Have aracil table. 100mg 2 (2x1) blister

Have aracil table. 100mg 2 (2x1) blister

Product Code: 12428
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Composition

active substance:& nbsp;sildenafil;

1 tablet contains sildenafil citrate in terms of 100% sildenafil 50 mg or 100 mg

other ingredients: lactose monohydrate, magnesium gluconate; sugar; calcium stearate, flavoring "Lemon", colouring agent tartrazine (E 102).

The

Dosage form

Pills.

basic physico-chemical properties:biconvex yellow or yellow-brown, interspersed with a notch on one side.

The

drug description

agents used for the treatment of erectile dysfunction. ATC code G04B E03.

The

Pharmacological properties

Pharmacological.

Erasil is an oral drug that is used for the treatment of erectile dysfunction in men. The drug is a sildenafil citrate salt, a selective inhibitor of cyclic guanosine monophosphate (cGMP) - specific phosphodiesterase type 5 (PDE-5).

the Physiological mechanism of penis erection is the release of nitric oxide (NO) in the cavernous body during sexual stimulation. NO activates the enzyme guanylate cyclase, which causes an increase in cGMP levels, relaxation of smooth muscles of the cavernous body and increased blood flow in them.

sildenafil has no direct relaxing effect on isolated human corpus cavernosum, but enhances the effectiveness of nitric oxide (NO) by inhibiting PDE5, which is responsible for degradation of cGMP in the cavernous body.

when local release of NO occurs during sexual stimulation, inhibition of PDE5 by sildenafil causes increased levels of cGMP in the cavernous body, resulting in relaxation of smooth muscles and increased blood flow to the cavernous body.

use of sildenafil in recommended doses is ineffective in the absence of sexual stimulation.

Research in vitro have shown that sildenafil is selective relative to PDE-5. Its effect on PDE5 is stronger than other known PDE (10 times stronger than ФДЭ6, 80 times than ФДЕ1, 700 times than ФДЕ2, PDAS, ФДЕ4, ФДЕ7-ФДЕ11). In particular sildenafil has 400 times better selectivity relative to PDE-5 than PDES, cGMP specific PDE isoforms, which takes part in processes of regulation of heart rate.

visual impairment.& nbsp;when using sildenafil at a dose of 100 mg in some patients after 1:00 found (using the test "Farnsworth-Munsell 100") slight variability of discoloration (blue/green); through 2:00 after taking the drug, these changes took place.

the Possible mechanism of color vision impairment is considered to be the suppression of PDE6, which is involved in the process of light transmission in the retina. The results of the studyin vitroshow that the effect of sildenafil on PDE6 is 10 times inferior to its activity against PDE5. Sildenafil does not affect visual acuity, contrast perception, electroretinograms, intraocular pressure, or pupilometry.

Efficiency.the efficacy of sildenafil, which was evaluated by the ability of the drug to ensure the onset and preservation of an erection sufficient for sexual intercourse, was demonstrated and maintained with prolonged use of the drug (1 year).

in the study, when taking sildenafil at doses of 25 mg, 50 mg, 100 mg improvement of erection was observed in 62%, 74%, 82% respectively. In addition to improving erectile function, analysis of IEF (international erectile function index) has shown that treatment with sildenafil also increases orgasm and satisfaction from sexual intercourse.

in the treatment of sildenafilom improvement was noted in 59% of patients with diabetes in patients who underwent radical prostatectomy - 43%, in patients with spinal cord injury - 83%.

