Maksigra tab n / 100mg film about 4 pc

Description

Composition
Active substance:
1 tablet contains (mg) of sildenafil citrate, sildenafil equivalent – 35.12 mg (25.0 mg) 70.24 mg (50.0 mg) and 140.48 mg (100.0 mg) ;.
Excipients:
1 tablet contains (mg) Tablet core Mannitol – 35.38 mg; 70.76 mg; 141.52 mg; crospovidone – 3.00 mg; 6.00 mg; 12.00 mg; Povidone – 3.00 mg; 6.00 mg; 12.00 mg; corn starch – 5.00 mg; 10.00 mg; 20.00 mg; colloidal silicon dioxide – 1.00 mg; 2.00 mg; 4.00 mg; Sodium lauryl sulfate – 1.00 mg; 2.00 mg; 4.00 mg; magnesium stearate – 1.50 mg; 3.00 mg; 6.00 mg. sheath: hypromellose – 2.36 mg; 4.13 mg; 5.90 mg; macrogol-6000 – 0.74 mg; 1.30 mg; 1.85 mg; titanium dioxide – 0.52 mg; 0.90 mg; 1.30 mg; talc – 0.24 mg; 0.43 mg; 0.60 mg; indigo carmine (E-132) – 0.14 mg; 0.24 mg; 0.35 mg.
Description:
Tablets, film-coated cyan, round, biconvex.
Product form:
Tablets, film-coated 25 mg, 50 mg, 100 mg According 1,4 tablets were placed in a foil blister Al / PVC / PVDC.
1 blister together with instructions for use placed in a pile of cardboard.
Contraindications
Hypersensitivity to the sildenafil, or any other component of the preparation.
Use in patients receiving continuously or intermittently nitric oxide donator, organic nitrates or nitrites in any form as sildenafil enhances the hypotensive effect of nitrates (see. See “The interaction with other drugs”).
The safety and efficacy of sildenafil when used together with other agents in the treatment of erectile dysfunction have not been studied, so the use of such combinations is not recommended (see. Section “Special Instructions”).
For registered indications Sildenafil is not intended for use in children under 18 years old.
For registered indications Sildenafil is not intended for use in women.
Carefully
The anatomical deformity of the penis (including the angulation, cavernous fibrosis or disease
Peyronie’s) (see. “Special Instructions” section).
Diseases that predispose to the development of priapism (sickle-cell anemia, multiple myeloma, leukemia, thrombocytopenia) (see. Section “Special Instructions”). Patients with episodes of anterior ischemic optic neuropathy, non-inflammatory genesis in history.
Diseases accompanied by bleeding.
Aggravation of gastric ulcer and duodenal ulcer.
Hereditary retinitis pigmentosa (see. “Special Instructions” section)
Heart failure, unstable angina, transferred in the last 6 months of myocardial infarction, stroke or life-threatening arrhythmia, hypertension (blood pressure> 170/100 mm Hg. V.) Or hypotension (blood pressure
Simultaneous treatment with alpha-blockers.
Indications
Treatment of erectile dysfunction characterized by the inability to achieve or maintain an erection of the penis, achieve or maintain penile erection sufficient for satisfactory sexual intercourse. The drug is effective only during sexual stimulation.
Interaction with other drugs
The effect of other drugs on the metabolism stdenafila
Sildenafil is metabolized mainly in the liver by the action of isozymes CYP3A4 (major route) and CYP2C9 (secondary path), so inhibitors of these isozymes may reduce the clearance of sildenafil.
When combined with inhibitors of isoenzyme CYP3A4 (such as ketoconazole, erythromycin, cimetidine) decreased clearance of sildenafil.
A single dose of sildenafil at a dose of 100 mg together with erythromycin, a specific inhibitor of isozyme CYP3A4 (in a dose of 500 mg 2 times a day for 5 days), in conditions of equilibrium concentration of erythromycin increases the AUC of sildenafil in 182%.
