Vizarsin Ku-tab - Instructions For The Use Of Tablets, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Vizarsin Ku-tab

Vizarsin Ku-tab: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Vizarsin Q-tab

ATX code: G04BE03

Active ingredient: sildenafil (sildenafil)

Manufacturer: Krka (Slovenia)

Description and photo update: 2018-26-10

Prices in pharmacies: from 705 rubles.

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Vizarsin Ku-tab - a medicine for the treatment of erectile dysfunction; PDE-5 inhibitor.

Release form and composition

Vizarsin Ku-tab is produced in the form of tablets dispersed in the oral cavity: slightly biconvex, round, almost white or white, with a mint smell, possibly the presence of dark inclusions (1 pc. In a blister, in a cardboard box 1 or 2 blisters; by 4 pcs. In a blister, in a cardboard box 1, 2 or 3 blisters).

Composition of 1 tablet:

• active substance: sildenafil - 25, 50 or 100 mg;
• additional components: aspartame, dihydrochalcone neohesperidin (E959), calcium silicate FM1000, crospovidone type A, mannitol, hyprolose, mint flavor, magnesium stearate, peppermint flavor (field mint oil, acacia gum, water, levomenthol, sorbitol), maltodextrin

Pharmacological properties

Pharmacodynamics

Sildenafil is a potent selective inhibitor of cyclic guanosine monophosphate (cGMP), a specific phosphodiesterase type 5 (PDE-5). The substance restores impaired erectile function under conditions of sexual stimulation by increasing blood flow in the vessels of the penis.

The physiological mechanism leading to penile erection is the release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation.

By activating the enzyme guanylate cyclase, NO causes an increase in cGMP levels and subsequent relaxation of the smooth muscle cells of the cavernous tissue, which promotes its filling with blood.

Without exerting a direct relaxing effect on the isolated human corpus cavernosum, sildenafil enhances the effect of NO due to the suppression of PDE-5, which is responsible for the breakdown of cGMP. During the activation of the NO / cGMP system, which occurs during sexual stimulation, inhibition of PDE-5 by sildenafil leads to an increase in the concentration of cGMP in the corpora cavernosa. Therefore, for the positive pharmacological effect of Vizarsin Ku-tab, sexual stimulation is necessary.

In vitro studies have demonstrated that sildenafil is selective for PDE-5, which is involved in the development of erection. This effect of the substance in relation to PDE-5 is significantly superior to its activity in relation to other known PDEs. In relation to PDE-6, which is involved in phototransmission in the retina, the selectivity of sildenafil is 10 times less. When the agent is used in the maximum recommended doses, its selectivity to PDE-5 exceeds that to PDE-1 by 80 times, and to PDE-2, 3, 4, 7, 8, 9, 10 and 11 - by 700 times or more. The observed activity of sildenafil to PDE-3 (cAMP-specific isoform of PDE), which takes part in the control of cardiac muscle contractility, is approximately 4000 times weaker than the activity to PDE-5.

The agent can cause a temporary slight decrease in blood pressure (BP), usually without clinical manifestations. After taking Vizarsin Ku-tab at a dose of 100 mg, the maximum decrease in systolic blood pressure in the supine position was approximately 8.3 mm Hg. Art., and diastolic blood pressure - 5.3 mm Hg. Art. This effect is associated with the vasodilating effect of sildenafil, presumably due to an increase in the level of cGMP in the smooth muscle cells of the vascular walls. In healthy volunteers, a single use of the drug at a dose of less than 100 mg did not cause clinically significant changes in the electrocardiogram (ECG). Sildenafil did not affect cardiac output and did not lead to impaired blood flow through stenotic arteries.

In the presence of erectile dysfunction and stable angina pectoris in patients who regularly received antianginal drugs (with the exception of nitrates), after taking Vizarsin Ku-tab in comparison with placebo, there were no significant differences in the time interval before the development of angina pectoris during an exercise test.

In some cases, 1 hour after taking sildenafil at a dose of 100 mg using the Farnsworth Munsell 100-shade test, patients showed a temporary change in the ability to distinguish certain shades of colors (blue / green). These changes were not detected 2 hours after taking the drug. It is assumed that the violation of color recognition is due to inhibition of PDE-6. No effect of the agent on contrast perception, visual acuity, electroretinogram, pupil diameter or intraocular pressure was noted. In patients diagnosed with an early stage of age-related macular degeneration, Vizarsin Ku-tab at a dose of 100 mg with a single dose did not lead to clinically significant changes in vision, assessed by the corresponding tests (visual acuity, color perception, Amsler grating, photostress and Humphrey perimetry).

