 A 33 year old woman who presents with complaints of fatigue

requiring daytime naps, weight gain, cold intolerance, and muscle

weakness for the last few months. These complaints are new since she
used to always feel “hot” noted difficulty sleeping, and could eat
anything that she wanted without gaining weight. She also would like
to become pregnant in the near future. Because of poor medication
adherence to methimzole and propranolol, she received radioactive
iodine (RAI) therapy, developed hypothyroidism and was started on
levothryroxine 100 mcg daily. Other medications include calcium
carbonate three times daily to protect her bones and omeprazole for
heartburn. On physical examination, her blood pressure is 130/89 mm
Hg with a pulse of 50 bpm. Her weight is 136lb (61.8 kg) an increase of
10 lb (4.5 kg) in the last year. Her thryroid gland is not palpable and her
reflexes are delayed. Laboratory findings include a thyroid stimulating
hormane (TSH) level of 24.9 µIU / mL (normal 0.45 – 4.12 µIU / mL) and
a free thyroxine level of 8 pmol/L (normal 10 – 18 Pmol / L). Evaluate
the management of her past history of hyperthyroidism and assess her
current thryoid status. Identify your treatment recommendations to
maximize control of her current thyroid status.
1. Crucial for normal growth & development
2. Metabolic homeostasis

 “Unique storage”

 Thyroid gland
 Secretes : T3 & T4
 Calcitonin
 1. Increased proteolysis of the
thryroglobulin – diminishes
follicular substance

2. Increased the rate of the iodide

pump – “iodide trapping”

3. Increased iodination of
tyrosine –

4. Increased size and

increased secretary activity
8
  Biosynthesis
1. (I-) Iodide trapping
2. Iodide organification
3. Coupling of iodotyrosine residues
4. Proteolysis and release of hormones
5. Transport in the blood
6. Peripheral conversion of T4 to T3

9
 IODIDE PUMP – The Sodium and Iodide
0
symporter
 IODIDE TRAPPING
3
12
Pharmacology of thyroid hormones
Pharmacokinetics:

 Absorbed from small intestine

 T3 completely absorbed
 Metabolic clearance increased in hyperthyroidism and
by inducing drugs
 TBG sites are increased during pregnancy,
with estrogens & OCP

17
18
 Growth and Development
 Intrauterine and Extrauterine

 Metabolic actions
 Protein
 Carbohydrate
 Fat

 Cardiovascular system
 Ionotropic & Chronotropic
 Direct genomic action and sensitivity to
catecholomines
 G I T: Diarrhoea and constipation

 Reproductive tract:

 Skin
 Cretinism
 Myxedema
 Hashimoto’s thyroiditis

 Primary hypothyroidism
 Secondary hypothyroidism
 tertiary hypothyroidism
 Levothryoxine Liothyronine
1. Absorption = 80% 100%

2. PPC – 2 – 4 Hrs PPC – 2 – 4 Hrs

3. Plasma Half life 7 days Plasma Half life 18 – 24 Hrs

4. Desirable for chronic Hormone Desirable when more rapid onset of

replacement therapy action is required

5. Acceptable marginal elevation of T4 Transient elevations of T3 – above

with normal TSH the normal range

6. Economic costly
 Thyroid Hormone Replacement Therapy in
Hypothyroidism:
 Primary Hypothyroidism
 Subclinical Hypothyroidism
 Hypothyroid women and pregnancy
 Myxedema coma
 Congenital hypothyroidism
 Thyroid Nodules

 TSH suppression Therapy in patients with

Thyroid cancer.
 Hyperthyroidism
 Grave’s disease
 Toxic goitre
1. Inhibitors of iodide transport : perchlorate,

thiocyanate
2. Inhibitors of iodination of thyroglobulin: Thioamides
Iodides
Thiocyanates
3. Inhibitors of coupling : Thioamides


26
 4. Inhibitors of hormonal release : Iodides, lithium salts

 5. Inhibitors of peripheral deiodination : ipodate

 β blockers
 Amiodarone
 Corticosteroids

 6. ablation of thyroid : Radio active iodine I131



27
 Drugs which interfere with hormonal synthesis
 Ionic Inhibitors –Thyocyanate, Perchlorate
 Thioamides – Propylthiouracil, Carbimazole

 Drugs that interfere with the hormonal release

and promote its storage
 Iodides and Lugol’s Iodine

 Radioactive iodine
 Certain Drugs –
 Amiodarone, glucocorticoids and beta blockers
 Rifampicin and phenytoin
 Potassium Perchlorate & Thiocyanate

 Blocks the uptake of iodide by the gland

through competitive inhibition of the iodide
transport mechanism.

 Perchlorate 750 mg daily has been used in

 Grave’s disease
 Amiodarone – iodine - induced thyrotoxicosis
NIS
 Carbimazole, Methyl and Propyl- thiouracil
 Binds and inhibit the thyroid peroxidase;
▪ Oxidation of Iodide
▪ Iodination of tyrosine
▪ Coupling of MIT & DIT
▪ Propylthyouracil – prevents the conversion of T4 to T3
 Therapeutic Uses:
 Management of hyperthyroidism
 Thyrotoxic crisis
 Surgical subtotal thyroidectomy
 Rationale of adding beta blockers (propanolol) with
thioamides -
 Rationale of adding beta blockers (propanolol) with
thioamides –

 Propylthyouracil safe in pregnancy?

 Concentrated selectively in thyroid gland

 Emits gamma and beta radiations

 Gamma radiation - to measure radioiodine uptake
and for thyroid scan
 25 – 100 millicurie have diagnostic use for evaluating
thyroid functions

 Beta radiation penetrates in soft tissues – act as

ionising radiation – selectively destroys the thyroidal
follicles produces fibrosis .
 5 – 15 millicurie is used for non surgical thyroid ablation
 Oldest remedy
 Quick onset of action
 BMR falls comparable to total thyroidectomy
 Acinar cells become smaller in size
 Colloidal content increases
 Maximum clinical benefit seen in 10 – 14 days
 Shuts down the release of preformed
hormones (Thyroid constipation)

 Inhibits synthesis of iodotyrosine and

iodothyronine

 It limits its own transport resulting in low

iodide levels
 Lugol’s Iodine
 5 g of iodine in 100 mL of 10% solution of
potassium iodine – 150 mg of iodine / mL

 SSKI (Saturated Solution of Potassium Iodide)

 30 g of KI in 21 mL of water
 Prevention of endemic goitre

 Preoperative preparation – important use of

iodides

 Rapid control of hyperthyroidism along with

a thioamide
 Hospitalisation
 Treatment of the precipitating cause
 Large doses of an antithyroid drug
 Iodide
 Sodium iodide 1g by infusion or through a nasogastric tube (0.3
mL of SSKI every 8 hour)
 Propranolol 2 – 10 mg repeated every 4 h or Labetalol every 4 –
6h
 Supportive measures – dexamethasone 8 hourly
 Oxygen, fluids, and glucose, B complex vitamins, antimicrobials
and treatment for hyperpyrexia and tepid sponging.
 Aspirin should be avoided – displaces thyroid hormone from its
binding proteins.