Cialis - medication for the treatment of erectile dysfunction (violations erection). It is the relaxation of arteries penis and increases the inflow of blood to tissues penis, causing erection is.
Latin name:
Cialis / Cialis.
The composition and the form of release:
Cialis tablets, coated, and 1, 2, 4 or 8 pieces. in the package.
1 tablet contains 20 mg Cialis tadalafila.
Active-existing substance:
Tadalafil / Tadalafil.
Pharmacological properties:
Cialis (tadalafil) is an effective, reversible inhibitor selective Glucosamine specific type 5 (FDE5) guanozin cyclic monophosphate (cGMP). When sexual arousal cause local release of nitric oxide, inhibition FDE5 tadalafilom leads to higher levels of cGMP in the cavernous television penis. The consequence is the relaxation of smooth muscles arteries and the flow of blood to the penis tissues that cause erection. Tadalafil has no effect in the absence of sexual stimulation.
Studies in vitro have shown that a selective inhibitor tadalafil FDE5. FDE5 enzyme is found in the cavernous smooth muscles of the body, in vascular smooth muscles of internal organs, skeletal muscle, platelets, kidneys, lungs, and the cerebellum. Effects on tadalafila FDE5 is more active than the other Glucosamine. Tadalafil is 10000 times more potent against FDE5 than for FDE1, FDE2 and FDE4 that localized in the heart, brain, blood vessels, liver and other organs. Tadalafil in the 10000 block FDE5 times greater than FDE3 - enzyme, which is found in the heart and blood vessels. This selectivity against FDE5 compared with FDEZ is important because FDEZ an enzyme, which is involved in reducing heart muscle. In addition, tadalafil approximately 700 times more active against FDE5 than for FDE6 found in the retina and is responsible for fotoperedachu. Tadalafil also shown up at 10000 times more potent against FDE5 compared to its impact on FDE7 - FDE10.
Tadalafil improves erection, and the possibility of a successful sexual intercourse. The drug is effective for a period of 36 hours. The effect is already evident in 16 minutes after taking the drug in the presence of sexual stimulation.
Tadalafil in healthy persons is a reliable change systolic and diastolic pressure compared with placebo in the recumbent position (average maximum reduction of 1, 6 / 0, 8 mm Art. Art. Respectively) and standing (average maximum reduction of 0, 2 / 4, 6 mm Art. art. respectively). Tadalafil is credible changes in heart rate.
Tadalafil is the recognition of changes colors (blue / green), because of its low affinity to FDEb. In addition, there is no impact on visual acuity tadalafila, elektroretinogrammu, intraocular pressure and the size of the pupil.
In the study tadalafila men in a daily dose of 10 mg is not detected clinically meaningful impact on the number of drug and sperm concentration, sperm motility and morphology.
Pharmacokinetics:
After receiving tadalafil Sialis inside quickly absorbed. Average maximum concentration (C max) in the plasma is achieved through an average of 2 hours after taking the inside.
The speed and extent of absorption tadalafila not depend on the meal, so SIALIS drug can be taken regardless of the meal. Admission (morning or evening) had no clinically significant effect on the speed and extent of absorption.
Tadalafila pharmacokinetics in healthy persons is linear with respect to time and dose. In the range of doses of 2, 5 and 20 mg area under the curve of concentration-time (AUC) increased dose proportionately. Equilibrium plasma concentrations are achieved within 5 days while taking the drug once a day.
Tadalafila pharmacokinetics in patients with violation of erection function similar to the pharmacokinetics of the drug in people without violating erection function.
The average distribution of about 63 liters, which indicates that Tadalafil distributed in the tissues of the body. At therapeutic concentrations of 94% tadalafila associated with the plasma protein-ing. Binding of the protein does not change with impaired renal function.
In healthy persons less than 0,% 0005 imposed doses found in semen.
Tadalafil is metabolized mainly involving isoenzyme (CYP) 3A4 cytochrome R450. The main circulating metabolite is metilkateholglyukuronid. This metabolite at least 13000 times less active against FDE5 than Tadalafil. Therefore, one can hardly suggest that this metabolite concentrations was observed in clinically meaningful.
In healthy individuals, with the average clearance tadalafila ingestion of 2, 5 l / h and the average period of half - 17, 5 hours. Tadalafil is derived mainly in the form of inactive metabolite, mostly with feces (about 61% of dose) and to a lesser extent with urine (about 36% of dose).
