Sealex Sildenafil pills 50mg, 4pcs

Composition

Tablets 50 mg

Active ingredient:

sildenafil citrate – 70.2 mg (in terms of sildenafil-50.0 mg).

Auxiliary substances:

corn starch — 156.0 mg,

microcrystalline cellulose-74.0 mg,

magnesium stearate-5.0 mg,

talc-5.0 mg, colloidal silicon dioxide-3.0 mg,

sodium carboxymethyl starch-10.0 mg.

Film coating pink-10.0 mg:

titanium dioxide-1.1 mg,

iron oxide red dye-1.6 mg,

hypromellose-3.2 mg,

macrogol-3.7 mg,

talc-0.4 mg

Pharmacological action

Sildenafil is a potent selective inhibitor of cyclic guanosine monophosphate (cGMP)- specific phosphodiesterase type 5 (PDE5).

Mechanism of action.

The realization of the physiological mechanism of erection is associated with the release of nitric oxide (MO) in the cavernous body during sexual stimulation. This, in turn, leads to an increase in cGMP levels, subsequent relaxation of the smooth muscle tissue

of the cavernous body, and increased blood flow.

Sildenafil does not have a direct relaxing effect on the isolated human cavernous body, but it enhances the effect of nitric oxide (MO) by

inhibiting PDE5, which is responsible for the breakdown of cGMP.

Sildenafil is selective for PDE5 and uigo, its activity against PDE5 exceeds that of other known phosphodiesterase isoenzymes: PDE6 – by 10 times; PDE1-by more than 80 times; PDE2, PDE4, PDE7-PDE11 – by more than 700 times. Sildenafil is 4000 times more selective for PDE5 compared to PDE5, which is of crucial importance, since PDE5 is one of the key enzymes

in the regulation of myocardial contractility.

A prerequisite for the effectiveness of sildenafil is sexual stimulation. Pharmacokinetics

The pharmacokinetics of sildenafil in the recommended dose range are linear. Suction

After oral use, sildenafil is rapidly absorbed. Absolute bioavailability averages about 40% (from 25% to 63%). sildenafil at a concentration of about 1.7 ng/ml (3.5 nM) suppresses human PDE5 activity by 50%. After a single 100 mg dose of sildenafil, the average maximum concentration of free

sildenafil in the blood plasma (Ctax) of men is about 18 ng / ml (38 nM). Schach when taking sildenafil inside fasting is achieved on average Chechenev 90 NDT poac In

combination with fatty foods, the rate of absorption decreases: Cmax omenn 66-8 Wednes for

29%, and the time to maximum concentration (tah) increases by 60 minutes, but the degree of absorption does not change significantly (area under the curve concentration-time (AOC) decreases by 11%).

Metabolism

Sildenafil is mainly metabolized in the liver by the cytochrome SURZA 4 isoenzyme (major pathway) and the cytochrome SURZA 2C9 isoenzyme (minor pathway). The main circulating active metabolite formed as a result of

Mg-demethylation of sildenafil, undergoes further — metabolism.

The selectivity of this metabolite against PDE is comparable to that of sildenafil, and its activity against PDE5 {t uIgo is about 50% of that of sildenafil. The concentration of the metabolite in the blood plasma of healthy volunteers was about 40% of the concentration of sildenafil. The M-demethyl metabolite undergoes further metabolism; its half-life (T 1/2) is about 4 hours.

Deduction

The total clearance of sildenafil is 41 l / h, and the final T!/? is 3-5 hours. After oral use, as well as after intravenous use, sildenafil is excreted as metabolites, mainly by the intestines (about 80% of the oral dose) and, to a lesser extent, by the kidneys (about 13% of the oral dose).

Pharmacokinetics in special patient groups:

Elderly patients

In the elderly (65 years and older), the clearance of sildenafil is reduced, and the concentration of free sildenafil in plasma is approximately 40% higher than in young people (18-45 years). Age does not have a clinically significant effect on the incidence of side effects. Impaired renal function

In mild (creatinine clearance 50-80 ml/min) and moderate (creatinine clearance 30-49 ml/min) renal insufficiency, the pharmacokinetics of sildenafil after

a single oral dose of 50 mg do not change. In severe renal insufficiency

, approximately two-fold increase in the area under the pharmacokinetic,

concentration-time curve (APS per 100%) and cross-section ratio (88%) compared with those indicators — with normal renal function in patients of the same age group.

