Effex Sildenafil, 50 mg 6 pcs

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Indications

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

Active ingredient

Composition

How to take, the dosage

Ingestion.

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

The dose may be increased to 100 mg, depending on efficacy and tolerability. The maximum recommended dose is 100 mg. The maximum recommended frequency of use is once daily.

Elderly patients

Renal dysfunction

Dose adjustment is not required for patients with mild to moderate renal impairment (CK 30-80 ml/min).

The concomitant use with other drugs

In order to minimize the risk of postural hypotension in patients taking α-adrenoblockers, sildenafil should be started only after hemodynamic stabilization has been achieved in these patients. A reduction in the starting dose of sildenafil should also be considered.

Interaction

Metabolism of sildenafil mainly occurs under the action of cytochrome CYP3A4 isoenzymes (main pathway) and CYP2C9, therefore inhibitors of these isoenzymes may decrease sildenafil clearance, and inducers, respectively, increase sildenafil clearance.

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

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

Special Instructions

To diagnose erectile dysfunction, determine its possible causes, and choose an adequate treatment, a complete medical history and a thorough physical examination must be taken.

The treatment of erectile dysfunction should be used with caution in patients with anatomic penile deformities (angulation, cavernous fibrosis, Peyronie’s disease), or those with risk factors for priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia).

In post-marketing studies, cases of prolonged erections and priapism have been reported. If an erection persists for more than 4 hours, immediate medical attention should be sought. If priapism is not treated immediately, it may result in damage to penile tissue and permanent loss of potency.

The drugs intended to treat erectile dysfunction should not be prescribed for men for whom sexual activity is undesirable.

Sexual activity poses some risk if you have heart disease, so your doctor should refer you for a cardiovascular physical exam before starting any erectile dysfunction therapy. Sexual activity is undesirable in patients with heart failure, unstable angina, stroke or myocardial infarction within the last 6 months, life-threatening arrhythmias, arterial hypertension (BP > 170/100 mm Hg) or hypotension (BP <90/50 mm Hg).

In clinical trials, there have been no differences in the incidence of myocardial infarction (1.1 per 100 people per year) or cardiovascular mortality (0.3 per 100 people per year) in patients receiving sildenafil compared to patients receiving placebo.

Cardiovascular Complications

In the postmarketing use of sildenafil for the treatment of erectile dysfunction, adverse events such as serious cardiovascular complications (including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmias, hemorrhagic stroke, transient ischemic attack, hypertension, and hypotension) that were temporarily associated with sildenafil use. Most, but not all, of these patients had risk factors for cardiovascular complications.

Many of these adverse events occurred shortly after sexual activity, and some occurred after sildenafil administration without subsequent sexual activity. It is not possible to establish a direct relationship between the reported adverse events and these or other factors.

Hypotension

Sildenafil has a systemic vasodilatory effect resulting in a transient decrease in BP, which is not clinically significant and has no effect in most patients. Nevertheless, before prescribing sildenafil, the physician should carefully evaluate the risk of possible adverse vasodilatory effects in patients with related conditions, especially with sexual activity.

Elevated susceptibility to vasodilators is seen in patients with left ventricular outflow tract obstruction (aortic stenosis, hypertrophic obstructive cardiomyopathy), and with the rare multiple systemic atrophy syndrome, manifested by severe autonomic nervous system BP dysregulation.

Contraindications

Hypersensitivity to sildenafil or any other component of the drug.

Patients receiving nitric oxide donators, organic nitrates or nitrites in any form continuously or intermittently, as EFEX Sildenafil enhances the hypotensive effect of nitrates.)

Safety and efficacy of EFEX Sildenafil when used together with other means of erectile dysfunction treatment have not been studied, therefore such combinations are not recommended.

Co-administration with ritonavir.

Liver function abnormalities.

Chronic renal failure of severe severity.

Severe heart failure, unstable angina, stroke or myocardial infarction within the last 6 months, life-threatening arrhythmias, arterial hypertension (BP > 170/100 mm Hg) or hypotension (BP < 90/50 mm Hg).

Anatomical deformity of the penis (angulation, cavernous fibrosis or Peyronie’s disease).

Diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocythemia).

Diseases accompanied by bleeding.

The exacerbation of gastric and 12 duodenal ulcers.

Hereditary retinitis pigmentosa.

Side effects

The most common side effects were headache and “hot flashes.

In general, the side effects of EFEX Sildenafil are mild to moderate and transient.

In fixed-dose studies, the incidence of some adverse events has been shown to increase with increasing dose.

Immune system disorders: infrequent hypersensitivity reactions (including skin rash), allergic reactions.

