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Tornethis - instructions for use, reviews, analogs and formulations (tablets 25 mg, 50 mg and 100 mg) of the drug for the treatment of erectile dysfunction, decreased potency or impotence in men. Composition and alcohol

Tornethis - instructions for use, reviews, analogs and formulations (tablets 25 mg, 50 mg and 100 mg) of the drug for the treatment of erectile dysfunction, decreased potency or impotence in men. Composition and alcohol

In this article, you can read the instructions for using the drug Tornethis. The reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Tornethis in their practice are presented. 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 Tornethis in the presence of existing structural analogs. Use to treat erectile dysfunction, reduce potency or impotence in men.Composition and interaction of the drug with alcohol.

 

Tornethis - a powerful selective inhibitor of cyclo-guanosine monophosphate (cGMP) -specific phosphodiesterase type 5 (PDE5). The realization of the physiological mechanism of erection is associated with the release of nitric oxide (NO) in the cavernous body during sexual stimulation. This, in turn, leads to an increase in the level of cGMP, subsequent relaxation of the smooth muscle tissue of the cavernous body and an increase in blood flow.

 

Sildenafil (an active substance of the drug Tornethis) does not have a direct relaxing effect on the isolated cavernous body of a person, but enhances the effect of nitric oxide (NO) by inhibiting PDE5, which is responsible for the decay of cGMP.

 

Sildenafil is selective for PDE5, its activity against PDE5 is higher than that of other known isoenzymes of phosphodiesterase: PDE6 - 10-fold; FDE1 - more than 80 times; PDE2, PDE4, PDE7-PDE11 - more than 700 times. Sildenafil is 4000 times more selective for PDE5 than with PDE3, which is of paramount importance, since PDE3 is one of the key enzymes in the regulation of myocardial contractility.

 

A mandatory condition for the effectiveness of Tornethis is sexual stimulation.

 

The use of Tornethis in doses up to 100 mg did not lead to clinically significant ECG changes in healthy volunteers. The maximum decrease in systolic blood pressure in the supine position after taking sildenafil in a dose of 100 mg was 8.3 mm Hg, and diastolic blood pressure was 5.3 mm Hg.

 

A more pronounced, but also transient, effect on blood pressure was noted in patients taking nitrates.

 

In some patients, one hour after taking Tornethis in a dose of 100 mg with the Farnsworth-Munssel 100 test, a slight and transient impairment in the ability to distinguish between shades of color (blue / green) was detected. In 2 after taking the drug, these changes were absent. It is believed that the violation of color vision is caused by the inhibition of PDE6, which is involved in the transmission of light in the retina of the eye. Sildenafil does not affect visual acuity, contrast perception, electroretinogram, intraocular pressure or pupil diameter.

 

Composition

 

Sildenafil citrate + excipients.

 

Pharmacokinetics

 

Tornetis is rapidly absorbed from the digestive tract. Bioavailability varies from 25 to 63%.Eating increases the absorption time of sildenafil by 60 minutes and reduces the Cmax of the drug in the blood plasma by 29%. However, the degree of absorption does not change significantly. Binding to blood plasma proteins - 96%. Less than 0.0002% of the dose of sildenafil (an average of 188 ng) was found in the sperm 90 minutes after taking the drug. Sildenafil had no effect on the motility or morphology of spermatozoa.

 

Metabolised in the liver by microsomal oxidation with CYP3A4 isoenzymes (the main route) and CYP2C9 (an additional pathway). The main circulating active metabolite (N-desmethylmetabolite), formed as a result of N-demethylation of sildenafil, undergoes further metabolism. The selectivity of this metabolite in relation to PDE is comparable to that of sildenafil, and its activity against PDE5 is about 50% of the activity of sildenafil.

 

After ingestion, sildenafil is excreted in the form of metabolites, mainly by the intestine (about 80% of the oral dose) and, to a lesser extent, by the kidneys (about 13% of the oral dose).

 

In patients with renal insufficiency (creatinine clearance less than 30 ml / min), cirrhosis of the liver and in elderly people, the clearance of sildenafil is reduced.

