Zidena, pills 100mg, 4pcs

Composition

1 tablet contains: Active ingredient:  udenafil-100 mgsupportable substances:  lactose, corn starch, colloidal silicon dioxide, L-hydroxypropylcellulose hydroxypropylcellulose-LF, talc, magnesium stearate; shell:  hydroxypropylmethylcellulose, talc, iron oxide red, iron oxide yellow, titanium dioxide.

Pharmacological action

Pharmacodynamics

Udenafil is a selective reversible inhibitor of cyclic guanosine monophosphate (cGMP) – specific phosphodiesterase type 5 (PDE-5).

Udenafil does not have a direct relaxing effect on the isolated cavernous body, but when sexually stimulated, it enhances the relaxing effect of nitric oxide by inhibiting PDE-5, which is responsible for the breakdown of cGMP in the 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. The drug has no effect in the absence of sexual stimulation.

In vitro studies have shown that udenafil is a selective inhibitor of the enzyme PDE-5. PDE-5 is present 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.

Udenafil is a 10,000-fold more potent inhibitor against PDE-5 than against PDE-1, PDE-2, PDE-3 and PDE-4, which are localized in the heart, brain, blood vessels, liver and other organs.

In addition, udenafil is 700 times more active against PDE-5 than against PDE-6, which is found in the retina and is responsible for color perception. Udenafil does not inhibit PDE-11, which means that there are no cases of myalgia, low back pain, or testicular toxicity.

Udenafil improves erection and the possibility of successful sexual intercourse. The action of the drug has an optimal duration of up to 24 hours. The effect appears as early as 30 minutes after taking the drug in the presence of sexual arousal.

Udenafil in healthy subjects does not cause significant changes in systolic and diastolic blood pressure compared to placebo in the supine and standing positions (the average maximum decrease is 1.6/0.8 mm Hg and 0.2/4.6 mm Hg, respectively).

Udenafil does not cause changes in color recognition (blue/green), which is due to its low affinity with PDE-6. Udenafil does not affect visual acuity, electroretinogram, intraocular pressure and pupil size. The study of udenafil in men did not reveal a clinically significant effect of the drug on the number and concentration of sperm, motility and morphology of spermatozoa.

Pharmacokinetics

Suction

After oral use, udenafil is rapidly absorbed. The time to reach the maximum concentration in blood plasma (tmax) is 30-90 minutes (on average-60 minutes). The half-life (half-life) is 12 hours, and the high binding of udenafil to plasma proteins (93.9%) extends the period of its effectiveness to 24 hours after taking just one dose.

High-calorie food intake does not affect the absorption of udenafil.

Alcohol intake in the amount of 112 ml of alcohol (in terms of 40% ethyl alcohol) in combination with oral use of udenafil at a dose of 200 mg does not affect the pharmacokinetic profile of udenafil.

Metabolism

Udenafil is mainly metabolized by the cytochrome isoenzyme (CYP)3A4. In healthy people, the total clearance of udenafil is 755 ml/min. After oral use, udenafil is excreted as metabolites in the faeces.

Udenafil does not accumulate in the body. No significant changes in udenafil pharmacokinetics were observed when healthy volunteers received udenafil daily at doses of 100 and 200 mg per day for 10 days.

Indications

Treatment of erectile dysfunction characterized by the inability to achieve or maintain a penile erection sufficient for satisfactory sexual intercourse.

Use during pregnancy and lactation

According to the registered indication, Zidena is not intended for use in women.

Contraindications

• Hypersensitivity to any of the components of the drug;
• simultaneous use of nitrates and other” donators ” of nitric oxide.

Caution Udenafil should be taken with caution in patients with uncontrolled arterial hypertension (blood pressure >170/100 mm Hg), hypotension (blood pressure).

The potential risk of developing complications during sexual activity should be considered in patients with cardiovascular diseases such as unstable angina or angina that occurs during sexual intercourse; chronic heart failure (NYHA functional Class II-IV, New York Heart Association) that developed during the last 6 months; uncontrolled cardiac arrhythmias.

