Sildenafil Cardio tablets coated. 20 mg 90 pcs. (sildenafil)

Description

Tablets, pink-coated, round, double. In a cross section, the tablet core is white or almost white.

Pharmacological action

Sildenafil is a powerful selective inhibitor of cycloguanosine monophosphate (cGMP) - specific phosphodiesterase-5 (PDE5). Since PDE5, responsible for the breakdown of cGMP, is contained not only in the cavernous body of the penis, but also in the vessels of the lungs, sildenafil, being an inhibitor of this enzyme, increases the content of cGMP in the smooth muscle cells of the pulmonary vessels and causes their relaxation. In patients with pulmonary hypertension (LH), the administration of sildenafil leads to the expansion of the vessels of the lungs and, to a lesser extent, other vessels. Sildenafil is selective for PDE5 in vitro. Its activity in relation to PDE5 is superior to activity against other known phosphodiesterase isoenzymes: PDE6, which is involved in the transmission of the light signal in the retina of the eye - 10 times PDE1 - 80 times PDE2, PDE4, PDE7-PDE11 - more than 700 times. The activity of sildenafil in relation to PDE5 is more than 4000 times higher than its activity against PDEZ, cAMP-specific phosphodiesterase, which is involved in heart contraction. Sildenafil causes a slight and transient decrease in blood pressure (BP), which in most cases is not accompanied by clinical symptoms. After oral administration of sildenafil in a dose of 100 mg, the maximum decrease in systolic and diastolic blood pressure in the supine position averaged 8.3 mm Hg. and 5.3 mmHg, respectively. After taking sildenafil at a dose of 80 mg 3 times a day, healthy male volunteers showed a maximum decrease in systolic and diastolic blood pressure in the supine position by an average of 9.0 mm Hg. and 8.4 mmHg, respectively. After taking sildenafil at a dose of 80 mg 3 times a day in patients with systemic arterial hypertension, systolic and diastolic blood pressure decreased by an average of 9.4 mm Hg. and 9.1 mmHg, respectively. In patients with PH who received 80 mg sildenafil 3 times a day, the decrease in blood pressure was less pronounced: systolic and diastolic blood pressure decreased by 2 mm RT. Art. With a single oral dose of up to 100 mg by healthy volunteers, sildenafil did not significantly affect the electrocardiogram (ECG). When using the drug at a dose of 80 mg 3 times a day in patients with LH, clinically significant ECG changes were not detected. When studying the hemodynamic effects of sildenafil with a single oral dose of 100 mg in 14 patients with severe coronary atherosclerosis (stenosis of at least one coronary artery more than 70%), the mean systolic and diastolic blood pressure at rest decreased by 7% and 6%, respectively compared to baseline. Systolic pressure in the pulmonary artery decreased by an average of 9%. Sildenafil did not affect cardiac output and did not impair blood flow in stenosed coronary arteries. In some patients, 1 hour after taking sildenafil at a dose of 100 mg using the Fansworth-Munsel 100 test, a slight and transient impairment of color perception ability (blue / green) was detected 2 hours after taking the drug, these changes disappeared. It is believed that color vision impairment is caused by the inhibition of PDE6, which is involved in the transmission of light in the retina of the eye. Sildenafil does not affect visual acuity, contrast perception, electroretinography data, intraocular pressure or pupil diameter. In patients with confirmed initial age-related macular degeneration, sildenafil, when taken once at a dose of 100 mg, did not cause significant changes in visual functions, in particular, visual acuity measured using the Amsler lattice, the ability to distinguish traffic light colors, evaluated by the Humphrey perimetry method, and transient visual impairment assessed using the photostress method. Efficacy in adult patients with LH The efficacy of sildenafil in 278 patients with primary LH (63%), LH associated with systemic connective tissue diseases (30%), and LH developed after surgical treatment of congenital heart defects (7%) was studied. Most patients had II (107 39%) or III (160 58%) LH functional class according to the World Health Organization (WHO) classification, less often I (1 0.4%) or IV (9 3%) functional classes were determined. Patients with a left ventricular ejection fraction of less than 45% or a left ventricular shortening fraction of less than 0.2 were not included in the study, as well as patients for whom bosentan therapy was ineffective. Sildenafil in doses of 20 mg, 40 mg or 80 mg was used together with standard therapy (patients in the control group received placebo). The primary endpoint was increased exercise tolerance using the 6-minute walk test 12 weeks after starting treatment. In all three groups of patients receiving sildenafil in different doses, it significantly increased compared with placebo. The increase in the distance traveled (adjusted for placebo) was 45 m, 46 m and 50 m in patients receiving sildenafil