Healthy persons of advanced age (65 years or more) had a lower clearance tadalafila with ingestion, which resulted in increase in the area under the curve of concentration-time “by 25% compared with healthy individuals aged 19 to 45 years. This distinction is not clinically significant and does not require selection of doses.
Do people with mild (creatinine clearance 51 - 80 mL / min) or moderate (clearance kreatinina31-50 mL / min) renal insufficiency area under the curve of concentration-time was more than in healthy individuals. U persons with severe renal insufficiency (creatinine clearance 30 mL / min) Tadalafil not studied (see “Special warnings and precautions in the application).
Tadalafila pharmacokinetics in people with low and moderate hepatic insufficiency comparable with any in healthy persons. Such patients selection dose is not required.
In patients with diabetes on a background application tadalafila area under the curve “concentration-time was less than about 19%, than in healthy individuals. This difference does not require dose selection.
Indications:
Cialis shows the erection of the violations.
Dosing and dose:
Cialis are inside.
Application Sialis middle-aged men
Sialis The recommended dose is 20 mg. Cialis take over alleged sexual activity regardless of the meal. Cialis should be taken at least 16 minutes prior to the alleged sexual activity.
Patients may have attempted sexual intercourse at any time during the 36 hours after admission Sialis to establish the optimal response time to receive the drug.
Maximum recommended frequency reception - once a day.
Application Sialis in older men
For older patients selection of a special dose is not required. Recommendations for Reception, described in the section “Use of middle-aged men” apply to older patients.
Application Sialis men with impaired kidney and liver function
For patients with impaired renal function (creatinine clearance 30 mL / min) and a special selection of liver dose is not required (see “Special warnings and precautions in specific application).
Application Sialis in children
Cialis does not apply to an individual under 18 years of age.
Overdose:
When a one-time appointment tadalafila healthy persons in a dose of 500 mg, and patients with erectile dysfunction - many times up to 100 mg per day., Unwanted effects were the same as when using lower doses. In case of overdose should be standard symptomatic treatment.
Contraindications:
established heightened sensitivity to tadalafilu or to any matter within the composition Sialis;
in the case of the reception preparations containing any organic nitrates;
applications from persons under 18 years of age.
The use during pregnancy and lactation:
Cialis is not intended to apply to women.
Side-Effects:
The most frequently observed undesirable events were headache and dyspepsia (11 cases and 7%, respectively). Undesirable events associated with hosting tadalafila were generally small or medium in degree, and decreased with tranzitornymi continue applying the drug.
Another undesirable effect of a conventional back pain, myalgia, nose and the nose “tides” of blood to a person.
Rarely - Century swelling, pain in the eyes, konyuktivy flushing and dizziness.
Precautions and special instructions:
Because no data controlled clinical studies on safety and efficacy Sialis in the following groups of patients:
Patients with severe renal insufficiency (creatinine clearance 30 mL / min)
Patients with severe hepatic insufficiency, such patients should appoint a drug with caution.
Sexual activity is a potential risk for patients with cardiovascular diseases. Therefore, treatment of erectile dysfunction, including using Sialis, should not be held in men with heart diseases, in which sexual activity is not recommended.
It should take into account the potential risk of complications in sexual activity in patients with cardiovascular disease:
myocardial infarction within the last 90 days;
stenocardia unstable or stenocardia occurred during sexual intercourse;
Class 2 cardiac insufficiency and higher NYHA, evolved during the last 6 months;
Violations of uncontrolled heart rate, hypotension (with AD <90/50 mm Art. art.), or uncontrolled hypertension;
stroke, moved in the last 6 months.
Cialis should be applied with caution in patients with a predisposition to priapizmu (for example, in sickle-cell anemia, leukemia and multiple myeloma), or in patients with anatomical deformation penis (for example, with angular Ol'shanskii, cavernous fibrosis patient or illness).
There are reports of the occurrence of priapizma using another inhibitor FDE5 - sildenafila, albeit against a backdrop of the admission Sialis no reported cases priapizma. Patients should be informed immediately of the need to seek medical assistance in the event of an erection, the continuing 4 hours or more. Late priapizma treatment leads to a loss of tissue penis, which can lead to long-term loss of potency.
