Description
Latin name
Sildenafilum
Release form
Coated tablets.
Packing
In a package of 4 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 with sexual stimulation.
Use during pregnancy and lactation
According to the registered indication, the drug is not intended for use in women.
Composition
active substances: sildenafil (as citrate) 100 m ,
Excipients: Microcrystalline cellulose 83.5 mg Lactose monohydrate 83.5 mg Sodium croscarmellose 15 mg, povidone 15 mg, magnesium stearate 3 mg.
film composition: Opadry II (polyvinyl alcohol, partially hydrolyzed 3.6 mg, titanium dioxide 2.061 mg, macrogol 1.818 mg, talc 1.332 mg, brilliant blue aluminum varnish 0.1728 mg, iron oxide (II) yellow 0.0153 mg, iron oxide ( Ii) black 0.0009 mg).
Dosing and dose
Sildenafil ingest . 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 or reduced to 25 mg.
The maximum recommended dose is 100 mg. The maximum recommended frequency of use is 1 time per day.
Impaired renal function. In case of mild to moderate degree of renal failure (Cl creatinine 30 80 ml / min) dose adjustment is not required, in severe renal failure (Cl creatinine
Impaired liver function. Since excretion of sildenafil is impaired in patients with liver damage (in particular, cirrhosis), the dose of Sildenafil should be reduced to 25 mg.
Joint use with other drugs.When combined with ritonavir, the maximum single dose of Sildenafil should not exceed 25 mg, and the frequency of use – 1 time in 48 h (see “Interaction”).
When used together with inhibitors of the cytochrome CYP3A4 isoenzyme (erythromycin, saquinavir, ketoconazole, itraconazole), the initial dose of Sildenafil should be 25 mg (see Interaction ).
To minimize the risk of developing postural hypotension in patients taking? -blockers, sildenafil should only be started after hemodynamic stabilization is achieved in these patients. The feasibility of lowering the initial dose of sildenafil should also be considered (see “Special Instructions” and “Interaction”).
Elderly patients. No dose adjustment for sildenafil is required.
Side effects
Usually, the side effects of Sildenafil are mild or moderate and are transient.
Fixed dose studies have shown that frequency
Organs and organ systems Adverse events Sildenafil,% Placebo,%
Most common adverse events (> 1/10)
Nervous system Headache 164
Cardiovascular system Vasodilation (hot flashes of blood to the face) 101 srdlp / 100 and <1/10) Nervous system Dizziness 21 Organ of vision Visual disturbances (blurred visual perception, impaired color vision) 2.50.4 Chromatopsia (slight and transient, mainly a change in the perception of color shades) 1.10.03 Cardiac -vascular system Goes serdtsebienie1,00, 2 Respiratory system Rhinitis (nasal congestion) 42 Digestive system Dyspepsia 72 Diarrhea 31 Urinary system Urinary tract infections 32 Skin and subcutaneous tissue Rash 21 When the drug was used, it was more common that the symptoms were more frequent, they were more frequent, but were more frequent, they were more frequent. General disorders: facial swelling, photosensitivity reactions, shock, asthenia, pain, chills, abdominal pain, chest pain. Allergic reactions: hypersensitivity reactions (including skin rash), Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome). Disorders from the central and peripheral nervous system: drowsiness, insomnia, hypesthesia, paresthesia, ataxia, neuralgia, neuropathy, tremor, depression, unusual dreams, decreased reflexes, stroke, transient ischemic attack, convulsions, including recurrent. Disorders from the cardiovascular system: tachycardia, increase or decrease in blood pressure, myocardial infarction, atrial fibrillation, atrial fibrillation, unstable angina pectoris, AV block, cerebral vascular thrombosis, heart failure, ECG disturbances, cardiomyopathy, sudden death, fainting. Respiratory disorders: nosebleeds, asthma, shortness of breath, laryngitis, pharyngitis, sinusitis, bronchitis, increased sputum production, increased coughing. Gastrointestinal disorders: vomiting, nausea, dry oral mucosa, glossitis, colitis, dysphagia, gastritis, gastroenteritis, esophagitis, stomatitis, rectal bleeding, gingivitis. Disorders of the organ of vision: eye pain, redness of the eyes / injection of sclera, conjunctival damage, lacrimation, anterior ischemic optic neuropathy, retinal vascular occlusion, visual field defects, mydriasis, cataracts, eye pain. Hearing impairment: vertigo, tinnitus, earache, deafness. Disorders from the blood and lymphatic system: anemia, leukopenia. Metabolic and nutritional disorders: thirst, gout, unstable diabetes, hyperglycemia, peripheral edema, hyperuricemia, hypoglycemic reaction, hypernatremia. Disorders of the musculoskeletal system: arthritis, arthrosis, myalgia, tendon rupture, tendovaginitis, bone pain, myasthenia gravis, synovitis. Disorders of the skin and subcutaneous tissues: urticaria, herpes simplex, itching, sweating, skin ulcers, contact dermatitis, exfoliative dermatitis. Disorders of the genitourinary system: cystitis, nocturia, frequent urination, gynecomastia, urinary incontinence, impaired ejaculation, genital