in doses of 20 mg, 40 mg and 80 mg, respectively. No significant differences were found between groups of patients taking sildenafil. An improvement in the results of the 6-minute walk test was noted after 4 weeks of therapy. This effect persisted at the 8th and 12th weeks of therapy. The average therapeutic effect was consistently observed in the results of the 6-minute walk test in all sildenafil groups compared with placebo in patient populations specially selected for the following characteristics: demographic, geographical and disease characteristics. The basic parameters (walking test and hemodynamics) and effects were mainly similar in groups of patients with PH of various functional classes according to WHO and various etiologies. A statistically significant increase in the results of the 6-minute walk test was observed in the group of patients receiving 20 mg of sildenafil. For patients with PH of functional classes II and III, the improvement in the 6-minute walk test, adjusted for placebo, is 49 m and 45 m, respectively. In patients receiving sildenafil in all doses, mean pulmonary pressure significantly decreased compared with placebo. In patients receiving sildenafil in doses of 20 mg, 40 mg and 80 mg, the decrease in pressure in the pulmonary artery adjusted for the placebo effect was: 2.7 mm RT. Art., 3.0 mm RT. Art. and 5.1 mmHg. Art. respectively. In addition, an improvement was found in the following indicators: pulmonary vascular resistance, pressure in the right atrium and cardiac output. Changes in heart rate and systemic blood pressure were minor. The degree of decrease in pulmonary vascular resistance exceeded the degree of decrease in peripheral vascular resistance. Patients receiving sildenafil showed a tendency to improve the clinical course of the disease, in particular, a decrease in the frequency of hospitalizations for PH. The proportion of patients whose condition has improved, at least one functional class according to the WHO classification for 12 weeks in the sildenafil groups was higher (28%, 36% and 42% of patients who received sildenafil in doses of 20 mg, 40 mg and 80 mg, respectively) than in the placebo group (7%) . In addition, treatment with sildenafil compared with placebo led to an improvement in the quality of life, especially in terms of physical activity, and a trend towards an improvement in the Borg's dyspnea index. The percentage of patients who had to add another class of drug to standard therapy was higher in the placebo group (20%) than in the groups of patients receiving sildenafil in doses of 20 mg (13%), 40 mg (16%) and 80 mg ( 10 %). Information on long-term survival A long-term study found that sildenafil increased the survival of patients with PH. Efficacy in adult patients with LH when combined with epoprostenol. The efficacy of sildenafil was studied in 267 patients with a stable course of LH on the background of intravenous administration of epoprostenol. The study included patients with primary LH and LH associated with systemic connective tissue diseases. Patients were randomized to placebo and sildenafil groups (with a fixed selection of doses, starting with a dose of 20 mg, up to 40 mg and then 80 mg, 3 times a day) with combination therapy with intravenous administration of epoprostenol. The primary endpoint was an increase in exercise tolerance by the 6 minute walk test 16 weeks after the start of treatment. The increase in the distance covered in the sildenafil group was 30.1 m versus 4.1 m in the placebo group. In patients taking sildenafil, the average pressure in the pulmonary artery significantly decreased by 3.9 mm RT. Art. compared to the placebo group. Clinical outcomes Sildenafil therapy significantly increased the time to clinical deterioration of LH compared with placebo. According to Kaplan-Mayer, in patients receiving placebo, the risk of worsening was three times higher (the proportion of patients with worsening in the placebo group was 0.187 (0.12-0.26), and in the sildenafil treatment group, 0.062 (0, 02-0.10), confidence interval 95%). The time period until clinical deterioration was defined as the time from randomization of patients to the first signs of deterioration (death, lung transplantation, initiation of bosentan therapy, or change in epoprostenol dose due to clinical deterioration). In 23 patients from the placebo group, signs of clinical deterioration were noted (17.6%), while in the sildenafil group, worsening was noted in 8 patients (6%). In patients with primary LH, an average deviation in the 6-minute walk test was noted: with simultaneous use with sildenafil - 26.39 m, with placebo - 11.84 m. In patients with LH associated with systemic connective tissue diseases - 18, 32 and 17.5 m respectively. Efficacy and safety of sildenafil use in adult patients with PH (with simultaneous use with bosentan) In general, the side effect profile in the two groups (simultaneous use of sildenafil and bosentan and bosentan monotherapy) was the same and corresponded to the side effect profile when using sildenafil.

