Instructions for using Cialis
Active substance: tadalafil. Excipients: lactose monohydrate - 109.65 mg; lactose monohydrate (spray dried) - 17.5 mg; hyprolose - 1.22 mg; hyprolose extra thin - 2.8 mg; sodium lauryl sulfate - 0.49 mg; MCC - 26.25 mg; croscarmellose sodium - 11.2 mg; magnesium stearate (vegetable) - 0.88 mg. Film shell: Opadry yellow (Y-30-12863- A) (lactose monohydrate - 3.72 mg, hypromellose - 2.59 mg, titanium dioxide - 1.54 mg, triacetin - 0.74 mg, iron oxide yellow dye - 0.16 mg) - 8.75 m.
Improving erectile function
The pharmacokinetics of tadalafil in patients with erectile dysfunction is similar to the pharmacokinetics of the drug in people without erectile dysfunction. Absorption After ingestion of the drug, tadalafil is rapidly absorbed. The average Cmax in plasma is reached on average 2 hours after ingestion. The rate and degree of absorption of tadalafil do not depend on the meal, so Cialis can be used regardless of the meal. The time of administration (morning or evening) had no clinically significant sildenafil citrate effect on the rate and degree of absorption. The pharmacokinetics of tadalafil in healthy individuals is linear in terms of time and dose. In the dose range from 2.5 to 20 mg, the AUC increases proportionally to the dose. The distribution of Css in plasma is achieved within 5 days when taking the drug 1 time / day. The average Vd is about 63 liters, which indicates that tadalafil is distributed in the tissues of the body. Binding to plasma proteins of tadalafil in therapeutic concentrations is 94%. In healthy individuals, less than 0.0005% of the administered dose was found in semen. Metabolism Tadalafil is mainly metabolized with the participation of the CYP3A4 isoenzyme. The main circulating metabolite is methylcatecholglucuronide. This metabolite is at least 13,000 times less active against PDE5 than tadalafil. Consequently, the concentration of this metabolite is not clinically significant. Excretion In healthy individuals, the average clearance of tadalafil when ingested is 2.5 l / h, and the average T1 / 2 is 17.5 h. Tadalafil is excreted mainly in the form of inactive metabolites, mainly with feces (about 61% of the dose) and, to a lesser extent, with urine (about 36% of the dose). Pharmacokinetics in special clinical cases, protein binding does not change with impaired renal function. Healthy elderly patients (65 years and older) had a lower tadalafil 20mg clearance of tadalafil when ingested, which was expressed in an increase in AUC by 25% compared with healthy individuals aged 19 to 45 years. This difference is not clinically significant and does not require dose adjustment. In patients with mild to moderate renal insufficiency, dose adjustment is not required. Due to the increased exposure of tadalafil (AUC), patients with severe renal insufficiency are not recommended to use Cialis. The pharmacokinetics of tadalafil in patients with mild to moderate hepatic insufficiency is comparable to that in healthy individuals. There are no data available for patients with severe hepatic insufficiency (Child-Pugh class C). When prescribing Cialis to patients with severe hepatic insufficiency, it is necessary to conduct a preliminary assessment of the risk and benefit of using the drug. In patients with diabetes mellitus on the background of the use of tadalafil, the AUC was about 19% lower than in healthy individuals. This difference does not require dose adjustment.
Simultaneous administration of drugs containing any organic nitrates; children and adolescents under 18 years of age; hypersensitivity to tadalafil
Use during pregnancy and lactation
The drug is not used in women
Method of administration and dosage
Inside. The use of the drug Cialis according to the indication of erectile dysfunction (ED). For patients with frequent sexual activity (more than 2 times a week): the recommended frequency of intake is daily, once a day, 5 mg, at the same time, regardless of the meal. The daily dose can be reduced to 2.5 mg, depending on individual sensitivity. For patients with infrequent sexual activity (less than 2 times a week): it is recommended to prescribe the drug Cialis at a dose of 20 mg, immediately before sexual activity, according to the instructions for the medical use of the drug. The maximum daily dose of Cialis is 20 mg. The use of the drug Cialis according to the indications of BPH or ED / BPH. The recommended dose of Cialis when used 1 time per day is 5 mg; the drug should be taken at approximately the same time of day, regardless of the time of sexual activity. The duration of treatment is determined by the doctor individually. In patients with mild renal insufficiency (creatinine Cl from 51 to 80 ml /min) and moderate (creatinine Cl from 31 to 50 ml /min) dose adjustment is not required. In patients with severe renal insufficiency (creatinine Cl <30 ml/min and on hemodialysis): the use of the drug Cialis is contraindicated
Most often: headache, dyspepsia. Possible: back pain, myalgia, nasal congestion, flushes of blood to the face. Rarely: swelling of the eyelids, pain in the eyes, conjunctival hyperemia, dizziness
Symptoms: with a single administration of tadalafil to healthy individuals at a dose of up to 500 mg and to patients with erectile dysfunction - repeatedly up to 100 mg / day, the undesirable effects were the same as when using the drug in lower doses. Treatment: in case of overdose, standard symptomatic treatment should be carried out. During hemodialysis, tadalafil is practically not excreted.
Interaction with other drugs
Tadalafil is mainly metabolized with the participation of the enzyme CYP3A4. The selective CYP3A4 inhibitor ketoconazole increases AUC by 107%, and rifampicin reduces it by 88%. Despite the fact that 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 the activity of tadalafil. With simultaneous administration of 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 occurs as a result of the additive action of nitrates and tadalafil on the metabolism of nitric oxide and cGMP. Therefore, the use of tadalafil in patients receiving nitrates is contraindicated
With extreme caution and only if absolutely necessary, it is possible to use tadalafil in patients with severe renal insufficiency (CC < 30 ml / min) and severe hepatic insufficiency. Against the background of treatment with tadalafil, patients with moderate renal insufficiency (CC from 31 to 50 ml/min) had back pain more often compared with patients with mild renal insufficiency (CC from 51 to 80 ml/min) or healthy volunteers. In patients with CC <50 ml / min, tadalafil should be used with caution. Therefore, the treatment of erectile dysfunction, including with the use of tadalafil, it should not be carried out in men with such heart diseases in which sexual activity is not recommended. It is necessary to take into account the potential risk of complications during sexual activity in patients with diseases of the cardiovascular system: myocardial infarction during the last 90 days; unstable angina or angina pectoris occurring during sexual intercourse; chronic heart failure (II functional class and higher according to the NYHA classification), developed during the last 6 months; uncontrolled disorders heart rate; arterial hypotension (blood pressure less than 90/50 mmHg) or uncontrolled hypertension; stroke suffered during the last 6 months. Tadalafil should be used with caution in patients with a predisposition to priapism (for example, with sickle cell anemia, multiple myeloma or leukemia) or in patients with anatomical deformity of the penis (for example, with angulation, cavernous fibrosis or Peyronie's disease). The patient should be informed of the need for immediate medical attention in case 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, no cases of priapism have been reported. It is not recommended to use tadalafil in combination with other types of erectile dysfunction treatment