Cialis 5mg

Instructions for use

Latin name

Cialis

Release form

Film-coated tablets.

Structure

1 film-coated tablet contains: tadalafil 5 mg.

Excipients: lactose monohydrate 109.65 mg, lactose monohydrate (spray dried) 17.50 mg, hyprolose 1.22 mg, hyprolose (extra fine) 2.80 mg, sodium lauryl sulfate 0.49 mg, microcrystalline cellulose 26.25 mg , croscarmellose sodium 11.20 mg, magnesium stearate (vegetable) 0.88 mg.

Shell composition: yellow opadry (Y-30-12863-A) 8.75 mg (lactose monohydrate 3.72 mg, hypromellose 2.59 mg, titanium dioxide 1.54 mg, triacetin 0.74 mg, iron dye yellow oxide 0 ,sixteen).

Packaging

The package contains 14 pcs.

pharmachologic effect

Cialis is a treatment for erectile dysfunction (impotence, erectile dysfunction) in men and belongs to a group of drugs called PDE-5 (phosphodiesterase type 5) inhibitors. The drug dilates the blood vessels of the penis during sexual arousal. As a result, blood circulation in the penis is increased, and this, in turn, contributes to the onset of a stable erection.

Indications

Erectile dysfunction.

Lower urinary tract symptoms in patients with benign prostatic hyperplasia.

Erectile dysfunction in patients with lower urinary tract symptoms associated with benign prostatic hyperplasia.

Contraindications

- Hypersensitivity to tadalafil or to any substance that is part of the drug.

- In case of taking medications containing any organic nitrates.

- Age under 18.

- Diseases of the cardiovascular system: myocardial infarction within the last 90 days, unstable angina pectoris, the occurrence of an attack of angina pectoris during intercourse, chronic heart failure of classes II-IV according to the NYHA classification, uncontrolled arrhythmias, arterial hypotension (BP less than 90/50 mm Hg Art.), uncontrolled arterial hypertension, ischemic stroke within the last 6 months.

Loss of vision due to non-arterial anterior ischemic neuropathy of the optic nerve (regardless of the connection with the use of PDE-5 inhibitors).

- Simultaneous administration 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 failure (creatinine clearance less than 30 ml / min).

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully:

- Severe liver failure (Child-Pugh class C).

- Patients taking alpha 1 -adrenergic blockers.

- Predisposition to priapism (with sickle cell anemia, multiple myeloma or leukemia).

- Anatomical deformity of the penis (angular curvature, cavernous fibrosis or Peyronie's disease).

- Simultaneous priming with powerful inhibitors of the CYP3A4 isoenzyme (ritonavir, saquinavir, ketoconazole, itraconazole, erythromycin), antihypertensive drugs.

Method of administration and dosage

For oral administration.

For patients with frequent sexual activity (more than twice a week), the recommended frequency of priming is 5 mg daily, once a day, 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 twice a week), it is recommended to prescribe the drug in a dose of 20 mg, immediately before sexual activity, according to the instructions for medical use of the drug. The maximum daily dose is 20 mg.

Side effects

Adverse events associated with the use of tadalafil are usually insignificant or moderate in severity, transient and decreased with continued use of the drug.

The most common (≥1%, headache, dyspepsia, back pain, myalgia, flushing, nasal congestion.

Violations of the cardiovascular system: infrequently - a feeling of palpitations, tachycardia, a decrease in blood pressure (in patients who have already taken antihypertensive drugs), an increase in blood pressure; rarely - myocardial infarction; unknown - unstable angina.

Nervous system disorders: very often - headache; often - dizziness; rarely - fainting, migraine, transient ischemic attacks, stroke.

Violations of the organs of vision: infrequently - blurred vision; rarely - visual field disturbance; unknown - non-arterial anterior ischemic optic neuropathy of the optic nerve, retinal vein occlusion.

Respiratory system disorders: infrequently - epistaxis.

Digestive system disorders: often - abdominal pain; infrequently - gastroesophageal reflux.

Violations of the skin and subcutaneous tissue: infrequently - rash, urticaria, hyperhidrosis (excessive sweating); unknown - Stevens-Johnson syndrome and exfoliative dermatitis.

General disorders: infrequently - chest pain; rarely - face off; unknown - sudden cardiac death.

Immune system disorders: infrequently - hypersensitivity reactions.

Reproductive system disorders: rarely - prolonged erection; unknown - priapism.

Observed in patients with previous cardiovascular risk factors. However, it is impossible to determine with certainty whether these events are directly related to these risk factors, tadalafil, sexual arousal, or a combination of these or other factors.

special instructions

Care must be taken when prescribing Cialis to patients taking alpha1-blockers, since concurrent use can lead to symptomatic arterial hypotension in some patients. In a clinical pharmacology study in 18 healthy volunteers taking a single dose of tadalafil, symptomatic arterial hypotension was not observed with the simultaneous administration of tamsulosin, an alpha-1-blocker. Diagnosis of erectile dysfunction should include identification of the potential underlying cause, appropriate medical evaluation and treatment. Sexual activity has a potential risk for patients with cardiovascular disease. Therefore, the treatment of erectile dysfunction, including with the drug Cialis, should not be carried out in men with heart diseases in which sexual activity is not recommended. There have been reports of the occurrence of priapism with the use of PDE-5 inhibitors, including tadalafil. Patients should be informed of the need for immediate medical attention in case of an erection lasting 4 hours or more. Late treatment of priapism leads to damage to the tissues of the penis, resulting in irreversible impotence. The safety and effectiveness of the combination of the drug Cialis with other types of treatment for disorders have not been studied. Therefore, the use of such combinations is not recommended. Like other PDE-5 inhibitors, tadalafil has systemic vasodilator properties, which can lead to a transient decrease in blood pressure. Before prescribing the drug Cialis, doctors should carefully consider whether patients with cardiovascular disease will be exposed to unwanted effects due to such vasodilating effects. Non-arterial anterior ischemic optic neuropathy (NAPION) is a cause of visual impairment, including complete loss of vision. There are rare post-marketing reports of cases of the development of NAPION, in time associated with the intake of PDE-5 inhibitors. It is currently impossible to determine whether there is a direct relationship between the development of NAPION and the use of PDE-5 inhibitors or other factors. Doctors should advise patients in case of sudden loss of vision to stop taking tadalafil and seek medical attention. Physicians should also advise patients that people who have undergone NAPION are at increased risk of re-developing NAPION. The effectiveness of the drug Cialis in patients who have undergone surgery on the pelvic organs or radical neurosaving prostatectomy is unknown.