 

Indications

  • treatment of erectile dysfunction (impotence of organic origin) characterized by inability to achieve or maintain an erection penis sufficient for a satisfactory sexual intercourse.

 

Forms of release

 

Tablets 25 mg, 50 mg and 100 mg.

 

Instructions for use and how to use them

 

Inside, about 1 hour before the planned sexual activity. A single dose for adults is 50 mg once a day. With regard to efficacy and tolerability, the dose can be increased to 100 mg or reduced to 25 mg. The maximum single dose is 100 mg once a day.

 

In patients with severe renal failure (CC less than 30 ml / min), it is recommended to reduce the dose of Tonnetis to 25 mg.

 

Since in patients with hepatic insufficiency the excretion of sildenafil decreases, the recommended dose of Tonnetis is 25 mg.

 

Adjustments in the dose of Tornethis in elderly patients are not required.

 

When combined with inhibitors of the isoenzyme CYP3A4 (erythromycin, saquinavir, ketoconazole, itraconazole), the initial dose of Tonnetis should be 25 mg.

 

To minimize the risk of postural hypotension in patients taking alpha-blockers,start taking the drug Tornethis should only after the stabilization of hemodynamics in these patients has been achieved. Consider the desirability of reducing the initial dose of Tornethis.

 

Side effect

  • headache;
  • dizziness;
  • drowsiness;
  • hypoesthesia;
  • stroke;
  • fainting;
  • transient ischemic attack;
  • convulsions, incl. recurrent;
  • "tides";
  • a feeling of palpitations;
  • tachycardia;
  • increase or decrease in blood pressure;
  • myocardial infarction;
  • atrial fibrillation;
  • ventricular arrhythmia;
  • unstable angina;
  • sudden death;
  • impaired vision;
  • violation of color perception;
  • defeat of the conjunctiva;
  • violation of lacrimation;
  • occlusion of the vessels of the retina;
  • defects in the fields of vision;
  • vertigo;
  • noise in ears;
  • deafness;
  • nasal congestion;
  • nose bleed;
  • dyspepsia;
  • vomiting, nausea;
  • dryness of the oral mucosa;
  • skin rash;
  • Stevens-Johnson syndrome;
  • toxic epidermal necrolysis (Lyell's syndrome);
  • priapism;
  • prolonged erection;
  • chest pain;
  • fatigue.

 

Contraindications

  • simultaneous reception of donators of nitric oxide (for example, amyl nitrite), organic nitrates or nitrites in any forms;
  • use in patients for whom sexual activity is undesirable (for example, with severe cardiovascular diseases, such as unstable angina, severe heart failure, arterial hypotension (BP ≤ 90/50 mm Hg));
  • recently suffered impaired cerebral circulation or myocardial infarction;
  • hereditary degenerative diseases of the retina, incl. pigment retinitis (a minority of these patients have a genetic disorder of retinal phosphodiesterase);
  • severe hepatic impairment;
  • simultaneous reception of ritonavir;
  • simultaneous reception of other drugs for the treatment of erectile dysfunction;
  • use of the drug in women;
  • age to 18 years;
  • hypersensitivity to sildenafil or to any other component of the drug.

 

Application in pregnancy and lactation

 

Tornetis does not apply to women.

 

Use in children

 

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

 

Application in elderly patients

 

Adjustments in the dose of Tornethis in elderly patients are not required.

 

special instructions

 

For the diagnosis of erectile dysfunction,determine their possible causes and choose an adequate treatment, you must collect a complete medical history and conduct a thorough physical examination.

 

Sexual activity represents a certain risk in the presence of heart disease, so before starting any therapy for erectile dysfunction, the doctor should refer the patient to a cardiovascular system examination. The use of sildenafil is contraindicated in patients with heart failure, unstable angina, suffered in the last 6 months myocardial infarction or stroke, hypotension (blood pressure less than 90/50 mm Hg). Sildenafil has a systemic vasodilating effect, leading to a transient decrease in blood pressure, which is not clinically significant and does not lead to any consequences in most patients. However, before the appointment of Tornethis, the doctor should carefully evaluate the risk of possible undesirable manifestations of vasodilating action in patients with the corresponding diseases, especially against the background of sexual activity.Increased susceptibility to vasodilators is observed in patients with obstruction of the left ventricular outflow tract (aortic stenosis, hypertrophic obstructive cardiomyopathy), as well as with a rare syndrome of multiple systemic atrophy, manifested by severe violation of the regulation of arterial pressure from the autonomic nervous system.

