Levitra - instructions for use, reviews, analogs and formulations (5 mg, 10 mg and 20 mg tablets) drug for the treatment of erectile dysfunction and impotence in men and women. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Levitra. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of physicians specialists on the use of Levitra in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Levitra in the presence of existing structural analogues. Use to treat erectile dysfunction and impotence in men and women.Composition and interaction of the drug with alcohol.

Levitra - a drug for the treatment of erectile dysfunction, an inhibitor of PDE5.

Erection of the penis is a hemodynamic process, which is based on relaxation of smooth muscles of cavernous bodies and arterioles located in it. During sexual stimulation, the nerve endings of the cavernous bodies release nitric oxide (NO) 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, the smooth muscles of the cavernous bodies relax, which increases the flow of blood into the penis.

Vardenafil (Levitra's active ingredient) blocks PDE5, which undergoes cleavage of cGMP, as a result of which the local action of endogenous NO in cavernous bodies during sexual stimulation is enhanced, which causes Levitra's ability to intensify the response to sexual stimulation.

Composition

Vardenafil hydrochloride trihydrate + auxiliary substances.

Pharmacokinetics

After taking the drug inside Levitra is quickly absorbed from the digestive tract.The beginning of action after ingestion at a dose of 20 mg and 10 mg - 10 minutes, which provides an erection sufficient for penetration and successful completion of sexual intercourse in 34% and 40% of patients with mild to moderate erectile dysfunction, respectively. After 25 minutes, the effect occurs in 53% and 50% of patients, which coincides with the onset of the appearance of the drug in the blood and the rapid increase in its concentration. The duration of action is 8-12 hours. When taken with normal food containing not more than 30% fat, pharmacokinetic parameters of vardenafil do not change. Vardenafil is metabolized in the liver. After oral administration, vardenafil in the form of metabolites is excreted mainly through the intestine - 91-95%, to a lesser extent by kidneys - 2-6%.

Indications

• erectile dysfunction (inability to achieve and maintain the erection necessary for sexual intercourse).

Forms of release

Tablets, dispersible in the oral cavity 10 mg.

Tablets coated with 5 mg, 10 mg and 20 mg.

Instructions for use and dosage

The drug is taken orally regardless of food intake. The initial recommended dose is 10 mg for 25-60 minutes before sexual contact.You can also take in the period from 4-5 hours to 25 minutes before sexual activity. The maximum frequency of reception is 1 time per day. To achieve efficiency, a sufficient level of sexual stimulation is needed.

Depending on the effectiveness and tolerability, the dose can be increased to 20 mg or reduced to 5 mg per day. The maximum daily dose is 20 mg.

Correction of the dosing regimen in elderly patients is not required.

In patients with mild hepatic insufficiency, correction of the dosing regimen is not required. In patients with moderate hepatic insufficiency, the initial dose is 5 mg per day. Further, depending on the effectiveness and tolerability of treatment, the dose can be increased to 10 mg and then to 20 mg.

In patients with mild to moderate impairment of renal function, correction of the dosing regimen is not required.

Side effect

• headache;
• dizziness;
• drowsiness;
• anxiety;
• fainting;
• tides (periodic sudden reddening of the face, sensation of heat);
• increased blood pressure;
• a decrease in blood pressure;
• orthostatic hypotension;
• angina pectoris;
• myocardial ischemia;
• dyspepsia;
• nausea;
• congestive hyperemia of the nasal mucosa (edema of the mucosa, rhinitis, rhinorrhea);
• dyspnea;
• nose bleed;
• laryngeal edema;
• increased tear;
• visual impairment (brightness of vision);
• increased intraocular pressure;
• swelling of the face;
• photosensitization;
• myalgia;
• backache;
• lengthening of an erection or a painful erection;
• priapism;
• hypersensitivity reactions.

Contraindications

• simultaneous therapy with nitrates or preparations that are donators of nitric oxide;
• combination with HIV protease inhibitors, such as indinavir or ritonavir;
• hypersensitivity to the components of the drug;
• It is not intended for use in children and adolescents under the age of 16 years.

Application in pregnancy and lactation

The drug is not intended for use in women and newborns.

Use in children

The drug is not intended for use in children and adolescents under the age of 16 years.

special instructions

Prior to the appointment of Levitra (as well as other drugs used to treat erectile dysfunction), the doctor should assess the condition of the cardiovascular system, since there is a risk of developing complications from the heart during sexual activity.

Vardenafil has vasodilating properties, which can be accompanied by a slight or moderate decrease in blood pressure.

Patients with left ventricular outflow obstruction, for example, with aortic stenosis, idiopathic hypertrophic subaortic stenosis, may be sensitive to the action of vasodilators, including PDE5 inhibitors.

In men who are not shown sexual activity, due to concomitant cardiovascular disease, drugs for the treatment of erectile dysfunction are not prescribed.

