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Sildenafil (Viagra) is a PDE5 inhibitor that enhances blood flow in response to sexual arousal by relaxing smooth muscle in penile vasculature. Available as 25/50/100 mg tablets, taken 30–60 minutes before sexual activity. Onset 30–60 minutes; duration ~4 hours. Works best on empty stomach or light meal; food and grapefruit juice reduce efficacy. Requires baseline cardiac assessment.
| Dose | Who / When | Timing | Food Interaction |
|---|---|---|---|
| 25 mg | Elderly (>65), liver/renal impairment, first-time users | 30–60 min before activity | Empty stomach preferred |
| 50 mg | Standard starting dose for most men | 30–60 min before activity | Light meal OK; avoid high-fat meals |
| 100 mg | If 50 mg ineffective; optimal for many patients | 30–60 min before activity | Empty stomach for best absorption |
| Duration | ~4 hours (effective window) | Plan sexual activity within this window | Cardiovascular monitoring baseline + ongoing |
| Contraindication | Nitrate use (nitroglycerin, isosorbide), uncontrolled BP, recent MI/stroke, severe heart disease | ||
Sildenafil's mechanism targets the vascular system to improve erectile function through a well-understood biochemical pathway. It works by enhancing the body's natural responses to sexual stimulation.
Sildenafil achieves ~41% oral bioavailability with rapid absorption. Peak plasma concentration occurs 30–120 minutes post-dose (faster on empty stomach). The active N-desmethyl-sildenafil metabolite contributes ~50% of the pharmacological activity. CYP3A4 metabolism is critical—inhibitors can double or triple sildenafil levels, creating safety concerns.
| Bioavailability | ~41% (oral) |
| Tmax (time to peak) | 30–120 minutes (variable with food/stomach) |
| Peak concentration (50mg dose) | ~1 µg/mL |
| Elimination half-life | 3–5 hours |
| Volume of distribution | ~1.6 L/kg |
| Protein binding | ~96% — highly protein-bound |
| Metabolism | Hepatic: CYP3A4 (major, ~70%), CYP2C9 (minor, ~20%). Critical—CYP3A4 inhibitors dramatically increase levels. |
| Active metabolite | N-desmethyl-sildenafil (~50% activity of parent). Contributes to prolonged duration. |
| Excretion | Fecal (~80%), renal (~13%). Minimal unchanged parent in urine. |
| Food effect | High-fat meal delays Tmax by ~60 min and reduces Cmax by ~29%. Empty stomach optimal. |
Sildenafil is dosed as needed, 25–100mg taken 30–60 minutes before sexual activity. Maximum once daily. Standard starting dose is 50mg. Standard approach is flexible dosing based on response and tolerability, not daily maintenance dosing.
Sildenafil is one of the most-studied medications in history with robust evidence spanning erectile dysfunction, cardiovascular performance, and athletic enhancement. Over 25 years of clinical data support safety and efficacy.
Sildenafil's side effect profile is well-characterized from decades of use in millions of men. Most effects are mild, reversible, and dose-dependent. At standard doses (25–100mg), serious adverse events are rare.
Sildenafil is metabolized by CYP3A4 and CYP2C9. CYP3A4 inhibitors can substantially increase sildenafil levels (2–10x), creating safety risks. Nitrates are an absolute contraindication. Your physician MUST review all medications.
Book a consultation with a licensed physician to discuss whether sildenafil is appropriate for you.