The instruction for medical use of Erekto-Fast medicine 10 the Trade name of Erekto-Fast 10 International unlicensed name Tadalafil Lekarstvennaya the Film form dispersed in an oral cavity, 10 mg One film contains Structure: active agent – tadalafit 10 mg, excipients: gipromelloza (5 cps), gipromelloza (15 cps), propylene glycol, glycerin, polysorbate 80, sucralose, mint oil (dementolizirovanny mint oil), gland (III) oxide yellow (E172). Description of a squared Film, light yellow color, opaque, not sticky, 15 long ± 1.00 mm, 25 wide ± 0.25 mm. Pharmacotherapeutic group Urinogenital system and sex hormones. Urological drugs. The drugs used in erectile dysfunction. Tadalafil. The ATX G04BE08 code the Pharmacological Tadalafil Pharmacokinetics Absorption properties is easily soaked up after oral introduction, and average maximum concentration in plasma (Cmax) is reached in median time. The absolute bioavailability of a tadalafil after use was not defined. Speed and extent of absorption of a tadalafil do not depend on food, thus, tadalafit films it is possible to accept irrespective of meal. Reception time (in the morning or in the evening) had no clinically significant effect on the speed and extent of absorption. Distribution the Average volume of distribution makes about 63 liters that indicates what tadalafit is distributed in fabric. At therapeutic concentration of 94% of a tadalafil in plasma contacts proteins. Linking with proteins does not change with a renal failure. At healthy faces less than 0.0005% of the entered dose are revealed in sperm. Metabolism Tadalafil is mainly metabolized with participation of P450 (CYP) 3A4 cytochrome. The main circulating metabolite is metilkatekholglyukoronid. It by 13000 times is less active concerning FDE5, than tadalafit. Therefore, this metabolite hardly is clinically significant. Removal At healthy faces average clearance of a tadalafil makes 2.5 l/h, and average T1/2 — 17.5 h Tadalafil is removed mainly in the form of inactive metabolites, generally with a stake (about 61%) and, to a lesser extent with urine (about 36%). The pharmacodynamics Tadalafil is an effective, reversible selection inhibitor of specific phosphodiesterase of type 5 (FDE5) cyclic guanine riboside of monophosphate (tsGMF). When sexual excitement causes local release of nitrogen oxide, FDE5 inhibition tadalafily leads to increase in the tsGMF levels in a cavernous body of a penis. The relaxation of unstriated muscles of arteries and inflow of blood to penis tissues is a consequence of it, as causes an erection. Tadalafil does not render effect in lack of sexual stimulation. Indications – treatment of erectile dysfunction at male adult patients. Sexual stimulation is necessary for manifestation of effect of a tadalafil. Erekto-Fast it is not intended for use by female persons. A route of administration and doses Adult men Erectile dysfunction at men of middle age: Usually recommended dose makes 10 mg, accepted to expected sexual activity irrespective of meal. Does not give to those patients at whom tadalafit 10 mg in a dose adequate effect, it is possible to accept a dose of 20 mg, at least, in 30 minutes prior to sexual activity. The maximum frequency of reception is once a day. Tadalafil of 10 mg is intended for use just before expected sexual activity and is not recommended for continuous use. Special groups of patients Elderly men: correction of a dose is not required. Men with a renal failure: correction of a dose is not required to patients with a slight or moderate renal failure. For patients with a heavy renal failure the maximum recommended dose makes 10 mg. Men with diabetes: correction of a dose is not required. Children: Erekto-Fast it is not applied to treatment of erectile dysfunction at children. A route of administration For oral administration. 1) To open a bag only in the specified place, slowly tearing off it. Not to cut a bag. 2) To accurately pull out a film from a bag, without having damaged it. 3) Before use to check for existence of damages of a film. It is necessary to use only the intact films. 4) The film is put on language dry hands in an empty mouth of the patient. 5) The film has to be dissolved in language without water within several seconds (in saliva which should be swallowed subsequently). Side effects Most often at reception of a tadalafil for treatment of erectile dysfunction or a benign hyperplasia of a prostate developed the following side effects: headache, dyspepsia, dorsodynias, myalgia. At the same time the frequency of development of these side effects increased in proportion to a dose of a tadalafil. These side effects were temporary, and most often easy or moderate. The majority of cases of development of a headache at reception of a tadalafil of 1 times a day were noted in the first 10 or 30 days from an initiation of treatment tadalafily. Symbol of frequency of side reactions: very often (≥1/10), it is frequent (≥ 1/100 – & lt, 1/10), infrequently (≥1/1.000 – & lt, 1/100), is rare (≥1/10.000 – & lt, 1/1, 000), is very rare (& lt, 1/10.000) and it is unknown (it is impossible to determine frequency by the available data). Often: headaches, reddening, congestion of a nose, dyspepsia, dorsodynias, myalgia, extremity pains. Infrequently: hypersensitivity reactions, dizziness, misting of sight, eye pain, a ring in ears, tachycardia, heartbeat strengthening, hypotension, hypertensia, short wind, nasal bleeding, an abdominal pain, vomiting, nausea, a gastroesophageal reflux, rashes, a hamaturia, a long erection, stethalgias, peripheral hypostases, weakness. Seldom: urticaria, a stroke, a syncope, the passing ischemic attack, migraine, spasms, passing amnesia, defect of a field of vision, puffiness a century, conjunctiva hyperaemia, front nearteriitny ischemic neuropathy of an optic nerve (NAION), occlusion of vessels of a retina, a sudden hearing loss, a myocardial infarction, unstable stenocardia, ventricular arrhythmia, a small tortoiseshell, Stephens-Johnson’s syndrome, exfoliative dermatitis, a hyperhidrosis, a priapism, bleeding from a penis, a gematospermiya, puffiness of the person, a sudden cardiac death. Contraindications – hypersensitivity to drug components – administration of drugs containing any organic nitrates – to men with heart diseases to which the sexual activity is not recommended. Doctors have to consider potential warm risk of sexual activity to patients with diseases of a cardiovascular system in the anamnesis Use of a tadalafil contraindicated in the following cardiovascular diseases: – a myocardial infarction during the last 90 days – the unstable stenocardia or stenocardia arising during sexual intercourse – heart failure the last 6 months – uncontrollable arrhythmia, hypotension (& lt, 90/50 mm Hg.) or uncontrollable hypertensia – a stroke within the last 6 months – loss of sight owing to not arterial front ischemic optical neuropathy of an optic nerve irrespective of whether this episode was connected with the previous influence of inhibitor of phosphodiesterase of type 5 (FDE5) – to persons with hereditary intolerance of fructose, glucose galactose malabsorption, deficiency of enzyme of sukrazy-isomaltase Medicinal interactions Influence of other substances on tadalafit P450 cytochrome Inhibitors: ketokonazol (400 mg a day) increased activity of a tadalafil (20 mg) by 4 times and Cmax by 22%. Ritonavir, protease inhibitor (200 mg 2 times a day) which is CYP3A4, CYP2C9, CYP2C19 and CYP2D6 inhibitor, increased action of a tadalafil (20 mg) twice without change of Cmax. Other inhibitors of protease, such as sakvinavir and other CYP3A4 inhibitors, such as erythromycin, klaritromitsin, itrakonazol and grapefruit juice, it is necessary to take with caution as they increase concentration of a tadalafil in plasma. P450 cytochrome stimulators: CYP3A4 stimulator, rifampicin, reduces the area under a curve ‘concentration time’ of a tadalafil by 88% in comparison with concentration time values only for a tadalafil. It is expected that this reduction of influence can reduce efficiency of a tadalafil, Other stimulators of CYP3A4, such as phenobarbital, Phenytoinum and carbamazepine, can also reduce concentration of a tadalafil in plasma. Influence of a tadalafil on other medicines Nitrates: in the published researches it is noted that tadalafit increases hypotensive effect of nitrates. Therefore tadalafit use to patients who use any form of organic nitrates, contraindicated. Thus, to patients to whom any dose of a tadalafil is ordered and administration of nitrate is considered vital, at least, has to there were pass 48 hours after the last dose of a tadalafil before administration of nitrate. In such conditions nitrates should be entered only under medical observation with the corresponding monitoring of a hemodynamics. Antihypertensive drugs: joint introduction of a docsazozin (4 and 8 mg a day) and the tadalafila (20 mg in the form of a single dose) considerably increases effect of action of this alpha blocker, this effect can not less than twelve hours last and can be symptomatic, including a syncope. Therefore this combination is not recommended. Ethinylestradiol and terbutalin: tadalafit causes increase in oral bioavailability of ethinylestradiol, similar increase can be expected at oral introduction of a terbutalin though clinical consequences are not clear. Alcohol: concentration of alcohol (average maximum concentration in blood of 0.08%) did not influence joint introduction with tadalafily. Tadalafil in a dose of 20 mg did not increase the average hypotensive action caused by alcohol (the man weighing 80 kg has 0.7 g/kg or about 180 ml of 40% of alcohol), but, at some subjects the postural dizziness and orthostatic hypotension were observed. Metabolism of medicines with P450 cytochrome participation: tadalafit has no clinically significant effect on clearance of drugs which metabolism proceeds with participation of an isoenzyme CYP450 cytochrome. Tadalafil does not inhibit and does not induce isoenzymes of