Pharmacokinetics.

sildenafil is rapidly absorbed. The maximum plasma concentration of the drug is achieved within 30-120 minutes (with a median of 60 minutes) after its oral administration on an empty stomach. The average bioavailability after oral administration is 41% (with a range of values from 25 to 63%). In the recommended dose range (25 to 100 mg), the area under the concentration-time curve (AUC) and the maximum concentration (C max) of sildenafil after oral administration increases proportionally to the dose.

in the application of sildenafil during meals extent of absorption is reduced, with an average lengthening of the T max up to 60 min and an average decline in C max 29%.

the average equilibrium volume of distribution (V d ) is 105 liters, indicating the distribution of the drug in the tissues of the body. After a single oral administration of sildenafil at a dose of 100 mg, the average maximum total plasma concentration of sildenafil is approximately 440 ng/ml (coefficient of variation is 40%). Since the binding of sildenafil and its main N-desmetil metabolite to plasma proteins reaches 96%, the average maximum plasma concentration of free sildenafil reaches 18 ng/ml (38 nmol). The degree of binding to plasma proteins does not depend on the total concentrations of sildenafil.

in healthy volunteers taking sildenafil once at a dose of 100 mg, 90 minutes later in the ejaculate was determined less than 0.0002% (average 188 ng) dose.

sildenafil Metabolism is carried out mainly with the participation of microsomal liver isoenzymes CYP3A4 (the main path) and CYP2C9 (minor route). The main circulating metabolite is formed by n-demethylation of sildenafil. Selectivity for PDE5 metabolite comparable with by selectivity of sildenafil and the active metabolite on PDE5 is approximately 50% activity of the initial substance. The plasma concentration of this metabolite is approximately 40% of the concentration of sildenafil in plasma. N-demethylated metabolite undergoes further metabolism, during its half-life is approximately 4:00.

the total clearance of sildenafil is 41 l/h, causing a half-life of 3-5 hours. Both after administration and after administration sildenafil excretion in the form of metabolites is carried out mainly with feces (about 80% of the administered dose) and to a lesser extent with urine (about 13% of the administered dose).

elderly Patients. in healthy volunteers of advanced age (over 65 years) showed reduced clearance of sildenafil, resulting in increased plasma concentrations of sildenafil and its active N-demethylated metabolite is approximately 90% compared to the corresponding concentrations in healthy volunteers of young age (18-45 years). Due to age differences in plasma protein binding, the corresponding increase in the plasma concentration of free sildenafil was approximately 40%.

Renal failure. in volunteers with impaired renal function or moderate (creatinine clearance 30 to 80 ml/min) the pharmacokinetics of sildenafil was unchanged after a single oral dose of 50 mg. Average AUC and Cmax N-demethylated metabolite increased 126% and 73%, respectively, compared to such indicators in volunteers of similar age without renal dysfunction. However, due to the high inter-individual variability, these differences were not statistically significant. In volunteers with severe renal impairment (creatinine clearance below 30 ml/min), sildenafil clearance decreased, resulting in average increases of AUC and Cmaxby 100% and 88%, respectively, compared to volunteers of similar age without renal impairment. In addition, the AUC and Cmax N-demethylated metabolite significantly increased 79% and 200%, respectively.

Hepatic insufficiency.in volunteers with mild to moderate cirrhosis (classes a and B according to the child-Pugh classification), the clearance of sildenafil decreased, which led to an increase in AUC (84%) and C max(47%) compared to volunteers of similar age without impaired liver function. Pharmacokinetics of sildenafil in patients with impaired hepatic function was not studied heavily. 

Reading

treatment of erection disorders, which are defined as inability to achieve and maintain the erection of the penis necessary for successful sexual intercourse. For effective action of Erosio need sexual arousal.

Contra

The
  • hypersensitivity to sildenafil or other components of the drug.
  • The
  • Concurrent use of nitric oxide donors (such as amyl nitrite) or nitrates in any form, since it is known that sildenafil affects the metabolic pathways of nitric oxide/cyclic guanosine monophosphate (cGMP) and potentiates hypotensive effect of nitrates.
  • Diseases in which sexual activity is not recommended (e.g. severe cardiovascular disorders such as unstable angina and severe heart failure).
  • loss of vision per eye due to nonarterial anterior ischemic optic neuropathy, regardless of whether this pathology is associated with previous use of PDE5 inhibitors.
  • The
  • abnormal liver function, severe, hypotension (blood pressure below 90/50 mm Hg. St.), Recently moved stroke or myocardial infarction and known hereditary degenerative retinal disorders such as retinitis pigmentosa (a small number of these patients have genetic disorders of retinal PDE) , as the safety of sildenafil has not been investigated in patients with such diseases.

