|
![]() |
|
|
Viagra: profile and news
SEEK a Liitle Relationship Help From Viagra 17 May 2006 Viagra tops list of fake drugs 17 May 2006 Viagra- Unsurprisingly the Champ 17 May 2006 Beware! Fake sex drugs on sale, warns company 17 May 2006 Mark Ritson on branding: Pfizer trial reveals brand malady 17 May 2006 One man, 353 commercials, no remote 17 May 2006 Viagra and the wine blogosphere May 15, 2006 Viagra creating a dizzy spell in the world of male impotency May 14, 2006 Fake Viagra maker given 10-year prison term May 9, 2006 An effort to entice cures for diseases May 15, 2006 Enrich Life with Erectile Dysfunction Drug's Viagra and Cialis May 11, 2006 What can Viagra do for you? May 10, 2006 Fake Chinese Viagra maker sentenced to 10-year prison term May 10, 2006 Fake Viagra May 9, 2006 Back to the First Time You ever heard of Viagra May 12, 2006 Proof of Viagra Use Rebuts Wife's Claim of Abandonment May 13, 2006 Brazilian court eases Viagra's firm grip on market May 11, 2006 Levitra, Viagra launch new ad campaigns May 2, 2006 Younger Men Using Viagra Without Prescription, Survey Reveals May 1, 2006 Levitra, Viagra Launch New Ad Campaigns May 2, 2006 Potential new usage for Viagra May 1, 2006 Viagra plus recreational drugs equals risky sexual behaviour May 1, 2006 Study finds young men having erectile dysfunction ... May 1, 2006 Viagra-firm lobbyist to stand for Labour in Blaenau Gwent May 8, 2006 Viagra is sexy again May 8, 2006 Viagra college May 3, 2006 Pfizer Unveils Next Generation Viagra Spot May 4, 2006 Spark your sexual life with Viagra May 4, 2006 SATISFACTION in the Bedroom with Viagra May 8, 2006 Ayoon Wa Azan(Viagra or PhD?) May 1, 2006 ANGER IS RISING OVER HONCHO'S VIAGRA QUIP May 3, 2006 Viagra may help children with fatal lung disorder May 8, 2006 Poor performance not curable with Viagra May 3, 2006 Pfizer Faces Viagra Suits Over Users' Vision Loss Apr 19, 2006 Cinematic Viagra struggles to prop up flagging plot Apr 26, 2006 Viagra peddlers can expect stiff sentence Apr 19, 2006 Ensure Quality Sexual Health with Viagra Apr 19, 2006 Viagra Goes to Court – l Apr 19, 2006 Some visually impaired men shouldn't take Viagra, panel says Apr 28, 2006 Viagra Goes to Court – ll Apr 19, 2006 The Blessed Viagra! Apr 26, 2006 Generic Viagra suiting a common man’s purse Apr 26, 2006 General Motors Spending $17 Million a Year on Viagra and Other " ... Apr 17, 2006 GM Spends $17 Million Per Year on Viagra Apr 18, 2006 Viagra to go legit in Pakistan soon Apr 28, 2006 YourLife: How Viagra is Helping to Keep Me Alive ; HEALTH: One ... Apr 17, 2006 GM Spends $17 Million On Employee Viagra Apr 18, 2006 Walking In The Search Engines’ Shoes May 15, 2006 Sack-happy Canucks prop up Viagra Apr 22, 2006 Other information Indication For the treatment of erectile dysfunction Pharmacology Sildenafil is used to treat male erectile dysfunction (impotence) and pulmonary arterial hypertension (PAH). Part of the physiological process of erection involves the release of nitric oxide (NO) in the corpus cavernosum. This then activates the enzyme guanylate cyclase which results in increased levels of cyclic guanosine monophosphate (cGMP), leading to smooth muscle relaxation in the corpus cavernosum, resulting in increased inflow of blood and an erection. Sildenafil is a potent and selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum. This means that, with Sildenafil on board, normal sexual stimulation leads to increased levels of cGMP in the corpus cavernosum which leads to better erections. Without sexual stimulation and no activation of the NO/cGMP system, Sildenafil should not cause an erection. Mechanism Of Action Sildenafil inhibits the cGMP specific phosphodiesterase type 5 (PDE5) which is responsible for degradation of cGMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cGMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The inhibition of phosphodiesterase type 5 (PDE5) by Sildenafil enhances erectile function by increasing the amount of cGMP. Drug Category Vasodilator Agents; Phosphodiesterase Inhibitors; ATC:G04BE03 Brand Names/Synonyms Sildenafil; Sildenafil Viagra; Viagra Dosage Forms TABLET Absorption ~40% Interactions -->Interactions for Sildenafil: Effects