Effex Sildenafil tablets coated.pl.ob. 100 mg 1 pc. (sildenafil)

Release form

Film-coated tablets, 100 mg.

Indications

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

EFFEX® Sildenafil is effective only with sexual stimulation.

Contraindications

Hypersensitivity to sildenafil or to any other component of the drug.

Use in patients receiving continuous or intermittent nitric oxide donors, organic nitrates or nitrites in any form, since

EFFEX ® Sildenafil enhances the hypotensive effect of nitrates (see section "Interaction with other drugs").

The safety and efficacy of EFFEX® Sildenafil when used together with other treatments for erectile dysfunction have not been studied, therefore, the use of such combinations is not recommended (see section "Special Instructions").

Co-administration with ritonavir.

Impaired liver function.

Severe chronic renal failure.

Severe heart failure, unstable angina pectoris, stroke or myocardial infarction during the last 6 months, life-threatening arrhythmias, arterial hypertension (BP> 170/100 mm Hg) or hypotension (BP <90/50 mm Hg) (see section “ Special instructions").

According to the registered indication, the drug EFFEX® Sildenafil is not intended for use in children under 18 years of age.

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

Precautions

Anatomical deformation of the penis (angulation, cavernous fibrosis, or Peyronie's disease) (see Special Instructions).

Diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia) (see section "Special instructions").

Diseases accompanied by bleeding.

Exacerbation of gastric ulcer and 12 duodenal ulcer.

Hereditary retinitis pigmentosa (see Special Instructions).

Use during pregnancy and lactation

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

Composition of

Sildenafil citrate (in terms of sildenafil) 140.50 mg (100.00 mg).

Dosage and Administration

Inside.

The recommended dose for most adult patients is 50 mg of sildenafil approximately 1 hour before sexual activity.

Given the effectiveness and tolerability, the dose may be increased to 100 mg. The maximum recommended dose is 100 mg. The maximum recommended frequency of use is 1 time per day.

Elderly patients

Efex® sildenafil dose adjustment is not required.

Impaired renal function

Dose adjustment is not required for patients with mild or moderate severity of renal failure

(CC 30-80 ml / min).

Co-administration with other medicines

To minimize the risk of developing postural hypotension in patients taking? -adrenergic blockers, sildenafil should be started only after hemodynamic stabilization is achieved in these patients. The feasibility of lowering the initial dose of sildenafil should also be considered (see the section "Interaction with other drugs" and "Special instructions").

Side effects

The most common side effects were headache and hot flashes.

Usually, the side effects of EFFEX® Sildenafil are mild or moderate and are transient.

In studies using a fixed dose, it has been shown that the frequency of some adverse events increases with increasing dose.

The frequency of adverse reactions is presented by the following classification:

Very often

? 10%

Often

? 1% and <10%

Infrequently

? 0.1% and <1%

Rarely

? 0.01% and <0, 1%

Very rare

<0.01%

Frequency unknown

Impossible to determine based on available

data. From the immune system: infrequently - hypersensitivity reactions (including skin rash), allergic reactions.

From the side of the organ of vision: often - blurred vision, impaired vision, cyanopsia infrequently - eye pain, photophobia, photopsia, chromatopsia, redness of the eyes / injection of sclera, change in brightness of light perception, mydriasis, conjunctivitis, hemorrhage in the tissue of the eye, cataract, malfunction rarely, lacrimal apparatus - swelling of the eyelids and adjacent tissues, a feeling of dryness in the eyes, the presence of rainbow circles in the field of view around the light source, increased eye fatigue, seeing objects in yellow (xantopsia), seeing objects in red color (eritropsiya), conjunctival hyperemia, eye irritation, eye discomfort frequency is unknown - nearteriitnaya anterior ischemic optic neuropathy (NPINZN), retinal vein occlusion, visual field defects, diplopia * temporary loss of vision or decreased visual acuity, increased intraocular pressure, retinal edema, retinal vascular disease, vitreous detachment / vitreous traction.

On the part of the hearing organ: infrequently - sudden decrease or loss of hearing, tinnitus, earache.

From the cardiovascular system: often - “tides” infrequently - tachycardia, palpitations, decreased blood pressure, increased heart rate, unstable angina, atrioventricular block, myocardial ischemia, cerebral thrombosis, cardiac arrest, heart failure, deviations in the indications of the electrocardiogram, cardiomyopathy is rarely atrial fibrillation.

From the blood and lymphatic system: infrequently - anemia, leukopenia.

From the side of metabolism and nutrition: infrequently - thirst, swelling, gout, uncompensated diabetes, hyperglycemia, peripheral edema, hyperuricemia, hypoglycemia, hypernatremia.

From the respiratory system: often - nasal congestion infrequently - nosebleeds, rhinitis, asthma, dyspnea, laryngitis, pharyngitis, sinusitis, bronchitis, increased sputum discharge, increased coughing rarely - a feeling of tightness in the throat, dryness of the nasal mucosa, swelling mucous membrane of the nose.

