Open Arthritis]]
* [[Aleve Gelcap]]
* [[amiodarone]]
* [[amprenavir]]
* [[Anafranil]]
* [[anagrelide]]
* [[Anaprox]]
* [[Anaprox-DS]]
* [[Ansaid]]
* [[aprepitant]]
* [[armodafinil]]
* [[Arthritis Pain]]
* [[ASA]]
* [[Ascriptin Enteric]]
* [[Aspergum Cherry]]
* [[Aspergum Orginal]]
* [[Aspir-Low]]
* [[aspirin]]
* [[aspirin extended release]]
* [[Aspirin Lite Coat]]
* [[Aspirin Litecoat]]
* [[Aspirin Low Strength]]
* [[Aspirtab]]
* [[atazanavir]]
* [[Bayer Aspirin]]
* [[Bayer Aspirin Regimen]]
* [[Bayer Aspirin Sugar Free]]
* [[Bayer Aspirin with Calcium]]
* [[Bayer Childrens Aspirin]]
* [[Bayer Low Strength]]
* [[Bayer Plus]]
* [[Biaxin]]
* [[Biaxin XL]]
* [[Biaxin XL-Pak]]
* [[bortezomib]]
* [[bosentan]]
* [[bromfenac]]
* [[bromfenac ophthalmic]]
* [[bromocriptine]]
* [[Buffered Aspirin]]
* [[Bufferin]]
* [[Bufferin Arthritis Strength]]
* [[Bufferin Extra Strength]]
* [[Buffex]]
* [[Calan]]
* [[Calan SR]]
* [[Cardizem]]
* [[Cardizem CD]]
* [[Cardizem LA]]
* [[Cardizem Monovial]]
* [[Cardizem SR]]
* [[Cartia XT]]
* [[Cataflam]]
* [[Celexa]]
* [[Childrens Ibuprofen Berry]]
* [[Chloracol]]
* [[chloramphenicol]]
* [[Chloromycetin]]
* [[Chloromycetin Sodium Succinate]]
* [[cimetidine]]
* [[citalopram]]
* [[clarithromycin]]
* [[clarithromycin extended release]]
* [[Clinoril]]
* [[clomipramine]]
* [[clopidogrel]]
* [[clotrimazole]]
* [[conivaptan]]
* [[Cordarone]]
* [[Cordarone I.V.]]
* [[Covera-HS]]
* [[Crixivan]]
* [[Cyclosporine]]
* [[Cymbalta]]
* [[D.H.E. 45]]
* [[dalfopristin]]
* [[danazol]]
* [[Danocrine]]
* [[darunavir]]
* [[Daypro]]
* [[delavirdine]]
* [[desvenlafaxine]]
* [[dexfenfluramine]]
* [[diclofenac]]
* [[diclofenac ophthalmic]]
* [[diclofenac potassium]]
* [[diclofenac sodium]]
* [[diclofenac sodium extended release]]
* [[diclofenac topical]]
* [[Diflucan]]
* [[dihydroergotamine]]
* [[dihydroergotamine nasal]]
* [[Dilacor XR]]
* [[Diltia XT]]
* [[diltiazem]]
* [[diltiazem 24 hour extended release]]
* [[diltiazem extended release]]
* [[Diltiazem Hydrochloride CD]]
* [[Diltiazem Hydrochloride SR]]
* [[Diltiazem Hydrochloride XR]]
* [[Diltiazem Hydrochloride XT]]
* [[dipyridamole]]
* [[duloxetine]]
* [[DurAct]]
* [[E-Mycin]]
* [[E.E.S. Granules]]
* [[E.E.S.-200]]
* [[E.E.S.-400]]
* [[E.E.S.-400 Filmtab]]
* [[Easprin]]
* [[EC-Naprosyn]]
* [[Ecotrin]]
* [[Ecotrin Adult Low Strength]]
* [[Ecotrin Maximum Strength]]
* [[Effexor]]
* [[Effexor XR]]
* [[Elmiron]]
* [[Emend]]
* [[Emend 3-Day]]
* [[Emend for Injection]]
* [[Empirin]]
* [[Entaprin]]
* [[Entercote]]
* [[eptifibatide]]
