Homosildenafil (also known as methyl-sildenafil) is a synthetic

drug A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...

which acts as a phosphodiesterase inhibitor. It is an

analog Analog or analogue may refer to: Computing and electronics * Analog signal, in which information is encoded in a continuous variable ** Analog device, an apparatus that operates on analog signals *** Analog electronics, circuits which use analo ...

sildenafil Sildenafil, sold under the brand name Viagra, among others, is a medication used to treat erectile dysfunction and pulmonary arterial hypertension. It is unclear if it is effective for treating sexual dysfunction in women. It is taken by ...

and vardenafil. Homosildenafil was first identified as an adulterant in sex enhancement products in 2003 and was more recently detected in dietary supplements. Homosildenafil has 35% the PDE5 inhibition activity of sildenafil itself with similar selectivity. Sildenafil is mainly metabolized by the microsomal isozymes

CYP3A4 Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from t ...

with secondary metabolism by CYP2C9. The major active metabolite is ''N''-desmethylsildenafil. The plasma level of the equivalent homosildenafil metabolite reaches 40% of sildenafil's bioavailability. The ''N''-desmethyl metabolite is further metabolized, with a half-life of 4 hours.

References

{{Phosphodiesterase inhibitors Designer drugs PDE5 inhibitors Propyl compounds Ethoxy compounds Piperazines Sulfonamides

See also

References