When taking 100 mg of sildenafil in healthy volunteers, no changes in sperm morphology or motility were observed.

In studies using fixed doses of sildenafil, the number of men who reported improved erections was 62% at a dose of 25 mg, 74% at a dose of 50 mg, 82% at a dose of 100 mg, compared with 25% in the placebo group. … The analysis of the international index of erectile dysfunction showed that in addition to improving erection, the use of the drug also increased the quality of orgasm and ensured the achievement of satisfaction from intercourse. The effectiveness and safety of Vizarsin Ku-tab were preserved with prolonged use.

Pharmacokinetics

Sildenafil is rapidly absorbed. After oral administration on an empty stomach, the maximum concentration (Cmax) of the substance in the blood plasma is reached within 30–120 minutes (median 60 minutes). The absolute bioavailability is approximately 41% (25 to 63%). In the dose range of 25–100 mg sildenafil pharmacokinetics [Cmax and area under the concentration-time curve (AUC)] is linear. Taking the drug with food reduces the rate of absorption, while the period for reaching the maximum concentration (T _Cmax) increases by about 60 minutes, and Cmax decreases by about 29%.

The volume of distribution (Vd) of the drug in the state of equilibrium concentration is on average 105 liters, after a single oral dose of 100 mg Cmax can be equal to 440 ng / ml (the coefficient of variation is 40%). Due to the fact that the binding of the active substance and its main circulating metabolite to blood plasma proteins reaches 96%, the average plasma concentration of the free fraction of sildenafil can be 18 ng / ml (38 nmol). 1.5 hours after oral administration of 100 mg of Vizarsin Q-tab in healthy volunteers, less than 0.0002% of the dose was found in the semen (average 188 ng).

The process of metabolic transformation of sildenafil occurs mainly in the liver with the participation of cytochrome P450 microsomal isoenzymes: CYP3A4 (main pathway) and CYP2C9 (additional pathway). Sildenafil's main circulating metabolite is formed by N-demethylation of sildenafil. The selectivity of the metabolite in relation to PDE is comparable to that of sildenafil, the activity of the metabolite to PDE-5 in vitro can be 50% of the activity of the substance in the initial dose. In the blood plasma of healthy volunteers, the level of this metabolic product is 40% of the level of sildenafil, and it undergoes further biotransformation, its half-life (T _1/2) is approximately 4 hours.

The total clearance of sildenafil is 41 liters per hour, the final T _1/2 is 3-5 hours. Excretion of the substance in the form of metabolites is carried out mainly by the intestines - about 80% of the dose, and in a smaller amount by the kidneys - about 13% of the dose.

Indications for use

According to the instructions, Vizarsin Ku-tab is recommended for use 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 satisfactory intercourse.

Sexual arousal is required for the effect of the drug.

Contraindications

Absolute:

• myocardial infarction or cerebrovascular accident (stroke), suffered in the last 6 months;
• arterial hypotension (blood pressure below 90/50 mm Hg. Art.);
• severe heart failure, unstable angina and other severe forms of cardiovascular lesions, in the presence of which sexual activity is not recommended for men;
• severe functional disorders of the liver;
• congenital fructose intolerance (since sorbitol is included in Vizarsin Q-tab);
• phenylketonuria (since the aspartame contained in the product is a source of phenylalanine);
• loss of vision in one eye due to a non-arteritic form of anterior ischemic neuropathy of the optic nerve (non-arteritis AION), regardless of whether this pathology is associated or not with the previous use of PDE-5 inhibitors;
• hereditary degenerative diseases of the retina (hereditary retinal dystrophies), such as retinitis pigmentosa (with the possible presence of genetic disorders of the retinal PDE), since the safety profile of sildenafil in such patients has not been studied;
• simultaneous use with NO donors (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 drugs for the treatment of erectile dysfunction, since the efficacy and safety of Vizarsin Ku-tab in this combination has not been studied;
• age up to 18 years;
• combination with ritonavir;
• hypersensitivity to any of the constituents of the drug.

