Vardenafil hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Vardenafil was the second agent to be marketed and had the advantage that its onset time was not
reduced by taking the medication on a full stomach . It is 30 times more potent
as an inhibitor of PDE5 (mean IC50, 3.9 nM) than sildenafil and 10 times more potent than tadalafil,
with a greater selectivity (>1,000 times) for human PDE5 than for human PDE2, PDE3, and PDE4
and moderate selectivity (>80 times) for PDE1. The PDE inhibitory selectivity
and both the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Vardenafil specifically
inhibited the hydrolysis of cGMP by PDE5, with an IC50 of 0.7 nM (sildenafil 6.6 nM). The IC50 of
vardenafil for PDE1 was 180 nM, for PDE6 11 nM, and for PDE2, PDE3 and PDE4 more than 1,000
nM.
Chemische Eigenschaften
White to Off-White Cyrstalline Solid
Verwenden
vardenafil hydrochloride is a selective phsphodiesterase type 5 (pde5) inhibitor that is used as a urological agent in the treatment of erectile dysfunction.
Allgemeine Beschreibung
Vardenafil, 4-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonyl-phenyl]-9-methyl-7-propyl-3,5,6,8-tetrazabicyclo[4.3.0]nona-3,7,9-trien-2-one(Levitra), was the second PDE5 introduced in the U.S. market.The metabolism of vardenafil is primarily by CYP3A4.As such, concomitant use of CYP3A4 inhibitors such as ritonavir,indinavir, ketoconazole, as well as moderate CYP3Ainhibitors such as erythromycin typically results in significantincreases of plasma levels of vardenafil.
Enzyminhibitor
Vardenafil also is rapidly absorbed and peaks in concentration (9.05 μg/mL after a 10-mg dose) after 0.9 hours, displaying a half-life of
4 to 5 hours. The absorption rate of both sildenafil and vardenafil are reduced when taken with a high-fat diet. The drug also is
metabolized by hepatic CYP3A4, and a potential for drug–drug interaction with inhibitors or enhancers of CYP3A4 exists. Biochemical
studies demonstrate a significant increase in selectivity of vardenafil over sildenafil for PDE5 versus PDE6. Whether this translates
into a significant improvement in side effects must await studies in a greater population of patients.
Vardenafil hydrochloride Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
