Sildenafil

When ATH:
G04BE03

Characteristic.

White or almost white crystalline powder, solubility in water 3,5 mg / ml.

Pharmacological action.
Improve erectile function.

Application.

Infringement erection.

Contraindications.

Hypersensitivity, therapy nitratami.

Restrictions apply.

Anatomical deformity of the penis (angulation, kavyernoznyi fibrosis, Peyronie's disease), disease, predisposing to the development of priapism (multiple myeloma, drepanocytemia, leukemia), increased bleeding tendency, aggravation of gastric ulcer and duodenal ulcer, hereditary retinitis pigmentosa, abnormal liver function, incl. with cirrhosis, severe renal insufficiency (Cl creatinine less than 30 ml / min), severe hypertension (BP above 170/110 mmHg.) and hypotension (HELL below 90/50 mmHg.), anamnestic indications carried in the preceding 6 months of myocardial infarction or stroke, life-threatening arrhythmias, heart failure, unstable angina, concomitant use of drugs, ингибирующих CYP3A4.

Side effects.

Side effects of sildenafil, received a dose adjustment, observed in placebo-controlled trials and marked in ≥2% of patients, taking sildenafil, with a frequency of more than placebo (in parentheses % occurrence placebo).

From the nervous system and sensory organs: headache 16% (4%), dizziness 2% (1%), flushing 10% (1%), blurred vision (change of color, sensitivity to light, blurred vision) 3% (0%).

From the respiratory system: nasal congestion 4% (2%).

On the part of the digestive tract: dyspepsia 7% (2%), diarrhea 3% (1%).

With the genitourinary system: urinary tract infection 3% (2%).

For the skin: rash 2% (1%).

Other side effects, Dating a comparable rate (more 2%) in the group treated with sildenafil and placebo groups: respiratory tract infections, backache, flu-like symptoms, arthralgia.

In studies with a fixed dose dyspepsia (17%) and blurred vision (11%) There were more common when taking sildenafil dose 100 mg compared to lower doses of. Using doses, than recommended, observed similar side effects, but with a higher frequency.

Side effects of sildenafil, observed in placebo-controlled trials and occur with a frequency of less than 2% (communication with sildenafil is not clear).

From the nervous system and sensory organs: asthenia, dizziness, migraine, hypertension, ataxia, tremor, neuralgia, weakening of reflexes, paraesthesia, gipesteziya, fainting, depression, sleep disturbance (insomnia / drowsiness), conjunctivitis, photophobia, hemorrhages in the eyeball, midriaz, Cataract, xerophthalmia, pain in the eyeballs and ears, tinnitus, deafness.

Cardio-vascular system and blood (hematopoiesis, hemostasis): hypotension, orthostatic hypotension, tachycardia, heartbeat, myocardial ischemia, angina, cardiomyopathy, heart failure, ECG changes, incl. AV блокада, cardiac arrest, cerebral thrombosis, anemia, leukopenia.

From the respiratory system: pharyngitis, sinusitis, laringit, bronchitis, dyspnoea, increase in the number of sputum, increased cough, bronchial asthma.

On the part of the digestive tract: glossitis, gingivitis, stomatitis, dry mouth, dysphagia, esophagitis, nausea, gastritis, gastroenteritis, colitis, rectal bleeding, changes in biochemical parameters of liver.

Metabolism: thirst, gipernatriemiya, gout, hyperuricemia, labilynыy diabetes, Hyper- and hypoglycemia.

With the genitourinary system: nocturia, frequent urination, cystitis, urinary incontinence, abnormal ejaculation, anorgazmija, swelling of the genitalia, gynecomastia.

On the part of the musculoskeletal system: arthritis, arthrosis, ossalgia, myalgia, myasthenia, tendon rupture, tendosinoviit, synovitis.

For the skin: hives, herpes simplex, itch, skin ulceration, contact dermatitis, exfoliative dermatitis.

Other: peripheral edema, incl. swelling of the face, pain syndromes, incl. pain in the abdomen and chest, accidental falls, wounds and injuries, Sweating, chills, photosensitivity, shock, allergic reactions.

