Composition, form of production and packaging
The tablets covered with a filmy cover of light pink color with a beige tint, oval, with a squashed symbol "100" on one side and symbols in the form of separated letters "Z" and "Y" on the other; on the bend - white or almost white.
Udenafil 100 mg
Excipients: lactose, corn starch, colloidal silicon dioxide, L-hydroxypropylcellulose, hydroxypropyl cellulose-LF, talc, magnesium stearate.
Sheath composition: hydroxypropylmethylcellulose, talc, iron oxide red, iron oxide yellow, titanium dioxide.
1 PC. - packings of cellular contour (1) - packs cardboard.
1 PC. - packings cellular planimetric (2) - packs cardboard.
2 pcs. - packings of cellular contour (1) - packs cardboard.
2 pcs. - packings cellular planimetric (2) - packs cardboard.
4 things. - packings of cellular contour (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
The drug for the treatment of erectile dysfunction. It is a reversible selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5).
Udenafil does not have a direct relaxing effect on an isolated cavernous body, but with sexual stimulation enhances the relaxing effect of nitric oxide by inhibiting PDE5, responsible for the disintegration of cGMP in the cavernous body. The consequence of this is the relaxation of the smooth muscles of the arteries and the flow of blood 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 PDE5 enzyme. PDE5 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 the cerebellum. Udenafil is 10,000 times more potent inhibitor of PDE5 than with PDE1, PDE2, PDE3 and PDE4, which are localized in the heart, brain, blood vessels, liver and other organs.
In addition, udenafil is 700 times more active against PDE5 than with PDE6, found in the retina and responsible for color perception. Udenafil does not inhibit PDE11, which causes absence of cases of myalgia, back pain and manifestations of testicular toxicity.
Udenafil improves the erection and the possibility of a successful sexual intercourse. The effect of the drug has an optimal duration - up to 24 hours. The effect manifests itself 30 minutes after taking the drug in the presence of sexual arousal.
Udenafil in healthy individuals does not cause a significant change in systolic and diastolic pressure in comparison with placebo in the supine and standing position (the average maximum decrease is 1.6 / 0.8 mmHg and 0.2 / 4.6 mmHg, respectively).
Udenafil does not cause changes in color recognition (blue / green), which is explained by its low affinity with PDE6. Udenafil does not affect visual acuity, electroretinogram, intraocular pressure and pupil size.
In the study of udenafil in men, there was no clinically significant effect of the drug on the number and concentration of sperm, motility and morphology of spermatozoa.
After oral administration, udenafil is rapidly absorbed. T max is 30-90 minutes (on the average - 60 minutes). Eating high in fat does not affect the absorption of udenafil.
High binding of udenafil with plasma proteins (93.9%) prolongs the period of its effectiveness to 24 hours after taking one dose.
Udenafil does not accumulate in the body. With the daily intake of healthy volunteers of udenafil in doses of 100 mg and 200 mg per day for 10 days, there were no significant changes in its pharmacokinetics.
Udenafil is mainly metabolized with the participation of the CYP3A4 isoenzyme.
T 1/2 is 12 hours. In healthy volunteers, the total clearance of udenafil is 755 ml / min. After ingestion, udenafil is excreted as metabolites with feces.
Pharmacokinetics in special clinical cases
The intake of alcohol in the amount of 112 ml (in terms of 40% ethyl alcohol) in combination with the intake of udenafil inside at a dose of 200 mg does not affect the pharmacokinetic profile of udenafil.
- treatment of erectile dysfunction characterized by an inability to achieve or maintain an erection penis sufficient for a satisfactory sexual intercourse.
The drug is taken orally, regardless of food intake, 30 minutes before the alleged 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. The maximum recommended frequency of application is 1 time / day.
The table lists the side effects, depending on the incidence, observed during clinical studies of udenafil.
Organ organs and systems Side effects
very often often sometimes
> 10% 1% -10% 0.1-1%
From the cardiovascular system, the flow of blood to the face
From the side of the central nervous system, dizziness, rigidity of the neck muscles, paresthesia
From the side of the organ of vision reddened eyes blurred vision, pain in the eyes, increased lacrimation
Dermatological reactions of the eyelid edema, edema of the face, urticaria
On the part of the digestive system, dyspepsia, discomfort in the abdomen, nausea, toothache, constipation, gastritis
On the part of the endocrine system, thirst
On the part of the respiratory system, the stuffiness of the nose is shortness of breath, dryness in the nose
From the side of the musculoskeletal system, periarthritis
On the part of the body as a whole, headache, discomfort in the chest, a sensation of heat chest pain, abdominal pain, fatigue
In the process of postmarketing observations: heart palpitations, nosebleeds, tinnitus, diarrhea, allergic reactions (skin rash, erythema), a prolonged erection, a feeling of general discomfort, a feeling of cold or heat, postural dizziness, coughing.