Cimetidine (800 mg), which is an inhibitor of cytochrome P450 and a nonspecific inhibitor of isozyme CYP3A4, when used together with sildenafil (50 mg) in healthy volunteers induced increase in plasma sildenafil concentration of 56%. The simultaneous use of sildenafil (single dose 100 mg), and the HIV protease inhibitor ritonavir (500 mg, 2 times a day), a potent inhibitor of cytochrome P450, in conditions of equilibrium concentrations of ritonavir in the blood leads to an increase in Cmax of sildenafil in 300% (at 4 times), a AUC sildenafil – 1000% (11 -fold). After 24 hours the concentration of sildenafil in plasma was about 200 ng / ml, compared with approximately 5 ng / ml when used alone sildenafil. The simultaneous use of sildenafil (single dose 100 mg), and the HIV protease inhibitor saquinavir, an inhibitor of isozyme CYP3A4, in the equilibrium concentration conditions (at a dose of 1200 mg 3 times daily) resulted in an increase Stdh sildenafil in 140%, a AUC sildenafil – on 210%. Sildenafil had no effect on the pharmacokinetics of saquinavir.
More potent inhibitors isoenzyme CYP3A4, such as itraconazole and ketoconazole, may cause more pronounced changes sildenafil pharmacokinetics.
CYP2C9 inhibitors (such as tolbutamide, warfarin, phenytoin), inhibitors of CYP2D6 (e.g., selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazides and thiazide diuretics, “loop” and potassium-sparing diuretics, angiotensin converting enzyme inhibitors, beta-blockers, calcium antagonists and CYP450 metabolism inducers (e.g. rifampicin, barbiturates) have no effect on the pharmacokinetics of sildenafil.
A single dose of antacid (hydroxide / magnesium hydroxide, aluminum) did not affect the bioavailability of sildenafil.
In healthy male volunteers simultaneous reception of azithromycin (500 mg daily for 3 days) did not affect the AUC, Cmax, rmax, and the elimination rate constant Tyr sildenafil or its main circulating metabolite.
Grapefruit juice is a weak inhibitor of CYP3A4 metabolism in the wall of the gastrointestinal tract and can cause moderate increase in the concentration of sildenafil in the blood plasma.
The effect of sildenafil on other drugs
Sildenafil is a weak inhibitor of cytochrome P450 isoenzymes – 1A2, and ZA4 2S9,2S19,2D6,2E1 (IKzo150 mol). It is unlikely that sildenafil can affect the clearance of substrates of these isoenzymes.
Sildenafil increases the hypotensive effects of nitrates, however its combined use with nitric oxide donators or nitrates in any form is contraindicated.
In certain sensitive patients treated with alpha-adrenergic blockers, the simultaneous use of sildenafil may result in symptomatic hypotension. When simultaneous administration of alpha-adrenergic blocker doxazosin (4 mg and 8 mg) and sildenafil (25 mg, 50 mg and 100 mg) in patients with benign prostatic hyperplasia with stable haemodynamics average additional reduction in systolic / diastolic blood pressure in a supine position, was 7.7 mmHg. st., 9/5 mm Hg. Art. and 8/4 mm Hg. Art., Respectively, while standing in the position of – 6.6 mm Hg. st., 11/4 mm Hg. Art. and 4/5 mm Hg. Art., respectively. It reported rare cases of such patients symptomatic orthostatic hypotension, manifested in the form of dizziness (without fainting).
No evidence of significant interaction sildenafil (50 mg) or combined with tolbutamide (250 mg) or warfarin (40 mg) are metabolized by CYP2C9, is not revealed.
Sildenafil (100 mg) had no effect on the pharmacokinetic parameters VIChproteazy inhibitors in an equilibrium state, such as saquinavir and ritonavir are simultaneously substrates CYP3A4.
Sildenafil (50 mg) did not cause an additional increase in bleeding time caused by the admission of acetylsalicylic acid (150 mg).
Sildenafil (50 mg) did not enhance the hypotensive effect of alcohol in healthy volunteers at the maximum blood concentration of alcohol in average 80 mg / dl.
Patients with signs of hypertension interaction sildenafil (100 mg) with amlodipine was not revealed. The average additional reduction in blood pressure in the supine position is: systolic – 8 mm Hg. Art., Diastolic – by 7 mmHg. Art.
The use of sildenafil in combination with antihypertensive drugs does not lead to additional side effects.