Since Levitra at therapeutic doses (10 mg) causes prolongation of the QT interval, the drug should not be administered to patients with congenital QT interval elongation and those taking antiarrhythmic drugs of class 1A (quinidine, procainamide) or class 3 (amiodarone, sotalol).

The safety and effectiveness of vardenafil in combination with other drugs for the treatment of erectile dysfunction has not been studied, so their joint use is not recommended.

The safety of vardenafil has not been studied and its use is not recommended in the following groups of patients: severe liver dysfunction, end-stage renal disease requiring hemodialysis, arterial hypotension (systolic pressure at rest <90 mm Hg.), a recent stroke or myocardial infarction (within the last 6 months), unstable angina, as well as hereditary degenerative diseases of the retina, for example, retinitis pigmentosa.

Against the background of Levitra and other PDE5 inhibitors, cases of transient loss of vision and non-arterial ischemic neuropathy of the optic nerve were recorded. In the event of a sudden loss of vision, the patient should stop taking Levitra and consult a doctor immediately.

Combined therapy with alpha-adrenoblockers and vardenafil may be accompanied by the development of arterial hypotension with a corresponding clinical picture, as these drugs have a vasodilating effect. The combined use of Levitra and alpha-blockers is permissible only if there are stable indices of blood pressure on the background of taking alpha-blockers, and Levitra should be prescribed in the minimum recommended dose of 5 mg. Do not take Levitra at the same time with alpha-blockers, with the exception of tamsulosin, the reception of which may coincide with the administration of vardenafil.In case of taking a selected dose of Levitra, alpha-blockers should be started at the lowest 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.

The dose of Levitra should not exceed 5 mg when it is combined with erythromycin, ketoconazole, itraconazole. The dose of Ketoconazole and Itraconazole should not exceed 200 mg.

The combination with indinavir and ritonavir is contraindicated.

Since vardenafil has not been used in patients with a tendency to bleeding and in patients with peptic ulcer exacerbation, its appointment in these cases is possible only after a careful assessment of the relationship between the benefits and risks of therapy.

Vardenafil does not affect the duration of bleeding, nor does it affect this index when combined with acetylsalicylic acid.

Levitra does not increase the platelet aggregation caused by various drugs. In a higher therapeutic concentration, vardenafil causes a slight increase in the antiplatelet effect of sodium nitroprusside, which is a donator of nitric oxide.

The effect of vardenafil and Heparin with simultaneous application on the duration of bleeding has not been studied.

The effect of vardenafil on the hypotensive effect of nitrates in patients is not known, therefore the combined use of Levitra and nitrates is contraindicated.

Impact on the ability to drive vehicles and manage mechanisms

Before prescribing the drug, patients who drive vehicles and work with mechanisms need to find out their individual response to Levitra.

Drug Interactions

Vardenafil is metabolized predominantly with the participation of hepatic enzymes of the cytochrome P450 system, namely, the isoenzyme CYP3A4, and also with some participation of the CYP3A5 and CYP2C isoenzymes. Inhibitors of these enzymes can reduce the clearance of vardenafil. With the simultaneous use of Levitra with ketoconazole, itraconazole, indinavir and ritonavir (potent inhibitors of CYP3A4), a significant increase in vardenafil concentration in plasma can be expected.

With the simultaneous use of cimetidine (400 mg twice daily), which is a nonspecific inhibitor of cytochrome P450 isoenzymes, does not affect the values ​​of AUC and Cmax values ​​of vardenafil (20 mg).

With the simultaneous use of Levitra (10 mg) and the inhibitor of HIV proteases indinavir (800 mg 3 times a day) there is an increase in AUC vardenafil 16 times (1500%) and Cmax vardenafil 7 times (600%). At 24 hours after administration, the concentration of vardenafil in plasma is approximately 4% of its Cmax.

With the simultaneous use of Levitra (5 mg) ritonavir (600 mg twice daily) increases 13 times the Cmax of vardenafil and 49 times its total daily AUC. The interaction is due to the fact that ritonavir, being a potent inhibitor of CYP3A4 and CYP2C9, blocks the hepatic metabolism of vardenafil. Ritonavir significantly prolongs T1 / 2 vardenafil to 25.7 h.

In healthy volunteers, Levitra (10 mg) when taken 24-1 hour before taking Nitroglycerin (400 μg sublingually) does not cause an increase in its hypotensive effect, at a dose of 20 mg 1-4 hours before the application of nitrates (400 μg sublingually) enhances their hypotensive action, but with the appointment for 24 h, the intensification of the hypotensive effect does not occur.

Vardenafil (20 mg) does not change the values ​​of AUC and Cmax glibenclamide (glyburide at a dose of 3.5 mg) when combined and vice versa.

