Levitra pills dispersible 2 pieces
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Active ingredients
Vardenafil
Release form
Pills
Composition
1 tab.: Vardenafil hydrochloride trihydrate (micronized) 11.852 mg, which corresponds to the content of rdenafil 10 mg. Additional substances: aspartame - 1.8 mg, peppermint flavoring (acacia gum, maltodextrin, menthol, peppermint leaf oil, peppermint field oil) - 2.7 mg, magnesium stearate - 4.5 mg, pharmaburst (Pharmaburst) (crospovidone, mannitol, colloidal silicon dioxide, sorbitol) - 159.15 mg.
Pharmacological effect
Drug for the treatment of erectile dysfunction. PDE5 inhibitor. An erection of the penis is a hemodynamic process, which is based on the relaxation of smooth mice of the cavernous bodies and arterioles located in it. During sexual stimulation, nitric oxide is released from the nerve endings of the cavernous bodies, activating the enzyme guanylate cyclase, which leads to an increase in the content of cyclic guanosine monophosphate (cGMP) in the cavernous bodies. As a result, smooth muscles of the cavernous bodies relax, which contributes to an increase in blood flow to the penis. The level of cGMP is regulated, on the one hand, by the synthesis of guanylate cyclase, and on the other hand, by the degradation (splitting) of cGMP by hydrolysis by phosphodiesterase (PDE). The best known PDE is cGMP specific phosphodiesterase type 5 (PDE5). By blocking PDE5 involved in the cleavage of cGMP, vardenafil thereby enhances the local action of endogenous nitric oxide in the corpus cavernosum during sexual stimulation. An increase in cGMP level due to inhibition of PDE5 leads to relaxation of smooth muscles of the corpus cavernosum and an increase in blood flow to them. This effect determines the ability of vardenafil to enhance the natural response to sexual stimulation. nM). The inhibiting activity of vardenafil on PDE5 is more pronounced than on other known PDEs (15 times more than PDE6, 130 times more than PDE1, 300 times more than PDE11 and 1000 times more than PDE- 2,3,4,7,8,9,10). Vardenafil increased cGMP in an isolated cavernous body, which led to the relaxation of smooth muscles. Vardenafil causes an erection of the penis, which depends on endogenous nitric oxide and is stimulated by donators of nitric oxide. The admission of vardenafil in a dose of 20 mg in some men caused an erection (sufficient for penetration) after 15 minutes. A complete response was achieved after 25 minutes (statistically significant and comparable to placebo).
Pharmacokinetics
Absorption The average time to reach Cmax after taking the drug on an empty stomach varies from 45 to 90 minutes. When comparing Levitra ODT (10 mg) with coated pills (10 mg), an increase in the average AUC value of vardenafil from 21% to 29% and a decrease in Cmax by 8-19% were noted. Meal, containing a large amount of fat, had no effect on the AUC and the time to reach Cmax of vardenafil, however, there was a decrease in the average Cmax of vardenafil by 35%. With these results in mind, Levitra ODT in the form of pills dispersed in the oral cavity can be taken regardless of the meal. If the pills dispersed in the oral cavity are washed down with water, the vardenafil AUC is reduced by 29%, and the median Tmax is reduced by 60 minutes, while Cmax does not change. Therefore, the drug Levitra ODT in the form of pills dispersed in the mouth should be taken without drinking water. The study of bioequivalence showed that Levitra ODT, in the form of pills dispersed in the mouth (10 mg), is not bioequivalent to Levitra ODT in the form of coated pills (10 mg). Therefore, pills dispersed in the oral cavity should not be used as equivalent to coated pills. Distribution Medium Vd vardenafil in a stable state of pharmacokinetic parameters averages 208 l, which demonstrates its good distribution in the tissues. Vardenafil and its main metabolite (M1) bind well to plasma proteins (up to 95%), and this property is reversible and does not depend on the total concentration of the drug. 90 minutes after taking vardenafil, no more than 0.00012% of the received dose can be determined in healthy sperm Patients. Metabolism Vardenafil is metabolized mainly by liver enzymes with the participation of cytochrome P450 (CYP) isoenzymes - CYP3A4, as well as CYP3A5 and CYP2C9. The blood contains glucuronide in the form of a conjugate (glucuronic acid), which is part of the M1 metabolite. The concentration of the rest of the M1 metabolite (non-glucuronic) is 26% of the concentration of the active substance. The phosphodiesterase selectivity profile of M1 is similar to that of vardenafil; The in vitro ability to suppress PDE5 is 28% compared with vardenafil, which corresponds to 7% of the drug's efficacy. Injecting