Tadalafil (Tadalafilum)

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

Potency regulators

Included in the formulation
  • Cupid 36
    pills inwards 
    Cadil Pharmaceuticals Co., Ltd.     India
  • Cialis®
    pills inwards 
    Eli Lilly East SA     Switzerland
  • Tadalafil-SZ
    pills inwards 
    NORTH STAR, CJSC     Russia
  • Tadalafil-Teva
    pills inwards 
    Teva Pharmaceutical Enterprises Co., Ltd.     Israel
  • Tedallis®
    pills inwards 
    Sandoz d.     Slovenia
    • АТХ:

    G.04.B.E.08   Tadalafil

    Pharmacodynamics:

    Tadalafil is a reversible selective inhibitor of PDE-5 cGMP - an enzyme responsible for the destruction of cGMP in the cavernous bodies of the penis.

    During sexual stimulation, local release of nitric oxide occurs, and the inhibition of PDE-5 leads to an increase in cGMP concentration. The consequence of this is the relaxation of the smooth muscles of the arteries, the smooth muscles of the cavernous bodies and the flow of blood to the tissues of the penis, resulting in an intensification of the erection. In the absence of sexual stimulation, the drug does not affect the erection.

    The effect of tadalafil occurs 30 minutes after administration, the duration of action is 36 hours.

    Pharmacokinetics:

    After ingestion, the drug is rapidly absorbed. The speed and extent of absorption are not dependent on food intake.The connection with plasma proteins is high - 94%. The equilibrium concentration in the plasma is reached within 5 days with the drug taken once a day. Biotransformation occurs in the liver. Tadalafil is mainly metabolized with the participation of isoenzyme CYP3A4 cytochrome P450. The half-life is 17.5 hours. Tadalafil is excreted mainly in the form of inactive metabolites kidneys - 36%, with feces - 61%.

    Indications:erectile disfunction
    ICD-10

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

    Contraindications:
    • Hypersensitivity to the drug
    • Simultaneous reception of donators of nitric oxide and organic nitrates (in any form)
    • Age under 18 years old
    • Angina pectoris arising during intercourse
    • Heart failure, developed during the last 6 months
    • Degenerative diseases of the retina, including retinitis pigmentosa
    • Arterial hypotension (blood pressure less than 90/50 mm Hg)
    • Myocardial infarction within the last 90 days
    • Ischemic stroke, lasting for the last 6 months
    • Uncontrolled disturbances of heart rhythm
    • Uncontrolled AH (blood pressure above 170/100 mmHg)
    • Unstable angina
    • Chronic Renal Failure
    • Visual loss due to non-arterial anterior ischemic optic neuropathy optic nerve.
    • Simultaneous use of doxazosin and other drugs for the treatment of erectile dysfunction.
    • Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption
    Carefully:
    • Diseases of the cardiovascular system, aortic stenosis, idiopathic subaortal hypertrophic stenosis
    • Hepatic or moderate liver failure
    • Renal failure (CC less than 80 ml / min)
    • Predisposition to priapism
    • Anatomic deformation of the penis (angular curvature, cavernous fibrosis or Peyronie's disease)
    • Propensity to bleeding
    • Peptic ulcer of stomach and duodenum in acute stage
    Pregnancy and lactation:Not intended for use in women.
    Dosing and Administration:

    For oral administration, regardless of food intake.

    For sexually active patients (more than 2 times a week): daily 5 mg once a day. The dose can be reduced to 2.5 mg per day, based on the individual characteristics of the body.

    For sexually inactive patients (less than 2 times per week): 20 mg of the drug at least 15 minutes before the alleged sexual activity.

    The maximum daily dose of the drug is 20 mg.

    Side effects:Frequently occurring reactions to the drug:
    • Headache, dizziness
    • Abdominal pain
    • Backache
    • Myalgia
    • Tides of blood to the face
    • Dyspepsia
    • Nasal congestion
    Infrequent reactions to the drug:
    • Blurred vision
    • Nose bleed
    • Rash, urticaria
    • Hyperhidrosis
    • Chest pain
    • Prolonged erection
    Overdose:

    Symptoms: increased side effects.

    Treatment: symptomatic. It is not excreted by hemodialysis.

    Interaction:

    Ketoconazole increases the activity of tadalafil.

    Ritonavir and other HIV protease inhibitors increase the activity of tadalafil.

    Rifampicin reduces the effect of tadalafil with simultaneous use.

    Simultaneous reception with an antacid (magnesium hydroxide / aluminum hydroxide) reduces the rate of absorption of tadalafil.

    Tadalafil enhances the hypotensive effect of nitrates.

    Tadalafil has systemic vasodilator properties and can enhance the action of antihypertensive drugs, reducing blood pressure.

    The simultaneous use of tadalafil with doxazosin is contraindicated.

    Special instructions:

    In the case of an erection lasting more than 4 hours, the patient should immediately seek medical help, since untimely treatment of priapism leads to damage to the tissues of the penis, and then to the onset of impotence.

    In patients who underwent non-arterial anterior ischemic optic neuropathy, the risk of re-development of this disease increased. In case of sudden loss of vision, the patient should stop taking the drug and seek medical help.

    Because of the possible occurrence of dizziness during the treatment period, care must be taken when driving vehicles and working with potentially dangerous mechanisms, requiring concentration of attention and speed of psychomotor reactions.

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