Description
Release form
Sustained-release film-coated tablets.
Indications
Treatment of erectile dysfunction characterized by an inability to achieve or maintain an erection of the penis sufficient for satisfactory intercourse. Sildenafil is effective only in the presence of sexual stimulation.
Contraindications
Hypersensitivity to sildenafil or any other component of the drug. Use in patients receiving continuously or intermittently nitric oxide donors, organicchemical nitrates or nitrites in any form, since sildenafil enhances the hypotensive effect of nitrates (see section “Interaction with other drugs”).
Use in patients for whom sexual activity is undesirable (for example, with severe cardiovascular diseases such as severe heart failure, unstable angina pectoris).
Arterial hypotension (blood pressure less than 90/50 mm Hg).
Severe renal failure (CC <30 ml / min). Hepatic failure, cirrhosis. A cerebrovascular accident or myocardial infarction over the past six months. Hereditary degenerative diseases of the retina, including retinitis pigmentosa. Lactose intolerance, lactase deficiency, glucose-galactose malabsorption. Concomitant use of ritonavir (for dosages of 50 mg and 100 mg). The safety and effectiveness of sildenafil when used together 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 a registered indication, sildenafil is not intended for use in women. Precautions Arterial hypertension (BP> 170/100 mmHg).
Heart failure.
Life-threatening arrhythmias.
Anatomical deformation of the penis (angulation, cavernous fibrosis or Peyronie’s disease) (see section “Special instructions”).
Diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia, thrombocytes) (see section “Special instructions”).
Patients with a history of anterior non-arteritic ischemic neuropathy of the optic nerve.
Diseases accompanied by bleeding.
An exacerbation of peptic ulcer of the stomach and duodenum. Simultaneous administration of alpha-blockers.
Simultaneous administration with ritonavir, the maximum single dose of sildenafil should not exceed 25 mg, the frequency of use every 48 hours (you must use a tablet with a dosage of 25 mg).
Simultaneous administration with CYP3A4 cytochrome isoenzyme inhibitors (erythromycin, saquinavir, ketoconazole, itraconazole), the initial dose of sildenafil should be 25 mg (a 25 mg tablet should be used).
Use during pregnancy and lactation
According to the registered indication, the drug is not intended for use in women.
Special instructions
To diagnose erectile dysfunction, determine their possible causes and choose an adequate treatment, you need to collect a complete medical history and conduct a thorough physical examination. Treatments for erectile dysfunction should be used with caution in patients with anatomical deformation of the penis (angulation, cavernous fibrosis, Peyronie’s disease), or in patients with risk factors for priapism (sickle cell anemia, multiple myeloma, leukemia) (see section Carefully”). Drugs intended for the treatment of erectile dysfunction should not be prescribed to men for whom sexual activity is undesirable.
If an erection persists for more than 4 hours, seek medical attention. If priapism therapy is not performed in a timely manner, this can lead to damage to the tissues of the penis and irreversible loss of potency.
Sexual activity poses a certain risk in the presence of heart disease, therefore, before starting any treatment for erectile dysfunction, the doctor should refer the patient to an examination of the state of the cardiovascular system. Sexual activity is undesirable in patients with heart failure, unstable angina pectoris, myocardial infarction or stroke in the last 6 months, life-threatening arrhythmias, arterial hypertension (BP> 170/100 mm Hg) or hypotension (BP <90/50 mm Hg). Art.). In clinical studies, there was no difference in the incidence of myocardial infarction (1.1 per 100 people per year) or the mortality rate from cardiovascular diseases (0.3 per 100 people per year) in patients treated with sildenafil, compared with patients receiving placebo. Cardiovascular complications During the post-marketing 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 arrhythmia, hemorrhagic insomnia, were reported ischemic attack, hypertension and hypogenia), which had a temporary connection 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. Hypotension Sildenafil has a systemic vasodilating effect, leading to a transient decrease in blood pressure, which is not a clinically significant phenomenon and does not lead to any consequences in most patients. Nevertheless, before prescribing sildenafil, the doctor should carefully assess the risk of possible unwanted manifestations of vasodilating action in patients with relevant diseases, especially against the background of sexual activity. Increased