Thyroid Drugs Flashcards
What are the steps of thyroid hormone synthesis?
- Uptake of iodine
- Iodine organification: oxidized by peroxidase, and iodinates tyrosine
- Coupling of MIT & DIT
- Secretion of thyroid hormones
- Conversion of T4 to T3 (periphreal conversion)
What is biologically available for tissue use?
Free thyroid hormone (T3); rest are bound.
What are the differences of T3 and T4?
- T4: Combination of two DIT molecules, less potent, 75% protein bound, converted to T3 in periphreal tissues, liver, and kidney. 0.04% free form.
- T3: One MIT and one DIT molecule, more potent, 25% bound, binds actively to nuclear receptor. 0.4% free form.
What is a lack of thyroid hormone in fetal life known as?
Cretinism.
What are symptoms of hypothyroidism?
Fatigue, cold intolerance, weight gain despite lack of appetite, irregular menses, non-pitting edema, high cholestrol.
Etiology: Hashimoto’s, drugs or radiation exposure, or pituitary tumor
What treats hypothyroidism?
Levothyroxine; consistent potency with long duration , in emergencies Liothyronine sodium.
This also prevents mental retardations in infants with thyroid deficiency
What are some ADR of Levothyroxine (T4)?
Tachycardia, heat intolerance, and tremors
What are indications and ADRs of Liothyronine Sodium (T3)?
Myexdema coma (medical emergency with hypothermia, respiratory depression, and loss of conciousness)
ADR: More cardiotoxic than Levothyroxine, do not use in patients with heart disease.
What are symptoms of hyperthyroidism?
Excitability, intolerance to heat, excessive sweating, mild to extreme weight loss, muscle weakness, extreme fatigue with inability to sleep, EXOPTHALMUS,
View table on Slide 19
Has a star dawg
What are thioamidines, and MOA?
Propothyiouracil (PTU), Methimazole, Carbimazole; treat hyperthyroidism.
MOA: Inhibit peroxidase enzyme preventing iodination and coupling, which inhibits synthesis of thyroid hormones
What are some ADRs of thioamidines?
Urtictrical papular rash and agranulocytosis.
What are some ADRs of Methimazole itself?
Cholestatic dysfunction, teratogenic but used in 2nd or 3rd trimester to avoid PTU liver toxicity
What are some ADRs of PTU itself?
Liver failure, not used in children unless Methimazole allergy, teratogenic as well but preferred in 1st trimester due to excessive protein binding
What are some uses of thioamidines?
- Graves disease
- Conjunction with radioactive iodine
- Preop preperation of the thyroid gland
- Thyrotoxic crisis