CYP3A4, CYP1A2, CYP2D6, CYP2E1 and CYP2C9 and CYP 2C19. CYP2C9 substrates (for example, R-warfarin): tadalafit had no clinical effect on AUC of S-warfarin or R-warfarin. Also tadalafit had no effect on the change of a prothrombin time induced by warfarin. Aspirin: tadalafit did not strengthen increase in the bleeding time caused by intake of acetylsalicylic acid. Special instructions Before an initiation of treatment tadalafily: • Before purpose of treatment it is necessary to study the medical anamnesis of the patient and to perform physical examination of diagnosis of erectile dysfunction or benign hyperplasia of a prostate and also identification of the potential initial reasons. • Before any drugs for treatment of erectile dysfunction it is necessary to study a condition of a cardiovascular system the patient as a certain degree of risk for a cardiovascular system is connected with sexual activity. Tadalafil has the vasodilating properties leading to a slight and passing lowering of arterial pressure and per se exponentiates hypotensive effect of nitrates. • Assessment of erectile dysfunction has to include definition of the potential initial reasons and identification of suitable treatment, after the performed physical examination. It is unknown, it is effective tadalafit for the patients who underwent operation on pelvic bodies or on nervosberegayushchy prostatectomy. Cardiovascular system: • It was reported about development the serious cardiovascular illness connected with reception of a tadalafil such as myocardial infarction, sudden cardiac death, unstable stenocardia, ventricular arrhythmia, stroke, passing ischemic attack, stethalgias, strengthening of heartbeat and tachycardia. • At the patients accepting alfa-1 blockers, joint reception of a tadalafil can lead to development of symptomatic hypotension. Joint reception of a tadalafil and docsazozin is not recommended. Decrease in sight and sudden hearing loss • It was reported about development of the visual impairments and cases of development of a front nearteriitny ischemic neuropathy of an optic nerve (NAION) caused by reception of a tadalafil and other PDE5 inhibitors. Patients have to know that in case of sudden decrease in sight and decrease, or a sudden hearing loss it is necessary to stop reception of a tadalafil and to see immediately a doctor. Liver failure • It is necessary to be careful when assigning a tadalafil to patients with a heavy liver failure. If purpose of a tadalafil is necessary, the doctor has to estimate carefully a ratio “advantage/risk” in each individual case. Priapism and anatomic deformation of a penis • The patients testing the long erection lasting for 4 hours and more have to ask for medical care surely. Without timely treatment the damage of tissues of penis and permanent loss of potency is possible. Tadalafil patients should take with caution with anatomic deformation of a penis (such as curvature, cavernous fibrosis, or Peyroni’s disease (fibroplastic induration of a penis) and also to patients with the states contributing to a priapism (such as sickemia, multiple myeloma or leukemia). Care it is necessary to appoint use together with CYP3A4 C inhibitors tadalafit to the patients accepting CYP3A4 inhibitors (ritonavir, sakvinavir, ketokonazol, itrakonazol, and erythromycin) as at the same time the increased action of a tadalafil was observed (AUC, the area under a curve “concentration – time”). Tadalafil and other drugs for treatment of erectile dysfunction tadalafit Safety and efficiency of combinations with other PDE5 inhibitors or other drugs for treatment of erectile dysfunction is not studied. Patsiyentov it is necessary to inform that it is impossible to combine these drugs. Overdose At single appointment to healthy volunteers in a dose of 500 mg and to patients with erectile dysfunction repeatedly, up to 100 mg, undesirable effects were the same, as well as at use of drug in lower doses. Treatment: performing standard symptomatic therapy. The hemodialysis is inefficient for removal of a tadalafil. A form of release and packing On 1 film in a bag from the triple laminated aluminum foil. On 4 bags together with the instruction for medical use in the state and Russian languages place in a pack from cardboard. To Store storage conditions in the dry, protected from light place at a temperature not above 25 °C. To store out of children’s reach! 2 years not to apply a period of storage after an expiration date. Prescription status According to the prescription Producer Zim Laboratories Limited B-21/22, MIDC Area, Kalmeshwar-441,501, Dist. Nagpur, Maharashtra, India Holder of the registration certificate of VISTA LABS DMCC Unit No: 3O-01-3048, Jewellery & Gemplex 3 Plot No: DMCC-PH2-J&GPlexs, Jewellery & Gemplex, Dubai, the United Arab Emirates 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 medicines: Metabol Kazakhstan LLP, M01M09A1, Karaganda, Ermekov St. 110/2 ph. +7 (212) 43-38-11, fax +7 (212) 43-38-15
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