Acetildenafil Sex Enhancement Powder 831217-01-7 Penile Erectile Dysfunction Treatment

CAS:831217-01-7 Acetildenafil It is suitable for the treatment of penile erectile dysfunction

Basic information editing

Reddenafil, also known as grand denafil, was originally developed by Pfizer (Pfizer) in the United States as a treatment for angina. The unexpected discovery that it was only moderately effective in treating angina in clinical trials but had a specific effect on impotence prompted manufacturers to declare it as an impotence drug. Food and Drug Administration (FDA) in the United States on March 27, 1997 officially approved the drug as the treatment of impotence drugs.

[English name] Acetildenafil [1]

5-[2-ethoxy-5 -[2-(4-ethyl-1-piperazinyl)acetyl]phenyl]-1,6-dihydro-1-methyl? - 3 - propyl - 7 h - pyrazolo [4, 3 - d] pyrimidin - 7 - one

[Molecular formula] C25H34N6O3 [molecular weight] 466.58 [2]

CAS 】 【 831217-01-7

[Content] 99%

[Product specifications] raw material, powder

[Packing] 1kg/20kg/50kg

Trait description editor

1. White crystalline powder, odorless, bitter taste, soluble in water and ethanol

2. The melting point of 75-78 ℃

3.102127-34-4/4-bromo-3-methoxyphenol

Derivatives of sildenafil citrate

Principle of Action Editing

The action principle of reddenafil is equivalent to sildenafil, with slightly less sildenafil added, and it has been called "undetectable sildenafil". Reddenafil is modified on the basis of sildenafil citrate. The action principle of reddenafil is equal to sildenafil citrate, and the added amount is slightly less than sildenafil citrate. Reddenafil was once known as "undetectable sildenafil". Reddenafil has been listed as the test object in China, and the approval document is the National Supplementary Test Method for Drug Control 2008016. [3]

pharmacokinetics

Reddenafil is absorbed rapidly after oral administration and has an absolute bioavailability of about 40%. Its pharmacokinetic parameters are proportional to the dose within the recommended dose range. Eliminate the liver metabolism (cytochrome P450 isoenzyme 3A4 pathway) and produce an active metabolite similar in nature to sildenafil. A potent inhibitor of cytochrome P450 isoenzyme 3A4 (CYP450 3A4) (e.g., erythromycin, ketoconazole, itraconazole) and a nonspecific inhibitor of cytochrome P450 (CYP450), such as cimetidine, in combination with sildenafil, may lead to elevated plasma levels of erydenafil. The elimination half-life of reddenafil and its metabolites is about 4 hours. The maximum plasma concentration (Cmax) was 127 ~ 560ng/ml in about 1 hour when 25 ~ 100mg was given in the fasting state. Reddenafil or its main metabolite, N-demethylmethyl metabolite (N-desmethyl), has a selectivity of about 50% for PDE5 and a protein binding rate of 96%. At the maximum plasma concentration of total erydenafil, Cmax of free erydenafil was 22ng/ml. After oral or intravenous administration, reddenafil is excreted mainly in the feces as metabolites (approximately 80% of the oral dose) and a small amount is excreted in the urine (approximately 13% of the oral dose).

Pharmacokinetics in a special population: Older adults: Sildenafil clearance was reduced in healthy elderly volunteers (≥65 years) and free blood concentrations were approximately 40% higher than in young healthy volunteers (18-45 years). Renal insufficiency in sildenafil citrate bottles: There was no pharmacokinetic change in volunteers with mild (creatinine clearance = 50-80 mL/min) and moderate (creatinine clearance = 30-49 mL/min) renal impairment with a single dose of sildenafil 50mg. In volunteers with severe renal impairment (creatinine clearance = ≤30 mL/min), clearance of sildenafil was reduced and area under the time-curve (AUC) and Cmax almost doubled compared to volunteers in the same age group without renal impairment.

Liver insufficiency: Sildenafil clearance was reduced in volunteers with cirrhosis (Child-Pugh grade A and grade B), and AUC and Cmax were increased by 84% and 47%, respectively, compared with volunteers in the same age group without liver damage. Thus, high plasma sildenafil levels are associated with age over 65, liver impairment, and severe renal impairment. A starting dose of 25mg is appropriate for these patients

Product application editor

For the treatment of erectile dysfunction (ED)