the average T1 / 2 of vardenafil after taking pills dispersed in the oral cavity is 4-6 h, and the main metabolite M1 molecules) - from 3 to 5 h. The general clearance of vardenafil is 56 l / h.After ingestion, vardenafil in the form of metabolites is excreted mainly in the gastrointestinal tract (91-95% of the dose), to a lesser extent by the kidneys (2-6% of the dose). Pharmacokinetics in special groups of patients Patients aged 65 years and older when taking pills dispersed in of the mouth, there was an increase in AUC from 31 to 39% and Cmax from 16 to 21%, compared with patients aged 45 and under. When taking one tablet dispersed in the mouth for 10 days, patients under the age of 45 years and at the age of 65 and over did not show any accumulation of vardenafil in the plasma. There were no differences in the efficacy or safety of the drug in the elderly and younger patients. in patients with mild (CC more than 50-80 ml / min) and moderate (CC more than 30-50 ml / min) renal insufficiency, the pharmacokinetic parameters of vardenafil are comparable to those of healthy men. In severe renal failure (CC less than 30 ml / min), the average value of AUC increases by 21%, and Cmax decreases by 23%. There is no significant correlation between creatinine clearance and plasma vardenafil concentration (AUC and Cmax). In patients on hemodialysis, the pharmacokinetics of vardenafil have not been studied. In patients with mild and moderate hepatic impairment, vardenafil clearance decreases proportionally to the degree of hepatic impairment. With a mild degree of liver failure (class A on the Child-Pugh scale), there was an increase in AUC and Cmax by 1.2 times (AUC - by 17%, Cmax - by 22%), and in moderate (class B on the Child-Pugh scale) AUC in 2.6 (160%) and Cmax in 2.3 (130%) times, respectively, compared with healthy subjects. The safety of using pills dispersed in the mouth has not been studied in patients with mildly impaired liver function (Child-Pugh class B) therefore, it is not recommended to use this category of patients. In patients with severe hepatic impairment. The level of pharmacokinetics of vardenafil has not been studied (class C on the Child-Pugh scale).
Indications
- Erectile dysfunction (inability to achieve and maintain an erection necessary for sexual intercourse).
Contraindications
- simultaneous use with nitrates or drugs that are nitric oxide donors; - simultaneous use with moderately active or potent CYP3A4 inhibitors, such as ketoconazole,Itraconazole, ritonavir, indinavir, erythromycin and clarithromycin; - children and adolescents up to 18 years; - hypersensitivity to any of the components of the drug. The safety of Levitra ODT has not been studied and, until relevant data are obtained, its use is not recommended in patients with the following conditions: - severe liver dysfunction; - end-stage kidney disease, requiring hemodialysis; - arterial hypotension (systolic blood pressure at rest less than 90 mm Hg); - recently suffered a stroke or arctic myocardium (during the last 6 months); - unstable stenocardia; - hereditary degenerative diseases of the retina, for example, pigmentary retinitis. With caution, use the drug in patients with anatomical deformation of the penis (curvature, cavernous fibrosis, Peyronie's disease), with diseases predisposing to priapism (sickle cell anemia, multiple myeloma, leukemia). Patients with a tendency to bleeding and with an exacerbation of peptic ulcer disease, the drug should be prescribed only after evaluating the benefit / risk ratio.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
The drug is not indicated for use in women, newborns and children.
Dosage and administration
Levitra ODT is taken orally, regardless of the meal. The tablet is taken immediately after it is removed from the package. The tablet should be kept on the tongue until it is completely dissolved and then swallowed without washing it down. At the beginning of treatment, the recommended dose is 10 mg (approximately 25-60 minutes before sexual contact). The maximum recommended dose is 10 mg 1 time / day. Sexual stimulation is necessary to ensure an adequate response to treatment. Levitra ODT showed its effectiveness when taken 4-5 hours before sexual intercourse. Dose correction in elderly patients (over 65) is not required. In patients with minor hepatic impairment (class A on the Child-Pugh scale), the dosage regimen not required. The use of Levitra ODT is not recommended in patients with moderately impaired liver function (class B on the Child-Pugh scale). Changes in the dosing regimen are not required in patients with lungs (CC more than 50-80 ml / min), moderate (CC more than 30-50 ml / min) and severe (CC less than 30 ml / min) impaired renal function.
