Description
Pharmacological action
Selective inhibitor of cycloguanosine monophosphate (cGMP-specific). PDE5, responsible for the breakdown of cGMP, is found not only in the cavernous body of the penis, but also in the vessels of the lungs.
Restores impaired erectile function and provides a natural response to sexual arousal. Sildenafil does not have a direct relaxing effect on the cavernous body, but it actively enhances the relaxing effect of nitric oxide on this tissue. With sexual arousal, a local release of NO under the influence of sildenafil leads to inhibition of PDE5 and an increase in the level of cGMP in the cavernous body, as a result of which there is a relaxation of smooth muscles and increased blood flow in the cavernous body.
Being an inhibitor of PDE5, sildenafil increases the content of cGMP in smooth muscle cells of the pulmonary vessels and causes their relaxation. In patients with pulmonary hypertension, taking sildenafil leads to vasodilation of the lungs and, to a lesser extent, other vessels.
Sildenafil is selective for PDE5 in vitro. Its activity in relation to PDE5 is superior to activity against other known PDE isoenzymes: PDE6, which is involved in the transmission of the light signal in the retina of the eye – 10 times PDE1 – 80 times PDE2, PDE4, PDE7-PDE11 – more than 700 times. The activity of sildenafil in relation to PDE5 is more than 4000 times greater than its activity against PDE3, a cAMP-specific PDE involved in heart contraction.
Sildenafil may cause a mild and transient impairment of color discrimination (blue / green). The supposed mechanism of color vision impairment is considered to be the inhibition of PDE6, which is involved in the process of light transmission in the retina. In vitro studies have shown that the effect of sildenafil on PDE6 is 10 times less than its activity against PDE5.
Indications
Treatment of erectile dysfunction characterized by an inability to achieve or maintain an erection of the penis sufficient for satisfactory intercourse.
Pulmonary hypertension.
Contraindications
Simultaneous administration of donors of nitric oxide or nitrates in any form, hypersensitivity to sildenafil.
Recommendations for the use of
Treatment of erectile dysfunction: taken orally about 1 hour before the planned sexual activity. A single dose is 50 mg. Given the effectiveness and tolerability, the dose can be increased to 100 mg or reduced to 25 mg. The maximum single dose is 100 mg. The maximum frequency of use is 1 time / day. For elderly patients over the age of 65 and with concomitant impaired renal or hepatic function, the dose is 25 mg.
Pulmonary hypertension: by mouth, 20 mg 3 times / day with an interval of about 6-8 hours, regardless of food intake. The maximum daily dose is 60 mg. Dose adjustment is not required for patients with impaired renal function, but with poor tolerance, the dose is reduced to 20 mg 2 times / day.
Special instructions
Before taking sildenafil for the treatment of erectile dysfunctions, an examination of the cardiovascular system should be carried out.
Caution should be used in patients with anatomical deformation of the penis (e.g., angulation, cavernous fibrosis, or Peyronie’s disease) and people with diseases that predispose to the development of priapism (such as sickle cell anemia, multiple myeloma, or leukemia).
Should not be used in patients for whom sexual activity is undesirable.
Use with caution in patients with a tendency to bleeding, with peptic ulcer of the stomach and duodenum in the acute phase, with hereditary retinitis pigmentosa.
Sildenafil is not used in patients under the age of 18 years.
Influence on the ability to drive vehicles and control mechanisms
Sildenafil does not affect the ability to drive vehicles and control mechanisms.
Composition
Oral dispersible tablets, blue, diamond-shaped, with V50 engraving on one side and smooth on the other.
1 tab.
sildenafil citrate 70.225 mg,
which corresponds to the content of sildenafil 50 mg
Excipients: ludiflesh – 343.525 mg (mannitol ~ 302.3 mg, crospovidone ~ 17.18 mg, polyvinyl acetate ~ 16.32 mg, povidone ~ 1.46 mg sodium, krolo) microcrystalline – 25 mg, colloidal silicon dioxide – 3.75 mg, sucralose – 5 mg, indigo carmine (30-36%) – 2.5 mg, sweetener (Sweetness Enhancer) – 5 mg (maltodextrin ~ 3.565 mg, flavoring ~ 0.79 mg, dextrin ~ 0.395 mg residual water ~ 0.25 mg), natural flavor (5) (maltodextrin ~ 4.3 mg, propylene glycol ~ 0.185 mg, glycerol ~ 0.18 mg, flavor ~ 0.085 mg, residual water ~ 0.25 mg), lemon flavor (Lemon Flavor) – 5 mg (maltodextrin ~ 4 mg, flavor ~ 0.75 mg, -Tocopherol ~ 0.0003 mg, residual water ~ 0.25 mg), magnesium stearate – 10 mg.
Side effects
From the side of the central nervous system: headache, flushing, dizziness, insomnia are possible.
From the digestive system: dyspepsia, asthenia, diarrhea, abdominal pain, nausea are possible.
From the musculoskeletal system: arthralgia, myalgia, increased muscle tone.
From the respiratory system: nasal congestion, pharyngitis, rhinitis, sinusitis, respiratory tract infections, respiratory failure.
From the side of the organ of vision: a change in vision (a slight and transient mainly color change of objects, as well as increased perception of light and a violation of the clarity of vision), conjunctivitis.
Other: possible flu-like syndrome, the development of infectious diseases, symptoms of vasodilation, back pain, rash, urinary tract infection, impaired prostate function in rare cases – priapism.
active substance
Sildenafil
Terms of delivery from
pharmacies Prescription
Dosage Orma
tablets
