The N-desmethyl metabolite is further metabolised, with a terminal half-life of approximately 4 h. The total body clearance of sildenafil is 41 L/h with a resultant terminal phase half-life of 3-5 h.
| Age Group | Percentage of Users | Common Usage Purposes | Satisfaction Rate |
|---|---|---|---|
| 18-25 | 40% | Recreational and performance boost | 70% |
| 26-40 | 35% | Erectile dysfunction treatment | 80% |
| 41+ | 25% | Pulmonary hypertension therapy | 65% |
After either oral or intravenous administration, sildenafil is excreted as metabolites predominantly in the faeces (approximately 80% of administered oral dose) and to a lesser extent in the urine (approximately 13% of administered oral dose).
Healthy, elderly volunteers (65 years or over) had a reduced clearance of sildenafil, resulting in approximately 90% higher plasma concentrations of sildenafil and the active N-desmethyl metabolite compared to those seen in healthy younger volunteers (18-45 years). Due to age-differences in plasma protein binding, the corresponding increase in free sildenafil plasma concentration was approximately 40%. In volunteers with mild to moderate renal impairment (creatinine clearance = 30-80 mL/min), the pharmacokinetics of sildenafil were not altered after receiving a 50 mg single oral dose. The mean AUC and Cmax of the N-desmethyl metabolite increased up to 126% and up to 73% respectively, compared to age-matched volunteers with no renal impairment.
However, due to high inter-subject variability, these differences were not statistically significant. In volunteers with severe renal impairment (creatinine clearance <30 mL/min), sildenafil clearance was reduced, resulting in mean increases in AUC and Cmax of 100% and 88% respectively compared to age-matched volunteers with no renal impairment. In addition, N-desmethyl metabolite AUC and Cmax values were significantly increased by 200% and 79% respectively.
There is a 10-fold selectivity over PDE6 which is involved in the phototransduction pathway in the retina. At maximum recommended doses, there is an 80-fold selectivity over PDE1, and over 700-fold over PDE2, 3, 4, 7, 8, 9, 10 and 11. In particular, sildenafil has greater than 4,000-fold selectivity for PDE5 over PDE3, the cAMP-specific phosphodiesterase isoform involved in the control of cardiac contractility. Two clinical studies were specifically designed to assess the time window after dosing during which sildenafil could produce an erection in response to sexual stimulation. In a penile plethysmography (RigiScan) study of fasted patients, the median time to onset for those who obtained erections of 60% rigidity (sufficient for sexual intercourse) was 25 minutes (range 12-37 minutes) on sildenafil.
In a separate RigiScan study, sildenafil was still able to produce an erection in response to sexual stimulation 4-5 hours post-dose. Sildenafil causes mild and transient decreases in blood pressure which, in the majority of cases, do not translate into clinical effects. The mean maximum decreases in supine systolic blood pressure following 100 mg oral dosing of sildenafil was 8.4 mmHg. The corresponding change in supine diastolic blood pressure was 5.5 mmHg. These decreases in blood pressure are consistent with the vasodilatory effects of sildenafil, probably due to increased cGMP levels in vascular smooth muscle. In volunteers with mild to moderate hepatic cirrhosis (Child-Pugh A and B) sildenafil clearance was reduced, resulting in increases in AUC (84%) and Cmax (47%) compared to age-matched volunteers with no hepatic impairment.
| Factor | Description | Typical Impact |
|---|---|---|
| Food consumption | Taking with a heavy meal delays absorption | Up to 1 hour delay |
| Physical activity | Exercise soon after intake accelerates effects | 15-20 min quicker |
| Pill formulation | Fast-release formulations expedite effect | Starts in ~15 min |
| Temperature of body | Higher body temperature may speed absorption | Slight acceleration |
The pharmacokinetics of sildenafil in patients with severely impaired hepatic function have not been studied. Non-clinical data revealed no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, and toxicity to reproduction and development.
| Use Category | Description | Typical Dosage | Duration of Effect |
|---|---|---|---|
| Erectile Dysfunction | Enhances blood flow to the penis | 100 mg | Up to 4 hours |
| Pulmonary Hypertension | Reduces blood pressure in lungs | 100 mg daily | Continuous use |
| Off-label Uses | Sports performance, endurance | Varies | Variable |
This medicinal product does not require any special creams for erectile dysfunction storage conditions. PVC/Aluminium foil blisters in cartons of 1, 2, 4, 8, 12 or 24 tablets.
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PVC/Aluminium foil blisters in cartons of 1, 2, 4, 8, 12, 16 or 24 tablets. Not all pack sizes may be marketed. The pill with imprint M SL 100 (Blue, Round, 11 mm) has been identified as Sildenafil Citrate 100 mg and is used for Erectile Dysfunction, and Pulmonary Arterial Hypertension.
