Cialis is a drug which was created not long ago but it won the entire pharmaceutical market. Cialis is a modern and very effective drug which is used for the treatment of erectile dysfunction. New properties of Cialis help to gain powerful and fast action and thanks to this every man will easily get rid of erectile dysfunction. Due to Cialis erection disorder is not a big problem now because the treatment is very successful and safe. Using Cialis you will not have a single thought about your erection that it could be failed and let you down. Therefore Cialis is a medical product that you need and you will feel a real man.
Drug for the treatment of erectile dysfunction. PDE-5 inhibitors
Composition, structure and packing
Tablets, film-coated yellow, almond-shaped, marked "C 20" on one side.
tadalafil 20 mg
Excipients: lactose monohydrate - 245,195 mg giproloza (hydroxypropyl) - 8.05 mg sodium croscarmellose - 22.4 mg, 52.5 mg microcrystalline cellulose, magnesium stearate - 0.875 mg sodium lauryl sulfate - 0.98 mg.
The composition of the film-coating: Opadry II yellow (lactose monohydrate, hypromellose, titanium dioxide, triacetin, dye yellow iron oxide) - 14 mg.
1 PC. - Blisters (1) - packs cardboard.
2 pcs. - Blisters (1) - packs cardboard.
2 pcs. - Blisters (2) - packs cardboard.
2 pcs. - Blisters (4) - packs cardboard.
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Drug for the treatment of erectile dysfunction. Tadalafil is a reversible selective inhibitor of PDE5 cyclic guanosine monophosphate (cGMP). When sexual stimulation causes local release of nitric oxide, inhibition of PDE5 tadalafil leads to increased concentrations of cGMP in the corpus cavernosum of the penis. The result is relaxation of smooth muscles of arteries and blood flow to the tissues of the penis that causes erections. Tadalafil has no effect in the absence of sexual stimulation.
Studies in vitro have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in corpus cavernosum smooth muscle, vascular smooth muscle internal organs, skeletal muscle, platelets, kidneys, lungs and cerebellum. Effects of tadalafil for PDE5 is more active than the other PDE. Tadalafil is 10 000 times more potent for PDE5 than for FDE1, PDE2, and PDE4 FDE7, which are located in the heart, brain, blood vessels, liver, leukocytes, skeletal muscle and other organs. Tadalafil 10 000 times more active blocks PDE5 than PDE3 - an enzyme that is found in the heart and blood vessels. This selectivity for PDE5 compared to PDE3 is important because PDE3 is an enzyme participating in the reduction of the heart muscle. Additionally, tadalafil is approximately 700-fold more potent for PDE5 than for PDE6, found in the retina and is responsible for fotoperedachu. Cialis is also showing the action in 9000 times more potent for PDE5 compared with its effect on FDE8, FDE9 and FDE10, and 14 times more potent for PDE5 compared to FDE11. Tissue distribution and physiological effects of inhibiting FDE8 - FDE11 has not yet been clarified.
Cialis improves erection and increases the possibility of full sexual intercourse.
Tadalafil in healthy individuals does not cause significant changes in systolic and diastolic blood pressure compared with placebo in the prone position (mean maximum decrease of 1.6 / 0.8 mm Hg. Art., Respectively) and standing (mean maximum decrease of 0.2 / 4.6 mm Hg. Art . respectively). Tadalafil
does not cause significant changes in heart rate. Tadalafil does not cause changes in the recognition of colors (blue / green), due to its low affinity to the PDE6. Furthermore, there is no effect on visual acuity tadalafil, electroretinogram, intraocular pressure and pupil size.
In order to assess the effect of the daily administration of tadalafil on spermatogenesis have been several studies. None of the studies was not observed undesired effects on sperm morphology and motility. In one study showed a reduction in the average sperm concentration relative to placebo. Reduced sperm concentration was associated with a higher frequency of ejaculation. Furthermore, there was no adverse effect on the average concentration of the sex hormones, testosterone, LH and FSH when taking Cialis, compared to placebo.
The efficacy and safety of Cialis (in doses of 2.5 mg and 5 mg) was studied in clinical trials. It was noted improved erections in patients with erectile dysfunction of all severities when taking tadalafil 1 time / day. In the primary efficacy studies, the use of tadalafil 5 mg 62% and 69% of attempts at sexual intercourse were successful compared to 34% and 39% of patients taking placebo. Tadalafil 5mg significantly improved erectile function for 24 hours between doses.
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The pharmacokinetics of tadalafil in patients with erectile dysfunction is similar to pharmacokinetics in subjects without erectile dysfunction.
After oral administration of tadalafil is rapidly absorbed. The average Cmax plasma is on average 2 hours after ingestion. The rate and extent of absorption of tadalafil are independent of food intake, however Cialis may be used regardless of the meal. Reception time (morning or evening) had no clinically significant effect on the rate and extent of absorption.
Tadalafil pharmacokinetics in healthy individuals is linear with respect to time and dose. In the dose range from 2.5 to 20 mg AUC increases proportionally with dose.