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;
• syndrome of multiple system atrophy or obstruction of the outflow tract of the left ventricle of the heart [hypertrophic obstructive cardiomyopathy (GOKMP), aortic stenosis];
• blood pressure readings above 170/100 mm Hg. Art.;
• conditions that predispose to the occurrence of priapism (leukemia, multiple myeloma, sickle cell anemia);
• anatomical deformity of the penis (cavernous fibrosis, angulation, or Peyronie's disease);
• the period of exacerbation of gastric ulcer or 12 duodenal ulcer, diseases accompanied by bleeding (due to the lack of information on the safety of use);
• a history of indications of episodes of development of non-arteritis AION;
• simultaneous administration of alpha-blockers.

Instructions for use of Vizarsin Ku-tab: method and dosage

Vizarsin Ku-tab is taken orally.

Oral dispersible tablets can be used as an alternative form for patients who have difficulty swallowing film-coated tablets of Vizarsin. As oral dispersible tablets are fragile and break easily, it is not recommended to squeeze them through the foil of the package. Do not take the tablet with wet hands as it may begin to dissolve.

Before taking, you need to take a blister with the drug and bend it along the line of the gap. To open the blister, gently pull on the edge of the foil and carefully remove the tablet by shaking it out into your palm. After that, the pill must be immediately put on the tongue, and in order to facilitate swallowing, it must be kept in the mouth for several seconds until it is completely dissolved. Then Vizarsin Ku-tab can be washed down with liquid.

Do not mix the dispersible tablet in the mouth with food. When using the drug with fatty foods, its effect may 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 needed. The dose of Vizarsin 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 - seizures, transient ischemic attack, recurrent seizures;
• gastrointestinal tract: often - dyspepsia; infrequently - nausea, dry mouth, vomiting;
• musculoskeletal and connective tissue: infrequently - myalgia;
• mammary gland and genitals: infrequently - bleeding from the penis, hematospermia; with an unknown frequency - prolonged erection, priapism;
• urinary system: infrequently - hematuria;
• skin and subcutaneous tissue: infrequently - skin rash; with an unknown frequency - toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome;
• cardiovascular system (CVS): often - a feeling of hot flashes; infrequently - tachycardia, palpitations; rarely - atrial fibrillation, increase / decrease in blood pressure, myocardial infarction; with an unknown frequency - unstable angina pectoris, ventricular arrhythmia, sudden cardiac death;
• labyrinthine disorders and the organ of hearing: often - tinnitus, vertigo; rarely - deafness;
• organ of vision: often - visual impairment, chromatopsia (impaired color perception); infrequently - violation of lacrimation, damage to the conjunctiva; with unknown frequency - visual field defect, retinal vascular occlusion, non-arteritic AION;
• organs of the chest and mediastinum, respiratory system: often - nasal congestion; rarely - nosebleeds;
• immune system: rarely - hypersensitivity reactions;
• laboratory and instrumental data: infrequently - increased heart rate;
• other disorders: infrequently - increased fatigue, chest pain.

Overdose

With a single dose of Vizarsin Ku-tab in doses less than 800 mg, the side effects were similar to those when using sildenafil in lower doses, but the frequency and severity of these disorders increased. The use of the drug at a dose of 200 mg did not lead to an increase in its effect, however, it caused an increase in the frequency of undesirable reactions, such as nasal congestion, dyspepsia, headache, dizziness, hot flushes, and visual disturbances.

In case of an overdose, symptomatic treatment is performed. Hemodialysis is ineffective because sildenafil has a strong bond with blood plasma proteins and is not excreted by the kidneys.

special instructions

Before starting drug therapy in order to diagnose erectile dysfunction and determine the 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 from CVS associated with sexual activity, it is necessary to assess the patient's condition before starting any course of treatment for erectile dysfunction. Mortality rates from CVD diseases and the incidence of myocardial infarction with sildenafil did not differ from those in the placebo group.

