sildenafil | Vizarsin Ku-tab dispersible tablets in the oral cavity 100 mg 4 pcs.

Latin name

Vizarsin Q- tab

Release form

Oral dispersible tablets: slightly biconvex, round, almost white or white, with a minty odor, dark spots are possible



packaging 4 pcs

Pharmacological action of

Selective inhibitor of cycloguanosine monophosphate (cGMP) -specific PDE5. PDE5, responsible for the breakdown of cGMP, contained not only in the cavernous body of the penis, but also in the vessels of the lungs.

Restores impaired erectile function and provides a natural response to sexual arousal.

Sildenafil does not have a direct relaxing effect on the cavernous body, but it actively enhances the relaxing effect of nitric oxide on this tissue. With sexual arousal, a local release of NO under the influence of sildenafil leads to inhibition of PDE5 and an increase in the level of cGMP in the cavernous body, as a result of which there is a relaxation of smooth muscles and increased blood flow in the cavernous body.

Being an inhibitor of PDE5, sildenafil increases the content of cGMP in smooth muscle cells of the pulmonary vessels and causes their relaxation. In patients with pulmonary hypertension, taking sildenafil leads to vasodilation 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 PDE 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 greater than its activity against PDE3, a cAMP-specific PDE involved in heart contraction.

Sildenafil may cause a mild and transient impairment of color discrimination (blue / green). The supposed mechanism of color vision impairment is considered to be the inhibition of PDE6, which is involved in the process of light transmission in the retina. In vitro studies have shown that the effect of sildenafil on PDE6 is 10 times less than its activity against PDE5.

Indications

According to the instructions, Vizarsin Ku-tab is recommended for the treatment of erectile dysfunction, which is characterized by the inability to achieve or maintain an erection of the penis, which is necessary for a satisfactory intercourse. Sexual arousal is required to manifest the effect of the drug.

Contraindications

Absolute:

myocardial infarction or cerebrovascular accident (stroke) suffered in the last 6 months

hypotension (blood pressure below 90/50 mmHg)

severe heart failure, unstable heart disease vascular lesions in the presence of which the sexual activity of

is not recommended for men, expressed functional liver disorders

congenital intolerance to fructose (since sorbitol is included in the composition of Visarsin Ku-tab)

phenylketonuria (since aspartame contained in the product is a source of phenylalanine)

loss of vision per one eye caused by a non-arteritic form of anterior ischemic optic neuropathy (non-arteritic AION), regardless of whether this pathology is associated or not with previous use m PDE5 inhibitors

hereditary degenerative retinal disease (Hereditary retinal dystrophies), such as retinitis pigmentosa (with the possible presence of genetic disorders of the retina PDE), t. k. the safety profile of sildenafil in such patients has not been studied

concurrent use with donors NO (including amyl nitrite) or nitrates in any form due to the fact that sildenafil can enhance the antihypertensive effect of nitrates (mediated through NO / cGMP)

combined use with other agents for the treatment of erectile dysfunction , since the efficacy and safety of Vizarsin Ku-tab in this combination has not been studied

age under 18

combination with ritonavir

hypersensitivity to any of the components of the drug ata.

Vizarsin Ku-tab is not intended for use in women.

Relative contraindications (sildenafil must be used with extreme caution in the presence of the following conditions / diseases):

life-threatening arrhythmias

multiple systemic atrophy syndrome or left ventricular outflow tract obstruction [hypertrophic obstructive cardiomyopathy (GOKMP), aortic stenosis]

blood pressure readings above 170/100 mm Hg. Art.

conditions predisposing to the occurrence of priapism (leukemia, multiple myeloma, sickle-cell anemia)

anatomical deformation of the penis (cavernous fibrosis, angulation or Peyronie's disease)

period of exacerbation of gastric ulcer or 12 duodenal ulcer disease lack of information on the safety of use)

history of history of episodes of the development of non-arteritic AION

administration of alpha-blockers.