susceptibility to vasodilators is observed in patients with left ventricular outflow tract obstruction (aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as with rare syndrome of multiple systemic atrophy, manifested severe violation of the regulation of blood pressure by the autonomic nervous system. Since the combined use of sildenafil and β-blockers can lead to symptomatic hypotension in some sensitive patients, the drug should be used with caution in patients taking β-blockers (see section Interaction with other drugs ). To minimize the risk of developing postural hypotension in patients taking -Adrenergic blockers, sildenafil should only be started after the hemodynamic parameters in these patients have stabilized. It should also consider the feasibility of lowering the initial dose of sildenafil (see section “Method of application and dose”). The doctor should inform patients that what actions should be taken in case of symptoms of postural hypotension. Visual disturbances Rare cases of the development of anterior non-arteritic ischemic neuropathy of the optic nerve have been noted as a cause of deterioration or loss of vision against the background of the use of all PDE5 inhibitors, including sildenafil. Most of these patients had risk factors such as excavation (deepening) of the optic nerve head, over the age of 50 years, diabetes mellitus, hypertension, coronary heart disease, hyperlipidemia, and smoking. A small number of patients with hereditary retinitis pigmentosa have genetically determined dysfunctions of the retinal phosphodiesterases. There is no information on the safety of sildenafil in patients with retinitis pigmentosa. Hearing impairment Some post-marketing and clinical studies report cases of sudden impairment or loss of hearing associated with all PDE5 inhibitors, including sildenafil. Most of these patients had risk factors for sudden impairment or hearing loss. A causal relationship with food> using PDE5 inhibitors and sudden hearing loss or hearing loss has not been established. In case of sudden hearing loss or hearing loss while taking sildenafil, you should immediately consult your doctor.
Bleeding
Sildenafil enhances the antiplatelet effect of sodium nitroprusside, a nitric oxide donor, on human platelets in vitro. There is no safety data on the use of sildenafil in patients with a tendency to bleeding or exacerbation of peptic ulcer of the stomach and duodenum, therefore, sildenafil should be used with caution in these patients (see the “Caution” section). The frequency of nosebleeds in patients with LH associated with diffuse connective tissue diseases was higher (sildenafil 12.9%, placebo 0%) than in patients with primary pulmonary hypertension (sildenafil 3.0%, placebo 2.4%) . In patients receiving sildenafil in combination with a vitamin K antagonist, the frequency of nosebleeds was higher (8.8%) than in patients who did not take a vitamin K antagonist (1.7%).
Use in conjunction with other treatments for erectile dysfunction
The safety and effectiveness of sildenafil in combination with other treatments for erectile dysfunction has not been studied, therefore, the use of such combinations is not recommended (see section “Contraindications”),
Effect on the ability to drive a car and control the mechanisms of
Since when taking sildenafil, a decrease in blood pressure, the development of chromatopsy, blurred vision, etc., are possible. side effects, you should be careful about the individual action of the drug in these situations, especially at the beginning of treatment and when changing the dosage regimen and be careful when driving and engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Composition
Active ingredient: sildenafil citrate – 140.4800 mg, in terms of sildenafil base – 100.0000 mg.
excipients (core): hypromellose – 110.0000 mg, lactose monohydrate (milk sugar) – 82.5200 mg, povidone – K25 – 14.0000 mg, magnesium stearate – 3.0000 mg.
excipients (shell): Opadry II 85F205024 blue -12.0000 mg, polyvinyl alcohol – 4.8000 mg, macrogol-4000 – 2.4240 mg, aluminum varnish with indigo carmine dyes and brilliant blue – 0.7476 mg, iron dye oxide yellow – 0.0324 mg, talc – 1.7760 mg, titanium dioxide – 2.2200 mg.
Dosage and Administration
Inside.
The recommended dose for most adult patients is 50 mg approximately 1 hour before sexual activity. Given 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.
Impaired renal function
Dose adjustment is not required for mild to moderate degree of renal failure (CC 30-80 ml / min).
Co-administration with other drugs To minimize the risk of postural hypotension in patients, taking ?-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 sections “Special Instructions” and “Interaction with Other Medicines”).
Elderly patients
Sildenafil dose adjustment not required.