Interaction with other drugs and other forms of interaction

the Effect of other drugs on sildenafil.

Researchin vitro.

the metabolism of sildenafil occurs mainly with the participation of ZA4 isoform (the main pathway) and 2C9 isoform (the secondary pathway) of cytochrome P450 (CYP), so the inhibitors of these isoferments are able to reduce the clearance of sildenafil.

Research in vivo .

there has been a decrease in clearance of sildenafil while the use of inhibitors CYP3A4 (such as ketoconazole, erythromycin, cimetidine). Although no increase in the frequency of side effects was observed with the simultaneous use of sildenafil and CYP3A4 inhibitors, the recommended initial dose of sildenafil is 25 mg.

the Simultaneous use of the protease inhibitor of HIV, a very powerful inhibitor P450, in a state of equilibrium concentration (500 mg 1 time per day) and sildenafil (single dose 100 mg) led to an increase in C max sildenafil 300% (4 times) and an increase in plasma AUC sildenafil 1000% (11 times). After 24 hours, plasma levels of sildenafil were still approximately 200 ng/ml compared to about 5 ng/ml, typical of sildenafil alone, corresponding to the significant effect of ritonavir on a wide range of P450 substrates. Sildenafil does not affect the pharmacokinetics of ritonavir. Given these pharmacokinetic data, the simultaneous use of sildenafil and ritonavir is not recommended; in any case, the maximum dose of sildenafil under what circumstances should not exceed 25 mg for 48 hours.

the Simultaneous use of an inhibitor of HIV protease of saquinavir, a CYP3A4 inhibitor, at a dose that provides the equilibrium concentration (1200 mg 3 times a day) and sildenafil (100 mg single) resulted in higher Cmax sildenafil to 140% and an increase in systemic exposure (AUC) to sildenafil by 210%. No influence of sildenafil on the pharmacokinetics of saquinavir was revealed. It is assumed that more potent CYP3A4 inhibitors such as ketoconazole and Itraconazole will have a more pronounced effect.

the use of sildenafil (100 mg dose) and erythromycin, a specific CYP3A4 inhibitor, at steady state (500 mg 2 times a day for 5 days) was observed increase in systemic exposure to sildenafil 182% (AIS). In healthy male volunteers there was no effect of azithromycin (500 mg daily for 3 days) on the AUC, max  T max , rate constant of elimination and subsequent halflife of sildenafil or its primary circulating metabolite. Cimetidine (cytochrome P450 inhibitor and non-specific CYP3A4 inhibitor) at a dose of 800 mg, while the use of sildenafil at a dose of 50 mg in healthy volunteers led to an increase in plasma concentrations of sildenafil by 56%.

grapefruit juice Is a weak CYP3A4 inhibitor in the intestinal wall and can cause a moderate increase in plasma levels of sildenafil.

one-time use of antacid (magnesium hydroxide/aluminium hydroxide) did not affect the bioavailability of sildenafil.

Although studies of specific interactions with all drugs have not been conducted, according to population pharmacokinetic analysis pharmacokinetics sildenafil did not change with the simultaneous use of drugs belonging to the group of inhibitors CYP2C9 (tolbutamide, warfarin, phenytoin), group of inhibitors CYP2D6 (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), groups of thiazide and thiazide-like diuretics, loop and potassium-sparing diuretics, ACE inhibitors, calcium antagonists, antagonists of ?-adrenergic receptors, or inducers of CYP450 metabolism (such as rifampicin, barbiturates).

Nicorandil is a hybrid of calcium channel activator and nitrate. Nitrate component determines the possibility of its serious interaction with sildenafil.

the effect of sildenafil on other drugs.