 

Since the combined use of sildenafil and alpha-blockers can lead to symptomatic hypotension in selected sensitive patients, Tornethis should be used with caution in appointing patients taking alpha-blockers. To minimize the risk of postural hypotension in patients taking alpha-adrenoblockers, it is only necessary to start taking sildenafil after hemodynamic stabilization in these patients has been achieved. Consider the desirability of reducing the initial dose of sildenafil. In addition, the doctor should inform patients about what actions should be taken in case of symptoms of postural hypotension.

 

Sildenafil enhances the anti-aggregation effect of sodium nitroprusside (a donator of nitric oxide) on human platelets. Information on the safety of sildenafil in patients with internal bleeding or active peptic ulcer of the stomach is not available, so it should be used with caution.

 

In some post-marketing and clinical trials using all PDE5 inhibitors, including sildenafil, sudden depression or hearing loss in patients was reported. However, in most cases, these patients had risk factors for this pathology, and there was no correlation between the use of PDE5 inhibitors and sudden decline or loss of hearing. The patient should be warned that in the event of a sudden decrease or loss of hearing, sildenafil therapy should be discontinued and immediately consult a physician.

 

The safety and efficacy of Tornethis, together with other means of treating erectile dysfunction, have not been studied, so the use of such combinations is not recommended.

 

Special precautions when destroying an unused preparation

 

There is no need for special precautions when destroying an unused preparation.

 

Impact on the ability to drive vehicles and manage mechanisms

 

Data on the adverse effects of Tornethis in the recommended doses on the ability to drive or work with machinery are not. However, since taking a drug can reduce blood pressure, the development of chromatopsy, blurred vision, you should carefully consider the individual effect of the drug in these situations, especially at the beginning of treatment and when changing the dosage regimen.

 

Drug Interactions

 

The effect of other drugs on the metabolism of sildenafil

 

Metabolism of sildenafil occurs mainly in the liver under the action of isoenzymes CYP3A4 (the main way) and CYP2C9, therefore inhibitors of these isoenzymes can reduce the clearance of sildenafil, and inductors, respectively, increase the clearance of sildenafil.

 

With the simultaneous use of CYP3A4 inhibitors (such as ketoconazole, erythromycin, cimetidine), a decrease in sildenafil clearance was noted.

 

Cimetidine (800 mg), which is a nonspecific inhibitor of CYP3A4, while taking with sildenafil (50 mg) causes an increase in the concentration of sildenafil in plasma by 56%.

 

A single dose of sildenafil 100 mg concomitantly with erythromycin, a specific inhibitor of CYP3A4 (when taking Erythromycin twice daily for 500 mg for 5 days), with the achievement of a constant level of erythromycin in the blood leads to an increase in the AID of sildenafil by 182%.

 

With the simultaneous use of sildenafil (once in a dose of 100 mg) and saquinavir, which is both an inhibitor of the HIV protease, and an inhibitor of CYP3A4 (when taking saquinavir 3 times a day at a dose of 1200 mg), against the background of achieving a constant level of saquinavir in the blood, Cmax sildenafil in the blood increased by 140%, and the AUC increased by 210%. Sildenafil does not affect the pharmacokinetic parameters of saquinavir.

 

More potent inhibitors of the CYP3A4 isoenzyme, such as Ketoconazole or itraconazole, can cause more pronounced changes in the pharmacokinetics of sildenafil.