Indications

Pulmonary hypertension.

Contraindications

Hypersensitivity to any component of the drug. Veno-occlusive disease of the lungs. Joint use with nitric oxide donors or nitrates in any form. Concomitant use with potent inhibitors of the CYP3A4 isoenzyme (including ketoconazole, itraconazole and ritonavir) (see Interaction with other drugs section). The combined use of PDE5 inhibitors, including sildenafil, with antihypertensive agents - guanylate cyclase stimulants, such as riotsiguat, as this can lead to symptomatic arterial hypotension. Loss of vision in one eye due to anterior non-arteritic ischemic neuropathy of the optic nerve, hereditary degenerative diseases of the retina of the eye (retinitis pigmentosa). Severe impairment of liver function (more than 9 points on the Child-Pugh scale). A history of stroke or myocardial infarction. Severe arterial hypotension (systolic blood pressure less than 90 mm Hg, diastolic blood pressure less than 50 mm Hg). Lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome. Age up to 18 years (studies of efficacy and safety have not been conducted). With caution: I or IV (efficacy and safety not established) functional classes of PAH. Anatomical deformation of the penis (angulation, cavernous fibrosis or Peyronie's disease) and diseases predisposing to the development of priapism (sickle cell anemia, multiple myeloma, leukemia). Diseases accompanied by bleeding, or exacerbation of peptic ulcer of the stomach and duodenum. Heart failure, unstable angina, life-threatening arrhythmias, arterial hypertension (BP> 170/100 mm Hg), left ventricular outlet tract obstruction (aortic stenosis, hypertrophic obstructive cardiomyopathy), a rare syndrome of multiple systemic atrophy, manifested by a severe violation of the regulation of blood pressure by the autonomic nervous system, hypovolemia. Anterior non-arteritic ischemic neuropathy of the optic nerve in history. Concomitant use with moderate inhibitors of the CYP3A4 isoenzyme (including erythromycin, saquinavir, clarithromycin, telithromycin and nefazodone) and -Adrenoblockers. Joint use with inducers of CYP3A4 isoenzyme.

Recommended use for

Inside. The recommended dose of Sildenafil Cardio is 20 mg 3 times a day with an interval of about 6-8 hours, regardless of food intake. The maximum recommended dose is 60 mg. Impaired renal function Dose adjustment is not required, however, with poor tolerability of the drug, the dose is reduced to 20 mg 2 times a day. Impairment of liver function Dose adjustment in patients with mild or moderate impairment of liver function (5-9 points on the Child-Pugh scale) is not required, however, if the drug is poorly tolerated, the dose is reduced to 20 mg 2 times a day. In patients with severe hepatic impairment (more than 9 points on the Child-Pugh scale), the use of the drug has not been investigated (see section Contraindications). Elderly patients ( 65 years of age) Dose adjustment not required. Children The use of sildenafil in children under the age of 18 is not recommended (insufficient data on efficacy and safety). Use in patients receiving concomitant therapy The combined use of sildenafil and epoprostenol is considered in the sections Pharmacodynamics and Side effects. Controlled studies to evaluate the efficacy and safety of sildenafil in combination with other drugs (bosentan, iloprost) have not been conducted to treat pulmonary hypertension. Combined therapy with Sildenafil Cardio with these drugs should be carried out with caution, it may be necessary to adjust the dose of sildenafil. However, there is no evidence of the need to increase the dose of sildenafil with simultaneous use with bosentan. The efficacy and safety of using Sildenafil Cardio in combination with other PDE5 inhibitors in patients with pulmonary arterial hypertension has not been studied. The simultaneous use of sildenafil with potent inhibitors of the CYP3A4 isoenzyme (e.g. ketoconazole, itraconazole, ritonavir) is not recommended. However, if such a combination is necessary, the dose of Sildenafil Cardio should be reduced to 20 mg 2 times a day in patients who already receive such CYP3A4 isoenzyme inhibitors as erythromycin and saquinavir. If necessary, the simultaneous use with more powerful inducers of the CYP3A4 isoenzyme, such as clarithromycin, telithromycin and nefazodone, the dose of Sildenafil Cardio should be reduced to 20 mg once a day.