Application for impaired liver function: since there are no data on patients with severe hepatic insufficiency (class C according to the Child-Pugh classification), caution must be exercised when prescribing the drug to this group of patients.

Influence on the ability to drive vehicles and control mechanisms: despite the fact that the incidence of dizziness against the background of placebo and tadalafil is the same, during the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

Effect of other drugs on tadalafil

Tadalafil is mainly metabolized with the participation of the CYP3A4 isoenzyme. Selective inhibitor of the isoenzyme CYP3A4 ketoconazole (400 mg per day) increases the exposure of a single dose of tadalafil (AUC) by 312% and C max by 22%, and ketoconazole (200 mg per day) increases the exposure of a single dose of tadalafil (AUC) by 107% and C max by 15% relative to AUC and C max values ​​for tadalafil alone.

Ritonavir (200 mg twice daily), an inhibitor of isoenzymes CYP3A4, 2C9, 2C19 and 2D6, increases the exposure of a single dose of tadalafil (AUC) by 124% without changing C max. Despite the fact that specific interactions have not been studied, it can be assumed that other HIV protease inhibitors, such as saquinavir, as well as inhibitors of the CYP3A4 isoenzyme, such as erythromycin and intraconazole, increase the activity of tadalafil.

A selective inducer of the CYP3A4 isoenzyme, rifampicin (600 mg per day), reduces the exposure of a single dose of tadalafil (AUC) by 88% and C max by 46%, relative to AUC and C max values ​​for tadalafil alone. It can be assumed that the simultaneous use of other inducers of the isoenzyme CYP3A4 should also reduce plasma concentrations of tadalafil.

Concomitant administration of an antacid (magnesium hydroxide / aluminum hydroxide) and tadalafil reduces the rate of absorption of tadalafil without changing the area under the pharmacokinetic curve for tadalafil.

An increase in gastric pH as a result of the priming of nizatidine H2-histamine receptor blockers did not affect the pharmacokinetics of tadalafil.

The safety and effectiveness of the combination of tadalafil with other treatments for erectile dysfunction have not been studied, so the use of such combinations is not recommended. Tadalafil does not potentiate the increase in bleeding time caused by the intake of acetylsalicylic acid.

The effect of tadalafil on other drugs

It is known that tadalafil enhances the hypotensive effect of nitrates. This is due to the additive effect of nitrates and tadalafil on the metabolism of nitric oxide II (NO) and cGMP. Therefore, the use of tadalafil against the background of prima nitrates is contraindicated.

Tadalafil does not have a clinically significant effect on the clearance of drugs, the metabolism of which occurs with the participation of cytochrome P450. Studies have confirmed that tadalafil does not inhibit or induce isoenzymes CYP1A2, CYP3A4, CYP2C9, CYP2C19, CYP2D6, CYP2E1.

Tadalafil has no clinically significant effect on the pharmacokinetics of S-warfarin or R-warfarin. Tadalafil does not affect the prothrombin time effect of warfarin. Tadalafil does not increase the duration of bleeding caused by acetylsalicylic acid.

Tadalafil has systemic vasodilating properties and can enhance the effect of antihypertensive drugs aimed at lowering blood pressure. Additionally, in patients taking several antihypertensive drugs, in whom arterial hypertension was poorly controlled, a slightly greater decrease in blood pressure was observed. In the vast majority of patients, this decrease was not associated with hypotensive symptoms. Patients receiving treatment with antihypertensive drugs and taking tadalafil should be given appropriate clinical guidelines.

There was no significant decrease in blood pressure with the use of tadalafil by individuals taking the selective alpha 1A-blocker tamsulosin.

The simultaneous use of tadalafil with doxazosin is contraindicated. When tadalafil was used by healthy volunteers who took doxazosin (4-8 mg per day), an alpha1-blocker, an increase in the hypotensive effect of doxazosin was observed. Some patients experienced dizziness. No fainting was observed. The use of doxazosin at lower doses has not been studied.

Tadalafil did not affect the concentration of alcohol, as well as alcohol did not affect the concentration of tadalafil. At high doses of alcohol (0.7 g / kg), tadalafil did not cause a statistically significant decrease in mean blood pressure. Some patients experienced postural dizziness and orthostatic hypotension. When taking tadalafil in combination with lower doses of alcohol (0.6 g / kg), a decrease in blood pressure was not observed, and dizziness occurred with the same frequency as when taking alcohol alone.

Tadalafil has no clinically significant effect on the pharmacokinetics or pharmacodynamics of theophylline.

Overdose

Symptoms: with a single appointment to healthy volunteers at a dose of up to 500 mg and 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: carrying out standard symptomatic therapy. With hemodialysis, tadalafil is practically not excreted.

Storage conditions

Store at a temperature not exceeding 30 ° C.

Shelf life

3 years.