Css in plasma reached within 5 days of taking the drug in 1 time / day.
Middle Vd is about 63 liters, this indicating that tadalafil is distributed in body tissues.
The binding to plasma proteins at therapeutic concentrations of tadalafil is 94%.
In healthy persons less than 0.0005% of the administered dose was found in semen.
Tadalafil is mainly metabolized with isoenzyme CYP3A4. The major circulating metabolite is metilkateholglyukuronid. This metabolite is at least 13 000 times less active against PDE5 than tadalafil. Consequently, the concentration of this metabolite is not clinically significant.
In healthy individuals the average clearance of tadalafil ingestion of 2.5 l / h and the average T1 / 2 - 17.5 hours. Tadalafil is excreted mainly in the form of inactive metabolites, mainly in the feces (about 61% of the dose) and, to a lesser degree, with urine (about 36% of the dose).
Pharmacokinetics in special clinical situations
Protein binding is not altered by impaired renal function.
Healthy older patients (65 years or over) had a lower clearance of tadalafil ingestion, which was reflected in an increase in AUC by 25% compared with healthy people aged 19 to 45 years. This difference is not clinically significant and does not require dose.
In patients with renal insufficiency mild to moderate dose adjustment is required. Due to increased tadalafil exposure (AUC), in patients with severe renal impairment is not recommended Cialis.
The pharmacokinetics of tadalafil in patients with mild to moderate hepatic impairment is comparable to that in healthy individuals. For patients with severe hepatic insufficiency (class C according to Child-Pugh classification) data are not available. In the appointment of Cialis to patients with severe hepatic insufficiency, you must first assess the risks and benefits of the drug.
In patients with diabetes mellitus during treatment with tadalafil AUC was lower by about 19%, than in healthy individuals. This difference does not require dose.
The drug is taken orally.
For patients with frequent sexual activity (more than 2 times per week) recommended frequency of administration - 5 mg 1 time / day, at one and the same time, regardless of the meal. The daily dose can be reduced to 2.5 mg depending on the individual sensitivity.
For patients with infrequent sexual activity (at least 2 times per week) is recommended use of the drug Cialis is 20 mg immediately before sexual activity.
The maximum daily dose of Cialis is 20 mg.
Symptoms: single appointment healthy individuals tadalafil in a dose of 500 mg and patients with erectile dysfunction - repeatedly to 100 mg / day, adverse effects were the same as in the use of the drug at lower doses.
Treatment: In case of overdose should be carried out standard symptomatic treatment. With hemodialysis tadalafil virtually output.
The influence of other drugs on tadalafil
Tadalafil is mainly metabolized with the participation of isoenzyme CYP3A4. When taken in a single dose tadalfila selective inhibitor of CYP3A4 ketoconazole at a dose of 400 mg / day tadalafil AUC increases by 312% and Cmax by 22%; ketoconazole at a dose of 200 mg / day tadalafil AUC increases by 107% and Cmax by 15% relative to the AUC and Cmax values for only one of tadalafil.
Ritonavir (200 mg 2 times / day), an inhibitor of isozymes CYP3A4, 2C9, 2C19 and 2D6, while the use of tadalfilom in a single dose of tadalafil AUC increases by 124% without changing the Cmax.
Despite the fact that a specific interaction is not known, it is possible to assume that other HIV protease inhibitors such as saquinavir, and CYP3A4 isozyme inhibitors, such as erythromycin and itraconazole, increase the activity of tadalafil.
Selective isoenzyme CYP3A4 inducer, rifampicin (600 mg / day), AUC tadalafil decreases when receiving a single dose of 88% and Cmax by 46% relative AUC and Cmax values for only one of tadalafil. We can assume that the simultaneous use of other inducers of CYP3A4 will also cause a reduction in the concentration of tadalafil in plasma.
Simultaneous treatment with an antacid (magnesium hydroxide / aluminum hydroxide) and tadalafil reduced the rate of absorption of tadalafil without altering the area under the concentration-time curve for tadalafil.
Increasing the pH of the stomach as a result of receiving the histamine H2-receptor nizatidine had no effect on the pharmacokinetics of tadalafil.
Safety and efficacy of combinations of Cialis with other treatments for erectile dysfunction have not been studied, so the use of such combinations is not recommended.
Tadalafil did not potentiate the increase in bleeding time caused by taking aspirin.
Effect of tadalafil on other drugs
It is known that tadalafil enhances hypotensive effects 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.
Tadalafil has no clinically significant effect on clearance of drug metabolism of which proceeds with the participation of cytochrome P450. Studies have confirmed that tadalafil does not inhibit or induce isozymes CYP1A2, CYP3A4, CYP2C9, CYP2C19, CYP2D6, CYP2E1.
Tadalafil has no clinically significant effect on the pharmacokinetics of S-warfarin or R-warfarin. Tadalafil has no effect on the action of warfarin on prothrombin time.
Tadalafil does not increase the duration of bleeding caused by acetylsalicylic acid.
Cialis has a systemic vasodilating properties and may exacerbate the effects of antihypertensive drugs aimed at reducing blood pressure.