Safety and efficacy Sialis combination with other types of treatment of erection function not studied. Therefore, the use of such combinations is not recommended.
Against the backdrop Sialisom treatment in patients with renal failure secondary to the gravity of (creatinine clearance 31 -50 ml / min) often met this undesirable phenomenon of back pain, compared with patients with poorly pronounced renal insufficiency (creatinine clearance 51-80 mL / min), or healthy individuals. In patients with severe renal function violation (creatinine clearance 30 mL / min) Tadalafil not studied. Cialis should be appointed with caution in patients with creatinine clearance 50 mL / min.
Drug Interactions:
Effect of other agents on Cialis (tadalafil):
Tadalafil mainly metabolized with the CYP3A4 enzyme. Selective inhibitors of CYP3A4, ketoconazole, increases the area under the curve of concentration-time at 107%, and rifampicin it reduces by 88%.
Despite the fact that no specific interactions were studied, it may be assumed that the protease inhibitors such as ritonavir and saquinavir, as well as inhibitors of CYP3A4, such as erythromycin and itraconazole tadalafila increase activity.
Simultaneous treatment antatsida (aluminum hydroxide and magnesium) and tadalafila tadalafila intake reduces the speed without changing the area under the curve for the Pharmaceutical tadalafila.
The increase gastric pH as a result of the admission nizatidina H2-antagonist, had no effect on the pharmacokinetics tadalafila.
Influence Sialis (tadalafila) on other drugs:
It is known that reinforces Tadalafil hypotensive effect of nitrates (nitroglycerin, isosorbide dinitrate, isosorbide mononitrate). This occurs as a result of the additive action tadalafila nitrate and nitric oxide metabolism in and rebuild. Therefore, the use of the application against the backdrop Sialis protivopokazano nitrate.
Cialis does not provide clinically meaningful action on the clearance of drugs whose metabolism runs with the cytochrome isoenzyme R450. Studies have confirmed that Tadalafil not inhibited and not izofermenty induces CYP3A4, CYP1 A2, CYP2D6, CYP2E1, and CYP2C9.
Tadalafil has no clinically noticeable impact on the pharmacokinetics of S-and R-coumafuryl coumafuryl. Tadalafil not affect the validity coumafuryl against prothrombin time.
Tadalafil not increase the duration of bleeding caused acetylsalicylic acid.
Tadalafil showed no clinically significant interaction with the major classes of antihypertensives means, including calcium channel blockers (amlodipin), angiotensin-converting enzyme inhibitors (enalapril), beta-blockers adrenergic receptors (labetalol), alpha-blockers, tiazidnye Diuretics (bendoflyuazid) and angiotensin II receptor blockers , which have been used in various doses as monotherapy or in combination. No differences in unwanted events in patients taking Tadalafil antihypertensives in combination with drugs or without them.
No single admission tadalafila impact on the concentration of alcohol in the blood, the influence of alcohol on cognitive function and blood pressure. In addition, there was no change tadalafila level concentrations in the blood after 3 hours after his admission in combination with alcohol.
Tadalafil has no clinically significant effect on the pharmacokinetics of theophylline or farmakodinamiku.
The impact on driving ability and work mechanisms:
No special requirements.
Storage conditions:
Store at temperatures below 30 ° C in the original packaging.
Keep in places inaccessible to children.
Cautions 2 years. Do not use a later date specified on the package.
Terms of the leave pharmacies - with a doctor.
Cialis - information for patients:
What is Cialis?
Cialis - medication for the treatment of erectile dysfunction. Cialis belongs to the class of enzyme inhibitors Glucosamine-5. Its effect is based on a selective and effective blockade Glucosamine-5, which contributes to relax smooth muscle cells and increase blood flow in sexual member. Cialis treats erectile dysfunction by increasing blood inflow to sex with a corresponding member of sexual initiation.
Cialis is intended for the treatment of erectile dysfunction in any degree of seriousness. His recommended for use inside the 20 mg dose over alleged sexual activity, regardless of the collateral meals or alcohol.
Currently Cialis - the only Glucosamine-5 inhibitor, the effect of which persists more than a day - up to 36 hours. It is important to note that the erection occurs only with sexual initiation. This will allow couples do not plan their sexual relationships and not to abandon the usual rhythm of life. After taking the drug the morning, you can take advantage of its effect evening.