Composition

1 film-coated tablet contains: active ingredient: sildenafil citrate - 28, 1 mg (in terms of sildenafil - 20 mg) excipients (core): microcrystalline cellulose - 50.0 mg croscarmellose sodium (primellose) - 7.5 mg, povidone K-30 (medium molecular weight polyvinylpyrrolidone) - 4.5 mg, lactose monohydrate (milk sugar) - 58.4 mg magnesium stearate - 1.5 mg excipients (shell): hypromellose - 2.39988 mg polysorbate-80 (tween-80) - 1.09994 mg talc - 0.99995 mg titanium dioxide E 171 - 0.49998 mg dye carmuazine (azorubine) - 0.00025 mg.

Side effects

Side effects are distributed according to the MedDRA classification system according to organ systems and frequency: very frequent (> 1/10), frequent (> 1/100, <1/10), rare (> 1/1000. <1 / 100), very rare (<1/1000), the frequency is unknown (the frequency cannot be determined based on available data). Infections and infestations: Frequent: inflammation of the subcutaneous tissue, influenza, unspecified sinusitis. On the part of the blood system and lymphatic system: Frequent: unspecified anemia. Metabolism and nutrition: Frequent: fluid retention (edema). Mental disorders: Frequent: insomnia, anxiety. From the central nervous system: Very frequent: headache. Frequent: tremor, paresthesia, unspecified burning sensation, hypoesthesia. Frequency unknown: migraine. From the side of the organ of vision: Frequent: hemorrhage in the retina of the eye, unspecified visual impairment, blurred vision, photophobia, chromatopsia, cyanopsia, eye inflammation, redness of the eyes. Rare: decreased visual acuity, diplopia, impaired eye sensitivity. On the part of the organ of hearing and labyrinth disorders: Frequent: vertigo. Frequency unknown: sudden deafness. Vascular disorders: Very frequent: hyperemia (redness of the skin of the face). Frequency unknown: decrease in blood pressure. From the respiratory system, chest and mediastinum: Frequent: unspecified bronchitis, nosebleeds, unspecified rhinitis, cough, nasal congestion. From the gastrointestinal tract: Very frequent: diarrhea, dyspepsia. Frequent: unspecified gastritis, unspecified gastroenteritis, gastroesophageal reflux disease, hemorrhoids, bloating, dry oral mucosa. On the part of the skin and subcutaneous tissues: Frequent: alopecia, erythema, increased sweating at night. Frequency unknown: skin rash. From the musculoskeletal system and connective tissue: Very frequent: pain in the limbs. Frequent: myalgia, back pain. From the reproductive system and mammary gland: Frequent: gynecomastia, hemospermia. Frequency unknown: priapism, prolonged erection. General disorders and reactions at the injection site: Frequent: fever. The total frequency of discontinuation of sildenafil treatment at a recommended dose of 20 mg 3 times a day was low and did not differ from that in the placebo group (2.9%). In a placebo-controlled study, the effect of adjuvant therapy with sildenafil was studied as an adjunct to the intravenous administration of epoprostenol. 134 patients with PAH received sildenafil in daily doses from 20 mg to 80 mg 3 times a day and epoprostenol, and 131 patients received placebo and epoprostenol. The duration of treatment was 16 weeks. The overall frequency of discontinuation of therapy due to adverse events in the sildenafil / epoprostenol group was 5.2% compared with 10.7% in the placebo / epoprostenol group.

Overdose

Symptoms: headache, flushing of the face, dizziness, dyspepsia, nasal congestion, visual impairment. Treatment: symptomatic. Hemodialysis is ineffective (sildenafil actively binds to plasma proteins).

Storage conditions

In a dark place at a temperature of no higher than 25 ° C.

Expiration

3 years. Do not use after the expiry date stated on the packaging.

Deystvuyuschee substances

sildenafil

Dosage form

tablet



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