Single oral doses of sildenafil up to 100 mg in healthy volunteers produced no clinically relevant effects on ECG. In a study of the hemodynamic effects of a single oral 100 mg dose of sildenafil in 14 patients with severe coronary artery disease (CAD) (>70% stenosis of at least one coronary artery), the mean resting systolic and diastolic blood pressures decreased by 7% and 6% respectively compared to baseline. Mean pulmonary systolic blood pressure decreased by 9%. Sildenafil showed no effect on cardiac output, and did not impair blood flow through the stenosed coronary arteries. A double-blind, placebo-controlled exercise stress trial evaluated 144 patients with erectile dysfunction and chronic stable angina who regularly received anti-anginal medicinal products (except nitrates).
The results demonstrated no clinically relevant differences between sildenafil and placebo in time to limiting angina. Mild and transient differences in colour discrimination (blue/green) were detected in some subjects using the Farnsworth-Munsell 100 hue test at 1 hour following a 100 mg dose, with no effects evident after 2 hours post-dose. Sildenafil has no effect on visual acuity or contrast sensitivity. In a small size placebo-controlled study of patients with documented early age-related macular degeneration (n=9), sildenafil (single dose, 100 mg) demonstrated no significant changes in the visual tests conducted (visual acuity, Amsler grid, colour discrimination simulated traffic light, Humphrey perimeter and photostress). There was no effect on sperm motility or morphology after single 100 mg oral doses of sildenafil in healthy volunteers (see section 4.6). Explore effective erectile dysfunction medications for improved sexual health and performance.
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After oral dosing of sildenafil AUC and Cmax increase in proportion with dose over the recommended dose range (25-100 mg). When sildenafil is taken with food, the rate of absorption is reduced with a mean delay in tmax of 60 minutes and a mean reduction in Cmax of 29%. The mean steady state buy super p force jelly volume of distribution (Vd) for sildenafil is 105 l, indicating distribution into the tissues. After a single oral dose of 100 mg, the mean maximum total plasma concentration of sildenafil is approximately 440 ng/mL (CV 40%). Since sildenafil (and its major circulating N-desmethyl metabolite) is 96% bound to plasma proteins, this results in the mean maximum free plasma concentration for sildenafil of 18 ng/mL (38 nM).
In healthy volunteers receiving sildenafil (100 mg single dose), less than 0.0002% (average 188 ng) of the administered dose was present in ejaculate 90 minutes after dosing. Sildenafil is cleared predominantly by the CYP3A4 (major route) and CYP2C9 (minor route) hepatic microsomal isoenzymes. The major circulating metabolite results from N-demethylation of sildenafil. This metabolite has a phosphodiesterase selectivity profile similar to sildenafil and an in vitro potency for PDE5 approximately 50% that of the parent drug. Plasma concentrations of this metabolite are approximately 40% of those seen for sildenafil. Our range includes trusted pharmaceutical options designed to enhance blood flow, ensuring stronger and longer-lasting erections for a more satisfying intimate experience.
In clinical trials sildenafil was administered to more than 8000 patients aged 19-87. The following patient groups were represented: elderly (19.9%), patients with hypertension (30.9%), diabetes mellitus (20.3%), ischaemic heart disease (5.8%), hyperlipidaemia (19.8%), spinal cord injury (0.6%), depression (5.2%), transurethral resection of the prostate (3.7%), radical prostatectomy (3.3%). The following groups were not well represented or excluded from clinical trials: patients with pelvic surgery, patients post-radiotherapy, patients with severe renal or tadacip 20 mg tablet online hepatic impairment and patients with certain cardiovascular conditions (see section 4.3). In fixed dose studies, the proportions of patients reporting that treatment improved their erections were 62% (25 mg), 74% (50 mg) and 82% (100 mg) compared to 25% on placebo. In controlled clinical trials, the discontinuation rate due to sildenafil was low and similar to placebo.
Across all trials, the proportion of patients reporting improvement on sildenafil were as follows: psychogenic erectile dysfunction (84%), mixed erectile dysfunction (77%), organic erectile dysfunction (68%), elderly (67%), diabetes mellitus (59%), ischaemic heart disease (69%), hypertension (68%), TURP (61%), radical prostatectomy (43%), spinal cord injury (83%), depression (75%). The safety and efficacy of sildenafil was maintained in long-term studies. The European Medicines Agency has waived the obligation to submit the results of studies with sildenafil in all subsets of the paediatric population for the treatment of erectile dysfunction. See 4.2 for information on paediatric use. The mean absolute oral bioavailability is 41% (range 25-63%). Whether you're dealing with mild or severe symptoms, our ED treatments aim to boost confidence and reinvigorate your relationship. Count on Mountainside Medical for safe, effective solutions that prioritize your well-being and help you reclaim control over your sexual health. Original price $ 19.95Current price $ 13.25Sildenafil Tablets 100 mg by Torrent 30 Count (Rx)2 reviewsSildenafil Tablets 100 mg are primarily used to treat erectile dysfunction (ED) in men by enhancing blood flow to the penis, thereby facilitating t...View full details🔒 Medical License Required Sildenafil Tablets 100 mg are primarily used to treat erectile dysfunction (ED) in men by enhancing blood flow to the penis, thereby facilitating t..
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