ZELBORAF

INSTRUCTIONS for medical use of the medicinal product TADALAFIL

Composition

The active substance: tadalafil; 1 film-coated tablet contains tadalafil 10 mg (mg) or 20 mg (mg); excipients: lactose monohydrate, sodium croscarmellose, microcrystalline cellulose RH102, hydroxypropylcellulose, sodium lauryl sulfate, magnesium stearate, film coating mixture 03K12429: hypromellose 6mPas, titanium dioxide (E 171), talc, triacetin, yellow iron oxide (E 172).

Pharmaceutical form

Film-coated tablets.

Main physical and chemical properties

10 mg: film-coated tablets, from pale yellow to yellow in color, round in shape, biconvex, with engraving “45” on one side and smooth on the other. 20 mg: film-coated tablets, from pale yellow to yellow in color, round in shape, biconvex, with engraving “47” on one side and smooth on the other.

Pharmacotherapeutic group

Drugs for the treatment of erectile dysfunction. ATC code G04B E08.

Pharmacological properties

Pharmacodynamics

Mechanism of action

Tadalafil is a selective reversible inhibitor of cyclic guanosine monophosphate (cGMP) - specific phosphodiesterase type 5 (PDE 5). When sexual stimulation causes local release of nitric oxide, inhibition of PDE 5 by tadalafil produces increased levels of cGMP in the cavernous body. This leads to relaxation of smooth muscles and increased blood flow to the tissues of the penis, thereby creating an erection. Tadalafil does not act without sexual stimulation.

Pharmacokinetics

Absorption. Tadalafil is well absorbed after oral administration. The mean maximum plasma concentration (Cmax) is reached on average 2 hours after administration. The absolute bioavailability of tadalafil after oral administration has not been established.

Clinical efficacy and safety

Three clinical trials were conducted involving 1054 patients to determine the onset of action of tadalafil, which demonstrated statistically significant improvement in erectile function, as well as efficacy over 36 hours and detection of effect as early as 16 minutes after administration compared to placebo.

Clinical characteristics

Indications

For the treatment of erectile dysfunction in adult men. The drug is effective in the presence of sexual stimulation. Tadalafil is not indicated for use in women.

Contraindications

Hypersensitivity to tadalafil or to any other component of the medicinal product.

Interaction with other medicinal products and other forms of interaction

Studies on interactions, the results of which are presented below, were conducted for doses of 10 mg and 20 mg.

Influence of other medicinal products on tadalafil

CYP450 inhibitors. Tadalafil is metabolized mainly by CYP3A4. The selective inhibitor of CYP3A4 - ketoconazole (200 mg daily) - increases the exposure (AUC) of tadalafil (10 mg) by 2 times, and Cmax by 15%.

Special instructions

Before prescribing the medicinal product Tadalafil

Before administering the drug, the doctor should determine the underlying causes of erectile dysfunction and prescribe the appropriate course of treatment.

Cardiovascular system

In the post-marketing period and/or during clinical trials, serious cardiovascular events have been reported, including myocardial infarction, sudden cardiac death, unstable angina, ventricular arrhythmia, cerebrovascular disorders, transient ischemic attack, chest pain, accelerated heart rate, and tachycardia.

Ability to affect reaction speed when driving vehicles or operating other mechanisms

The effect of Tadalafil on the ability to drive vehicles and other mechanisms is minimal.

Method of administration and dosage

For oral administration. The medicinal product should be taken with the recommended content of the active substance.

Adult men

The recommended dose is 10 mg before predicted sexual activity, regardless of food intake.

Overdose

Symptoms. When administered to healthy volunteers in a single dose of tadalafil up to 500 mg and in multiple doses up to 100 mg per day, undesirable effects were similar to those observed with smaller doses of the drug.

Adverse reactions

Undesirable effects most frequently reported during the treatment of erectile dysfunction were headache, dyspepsia, back pain, myalgia, the frequency of which increased with increasing doses of the drug.

Shelf life

3 years.

Storage conditions

Store in the original packaging in a place inaccessible to children at a temperature not exceeding 25 °C.

Packaging

For 10 mg: 4 or 7 film-coated tablets in a blister pack. 1 blister pack in a cardboard box.

Release category

By prescription.

Manufacturer

Chilu Pharmaceutical (Hainan) Co., Ltd.

Location of the manufacturer and address of the place of business

No. 273-A, Nanhai Avenue, Neshinl Hi-Tech Zone, Haikou, Hainan 570 314, China.