* [[Ergomar]]
* [[ergotamine]]
* [[Ery-Tab]]
* [[Eryc]]
* [[EryPed]]
* [[EryPed 200]]
* [[EryPed 400]]
* [[Erythrocin Lactobionate]]
* [[Erythrocin Stearate Filmtab]]
* [[Erythrocot]]
* [[erythromycin]]
* [[erythromycin base]]
* [[erythromycin estolate]]
* [[erythromycin ethylsuccinate]]
* [[erythromycin lactobionate]]
* [[erythromycin stearate]]
* [[escitalopram]]
* [[esomeprazole]]
* [[etodolac]]
* [[etodolac extended release]]
* [[etravirine]]
* [[Extra Strength Bayer]]
* [[Fasprin]]
* [[felbamate]]
* [[Felbatol]]
* [[Feldene]]
* [[Femara]]
* [[fenfluramine]]
* [[fenoprofen]]
* [[FK506]]
* [[Flector Patch]]
* [[fluconazole]]
* [[fluoxetine]]
* [[fluoxetine extended release]]
* [[flurbiprofen]]
* [[flurbiprofen ophthalmic]]
* [[fluvoxamine]]
* [[fluvoxamine extended release]]
* [[Fortovase]]
* [[fosamprenavir]]
* [[fosaprepitant]]
* [[Genacote]]
* [[Gengraf]]
* [[Gennin-FC]]
* [[Genpril]]
* [[Genprin]]
* [[Gleevec]]
* [[Halfprin]]
* [[Haltran]]
* [[hemin]]
* [[Ibu]]
* [[IBU-200]]
* [[Ibu-4]]
* [[Ibu-6]]
* [[Ibu-8]]
* [[Ibu-Tab]]
* [[ibuprofen]]
* [[Ibuprofen PMR]]
* [[iloprost]]
* [[Ilosone]]
* [[Ilotycin Gluceptate]]
* [[imatinib]]
* [[indinavir]]
* [[Indocin]]
* [[Indocin SR]]
* [[indomethacin]]
* [[indomethacin extended release]]
* [[INH]]
* [[Integrilin]]
* [[Intelence]]
* [[Invirase]]
* [[isoniazid]]
* [[Isoptin]]
* [[Isoptin I.V.]]
* [[Isoptin SR]]
* [[itraconazole]]
* [[Ketek]]
* [[Ketek Pak]]
* [[ketoconazole]]
* [[ketoprofen]]
* [[ketoprofen extended release]]
* [[ketorolac]]
* [[ketorolac ophthalmic]]
* [[lanreotide]]
* [[lapatinib]]
* [[Leader Naproxen Sodium]]
* [[letrozole]]
* [[Lexapro]]
* [[Lexiva]]
* [[Litecoat Aspirin]]
* [[Lodine]]
* [[Lodine XL]]
* [[Low Dose ASA]]
* [[Luvox]]
* [[Luvox CR]]
* [[meclofenamate]]
* [[Meclomen]]
* [[mefenamic acid]]
* [[meloxicam]]
* [[Menadol]]
* [[Meridia]]
* [[mibefradil]]
* [[miconazole]]
* [[Midol Extended Relief]]
* [[Midol IB]]
* [[Midol Maximum Strength Cramp Formula]]
* [[Migranal]]
* [[Minitabs]]
* [[Mobic]]
* [[modafinil]]
* [[Monistat I.V.]]
* [[Motrin]]
* [[Motrin Childrens]]
* [[Motrin IB]]
* [[Motrin Infant Drops]]
* [[Motrin Junior Strength]]
* [[Motrin Migraine Pain]]
* [[MY-E]]
* [[Mycelex Troche]]
* [[nabumetone]]
* [[Nalfon]]
* [[Naprelan '375']]
* [[Naprelan '500']]
* [[Naprosyn]]
* [[naproxen]]
* [[naproxen sodium]]
* [[Naproxen Sodium DS]]
* [[naproxen sodium extended release]]
* [[nefazodone]]
* [[nelfinavir]]
* [[NeoProfen]]
* [[Neoral]]
* [[nepafenac ophthalmic]]
* [[Nevanac]]
* [[Nexium]]
* [[Nexium I.V.]]