Research in vitro .

sildenafil is a weak inhibitor isoforms 1A2, 2C9, 2C19, 2D6, 2E1 and ZA4 (IR 50 > 150 mmol) of cytochrome P450. Since peak plasma concentrations of sildenafil are approximately

1 mol, the effect of sildenafil on the clearance of substrates of these isoenzymes unlikely.

there are No data on the interaction of sildenafil and such nonspecific phosphodiesterase inhibitors like theophylline and dipyridamole.

Research in vivo .

since it is known that sildenafil affects the metabolism of nitric oxide/cyclic guanosine monophosphate (cGMP), it has been found that this drug potentiates the hypotensive effect of nitrates, so its simultaneous use with nitric oxide donors or nitrates in any form is contraindicated.

in some predisposed patients simultaneous use of sildenafil and blockers ?-adrenoretseptorov can lead to the development of symptomatic hypotension, most often occurred within 4:00 after the use of sildenafil. In the course of the research the specific interaction between drugs blocker of ?-adrenergic receptors doxazosin (4 mg and 8 mg) and sildenafil (25 mg, 50 mg and 100 mg) were applied simultaneously to patients with benign hyperplasia of the prostate, stabilization of a condition which was achieved with the use of doxazosin. In these study populations was observed, the average additional reduction in blood pressure in the supine position on a 7/7 mm Hg. art., 9/5 mm Hg. article and 8/4 mm Hg. C. the average reduction of blood pressure in the standing position on 6/6 mm Hg. art., 11/4 mm Hg. art., 4/5 mm Hg. the article under. With the simultaneous use of sildenafil and doxazosin, patients whose stabilization was achieved by using doxazosin were sometimes reported to develop symptomatic orthostatic hypotension. In these, it has been reported cases of dizziness and lightheadedness, but no syncope.

no significant interactions were observed with simultaneous use of sildenafil (50 mg) and tolbutamide (250 mg) and warfarin (40 mg), which were metabolized by CYP2C9.

sildenafil (50 mg) did not lead to an increase in bleeding time caused by acetylsalicylic acid (150 mg).

sildenafil (50 mg) without potentiating the antihypertensive effect of alcohol in healthy volunteers at medium maximum blood ethanol levels of 80 mg/DL.

in patients receiving sildenafil, there was no difference in side effect profile compared to placebo while the use of such classes of antihypertensive drugs, like diuretics, ?-adrenergic blocker, ACE inhibitors, angiotensin II antagonists, antihypertensive medicinal products (vasodilator and centrally acting) , adrenergic neuron blockers, calcium channel blockers, and blockers of ?-adrenergic receptors. In a special study of interaction with the simultaneous use of sildenafil (100 mg) and amlodipine in patients with hypertension, there was an additional decrease in systolic blood pressure in the lying position of 8 mm Hg. Art.

the Decrease in diastolic blood pressure was 7 mm Hg. article the magnitude of these additional reductions in blood pressure were comparable with those observed with the use of sildenafil in healthy volunteers.

sildenafil in a dose of 100 mg did not affect the pharmacokinetic parameters of HIV protease inhibitors, saquinavir and ritonavir, which are substrates of CYP3A4. 

application Features

prior to therapy, a medical history of the patient should be collected and a physical examination conducted to diagnose erectile dysfunction and determine its possible causes.

since sexual activity is accompanied by a certain risk from the heart, the doctor must assess the patient's cardiovascular system prior to any treatment of erectile dysfunction. Sildenafil has a vasodilating effect, which is manifested by a slight and short-term decrease in blood pressure. Prior to sildenafil's appointment, the physician should carefully consider whether such an effect can adversely affect patients with certain underlying diseases, especially when combined with sexual activity. To patients with hypersensitivity to vasodilators include patients with obstruction of the excretory tract of the left ventricle (eg aortic stenosis, hypertrophic obstructive cardiomyopathy), or patients with a rare syndrome, Multisystem atrophy, one manifestation of which is severe dysregulation of blood pressure the autonomic nervous system.

sildenafil potentiates the hypotensive effect of nitrates.

