Potential 4's 50 mg coated tablets

The instruction for medical use of medicine POTENTIAL the Trade name Potential the International unlicensed name Sildenafil Lekarstvennaya the Tablet form, coated 50 mg and 100 mg One tablet contains Structure: active agent: sildenafit – 50 mg or 100 mg (in the form of a sildenafil of citrate), excipients: microcrystalline cellulose, sodium of a kroskarmelloz, gipromelloz, magnesium stearate, silicon dioxide colloidal, titan dioxide (E 171), talc, propylene glycol, polyethyleneglycol 6000 (macrogoal 6000), indigo carmine (E 132). The description of the Tablet of round shape, coated, blue (for a dosage of 50 mg) or blue (for a dosage of 100 mg) colors, upper and lower surfaces of which convex. On a break when examining under a magnifying glass the kernel surrounded with one continuous layer is visible. Pharmacotherapeutic group Drugs for treatment of diseases of urogenital bodies and sex hormones. Drugs for treatment of urological diseases. Other drugs for treatment of urological diseases, including spasmolysants. Drugs for treatment of disturbances of an erection. Sildenafil. ATX G04BE03 code. Pharmacological Pharmacokinetics properties. Sildenafil is quickly soaked up from digestive tract. The maximum concentration in blood plasma is reached in 30-120 minutes (on average in 60 minutes) after oral administration on an empty stomach. The bioavailability at intake is 40%. If the drug is taken with greasy food, the speed of absorption decreases and time of the maximum concentration in blood plasma increases on average for 60 min., and the maximum concentration in blood plasma decreases on average by 29%. The volume of distribution (Vss) of a sildenafil in an equilibrium state averages 105 l that indicates its distribution in fabrics. Sildenafil and his main metabolite circulating M-desmetilovy approximately for 96% contact proteins of plasma. Linking with proteins does not depend on the general concentration of drug. Sildenafil is metabolized mainly under the influence of CYP3A4 (main way) and CYP2C9 (additional way) of microsomal isoenzymes of a liver. The main circulating metabolite is formed as a result of M-desmetilirovaniya sildenafit. On selectivity of action on FDE the metabolite is comparable with sildenafily, and its activity concerning FDE5 is about 50% of activity of the drug. Concentration of a metabolite in plasma make about 40% of those sildenafit. M-desmetilmetabolit is exposed to further metabolism, the final period of its semi-removal is equal about 4 hours. The general clearance of a sildenafil is 41 l/h, elimination half-life – 3-5 hours. Sildenafil is excreted in the form of metabolites, mainly with a stake (80% of the accepted dose) and to a lesser extent – with urine (13% of the accepted dose). Pharmacodynamics. Potential is oral drug for treatment of patients with erectile dysfunction. Selection inhibitor of tsGMF-specific phosphodiesterase of type 5 (FDE5). Sildenafil has no direct relaxing impact on smooth muscle cells of cavernous bodies, however considerably increases the relaxing effect of oxide of nitrogen (NO) by oppression of FDE5 which is responsible for splitting of tsGMF in cavernous bodies. At activation of a metabolic way NO/tsGMF which happens at sexual stimulation the oppression of FDE5 sildenafily leads to increase in concentration of tsGMF in cavernous bodies. Therefore manifestation of pharmacotherapeutic effect of a sildenafil requires sexual excitement. Indications - the erectile dysfunction which is characterized by inability to achievement or preservation of an erection of a penis sufficient for satisfactory sexual intercourse. It is effective only in the presence of sexual stimulation. The route of administration and doses the Adult appoint inside in a dose 50 mg in 1 hour prior to sexual intercourse. Depending on effect the dose can be reduced up to 25 mg or is increased up to 100 mg. The maximum recommended dose of 100 mg of 1 times a day. The tablet should be swallowed entirely with a small amount of water. Side effects Very often ≥1/10 - a headache - inflows Often ≥1/100 to & lt, 1/10 - a disorder of vision (photosensitization, disturbance of visual acuity) - a tranzitorny chromatopsia of weak intensity - the strengthened heartbeat - congestion of a nose - dyspepsia Seldom ≥1/10000 to & lt, 1/1000 - skin rash - eye pain and reddening of eyes - tachycardia, ventricular arrhythmia, a myocardial infarction, unstable stenocardia - nasal bleeding - intracerebral bleeding - the tranzitorny ischemic attack - arterial hypertension or hypotension, a faint - vomiting - a priapism, a long erection of the Contraindication - hypersensitivity to a sildenafil or any of drug components - diseases of a cardiovascular system (for example, unstable stenocardia, heavy heart failure) - patients should not use drug, undergoing treatment by the nitrates and other medicines releasing nitrogen oxide - a heavy liver failure - arterial hypotension (the ABP is lower than 90/50 mm Hg.) - recently had myocardial infarction or a stroke of a brain - hereditary degenerative diseases of a retina (for example, retinitis pigmentosa) - loss of sight in one eye owing to the front ischemic neuropathy of an optic nerve which is not connected with inflammation of an artery regardless of whether this episode was connected with the previous use of FDE5 inhibitor or not - the children's and teenage age up to 18 years Medicinal interactions on sildenafit Effects of other medicines. Researches in vitro. Metabolism of a sildenafil happens mainly with the participation of isoform 3A4 (main way) and isoform 2C9 (minor way) of P450 cytochrome (CYP). Therefore inhibitors of these isoenzymes are capable to reduce clearance of a sildenafil. Researches in Vivo. The population pharmacokinetic analysis of these clinical trials showed decrease in clearance of a sildenafil at simultaneous use with CYP3A4 inhibitors (such as ketokonazol, erythromycin, Cimetidinum). Though at simultaneous use of a sildenafil and CYP3A4 inhibitors of growth of frequency of by-effects it was not observed, the recommended initial dose of a sildenafil makes 25 mg. Simultaneous use of inhibitor of HIV protease, very powerful P450 inhibitor, in a condition of equilibrium concentration (500 mg of 1 times a day) also sildenafit (a single dose of 100 mg), led to increase in Cmax of a sildenafil for 300% (by 4 times) and increases in plasma AUC of a sildenafil for 1000% (by 11 times). In 24 hours the plasma levels of a sildenafil still were about 200 ng/ml in comparison with the level about 5 ng/ml characteristic of use sildenafit separately that corresponds to considerable influence of a ritonavir on a wide range of P450 substrates. Sildenafil does not influence pharmacokinetics of a ritonavir. On the basis of results of pharmacokinetic interactions the co-administration of a sildenafil and ritonavir is not recommended, anyway under no circumstances the maximum dose of a sildenafil should not exceed 25 mg within 48 hours. In a dose that provides equilibrium concentration (1200 mg three times a day) and a sildenafila (100 mg once) led simultaneous use of inhibitors of HIV protease of a sakvinavir, CYP3A4 inhibitor to increase in Cmax of a sildenafil for 140% and to increase in system exposure (AUC) in a sildenafil by 210%. Influence of a sildenafil on pharmacokinetics of a sakvinavir is not revealed. It is supposed that more powerful CYP3A4 inhibitors, such as ketokonazol and itrakonazol, will have more significant influence. At use of a sildenafil (100 mg once) and erythromycin, specific CYP3A4 inhibitor, in an equilibrium state (500 mg twice a day within 5 days) increase in system exposure of a sildenafil for 182% (AUC) was observed. At male healthy volunteers the azithromycin influence (500 mg a day within 3 days) on AUC, Cmax, Tmax, a constant of speed of elimination and the subsequent elimination half-life of a sildenafil or its main circulating metabolite was not observed. Cimetidinum (inhibitor of P450 cytochrome and nonspecific CYP3A4 inhibitor) in a dose of 800 mg at simultaneous use with sildenafily in a dose of 50 mg at healthy volunteers led to increase in plasma concentration of a sildenafil for 56%. Grapefruit juice is weak CYP3A4 inhibitor in a wall of intestines and can cause moderate increase in plasma levels of a sildenafil. Single use of antiacid means (hydroxide aluminum hydroxide magnesium) does not affect bioavailability of a sildenafil. Though researches of specific interaction with all medicines were not conducted, according to the population pharmacokinetic analysis the pharmacokinetics of a sildenafil did not change at its simultaneous use with medicines which belong to group of CYP2C9 inhibitors (tolbutamide, warfarin, Phenytoinum), groups of CYP2D6 inhibitors (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), group of thiazide and tiazidopodobny diuretics, loopback and kaliysokhranyayushchy diuretics, inhibitors of angiotensin-converting enzyme, antagonists of calcium, antagonists of beta adrenoceptors or inductors of metabolism CYP450 (such as rifampicin, barbiturates). Nikorandil represents a hybrid of the activator of calcium channels and nitrate. The nitrate component causes a possibility of its serious interaction with sildenafily. Effects of a sildenafil on