Comparative Pharmacology
Head-to-head clinical analysis: ATMEKSI versus TADALAFIL.
Head-to-head clinical analysis: ATMEKSI versus TADALAFIL.
ATMEKSI vs TADALAFIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
ATMEKSI (atazanavir/cobicistat) is a fixed-dose combination of atazanavir, an HIV-1 protease inhibitor that inhibits viral protease, preventing cleavage of viral polyproteins and resulting in immature non-infectious virions, and cobicistat, a pharmacokinetic enhancer that inhibits CYP3A, increasing atazanavir exposure.
Inhibitor of phosphodiesterase type 5 (PDE5), enhancing cyclic guanosine monophosphate (cGMP)-mediated relaxation of smooth muscle in the corpus cavernosum and pulmonary vasculature.
1.5 mg/kg IV every 4 weeks
Erectile dysfunction: 10-20 mg orally as needed, 30-60 minutes before sexual activity; maximum 1 dose per day. Benign prostatic hyperplasia: 5 mg orally once daily. Pulmonary arterial hypertension: 40 mg orally once daily.
None Documented
None Documented
Clinical Note
moderateTadalafil + Torasemide
"Tadalafil may increase the antihypertensive activities of Torasemide."
Clinical Note
moderateTadalafil + Travoprost
"Tadalafil may increase the antihypertensive activities of Travoprost."
Clinical Note
moderateTadalafil + Unoprostone
"Tadalafil may increase the antihypertensive activities of Unoprostone."
Clinical Note
moderateTadalafil + Hydrochlorothiazide
"Tadalafil may increase the antihypertensive activities of Hydrochlorothiazide."
Terminal elimination half-life is 12 hours; renally impaired patients have prolonged half-life up to 24 hours.
Terminal elimination half-life is 17.5 hours in healthy subjects; supports once-daily dosing and prolonged effect (up to 36 hours for erectile function).
Primarily renal (80% unchanged) and biliary/fecal (15% as metabolites).
Primarily hepatic metabolism (CYP3A4); 36% excreted in urine (mainly metabolites), 61% in feces (mainly metabolites), <0.1% unchanged in urine.
Category C
Category A/B
PDE5 Inhibitor
PDE5 Inhibitor