- simultaneous reception of nitrates and other donators of nitric oxide;
- Hypersensitivity to any of the components of the drug.
Caution should be given to udenafil patients with uncontrolled arterial hypertension (BP> 170/100 mmHg), arterial hypotension (BP <90/50 mmHg); patients with hereditary degenerative diseases of the retina (including retinitis pigmentosa, proliferative diabetic retinopathy); patients who have had stroke, myocardial infarction, or coronary artery bypass in the last 6 months; patients with severe hepatic or renal insufficiency; if there is a congenital syndrome of prolongation of the QT interval or with an increase in the QT interval due to drug administration.
The potential risk of developing complications associated with sexual activity in patients with cardiovascular diseases such as unstable angina or angina arising during intercourse should be considered; chronic heart failure II-IV functional class (according to the NYHA classification), developed during the last 6 months;uncontrolled disturbances of the heart rhythm.
Caution should be applied to udenafil in patients with a predisposition to priapism, as well as in patients with an anatomical deformation of the penis, if there is an implant of the penis.
With the simultaneous administration of udenafil and calcium channel blockers, alpha-blockers or other antihypertensive agents, an additional decrease in systolic and diastolic blood pressure can be observed at 7-8 mmHg.
PREGNANCY AND LACTATION
According to the registered indication the drug is not intended for use in women.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution, the patient will prescribe the drug to patients with renal insufficiency.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution, the patient will prescribe the drug to patients with hepatic insufficiency.
APPLICATION FOR CHILDREN
APPLICATION IN ELDERLY PATIENTS
Due to the lack of clinical data on the use of udenafil in patients older than 71 years of this category of patients, this drug is not recommended.
Sexual activity has a potential risk for patients with cardiovascular diseases, so the treatment of erectile dysfunction, incl. with the use of udenafil, should not be performed in men with heart disease, in which sexual activity is not recommended.
Patients with difficulty in bleeding from the left ventricle (aortic stenosis) may be more sensitive to the action of vasodilators, including PDE inhibitors. Despite the absence of prolonged erections (more than 4 hours) and priapism (a painful erection lasting more than 6 hours) in clinical trials, such phenomena are peculiar to this class of drugs. In the case of an erection lasting more than 4 hours (regardless of the presence of pain) patients should immediately seek medical help. In the absence of timely treatment, priapism can lead to irreversible damage to erectile tissue and erectile function.
Due to the lack of clinical data on the use of udenafil in patients older than 71 years of this category of patients, this drug is not recommended. It is not recommended to use udenafil in combination with other treatments for erectile dysfunction.
Impact on the ability to drive vehicles and manage mechanisms
Patients whose activities are associated with driving vehicles and managing mechanisms, should determine the individual response to taking the drug.
At a single administration of the drug at a dose of 400 mg, adverse events were comparable to those observed with the use of uadenafil in lower doses, but were more common.
Treatment: symptomatic therapy. Dialysis does not accelerate the excretion of udenafil.
Inhibitors of cytochrome isoenzymes CYP3A4 (ketoconazole, itraconazole, ritonavir, indinavir, cimetidine, erythromycin, grapefruit juice) can enhance the action of udenafil.
Ketoconazole (400 mg dose) increases the bioavailability and C max of udenafil (at a dose of 100 mg) by almost 2 times (212%) and 0.8 times (85%), respectively.
Ritonavir and indinavir significantly enhance the action of udenafil.
Dexamethasone, rifampicin and anticonvulsants (carbamazepine, phenytoin and phenobarbital) can accelerate the metabolism of udenafil, so when combined, the effectiveness of udenafil decreases.
In experimental studies with combined administration of udenafil (30 mg / kg orally) and nitroglycerin (2.5 mg / kg once iv) no effect on the pharmacokinetics of udenafil was observed, however, the simultaneous clinical use of nitroglycerin and udenafil is not recommended because of the possible reduction HELL.
Udenafil and drugs from the group of alpha-blockers are vasodilators, therefore, if simultaneous application is necessary, both drugs should be prescribed in the minimum effective doses
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 30 В° C. Shelf life - 3 years.