Cialis already well-proven case in Europe, Australia and New Zealand. The first countries where the drug has become Britain, Denmark, Finland, Sweden and Germany.
To date, more than 4000 men have participated in more than 60 clinical studies have proven the effectiveness and safety of the drug. Cialis improved erectile function with 81% of men and showed good portability.
Cialis positive effect on the following manifestations and consequences of erectile dysfunction:
Erection as a whole;
The opportunity to achieve erection sufficient for sexual intercourse;
Ability to support erection when sexual intercourse;
Getting satisfaction from sexual intercourse;
Positive emotions;
The satisfaction of a good erection;
Confidence in the ability to achieve and maintain erection;
Addressing a partner of sexual intercourse;
Because Cialis has a prolonged effect, men can now not to think constantly about the admission of the drug.
Sialis Why?
Cialis has high efficiency, which not only improves erection but also help the patient regain naturalness of sexual relations. Cialis is reliable, efficient, easy to use and secure, it restores a normal sex life for patients suffering from erectile dysfunction, freeing them from the constant thoughts about treatment.
For a certain number of patients in the clinical effect starts within 16 minutes. Sialis after administration and lasts 36 hours.
Cialis, which is taken as required, to once a day, improves erectile function for the majority of men suffering from erectile dysfunction in any degree.
What are the methods for the treatment of Erectile dysfunction is more prevalent?
There are various methods. Oral drugs penialnye injections, and vacuum-erektory implants can help with erectile dysfunction.
The psychological or sexual advice can be useful in violation of psychogenic erection type.
If a patient’s severe degree of erectile dysfunction, could help Cialis?
Yes. In clinical trials, 81% of patients receiving Cialis tablets of 20 mg potency seen improvement. The study included patients with varying degrees of erectile dysfunction, from the poor to severe.
Can Cialis help patients suffering from diabetes?
Yes. In clinical trials, 68% of men with diabetes who took Cialis tablets of 20 mg witnessed improvement of erection.
When taking Cialis?
Patients must take Cialis as prescribed by a doctor or consultant. The drug takes effect within 30 minutes and remain effective up to 36 hours. Cialis can be taken regardless of the meal. The successful outcome must be sexual arousal.
What side effects can be expected from Sialis?
Patients receiving any form of organic nitrates should not take Cialis, or any other FDE5 inhibitor. This combination can cause a dangerous drop in blood pressure. If the patient during sex classes complained of chest pain or other symptoms related to cardiopulmonary resuscitation, he should immediately consult a doctor. In clinical trials, the most frequent side effect was headache, dyspepsia, back pain, aching muscles and the tide of blood to a person. Usually, the side effects of weak or moderate, and quickly pass their frequency decreases with constant use of the drug. In clinical studies, most men did not suffer serious side-effects, which would have forced them to stop taking Cialis.
Can I take Cialis if taken with nitrates?
No patients receiving any form of nitrates should not take Cialis. If the patient is taking Cialis at the same time taking any medication on the basis of nitrates, blood pressure can drop to dangerous levels. Many medicines for the treatment of pain can put in the sternum caused by heart disease contain nitrates. These medications include nitroglycerine (aerosols, ointments, paste and plaster or tablets rassasyvaniya under the tongue) or dinitrate and isosorbide mononitrate (who swallow pills, nicotine or kept under the tongue). Certain drugs such as light pop nitrate also contain nitrates. Listed list is not complete, so it is important to know you are taking nitrates or preparations containing them.
If any restrictions on the admission of food in the treatment Sialisom?
Net. Cialis can be taken in conjunction with or without food.
How best to take Cialis?
Some men Cialis takes effect within 16 minutes. For most patients this time is 30 minutes. But remember, without sexual stimulation effect is not. Most patients taking Cialis, in order to be ready for intimacy with a partner at any time convenient for them within 36 hours. Recommended limit of one 20 mg tablet a day.
Can I use daily Cialis over a long period of time?
Daily use of the drug is strongly not recommended.
Would patients suffer erection if they do not want?
No, Sialis required for the effectiveness of sexual arousal.
Will take effect only if Cialis half tablets?
Cialis is designed for use in a dosage of 20 mg, split pills into smaller doses can not.
Can women take Cialis?
Net. Cialis is only for men.