In the course of post-marketing use of sildenafil, there have been reports of serious cardiovascular complications (associated with the use of this drug) including sudden cardiac death, myocardial infarction, ventricular arrhythmia, unstable angina pectoris, transient ischemic attack, cerebrovascular hemorrhage / hypotension. Most of the patients in 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 starting it, it is necessary to carefully assess the possible threat of these undesirable manifestations against the background of certain concomitant diseases, especially during sexual activity. An increased susceptibility to vasodilating action is observed in patients with GOKMP, aortic stenosis, or with a rare syndrome of multiple systemic atrophy, accompanied by severe impairment of autonomic 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, since with an individual predisposition this can cause 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 Vizarsin Ku-tab against the background of treatment with alpha-blockers only after stabilization of hemodynamic parameters is achieved. Also in this case, it is recommended to reduce the initial dose of sildenafil to 25 mg. For patients already receiving sildenafil when prescribing alpha-blocker therapy, it is advisable to start the use of the latter with a low dose. The subsequent decrease in blood pressure with this combination can be caused by a gradual increase in the dose of alpha-blockers. The patient should be informed about how to act if signs of orthostatic hypotension occur.

During treatment with all PDE-5 inhibitors (including sildenafil), there have been rare reports of the occurrence of non-arteritic AION, which proceeds with deterioration or loss of vision. The development of this pathology was observed in patients, most of whom had such risk factors as hyperlipidemia, diabetes mellitus, age over 50 years, deepening (excavation) of the optic nerve head, ischemic heart disease (IHD), arterial hypertension. The 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.

During therapy with PDE-5 inhibitors, including sildenafil, cases of hearing loss or sudden hearing loss have been reported, mainly in patients who had risk factors for these adverse reactions. It is impossible to establish whether the loss or sudden deterioration of hearing is related to taking sildenafil. With the development of these violations, it is required to refuse to take the drug and immediately seek medical help.

Influence on the ability to drive vehicles and complex mechanisms

There is no information about the negative impact of Vizarsin Ku-Tab on the ability to work with complex mechanisms and drive a car. However, since dizziness, decreased blood pressure, blurred vision, chromatopsia and other similar effects may occur while taking the drug, in these situations patients need to determine their individual susceptibility to the use of sildenafil, especially at the beginning of therapy and when adjusting the dose.

Application during pregnancy and lactation

Vizarsin Ku-tab according to the registered indication is not intended for use in women.

Pediatric use

Vizarsin Ku-tab is not used in pediatric practice.

With impaired renal function

In the presence of mild or moderate functional renal impairment [creatinine clearance (CC) 30–80 ml / min], the pharmacokinetic parameters of sildenafil did not change after a single dose of 50 mg. When compared with healthy peers, the average Cmax and AUC values of the N-demethylated metabolite increased by 73 and 126%, respectively. Against the background of severe renal failure (CC below 30 ml / min), there was a decrease in the clearance of sildenafil, leading to an increase in Cmax and AUC values by about 2 times (by 88 and 100%, respectively) when compared with patients without renal impairment from the same age group. groups.

With renal failure of mild and moderate severity (CC 30–80 ml / min), dose adjustment is not necessary.

For patients with severe renal insufficiency, the dose of Vizarsin Q-tab needs to be reduced to 25 mg. Depending on the tolerance and effectiveness of the drug, it can be further increased to 50 and 100 mg.

For violations of liver function

In the presence of class A and B liver cirrhosis according to the Child-Pugh classification, the clearance of sildenafil decreases, which causes an increase in Cmax and AUC (by 47 and 84%, respectively) in comparison with patients of the same age group with normal liver function. In patients with severe liver dysfunction, the pharmacokinetics of the drug have not been studied.

With existing hepatic pathologies (in particular, with cirrhosis), the dose of Vizarsin Ku-tab must be reduced to 25 mg, with a possible further increase to 50 and 100 mg, taking into account the tolerability and result of therapy.

Use in the elderly

In healthy patients aged 65 and over, the clearance of sildenafil is reduced, and the plasma levels of this substance and its active N-demethylated metabolite are approximately 90% higher than in young men 18–45 years old. The plasma concentration of free sildenafil, taking into account the age-related characteristics of binding to proteins, increases by about 40%.

Elderly patients dose adjustment of Vizarsin Ku-tab is not required.