Overdose
In single dose of the drug at a dose of 800 mg in studies in healthy volunteers, adverse events were comparable to those when taking sildenafil at lower doses but the frequency and severity increased.
Sildenafil 200 mg dose did not increase efficiency, but increases the frequency of adverse events (headache, “flushing” of blood to the face, dizziness, dyspepsia, nasal congestion, visual disturbances).
Treatment: symptomatic. It does not appear in hemodialysis.
pharmachologic effect
Pharmacological group:
Erectile dysfunction treatment for – FDE5- inhibitor.
Pharmacodynamics:
Sildenafil – a drug for the treatment of erectile dysfunction. When sexual stimulation restores impaired erectile function by increasing blood flow to the penis.
Sildenafil is a potent and selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5). Sildenafil has no direct relaxing action on isolated corpus cavernosum, but enhances actively relaxing effects of nitric oxide (NO) in this tissue, by inhibiting PDE5, which is responsible for the breakdown of cGMP in the cavernous body. When the activation of the NO / cGMP PDE-5 inhibition under the influence of sildenafil increases the levels of cGMP in the cavernous body, resulting in muscle relaxation and increased blood flow in the cavernous body. The pharmacological effect is achieved only if there is sexual stimulation. Activity against PDE5 10-10,000 times greater activity against other PDE isoenzymes (1-11).
In clinical studies it was shown that the average time to achieve an erection resistant 60% (sufficient for sexual intercourse) was 25 minutes (range 12 to 37 minutes).
Some patients after 1 hour after dosing at a dose of 100 mg via Famsworth-Munsell 100 test revealed mild and transient impaired ability to distinguish colors (blue / green), after 2 hours after ingestion, these changes were absent. Mechanism of color vision disturbances believe inhibition of PDE6, which is involved in the transmission of light in the retina. Sildenafil has no effect on visual acuity, contrast perception, electroretinogram, intraocular pressure or the pupil diameter.
In healthy volunteers after a single dose of sildenafil 100 mg effects on sperm motility or morphology were noted.
Pharmacokinetics:
Suction
After oral administration, sildenafil is rapidly absorbed. Absolute bioavailability is on average 41% (range 25-63%). The maximum concentration (C max) in plasma after a single 100 mg fasted drug inside is 18 ng / ml (38 nM) and is achieved within 30 to 120 minutes (median 60 minutes).
When receiving the sildenafil together with fatty food Cmax is reduced by 20-40% and 1.5- 3 reached after hours.
Distribution
The volume of distribution (Vd) of sildenafil in the equilibrium state is on average 105 liters.
Sildenafil and its main circulating metabolite N-desmetilny about 96 g% bound to plasma proteins. Protein binding does not affect the overall concentration of the drug.
In healthy volunteers receiving sildenafil (single dose 100 mg), 90 minutes after administration was determined in sperm less than 0.0002% (average 188 ng) of the administered dose.
Metabolism
Sildenafil is metabolized mainly liver microsomal isozymes CYP3A4 (major route) and CYP2C9 (minor route). Tsirkuliruschy main metabolite formed from sildenafil by N-demethylation. This metabolite has the profile of selectivity for phosphodiesterase similar to that of sildenafil and its activity against PDE5 in vitro is approximately 50% of the initial activity of the drug. The concentration of this metabolite in the plasma is about 40% of the concentration of sildenafil. The N-desmethyl metabolite is metabolized further, with its half-life (Tyr) is about 4 hours.
breeding
Total clearance of sildenafil is 41 l / h, and T1L to the terminal phase -. 5.3 h after oral administration of sildenafil is derived mainly as metabolites intestine (about 80% of the dose) and to a lesser extent by the kidneys (approximately 13% of the dose). Pharmacokinetics in special clinical situations
elderly patients
In the elderly (over 65 years) patients sildenafil clearance was reduced, and the concentration of free active substance in plasma is approximately 40% higher than its concentration in young (18-45 years) patients.
Patients with renal insufficiency
In renal failure light (CC 50-80 ml / min) and average (CC 30-49 ml / min), the severity of pharmacokinetic parameters after oral administration of sildenafil once (50 mg) was not changed.
