Udenafil (Udenafilum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Means that regulate the function of the genitourinary system and reproduction

Included in the formulation
  • Ziden®
    pills inwards 
    Mezzon Pharma Co., Ltd.     The Republic of Korea
    • АТХ:

    G.04.B.E   Drugs for the treatment of erectile dysfunction

    G.04.B.E.11   Udenafil

    Pharmacodynamics:

    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. Has no effect in the absence of sexual stimulation.

    It is a selective inhibitor of the enzyme PDE5. 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. It 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.

    It is 700 times more active with respect to PDE5 than with respect to PDE6, found in the retina and responsible for color perception. It does not inhibit PDE11, which causes absence of cases of myalgia, low back pain and manifestations of testicular toxicity.

    Improves the erection and the possibility of a successful sexual intercourse. The effect of the drug lasts up to 24 hours. The effect manifests itself 30 minutes after admission with the presence of sexual arousal.

    In healthy individuals, there is no significant change in systolic and diastolic pressure compared with placebo in the supine and standing position (the mean maximum decrease is 1.6 / 0.8 mm Hg and 0.2 / 4.6 mm Hg. respectively).

    Does not cause changes in color recognition (blue / green), which is explained by its low affinity with PDE6. Does not affect visual acuity, electroretinogram, intraocular pressure and pupil size.

    Pharmacokinetics:

    The time to reach the maximum concentration after oral administration is 30-90 minutes (on average - 60 minutes). Eating high in fat does not affect absorption.

    Binding to blood plasma proteins (93.9%). With daily intake of healthy volunteers at doses of 100 mg and 200 mg per day for 10 days, no significant changes in its pharmacokinetics were found.

    Metabolized with the participation of the isoenzyme CYP3A4. The half-life is 12 hours. In healthy volunteers, the total clearance of udenafil is 755 ml / min.After oral administration, it is excreted as metabolites with feces.

    Indications:

    Erectile dysfunction, characterized by inability to achieve or maintain an erection penis sufficient for a satisfactory sexual intercourse.

    ICD-10

    XIV.N40-N51.N48.4   Impotence of organic origin

    V.F50-F59.F52.2   Insufficiency of the genital reaction

    Contraindications:

    Hypersensitivity, child and elderly age, liver and kidney disease.

    Carefully:

    In patients with uncontrolled arterial hypertension (BP> 170/100 mm Hg), arterial hypotension (BP <90/50 mm Hg); 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; in the presence of a congenital syndrome of QT interval prolongation or with an increase in the QT interval due to drug intake; in patients with a predisposition to priapism, as well as in patients with an anatomical deformation of the penis, in the presence of a penile implant.

    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.

    Pregnancy and lactation:

    The category of recommendations for the FDA is not defined.

    Adequate and well-controlled studies in humans and animals have not been conducted. Do not apply! There is no information on the penetration into breast milk. Do not apply! The drug is not intended for use by women.

    Dosing and Administration:

    Inside. 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 per day.

    Side effects:

    From the side of cardio-vascular system: very often (> 10%) - the flush of blood to the face.

    From the side nervous system: sometimes (0,1-1%) - dizziness, rigidity of neck muscles, paresthesia.

    From the side organ of vision: often (1-10%) - redness of the eyes; sometimes (0.1-1%) - blurred vision, pain in the eyes, increased lacrimation.

    Dermatological reactions: sometimes (0.1-1%) - edema of the eyelids, edema of the face, urticaria.

    From the side digestive system: often (1-10%) - dyspepsia, abdominal discomfort; sometimes (0,1-1%) - nausea, toothache, constipation, gastritis.

    From the side endocrine system: sometimes (0.1-1%) is thirst.

    From the side respiratory system: often (1-10%) - nasal congestion; sometimes (0,1-1%) - dyspnea, dryness in the nose.

    From the side musculoskeletal system: sometimes (0,1-1%) - periarthritis.

    From the side organism as a whole: often (1-10%) - headache, chest discomfort, sensation of fever; sometimes (0,1-1%) - chest pain, abdominal pain, fatigue.

    Overdose:

    Symptoms: with a single dose of 400 mg, adverse events were comparable to those observed with admission of uadenafil at lower doses, but were more common.

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

    Interaction:

    In simultaneous reception udenafil and calcium channel blockers, alpha-blockers and other antihypertensive agents there may be a further reduction in systolic and diastolic blood pressure at 7-8 mmHg

    Special instructions:

    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.

    Patients whose activities are related to driving vehicles and controlling mechanisms, should determine the individual response to taking udenafil.

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