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Main Classes of Drugs
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
Phosphodiesterase inhibitorApremilastAvanafilCilostazolInamrinoneMilrinoneRoflumilastSildenafilTadalafilVardenafil
A review on pharmacological options for the treatment of erectile dysfunction: state of the art and new strategies
Published in Expert Opinion on Pharmacotherapy, 2023
Mattia Longoni, Alessandro Bertini, Nicolò Schifano, Emanuele Zaffuto, Paolo Maggio, Rossi Piercarlo, Sara Baldini, Giulio Carcano, Gabriele Antonini, Andrea Salonia, Francesco Montorsi, Federico Dehò, Paolo Capogrosso
Avanafil is one of the most recently developed PDE5I, approved for the treatment of ED in 2012 at dosages of 50, 100, or 200 mg [41]. Administered orally, this agent reaches the maximum plasma concentration 30–45 minutes within of oral administration, after a rapid absorption from the gastrointestinal tract [9] with a half-life of approximately 6 hours. Therefore, it is recommended to take avanafil on-demand about 30 minutes before intercourses. Avanafil produces a potent inhibition of PDE5 (IC50 5.2 mmol/L) with high enzyme-subtype selectivity compared to other PDE5Is, thus resulting in a lower rate of visual disturbances, myalgia, lower back pain, tachycardia, and flushing [42]. Even at the highest dose, this drug has shown great tolerability with mild adverse effects, making it a good choice for proper on-demand patient treatment [42]. Unfortunately, as data regarding the use of avanafil in patients with severe hepatic (Child-Pugh class C) or renal impairment (estimated creatinine clearance <30 mL/min) are lacking, it is not recommended in these particular populations [43].
Treatment of lower urinary tract symptoms/benign prostatic hyperplasia and erectile dysfunction
Published in The Aging Male, 2018
Aldo E. Calogero, Giovanni Burgio, Rosita A. Condorelli, Rossella Cannarella, Sandro La Vignera
In single-dose pharmacokinetic studies, avanafil had a time to maximum plasma drug concentration of 30–45 min and a half-life of approximately 3–5 h. Other PDE5i achieve time to maximum plasma drug concentration at approximately 60 (sildenafil and vardenafil) to 120 (tadalafil) minutes after dosing. Phase 2 studies that assessed penile tumescence and rigidity in response to visual stimulation in men with ED found that avanafil, 50, 100, and 200 mg, was statistically superior to placebo, with peak effects occurring 20–40 min after dosing, consistent with the drug’s pharmacokinetic profile. Flushing and headache were again the most common side effects, but usually transient and only mild to moderate. Furthermore, the actual rates of the most common side effects were particularly low (ranging from 1.6 to 3.7%). Fewer than 2% of patients discontinued therapy due to an adverse drug reaction in one study. Interestingly, avanafil had lower rates of hypotensive episodes (15%, 29%, and 12% for avanafil, sildenafil, and placebo, respectively) with monitored co-administration of nitroglycerin in males. This might suggest a possible role for use in patients with concurrent nitrate use, but further studies need to assess this effect. No drug accumulation was observed in multiple-dose pharmacokinetic studies that evaluated once- and twice-daily dosing with avanafil for up to 2 weeks [47]. Therefore, it is possible to suppose that, in relation to low half-life of avanafil, this drug could achieve a minor effect on physiopathological effects of LUTS/BPH compared with other PDE5Is, if not administered multiple times a day. To our knowledge, no studies so far have established a possible role of avanafil in specifically in LUTS/BPH – ED therapy.