Cilostazol

Bezeichnung:Cilostazol

CAS-Nr73963-72-1

Englisch Name:Cilostazol

CBNumberCB2362876

SummenformelC20H27N5O2

Molgewicht369.46

MOL-Datei73963-72-1.mol

Cilostazol physikalisch-chemischer Eigenschaften

Schmelzpunkt	159-160°C
Siedepunkt	499.57°C (rough estimate)
Dichte	1.1832 (rough estimate)
Brechungsindex	1.7600 (estimate)
storage temp.	Inert atmosphere,Room Temperature
Löslichkeit	DMSO: 18 mg/mL, soluble
Aggregatzustand	solid
pka	14.22±0.20(Predicted)
Farbe	off-white
maximale Wellenlänge (λmax)	257nm(MeOH)(lit.)
Merck	14,2277
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months
InChIKey	RRGUKTPIGVIEKM-UHFFFAOYSA-N

Sicherheit

Kennzeichnung gefährlicher	Xi
WGK Germany	2
RTECS-Nr.	VC8277500
HS Code	29339900
Giftige Stoffe Daten	73963-72-1(Hazardous Substances Data)
Toxizität	LD50 in mice, rats (mg/kg): >2000, >2000 i.p.; >5000, >5000 orally (Nomura)

Gefahreninformationscode (GHS)

Cilostazol Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Cilostazol is a platelet aggregation inhibitor with cerebral vasodilating activity, indicated for use in stroke and myocardial infarction. In patients with cerebral thrombosis, transient ischemia and cerebral arteriosclerosis, cilostazol significantly inhibits ADP-, collagenand epinephrine-induced platelet aggregation. Side effects include headache and tachycardia.
Chemische Eigenschaften
Colourless Needles
Originator
Otsuka (Japan)
Verwenden
An inhibitor of phosphodiesterase III
Verwenden
antibacterial; LD50(iv) 280mg/kg(mouse)
Verwenden
A potent phosphodiesterase III A (PDE3A) inhibitor (IC50=0.2uM) and inhibitor of adenosine uptake. Has antimitogeni, antithrombotic, vasodilatory and cardiotonic properties in vivo. Also affects lipid levels in vivo
Definition
ChEBI: A lactam that is 3,4-dihydroquinolin-2(1H)-one in which the hydrogen at position 6 is substiuted by a 4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy group.
Trademarks
Pletal (Otsuka);Reta.
Allgemeine Beschreibung
Cilostazol is a potent cyclic nucleotide phosphodiesterase inhibitor. It is mainly used as antiplatelet agent.
Biologische Aktivität
Potent phosphodiesterase III A (PDE3A) inhibitor (IC 50 = 0.2 μ M) and inhibitor of adenosine uptake. Has antimitogenic, antithrombotic, vasodilatory and cardiotonic properties in vivo . Also affects lipid levels in vivo .
Mechanism of action
Cilostazol exhibits greater selectivity than dipyridamole as an inhibitor of PDE3A. The drug does not affect the other PDEs (PDEs 1, 2, or 4). Cilostazol reversibly inhibit platelet aggregation induced by a number of stimuli, such as thrombin, ADP, collagen, or stress from exercise. Additionally, cilostazol inhibits adenosine uptake, leading to increased activity of adenosine at A1 and A2 receptors.
Clinical Use
Cilostazol, a quinolinone derivative, is a potent orally active antiplatelet drug approved for the treatment of intermittent claudication (a peripheral artery disease resulting from blockage of blood vessels in the limbs).
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Anagrelide: avoid concomitant use. Antibacterials: concentration increased by clarithromycin and erythromycin - consider reducing cilostazol dose.
Antifungals: concentration possibly increased by ketoconazole and itraconazole - consider reducing cilostazol dose.
Antivirals: concentration possibly increased by boceprevir, ritonavir and telaprevir - reduce cilostazol dose to 50 mg twice daily.
Calcium-channel blockers: concentration increased by diltiazem - consider reducing cilostazol dose.
Ulcer-healing drugs: concentration increased by omeprazole - consider reducing cilostazol dose.
Stoffwechsel
Cilostazol is rapidly absorbed after oral administration, particularly with a high-fat meal, which greatly increases its bioavailability to approximately 90%. It is extensively metabolized in the liver by various cytochromes. The most important cytochromes appear to be CYP3A4 and, to lesser extent, by CYP2C19, with an elimination half-life of approximately 11 to 13 hours. Among the various metabolites produced (11 metabolites are known), the two major metabolites are 3,4-dehydrocilostazol and 4′-trans-hydroxycliostazol. These two metabolites are pharmacologically active. Studies indicate that the concomitant administration of cilostazol with CYP3A inhibitors can greatly increase cilostazol blood concentrations, and a dose reduction may be required. Similar results are seen when CYP2C19 is inhibited, leading to decreased formation of 4-trans-hydroxycliostazol and significant increases in cilostazol and 3,4-dehydrocilostazol.
Lager
Store at RT
Einzelnachweise
1) Schror (2002) The pharmacology of cilostazol; Diabetes Obes. Metab., 4 S14

Cilostazol Upstream-Materialien And Downstream Produkte

Cilostazol Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

73963-72-1, Cilostazol Verwandte Suche:

Send Inquriy