Pyrfenidone (Pirfenidone)

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

Other antineoplastic agents

Immunosuppressive drugs

Included in the formulation
  • Esbriet
    capsules inwards 
    Hoffmann-La Roche Ltd.     Switzerland
    • АТХ:

    L.04.A.X.05   Pyrfenidone

    Pharmacodynamics:

    Suppresses the activation of the transforming growth factor beta, which is involved in the process of differentiation of fibroblasts, thereby inhibiting the proliferation of fibroblasts in the lungs, preventing the deposition of collagen and the development of pulmonary fibrosis.

    Suppresses the release of proinflammatory cytokines, tumor necrosis factor growth factor and platelet-derived growth factor. Has antioxidant activity.

    Pharmacokinetics:

    After ingestion with meals, up to 60% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 30 minutes. The connection with plasma proteins is 60%.

    Metabolism in the liver to an inactive metabolite of 5-carboxy-pyrphenidone.

    The elimination half-life is 2 hours. Elimination by the kidneys.

    Indications:

    It is used to treat idiopathic pulmonary fibrosis.

    ICD-10

    X.J80-J84.J84   Other interstitial lung diseases

    Contraindications:

    Age under 18 years, severe renal and hepatic insufficiency, pregnancy and lactation, simultaneous use with fluvoxamine, smoking, individual intolerance.

    Carefully:

    Renal and hepatic insufficiency of mild and moderate severity, concomitant use with ciprofloxacin and moderate inhibitors of CYP1A2.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside, with meals, 801 mg 3 times a day.

    The highest daily dose: 2403 mg.

    The highest single dose: 801 mg.

    Side effects:

    Central and peripheral nervous system: headache, dizziness, insomnia, apathy.

    Respiratory system: shortness of breath, productive cough.

    Hemopoietic system: rarely - agranulocytosis.

    The cardiovascular system: tides.

    Digestive system: anorexia, weight loss, nausea, vomiting, gastroesophageal reflux disease, flatulence, gastritis, constipation.

    Musculoskeletal system: arthralgia, myalgia.

    Dermatological reactions: a rash, photosensitivity.

    Sense organs: a violation of taste.

    urinary system: infection of the urinary system.

    Allergic reactions.

    Overdose:

    Increased side effects, sunburn.

    Treatment is symptomatic.

    Interaction:

    Smoking patients decrease the concentration of pyrfenidone in the blood plasma.

    With simultaneous use with ciprofloxacin, the risk of side effects increases.

    Omeprazole reduces the concentration of pyrfenidone in the blood plasma.

    Special instructions:

    It is recommended to refrain from smoking during taking the drug.

    When taking the drug is not recommended driving and working with moving machinery.

    Instructions
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