* [[Nifediac CC]]
* [[Nifedical XL]]
* [[Nifedipine]]
* [[Nifedipine Extended Release]]
* [[nilotinib]]
* [[Nizoral]]
* [[Norvir]]
* [[Norvir Soft Gelatin]]
* [[Norwich Aspirin]]
* [[Noxafil]]
* [[Nuprin]]
* [[Nuvigil]]
* [[Nydrazid]]
* [[octreotide]]
* [[Ocufen]]
* [[omeprazole]]
* [[Orudis]]
* [[Orudis KT]]
* [[Oruvail]]
* [[oxaprozin]]
* [[oxcarbazepine]]
* [[Pacerone]]
* [[Panhematin]]
* [[Parlodel]]
* [[paroxetine]]
* [[paroxetine extended release]]
* [[paroxetine mesylate]]
* [[Paxil]]
* [[Paxil CR]]
* [[PCE Dispertab]]
* [[Pediacare Fever]]
* [[pentosan polysulfate sodium]]
* [[Persantine]]
* [[Persantine IV]]
* [[Pexeva]]
* [[phenylbutazone]]
* [[piroxicam]]
* [[Plavix]]
* [[Pondimin]]
* [[Ponstel]]
* [[posaconazole]]
* [[Posicor]]
* [[Prezista]]
* [[Priftin]]
* [[Prilosec]]
* [[Prilosec OTC]]
* [[Pristiq]]
* [[Procardia]]
* [[Procardia XL]]
* [[Prograf]]
* [[Provigil]]
* [[Prozac]]
* [[Prozac Weekly]]
* [[Q-Profen]]
* [[Rapamune]]
* [[Rapiflux]]
* [[Redux]]
* [[Relafen]]
* [[Remodulin]]
* [[Reopro]]
* [[Rescriptor]]
* [[Reyataz]]
* [[rifapentine]]
* [[ritonavir]]
* [[Robimycin]]
* [[Rufen]]
* [[Saleto-200]]
* [[Saleto-400]]
* [[Saleto-600]]
* [[Saleto-800]]
* [[Sandimmune]]
* [[Sandostatin]]
* [[Sandostatin LAR Depot]]
* [[saquinavir]]
* [[saquinavir mesylate]]
* [[Sarafem]]
* [[Selfemra]]
* [[sertraline]]
* [[Serzone]]
* [[sibutramine]]
* [[sirolimus]]
* [[Sloprin]]
* [[Solaraze]]
* [[Somatuline Depot]]
* [[Sporanox]]
* [[St. Joseph Aspirin]]
* [[St. Joseph Aspirin Adult Chewable]]
* [[St. Joseph Aspirin Adult EC]]
* [[Stanback Analgesic]]
* [[sulindac]]
* [[suprofen ophthalmic]]
* [[tacrolimus]]
* [[Tagamet]]
* [[Tagamet HB]]
* [[Tao]]
* [[Tasigna]]
* [[Taztia XT]]
* [[telithromycin]]
* [[Telzir]]
* [[Therapy Bayer]]
* [[Tiazac]]
* [[Ticlid]]
* [[ticlopidine]]
* [[tirofiban]]
* [[Tolectin]]
* [[Tolectin 600]]
* [[Tolectin DS]]
* [[tolmetin]]
* [[Toradol]]
* [[Toradol IM]]
* [[Toradol IV/IM]]
* [[Tracleer]]
* [[treprostinil]]
* [[Tri-Buffered Aspirin]]
* [[Trileptal]]
* [[troleandomycin]]
* [[Tykerb]]
* [[Vaprisol]]
* [[Velcade]]
* [[venlafaxine]]
* [[venlafaxine extended release]]
* [[Ventavis]]
* [[verapamil]]
* [[verapamil 24 hour extended release]]
* [[verapamil extended release]]
* [[Verelan]]
* [[Verelan PM]]
* [[Vfend]]
* [[Viracept]]
* [[Voltaren]]
* [[Voltaren Ophthalmic]]
* [[Voltaren Topical]]
* [[Voltaren-XR]]
* [[voriconazole]]
* [[Xibrom]]
* [[YSP Aspirin]]
* [[zafirlukast]]
* [[Zegerid (Original Formulation)]]
* [[Zero-Order Release]]
* [[Zoloft]]
* [[Zorprin]]
{{refend}}
 
===Minor Interactions===
{{refbegin|3}}
* [[bexarotene]]
* [[capsaicin]]
* [[capsicum]]
* [[chamomile]]
* [[Coumadin]]
* [[fenugreek]]
* [[Hep-Lock]]
* [[Hep-Pak]]
* [[Hep-Pak CVC]]
* [[heparin]]
* [[Heparin Lock Flush]]
* [[Jantoven]]
* [[matricaria]]
* [[Targretin]]
* [[warfarin]]
{{refend}}
 
 
{{FDA}}
 
 
==References==
http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=24d75b58-bafb-4440-b8d7-4f4079c08b0b
[[Category:Cardiovascular Drugs]]
[[Category:Drugs]]

Latest revision as of 22:25, 21 July 2014