Side effects
Classification of the incidence of side effects (WHO): very often> 1/10, often from> 1/100 to <1/10, infrequently from> 1/1000 to <1/100, rarely from> 1 / 10000 to <1/1000, very rarely from <1/10000, including single messages. From the nervous system: very often – headache often – dizziness infrequently – drowsiness, hypesthesia rarely – stroke, fainting frequency is unknown – transient ischemic attack, convulsions, incl. recurrent. From the cardiovascular system: often – vasodilation (“flushing”) infrequently – a feeling of palpitations, tachycardia rarely – increase or decrease in blood pressure, myocardial infarction, atrial fibrillation, frequency is unknown – ventricular arrhythmia, unstable angina pectoris, sudden cardiac arrest. From the side of the organs of vision: often – visual impairment, infringement of color perception infrequently – conjunctival lesion, lacrimation impaired, frequency unknown – anterior ischemic optic neuropathy, retinal vascular occlusion, visual field defects. On the part of the hearing organs: infrequently – vertigo, tinnitus rarely – sudden decrease or loss of hearing. From the respiratory system, chest and mediastinal organs: often – nasal congestion rarely – nosebleeds. From the gastrointestinal tract: often – dyspepsia infrequently – vomiting, nausea, dry oral mucosa. Allergic reactions: infrequently – skin rash frequency is unknown – Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome). From the genital organs: infrequently – hematospermia, bleeding from the penis, frequency unknown – priapism, prolonged erection. From the side of the musculoskeletal system: infrequently – myalgia. Other: rarely – chest pain, fatigue. Drug Interactions Effect of other drugs on the pharmacokinetics of sildenafil. Sildenafil metabolism occurs mainly under the influence of cytochrome CYP3A4 isoenzymes (main pathway) and CYP2C9, therefore inhibitors of these isoenzymes can reduce sildenafil clearance, and inductors, respectively, increase sildenafil clearance. A decrease in the clearance of sildenafil was noted with the simultaneous use of inhibitors of the cytochrome CYP3A4 isoenzyme (ketoconazole, erythromycin, qi methidine). Cimetidine (800 mg), a non-specific inhibitor of the cytochrome CYP3A4 isoenzyme, when taken 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 specific 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%. With the combined use of 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 P450 inhibitor, while achieving a constant concentration of ritonavir in the blood leads to an increase in Cmax of sildenafil by 300% (in 4 times), a 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 taken in recommended doses by patients receiving at the same time strong inhibitors of the cytochrome CYP3A4 isoenzyme, then Cmax 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. Inhibitors of the cytochrome CYP2C9 isoenzyme (tolbutamide, warfarin), cytochrome CYP2D6 isoenzyme (selective serotonin reuptake inhibitors, three cyclic 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. With the simultaneous use of the antagonist of the endogenous receptors of bosentan and sildenafil, there was a decrease in AUC and Stax of sildenafil by 62.6% and 52.4%, respectively. The effect of sildenafil on other drugs Sildenafil is a weak inhibitor of the cytochrome P450-1A2, 2C9, 2C19, 2D6, 2E1 and ZA4 zofer inhibitors (IC50> 150 μmol). When taking sildenafil at recommended doses, its Stax is about 1 μmol, so it is unlikely that sildenafil can affect the clearance of the substrates of these and zoferments.
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 (25 mg, 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 7 / 7 mmHg Art., 9/5 mm RT. Art. and 8/4 mm RT. Art., respectively, and in a standing position – 6/6 mm RT. Art., 11/4 mm RT. Art. and 4/5 mm RT. Art., respectively. Rare cases of the development of symptomatic postural hypogensia 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 CYP2C9 isoenzyme, 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. 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. With the simultaneous use of sildenafil with bosentan (inducer of isoenzymes CYP3A4, CYP2C9), there was a decrease in AUC and Stax of sildenafil by 62.6% and 52.4%, respectively. Sildenafil increased AUC and Cmax of bosentan by 49.8% and 42%, respectively.
Overdose of
With a single dose of the drug up to 800 mg, adverse events were comparable to those with the drug at lower doses, but were more common. The treatment is symptomatic. Hemodialysis does not accelerate the clearance of sildenafil, since the latter actively binds to plasma proteins and is not excreted by the kidneys.
Storage Conditions
In a dark place at a temperature not exceeding 25 ° C.
Keep out of the reach and sight of children.
The Expiration of
is 3 years.
Active ingredient
Sildenafil
conditions granted through pharmacies
In retseptu
