An open-label, single-dose, randomized, parallel-group study of the safety and relative bioavailability of topical sildenafil cream vs oral sildenafil in healthy male adults
Abstract
Introduction: Oral phosphodiesterase-5 (PDE5) inhibitors are commonly prescribed for erectile dysfunction (ED), but have limiting side effects, particularly for men with serious cardiovascular disease. Topical sildenafil cream was developed based on the hypothesis that local genital application would result in less systemic exposure and fewer side effects compared to oral sildenafil citrate. The objective of this study was to describe the systemic pharmacokinetics (PK) and safety of topical sildenafil cream 3.6% in healthy men, applied to the penis with and without male condom use, compared to oral sildenafil.
Methods: Phase 1, open-label, single-dose, randomized, parallel-group design. Participants were randomized 1:1:1:1:1 to 36 mg of sildenafil in 1 g of cream or 71 mg of sildenafil in 2 g of cream self-applied to the penile skin with or without male condom use vs a 50 mg oral dose of sildenafil. Blood and orthostatic vital signs were taken prior to dosing and up to 32 hours post dosing. Safety was assessed by treatment emergent adverse events (TEAEs) and physical exam. Single dose PK parameters for plasma sildenafil and its active metabolite, N-desmethyl sildenafil were calculated.
Results: Sixty-two men received study medication. All TEAEs (n = 14) were mild. Half of the TEAEs (7/14, 50%), including headache (n = 4) and flushing (n = 2), resulted from oral dosing. The mean maximum plasma concentration (Cmax) of sildenafil after topical application (all 4 dosing groups)…
How strong is the evidence?
Evidence Hub reads this as a randomized trial, done in people. Its evidence level is 3 of 5 (Moderate · trial / cohort / secondary analysis). Trials without a large randomized design, cohorts and secondary analyses give moderate evidence. Reported size: 14 participants or records.
Read the paper
Related studies
- Drug repositioning: a brief overview
- Cyclic nucleotide phosphodiesterases in Drosophila melanogaster
- Time-resolved in silico modeling of fine-tuned cAMP signaling in platelets: feedback loops, titrated phosphorylations and pharmacological modulation
- Current View on Green Tea Catechins Formulations, Their Interactions with Selected Drugs, and Prospective Applications for Various Health Conditions
- In silico Structure-based Identification of Novel Acetylcholinesterase Inhibitors Against Alzheimer’s Disease
- Development and In Vitro Evaluation of Controlled Release Viagra® Containing Poloxamer-188 Using Gastroplus™ PBPK Modeling Software for In Vivo Predictions and Pharmacokinetic Assessments
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.