Side effects
When using the drug Levitra ODT in the recommended doses, the following adverse reactions were reported (according to the terminology adopted by WHO). Depending on the incidence, very frequent (≥10%), frequent (≥1% and less than 10%), infrequent (≥0.1) % and less than 1%) and rare (≥ 0.01% and less than 0.1%) adverse reactions. From the immune system: infrequently - allergic edema, angioedema; rarely - an allergic reaction. From the nervous system: very often - headache; often - dizziness; infrequently - a violation of sensitivity, drowsiness, sleep disorders; rarely, fainting, amnesia, convulsions. On the part of the organ of vision: infrequently, visual impairment, hyperemia of the conjunctiva of the eyeball, disturbed color vision, pain in the eyeballs and discomfort in the eyes, photophobia; rarely, increased intraocular pressure, conjunctivitis. For the organ of hearing and labyrinth disturbances: infrequently, tinnitus, vertigo. For the cardiovascular system: often for vasodilatation; infrequently - palpitations, tachycardia; rarely - angina, myocardial infarction, ventricular tachyarrhythmias, hypotension. On the respiratory system: often - nasal congestion; infrequently - shortness of breath, congestion of the paranasal sinuses. On the part of the digestive system: often - dyspepsia; infrequently - nausea, abdominal pain, dry mouth, diarrhea, gastroesophageal reflux disease, gastritis, vomiting, increased transaminase levels. On the side of the skin and subcutaneous tissues: rarely - erythema, rash. On the part of the musculoskeletal system: infrequently - pain in back, increased levels of CPK, increased muscle tone and cramps. From the reproductive system: infrequently - increased erection; seldom - priapism. Others: infrequently - feeling unwell; rarely - chest pain. There have been reports of cases of myocardial infarction associated in time with vardenafil and sexual activity, but it has not been established whether this condition is directly related to vardenafil, or sexual activity, or with concomitant diseases, or a combination of these factors. There are rare reports of cases of development of anterior ischemic neuropathy of the optic nerve (PINSS), resulting in visual impairment (including persistent loss of vision), associated in time with taking PDE5 inhibitors, includingand the drug Levitra ODT, in patients, many of whom, have associated risk factors for the development of this condition, such as: anatomical defect of the optic nerve head, age over 50 years, diabetes, hypertension, coronary heart disease, hyperlipidemia and smoking. It has not been established whether the development of PINZN is directly related to the use of PDE5 inhibitors, or to the patient’s accompanying vascular risk factors and anatomical defects, or to a combination of these factors, or to other causes. Cases of visual impairment, including temporary or permanent loss of vision, are reported. which are associated in time with the intake of PDE5 inhibitors, including and drug Levitra ODT. It has not been established whether these cases are directly related to the intake of PDE5 inhibitors, or to concomitant vascular risk factors, or to other causes. There have been a few cases of sudden deafness or hearing loss when using drugs from the group of PDE5 inhibitors, including and drug Levitra ODT. It has not been established whether these cases are directly related to the intake of Levitra ODT, the concomitant risk factors for hearing loss, a combination of these factors or other causes.
Overdose
Evaluation of side effects was carried out with the administration of vardenafil at a dose of up to 120 mg / day. When prescribing vardenafil at a dose of up to 80 mg 1 time / day and at a dose up to 40 mg several times a day, no serious adverse reactions were observed. When using doses of vardenafil from 80 mg to 120 mg increases the risk of side effects. When using vardenafil in a dose of 40 mg 2 times / day there was marked back pain without signs of toxic effects on the muscular and nervous systems. In cases of overdose, standard maintenance therapy should be performed . Since vardenafil is highly bound to plasma proteins, and only a small amount of the drug is excreted by the kidneys, hemodialysis is unlikely to work.