other medicines. Researches in vitro. Sildenafil – weak inhibitor of isoforms 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 (IК5о>, 150 mM) P450 cytochrome. As peak plasma concentration of a sildenafil are equal to about 1 µmol, influence of drug on clearance of substrates of these isoenzymes is improbable. There are no data on interaction of a sildenafil and such nonspecific inhibitors of phosphodiesterase as theophylline and Dipiridamolum. Researches in Vivo. As it is known that sildenafit influences nitrogen oxide metabolism / the cyclic guanozinmonofosfat (tsGMF), it was established that this drug exponentiates hypotensive effect of nitrates therefore its simultaneous use with donors of nitrogen oxide or nitrates in any form is contraindicated. Some predisposed patients have a simultaneous use of a sildenafil and blockers of alpha adrenoceptors can lead to development of symptomatic hypotension that most often arises within 4 hours after use of a sildenafil. During the researches of specific interaction of medicines the blocker of alpha adrenoceptors docsazozin (4 mg and 8 mg) also sildenafit (25 mg, 50 mg and 100 mg) were applied at the same time to patients with the benign hyperplasia of a prostate (BHP) whose stabilization of a state was reached at use of a docsazozin. In these researches the studied populations the average additional lowering of arterial pressure in a prone position na7/7 by mm Hg., 9/5 mm Hg was observed. both 8/4 mm Hg., and an average lowering of arterial pressure in a standing position on 6/6 mm Hg., 11/4 mm Hg., 4/5 mm Hg. respectively. At simultaneous use of a sildenafil and docsazozin for patients whose stabilization was reached at use of a docsazozin, it was sometimes reported about development of symptomatic orthostatic hypotension. It was said in these statements about cases of dizziness and a preunconscious state, but without syncope. No significant interactions at simultaneous use of a sildenafil (50 mg) and tolbutamide (250 mg) or warfarin (40 mg) which are metabolized by CYP2C9 were observed. Sildenafil (50 mg) did not lead to lengthening of the bleeding time caused by use of acetylsalicylic acid (150 mg). Sildenafil (50 mg) did not exponentiate hypotensive effect of alcohol at healthy volunteers at the average maximum levels of ethanol in blood of 80 mg/dl. At the patients accepting sildenafit, no distinctions of a profile of side effects in comparison with placebo at simultaneous use of such classes of hypotensive medicines were observed as diuretics, blockers of beta adrenoceptors, APF inhibitors, antagonists of angiotensin II, antihypertensive medicines (vasodilating and the central action), blockers of adrenergic neurons, blockers of calcium channels and blockers of alpha adrenoceptors. In a special research of interaction at simultaneous use of a sildenafil (100 mg) and an amlodipina to patients with arterial hypertension the additional decrease in systolic arterial blood pressure in a prone position on 8 mm Hg was observed. The corresponding decrease in diastolic arterial blood pressure was 7 mm Hg. In size these additional lowerings of arterial pressure were comparable to those which were observed at use of a sildenafil only by healthy volunteers. Sildenafil in a dose of 100 mg did not influence pharmacokinetic indicators of inhibitors of HIV protease, a sakvinavir and a ritonavir which are CYP3A4 substrates. Special instructions With care to apply in the heart failure, unstable stenocardia transferred to the last 6 months of myocardial infarctions, strokes or zhizneugrozhayushchy arrhythmias, arterial hypertension (arterial blood pressure (the ABP & gt, 170/100 mm Hg.) or hypotonias (ABP & lt, 90/50 mm Hg.). Prior to therapy it is necessary to collect the medical anamnesis of the patient and to perform physical examination for diagnosis of erectile dysfunction and definition of its possible reasons. As the sexual activity is followed by a certain risk from heart, prior to any treatment of erectile dysfunction the doctor has to estimate a condition of a cardiovascular system of the patient. Potential has vasodilating effect that is shown by a slight and short-term lowering of arterial pressure. Before appointment Potential the doctor has to weigh carefully whether such effect can have adverse impact on patients with certain basic diseases, especially in a combination with sexual activity. Patients with obstruction of an output path of a left ventricle belong to patients with hypersensitivity to vazodilatator (for example, an aorta stenosis, a hypertrophic subaortic stenosis), or patients with a rare syndrome of a multisystem atrophy, one of