of Other Drugs on Sildenafil Citrate In Vitro Studies: Sildenafil metabolism is principally mediated by the cytochrome P450 (CYP) isoforms 3A4 (major route) and 2C9 (minor route). Therefore, inhibitors of these isoenzymes may reduce sildenafil clearance. In Vivo Studies: Cimetidine (800 mg), a nonspecific CYP inhibitor, caused a 56% increase in plasma sildenafil concentrations when coadministered with sildenafil citrate (50 mg) to healthy volunteers. When a single 100 mg dose of sildenafil citrate was administered with erythromycin, a specific CYP3A4 inhibitor, at steady state (500 mg bid for 5 days), there was a 182% increase in sildenafil systemic exposure (AUC). In addition, coadministration of the HIV protease inhibitor saquinavir, also a CYP3A4 inhibitor, at steady state (1200 mg tid) with sildenafil citrate (100 mg single dose) resulted in a 140% increase in sildenafil Cmax and a 210% increase in sildenafil AUC. Sildenafil citrate had no effect on saquinavir pharmacokinetics. Stronger CYP3A4 inhibitors such as ketoconazole or itraconazole would be expected to have still greater effects, and population data from patients in clinical trials did indicate a reduction in sildenafil clearance when it was coadministered with CYP3A4 inhibitors (such as ketoconazole, erythromycin, or cimetidine). Coadministration with the HIV protease inhibitor ritonavir, which is a highly potent P450 inhibitor, at steady state (400 mg bid) with sildenafil citrate (100 mg single dose) resulted in a 300% (4-fold) increase in sildenafil Cmax and a 1000% (11-fold) increase in sildenafil plasma AUC. At 24 hours the plasma levels of sildenafil were still approximately 200 ng/mL, compared to approximately 5 ng/mL when sildenafil was dosed alone. This is consistent with ritonavir's marked effects on a broad range of P450 substrates. Sildenafil citrate had no effect on ritonavir pharmacokinetics. It can be expected that concomitant administration of CYP3A4 inducers, such as rifampin, will decrease plasma levels of sildenafil. Single doses of antacid (magnesium hydroxide/aluminum hydroxide) did not affect the bioavailability of sildenafil citrate. Pharmacokinetic data from patients in clinical trials showed no effect on sildenafil pharmacokinetics of CYP2C9 inhibitors (such as tolbutamide, warfarin), CYP2D6 inhibitors (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazide and related diuretics, ACE inhibitors, and calcium channel blockers. The AUC of the active metabolite, N-desmethyl sildenafil, was increased 62% by loop and potassium-sparing diuretics and 102% by nonspecific beta-blockers. These effects on the metabolite are not expected to be of clinical consequence. Effects of Sildenafil Citrate on Other Drugs In Vitro Studies: Sildenafil is a weak inhibitor of the cytochrome P450 isoforms 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 (IC50 >150 mM). Given sildenafil peak plasma concentrations of approximately 1 mcM after recommended doses, it is unlikely that sildenafil citrate will alter the clearance of substrates of these isoenzymes. In Vivo Studies: When sildenafil citrate 100 mg oral was coadministered with amlodipine, 5 mg or 10 mg oral, to hypertensive patients, the mean additional reduction on supine blood pressure was 8 mmHg systolic and 7 mmHg diastolic. No significant interactions were shown with tolbutamide (250 mg) or warfarin (40 mg), both of which are metabolized by CYP2C9. Sildenafil citrate (50 mg) did not potentiate the increase in bleeding time caused by aspirin (150 mg). Sildenafil citrate (50 mg) did not potentiate the hypotensive effect of alcohol in healthy volunteers with mean maximum blood alcohol levels of 0.08%. Sildenafil (100 mg) did not affect the steady state pharmacokinetics of the HIV protease inhibitors, saquinavir and ritonavir, both of which are CYP3A4 substrates. Chemical IUPAC Name 3-[2-ethoxy-5-(4-methylpiperazin-1-yl)sulfonyl-phenyl]-7-methyl-9-propyl-2,4,7,8-tetrazabicyclo[4.3.0]nona-3,8,10-trien-5-one Chemical Formula C22H30N6O4S Half Life 4 hours Drug Type Approved Drug # Accession No APRD00556 CAS Registry Number 139755-83-2 |
|
Home | About | Cancers | Treatment | Medications Copyright onconews.org 2005. All Rights Reserved. |