Additionally, patients taking multiple antihypertensive agents whose hypertension poorly controlled, there was a slightly greater blood pressure reduction. The vast majority of patients, this reduction was not associated with hypotensive symptoms. Patients receiving treatment with antihypertensive drugs and receiving tadalafil should be given appropriate clinical guidelines.
There was no significant reduction in blood pressure when using Cialis makers selective alpha1-blocker tamsulosin. In clinical pharmacology studies in 18 healthy volunteers who received a single dose of tadalafil showed no symptomatic hypotension while the introduction of tamsulosin, alpha 1-blockers. Concomitant use of tadalafil with doxazosin is contraindicated. When using tadalafil in healthy volunteers who took doxazosin (4-8 mg / day), alpha1-blocker, were increased hypotensive action of doxazosin. Some patients experienced dizziness. Syncope was observed. The use of doxazosin in lower doses has not been studied.
Tadalafil did not affect the concentration of alcohol, as well as alcohol does not affect the concentration of tadalafil. At high doses of alcohol (0.7 g / kg) dose of tadalafil did not cause a statistically significant decrease in the average value of blood pressure. Some patients experienced postural dizziness and orthostatic hypotension. When receiving tadalafil in combination with lower doses of alcohol (0.6 g / kg) decrease in blood pressure were observed, and dizziness occurred with the same frequency as in the admission of alcohol.
Tadalafil has no clinically meaningful effect on the pharmacokinetics or pharmacodynamics of theophylline.
Pregnancy and lactation
Cialis is not intended for use in women.
Adverse reactions associated with taking tadalafil, are usually minor or moderate in severity, transient and decreases with continued use of the drug.
The most commonly (≥ 1%, <10%) include headache, indigestion, back pain, myalgia, flushing, nasal congestion.
Spontaneous (postmarketing) data
The frequency of adverse reactions occur more frequently than in isolated cases: very common (≥10%), often (≥ 1%, <10%); uncommon (> 0.1%, <1%), rarely (> 0.01%, <0.1%), very rare (<0.01%), not known (not possible to estimate the frequency of responses from the available data).
Since the cardiovascular system: rarely - a feeling serdtsebieniya1, tahikardiya1, lower blood pressure (in patients who are already taking antihypertensive agents), increased blood pressure; rarely - myocardial miokarda1; unknown - unstable angina, sudden cardiac smert1.
Co nervous system: very often - headache; often - dizziness; rarely - syncope, migraine, transient ischemic attack, stroke.
On the part of the organ of vision: rarely - blurred vision; rarely - a violation of the visual fields; unknown - nearterialnaya anterior ischemic optic neuropathy, optic nerve, retinal vein occlusion.
The respiratory system: rarely - nosebleeds.
From the digestive system: often - pain in the abdomen; infrequently - gastroesophageal reflux.
Dermatological reactions: seldom - rash, hives, rash; unknown - Stevens-Johnson syndrome, and exfoliative dermatitis.
Reproductive system: rarely - prolonged erection; unknown - priapism.
Immune system: rarely - hypersensitivity reactions.
General disorders: uncommon - chest pain; 1 rarely - swelling of the face.
1 were observed in patients with previous cardiovascular risk factors. However, it is impossible to pinpoint whether these phenomena directly with these risk factors with tadalafil, to sexual arousal, or a combination of these or other factors.
Conditions and terms
The drug should be stored out of reach of children at or above 30 ° C. Shelf life - 3 years.
- erectile disfunction.
- Use during treatment with drugs containing any organic nitrates;
- Contraindications to the sexual activity in patients with diseases of the cardiovascular system: myocardial infarction within the last 90 days, unstable angina, the occurrence of angina attack during intercourse, chronic heart failure II-IV class classification NYHA, uncontrolled arrhythmias, hypotension (BP less than 90/50 mmHg), uncontrolled hypertension, ischemic stroke within the last 6 months;
- Loss of vision due nearterialnoy anterior ischemic optic neuropathy (whether due to intake of PDE5 inhibitors);
- Concomitant use of doxazosin as well as drugs for the treatment of erectile dysfunction;
- Frequent (more than 2 times a week) use in patients with chronic renal insufficiency (creatinine clearance less than 30 ml / min);
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- The use in children and adolescents up to 18 years;
- Hypersensitivity to the drug.
Caution should be used in patients with severe hepatic insufficiency (class C according to Child-Pugh classification), as Information about the use of the drug in these patients is not available; patients taking alpha-blockers, as the simultaneous use can lead to symptomatic hypotension; in patients with a predisposition to priapism (with sickle cell anemia, multiple myeloma or leukemia), or in patients with anatomical deformation of the penis (angulation, cavernous fibrosis or Peyronie's disease); together with potent inhibitors of CYP3A4 isoenzyme (ritonavir, saquinavir, ketoconazole, itraconazole, erythromycin), with antihypertensives.
Diagnosis of erectile dysfunction include identification of potential underlying cause, appropriate medical examination and determination of treatment.