From the gastrointestinal tract: often - nausea, dyspepsia infrequently - gastroesophageal reflux disease, vomiting, abdominal pain, dry mucous membrane of the oral cavity, glossitis, gingivitis, colitis, dysphagia, gastritis, gastroenteritis, esophagitis, stomatitis, liver function tests from the norm, rectal bleeding rarely - hypoesthesia of the oral mucosa.

From the musculoskeletal system: often - back pain infrequently - myalgia, pain in the extremities, arthritis, arthrosis, tendon rupture, tenosynovitis, bone pain, myasthenia gravis, synovitis.

From the genitourinary system: infrequently - cystitis, nocturia, breast enlargement, urinary incontinence, hematuria, impaired ejaculation, genital edema, anorgasmia, hematospermia, tissue damage to the penis rarely - prolonged erection and / or priapism.

From the central and peripheral nervous system: very often - headache often - dizziness infrequently - drowsiness, migraine, ataxia, hypertonicity, neuralgia, neuropathy, paresthesia, tremor, vertigo, symptoms of depression, insomnia, unusual dreams, increased reflexes, hypesthesia rarely - cramps *, repeated cramps *, fainting.

From the skin and subcutaneous tissues: infrequently - skin rash, urticaria, herpes simplex, itching, increased sweating, ulceration of the skin, contact dermatitis, exfoliative dermatitis, frequency unknown - Stevens-Johnson syndrome, toxic epidermal necrolysis.

Other: infrequently - sensation of heat, swelling of the face, photosensitivity reaction, shock, asthenia, fatigue, pain of various localization, chills, accidental falls, pain in the chest area, occasional injuries rarely - irritability.

* Side effects identified during post-marketing research.

Cardiovascular complications

During the post-marketing use of sildenafil for the treatment of erectile dysfunction, adverse events such as severe cardiovascular complications were reported (i.e. including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, hemorrhagic stroke, transient ischemic attack, hypertension and hypotension), which had a temporary relationship with the use of sildenafil. Most of these patients, but not all of them, had risk factors for cardiovascular complications. Many of these adverse events were observed shortly after sexual activity, and some of them were noted after taking sildenafil without subsequent sexual activity. It is not possible to establish the existence of a direct relationship between the observed adverse events and the indicated or other factors.

Visual disturbances

In rare cases, during the post-registration use of all PDE5 inhibitors, including sildenafil, reported non-arteritic anterior ischemic optic nerve neuropathy (NEPIN), a rare disease and the cause of decreased or loss of vision. Most of these patients had risk factors, in particular a decrease in the ratio of the diameters of excavation and optic disc (“congestive disc”), over 50 years old, diabetes mellitus, hypertension, coronary heart disease, hyperlipidemia, and smoking. An observational study evaluated whether the recent use of PDE5 inhibitor class drugs is associated with acute onset of NPINZN. The results indicate an approximately 2-fold increase in the risk of NPINZN within 5 half-lives after the use of a PDE5 inhibitor. According to published literature, is the annual incidence of NPINZN 2.5–11.8 cases per 100,000 men aged? 50 years in the general population. In case of sudden loss of vision, patients should be advised to discontinue sildenafil therapy and consult a physician immediately. Individuals who have already had a case of NPINZN have an increased risk of relapse of NPINZN. Therefore, the doctor should discuss this risk with such patients, and also discuss with them the potential chance of adverse effects of PDE5 inhibitors. PDE5 inhibitors, including sildenafil, in such patients should be used with caution and only in situations where the expected benefits outweigh the risk.

Drug interaction

The influence of other drugs on the pharmacokinetics of sildenafil

Metabolism of sildenafil occurs mainly under the influence of isoenzymes of cytochrome CYP3A4 inhibitors, these are the main pathway inhibitors increase the clearance of sildenafil.

A marked decrease in clearance of sildenafil with the simultaneous use of inhibitors of the cytochrome CYP3A4 isoenzyme (ketoconazole, erythromycin, cimetidine).

Cimetidine (800 mg), a non-specific inhibitor of the cytochrome CYP3A4 isoenzyme, when taken together with sildenafil (50 mg) causes an increase in plasma concentration of sildenafil by 56%.

A single dose of 100 mg of sildenafil together with erythromycin (500 mg / day 2 times a day for 5 days), a moderate inhibitor of the cytochrome CYP3A4 isoenzyme, against the background of achieving a constant concentration of erythromycin in the blood, leads to an increase in AUC of sildenafil by 182%.

When co-administered with sildenafil (once 100 mg) and saquinavir (1200 mg / day 3 times a day), an inhibitor of HIV protease and isoenzyme of cytochrome CYP3A4, against the background of achieving a constant concentration of saquinavir in the blood, Cmax of sildenafil increased by 140%, and AUC increased by 210%. Sildenafil has no effect on the pharmacokinetics of saquinavir.

