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    Thyroidv and Antithyroid Drugs

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    Sai Sreedhar

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    Thyroidv and Antithyroid Drugs

    Uploaded by

    Sai Sreedhar
    1 views18 pages

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    Thyroidv and antithyroid drugs-converted

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    1 views18 pages

    Thyroidv and Antithyroid Drugs

    Uploaded by

    Sai Sreedhar

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 18

    Thyroid & Antithyroid Drugs

    • Thyroid gland secretes thyroid hormones


    Triiodothyronine (T3)
    Thyroxine (T4)
    calcitonin
    Pharmacological actions of thyroid
    hormons
    • On carbohydrate metabolism
    • ↑ Glycogenolysis
    • ↑ Gluconeogenesis
    • ↑ Glucose absorption from GIT
    • Enhance glycolysis (Rapid uptake of glucose
    by the cells)
    • Net result – Increased blood glucose levels
    On protein metabolism-
    ↑ protein catabolism
    On fat metabolism
    ↑ mobilisation of fat
    Oxidation of fatty acids
    On BMR-
    ↑ Basal metabolic rate
    • On growth-
    ↑ growth
    On GIT-
    Increase appetite and food intake
    ↑ rate of secretion of digestive juice
    ↑ GI motility
    On CVS-
    ↑ tissue sensitivity to catecholamines
    ↑ cardiac output

    On nervous system
    Excitable effect
    Plays a role in development of brain in fetal and 1st
    few weeks of postnatal life.
    Muscle weakness due to protein catabolism
    Synthesis of thyroid hormone
    • Transport of iodide into thyroid gland by
    Sodium iodide symporter
    Oxidation of iodide by thyroperoxidase to
    iodine.
    Tyrosine in thyroglobulin is iodinated and forms
    monoiodo tyrosine(MIT) and
    diiodotyrosine(DIT).
    • Iodotyrosine condensation within
    thyroglobulin molecule
    MIT+ DIT→ Triiodo thyronine(T3)
    DIT+DIT → Thyroxine T4
    T4,T3,MIT and DIT are rekeased from
    thyroglobulin by exocytosis & proteolysis of
    thyroglobulin.

    7
    • Thyroid hormones (T4 % T3) transported in
    plasma.
    • They bound to protein thyroxine binding
    globulin in reversible manner.
    • Only about 0.04% of total T4 & 0.4% T3 exist
    in the free form.
    Thyroid drugs
    • Levothyroxine (L-T4)
    • Levothyronine (T3)
    • They produce all the effects via binding to
    nuclear receptors,which induce new protein
    generation which produce effects
    Use- short term suppression of TSH
    Used to treat hypothyroidism.
    Antithyroid drugs
    • Classification
    1.Thioamides
    Ex: propylthiouracil
    Methimazole
    Carbimazole
    Anion inhibitors
    Ex: Perchlorate
    Thiocyanate
    • Iodinated contrast media:
    Ex: Diatriazoate
    Iohexol
    Iodides:
    Ex; KI & NaI
    Rdioactive Iodine:
    Ex: I 131
    • Thioamides prevent hormone synthesis by
    inhibiting the thyroid peroxidase catalized
    reactions and blocking iodine organification.
    • Blocks coupling of iodotyrosines
    • Propylthiouracil and methimazole inhibits
    peripheral deiodination T4 & T3.
    • Their effect requires 4 weeks
    • Carbimazole & methimazole are teratogenic
    • Propylthiouracil is safe in pregnancy
    Adverse effects
    • An altered sense of taste and smell occurs
    with methimazole.
    • Maculopapular pruritic rash is most common
    • Hepatitis and cholestatic jaundice can be fatal.
    Clinical use
    Used in thyrotoxicosis
    For preoperatively to make euthyroid
    Anion Inhibitors
    • Block uptake of iodine by the gland through
    competitive inhibition of the iodide transport
    mechanism
    • Potassium iodide block thyroidal reuptake of
    iodide in patients with iodide iduced
    hyperthyroidism
    • Potassium perchlorate is rarely
    used,associated with aplastic anaemia.
    Iodides-Inhibitors of hormone release
    • They inhibit organification
    • Hormone release
    • Decrease size and vascularity of the
    hyperplastic gland.
    Clinical use:
    • Prophylaxis in endemic goiter
    • Preparation for thyroidectomy
    Adverse effects
    Acute: swelling of lip, eyelid, face,edema of
    larynx, fever, joint pain and thrombocytopenia
    Chronic: ulcers in the mouth, salivation,
    lacrimation, burning sensation in the mouth,
    rhinorrhoea and GI intolerence
    Radioactive iodine
    Used for treatment of thyrotoxicosis
    As a diagnostic tool for thyroid function test

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