In renal failure, severe gravity (CC
Patients with hepatic insufficiency
Patients with mild to moderate hepatic cirrhosis (class A and B on a scale Chayld- Pyo) sildenafil clearance is reduced, leading to an increase in AUC (84%) and Cmax (47%) compared with those indices in normal liver function in patients the same age group.
The pharmacokinetic parameters of sildenafil in patients with severe hepatic impairment have not been studied.
Pregnancy and breast-feeding
Sildenafil is not intended for use in women.
Conditions of supply of pharmacies
Drug prescription.
side effects
The frequency of side effects is given in accordance with the following classification: very often (> 1/10), often (> 1/100
special instructions
Before the appointment of treatment is necessary to gather medical history and conduct a physical examination to diagnose erectile dysfunction and determine possible causes of its development.
Means the treatment of 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 the development of priapism (sickle-cell anemia, multiple myeloma, leukemia) (see. Section ”
Carefully “).
In the case of maintaining an erection more than 4 hours should seek immediate medical attention.
If priapism treatment is not carried out in due time, it may cause damage to the tissues of the penis and irreversible loss of potency.
Preparations for the treatment of erectile dysfunction, should not be given to men for whom sexual activity is undesirable.
Because sexual activity is a risk in the presence of heart disease, before beginning any therapy for erectile dysfunction doctor should refer the patient to the examination of the cardiovascular system of patients.
Sexual activity is undesirable in patients with heart failure, unstable angina, transferred in the last 6 months of myocardial infarction or stroke, life-threatening arrhythmias, hypertension (blood pressure> 170/100 mm Hg. Art.) Or hypotension (blood pressure
In clinical studies have shown no difference in the incidence of myocardial infarction (1.1 per 100 person-years), or the frequency of death from cardiovascular disease (0.3 per 100 person-years) in patients receiving sildenafil compared with patients placebo.
Cardiovascular complications
During post-marketing use of sildenafil for the treatment of erectile dysfunction was reported adverse events such as severe cardiovascular events (including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, hemorrhagic stroke, transient ischemic attack, hypertension and hypotension ) which have a temporary connection with the use of sildenafil. The majority 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 observed after administration of sildenafil without subsequent sexual activity. It is not possible to establish a direct link between the reported adverse events and indicated or other factors.
hypotension
Viagra has systemic vasodilatory effect resulting in a transient decrease in blood pressure that is not clinically significant phenomenon and does not lead to any consequences in most patients. However, before prescribing sildenafil physician should carefully assess the risk of potential adverse manifestations vasodilating action in patients with relevant diseases, especially against sexual activity.
Increased susceptibility to vasodilators observed in patients with obstruction of the left ventricular outflow tract (e.g., aortic stenosis, hypertrophic obstructive cardiomyopathy), and is rarely encountered with multiple system atrophy syndrome, manifesting severe impairment of blood pressure regulation of the autonomic nervous system.
Sildenafil should be used with caution in patients receiving alpha blockers, since their combined use can lead to symptomatic hypotension in certain sensitive patients.
The most likely to develop this effect during 4 hours after administration of sildenafil. To minimize the risk of postural hypotension in patients taking alfaadrenoblokatory, treatment with sildenafil should be started after the stabilization of hemodynamic parameters in these patients. Следует также рассмотреть целесообразность снижения начальной дозы силденафила. Врач должен проинформировать пациентов, какие действия следует предпринять в случае появления симптомов постуральной гипотензии.
Зрительные нарушения
При применении всех ингибиторов ФДЭ5, в том числе силденафила были отмечены редкие случаи развития передней ишемической нейропатии зрительного нерва невоспалительного генеза, как причины ухудшения или потери зрения. Большинство этих пациентов имели факторы риска, такие как снижение отношения диаметров экскавации и диска зрительного нерва («застойный диск»), возраст старше 50 лет, сахарный диабет, артериальная гипертензия, ишемическая болезнь сердца, гиперлипидемия и курение. В случае внезапного ухудшения зрения пациенту следует рекомендовать прекратить прием силденафила и незамедлительно проконсультироваться с врачом.