edema, anorgasmia. Reproductive system disorders: prolonged erection and / or priapism. Drug Interaction Effect of Other Drugs on the Pharmacokinetics of Sildenafil Sildenafil metabolism occurs mainly by cytochrome CYP3A4 isoenzymes (a major pathway) and CYP2C9, therefore, inhibitors of these isoenzymes may decrease the clearance of sildenafil, and the inducers, respectively, increase the clearance of sildenafil. There was a decrease in the clearance of sildenafil with concomitant use of cytochrome CYP3A4 isoenzyme inhibitors (ketoconazole, erythromycin, cimetidine). Cimetidine (800 mg), a nonspecific cytochrome isoenzyme inhibitor of CYP3A4, when co-administered with sildenafil (50 mg), causes a 56% increase in plasma sildenafil concentration. Single administration of 100 mg of sildenafil with erythromycin (500 mg / day 2 times a day for 5 days), a specific cytochrome CYP3A4 isoenzyme inhibitor, on the background of achieving a constant erythromycin concentration in the blood, results in an increase in sildenafil AUC of 182%. When co-administered with sildenafil (100 mg once) and saquinavir (1200 mg / day 3 times daily), HIV protease inhibitor and CYP3A4 cytochrome isoenzyme, while achieving a constant saquinavir blood concentration of sildenafil Cmax increased by 140% and AUC increased by 210%. Sildenafil has no effect on the pharmacokinetics of saquinavir. Stronger cytochrome isoenzyme inhibitors of CYP3A4, such as ketoconazole and itraconazole, can also cause more severe changes in the pharmacokinetics of sildenafil. Concomitant use of sildenafil (100 mg once) and ritonavir (500 mg twice daily), an HIV protease inhibitor and a potent cytochrome P450 inhibitor, on the background of achieving a constant concentration of ritonavir in the blood leads to an increase in Cmax of 300% of sildenafil times), and the AUC is 1000% (11 times). After 24 hours, the concentration of sildenafil in the blood plasma is about 200 ng / ml (after single use of one sildenafil – 5 ng / ml), which is consistent with the information on the pronounced effect of ritonavir on the pharmacokinetics of various cytochrome P450 substrates. Sildenafil has no effect on the pharmacokinetics of ritonavir. The combined use of sildenafil with ritonavir is not recommended. If sildenafil is taken at recommended doses in patients receiving concomitantly potent cytochrome CYP3A4 isoenzyme inhibitors, then sildenafil free Cmax does not exceed 200 nm and the drug is well tolerated. Single administration of an antacid (magnesium hydroxide / aluminum hydroxide) does not affect the bioavailability of sildenafil. CYP2C9 cytochrome isoenzyme inhibitors (tolbutamide, warfarin), CYP2D6 cytochrome isoenzyme (selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazide and thiazide-like diuretics, ACE inhibitors and calcium antagonists have no effect on the pharmacokinetics of sildenafil. Azithromycin (500 mg / day for 3 days) had no effect on AUC, Cmax Tmax, excretion rate constant, and T1 / 2 of sildenafil or its major circulating metabolite. Effects of sildenafil on other drugs Sildenafil is a weak inhibitor of cytochrome P450 -1A2, 2C9, 2C19, 2D6, 2E1 and ZA4 isoenzymes (IR50> 150 μmol). When taking sildenafil at the 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 antihypertensive effect of nitrates, both with prolonged use and with acute administration. 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 7 / 7 mm Hg. 9/5 mm Hg and 8/4 mm Hg, respectively, and in the standing position – 6/6 mm Hg, 11/4 mm Hg and 4/5 mm Hg, respectively. Rare cases have been reported in such patients of symptomatic postural hypotension, manifested as dizziness (without fainting). In some sensitive patients receiving β-blockers, concomitant administration of sildenafil may lead to symptomatic hypotension.
No significant interaction with tolbutamide (250 mg) or warfarium (40 mg) metabolised by the CYP2C9 cytochrome isoenzyme has been identified.
Sildenafil (100 mg) had no effect on the pharmacokinetics of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of the CYP3A4 cytochrome isoenzyme, at constant levels in the blood. Sildenafil (50 mg) did not cause an additional increase in bleeding time with acetylsalicylic acid (150 mg). Sildenafil (50 mg) does not potentiate the antihypertensive effect of alcohol in healthy volunteers with an average blood alcohol concentration of 0.08% (80 mg / dL).
No signs of interaction of sildenafil (100 mg) with amlodipine were found in patients with hypertension. The average additional reduction in blood pressure in the supine position is 8 mm Hg. (systolic) and 7 mm Hg (diastolic).
The use of sildenafil in combination with antihypertensive agents does not lead to additional side effects.
Overdose
With single administration of Sildenafil at doses up to 800 mg, undesirable effects were comparable to those seen at lower doses, but were more common.
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 dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
Expiration
3 years.
Active substance
Sildenafil
pharmacy terms for
Dosage form
dosage form
tablets
Northern Star, Russia
