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    Tyroid Drug - ppt3

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    nurliah armand
    This document discusses thyroid and antithyroid drugs. It covers: 1) Iodide metabolism and the recommended daily iodide intake. Iodide is absorbed from food and supplements. 2) The biosynthesis of thyroid hormones and the pharmacokinetics of thyroid hormone absorption and metabolism. 3) The mechanisms and pharmacokinetics of common antithyroid drugs including thioamides like methimazole and propylthiouracil, anion inhibitors, and iodides. Adverse effects and complications are also outlined.

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    Tyroid Drug - ppt3

    Uploaded by

    nurliah armand
    46 views15 pages
    This document discusses thyroid and antithyroid drugs. It covers: 1) Iodide metabolism and the recommended daily iodide intake. Iodide is absorbed from food and supplements. 2) The biosynthesis of thyroid hormones and the pharmacokinetics of thyroid hormone absorption and metabolism. 3) The mechanisms and pharmacokinetics of common antithyroid drugs including thioamides like methimazole and propylthiouracil, anion inhibitors, and iodides. Adverse effects and complications are also outlined.

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    bhn kul

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    Tyroid Drug.ppt3

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    This document discusses thyroid and antithyroid drugs. It covers: 1) Iodide metabolism and the recommended daily iodide intake. Iodide is absorbed from food and supplements. 2) The biosynthesis of thyroid hormones and the pharmacokinetics of thyroid hormone absorption and metabolism. 3) The mechanisms and pharmacokinetics of common antithyroid drugs including thioamides like methimazole and propylthiouracil, anion inhibitors, and iodides. Adverse effects and complications are also outlined.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    46 views15 pages

    Tyroid Drug - ppt3

    Uploaded by

    nurliah armand
    This document discusses thyroid and antithyroid drugs. It covers: 1) Iodide metabolism and the recommended daily iodide intake. Iodide is absorbed from food and supplements. 2) The biosynthesis of thyroid hormones and the pharmacokinetics of thyroid hormone absorption and metabolism. 3) The mechanisms and pharmacokinetics of common antithyroid drugs including thioamides like methimazole and propylthiouracil, anion inhibitors, and iodides. Adverse effects and complications are also outlined.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    of 15

    THYROID AND ANTITHYROID DRUG

    IODIDE METABOLISM

    - The recommended daily adult iodide (I-)


    intake is 150 g (200 g during pregnancy)
    - Iodide ingested from : food, water,
    medication
    - Iodide ingested is rapidly absorbed and
    enters extracellular fluid pool
    - Iodide intake increase  fractional iodine
    up take by the thyroid is diminished
    Biosynthesis of thyroid humane
    Pharmacokinetics of Thyroid Hormone
    - Thyroxin is well absorbed in duodenum and
    ileum
    - Oral bioavailability of thyroid hormone :
    The metabolism of both T3 and T4 are increased by
    dregs that induce hepatic microsomal enzymes
    ANTITHYROID AGENTS
    1. Thioamides
    - Consist of Methimazole and PropyHhiouracil (PTU)
    - Methimazole is ± ten times more potent than PTU
    - cd The chemical structure of thioamides are shown
    below :
    PHARMACOKINETICS THIOAMIDES
    PTU
    - Rapidly absorbed, reaching peak serum levels after 1 hour
    - The volume of distribution approximates total body water with
    accumulation in the thyroid gland
    - Half-life is 1.5 hours
    - Excreted by the kidney as the inactive glucuronide within 24
    hours
    - PTU is given every 6 -10 hours with a single 100 mg dose
    - PTU crosses the placental barrier less readily and concentrated
    by fetal thyroid
    - It is more strongly protein – bound
    - It is not secreted in sufficient quantity in breast milk to
    preclude breast - feeding
    METHIMAZOLE
    - Completely absorbed but at variable rates
    - Volume of distribution is similar to PTU
    - Half-life is 6 hours
    - Excretion is slower than PTU ; 65,70 % of dose
    is recovered in the urine in 48 hours
    - Methimazole is given in 24 hours with a single
    30 mg dose
    - Methimazole crosses the placental barrier and
    consentrated by fetal thyroid
    PHARMACODYNAMICS OF THIOAMIDES
    - Prevent hormone synthesis by inhibiting the
    thyroid peroxidase – catalysed reactions
    - Blocking iodine organification
    - Thioamides block coupling of the
    iodotyrosines
    - Thioamides do not inhibit uptake of iodine
    by the gland
    - PTU & methimazole inhibit the peripheral
    deiodination of T4 and T3
    Toxicity of Thioamides
    Adverse effect of thioamides are :
    - Maculopapular pruritic rash »
    - Fever
    - Urticarial rash
    - Vasculitis
    - Arthralgia
    - A lupus-like reaction
    - Cholestatic jaundice
    - Hepatitis
    - Lymphadenopathy
    - Hypoprothrombinemia
    - Exfoliative dermatitis
    - Polyserositis
    Complication of Thioamides
    Agranulocytosis
     Infrequent but potentially fatal adverse
    reaction
     Occurs in 0,3 – 0,6 % of patient
     The risk of agranuloagtosis may be
    increased in older patient and in those
    receiving high – dose methimazole
    therapy (over 40 mg/d)
    2. Anion Inhibitors
     Consist of monovalent anions such as :
     Perclorate (ClO4-)
     Pertechnetate (Tc04-)
     Thiocyanate ( SCN-)
     This agents block uptake of iodide by the gland through
    competitive inhibition of the iodide transport
    mechanism
     The major clinical use of potassium perchlorate is to block
    thyroidal reuptake of I- in patient with iodide induced
    hyperthyroidism
     Side effect of potassuim perchlorate is aplastic anemia
    3. Iodides
     Rarely used as sole therapy
     Pharmacodynamics
     Inhibit organification and hormone release
     Decrease the size and vascularity of the hyperplastic
    gland  valuable as preoperative preparation for
    surgery
     Dosage > 6 mg daily  inhibit hormon release ;
    inhibit thyroglobulin proteolysis
     Clinical use of Iodide
     Iodides are used after onset of Thioamide therapy
     Iodides should not be used alone  its withdrawal
    may produce severe
    exacerbation of
    tyrotoxicosis
     Iodides cross the placental barrier and can cause
    fetal goiter
    Side effect :  acneiform rash,
     swollen salivary gland
     mucous membrane ulcerations
     conjunctivitis
     rhinorrhea
     drug fever
     bleeding disorders
     rarely anaphylactoid reactions
    THANK YOU

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