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    A ppt on

    THYROID HORMONESAND THYROIDINHIBITORS

    By

    Dr.Nanita Agrawal, Dr. Prashant ,MD

    Pharmacology4students.com

    [email protected]

    1dr prashant'swww.pharmacology4students.com

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    THYROID

    HORMONESAND

    THYROID INHIBITORS

    dr prashant'swww.pharmacology4students.com

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    I. THYROID HORMONE

    A. INTRODUCTION

    The thyroid hormone secretes 3 hormones:

    1. Thyroxine (T4)2. Tryiodothyronine (T3)

    3. Calcitonin

    Former 2 are produced by thyroid follicles.

    Calcitonin produced by interfollicular c cells.3dr prashant'swww.pharmacology4students.com

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    B. ACTIONS

    Growth and development: Essential for normalgrowth and development.

    Intermediary metabolism: Marked effect on lipid,carbohydrate and proteinmetabolism.

    Calorigenesis: Increase BMR.

    CVS: Heart rate, contractility and output are

    increased.

    4dr prashant's

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    acology4students.com

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    Nervous system: Mental retardation is thehallmarkof cretinism.

    Skeletal muscle: Muscles flabby and weak inmyxoedema.

    Kidney: Rate of urine flow is often increased.

    Haemopoiesis: Facilitatory to erythropoiesis.

    Reproduction: Indirect effect on 5dr prashant'swww.pharmacology4students.com

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    C. MECHANISM OF ACTIONS

    T3 (and T4) penetrate cells.

    Combine with a nuclear receptor.

    A specific DNA sequece called thyroid hormone

    response element has been identified.

    T3-receptor complex binds.

    Derepression of gene transcription 6dr prashant'swww.pharmacology4students.com

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    D. PREPRATIONS

    1-thyroxin sod:

    Electroxin

    Roxin 100 ug tab.

    Thyranorm

    Thyrox 25 ug, 50 ug, 100 ug tabs.7dr prashant's

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    E. USES

    Cretinism: Due to failure of thyroid development.Detected during infancy or childhood. Mental

    retardation.

    Adult hypothyroidism: Develops as a consequence

    of thyroiditis, thyroidectomy, treatment with

    goiterogens; may accompany simple goiter if iodine.

    Myxoedema coma:

    Th roid nodule:8dr prashant's

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    Nontoxic goiter: May be endemic or

    sporadic.deficient production of thyroid hormone

    leads to excess TSH-throid enlarges.

    Papillary carcinoma of thyroid:

    Empirical uses:

    Refractory anaemias

    Menstrual disorders, infertility not corrected byusual treatment.

    Chronic/ non healing ulcers

    Obstinate constipation 9dr prashant'swww.pharmacology4students.com

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    2. THYROID INHIBITORS

    A. INTRODUCTION

    Drugs used to lower the functional capacity of the

    hyperactive thyroid gland.

    Throtoxicosis

    Two main causes are Graves disease and toxic

    nodular goiter10dr prashant's

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    B. CLASSIFICATION

    Inhibit hormone synthesis (Antithyroid drugs)propylthiouracil, methimazole, carbimazole.

    Inhibit iodide trapping (ionic inhibitors)thiocynates (-SCN) , perchlorates (-C1O4), nitrates

    (-NO3).

    Inhibit hormone release iodine, iodides of Na and

    K, organic iodide.

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    3. ANTITHYROID DRUGS

    A. INTRODUCTION

    Inhibit iodination of tyrosine residues inthyroglobulin.

    Inhibit coupling of iodotyrosine residues to formT3 and T4.

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    B. PHARMACOKINETICS

    Quickly absorbed orally

    Cross placenta

    Metabolised in liver

    Excreted in urine

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    C. ADVERSE EFFECTS

    Hypothyroidism due to over treatment common butreversible.

    G.I. Intolerance, skin rashes and joint pain.

    Loss or graying of hair, loss of taste, fever and liver

    damage.

    Agranulocytosis14dr prashant'swww.pharmacology4students.com

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    D. PREPARATIONS AND DOSE

    Propyltjiouracil : 50-150 mg TDS followed by 25-

    50 mg BD-TDS for maintenance PTU 50 mg tab.

    Methimazole: 5-10 mg TDS initially, maintenance

    dose 5-15 mg daily in 1-2 divided doses.

    Carbimazole: 5-15 mg TDS initially, maintenancedose 2.5-10 mg daily in 1-2 divided doses, neo

    mercazole, thyrozole, antithyrox 5 mg tab.

    Carbimazole is more commonly used in india. 15dr prashant'swww.pharmacology4students.com

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    E. USES

    The following strategies are adopted:

    1) Definitive therapy: Preferred in young patient

    with a short history.

    2) Preoperatively: Carbimazole before performing

    partial thyroidectomy.

    3) Along with 131 I.

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    F. ADVANTAGES OVER SURGERY

    No surgical risk

    Hypothyroidism, if induced, is reversible.

    Can be used even in children and young adults.

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    G. DISADVANTAGES

    Prolonged treatment is needed.

    Not practicable in uncooperative/ unintelligentpatient.

    Drug toxicity.

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    4. IODINE AND IODIDES

    A. INTRODUCTION

    Inhibition of hormone release- thyroid

    constipation.

    B. PRERARATION AND DOSE

    Lugols solution

    Colloid iodine 10%19dr prashant'swww.pharmacology4students.com

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    C. USES

    Preoperative preparation

    Thyroid storm

    Prophylaxis of endemic goiter

    Expectorant

    Antiseptic 20dr prashant'swww.pharmacology4students.com

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    D. ADVERSE EFFECTS

    Acute reactions: Swelling of lips. Eyelids,

    angioedema of larynx (may be dangerous), fever,

    joint pain.

    Chronic overdose (iodism): Long term use of high

    doses can cause hypothyroidism and goiter.

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    5.RADIOACTIVE IODINE

    A. INTRODUCTION

    131I: Physical half life 8 days- most commonly

    used.

    123I: Physical half life 13 hours- only rarely used

    diagnostically.

    125I: Physical half life 60 days.

    -22dr prashant'swww.pharmacology4students.com

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    B particles utilized for their destructive effect on

    thyroid cells.

    131I is concentrated by thyroid.

    Incorporated in colloid- emits radiation from within

    the follicles

    Thyroid follicular cellsundergo pyknosisand

    necrosis followed by fibrosis.

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    Diagnostic 25-100 u curie is given.

    Therapeutic

    Average therapeutic dose is 3-6 m curie.

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    B. ADVANTAGES

    Treatment is simple, conveniently inexpensive.

    No surgical risk, scar or injury to parathyroids/recurrent laryngeal nerves.

    Cure is permanent.

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    C. DISADVANTAGES

    Hypothyroidism

    Long latent period of response.

    Contraindicated during pregnancy- cretinism.

    Not suitable for Young patients.

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    6. B ADRENERGIC BLOCKERS

    Propranolol

    During thyrotoxic crisis.

    While awaiting response to carbimazole or 131I.

    Along with iodide for preoperative preparation

    before subtotal thyroidectomy.27dr prashant's

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    Our other websitesNaukridoctors.com

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    We thank our students who

    attend our classes in large

    numbers and motivate/encourage

    us to learn and teach better.

    You can also send any study material

    suitable for undergrads to us [email protected]