Reported serious adverse reactions from the cardiovascular system, including myocardial infarction, unstable angina, sudden cardiac death, ventricular arrhythmia, cerebrovascular hemorrhage, transient ischemic attack, arterial hypertension and arterial hypotension, which coincided with the use of sildenafil. Most patients (but not all), there were risk factors of cardiovascular diseases. Many of these adverse reactions were observed during or immediately after sexual intercourse, and only a few occurred shortly after the use of sildenafil without sexual activity. Therefore, it is impossible to determine whether the development of such adverse reactions is directly related to risk factors or their development is due to other factors.

preparations for the treatment of erectile dysfunction, including sildenafil, should be administered with caution in patients with anatomical deformities of the penis (such as angulation, cavernous fibrosis or Peyronie's disease) or patients with conditions that contribute to the development of priapism (such as sickle cell anemia, multiple myeloma, or leukemia).

Safety and efficacy of simultaneous use of sildenafil with other methods of treatment of erectile dysfunction have not been studied, so the appointment of such combinations is not recommended.

it was Reported about disorders of view cases partiranno anterior ischemic optic neuropathies associated with the use of sildenafil and other inhibitors PDE-5. Patients should be warned that in the event of a sudden impairment of the drug was Aerosil should stop and immediately consult a doctor.

Simultaneous use of sildenafil and ritonavir is not recommended.

Patients receiving blockers ?-adrenergic receptors, assign sildenafil should be used with caution as this combination may lead to symptomatic hypotension in some predisposed patients. Symptomatic hypotension usually occurs within 4: 00 after the use of sildenafil. In order to minimize the risk of orthostatic hypotension, sildenafil therapy can be started only in hemodynamically stable patients taking ?-adrenoreceptor blockers. The recommended starting dose for such patients is 25 mg of sildenafil. In addition, patients should be informed how to act in case of symptoms of orthostatic hypotension.

Studies of human platelets demonstrated that in vitro sildenafil potentiates the antiaggregatory effects of sodium nitroprusside. There is no information about the safety of the use of sildenafil in patients with coagulation disorders or acute peptic ulcer disease. Thus, the use of sildenafil in patients of this group is possible only after a thorough assessment of the ratio of benefit and risk.

the Drug was Aerosil contains lactose, therefore it should not be used men with such rare genetic disorders as galactose intolerance, lactase deficiency or malabsorption of glucose-galactose. 

use during pregnancy or lactation.

the Drug is used for women.

Ability to influence the reaction rate when driving motor transport or operating other mechanisms.

no study was conducted on the effect of the drug on the ability to drive or operate machinery.

Because during clinical studies of sildenafil were observed dizziness and blurred vision, patients should know their individual reactions to the drug was Aerosil before you drive or operate machinery.

Method of application and doses

Tablets are intended for oral administration. For realization of effect of sildenafil sexual excitement is necessary.

the recommended dose of Eurosilo is 50 mg and is used when needed, around 1:00 to sexual intercourse. Depending on the effectiveness and tolerance of the drug dose can be increased to 100 mg or reduced to 25 mg. (tablets Are used in the appropriate dosage). The maximum recommended dose is 100 mg. the Maximum recommended frequency of use-1 time per day. In applying the drug was Aerosil during the meal its effect may come later than when applied on an empty stomach.

elderly Patients.

there is no need for dose adjustment for elderly patients.

patients with renal insufficiency.

for patients with mild to moderate renal insufficiency (creatinine clearance 30 to 80 ml/min), the recommended dose is similar to the dose given above.

Because patients with severe renal failure (creatinine clearance

patients with hepatic insufficiency.

since the clearance of sildenafil is reduced in patients with hepatic insufficiency (e.g. cirrhosis of the liver), the recommended dose is 25 mg. (tablets Are used in the appropriate dosage). Depending on the effectiveness and tolerance of the drug dose can be increased to 50 mg or 100 mg.