Stronger inhibitors of the cytochrome CYP3A4 isoenzyme, such as ketoconazole and itraconazole, can also cause stronger changes in the pharmacokinetics of sildenafil.

The simultaneous use of sildenafil (once 100 mg) and ritonavir (500 mg 2 times a day), an HIV protease inhibitor and a strong cytochrome P 450 inhibitor, while achieving a constant concentration of ritonavir in the blood leads to an increase in Cmax of sildenafil by 300% (in 4 times), and AUC by 1000% (11 times). After 24 hours, the concentration of sildenafil in the blood plasma is about 200 ng / ml (after a single use of one sildenafil - 5 ng / ml).

If sildenafil is used in recommended doses for patients receiving at the same time strong inhibitors of the cytochrome CYP3A4 isoenzyme, then C max of free sildenafil does not exceed 200 nM, and the drug is well tolerated.

A single dose of antacid (magnesium hydroxide / aluminum hydroxide) does not affect the bioavailability of sildenafil.

In studies involving healthy volunteers with the simultaneous use of an endothelin receptor antagonist, bosentan (inducer of the isoenzyme CYP3A4 (moderate), CYP2C9 and possibly CYP2C19) in equilibrium concentration (125 mg twice daily) and sildenafil in equilibrium concentration (80 mg three times a day) there was a decrease in AUC and C max of sildenafil by 62.6% and 52.4%, respectively. Sildenafil increased AUC and Cmax of bosentan by 49.8% and 42%, respectively. Supposed that the simultaneous use of sildenafil with powerful inducers of the CYP3A4 isoenzyme, such as rifampicin, can lead to a large decrease in the concentration of sildenafil in the blood plasma.

Inhibitors of the cytochrome CYP2C9 isoenzyme (tolbutamide, warfarin), CYP2D6 cytochrome isoenzyme inhibitors (selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazide and thiazide-like diuretics, pharmacokin and antagonists of pharmacokin

Azithromycin (500 mg / day for 3 days) does not affect AUC, Cmax, Tmax, excretion rate constant, and T? sildenafil or its main circulating metabolite.

Effect of sildenafil on other drugs

Sildenafil is a weak inhibitor of cytochrome P 450 isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 (IC50> 150 μmol). When taking sildenafil at recommended doses, its Cmax is about 1 μmol, so it is unlikely that sildenafil can affect the clearance of substrates of these isoenzymes.

Sildenafil enhances the hypotensive effect of nitrates both with prolonged use of the latter, and with their appointment for acute indications. In this regard, the use of sildenafil in combination with nitrates or nitric oxide donors is contraindicated.

With the simultaneous administration of? -adrenoblocker doxazosin (4 mg and 8 mg) and sildenafil (50 mg and 100 mg) in patients with benign prostatic hyperplasia with stable hemodynamics, the average additional decrease in systolic / diastolic blood pressure in the supine position was 9/5 mmHg Art. and 8/4 mm RT. Art., respectively, and in a standing position - 11/4 mm RT. Art. and 4/5 mm RT. Art., respectively. Rare cases of the development of symptomatic postural hypotension in such patients, manifested in the form of dizziness (without fainting), have been reported. In some sensitive patients receiving? -Adrenergic blockers, the simultaneous use of sildenafil can lead to symptomatic hypotension.

Signs of significant interaction with tolbutamide (250 mg) or warfarin (40 mg), which are metabolized by the cytochrome CYP 2 C 9 isoenzyme, were not detected.

Sildenafil (100 mg) has no effect on the pharmacokinetics of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of the cytochrome CYP3A4 isoenzyme, at their constant blood level.

The simultaneous use of sildenafil in equilibrium (80 mg three times a day) leads to an increase in AUC and Cmax of bosentan (125 mg twice a day) by 49, 8% and 42%, respectively.

Sildenafil (50 mg) does not cause an additional increase in bleeding time when taking acetylsalicylic acid (150 mg).

Sildenafil (50 mg) does not enhance the hypotensive effect of alcohol in healthy volunteers with a maximum blood alcohol concentration of 0.08% (80 mg / dl) on average.

In patients with arterial hypertension, no signs of interaction of sildenafil (100 mg) with amlodipine were detected. The average additional decrease in blood pressure in the supine position is 8 mm RT. Art. (systolic) and 7 mmHg. Art. (diastolic).

The use of sildenafil in combination with antihypertensive agents does not lead to additional side effects.

Overdose of

When using the EFFEX® Sildenafil preparation in doses exceeding the recommended ones, adverse events were similar to those noted above, but were usually more common.

Symptomatic treatment. Hemodialysis does not accelerate the elimination of the drug, since sildenafil is firmly bound to plasma proteins and is not excreted by the kidneys.

Storage conditions

Do not store above 25 ° C.

Keep out of the reach and sight of children.

Expiration

3 years.

active substance

Sildenafil

lekarstvennaja form

tablets



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