Sildenafil

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Sildenafil

DIN 00496545
100 mg
30 Tablets, Square container


Systematic name: 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)phenylsulfonyl]-4-methylpiperazine

Availability: In stock

$0.00
Pharmacokinetic data

Drug Class: Antihypertensive, Erectile Dysfunction Agent (Phosphodiesterase-5 (PDE5) inhibitor)                                               

Route: Oral

Effective Dose: Men, 50-100 mg

Effective Dose: Women, not recommended

Frequency: As required

Half-Life: 4 Hours

Excretion: Fecal, urine 

Side Effects

Acne: None

Fluid retention: None

Hypotension : Yes

Hepatotoxicity: Potential

Identifiers

CAS number : 139755-83-2 
PubChem CID: 5281023

ChemSpider ID: 56586

 

Chemical data

Formula: C22H30N6O4S
Mol. mass: 474.6

Melting point: 298-300°C

 

DESCRIPTION
Sildenafil, also known under the name of Viagra, is a phosphodiesterase type 5 inhibitor.
Phosphodiesterase type 5 is used in the treatment of erectile dysfunction (impotence). It
helps to produce and maintain a sufficient state of erection to take part in sexual activities by
increasing the inflow of blood inside the penis of a man sexually aroused at the time of taking
the medication. It should be taken only after sexual stimulation, yet it does not increase
sexual desire.
It is also used as a treatment for pulmonary hypertension.


COMPOSITION
Each Tablet contains:
Medicinal ingredients. Sildenafil 100 mg.
Non-medicinal ingredients. Microcrystalline cellulose, calcium carbonate, steric acid,
magnesium stearate.


CLINICAL PHARMACOLOGY
Sildenafil enhances the effect of Nitric oxide (NO) in the corpus cavernosum of the penis
binds to guanylate cyclase receptors, which results in increased levels of cGMP, leading to
smooth muscle relaxation (vasodilation) of the intimal cushions of the helicine arteries. This
smooth muscle relaxation leads to vasodilation and increases inflow of blood into the spongy
tissue of the penis, causing an erection.


INDICATIONS
Sildenafil is used to treat erectile dysfunction and pulmonary arterial hypertension.


CONTRAINDICATIONS
Sildenafil is contraindicated in patients taking nitric oxide, organic nitrites and nitrates or
drugs that contain nitrates, as there is a risk of life-threatening hypotension. Taking nitrates
in any form whatsoever (oral, sublingual, transdermal, inhalation), continuous treatment or as
needed, is absolutely contraindicated.


ADVERSE REACTIONS
Common side effects of Sildenafil include facial flushing, headaches, stomach pain, nasal
congestion, nausea, diarrhea, an inability to differentiate between the colors green and blue,
a loss of hearing, and ringing in the ears and dizziness.


MECHANISM OF ACTION
The physiologic mechanism of erection of the penis involves a release of nitric oxide (NO) in
the corpus cavernosum during sexual stimulation. NO then activates the enzyme guanylate
cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP),
allowing smooth muscle relaxation in the corpus cavernosum and inflow of blood.
Sildenafil enhances the effect of NO by inhibiting phosphodiesterase type 5 (PDE5), which is
responsible for degradation of cGMP in the corpus cavernosum. Sildenafil has no direct
relaxant effect on isolated human corpus cavernosum. When sexual stimulation causes local
release of NO, inhibition of PDE5 by sildenafil increases levels of cGMP in the corpus
cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus
cavernosum. Sildenafil, at recommended doses, has no effect in the absence of sexual
stimulation.


STORAGE INSTRUCTIONS
Store sildenafil at room temperature, between 15-30 degrees Celsius (59° to 86° F),
in a tightly closed, light-resistant container. Keep out of reach of children.

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