Zidena

General characteristics. Structure:

Active agent: udenafit 100 mg

Excipients: lactose — 87,5 mg; starch corn — 20 mg; silicon dioxide colloid — 12,5 mg; L-hydroxypropyl cellulose — 12,5 mg; hydroxypropyl cellulose-LF — 7,5 mg; talc — 7,5 mg; magnesium stearate — 2,5 mg  

The cover is film: a gidroksipropilmetiltsellyuloza — 6,9 mg; talc — 0,022 mg; iron oxide red — 0,0106 mg; iron oxide yellow — 0,0266 mg; titanium dioxide — 1,0408 mg.

Pharmacological properties:

Pharmacodynamics. Udenafil — the selection reversible inhibitor of the specific FDE-5 promoting metabolism of tsGMF.
Udenafil has no the direct weakening effect on the isolated cavernous body, but at sexual stimulation strengthens the weakening effect of nitrogen oxide by means of inhibition of FDE-5 responsible for disintegration of tsGMF in a cavernous body.
The relaxation of unstriated muscles of arteries and inflow of blood to penis tissues is a consequence of it, as causes an erection. Drug does not render effect for lack of sexual stimulation.
The researches in vitro showed that udenafit is the selection inhibitor of FDE-5 enzyme. FDE-5 is present at unstriated muscles of a cavernous body, at unstriated muscles of vessels of internals, at skeletal muscles, thrombocytes, kidneys, lungs and a cerebellum. Udenafil is by 10000 times more powerful inhibitor concerning FDE-5, than concerning FDE-1, FDE-2, FDE-3 and FDE-4 which are localized in heart, a brain, blood vessels, a liver and other bodies.
Besides, udenafit 700 times more actively concerning FDE-5, than concerning FDE-6 found in a retina and responsible for color perception. Udenafil does not inhibit FDE-11 that causes lack of cases of a mialgiya, back pains and manifestations of testicular toxicity.
Udenafil improves an erection and a possibility of carrying out successful sexual intercourse.
Effect of drug continues to 24 h. The effect is shown in 30 min. after administration of drug in the presence of sexual excitement.
Udenafil does not cause reliable change in healthy faces the GARDEN and DAD in comparison with placebo in a prone position and standing (average maximum decrease makes 1,6/0,8 and 0,2/4,6 mm of mercury. respectively).
Udenafil does not cause changes of recognition of flowers (blue/green) that is explained by its low affinity to FDE-6. Udenafil does not influence visual acuity, the electroretinogram, intraocular pressure and the size of a pupil.
At a research of an udenafil at men it is not revealed clinically significant influence of drug on quantity and concentration of sperm, mobility and morphology of spermatozoa.

Pharmacokinetics. Absorption. After intake udenafit quickly it is soaked up. Tmax in a blood plasma makes 30–90 min. (on average 60 min.).
T1/2 makes 12 h, high linkng of an udenafil with proteins of a blood plasma (93,9%) prolongs the period of its efficiency up to 24 h after reception of a single dose.
Meal with the high content of fat does not exert impact on absorbability of an udenafil.
Alcohol intake in number of 112 ml (in terms of 40% alcohol) in combination with oral administration of an udenafil in a dose of 200 mg does not influence a pharmacokinetic profile of an udenafil.

Metabolism. Udenafil is generally metabolized with participation of an isoenzyme of CYP3A4 of P450 cytochrome.

Removal. At healthy people the general clearance of an udenafil makes 755 ml/min. After intake udenafit it is removed in the form of metabolites with a stake.
Udenafil does not collect in an organism. At daily reception by healthy volunteers of an udenafil in a dose of 100 and 200 mg/days within 10 days essential changes of its pharmacokinetics were not revealed.

Indications to use:

Treatment of the disturbances of an erection which are characterized by inability to achievement or preservation of an erection of a penis sufficient for satisfactory sexual intercourse.

Route of administration and doses:

Inside, irrespective of meal.
The recommended drug dose — 100 mg, accept in 30 min. prior to estimated sexual activity.
The dose can be increased to 200 mg, taking into account individual efficiency and portability of drug.
The maximum recommended frequency rate of use — 1 time a day.

Features of use:

Sexual activity has potential risk for patients with cardiovascular diseases therefore treatment of erectile dysfunction, including with use of an udenafil, should not be carried out at men with heart diseases at which sexual activity is not recommended.
Patients with difficulty of outflow of blood from a left ventricle (an aortal stenosis) can be more sensitive to action of vazodilatator, including FDE inhibitors.
Despite the absence of during clinical trials of cases of the prolonged erection (more than 4 h) and a priapism (a painful erection lasting more than 6 h), such phenomena are inherent for this class of drugs. In case of an erection lasting more than 4 h (irrespective of existence of pain) patients have to ask for medical care immediately. In the absence of timely treatment the priapism can lead to irreversible damage of erectile fabric and erectile function.
Due to the lack of clinical data on use of an udenafil at patients 71 years of this category of patients are more senior administration of drug is not recommended.
It is not recommended to use udenafit in a combination with other types of treatment of erectile dysfunction.