Liver function disorders

In patients with cirrhosis of the liver (stages A and B according to the Child-Pugh classification), the clearance of sildenafil decreases, which leads to an increase in APS (84%) and Usax (47%) compared

to those with normal liver function in patients of the same age group. The pharmacokinetics of sildenafil in patients with severe hepatic impairment

(Child-Pugh stage C) have not been studied.

Indications

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

Sildenafil is effective only in the presence of sexual stimulation.

Contraindications

1. Hypersensitivity to sildenafil or any other component of the drug. Use in patients receiving continuous or intermittent nitric oxide donors, organic nitrates or nitrites in any form, as sildenafil increases the hypotensive effect of nitrates (see the section “Interaction with other drugs”).

2. Use in patients for whom sexual activity is undesirable (for example, with severe cardiovascular diseases, such as severe heart failure, unstable angina).

3. Hypotension (blood pressure less than 90/50 mm Hg).

4. Severe chronic renal failure.

5. A brain circulatory disorder or myocardial infarction that has occurred in the last six months.

6. Severe liver function disorders.

7. Hereditary degenerative diseases of the retina, including retinitis pigmentosa. Simultaneous use of ritonavir.

The safety and efficacy of sildenafil when co-administered with other treatments for erectile dysfunction have not been studied, so the use of such

combinations is not recommended (see section “Special instructions”).

According to the registered indication, sildenafil is not intended for use in children

under 18 years of age. According to the registered indication, sildenafil is not intended for

use in women.

With caution

1. Arterial hypertension (BP > 170/100 mm Hg).

2. Heart failure.

3. Life-threatening arrhythmias.

4. Anatomical deformity of the penis (angulation, cavernous fibrosis or Peyronie’s disease) (see the section “Special instructions”).

5. Diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia) (see the section “Special instructions”). Patients with a history of anterior non-arteritic ischemic optic neuropathy.

6. Diseases accompanied by bleeding.

7. Exacerbation of peptic ulcer of the stomach and duodenum.

8. Simultaneous use of alpha-blockers.

Use during pregnancy and lactation

According to the registered indication, the drug is not intended for use in women.

Side effects

Usually, the side effects of sildenafil are mild to moderate

Fixed-dose studies have shown that the frequency of some

adverse events increases with increasing dose.

Disorders of the general condition: chest pain, general weakness, irritability,

feeling hot, feeling tired. Allergic reactions: hypersensitivity reactions (including skin rash), Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome). Central and peripheral nervous system disorders: drowsiness, stroke, syncope, hypesthesia, transient ischemic attack, convulsions, including recurrent ones.

Cardiovascular disorders: tachycardia, increased or decreased blood pressure, myocardial infarction, atrial fibrillation, ventricular arrhythmia, unstable angina, hot flashes and palpitations, sudden death. Respiratory disorders: nasal bleeding, sinus congestion, tightness in the throat, dryness of the nasal mucosa, swelling of the nasal mucosa.

Disorders of the digestive system: vomiting, nausea, dryness of the oral mucosa, dyspepsia, abdominal pain, gastroesophageal reflux disease, hypesthesia of the oral mucosa.

Visual disorders: eye pain, redness of the eyes/sclera injections, conjunctival damage, lacrimation disorders, anterior ischemic optic neuropathy, retinal vascular occlusion, visual field defects, photophobia, photopsia, diplopia, glaucoma, decreased visual acuity, myopia, asthenopia, retinal edema, retinal vascular disease, eye discomfort, mydriasis, blurred vision, visual impairment, retinal hemorrhage, atherosclerotic retinopathy, eye irritation, edema of the eyelids, discoloration of the sclera.

Hearing disorders: vertigo, tinnitus, deafness, ringing in the ears. Musculoskeletal disorders: myalgia, pain in the extremities.

Reproductive system disorders: prolonged erections and / or priapism, hematospermia, and penile bleeding.

Disorders of the genitourinary system: hematuria.

How to take, course of use and dosage

Inside.

The recommended dose for most adult patients is 50 mg approximately 1 hour before sexual activity. Depending on the effectiveness and tolerability, the dose can be increased to 100 mg. The maximum recommended dose is 100 mg. The maximum recommended frequency of use is once a day.

Elderly patients

No dose adjustment of sildenafil is required.

Overdose

With a single dose of the drug up to 800 mg, adverse events were

comparable to those with lower doses of the drug, but were more common.

Description

Tablets covered with a film-coated pink color, biconvex, diamond-shaped with cut and rounded edges, with the inscription “50” on one side.

On a cross-section, the tablet core is white or almost white in color.

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Sildenafil

Conditions of release from pharmacies

By prescription

Dosage form

Tablets