Pharmacokinetic and pharmacodynamic interaction (effect on prothrombin time and coagulation factors 2, 7, 10) is not observed when vardenafil (20 mg) is combined with Warfarin (25 mg).

There is no significant pharmacokinetic interaction between Levitra (20 mg) and Nifedipine (30 or 60 mg): vardenafil causes an additional decrease in systolic and diastolic blood pressure in the supine position on average by 5.9 mm Hg. Art. and 5.2 mm Hg. Art. respectively.

Since it is known that alpha-adrenoblockers cause a decrease in blood pressure, especially postural hypotension and syncope, the question of the interaction of alpha-blockers and Levitra in a joint application has been carefully studied. Two studies of drug interaction involving healthy volunteers with normal BP who received alpha-adrenoblockers Tamsulosin or terazosin with a rapid increase in doses up to or near the maximum for 14 days or less were conducted. After adding Levitra to the treatment, arterial hypotension developed in a significant number of participants in the study. Among those receiving terazosin, arterial hypotension (systolic BP in the standing position below 85 mm Hg) developed more often if Levitra and terazosin were administered in such a way as to achieve a Cmax match in time than if Cmax disperse in time for 6 hours.These studies may have limited clinical significance, since they were conducted with the participation of healthy volunteers, as well as after forced titration of doses (thus, the participants of the study failed to achieve BP stabilization against the background of the use of alpha-adrenoblockers).

Levitra drug interaction studies were also performed in patients with benign prostatic hyperplasia (BPH) receiving stable doses of tamsulosin or terazosin. When Levitra was prescribed in doses of 5, 10 or 20 mg, patients who received stable doses of tamsulosin did not experience an additional decrease in the mean level of blood pressure. When Levitra was simultaneously given a dose of 5 mg and tamsulosin at a dose of 0.4 mg, in 2 of 21 patients orthostatic arterial hypotension was observed with a systolic blood pressure drop below 85 mm Hg. Art. When taking Levitra in a dose of 5 mg and tamsulosin with a 6-hour interval, orthostatic systolic arterial hypotension with a drop in blood pressure of less than 85 mm Hg. Art. also developed in 2 of 21 patients. In a follow-up study, one-step Levitra's appointment at doses of 10 mg and 20 mg and tamsulosin at doses of 0.4 mg and 0.8 mg of orthostatic systolic blood pressure drops below 85 mm Hg. Art. was not registered.With the simultaneous administration of Levitra in a dose of 5 mg and terazosin in doses of 5 mg or 10 mg in one of 21 patients, symptomatic postural hypotension was observed. When taking Levitra in a dose of 5 mg and terazosin at an interval of 6 hours, there was no drop in blood pressure. The results obtained should be taken into account when deciding on the timing of prescribing.

The combined use of Levitra and alpha-adrenoblockers is acceptable only if there are stable indicators of blood pressure on the background of taking alpha-blockers, and Levitra should be prescribed in the minimum recommended dose of 5 mg. Do not take Levitra at the same time with alpha-blockers, with the exception of tamsulosin, which may coincide with Levitra's reception.

The simultaneous use of Digoxin (0.375 mg) and Levitra (20 mg) every other day for more than 14 days is not accompanied by drug interaction.

One-time administration of Maalox (antacid, magnesium hydroxide / aluminum hydroxide) does not affect the indices of AUC and Cmax vardenafil.

Bioavailability of vardenafil (20 mg) is also not violated when it is combined with histamine H2 receptor blockers Ranitidine (150 mg twice daily) and cimetidine (400 mg twice daily).

Levitra (10 mg and 20 mg) does not affect the duration of bleeding when used as a monotherapy and in combination with low-dose Acetylsalicylic acid (2 tablets of 81 mg).

Levitra (20 mg) does not potentiate the hypotensive effect of ethanol (alcohol) (0.5 g / kg body weight), the pharmacokinetics of vardenafil is not impaired.

Acetylsalicylic acid, ACE inhibitors, beta-adrenoblockers, diuretics and hypoglycemic drugs (sulfonylureas and metformin), weak inhibitors of CYP3A4 do not affect the pharmacokinetics of vardenafil.

Analogues of Levitra drug

Structural analogs for the active substance:

• Vilitra;
• Zhevitra.

Analogues on the group (potency regulators):

• Afrodor 2000;
• Veromax;
• Verona;
• Viagra;
• Viassan LF;
• Vigrande;
• Vizarsin;
• Dynamics;
• Zidena;
• The Impaza;
• Iohimbin "Der Spiegel";
• Yohimbine hydrochloride;
• Maxigra;
• Muse;
• Reilis;
• Cialis;
• Sildenafil citrate;
• Spem;
• Spemann forte;
• Super Yohimbe Plus;
• Tentex forte;
• Testalamine powder;
• Testalamine;
• Himkoline;
• Edex.

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