Special instructions

Before starting drug therapy, in order to diagnose erectile dysfunction and identify possible causes of their development, it is necessary to study the patient's history and conduct a thorough clinical examination. Since there is a certain risk on the part of CVS due to sexual activity, it is necessary to assess the patient's condition before starting any course of treatment for erectile dysfunction. The mortality rates from CVD diseases and the incidence of myocardial infarction with sildenafil did not differ from those in comparison with patients from the placebo group. During the post-marketing use of sildenafil, there were reports of serious cardiovascular complications (time-related to taking this drug) including sudden cardiac death, myocardial infarction, ventricular arrhythmia, unstable angina, transient ischemic attack, cerebrovascular hemorrhage / hypertension. Most patients from this group had cardiovascular risk factors. Many of these cases occurred during or immediately after sexual activity, and a small number during the short period after taking sildenafil without sexual activity. It is impossible to establish a direct connection between the development of these pathologies and any factors. Due to the fact that Vizarsina Ku-tab has a vasodilating effect, leading to a temporary and slight decrease in blood pressure, before you start taking it, you must carefully evaluate the possible threat of these unwanted manifestations against the background of certain concomitant diseases, especially during sexual activity. Increased susceptibility to vasodilating action is noted in patients with GOKMP, aortic stenosis or with a rare syndrome of multiple systemic atrophy, accompanied by a severe violation of the autonomous regulation of blood pressure. Since alpha-blockers are vasodilators, when combined with PDE-5 inhibitors, the threat of an excessive decrease in blood pressure is aggravated. Patients receiving alpha-blockers should take Vizarsin Ku-tab with caution, because with an individual predisposition, this can cause the appearance of symptomatic arterial hypotension, usually observed within 4 hours after taking sildenafil. To minimize the likelihood of developing this complication, it is necessary to start taking Visarsin Ku-tab against the background of treatment with alpha-adrenergic blockers only after reaching stabilization of hemodynamic parameters. Also in this case, it is recommended to reduce the initial dose of sildenafil to 25 mg. For patients already receiving sildenafil when prescribing therapy with alpha-blockers, it is advisable to start using the latter with a low dose. A subsequent decrease in blood pressure with this combination may be caused by a gradual increase in the dose of alpha-blockers. The patient should be informed that how should he act in case of signs of orthostatic hypotension. Against the background of treatment with all PDE-5 inhibitors (including sildenafil), rare reports have been received about the occurrence of non-arteriotic AION, which occurs with deterioration or loss of vision. The development of this pathology was observed in patients, most of whom had risk factors such as hyperlipidemia, diabetes mellitus, age older than 50 years, deepening (excavation) of the optic head, coronary heart disease (CHD), and arterial hypertension. A causal relationship between the development of this complication and the use of PDE-5 inhibitors could not be determined. In case of sudden loss of vision, it is necessary to stop taking Vizarsin Ku-tab and immediately consult a specialist. When treating with PDE-5 inhibitors, including sildenafil, cases of loss or sudden hearing loss were recorded, mainly in patients who had risk factors for these adverse reactions. It is not possible to determine whether loss or sudden hearing loss is associated with sildenafil. With the development of these disorders, it is required to refuse to take the drug and immediately seek medical help.

Composition

Composition 1 tablet:

active substance: sildenafil - 100 mg

additional components: aspartame, neohesperidin dihydrochalcon (E959), calcium silicate FM1000, crospovidone type A, mannitol, hyprolose, peppermint flavoring (peppermint flavoring field mint oil, acacia gum, water, levomenthol, sorbitol, maltodextrin).

Dosage and administration of

Visarsin Ku-tab is taken orally. Dispersible tablets in the oral cavity can be used as an alternative form by patients who have difficulty swallowing Vizarsin film-coated tablets. Since tablets dispersible in the oral cavity are fragile and easily broken, it is not recommended to squeeze them out through the packaging foil. Do not take the tablet with wet hands due to the fact that it may begin to dissolve. Before taking, you need to take a blister with the drug and bend it along the break line. To open the blister, gently pull the edge of the foil and carefully remove the tablet by shaking it in the palm of your hand. After this, the tablet must be immediately put on the tongue, and in order to facilitate swallowing, keep for several seconds in the mouth until completely dissolved. Then Vizarsin Ku-tab can be washed down with liquid. Do not mix a dispersible tablet in your mouth with food. When using the drug with fatty foods, its effect can be observed later than when taken on an empty stomach. For most adult men, the recommended dose is 50 mg, which should be taken approximately 1 hour before sexual activity if necessary. The dose of Visarsin Ku-tab, taking into account its tolerability and effectiveness, can be increased to 100 mg or reduced to 25 mg. The maximum allowable dose should not exceed 100 mg, taken no more than 1 time per day.

Side effects

nervous system: very often - headache often - dizziness infrequently - hypesthesia, drowsiness rarely - fainting, impaired cerebral circulation with an unknown frequency - convulsions, transient ischemic attack, relapse of convulsions

gastrointestinal tract: often - dyspepsia infrequently - nausea, dry mouth, vomiting

musculoskeletal and connective tissue: infrequently - myalgia

mammary gland and genitals: infrequently - hemorrhage from the penis, with unknown frequency - prolonged erection, priapism

urinary system: infrequently - hematuria

skin and subcutaneous tissue: infrequently - skin rash with unknown frequency - toxic epidermal necrolysis (Lyell syndrome), Steve syndrome Jenson Johnson

cardiovascular system (CVS): often - hot flashes infrequently - tachycardia, palpitations rarely - atrial fibrillation, increased / decreased blood pressure, myocardial infarction with an unknown frequency - unstable angina, ventricular arrhythmia, sudden cardiac death

labyrinth disorders and hearing organ: often - tinnitus, vertigo rarely - deafness

organ of vision: often - visual impairment, chromatopsia (color perception disorder) infrequently - lacrimation, damage to the conjunctiva with an unknown frequency - visual field defect, occlusion vessels of the retina, non-arteritic AION

organs of the chest and mediastinum, respiratory system: often - nasal congestion rarely - nosebleeds

immune system: rarely - hypersensitivity reactions

laboratory e and instrumental data: infrequently - increased heart rate

other disorders: infrequently - increased fatigue, chest pain.