 

Simultaneous use of sildenafil (once in a dose of 100 mg) and ritonavir, which is an inhibitor of HIV protease and a potent inhibitor of cytochrome P450 isoenzymes (when ritonavir is taken 500 mg twice a day), when the level of ritonavir in the blood was reached, Cmax sildenafil increased by 300% (4 times), and AUC by 1000% (11 times).After 24 h of sildenafil plasma concentration was approximately 200 ng / ml (a single application of sildenafil - 5 ng / ml).

 

Grapefruit juice, a weak inhibitor of CYP3A4, may moderately increase the plasma concentration of sildenafil.

 

A single dose of antacid (hydroxide / magnesium hydroxide, aluminum) did not affect the bioavailability of sildenafil.

 

CYP2C9 inhibitors (such as tolbutamide, warfarin), CYP2D6 (such as selective serotonin reuptake inhibitors, tricyclic antidepressants), thiazides and thiazide diuretics, ACE inhibitors and calcium antagonists have no effect on the pharmacokinetic parameters of sildenafil.

 

Nicorandil is a hybrid of nitrate and potassium channel activator. Due to the presence of a nitrate component, it can enter into serious interactions with sildenafil.

 

Effect of sildenafil on other drugs

 

It is unlikely that sildenafil can affect the clearance of substrates of these isoenzymes.

 

Sildenafil enhances the hypotensive effects of nitrates, as a long-term use, and when used on acute indications.In this regard, the use of sildenafil in combination with nitrates or donators of nitric oxide is contraindicated.

 

With simultaneous administration of alpha-adrenoblocker Doxazosin (4 mg and 8 mg) and sildenafil (25 mg, 50 mg and 100 mg) in patients with benign prostatic hyperplasia with stable hemodynamics, the mean additional decrease in systolic / diastolic blood pressure in the supine position was 7 / 7 mm of mercury, 9/5 mm of mercury. and 8/4 mm Hg, respectively, and in the standing position - 6/6 mm Hg, 11/4 mm Hg. and 4/5 mm Hg, respectively. We report rare cases of development in these patients of symptomatic postural hypotension, manifested as dizziness (without syncope). In individual sensitive patients receiving alpha-blockers, simultaneous use of sildenafil can lead to symptomatic hypotension.

 

Signs of significant interaction of sildenafil (50 mg) with tolbutamide (250 mg) or Warfarin (40 mg), which are metabolized by CYP2C9, have not been identified.

 

Tornetis in a dose of 100 mg does not affect the pharmacokinetic parameters of HIV protease inhibitors at their constant concentration in the blood, such as saquinavir and ritonavir, which are simultaneously substrates of CYP3A4.

 

Sildenafil (50 mg) does not cause an additional increase in bleeding time when taking Acetylsalicylic acid (150 mg). Sildenafil (50 mg) does not enhance the hypotensive effect of ethanol (alcohol) in healthy volunteers with a maximum level of ethanol in the blood on average 80 mg / dl.

 

In patients with arterial hypertension, there was no evidence of Tornetis interaction (100 mg) with amlodipine. The average additional decrease in blood pressure in the prone position is: systolic - by 8 mm Hg, diastolic - by 7 mm Hg.

 

The use of sildenafil in combination with antihypertensive drugs does not lead to additional side effects.

 

Analogues of the drug Tornethis

 

Structural analogs for the active substance:

  • Viagra;
  • Viassan LF;
  • Vigrande;
  • Vizarsin;
  • Dynamics;
  • Maxigra;
  • Silafil;
  • Sildenafil;
  • Taxiere;
  • Erexel.

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Reviews (2):
Guests
Vitaliy
Advise, please, that it is necessary to accept for excitability?
Administrators
admin
VitaliyIf there is a lack of excitability, there are several possible reasons. The first - psychology, to be excited should be an attraction to a partner, without this in any way, treated a psychologist, in extreme cases, a psychiatrist. The second is the hormone testosterone, if it is not enough, then the desire may be absent. Diagnosed by the delivery of tests for the relevant hormones. The third reason is stress, it can refer to both the first reason and the second. In this case, only a full rest will help. So, if the problem does not go away on its own, I advise you to turn to the andrologist or urologist for the correct diagnosis and the appointment of competent treatment.

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