Absorption: rapid.
Protein binding: ~99%.
Metabolism: hepatic via CYP3A4 (major), CYP2C (minor); forms metabolites (active and inactive).
Half-life elimination: Terminal: ~5 hours.
Time to peak, plasma: 30 to 45 minutes (fasting); 1.12 to 1.25 hours (high-fat meal).
Excretion: Feces (~62%); urine (~21%).
禁忌症
Hypersensitivity to avanafil or any component of the formulation; coadministration with any form of organic nitrates or guanylate cyclase stimulators (eg, riociguat, vericiguat).
懷孕分類
哺乳分類
副作用
>10%: headache (1% to 12%). 1% to 10%: ECG abnormality (1% to 3%), flushing (3% to 10%), hypertension (1% to 2%), skin rash (1% to 2%), constipation (1% to 2%), dyspepsia (1% to 2%), nausea (1% to 2%), viral gastroenteritis (2%), influenza (1% to 2%), dizziness (1% to 2%), back pain (2% to 3%), bronchitis (1% to 2%), nasal congestion ((4%), nasopharyngitis (3% to 5%), paranasal sinus congestion (1% to 2%), sinusitis (1% to 2%), upper respiratory tract infection (1% to 3%).
劑量和給藥方法
Erectile dysfunction:
Oral: Initial: 100 mg (or 50 mg if concurrently receiving an alpha blocker) taken ~15 minutes prior to sexual activity; taken as one single dose and not more than once daily; dose may be increased to 200 mg ~15 minutes prior to sexual activity or decreased to 50 mg ~30 minutes prior to sexual activity using the lowest dose that provides benefit; maximum 200 mg daily.
小兒調整劑量
腎功能調整劑量
CrCl ≥ 30 mL/minute: no dosage adjustment necessary.
CrCl <30 mL/minute, ESRD requiring hemodialysis: Use is not recommended.
肝功能調整劑量
Mild to moderate hepatic impairment (Child-Pugh class A or B): no dosage adjustment necessary.
Severe hepatic impairment (Child-Pugh class C): Use is not recommended.