ZIDENA
Active material: Udenafil
When ATH: G04BE
CCF: Drug for the treatment of erectile dysfunction. PDE-5 inhibitor
ICD-10 codes (testimony): F52.2, N48.4
When CSF: 28.08.01.01.01
Manufacturer: DONG-A PHARMTECH (Korea South)
Pharmaceutical form, composition and packaging
Pills, Film-coated light pink color with Tan, Oval, with the embossed symbol “100” on one side and symbols as separated by Mark letters “FROM” and “AND” – another; of presentations – white or nearly white.
| 1 tab. | |
| udenafil | 100 mg |
Excipients: lactose, corn starch, colloidal silicon dioxide, L-hydroxypropyl cellulose, hydroxypropyl cellulose LF, talc, magnesium stearate.
The composition of the shell: hydroxypropyl, talc, iron oxide red, iron oxide yellow, Titanium dioxide.
1 PC. – packings Valium planimetric (1) – packs cardboard.
2 PC. – packings Valium planimetric (2) – packs cardboard.
4 PC. – packings Valium planimetric (1) – packs cardboard.
Pharmacological action
Medication for the treatment of erectile dysfunction. Is reversible selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5).
Udenafil has no direct relaxing effect on the isolated corpus cavernosum, but when sexual stimulation enhances the relaxing effect of nitric oxide by inhibiting PDE-5, responsible for the breakdown of cGMP in the cavernous body. The result is relaxation of smooth muscles of arteries and blood flow to the tissues of the penis, that causes erections. The drug has no effect in the absence of sexual stimulation.
Studies in vitro have shown, What is a selective inhibitor of udenafil enzyme PDE-5. PDE-5 is present in smooth muscle of the cavernous body, in smooth muscles receptacles internal organs, in skeletal muscle, platelets, kidney, light and the cerebellum. Udenafil is in 10 000 times more potent inhibitor against PDE-5, than for PDE-1, PDE-2, PDE-3 and PDE-4, which are located in the heart of, brain, blood vessels, the liver and other organs.
Besides, udenafil in 700 times more against PDE-5, than for PDE-6, found in the retina and is responsible for color perception. Udenafil not inhibits PDE-11, Hence the absence of myalgias, lower back pain and testicular toxicity.
Udenafil improves erections and the ability to conduct a successful sexual intercourse. The drug has an optimal duration – to 24 no. The effect is already in 30 minutes after taking the drug in the presence of sexual stimulation.
Udenafil healthy people does not cause reliable changes of systolic and diastolic pressure versus placebo in lying and standing (the average maximum reduction is 1.6/0.8 mmHg. and 0.2/4.6 mmHg. respectively).
Udenafil does not cause changes in color recognition (Blue/Green), because of its low affinity with PDE-6. Udenafil does not affect visual acuity, jelektroretinogrammu, intraocular pressure and pupil size.
In the study of udenafila men have not revealed clinically significant influence on the quantity and concentration of sperm, motility and morphology of sperm.
Pharmacokinetics
Absorption
After intake of rapidly absorbed udenafil. Tmax is 30-90 m (average – 60 m). Reception of high-calorie food does not affect absorption udenafila.
Distribution
High binding udenafila with plasma proteins (93.9%) prolongs its effectiveness to 24 h after a single dose.
Udenafil does not accumulate in the body. Daily admission healthy volunteers at doses of udenafila 100 mg 200 mg per day for 10 days, there were no significant changes in its pharmacokinetics.
Metabolism
Udenafil is mainly metabolized with the participation of izofermenta CYP3A4.
Deduction
T1/2 is 12 no. In healthy volunteers total klirens udenafila is 755 ml / min. Once inside Udenafil excreted as metabolites in the feces.
Pharmacokinetics in special clinical situations
Alcohol in quantities 112 ml (in terms of 40% ethanol) in conjunction with the acquisition of udenafila inside the dose 200 mg does not affect farmakokineticeski profile udenafila.
Testimony
-treatment of erectile dysfunction, characterized by the inability to achieve or retain an erection of the penis, sufficient for satisfactory sexual intercourse.
Dosage regimen
The drug is taken orally, regardless of the meal, for 30 minutes before anticipated sexual activity.
The recommended dose is 100 mg. If necessary,, taking into account individual efficacy and tolerability, the dose may be increased to 200 mg. Maximum recommended frequency of use- 1 time / day.