Interaction with other drugs
Vardenafil is metabolized primarily with the participation of hepatic enzymes of the cytochrome P450 system, namely the 3A4 isoform, as well as with some participation of the 3A5 and 2C9 isoforms. Inhibitors of these enzymes can reduce the clearance of vardenafil. Tsimetidin (400 mg 2 times / day): non-specific inhibitor of cytochrome P450 does not affect the magnitude of AUC and Cmax vardenafil (20 mg) with their simultaneous use. The drug Levitra ODT is contraindicated when used simultaneously with moderately active or potent inhibitors of CYP3A4, such as ketoconazole, itraconazole, ritonavir, indinavir,erythromycin and clarithromycin. With the combined use of Levitra ODT with ketoconazole, itraconazole, indinavir and ritonavir (potential CYP3A4 inhibitors), a significant increase in plasma vardenafil concentration can be expected. Nitrates, nitric oxide donators: Vardenafil intake (10 mg) in the period from 24 hours to 1 hour taking nitroglycerin (0.4 mg sublingually) does not cause an increase in its hypotensive effect when taken in healthy subjects. At a dose of 20 mg 1-4 hours before taking nitrates (0.4 mg sublingually), vardenafil enhances their hypotensive effect, but if vardenafil is prescribed for 24 hours, the hypotensive effect of nitrates does not increase when taken in healthy subjects of middle age. Nicorandil is an activator potassium channels and contains in its composition nitrogroup. The presence of a nitro group in the nicorandil composition causes a high probability of its interaction with vardenafil. However, there is not enough information about the potential hypotensive effects of vardenafil while being used with nitrates. In this regard, this combination is contraindicated. Vardenafil (20 mg) does not change the AUC and Cmax indices of glibenclamide (glyburide in a dose of 3.5 mg) when they are used together. It has also been shown that the pharmacokinetics of vardenafil do not change when used simultaneously with glibenclamide. Pharmacokinetic and pharmacodynamic interactions (effects on prothrombin time and coagulation factors II, VII, X) are not observed when co-administered vardenafil (20 mg) with warfarin (25 mg). Concurrent use with warfarin does not alter the pharmacokinetics of vardenafil. There is no significant pharmacokinetic interaction between vardenafil (20 mg) and nifedipine (30 mg or 60 mg). The combined use of vardenafil and nifedipine does not lead to significant pharmacodynamic interactions: vardenafil causes an additional decrease in systolic and diastolic blood pressure when measured in the supine position by an average of 5.9 mm Hg. and 5.2 mm Hg. respectively. Since it is known that alpha-blockers cause a decrease in blood pressure, especially postural hypotension and syncope, the question of the interaction of alpha-blockers and vardenafil when used together has been carefully studied. The assessment of blood pressure and pulse for 10 hours after taking vardenafil in 5 mg or 10 mg dosage appointed 4 hours after taking alfuzosin, did not reveal a clinically significant additional decrease in the maximum mean blood pressure compared with placebo.One patient experienced a decrease in systolic blood pressure from baseline by more than 30 mm Hg. in standing position after taking vardenafil in a dose of 5 mg. Another patient had a decrease in systolic blood pressure from baseline by more than 30 mm Hg. in standing position after taking vardenafil in a dose of 10 mg. Cases of lowering systolic blood pressure in the standing position below 85 mm Hg. in this case it was not revealed. It was reported about the presence of dizziness in two patients after taking vardenafil in a dose of 5 mg, in one patient - taking 10 mg of vardenafil, and in one - after taking placebo. Since a 4-hour interval between taking doses of vardenafil and alfuzosin was chosen to identify the maximum potential interactions, the time interval between taking the drugs is not required. There were no cases of fainting in this case and with simultaneous use of vardenafil with tamsulosin or terazosin. Combined administration of vardenafil and alpha blockers is permissible only if there are stable blood pressure indicators while taking alpha blockers, while vardenafil should be prescribed with the minimum recommended dose 5 mg. However, the drug Levitra ODT in the form of pills dispersed in the oral cavity should not be administered as an initial dose during concurrent therapy with alpha-blockers. Vardenafil should not be taken at the same time with alpha-blockers, with the exception of tamsulosin and alfuzosin, which can be the same as taking the drug Levitra ODT. The time interval should be observed between taking vardenafil and other alpha-blockers. With the simultaneous appointment of terazosin and vardenafil, it is necessary to observe the 6-hour interval between taking the drugs. Simultaneous use of digoxin (0.375 mg) and vardenafil (20 mg) every other day for more than 14 days is not accompanied by their interaction. A single dose of antacid (magnesium hydroxide / aluminum hydroxide ) does not affect the performance of AUC and Cmax of vardenafil. The bioavailability of vardenafil (20 mg) is also not impaired when combined with histamine H2 receptor blocker ranitidine (150 mg 2 times / day). Vardenafil (10 mg and 20 mg) does not affect the elnost bleeding when used as monotherapy and in combination with acetylsalicylic acid at a low dose (2 tab.on 81 mg). Vardenafil (20 mg) does not potentiate the hypotensive effect of ethanol (0.5 g / kg body weight), the pharmacokinetics of vardenafil is not disturbed. Acetylsalicylic acid, ACE inhibitors, beta-blockers, diuretics and antidiabetic drugs (sulfonylurea preparations and metformin) weak CYP3A4 inhibitors do not affect the pharmacokinetics of vardenafil.
