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Product Name: Sildenafil

Generics: Sildenafil

Common Brand Names: Viagra

Pharmaceutical Category: Men's Health / Women's Health

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Product	Pharmacy / Drugstore	Brand / Generic	Forms of Payment	Shipping
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There is an additional general information about this medication active ingredient sildenafil:

Pharmacological action

Sildenafil is a medication for the treatment of erectile dysfunction. This drug restores impaired erectile function and provides a natural response to sexual stimulation. Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5) which is responsible for the breakdown of cGMP in the cavernous body. This medicine has no direct relaxing effect on corpus cavernosum, but enhances the relaxing effect of active nitric oxide in this tissue. When sexually aroused the local release of NO under the influence of sildenafil leads to the inhibition of PDE-5 and increase of cGMP in the cavernous body, resulting in relaxation of smooth muscles and increasing blood flow to the cavernous body. Sildenafil may cause mild and transient violation of distinguishing colors (blue / green). Alleged violations of the mechanism of color vision is PDE6 oppression, which is involved in the transmission of light in the retina.

Pharmacokinetics

After oral administration Sildenafil is rapidly absorbed. The absolute bioavailability averages 40% (25-63%). After a single oral dose in 100 mg C_max is 18 ng / ml and is reached in the fasting during 30-120 min. When taking sildenafil in combination with fatty food the intake rate decreases; T_max increased by 60 min and C_max decreased by an average of 29%. V_d of sildenafil at steady state an average is 105 liters. Sildenafil and its major circulating N-desmethyl metabolite approximately 96% bound to plasma proteins. Protein binding does not depend on the total concentration of sildenafil. Less than 0.0002% of the dose (mean 188 ng) were detected in semen up to 90 min after administration of sildenafil.
Sildenafil is metabolized primarily by the action of microsomal liver isoenzymes CYP3A4 (major route) and CYP2C9.
The total clearance of sildenafil from the body is equal to 41 l / h, T_1/2 in the terminal phase is 3-5 hours. After oral administration, sildenafil is displayed in the form of metabolites mainly in the faeces (approximately 80% of dose) and to a lesser extent in the urine (approximately 13% of dose).
In elderly patients (aged 65 and older) sildenafil clearance is reduced, and the concentration of free active substance in the plasma by approximately 40% higher than its concentration in young (18-45 years) patients.
In renal insufficiency, mild (creatinine clearance 50-80 ml / min) and medium (CC 30-49 ml / min) the severity of the pharmacokinetic parameters of sildenafil after oral administration of a single dose (50 mg) did not change. In renal failure, severe (CC < 30 mL / min), sildenafil clearance is reduced, resulting in approximately twofold increase in AUC (100%) and C_max (88%) compared with those with normal indices of renal function in patients of the same age group.
In patients with liver cirrhosis (class A and B in Child-Pugh), sildenafil clearance is reduced, which leads to an increase in AUC (84%) and Cmax (47%) compared with those with normal parameters of liver function in patients of the same age group.

Why is Sildenafil prescribed?

Treatment of erectile dysfunction, characterized by an inability to achieve or maintain penile erection sufficient for satisfactory sexual intercourse.

Dosage and administration

Sildenafil is taken orally for about an hour before the planned sexual activity. A single dose is 50 mg. Given the efficacy and tolerability the dose may be increased to 100 mg or decreased to 25 mg. The maximum single dose is 100 mg. The maximum frequency of use is 1 time / day.
For elderly patients aged 65 years and with concomitant renal impairment or hepatic the dose is 25 mg.

Sildenafil side effects, adverse reactions

Central nervous system: possible headache, flushing, dizziness, insomnia.
Digestive system: dyspepsia, asthenia, diarrhea, abdominal pain, nausea.
Musculoskeletal system: arthralgia, myalgia, increased muscle tone.
Respiratory system: nasal congestion, pharyngitis, rhinitis, sinusitis, respiratory tract infections, respiratory failure.
Vision: vision changes (mild and transient, mostly to change the color of objects, as well as increased perception of light and blurred vision), conjunctivitis.
Other: there may be flu-like symptoms, development of infectious disease, symptoms of vasodilation, back pain, rash, urinary tract infection, dysfunction of the prostate gland; in single cases - priapism.

Sildenafil contraindications

The simultaneous administration of donor of nitric oxide or nitrates in any form, hypersensitivity to sildenafil.

Special instructions

Before taking Sildenafil it should be undertake a survey of the cardiovascular system.
This medication should be used with caution in patients with anatomical deformation of the penis (such as angulation, cavernous fibrosis or Peyronie's disease) and people with medical conditions that predispose to priapism (such as sickle cell anemia, multiple myeloma, or leukemia).
It should not be used in patients for whom sexual activity is contraindicated.
With caution ude Sildenafil in patients with a tendency to bleeding, gastric ulcer and duodenal ulcer in acute phase, with hereditary retinitis pigmentosa.
In experimental studies have not been found any evidence of carcinogenicity of sildenafil. Bacterial and in vivo mutagenicity tests for the study were negative.
This drug is not used in patients under the age of 18 years.
Sildenafil has no effect on the ability to drive and control mechanisms.

Sildenafil drug interactions

When this drug applied simultaneously with:
- inhibitors of CYP3A4 (erythromycin, cimetidine) decreased clearance of sildenafil, increasing the concentration of Sildenafil in plasma.
- indinavir, saquinavir, ritonavir increases the plasma C_max and AUC of sildenafil, which is due to inhibition of CYP3A4 isoenzyme under the influence of indinavir, saquinavir, ritonavir.
One might expect that stronger inhibitors of isoenzyme CYP3A4, such as ketoconazole or itraconazole would increase the concentration of this medication in the blood plasma.
While the use with nitrates the hypotensive effect of nitrates increases.
There was described a case of rhabdomyolysis symptoms after a single oral dose of sildenafil in patients receiving simvastatin.

Sildenafil in case of emergency / overdose

Symptoms: in studies in healthy volunteers in single dose of 800 mg of sildenafil was observed increased severity of side effects.
Treatment is symptomatic. Dialysis is ineffective because of the high degree of binding of sildenafil and its metabolite to plasma proteins.

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