manifestations of which is heavy disturbance of regulation of arterial blood pressure from the autonomic nervous system. Potential exponentiates hypotensive effect of nitrates. In the post-marketing period it was reported about heavy side reactions from a cardiovascular system, including a myocardial infarction, unstable stenocardia, a sudden cardiac death, ventricular arrhythmia, cerebrovascular hemorrhages, the tranzitorny ischemic attack, arterial hypertension and arterial hypotension which coincided using a sildenafil. Most of patients, but not at all, had risk factors of cardiovascular diseases. Many such side reactions were observed in time or right after sexual intercourse, and happened soon after use of drug without sexual activity some. Therefore it is impossible to define whether development of such side reactions directly is connected with risk factors, or their development caused by other factors. Means for treatment of erectile dysfunction including Potential, patients should appoint with care with anatomic deformations of a penis (such an angulation, cavernous fibrosis or Peyroni's disease), or to patients with states which contribute to the development to a priapism (such as sickemia, multiple myeloma or leukemia). Safety and efficiency of simultaneous use of a sildenafil with other methods of treatment of erectile dysfunction were not studied therefore use of such combinations is not recommended. It was reported about visual disturbances and cases of not arterial front ischemic neuropathy of an optic nerve that are connected with use of a sildenafil and other FDE5 inhibitors. Patsiyentov it is necessary to warn that in case of a sudden disorder of vision the drug use Potential should be stopped and to see immediately a doctor. Simultaneous use of a sildenafil and ritonavir is not recommended. Patients who prin
at blockers of alpha adrenoceptors should apply Potential with care as such combination can lead to symptomatic hypotension at some patients, inclined to it. Symptomatic hypotension usually arises for 4 hours after use Potential. For the purpose of minimizing risk of developing orthostatic hypotension the therapy sildenafily can be begun only at hemodynamically stable patients who apply blockers of alpha adrenoceptors. The recommended initial dose to such patients makes 25 mg of a sildenafil. Besides, it is necessary to inform patients how to work in case of symptoms of orthostatic hypotension. Researches of thrombocytes of the person showed that in vitro sildenafit exponentiates anti-aggregation effects of sodium of Sodium nitroprussidum. There is no information on safety of use Potential to patients with disturbances of fibrillation or with an acute round ulcer. Thus, use of a sildenafil to patients of this group perhaps only after careful assessment of a ratio of advantage and risks. Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms As drug can be the cause of dizziness and disorders of vision, it is necessary to be careful during the driving or work with dangerous mechanisms. The overdose the Dose exceeding 100 mg does not improve efficiency of drug, but can enhance severity of side effects. Treatment: in case of overdose it is necessary to carry out symptomatic treatment. Dialysis should not accelerate clearance of a sildenafil as the last actively contacts proteins of plasma and is not removed with urine. The form of release and packing On 2 tablets place in blister strip packaging from a film of polyvinylchloride EP-73 brand and material rolled packing on the basis of aluminum foil. On 1 or 2 planimetric pack together with the instruction for medical use in the state and Russian languages place in a pack from cardboard. To Store storage conditions at a temperature not over 30 of 0C. To store out of children's reach! Period of storage 3 years. Not to apply after an expiration date. Prescription status According to the prescription. Producer/packer CIAO "Technologist", Ukraine. 20300, Ukraine, city of Uman of the Cherkassk region, Staraya Street pro-carved, 8. Name and country of the owner of the registration certificate CIAO "Technologist", Ukraine. 20300, Ukraine, city of Uman of the Cherkassk region, Staraya Street pro-carved, 8. The name, the address and a contact information (phone, the fax, e-mail) of the organization in the territory of the Republic of Kazakhstan, the accepting claim (offer) on quality of medicines from consumers and responsible for post-registration observation of safety of medicine: L-Pharma LLP 050061, Republic of Kazakhstan, Almaty, mikr. "Tastak-1", house 3 ph./fax: (727) 374-88-75, 374-88-72
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