Drug interactions

Possible effect of other drugs / pharmacokinetic parameters of sildenafil:

isoenzymes of cytochrome P450 (according to in vitro studies): there may be a decrease in clearance of

inhibitors of isoenzyme CYP3A4 (including cirimetin, cicimetinum, is indicated) but the frequency of adverse reactions does not increase (taking sildenafil should be started with a dose of 25 mg)

ritonavir (a powerful inhibitor of cytochrome P450), an HIV protease inhibitor (2 times / day at a dose of 500 mg): AUC and Cmax in blood plasma increases by 11 and 4 times, respectively, after 24 hours, the plasma sildenafil level is approximately 200 ng / ml (when taking one sildenafil - 5 ng / ml combination is contraindicated)

saquinavir (CYP3A4 isoenzyme inhibitor), HIV protease inhibitor (3 times / day at a dose of 1200 mg): AUC and Cmax of sildenafil (1 time / day at a dose of 100 mg) increases by 210 and 140% respectively

itraconazole and ketoconazole (potent inhibitors of the CYP3A4 isoenzyme): a pronounced effect on the pharmacokinetics of the drug

erythromycin is possible (5 days, 2 times / day at a dose of 500 mg): AUC increases by 182% azithromycin (3 days at 500 mg per day): AUC, Tmax, Cmax, T sildenafil or its main metabolite does not change

cimetidine (800 mg): plasma concentration of sildenafil (50 mg) increases by 56%

aluminum / magnesium hydroxide: with a single dose, the bioavailability of the drug does not change

nicorandil (a hybrid of potassium channel nitrate and activator): there is the likelihood of a serious interaction of these agents

thiazides and thiazide-like diuretics, loop and potassium-sparing diuretics, inhibitors of the isoenzyme CYP2C9 (phenytoin, warfarin, tolbutamide), inhibitors of the isoenzyme CYP2D6 (tricyclic e antidepressants, selective serotonin reuptake inhibitors) isoenzyme inducers CYP450 (barbiturates, rifampicin), calcium antagonists, angiotensin converting enzyme (ACE) beta-blockers: changes in the pharmacokinetic parameters of the drug were not detected

grapefruit juice: a slight increase in the level of active substance in the blood plasma is possible.

Possible effect of Vizarsin Ku-tab on the pharmacokinetics of other drugs / agents:

isoenzymes of cytochrome P450 2C9, 1A2, 2C19, 2E1, 2D6, and 3A4 [half-maximum inhibition concentration (IC50) 150 μmol]: according to in vitro studies the drug for clearance of substrates of these isoenzymes is unlikely

doxazosin (alpha-blocker) in doses of 4/8 mg: in patients with benign prostatic hyperplasia and stable hemodynamics achieved with doxazosin, rare cases of symptomatic orthostatic hypotension, manifested by dizziness, but without syncope

warfarin (40 mg), tolbutamide (250 mg): interaction with sildenafil (50 mg) not found

acetylsalicylic acid (150 mg): additional prolongation of bleeding time when combined with the drug (50 mg) not found

ethanol : when combined with sildenafil (50 mg) in healthy volunteers, the hypotensive effect of ethanol does not increase (Cmax of ethanol in the blood serum is about 80 mg / dl)

alpha-blockers, slow calcium channel blockers, adrenergic neuron blockers, central de Corollary, vasodilators, angiotensin II receptor antagonists, ACE inhibitors, beta-blockers, diuretics and other hypotensive agents: differences between side effects in the data patterns of effects in patients treated with placebo, were observed

amlodipine: against the background of arterial hypertension, an additional decrease in blood pressure was established, which is comparable to that when using only sildenafil

saquinavir and ritonavir (HIV protease inhibitors): there were no changes in the pharmacokinetic parameters of these agents.

overdose

Side effects with a single intake of Vizarsin Ku-tab in doses of less than 800 mg were similar to those used with lower doses of sildenafil, but the frequency and severity of these disorders increased. The use of the drug at a dose of 200 mg did not increase its action, but caused an increase in the frequency of adverse reactions such as nasal congestion, dyspepsia, headache, dizziness, blood tides, disorders of the organ of vision. In case of overdose, symptomatic treatment is carried out. Hemodialysis is ineffective, as sildenafil has a strong association with blood plasma proteins and is not excreted by the kidneys.

Storage conditions

Store in the original package, out of the reach of children, at a temperature not exceeding 25 РC.

Shelf life

2 years.

Deystvuyushtee substance

Sildenafil

Terms and conditions

prescription

dosage form

tablets

Possible Product Names

Vizarsin Ku-Tab Dispersible Oral Tablets 100 mg 4 pcs