Tadalafil - instructions for use, analogs or generics, reviews and dosage forms (tablets 2.5 mg, 5 mg and 20 mg) of the drug for the treatment of impotence and increased erection or potency in men with erectile dysfunction. Composition

In this article, you can read the instructions for using the drug Tadalafil. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Tadalafil 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 Tadalafil in the presence of existing structural analogs or generics.Use to treat impotence and enhance erection or potency in men with erectile dysfunction. Composition of the preparation.

Tadalafil - an agent for the treatment of erectile dysfunction, is a reversible selective inhibitor of specific PDE5 cGMP. When sexual stimulation causes local release of nitric oxide, inhibition of PDE5 with tadalafil leads to an increase in the level of cGMP in the cavernous body of the penis. The consequence of this is the relaxation of the smooth muscles of the arteries and the flow of blood to the tissues of the penis, which causes an erection. Tadalafil is ineffective in the absence of sexual stimulation.

Studies have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in the smooth muscles of the cavernous body, in the smooth muscles of the vessels of internal organs, in skeletal muscles, platelets, kidneys, lungs, and the cerebellum.

The effect of tadalafil on PDE5 is more active than on other phosphodiesterases. Tadalafil is 10,000 times more active against PDE5 than with PDE1, PDE2, PDE4, which are located in the heart, brain, blood vessels, liver and other organs.Tadalafil 10,000 times more actively blocks PDE5 than PDE3 - an enzyme that is found in the heart and blood vessels. This selectivity for PDE5, in comparison with PDE3, is important, since PDE3 is an enzyme involved in contracting the heart muscle. In addition, tadalafil is approximately 700 times more active with respect to PDE5 than with respect to PDE6, found in the retina and is responsible for photo transmission. Tadalafil is also 10,000 times more active against PDE5, compared to its effect on PDE7-PDE10.

Effects for 36 hours The effect is manifested as early as 16 minutes after ingestion in the presence of sexual arousal.

Tadalafil in healthy individuals does not cause a significant change in systolic and diastolic pressure, compared with placebo in the supine position (mean maximum decrease is 1.6 / 0.8 mmHg, respectively) and standing (the average maximum decrease is 0.2 / 4.6 mmHg. respectively). Tadalafil does not cause a significant change in the heart rate (heart rate).

Tadalafil does not cause changes in color recognition (blue / green), which is explained by its low affinity for PDE6.In addition, there is no evidence of tadalafil's influence on visual acuity, electroretinogram, intraocular pressure and pupil size.

A clinically significant effect on the characteristics of sperm in men taking tadalafil in daily doses for 6 months was not detected.

Composition

Tadalafil + auxiliary substances.

Pharmacokinetics

After oral administration, the tadalafil is rapidly absorbed. The speed and degree of absorption do not depend on the intake of food. The pharmacokinetics of tadalafil in healthy individuals is linear in time and dose. In the dose range of 2.5 to 20 mg, the AUC increases in proportion to the dose. The pharmacokinetics of tadalafil in patients with impaired function of erection is similar to the pharmacokinetics of the drug in individuals without a violation of the function of erection. In therapeutic concentrations, 94% of tadalafil binds to plasma proteins. In healthy individuals, less than 0.0005% of the administered dose is found in the sperm. Metabolized with the participation of the isoenzyme CYP3A4. The main circulating metabolite is methyl catechol glucuronide, which is 13,000 times less active against PDE5 than tadalafil, so it is unlikely that this metabolite is clinically significant.Tadalafil is excreted mainly in the form of inactive metabolites, mainly with feces (about 61%) and to a lesser extent with urine (about 36%).

Indications

• erectile dysfunction (impotence).

Forms of release

Tablets coated with 2.5 mg, 5 mg and 20 mg.

Instructions for use and reception scheme

Men of middle age are recommended to take in a dose of 20 mg at least 16 minutes before the alleged sexual activity, regardless of food intake. Patients can attempt to have intercourse at any time within 36 hours after admission in order to establish an optimal response time for taking tadalafil. The maximum frequency of reception is 1 time per day.

In men of advanced age (65 years and older), dose adjustments are not required.

Side effect

• headache;
• dyspepsia;
• backache;
• myalgia;
• nasal congestion;
• flushes of blood to the face;
• swelling of the eyelids;
• Pain in the eyes;
• impaired vision;
• change in color vision;
• conjunctivitis (including conjunctival hyperemia);
• increased tear;
• dizziness.

Contraindications

• simultaneous administration of drugs containing any organic nitrates;
• myocardial infarction during the previous 90 days;
• unstable angina or angina arising during intercourse;
• Heart failure (class 2 and higher according to the NYHA classification), developed during the last 6 months;
• uncontrolled disturbances of the heart rhythm, arterial hypotension (blood pressure less than 90/50 mm Hg), or uncontrolled hypertension;
• stroke, lasting for the last 6 months.
• children and adolescents under 18;
• hypersensitivity to tadalafil.

