Dynamico Long pills 5mg, 14pcs

Composition

Auxiliary substances:

lactose monohydrate (spray dried) – 88.25 mg,

sodium lauryl sulfate-0.75 mg,

povidone K-12-12.5 mg,

crospovidone-12.5 mg,

sodium stearyl fumarate-1 mg.

Composition of the film shell:

 opadray II 85F32782 yellow – 4 mg (partially hydrolyzed polyvinyl alcohol-1.6 mg, macrogol-3350-0.808 mg, titanium dioxide (E 171) – 0.688 mg, talc-0.592 mg, iron oxide yellow dye (E 172) – 0.312 mg

Pharmacological action

The drug for the treatment of erectile dysfunction, is a reversible selective inhibitor of specific PDE5 cGMP. When sexual arousal causes a local release of nitric oxide, inhibition of PDE5 by tadalafil leads to an increase in cGMP levels in the penile cavernous body. The result is relaxation of the smooth muscles of the arteries and blood flow to the tissues of the penis, which causes an erection. Tadalafil is ineffective in the absence of sexual stimulation.

In vitro studies have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in the smooth muscles of the cavernous body, in the smooth muscles of the vessels of internal organs, in skeletal muscles, platelets, kidneys, lungs, and cerebellum.

The effect of tadalafil on PDE5 is more active than on other phosphodiesterases. Tadalafil is 10,000 times more active against PDE5 than against PDE1, PDE2, and PDE4, which are localized in the heart, brain, blood vessels, liver, and other organs. Tadalafil is 10,000 times more active in blocking PDE5 than PDE3, an enzyme found in the heart and blood vessels.

This selectivity for PDE5, compared to PDE3, is important because PDE3 is an enzyme involved in heart muscle contraction. In addition, tadalafil is approximately 700 times more active against PDE5 than against PDE6, which is found in the retina and is responsible for photo transmission. Tadalafil is also 10,000 times more active against PDE5, compared to its effect on PDE7-PDE10.

It works for 36 hours. The effect is manifested as early as 16 minutes after ingestion in the presence of sexual arousal.

Tadalafil in healthy subjects does not cause significant changes in systolic and diastolic blood pressure, compared with placebo in the supine position (the average maximum decrease is 1.6/0.8 mm Hg, respectively) and standing (the average maximum decrease is 0.2/4.6 mm Hg, respectively). Tadalafil does not cause a significant change in heart rate.

Tadalafil does not cause changes in color recognition (blue/green), which is due to its low affinity for PDE6. In addition, tadalafil does not affect visual acuity, electroretinogram, intraocular pressure and pupil size.

There was no clinically significant effect on semen characteristics in men who took tadalafil in daily doses for 6 months.

Indications

Erectile dysfunction.

Recommendations for use

Middle-aged men are recommended to take a dose of 20 mg at least 16 minutes before the intended sexual activity, regardless of food intake. Patients may attempt sexual intercourse at any time within 36 hours of ingestion in order to determine the optimal response time to tadalafil. The maximum frequency of reception is 1 time/day.

Contraindications

Concomitant use of drugs containing any organic nitrates; children and adolescents under 18 years of age; hypersensitivity to tadalafil.

Side effects

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.

Interaction

Tadalafil is mainly metabolized by the enzyme CYP3A4. The selective CYP3A4 inhibitor ketoconazole increases AUC by 107%, while rifampicin reduces it by 88%.

Although 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.

Concomitant use of antacid (magnesium hydroxide/aluminum hydroxide) and tadalafil reduces the rate of absorption of the latter without changing its AUC.

Tadalafil enhances the hypotensive effect 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.

Description

Tablets, film – coated from light yellow to yellow with a brownish tinge of color, oval, biconvex, with the inscription “5” on one of the sides.

Special instructions

Tadalafil may be used with extreme caution and only if absolutely necessary in patients with severe renal insufficiency (creatinine clearance < 30 ml/min) and severe hepatic insufficiency. Patients with moderate renal insufficiency (creatinine clearance from 31 to 50 ml/min) were more likely to have back pain during tadalafil treatment compared to patients with mild renal insufficiency (creatinine clearance from 51 to 80 ml/min) or healthy volunteers. In patients with creatinine clearance<50 ml / min, tadalafil should be used with caution. Therefore, treatment of erectile dysfunction, including with the use of tadalafil, should not be carried out in men with heart diseases in which sexual activity is not recommended. The potential risk of sexual activity complications in patients with cardiovascular diseases should be considered: myocardial infarction within the last 90 days; unstable angina or angina that occurs during sexual intercourse; chronic heart failure (functional class II and higher according to NYHA classification) that developed within the last 6 months; uncontrolled cardiac arrhythmias; hypotension (blood pressure less than 90/50 mm Hg) or uncontrolled arterial hypertension; stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, stroke, transferred within the last 6 months. Tadalafil should be used with caution in patients with a predisposition to priapism (for example, sickle cell anemia, multiple myeloma or leukemia) or in patients with anatomical deformity of the penis (for example, angulation, cavernous fibrosis or Peyronie’s disease). The patient should be informed about the need to immediately consult a doctor 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 there may be a long-term loss of potency. No cases of priapism have been reported with tadalafil. It is not recommended to use tadalafil in combination with other types of treatment for erectile dysfunction. In patients with renal insufficiency, tadalafil may be used with extreme caution and only if absolutely necessary in patients with severe renal insufficiency (creatinine clearance < 30 ml / min). Patients with moderate renal insufficiency (creatinine clearance from 31 to 50 ml/min) were more likely to have back pain when treated with tadalafil compared to patients with mild renal insufficiency (creatinine clearance from 51 to 80 ml/min) or healthy volunteers. In patients with creatinine clearance<50 ml / min, tadalfil should be used with caution when liver function is impaired, with extreme caution and only if absolutely necessary, tadalfil can be used in patients with severe hepatic insufficiency.

Active ingredient

Tadalafil

Conditions of release from pharmacies

By prescription

Dosage form

Tablets