VIight organ disorders: frequent – blurred vision, visual disturbances, cyanopsia; infrequent – eye pain, photophobia, photopsia, chromatopsia, eye redness/sclera injections, changes in brightness of light perception, mydriasis, conjunctivitis, bleeding in eye tissue, cataracts, disorders of the lacrimal system; rare – swelling of the eyelids and adjacent tissues, dry eye sensation, iridescent circles in the field of vision around the light source, increased eye fatigue, seeing objects in yellow (xanthopsia), seeing objects in red (erythropsia), conjunctival hyperemia, irritation of the mucous membrane in the eyes, unpleasant sensations in the eyes; frequency unknown – nonarteritic anterior ischemic optic neuropathy (NAPINZ), retinal vein occlusion, visual field defects, diplopia*, temporary vision loss or decreased visual acuity, increased intraocular pressure, retinal edema, retinal vascular disease, vitreous detachment/vitreal traction.

Hearing organ: infrequent – sudden decrease or loss of hearing, tinnitus, tinnitus pain.

Cardiovascular system disorders: frequent – “flushes”; infrequent – tachycardia, palpitations, decreased blood pressure, increased heart rate, unstable angina, atrioventricular block, myocardial ischemia, cerebral vascular thrombosis, cardiac arrest, heart failure, deviations in electrocardiogram readings, cardiomyopathy; rare – atrial fibrillation.

Blood and lymphatic system disorders: infrequent – anemia, leukopenia.

Mechanisms and nutrition: infrequent – sensation of thirst, edema, gout, uncompensated diabetes, hyperglycemia, peripheral edema, hyperuricemia, hypoglycemia, hypernatriemia.

Respiratory system: frequently – nasal congestion; infrequently – nasal bleeding, rhinitis, asthma, dyspnea, laryngitis, pharyngitis, sinusitis, bronchitis, increased volume of sputum, increased coughing; rarely – feeling of tightness in the throat, dry nasal mucosa, swelling of the nasal mucosa.

Gastrointestinal tract disorders: frequent – nausea, dyspepsia; infrequent gastroesophageal reflux disease, vomiting, abdominal pain, dry oral mucosa, glossitis, gingivitis, colitis, dysphagia, gastritis, gastroenteritis, esophagitis, stomatitis, deviation of “liver” functional tests from normal, rectal bleeding; rare – oral mucosa hyposthesia.

Musculoskeletal system: often – back pain; infrequent – myalgia, pain in the extremities, arthritis, arthrosis, tendon rupture, tenosynovitis, bone pain, myasthenia gravis, synovitis.

Urogenital system disorders: infrequent – cystitis, nycturia, breast enlargement, urinary incontinence, hematuria, ejaculation disorders, genital edema, anorgasmia, hematospermia, penile tissue damage; rarely – prolonged erection and/or priapism.

The central and peripheral nervous system: very common – headache; common – dizziness; infrequent – drowsiness, migraine, ataxia, hypertonicity, neuralgia, neuropathy, paresthesia, tremor, vertigo, symptoms of depression, insomnia, unusual dreams, increased reflexes, kinesthetic; rare – seizures*, recurrent seizures*, syncope.

Skin and subcutaneous tissue disorders: infrequent – skin rash, urticaria, herpes simplex, skin itching, increased sweating, skin ulceration, contact dermatitis, exfoliative dermatitis; frequency unknown – Stevens-Johnson syndrome, toxic epidermal necrolysis.

Others: infrequent – sensation of heat, facial edema, photosensitivity reaction, shock, asthenia, increased fatigue, pain in various localizations, chills, accidental falls, pain in the chest area, accidental injury; rarely – irritability.

*Side effects identified during post-marketing studies.

Cardiovascular complications

In postmarketing use of sildenafil for the treatment of erectile dysfunction, adverse events such as severe cardiovascular complications (including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmias, hemorrhagic stroke, transient ischemic attack, hypertension, and hypotension) that were temporarily associated with sildenafil use, most, but not all, of these patients had risk factors for cardiovascular complications.

Many of these adverse events were observed shortly after sexual activity, and some were noted after sildenafil administration without subsequent sexual activity. It is not possible to establish a direct relationship between the reported adverse events and these or other factors.

Visual impairment

In rare cases during post-registration use of all FDE5 inhibitors, including sildenafil, nonarteritic anterior ischemic arterial nerve neuropathy (NAPINN), a rare condition and cause of visual impairment or loss, has been reported. Most of these patients had risk factors, including a decreased ratio of optic disc diameters (“stagnant disc”), age over 50 years, diabetes mellitus, hypertension, coronary heart disease, hyperlipidemia, and smoking. The observational study evaluated whether recent use of drugs in the class of FDE5 inhibitors was associated with the acute onset of NSAIDs.

The results indicated an approximately 2-fold increased risk of NPINZN within 5 half-lives of use of an FDE5 inhibitor. According to published literature, the annual incidence of NPINZN is 2.5-11.8 cases per 100,000 men aged > 50 years in the general population.

Patients should be advised to discontinue sildenafil therapy and consult a physician immediately in the event of sudden vision loss. Individuals who have already had a history of NSAIDs have an increased risk of a recurrence of NSAIDs. Therefore, the physician should discuss this risk with such patients, as well as discuss with them the potential chance of adverse effects of FDE5 inhibitors. FDE5 inhibitors, including sildenafil, should be used with caution in such patients and only in situations where the expected benefits outweigh the risks.

Overdose

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