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Normal pooled
sera (NPS)
sodium/iodide
symporter
(NIS)
TG: Thyroglobulin
Amiodarone
-blockers
Corticosteroids
Severe illness or starvation
+: stimulatory influence
-: inhibitory influence
Phenytoin
rifampin
phenobarbital
P-450 enzyme
131I
(Thioamides )
Propylthiouracil (PTU)
Methimazole
Carbimazole (used in UK)
Anion inhibitors
Iodides
Adrenoceptor-blocking agents
Coticosteroids
Radioactive iodine
Orally in solution as sodium 131I
It is rapidly absorbed, concentrated by the
thyroid, and incorporated into storage of
follicles.
rays and rays
Half-life: 8 days; 2 months
Not be administered to pregnant women,
nursing mothers and children
Thioamides
Thiocarbamide
group
Pregnacy category D
Of the two, PTU is preferable in
pregnancy because it is more strongly
protein-bound
Pharmacodynamics
Prevent hormone synthesis by inhibiting
the thyroid peroxidase-catalyzed
reactions and blocking iodine
organification
Blocking coupling of the iodotyrosines
PTU inhibit the peripheral T4 to T3
conversion
I- Na+
SCN-, ClO4-
I- Na+
Extracellular
space Thioamides
TG Iodides(High)
Thyroid peroxidase
(organification) TG-MIT
TG-DIT
Thyroid peroxidase
(coupling)
T3 T4
Colloid
space
131I- TG
Iodides(High)
T3 T4
Follicular cell
Propylthiouracil (PTU)
T4
T3
Toxicity of thioamides (I)
3-12% of treated patients
Nausea and GI distress (occur early)
An altered sense of taste or smell may occur
with methimazole
Most common: maculopapular pruritic rash (4-
6%)
Rare adverse effect: urticarial rash, vasculitis,
lupus-like etc.
Hepatitis (more common with PTU)
Cholestatic jaundice (more common with
methimazole)
Toxicity of thioamides (II)
Agranulocytosis (most dangerous)
Granulocyte count < 500 cells/mm3
Older patients or high-dose methimazole
therapy (> 40 mg/day)
Cross-sensitivity between PTU and
methimazole is about 50%
switching drugs in patients with severe
reactions is not recommended
Anion inhibitors
Perchiorate (ClO4-) pertechnetate (TcO4-)
thiocyanate (SCN-)
Action
blocking uptake of iodide transporter mechanism
Major clinical use
potassium perchlorate for iodide-induced
hyperthyroidism
Side effect: aplastic anemia
Iodides
(I-)
H2O2
Propranolol
-adrenergic receptor antagonist
:
Guanethidine
Non-adrenergic-blocking agent (inhibits NE release)
Corticosteroids
T4 T3
Graves disease
Hyperthyroidism
NO NO
NO
Below Age 20
20-30 hypothyroidism
years old
YES YES
YES
YES
NO
NO
NO
PTU or YES
Methimazole
NO
NO YES
YES
6-12
T4
Thyroid storm (thyrotoxic crisis)
Thyroid storm
(nervous)
()
sinus tachycardiaatrium flutteratrial
fibrillation
pulmonary edema fatigue
convulsion
Treatments for thyroid storm (I)
Iodine-Lugol solution:
130 mg/ml (30)
Antithyroid drugPTU
-blockers
propranololmetoprolol
(beta1-blocker)
Treatments for thyroid storm (II)
Corticosteroids: 100 mg/q8h
fluid & electrolytedigitalis
thyroid storm
plasmapheresis
thyroid hormone & TSH
(I)
Hypothyroidism is a syndrome resulting
from deficiency of thyroid hormones
Slowing down of all body functions