Drug interactions

Potential effect of other drugs / agents on the pharmacokinetic parameters of sildenafil:

• cytochrome P450 isozymes (according to in vitro studies): a decrease in clearance may be observed;
• inhibitors of the isoenzyme CYP3A4 (including cimetidine, erythromycin, ketoconazole): there is a decrease in drug clearance, but the frequency of adverse reactions does not increase (sildenafil should be taken with a dose of 25 mg);
• ritonavir (a potent inhibitor of cytochrome P450), HIV protease inhibitor (2 times / day at a dose of 500 mg): AUC and Cmax in blood plasma increase 11 and 4 times, respectively, after 24 hours the plasma level of sildenafil is approximately 200 ng / ml (when taking one sildenafil - 5 ng / ml; the combination is contraindicated);
• saquinavir (an inhibitor of the isoenzyme CYP3A4), an inhibitor of HIV protease (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 is possible;
• erythromycin (5 days, 2 times / day at a dose of 500 mg): AUC increases by 182%;
• azithromycin (3 days, 500 mg per day): AUC, Tmax, Cmax, T _{½ of} sildenafil or its main metabolite do not change;
• cimetidine (800 mg): the 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 a nitrate and a potassium channel activator): there is a possibility of a serious interaction between these agents;
• thiazides and thiazide-like diuretics, loop and potassium-sparing diuretics, inhibitors of the CYP2C9 isoenzyme (phenytoin, warfarin, tolbutamide), inhibitors of the CYP2D6 isoenzyme (tricyclic antidepressants, selective inhibitors of serotonin reuptake of serotonin 50, serotonin reuptake inhibitors) (ACE), beta-blockers: changes in the pharmacokinetic parameters of the drug were not identified;
• grapefruit juice: a slight increase in the level of the active substance in the blood plasma is possible.

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

• cytochrome P450 isozymes 2C9, 1A2, 2C19, 2E1, 2D6, and 3A4 [concentration of semi-maximum inhibition (IC ₅₀) ≥150 μmol]: according to in vitro studies, the effect of the drug on the 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 fainting are possible;
• warfarin (40 mg), tolbutamide (250 mg): no interaction with sildenafil (50 mg) was found;
• acetylsalicylic acid (150 mg): additional lengthening of bleeding time when combined with the drug (50 mg) has not been established;
• ethanol: when combined with sildenafil (50 mg) in healthy volunteers, the hypotensive effect of ethanol does not increase (Cmax of ethanol in blood serum is about 80 mg / dl);
• alpha-blockers, slow calcium channel blockers, blockers of adrenergic neurons, centrally acting drugs, vasodilators, angiotensin II receptor antagonists, ACE inhibitors, beta-blockers, diuretics and other antihypertensive drugs: differences in side effects with these combinations from the effects in patients taking placebo, not marked;
• 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): no changes in the pharmacokinetic parameters of these agents were noted.

Analogs

Analogs of Vizarsin Ku-tab are: Silafil, Vizarsin, Viasan-LF, Dinamiko, Sildenafil, Ridzhamp, Vildegra, Taxier, Viatail, Erexesil, Revatsio, Maxigra, Sildenafil VERTEX, Viagra, Sildenafil SZ, Silden Strnetisron.

Terms and conditions of storage

Store in its original packaging out of the reach of children, at a temperature not exceeding 25 ° C.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Vizarsin Ku-Tab

According to the overwhelming majority of reviews, Vizarsin Ku-Tab is an effective tool used to treat erectile dysfunction to restore quality of life. Many patients also like that the drug does not need to be taken with a liquid and that it is compatible with alcoholic beverages.

Some patients note such disadvantages as the development of undesirable effects in the form of severe headache, flushing of the facial skin, a feeling of heaviness in the chest, nausea, dry mouth, allergies.

Price for Vizarsin Ku-Tab in pharmacies

The approximate price for Vizarsin Ku-tab can be within:

• tablets 50 mg: 1 pc. in the package - 260–420 rubles, 4 pcs. - 520-710 rubles;
• tablets 100 mg: 1 pc. in the package - 320-610 rubles, 4 pcs. - 620-880 rubles.

Vizarsin Ku-tab: prices in online pharmacies

Drug name Price Pharmacy

Vizarsin Ku-tab 50 mg tablets, dispersible in the oral cavity 4 pcs. 705 RUB Buy

Vizarsin KU-Tab tablets dispersion 100mg 4 pcs. 795 RUB Buy

Vizarsin Ku-tab 100 mg orodispersible tablets 4 pcs. 795 RUB Buy

Vizarsin Ku-tab 100 mg oral dispersible tablets 12 pcs. 1388 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!