Udenafil should be used with caution in patients with a predisposition to priapism, as well as in patients with anatomical deformity of the penis, in the presence of a penile implant.

Side effects

Side effects observed in clinical trials of udenafil, depending on the frequency of their occurrence: very often – ≥10% of cases; often-1-10%; sometimes-0.1-1%.

From the cardiovascular system:  very often — flushes of blood to the face.

From the central nervous system:  sometimes — dizziness, stiffness of the neck muscles, paresthesia.

From the side of the visual organs:  often-redness of the eyes; sometimes-blurred vision, pain in the eyes, increased lacrimation.

From the side of the skin:  sometimes-swelling of the eyelids, swelling of the face, urticaria.

From the digestive system:  often-dyspepsia, abdominal discomfort; sometimes-nausea, toothache, constipation, gastritis.

Respiratory system disorders:  often-nasal congestion; sometimes-shortness of breath, dryness in the nose.

From the musculoskeletal system:  sometimes-periarthritis.

The body as a whole:  often-headache, chest discomfort, feeling hot; sometimes-chest pain, abdominal pain, fatigue, thirst.

In the course of post-marketing observations when using udenafil, other adverse events were also described: severe palpitations, nosebleeds, tinnitus, diarrhea, allergic reactions (skin rash, erythema), prolonged erection, a feeling of general discomfort, a feeling of cold or heat, postural dizziness, cough.

Interaction

Inhibitors of cytochrome P450 CYP3A4 isoenzymes (ketoconazole, itraconazole, ritonavir, indinavir, cimetidine, erythromycin, grapefruit juice) may enhance the effect of udenafil.

Ketoconazole (at a dose of 400 mg) increases the bioavailability and Cmax of udenafil (at a dose of 100 mg) almost twice (212%) and 0.8 times (85%), respectively.

Ritonavir and indinavir significantly enhance the effect of udenafil. Dexamethasone, rifampin and anticonvulsants (carbamazepine, phenytoin and phenobarbital) they can accelerate the metabolism of udenafil, so co-use with the above drugs weakens the effect of udenafil.

Co-use of udenafil (30 mg / kg, oral) and nitroglycerin (2.5 mg/kg, single intravenous) has not shown any effect on the pharmacokinetics of udenafil in experimental studies, but the simultaneous use of nitroglycerin and udenafil is not recommended due to the possible decrease in blood pressure.

Udenafil and drugs from the group of alpha-blockers are vasodilators, so when taken together, they should be prescribed in minimal doses.

How to take, course of use and dosage

The drug is taken orally, regardless of food intake. The recommended dose of the drug is 100 mg, taken 30 minutes before the intended sexual activity.

The dose can be increased to 200 mg, taking into account the individual effectiveness and tolerability of the drug.

The maximum recommended frequency of use is once a day.

Overdose

With a single dose of 400 mg, adverse events were comparable to those observed with udenafil in lower doses, but were more common.

Treatment:  symptomatic. Dialysis does not accelerate the elimination of udenafil.

Special instructions

Sexual activity has a potential risk for patients with cardiovascular diseases, so treatment of erectile dysfunction, including with the use of udenafil, should not be carried out in men with heart diseases in which sexual activity is not recommended.

Patients with left ventricular outflow difficulties (aortic stenosis) may be more sensitive to the effects of vasodilators, including PDE inhibitors. Despite the absence in clinical studies of cases of prolonged erection (more than 4 hours) and priapism (painful erection lasting more than 6 hours), such phenomena are characteristic of this class of drugs.

 In the event of an erection lasting more than 4 hours (regardless of the presence of pain), patients should immediately seek medical attention. If left untreated, priapism can cause permanent damage to erectile tissue and erectile function.

Due to the lack of clinical data on the use of udenafil in patients over 71 years of age, this category of patients is not recommended to take this drug. It is not recommended to use udenafil in combination with other treatments for erectile dysfunction.

Product

form Zidena® film-coated tablets 100 mg,4 pcs.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Udenafil

Conditions of release from pharmacies

By prescription

Dosage form

Tablets