Patients who use other drugs.

the Recommended starting dose for patients who use CYP3A4 inhibitors, except ritonavir, is 25 mg. (tablets Are used at the appropriate dosage). 

in order to reduce the risk of orthostatic hypotension, the condition of patients taking ?-adrenoreceptor blockers should be stabilized before use of sildenafil. Also, the recommended dose of sildenafil is 25 mg. (tablets are Used in the appropriate dosage).

Children.

the Drug is not used for children.

Overdose

Symptoms.when using a single dose of sildenafil to 800 mg undesirable reactions were similar to those observed in the application of sildenafil at lower doses, but their frequency and severity grew. Taking 200 mg of sildenafil does not lead to increased efficiency, but leads to an increase in the number of cases of adverse reactions (headache, tides, dizziness, dyspepsia, nasal congestion, visual impairment).

Treatment.& nbsp;in case of overdose, if necessary, symptomatic therapy should be used. Since sildenafil largely binds to plasma proteins and is not excreted in the urine, there is no reason to expect renal dialysis to accelerate clearance.

Side effects

most Often it is possible adverse reactions such as headache, flushes, dyspepsia, visual disturbances, nasal congestion, dizziness and impaired color vision.

from the immune system:hypersensitivity reactions.

from the nervous system:headache, dizziness, drowsiness, hypesthesia, stroke, transient ischemic attack, convulsions, court relapses, fainting.

from the cardiovascular system:blood flow to the face, palpitations, tachycardia, arterial hypertension, arterial hypotension, myocardial infarction, atrial fibrillation, ventricular arrhythmia, unstable angina pectoris, sudden cardiac death.

on the part of the organ of vision: impaired vision; impaired color perception disorders of the conjunctiva, lacrimation disorder; other disorders of the organs of sight; partitially anterior ischemic neuropathy optic nerve, occlusion of retinal vessels, visual field defects.

hearing aid:vertigo, tinnitus, deafness.

from the respiratory system:nasal congestion, nasal bleeding.

from the digestive tract:dyspepsia, nausea, vomiting, dry mouth.

skin side:skin rashes, Stevens-Johnson syndrome, toxic epidermal necrolysis.

from the musculoskeletal system:myalgia.

from the urinary system:hematuria.

Common disorders:chest pain, fatigue.

Examinationincreased heart rate.

on the part of the reproductive system:hematospermia, bleeding from the penis, priapism, prolonged erection.

The

shelf Life

3 years.

storage Conditions

Store in its original packaging at a temperature not exceeding 25 ° CoC.

keep out of reach of children.

The

Packaging

1 or 2 or 4 tablets in a blister, 1 blister 1 or 2 or 4 in a cardboard box.

The

Category vacation

According to the recipe.

The

Manufacturer

LLC "Astrafarm".

location of the manufacturer and address of the place of business

Ukraine, 08132, Kiev region, Kievo-Svyatoshinsky district, g. . Vishnevoe, Kievskaya str., 6.

HOMVIO-PROSTAN ORAL DROPS 50ML

Homvio-Prostan drops for oral use – homeopathic medicine. The effect of the drug has a preventive and curative effect in diseases of the genitourinary tract. For easy use and accurate compliance with the dosing tool that comes in a vial-dropper. 

with prolonged use, analgesic, anti-inflammatory, antispasmodic effect is observed. At the same time normalizes the muscle membrane of the bladder.

When given

Uncontrolled self-medication may worsen physical condition, so the medication and therapy regimen are prescribed by a physician at:

    The
  • small Diseases of the genitourinary system.
  • The
  • Increase in size of the prostate gland (only male patients).
  • The
  • Urethritis.
  • The
  • Prostatitis.
  • The
  • Chronic form of cystitis.
  • Chronic, acute form of urination delay.
  • The
  • to suffer.
  • The
  • Pyelonephritis.
  • urinary Incontinence.

instructions for use

If you are diagnosed with the disease in the chronic form, Homvio-prostan issued at a dosage of 10 drops up to 3 times in 24 hours. The average daily norm can be increased to 15 drops on the lack of effectiveness of therapy. 

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