Influence on ability to manage vehicles and to work with the equipment. Before managing the equipment and vehicles, patients have to know how they react to administration of drug of Zidena®.

Side effects:

The side effects observed during clinical trials of an udenafil depending on the frequency of their emergence: very often — ≥10%; often — 1–10%; sometimes — 0,1–1%.

- From CCC: very often — rushes of blood to the person.
- From TsNS: sometimes — dizziness, neck muscle tension, paresthesia.
- From an organ of sight: often — reddening of eyes; sometimes — the obscured sight, eye pain, the raised dacryagogue.
- From skin: sometimes — the century, persons, a small tortoiseshell swelled.
- From the alimentary system: often — dyspepsia, discomfort in a stomach; sometimes — nausea, a dentagra, a lock, gastritis.
- From respiratory system: often — a nose congestion; sometimes — an asthma, dryness in a nose.
- From a musculoskeletal system: sometimes — a periarthritis.
- Organism in general: often — a headache, discomfort in breasts, feeling of heat; sometimes — a stethalgia, an abdominal pain, fatigue, thirst.

In the course of post-marketing observations at use of an udenafil other undesirable phenomena were also described: strong heartbeat, nasal bleeding, sonitus, diarrhea, allergic reactions (skin rash, erythema), long erection, feeling of the general discomfort, cryesthesia or heat, postural dizziness, cough.

Interaction with other medicines:

Inhibitors of an isoenzyme of P450 CYP3A4 cytochrome (кетоконазол, итраконазол, ритонавир, индинавир, Cimetidinum, erythromycin, grapefruit juice) can strengthen action of an udenafil.
Ketokonazol (in a dose of 400 mg) increases bioavailability and Cmax of an udenafil (in a dose of 100 mg) almost twice (212%) and by 0,8 times (85%) respectively.
Ritonavir and индинавир considerably strengthen action of an udenafil.
Dexamethasone, Rifampinum and anticonvulsive drugs (carbamazepine, Phenytoinum and phenobarbital) can accelerate metabolism of an udenafil therefore combined use with the above-stated drugs weakens action of an udenafil.
Combined use of an udenafil (30 mg/kg orally) and nitroglycerine (2,5 mg/kg once, in/in) did not show any influence on pharmacokinetics of an udenafil in pilot studies, however simultaneous use of nitroglycerine and an udenafila is not recommended because of possible decrease in the ABP.
Udenafil and drugs from group of α-adrenoblockers are vasodilators therefore at joint reception have to be appointed in the minimum doses.

Contraindications:

- hypersensitivity to any of drug components;

- concomitant use of nitrates and other donators of nitrogen oxide.

With care: patients with uncontrollable arterial hypertension (the ABP> of 170/100 mm of mercury), hypotonia (the ABP <90/50 mm of mercury.); patients with hereditary degenerative diseases of a retina (including a pigmental retinitis, a proliferative diabetic retinopathy); the patients who had a stroke, a myocardial infarction or aortocoronary shunting within the last 6 months; patients with a heavy liver or renal failure; existence of an inborn syndrome of lengthening of an interval of QT or increase in an interval of QT owing to administration of drugs; predisposition to a priapism; patients with anatomic deformation of a penis; existence of an implant of a penis; sexual activity at patients with such diseases of cardiovascular system as the unstable stenocardia or stenocardia arising during sexual intercourse, the chronic heart failure (the II-IV functional class on NYHA classification) which developed within the last 6 months, uncontrollable disturbances of a cordial rhythm — it is necessary to consider potential risk of development of complications; simultaneous reception of an udenafil and BKK, α-adrenoblockers or other antihypertensives the GARDEN and DAD on 7–8 mm of mercury can be noted additional decrease.

Drug is not intended for use aged up to 18 years.

Use at pregnancy and feeding by a breast
According to the registered indication drug is not intended for use for women.

Overdose:

Symptoms: at a single dose of drug in a dose of 400 mg the undesirable phenomena were comparable with observed at reception of an udenafil in lower doses, but met more often.

Treatment: symptomatic. Dialysis does not accelerate removal of an udenafil.

Storage conditions:

In the dry, protected from light place, at a temperature not above 30 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 100 mg. In packagings of planimetric PVC, cell from a film, and the printing aluminum foil varnished 1, 2 or 4 pieces. In a pack cardboard 1 (on 1, 2 or 4 pieces) or 2 (on 1 or 2 pieces) packagings.