У небольшого числа пациентов с наследственным пигментным ретинитом имеются генетически детерминированные нарушения функций фосфодиэстераз сетчатки глаза. Сведения о безопасности применения силденафила у пациентов с пигментным ретинитом отсутствуют.
Нарушение слуха
В некоторых постмаркетинговых и клинических исследованиях сообщается о случаях внезапного ухудшения или потери слуха, связанных с применением всех ингибиторов ФДЭ5, включая силденафил.
Большинство этих пациентов имели факторы риска внезапного ухудшения или потери слуха. Причинноследственной связи между применением ингибиторов ФДЭ5 и внезапным ухудшением или потерей слуха не установлено. В случае внезапного ухудшения или потери слуха на фоне приема силденафила следует немедленно проконсультироваться с врачом.
Кровотечения
Силденафил усиливает антиагрегантный эффект нитропруссида натрия, донатора оксида азота, на тромбоциты человека in vitro. Данные о безопасности применения силденафила у пациентов со склонностью к кровоточивости или обострением язвенной болезни желудка и 12-перстной кишки отсутствуют, поэтому силденафил у этих пациентов следует применять с осторожностью (см. раздел «
Carefully “). Частота носовых кровотечений у пациентов с ЛГ, связанной с диффузными заболеваниями соединительной ткани, была выше (силденафил 12,9%, плацебо 0%), чем у пациентов с первичной легочной гипертензией (силденафил 3,0%, плацебо 2,4%). У пациентов, получавших силденафил в сочетании с антагонистом витамина К, частота носовых кровотечений была выше (8,8%), чем у пациентов, не принимавших антагонист витамина К (1,7%).
Применение совместно с другими средствами лечения нарушений эрекции Безопасность и эффективность комбинированного применения силденафила с другими ингибиторами ФДЭ5, или другими препаратами для лечения легочной гипертензии, содержащими силденафил, или другими средствами лечения эректильной дисфункции не изучалась, поэтому применение подобных комбинаций не рекомендуется.
Влияние на способность к управлению транспортными средствами и работе с механизмами.
Влияние силденафила на способность управлять автомобилем и выполнять работу, требующую повышенного внимания, не изучалось.
Однако в период приема препарата необходимо соблюдать осторожность при вождении автотранспорта и занятии потенциально опасными видами деятельности, требующими повышенной концентрации внимания и быстроты психомоторных реакций, т.к. возможно головокружение и нарушение зрения.
Storage conditions
At a temperature of not higher than 30 ° C.
Keep out of the reach of children.
Dosing and Administration
Внутрь, примерно за 1 ч до планируемой сексуальной активности. Максимальная рекомендуемая кратность применения – один раз в сутки.
Разовая доза для взрослых – 50 мг 1 раз в сутки. С учетом эффективности и переносимости доза может быть увеличена до 100 мг или снижена до 25 мг. Максимальная разовая доза – 100 мг.
При приеме силденафила совместно с жирной пищей начало его действия может быть отсрочено по сравнению с приемом натощак.
Use in elderly patients
У пожилых пациентов коррекции дозы не требуется.
Применение у пациентов с нарушением функции почек
При почечной недостаточности легкой и средней степени тяжести (КК 30-80 мл/мин) корректировка дозы не требуется, при почечной недостаточности тяжелой степени тяжести (КК
С учетом эффективности и переносимости доза может быть повышена до 50 мг и 100 мг.
Применение у пациентов с нарушением функции печени
При нарушениях функции печени дозу препарата следует снизить до 25 мг.
С учетом эффективности и переносимости доза может быть повышена до 50 мг и 100 мг. Применение у пациентов, получающих другие лекарственные препараты За исключением ритонавира, с которым совместное введение силденафила не рекомендуется, у пациентов, получающих сопутствующее лечение ингибиторами изофермента CYP3A4, начальная доза должна составлять 25 мг.
Чтобы свести к минимуму возможность развития ортостатической гипотензии у пациентов, принимающих альфа-адреноблокаторы, лечение силденафилом следует начинать после стабилизации гемодинамики у этих пациентов. Кроме того, следует рассмотреть Целесообразность назначения силденафила в начальной дозе 25 мг.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist