Cilostazol

The PDE3 inhibitor, cilostazol, has been used as an antithrombotic agent and is currently being used in patients being treated for intermittent claudication. Cilostazol is also used for the prevention of restenosis after treatments such as angioplasty. Another PDE3 selective inhibitor, milrinone, has been used in the treatment of congestive heart failure. Milrinone also has been shown to increase the conductance of the CFTR transporter in vitro. 

Intermittent claudication is a group of symptoms characterized by pain in the calf muscle of one or both legp, caused by walking and relieved by rest. It is a manifestation of peripheral vascular disease, in which atherosclerotic lesions develop in the femoral artery, diminishing blood supply to the lower leg. Cilostazol is used to treat intermittent claudication. 

Take cilostazol (Pletal) 30 minutes before or 2 hours after meals. Do not take tiie drug with grapefruit j uice. 

C5H9CIO 5891-21-4) see Hydroxychloroquine 5-chloropentanoyI chloride (C5Hj Cl20 1575-61-7) see Cilostazol JV-(S-chloropentanoyl)cyclohexylamine (C11H20CINO 15865-18-6) see Cilostazol... 

C,7H, N20 93271-68-2) see Praziquantel l-cyclohexyl-5-(4-chlorobutyl)tetrazole (C, H C1N4 73963-42-5) see Cilostazol cyclohexylglyoxylic acid (CSH12O3 4354-49-8) see Cetiedil iV-cyclohexyl-AP-(2-hydroxyethyl)urea (C5HisN202 66929-46-2) see Lomustine... 

Anti-infective artemether, saguinavir Antilipemic atorrastatin, lovastatin, simvastatin Cardiovascular carvedilol, cilostazole, felodipine, nicardipine, nifedipine, nimodipine, nisoldipine, nitrendipine, verapamil... 

Pentoxifylline (Trental) or cilostazol (Pletal) may be useful in selected patients. Revascularization is successful in selected patients. 

PDE3 cGMP-inhibited PDE cAMP cGMP cGMP, milrinone, amrinone, anagrelide, cilostazol, lixazinone, NSP-513... 

CYP450 system Anagrelide enhanced the inhibition of platelet aggregation by aspirin and is an inhibitor of cyclic AMP PDE III (may exaggerate the properties of milrinone, enoximone, amrinone, olprinone, and cilostazol). 

Drugs that may be affected by proton pump inhibitors include azole antifungal agents (eg, itraconazole, ketoconazole), benzodiazepines, cilostazol, clarithromycin, digoxin, phenytoin, salicylates, sulfonylureas, and warfarin. Drugs that may affect proton pump inhibitors include sucralfate and clarithromycin. 

Drugs that may be affected by itraconazole include alfentanil, almotriptan, alprazolam, amphotericin B, aripiprazole, benzodiazepines, buspirone, busulfan, calcium blockers, carbamazepine, cilostazol, cisapride, corticosteroids, cyclosporine, digoxin, disopyramide, docetaxel, dofetilide, eletriptan, epierenone, ergot alkaloids, haloperidol, HMG-CoA reductase inhibitors, hydantoins (phenytoin), hypoglycemic agents, oral midazolam, phosphodiesterase type 5 inhibitors, pimozide, polyenes, protease inhibitors, quinidine, rifamycins, sirolimus, tacrolimus, tolterodine, triazolam, trimetrexate, vinca alkaloids, warfarin, and zolpidem. 

Cilostazol (Pletal) Drotrecogin Alfa (Xigris) Eculizumab (Soliris) Lanthanum Carbonate (Fosrenol)... 

WARNING Renal impair is the major tox foUow administration instructions Uses CMV retinitis w/ HIV Action Selective inhibition of viral DNA synth Dose Rx 5 mg/kg IV over 1 h once/wk for 2 wk w/ probenecid Maint 5 mg/kg IV once/2 wk w/ probenecid (2 g PO 3 h prior to cidofovir, then 1 g PO at 2 h 8 h after cidofovir) X in renal impair Caution [C, -] Contra Probenecid or sulfa allergy Disp Inj SE Renal tox, chills, fever, HA, NA /D, thrombocytopenia, neutropenia Interactions t Nephrotox W/ aminoglycosides, amphot icin B, foscar-net, IV pentamidine, NSAIDs, vancomycin t effects W/zidovudine EMS Monitor ECG for hypocalcemia (t QT int val) and hypokalemia (flattened T waves) OD May cause renal failure hydration may be effective in reducing drug levels/effects Cilostazol (Pletal) TAntiplatelet, Arterial Vasodilator/ Phosphodiesterase Inhibitor] Uses Reduce Sxs of intermittent claudication Action Phosphodiesterase in inhibitor t s cAMP in pits blood vessels, vasodilation inhibit pit aggregation Dose 100 mg PO bid, 1/2 h before or 2 h after breakfast dinner Caution [C, +/-] Contra CHE, hemostatic disorders. 

Toyobuku, H., Tamai, 1., Ueno, K. and Tsuji, A. (2003) Limited influence of P-glycoprotein on small-intestinal absorption of cilostazol, a high absorptive permeability drug. Journal of Pharmaceutical Sciences, 92, 2249-2259. 

Cilostazol is a selective cAMP phosphodiesterase inhibitor. It inhibits platelet aggregation and is a direct arterial vasodilator. It is used for the symptoms of intermittent claudication in individuals with peripheral vascular disease. Side-effects of cilostazol include headache, diarrhea, increased heart rate, and palpitations. Drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure. 

Atarashi H, Endoh Y, Saitoh H, Kiashida H, Hayakawa H. Chronotropic effects of cilostazol, a new antithrombotic agent, in patients with bradyarrhythmias. J Car-diovasc Pharmacol 1998 31 534-9. 

Cilostazol has been shown, in a multicenter, randomized, double-blind study (DP-PARA 2), to be superior to pentoxifylline for treatment of claudication symptoms... 

Avoid taking cilostazol with grapefruit juice because it may increase the drug s blood concentration and risk of toxicity... 

PLETAL (Otsuka America) (cilostazol) tablets May 2004 labeling... 

The bioavailability of felodipine was increased approximately twofold when taken with grapefruit juice. Orange juice does not appear to modify the kinetics of PLENDIL Grapefruit juice—Coadministration of felodipine with grapefruit juice resulted in more than twofold increase in the AUC and Cmax, but no prolongation in the half-life of felodipine Grapefruit juice increased the of cilostazol by approximately 50%, but had no effect on AUC... 

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