Cooperation.

A single dose of antacid (magnesium hydroxide / aluminum hydroxide) simultaneously with sildenafil does not affect its bioavailability. Enhances the hypotensive effect of nitrates (simultaneous reception contraindicated) and antiplatelet effect of sodium nitroprusside. When concomitantly with acetylsalicylic acid (150 mg) It does not increase bleeding time. Inhibitors CYR3A4 (cimetidine, ketoconazole, itraconazole, erythromycin and others.) increase in the plasma concentration of sildenafil (in particular, cimetidine in dose 800 mg-on 56%, when taking sildenafil 50 mg) and reduce its excretion. The one-time admission 100 mg sildenafil on the background of the equilibrium concentration of erythromycin (reception on 500 mg twice daily for 5 days) Sildenafil AUC increases by 182%, against the backdrop of the equilibrium concentration of saquinavir (1200 mg 3 once a day) C_max Sildenafil increases by 140%, The AUC is on 210%. Single dose 100 mg sildenafil on the background of the equilibrium concentration of ritonavir is a powerful inhibitor of cytochrome P450 (400 mg 2 once a day), It leads to 4-fold (on 300%) increase in C_max and 11-fold (on 1000%) increase in AUC of sildenafil. Sildenafil has no effect on the pharmacokinetics of ritonavir and saquinavir. Ингибиторы CYP2C9 (tolbutamid, warfarin), CYP2D6 (selective serotonin reuptake inhibitor, tricyclic antidepressants), thiazides and thiazide diuretics, loop and potassium-sparing diuretics, ACE inhibitors, calcium antagonists, бета-адреноблокаторы и индукторы цитохрома P450 (rifampicin, barbiturates) no effect on the pharmacokinetics of sildenafil. Expected, that while taking sildenafil with inducers of CYP3A4 (rifampicin and the like.), it will decrease the plasma concentration. AUC of the active metabolite increased by sildenafil 62% When receiving loop and kalisberegath dioretikov and 102% -When receiving a nonspecific beta-adrenoblokatorov (the clinical significance of these effects is not defined). There were no signs of interaction with amlodipine (5 and 10 mg): The average additional reduction in blood pressure in the supine position (Garden at 8 mmHg., Dad on 7 mmHg.) comparable to those achieved by a single sildenafil in healthy volunteers. Not increases gipotenzivne effect of alcohol in healthy volunteers when the concentration of alcohol in blood to 80 mg / dL.

Overdose.

Symptoms: studies on healthy volunteers of the one-time admission to 800 mg sildenafil was noted increased symptoms side effects.

Treatment: symptomatic. Dialysis is ineffective because of the high degree of binding of sildenafil and its metabolite plasma proteins.

Dosing and Administration.

Inside, approximately 1 h before sexual intercourse, 50 mg. Taking into account efficiency and endurance dose can be increased to 100 mg or reduced to 25 mg. The maximum daily dose 100 mg, maximum recommended frequency reception is 1 once a day.

Precautions.

Before taking to diagnose erectile dysfunction, determining its possible causes and the selection of adequate treatment is necessary to build a complete medical history and conduct a thorough physical examination, and urological, particularly in patients with underlying cardiovascular disease, which increased sexual activity is undesirable (eg, in severe forms of coronary artery disease and hypertension). Patients older 65 years, with hepatic and severe renal insufficiency (Cl creatinine less than 30 ml / min), as well as the simultaneous use of inhibitors of cytochrome P450 3A4 (Erythromycin, ketoconazole, itraconazole, saquinavir and others.), starting dose is 25 mg. If you are receiving maximum single dose of ritonavir should not exceed 25 mg for 48 no.

There are post-marketing reports of rare cases of erection, continued from above 4 no, and priapism, require immediate medical attention to prevent damage to the tissues of the penis and irreversible impotence.

Safety while taking sildenafil with other agents for the treatment of erectile dysfunction has not been studied, simultaneously is not recommended.

It is not indicated for use in neonates, Children and women.