Application in pregnancy and lactation

The drug is not used in women.

Tadalafil and / or its metabolites penetrate the placenta, which is manifested in the effect on the fetus in rats. Tadalafil and / or its metabolites are secreted into the milk of lactating rats and create concentrations about 2.4 times higher than those found in plasma. After oral administration of a single dose of 10 mg / kg, about 0.1% of the total administered radioactivity excreted in the milk for 3 hours. It is not known whether excreted tadalafil and / or its metabolites in breast milk of women.

There is no evidence of teratogenicity, embryotoxicity and fetotoxicity of tadalafil in rats and mice,who received it at doses up to 1000 mg / kg per day during organogenesis.

Adequate and strictly controlled studies of safety of use in pregnant women have not been conducted.

Use in children

Contraindicated in children and adolescents under the age of 18 years.

special instructions

With extreme caution and only in case of emergency, the use of tadalafil in patients with severe renal insufficiency (KC less than 30 ml / min) and severe hepatic insufficiency is possible.

Against the background of treatment with tadalafil in patients with moderate renal insufficiency (CK from 31 to 50 ml / min), back pain was more common compared with patients with mild renal insufficiency (SC from 51 to 80 ml / min) or healthy volunteers . In patients with SC less than 50 ml / min, tadalafil should be used with caution.

Therefore, the treatment of erectile dysfunction, incl. with the use of tadalafil, should not be performed in men with heart diseases in which sexual activity is not recommended.

The potential risk of developing complications associated with sexual activity in patients with cardiovascular disease should be considered: myocardial infarction within the last 90 days; unstable angina or angina pectoris,arising during sexual intercourse; chronic heart failure (2 functional class and higher according to the NYHA classification), developed during the last 6 months; uncontrolled disturbances of the heart rhythm; arterial hypotension (BP less than 90/50 mm Hg) or uncontrolled hypertension; stroke, lasting for the last 6 months.

Caution should be used tadalafil in patients with a predisposition to priapism (for example, sickle cell anemia, multiple myeloma or leukemia) or in patients with anatomical deformation of the penis (for example, with angulation, cavernous fibrosis or Peyronie's disease).

The patient should be informed of the need to seek immediate medical attention in the event of an erection lasting 4 hours or more. Untimely treatment of priapism leads to damage to the tissues of the penis, as a result of which a long-term loss of potency may occur.

Against the background of the use of tadalafil cases of priapism were not reported.

It is not recommended to use tadalafil in combination with other types of treatment for erectile dysfunction.

Drug Interactions

Tadalafil is mainly metabolized with the enzyme CYP3A4. The selective inhibitor of CYP3A4 Ketoconazole increases AUC by 107%, and rifampicin reduces it by 88%.

Although specific interactions have not been studied, it can be assumed that protease inhibitors such as ritonavir and saquinavir, as well as CYP3A4 inhibitors such as Erythromycin and itraconazole, increase tadalafil activity.

Alcohol and PDE5 inhibitors, including tadalafil, are weak systemic vasodilators, when combined, the hypotensive effect of each individual compound may increase. Significant consumption of alcohol in combination with tadalafil may increase the likelihood of orthostatic signs and symptoms, including increased heart rate, lowering blood pressure, dizziness, and headache.

With simultaneous administration of an antacid (magnesium hydroxide / aluminum hydroxide) and tadalafil, the rate of absorption of the latter decreases without changing its AUC.

Tadalafil enhances the hypotensive effect of nitrates. This is due to the additive effect of nitrates and tadalafil on the metabolism of nitric oxide and cGMP. Therefore, the use of tadalafil in patients receiving nitrates is contraindicated.

Analogues of the drug Tadalafil

Structural analogues or generics according to the active ingredient:

• Cialis;
• Tadalafil Teva;
• Tedallis.

Analogues on the curative effect (means for the treatment of impotence):

• Alisat;
• Allikor;
• Andriol;
• Afalase;
• Bromocriptine;
• Vazoton (L-arginine);
• Verona;
• Viagra;
• Viardot;
• Vivira;
• Vizarsin;
• Wook Wook;
• Dynaman;
• Dynamics;
• Zidena;
• The Impaza;
• Yohimbe;
• Carinate;
• Karinat Forte;
• Levitra;
• Maxigra;
• Muse;
• Omnadren 250;
• Optinat;
• Proviron;
• Simpletons;
• Reilis;
• Cialis;
• Sildenafil;
• Stalon;
• Super Yohimbe Plus;
• Sustanon 250;
• Tentex forte;
• Testalamine;
• Testis compositum;
• Tornethis;
• Tribestan;
• Himkoline;
• Edex;
• Eifitol;
• Erbisol;
• Erexel.

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