Metabolized with the participation of the isoenzyme CYP3A4. The main circulating metabolite is methylcatechol glucuronide, which is 13,000 times less active against PDE5 than sildenafil, therefore it is unlikely that this metabolite is clinically significant.
In healthy individuals, the average clearance of sildenafil when taken orally is 2.5 l / h, and the average T 1/2 is 17.5 hours.sildenafil is excreted mainly in the form of inactive metabolites, mainly with feces (about 61%) and, to a lesser extent, with urine (about 36%).
Sildenafil Description
In patients with mild renal insufficiency (CC from 51 to 80 ml / min) or moderate (CC from 31 to 50 ml / min) AUC is higher than in healthy individuals. Film-coated tablets, yellow, almond-shaped, with the designation "C 20" on one side.
Project sildenafil without a doctor's prescription
Excipients: lactose monohydrate - 245.195 mg, hyprolose (hydroxypropyl cellulose) - 8.05 mg, croscarmellose sodium - 22.4 mg, microcrystalline cellulose - 52.5 mg, magnesium stearate - 0.875 mg, sodium lauryl sulfate - 0.98 mg.
The composition of the film shell
Opadry II yellow (lactose monohydrate, hypromellose, titanium dioxide, triacetin, iron oxide yellow dye) - 14 mg. 1 PC. - blisters (1) - cardboard packs. 2 pcs. - blisters (1) - cardboard packs. 2 pcs. - blisters (2) - cardboard packs. 2 pcs. - blisters (4) - cardboard packs. Middle-aged men are advised to take 20 mg at least 16 minutes before expected sexual activity, regardless of food intake. Patients can attempt intercourse at any time within 36 hours after administration in order to establish the optimal response time to taking tadalafil. The maximum frequency of admission is 1 time / day. Tadalafil is mainly metabolized with the participation of the CYP3A4 enzyme. The selective CYP3A4 inhibitor ketoconazole increases AUC by 107%, and rifampicin reduces it by 88%.
Tadalafil enhances the hypotensive effect of nitrates. This is due to the additive effect of nitrates and tadalafil on the metabolism of nitric oxide and cGMP. Therefore, the use of tadalafil in patients receiving nitrates is contraindicated.
Possibly: back pain, myalgia, nasal congestion, flushing. Rarely: swelling of the eyelids, eye pain, conjunctival hyperemia, dizziness.
Technologies sildenafil 50mg tablets
Simultaneous administration of drugs containing any organic nitrates; children and adolescents up to 18 years old; hypersensitivity to tadalafil. With extreme caution and only if absolutely necessary, it is possible to use tadalfil in patients with severe renal insufficiency (CC≤30 ml / min).
With the simultaneous administration of an antacid (magnesium hydroxide / aluminum hydroxide) and tadalafil, the rate of absorption of the latter decreases without changing its AUC.
During treatment with tadalfil, patients with moderate renal insufficiency (CC from 31 to 50 ml / min) more often had back pain compared with patients with mild renal insufficiency (CC from 51 to 80 ml / min) or healthy volunteers ... In patients with CC ≤50 ml / min, tadalfil should be used with caution.
With extreme caution and only if absolutely necessary, it is possible to use tadalafil in patients with severe renal insufficiency (CC≤30 ml / min) and severe hepatic insufficiency.