Side effect
The following table lists the side effects depending on the frequency of, observed during clinical trials udenafila.
| Organs and organ systems | Side effects | ||
| Often | often | sometimes | |
| >10% | 1%-10% | 0.1-1% | |
| Cardio-vascular system | flushing | ||
| CNS | dizziness, stiff neck, paresthesia. | ||
| On the part of the organ of vision | red eyes | blurred vision, sore eyes, increased lacrimation | |
| Dermatological reactions | swelling of the eyelids, swelling of the face, hives | ||
| From the digestive system | dyspepsia, discomfort in the abdomen | nausea, toothache, constipation, gastritis | |
| On the part of the endocrine system | thirst | ||
| The respiratory system | nasal congestion | breathlessness, dry nose | |
| On the part of the musculoskeletal system | parasynovitis | ||
| From the body as a whole | headache, chest discomfort, feeling the heat | chest pain, stomach ache, fatigue | |
In the process of postmarketingovyh observations: palpitation, nose bleed, noise in ears, diarrhea, allergic reactions (skin rash, эritema), prolonged erection, feeling of general discomfort, sensation of cold or heat, postural dizziness, cough.
Contraindications
-simultaneous intake of nitrates and other nitric oxide donors;
- Hypersensitivity to any component of the drug.
FROM caution udenafil should be appointed patients with uncontrolled arterial hypertension (FROM >170/100 mmHg.), hypotension (FROM < 90/50 mmHg.); patients with inherited retinal degenerative diseases (including retinitis pigmentosa, Proliferative Diabetic Retinopathy); patients, have suffered in the past 6 months of stroke, myocardial infarction or Aortocoronary bypass surgery; patients with severe hepatic or renal failure; If there is a congenital syndrome elongation QT interval or when you increase the QT interval due to drugs.
Should take into account the potential risk of developing complications during sexual activity in patients with such diseases of cardiovascular system, as unstable angina or angina, occurring during sexual intercourse; chronic heart failure functional class II-IV (NYHA classification), evolved in the past 6 months; uncontrolled cardiac arrhythmia.
FROM caution udenafil should be used in patients with a predisposition to priapizmu, as well as in patients with anatomical deformation of the penis, If there are penile implant.
Together admission udenafila and calcium channel blockers, alpha blockers or other gipotenziveh funds may be an additional reduction in systolic and diastolic hell on 7-8 mmHg.
Pregnancy and lactation
Registered indication the product is not intended for use in women.
Cautions
Sexual activity is a potential risk for patients with cardiovascular disease, Therefore, treatment of erectile dysfunction, incl. using udenafila, There should be no men with heart disease, in which sexual activity is not recommended.
Patients with difficulty blood outflow from the left ventricle (aortalnыy stenosis) may be more sensitive to the effects of vasodilators, PDE5 inhibitors including. Despite the lack of research in clinical cases of prolonged erections (more 4 no) and priapism (painful erection, of more than 6 no), such phenomena peculiar to this class of drugs. In the event of an erection lasting more than 4 no (regardless of the existence of pain) patients should immediately seek medical assistance. In the absence of timely treatment of priapism can lead to permanent damage to the erectile tissue and erectile function.
Due to the lack of clinical data on the use of udenafila in patients over 71 year of this category of patients receiving this drug is not recommended. Udenafil is not recommended in combination with other treatments for erectile dysfunction.
Effects on ability to drive vehicles and management mechanisms
Patients, which activity is connected with driving vehicles and Office arrangements, You must define the individual responses to a drug.
Overdose
In single dose of the drug at a dose of 400 mg of adverse events were comparable to those observed in the employment udenafil at lower doses, but they were more frequent.
Treatment: symptomatic therapy. The dialysis does not accelerate the elimination of udenafil.
Drug Interactions
Inhibitors, izofermentov zitohroma CYP3A4 (ketoconazole, itraconazole, ritonavir, indinavir, cimetidine, Erythromycin, grapefruit juice) may enhance the action of udenafil.
Ketoconazole (dose 400 mg) increases the bioavailability and (C)max udenafila (dose 100 mg) almost in 2 times (212%) and in 0.8 times (85%), respectively.
Ritonavir and indinavir znachitelyno usilivayut action udenafil.
Dexamethasone, rifampicin and anticonvulsants (Carbamazepine, phenytoin and phenobarbital) may accelerate the metabolism udenafil, Therefore, when a joint application decreases the efficiency of udenafila.
In experimental studies, with the combined introduction of udenafila (30 mg/kg orally) and nitroglycerine (2.5 mg/kg once/in) There has been no impact on farmakokinetiku udenafila, However, simultaneous clinical use of nitroglycerin and udenafila is not recommended due to the possible lowering of HELL.
Udenafil and drugs from the Group Alpha-adrenoblockers is sosudorasshiratmi means, Therefore, if necessary, the simultaneous application of both drugs should be appointed at the minimum effective dose
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children, dry, dark place at temperatures not above 30 ° C. Shelf life – 3 year.
