THERAPY OF THYROID GLAND

DYSFUNCTION

Full Professor Isidora Samojlik

MEDICINE
Winter semester 2021/22
 Regulation of thyroid hormone production
mental state
THR – (Thyreotropin cold
Releasing Hormon) circadian rhythm
“stress"

TSH – thyreotropin
(thyroid stimulating
hormone)

SST – somatostatin
Synthesis & Transport of Thyroid Hormones,
Sites of action of some antithyroid drugs
 Key features of thyrotoxicosis and hypothyroidism
Thyrotoxicosis T4, T3
Warm, moist skin
Sweating, heat intolerance
Tachycardia, increased cardiac
output, pulse and pressure
Dyspnea
Increased appetite
Nervousness, hyperkinesia, tremor
Exophthalmos (Graves' disease)
Weakness, increased deep tendon
reflexes
Menstrual irregularity, decreased
fertility
Weight loss
Hypothyroidism T4, T3
Pale, cool, puffy skin
Sensation of being cold
Bradycardia, decreased cardiac
output, and pulse pressure
Reduced appetite
Lethargy, general slowing of mental
processes
Stiffness, decreased deep tendon
reflexes
Infertility, decreased libido,
impotence, oligospermia
Weight gain
 THERAPEUTIC APPROACH IN
HYPOTHYROIDISM
• PHARMACOLOGICAL - replacement therapy
• LEVOTHYROXINE (T4; L-thyroxine sodium)
• natural origin, synthetic
• pharmacokinetics:
– per os, bioavailability 80%
– t0.5 7 days, 1x/day
• metabolized in the liver as an endogenous T4 (conjugated with
sulfuric acid and excreted in bile)
• LIOTHYRONINE sodium (T3)
– t0.5 1.5 day; ADRs of CVS are more common than in T4
• ADRs: palpitation-tachycardia, angina, tremor, sweating, loss of
weight and muscle weakness (thyrotoxicosis), allergic reactions,
headache, …
 THERAPEUTIC APPROACH IN
HYPERTHYROIDISM
• NON-PHARMACOLOGICAL - Surgical removal of
thyroid tissue

• PHARMACOLOGICAL – drugs used to inhibit the

functional activity of hyper secretive thyroid gland.
• Antithyroid agents:
– Drugs that inhibit hormone synthesis
– Agents which inhibit Iodine trapping
– Agents which inhibit hormone release
– Agents which destroy thyroid gland tissue
 Agents which inhibit hormone synthesis
THIOAMIDES
• Propyl-thiouracil
• Methimazole (10x more potent; crosses FPB!)

• They bind to thyroid peroxidase and prevent the oxidation

of iodide and iodotyrosyl residue, which subsequently
inhibits the formation of tyrosine residue in thyroglobulin
and their coupling to T3 and T4.
 THIOAMIDES
• Pharmacokinetics:
• p.o. application, good absorption from gut
• short t0.5, but concentrating in the thyroid gland allows the use
of maintenance dose 1x/day
• metabolized in liver, excreted via kidneys
• ADRs:
• agranulocytosis, (sudden, within 3 months from the beginning
of th. is manifested by slow wound healing, oral mucosal
ulceration, mouth infections); transient leucopenia,
thrombocytopenia
• arthralgia, fever, vasculitis, SLE
• GIT (nausea)
• hepatic damage
 Agents which inhibit iodine trapping

Monovalent anions:
• Thiocyanates
• Perchlorates

• They block uptake of iodine by the gland through

competative inhibition of iodine transport mechanism.

• Requires higher dose which can cause ADR - aplastic

anaemia!
 Agents which inhibit hormone release
IODINE
• Lugol’s solution: 5% iodine in 10%KI
• Colloid iodine: 10% solution
• Sodium and potassium iodide; organic iodide

• They inhibit iodine organification and hormone release.

• They also decrease the size and vascularity of glad (used
preoperatively before thyroidectomy).

ADRs: allergic reactions!!!

• angioedema, fever, arthralgia, lymphadenopathy,
• swelling of the salivary glands, increased salivation
• “iodism" - metallic taste, burning of mouth and throat,
gingival pain
• swelling of lips, eyelids
 Agents which destroy thyroid gland tissue

Radioisotope of iodine - I131

• It emits gamma and beta radiations; available as sodium

solution.
• It is concentrated by thyroid, incorporated into the storage
follicles where destroy some tissue and produce fibrosis.

• ADR – hypothyroidism!
• CONTRAINDICATION - pregnancy
 THANK YOU!

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