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Zenegra

Zenegra
Zenegra is indicated for the treatment of erectile dysfunction.

Brand: Sildenafil

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: May 2024
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Package Price Per pill Save Order
Zenegra 100 mg
270 pills - 100 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$192.99 $0.71 $301.56 Add to cart
180 pills - 100 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$140.67 $0.78 $189.03 Add to cart
120 pills - 100 mg
+ 4 free Viagra 100 mg, 3% discount for future orders
$105.83 $0.88 $113.97 Add to cart
90 pills - 100 mg $89.55 $1.00 $75.30 Add to cart
60 pills - 100 mg $71.95 $1.20 $37.95 Add to cart
30 pills - 100 mg $54.95 $1.83 No Add to cart
Zenegra 50 mg
120 pills - 50 mg $95.99 $0.80 $79.97 Add to cart
90 pills - 50 mg $79.97 $0.89 $52.00 Add to cart
60 pills - 50 mg $63.95 $1.07 $24.03 Add to cart
30 pills - 50 mg $43.99 $1.47 No Add to cart

Product description

Drug title

Zenegra (Sildenafil)

Pharmacological action

Selective inhibitor of cycloguanosine monophosphate (cGMP)-specific FDE5. FDE5, which is responsible for the breakdown of cGMF, is found not only in the corpora cavernosa of the penis, but also in the pulmonary vessels.


It restores impaired erectile function and provides a natural response to sexual arousal. Zenegra (Sildenafil) has no direct relaxing effect on the cavernous body, but actively enhances the relaxing effect of nitric oxide on this tissue. During sexual excitement, local release of NO under the influence of sildenafil leads to inhibition of FDE5 and increase of cGMP level in the cavernous body, resulting in relaxation of smooth muscles and increase of blood flow in the cavernous body.


As an inhibitor of FDE5, sildenafil increases cGMP content in smooth muscle cells of pulmonary vessels and causes their relaxation. In patients with pulmonary hypertension, taking sildenafil causes dilation of the pulmonary vessels and, to a lesser extent, of other vessels.


Zenegra (Sildenafil) is selective against FDE5 in vitro. Its activity against FDE5 exceeds activity against other known FDE isoenzymes: FDE6, involved in transmission of light signal in retina - by 10 times; FDE1 - 80 times; FDE2, FDE4, FDE7-FDE11 - more than 700 times. Sildenafil activity against FDE5 is more than 4000 times higher than its activity against FDE3, cAMP-specific FDE involved in heart contraction.


Zenegra (Sildenafil) may cause mild and transient color (blue/green) impairment. The inhibition of FDE6, which is involved in the transmission of light in the retina, is thought to be the presumed mechanism of color vision impairment. In vitro studies have shown that the effect of sildenafil on FDE6 is 10 times inferior to its activity against FDE5.


Pharmacokinetics

After oral administration sildenafil is rapidly absorbed. Absolute bioavailability is on average 40% (25-63%). After a single oral dose of 100 mg, Cmax is 18 ng/ml and is reached when taken on an empty stomach within 30-120 minutes. When sildenafil is taken in combination with fatty foods, the rate of absorption is reduced; Tmax is increased by 60 min and Cmax is reduced by an average of 29%. The Vd of sildenafil in equilibrium is on average 105 L. Sildenafil and its main circulating N-desmethyl metabolite are approximately 96% bound to plasma proteins. Protein binding is independent of the total concentration of sildenafil. Less than 0.0002% of the dose (188 ng on average) was detected in semen 90 min after sildenafil administration.


Sildenafil is metabolized primarily by the microsomal liver isoenzymes CYP3A4 (main pathway) and CYP2C9.


The main circulating metabolite, which is formed as a result of N-desmethylation of sildenafil, undergoes further metabolism. The metabolite is comparable with sildenafil in FDE selectivity, and its activity against FDE5 in vitro is about 50% of sildenafil activity. Plasma concentration of the metabolite is about 40% of that of sildenafil. N-desmethylmetabolite is further metabolized; its terminal T1/2 is about 4 hours.


The total clearance of sildenafil from the body is 41 l/h, and the T1/2 in the terminal phase is 3-5 hours. After oral administration sildenafil is excreted as metabolites mainly in the faeces (about 80% of the dose) and to a lesser extent in the urine (about 13% of the dose).

Contraindications to use

Hypersensitivity to sildenafil; coadministration with nitric oxide donators, organic nitrates or nitrites in any form; coadministration with guanylate cyclase stimulators (such as riociguat); coadministration with other drugs for treatment of erectile dysfunction; Liver function abnormalities (Child-Pugh class C); concomitant use of ritonavir; severe heart failure, unstable angina pectoris, stroke or myocardial infarction within the last 6 months, life-threatening arrhythmias, arterial hypertension (BP >170/100 mm Hg), or arterial hypertension in any form. St.) or arterial hypotension (BP <90/50 mm Hg). ); pulmonary venoocclusive disease; vision loss in one eye due to anterior nonarteritic ischemic optic neuropathy, hereditary degenerative retinal diseases (retinitis pigmentosa) severe renal insufficiency, when co-administered with cytochrome CYP3A4 isoenzyme inhibitors (erythromycin, saquinavir, ketoconazole, itraconazole); children and adolescents under 18 years of age.


With caution: Anatomical deformity of the penis (angulation, cavernous fibrosis or Peyronie's disease); diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia); diseases accompanied by bleeding; gastric and duodenal ulcer in the acute stage; heart failure, left ventricular outflow tract obstruction (aortic stenosis, hypertrophic obstructive cardiomyopathy), rare syndrome of multiple systemic atrophy, manifested by severe autonomic nervous system BP regulation disorder, hypovolemia; LAH - functional classes I or IV; anterior nonarteritic ischemic optic neuropathy in history; co-administration with moderate CYP3A4 isoenzyme inhibitors (incl. including erythromycin, saquinavir, clarithromycin, telithromycin and nefazodone) and α-adrenoblockers. Concomitant use with inducers of CYP3A4 isoenzyme.


Administration during pregnancy and lactation

During pregnancy, it is possible to use for treatment of pulmonary hypertension in cases when the expected benefits to a mother exceed the potential risk to a fetus or an infant. If it is necessary to use during lactation, the question of stopping breastfeeding should be decided.


Use in patients with liver dysfunction

It is contraindicated in patients with hepatic impairment (class C of the Child-Pugh classification).


Administration in patients with impaired renal function

Patients with severe renal insufficiency are contraindicated.


Administration in children

Contraindications for use in children and adolescents under 18 years of age.


Administration in elderly patients

Correction of dosage regimen is recommended for elderly patients (over 65 years of age).

Indications of active substances of the drug Zenegra (Sildenafil)

Treatment of erectile dysfunction characterized by the inability to achieve or maintain a penile erection sufficient for satisfactory intercourse.

Pulmonary hypertension.


Dosing regimen

Oral. Dosing regimen is set individually, depending on indications, patient's age, effectiveness and tolerability of sildenafil, presence of concomitant renal or hepatic dysfunction, dosage form used.