special instructions
Before prescribing drugs used to treat erectile dysfunction, the doctor must assess the state of the cardiovascular system, since there is a risk of developing heart complications during sexual activity. Vardenafil has vasodilating properties, which may be accompanied by a slight or moderate decrease in blood pressure. Patients with obstruction of outflow pathways from the left ventricle, for example, with aortic stenosis, idiopathic hypertrophic subaortic stenosis, may be sensitive to the action of vasodilators, including PDE5 inhibitors. In men who do not show sexual activity due to concomitant cardiovascular disease, drugs for the treatment of erectile dysfunctions should not be used. When using the drug Levitra ODT in therapeutic (10 mg) or supertherapeutic (80 mg) doses, there is a lengthening of the interval and QT. The simultaneous use of vardenafil with other drugs that have a similar effect on the QT interval resulted in the summation of the effects on the duration of the QT interval in comparison with taking each of these drugs separately. This should be taken into account when co-administering Levitra ODT to patients with a prolonged QT interval in history or to patients who take drugs that prolong the QT interval. In this regard, the purpose of the drug Levitra ODT should be avoided in patients with congenital prolongation of the QT interval and in patients taking class I antiarrhythmic drugs (quinidine, procainamide) or class III (amiodarone, sotalol). Safety and efficacy of vardenafil in combination with other treatment methods erectile dysfunction has not been studied, so their combined use is not recommended. The safety of using pills that are dispersed in the mouth (10 mg) has not been studied in patients with moderate hepatic impairment ( SS on the scale of Child-Pugh), therefore not recommended to use in this group of patients receiving the drug patsientov.Na Levitra ODT and other PDE5 inhibitors have been reported cases of transient visual loss and nearteriitnoy ischemic optic neuropathy.When a sudden loss of vision occurs, it is necessary to stop taking Levitra ODT and immediately consult with your doctor. Combined therapy with alpha-blockers and vardenafil may be accompanied by the development of arterial hypotension with an appropriate clinical picture, since these drugs have a vasodilating effect. The combined appointment of vardenafil and alpha-blockers is permissible only if there are stable blood pressure indices against the background of taking alpha-blockers, while vardenafil should be prescribed in the minimum recommended dose of 5 mg. Patients receiving treatment with alpha-adrenergic blocking agents should not use Levitra OTD in the form of pills dispersed in the oral cavity (10 mg) as an initial dose. Vardenafil should not be taken at the same time with alpha-blockers, with the exception of tamsulosin or alfuzosin, which can be the same as taking vardenafil. The time interval should be observed between taking vardenafil and other alpha-blockers. In the case of receiving the selected dose of vardenafil, therapy with alpha-blockers should be started with a minimum dose. A gradual increase in the dose of alpha-blockers to patients receiving drugs from the group of PDE5 inhibitors may lead to a further decrease in blood pressure. Tablets that are dispersed in the mouth contain 1.8 mg of aspartame, a source of phenylalanine, which should be considered if the patient has phenylketonuria. Tablets that are dispersed are oral cavity, contain 7.96 mg of sorbitol. Patients with rare hereditary diseases of fructose intolerance should not take this drug. Additional safety dataNo toxic (including reproductive toxicity), genotoxic and carcinogenic effects of vardenafil are identified. Effect on ability to drive motor vehicles and control mechanismsBefore driving vehicles and mechanisms, patients should know how they react to taking Levitra Odt.