Tradename

Tesira, Тесира

International non-proprietary name

Tadalafil + Dapoxetine, Тадалафил + Дапоксетин

Compound

Each film-coated tablet contains:

active substance: Tadalafil 20 mg, Dapoxetine (as

Dapoxetine Hydrochloride) 60 mg excipients : Q. S

Dosage form

Tablets.

Pharmacological properties

Mechanism actions

Tadalafil and dapoxetine are potent selective serotonin reuptake inhibitors (SSRIs) with an IC 50 of 1.12 nM, while their major human metabolites, desmethyldapoxetine ( IC 50 < 1.0 nM) and didesmethyl dapoxetine ( IC 50 = 2.0 nM) are equivalent or less effective (dapoxetine- N ). -oxide ( IC 50 = 282 nM)).

Human ejaculation is primarily mediated by the sympathetic nervous system. The ejaculatory pathway originates from the brainstem-mediated spinal reflex center, which is initially influenced by a number of brain nuclei (medial preoptic and paraventricular nuclei).

It is assumed that the mechanism of action of dapoxetine in premature ejaculation is associated with inhibition of the reuptake of serotonin by neurons and a subsequent increase in the action of the neurotransmitter on pre- and postsynaptic receptors.

In rats, dapoxetine inhibits the ejaculatory ejection reflex by acting at the supraspinal level within the lateral paragigantocellular nucleus ( LPGi ). Postganglionic sympathetic fibers innervating the seminal vesicles, vas deferens, prostate gland, bulbourethral muscles, and bladder neck cause them to contract in a coordinated manner to achieve ejaculation. Dapoxetine modulates this ejaculatory reflex in rats.

Indications for use

Tesira shown for treatment premature ejaculation (PE) in adult men aged 18 to 64 years. Tesira should only be used in patients who meet everyone next criteria:

•        Latent time intravaginal ejaculations ( IELT ) less than two minutes;

•        Constant or recurring ejaculation with minimal sexual stimulation before, during, or shortly after penetration and before the patient wishes;

•        Severe personal distress or interpersonal difficulties as a consequence of PE;

•        Poor control over ejaculation.

Contraindications

Hypersensitivity to the active substance or any of the excipients listed in section 6.1.

Serious pathological conditions of the heart, such as:

•        Heart failure (class II - IV according to NYHA )

•        Conduction disorders such as atrioventricular block or sick sinus syndrome node.

•        Significant ischemic disease hearts

•        Significant illness valves

•        Story fainting.

History of mania or severe depression.

Special instructions and precautions

It should not be used by persons under 18 years of age.

It is indicated only for men with premature ejaculation. Tadalafil and Dapoxetine tablets should not be given to men who have not been diagnosed with premature ejaculation. Safety has not been established and there are no data on the effects of delayed ejaculation in men without premature ejaculation. Other forms of sexual dysfunction

Before starting treatment, subjects with other forms of sexual dysfunction, including erectile dysfunction, should be carefully evaluated by physicians. Tadalafil and dapoxetine tablets should not be used in men with erectile dysfunction (ED) host inhibitors PDE-5.

Side effect

•        Restlessness, agitation, restlessness, insomnia, unusual dreams, decreased libido, hypertension.

•        ringing in ears

•        nasal congestion, Yawn

•       Diarrhea, vomit, constipation, pain in belly, pain in upper abdomen, dyspepsia, flatulence, stomach discomfort, bloating, dry mouth, etc. d.

Interaction with other drugs

•        Thioridazine

•        Ethyl alcohol

•        L -tryptophan, triptans, tramadol, linezolid and others

Dosage and administration

Tadalafil and Dapoxetine tablets are not intended for continuous daily use. Tadalafil and Dapoxetine tablets should only be taken when sexual activity is expected. Tadalafil and Dapoxetine tablets should not be taken more than once every 24 hours.

If the individual response to tadalafil and dapoxetine tablets (20, 60 mg) is insufficient and the patient has not experienced moderate or severe adverse reactions or prodromal symptoms indicative of syncope, the dose may be increased to the maximum recommended dose of tadalafil and dapoxetine tablets. (20.60 mg) taken as needed approximately 1 to 3 hours before sexual activity. If the patient has experienced orthostatic reactions to the initial dose, do not increase dose.

After the first four weeks of treatment (or at least after 6 doses of treatment), the physician should conduct a careful assessment of the individual risk of benefiting from tadalafil and dapoxetine to determine whether continued treatment with tadalafil and dapoxetine tablets is appropriate.

Data on the efficacy and safety of tadalafil and dapoxetine tablets beyond 24 weeks are limited. The clinical need for continuation and the benefit/risk ratio of treatment with tadalafil and dapoxetine tablets should be reviewed at least every six months. months.

Elderly (65 years and older) The efficacy and safety of tadalafil and dapoxetine tablets in patients aged 65 years and older is not installed.

Child population

In this population, there are no data on the use of tadalafil and dapoxetine tablets for premature ejaculation.

Mode of application:

The tablets should be swallowed whole to avoid a bitter taste. Tablets are recommended to be taken with at least one full glass of water. Method of application: Oral application.

Film-coated tablets can be taken with or without food.

Overdose

No cases of overdose have been reported. Unexpected adverse events in a clinical pharmacological study of tadalafil and dapoxetine tablets at a daily dose of up to 240 mg (two doses of 120 mg with an interval of 3 hours) were observed. In general, symptoms of an SSRI overdose include serotonin-mediated adverse reactions such as drowsiness, gastrointestinal disturbances such as nausea and vomiting, tachycardia, tremor, agitation, and dizziness.

In case of overdose, standard supportive measures should be taken as needed. Because of the high protein binding and large volume of distribution of dapoxetine hydrochloride, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be beneficial. Specific antidotes for Tadalafil and Dapoxetine tablets are unknown.

Storage conditions

Store at a temperature not exceeding 30°C. Keep away from light and moisture.

Keep out of the reach of children!

Best before date

3    of the year. Do not use after the expiration date stated on packaging.

Holiday conditions

Released by prescription.

Release form

four      tablets in an aluminum foil blister. 1 blister with instructions for use in a carton box.