Subclass
"Graves disease tx
Thioamides/Thioureylenes/ Carbimazole, methimazole &
Thiourea Derivatives
Iodine
Drugs MOA
MMI PTU
"Contain thiourea &
thiocarbamide
(S-C-N) group"
1. Inhibit iodination of tyrosyl thyrotoxicosis"
group in thyroglobulin
propylthiouracil 2. Inhibit coupling of
iodotyrosine to form T3 & T4 iodinated tyrosine not
3. Inhibit peripheral
deiodination of T4 to T3
(propylthiouracil)
1. Convert I to I-
2. Inhibit TH release by
inhibiting thyroglobulin
proteolysis
Iodine 3. May inhibit iodination of
thyroglobulin, possibly by
⬇️
reducing H2O2 generation
4. size & vascularity of
gland [preoperative]
131^I
1. Emit β radiation
- Short ranged, absorbed by
tissue
Radioactive iodines - Exert powerful cytotoxic
action on thyroid follicle cells
(destroy tissue)
2. γ rays (pass through
tissues)
Uses
along with radioactive
iodine, hasten recovery
as radiation takes time
Control disorder while
⬇️
waiting for surgery
⬇️
TH output
Signs & symptoms of
*Delayed clinical effects
because stored
affected
PTU: 2nd line
1st trimester pregnancy/
MMI allergy
Avoid in peds, unless
MMI allergy
Monitor PTU therapy for
liver injury
1. Preparation for surgical
thyroidectomy
2. Use with PTU/MMI for
the treatment of thyroid
storm
3. Prophylaxis – protect
thyroid gland from taking
up radioiodine
after nuclear accident
Grave's disease in
younger pts, high relapse
rate associated with
antithyroid therapy
Adjunct tx in
well-differentiated CA
Pharmacokinetics
Completely absorbed
Mostly single oral dose
Plasma t½ = 6-15 hrs, slow
onset
Not bound to plasma proteins
Excreted in the urine
Does not inhibit T4 to T3
conversion
TH lowering to euthyroid 6-7
weeks
Given orally in solution as Na-I^131, single dose, t1/2=8 days
Rapidly absorbed, concentrated by thyroid & incorporated into
storage follicle
Delayed cytotoxic effect for 1-2 month, max action for further 2
months
Rapidly absorbed; 50-80 % (1st
pass effect)
Multiple oral dosing (2-3)
needed daily
Plasma t½ = 2 hrs, onset
faster*
Highly bound to plasma protein
(75 %)**
Excreted in the urine
*Inhibits peripheral conversion 5. Headache, fever, jaundice, joint
of T4 to T3
Slower, up to 16 weeks
ADR
Cross the placental barrier & are
concentrated by the fetal thyroid
1. Urticaria rashes (most common)
2. Agranulocytosis (reversible if drug
removed)- dose related with MMI &
older pts
3. Severe liver injury & acute liver
failure (PTU)
4. Cholestatic jaundice (MMI)
pain"
1. Cause fetal goiter
2. Monotherapy cause exacerbation
of thyrotoxicosis in an iodine-
enriched gland
3. Gland escape from iodine block in
2-8 weeks
4. Anaphylactic, rashes, swollen
salivary gland, ulcers, conjunctivitis,
fever, rhinorrhoea, metallic taste,
bleeding disorder
Destroy fetal thyroid gland, excreted
in breast milk
Sore throat, salivary gland swelling,
mild nausea
Precautions: Avoid prolonged
contact (11 days), sharing utensils &
food, Drink lots of liquid, void, flush
twice

β-adrenoceptor antagonist
Levothyroxine (L-T4)
Synthetics
Liothyronine (L-T3)
⬇️
1. Preparation of
1. symptoms of thyrotoxic patients for
AV blockade, hypotension,
hyperthyroidism eg. surgery
bradycardia,
tachycardia, dysrhythmias, 2. Initial treatment for
Propranolol Onset within 4-6 hours contraindicated in severe heart
tremor & agitation hyperthyroid patients while
failure and
2. Inhibit peripheral the thioamides or
asthma
conversion of T4 to T3 radioiodine take effect
3. Acute thyroid crisis tx
1. Thyroid replacement for
hypothyroidism &
Nervousness, palpitations,
cretinism 1. Long t1/2 (7days)
tachycardia, heat intolerance &
2. TSH suppression 2. Administered once daily
unexplained weight loss
therapy in pts w thyroid
CA, non-thyroid nodule
⬆️
1. More potent than levothyroxine,
For short-term 1. Shorter t1/2 (24hr)
risk of cardio-toxicity,
suppression of TSH and 2. Administer IV multiple time
contraindicated in cardiac ds pts
myxedema coma 3. Difficult monitoring
2. Higher cost