Exam 4: Endocrine Pharmacology Flashcards
Role of thyroid in infants:
Development of nervous system, growth
Thyroid gland secretes:
T3, T4, calcitonin
Thyroid hormones are made up of:
Two tyrosine molecules, iodinated, joined by ester linkage
More active form of thyroid hormone:
T3
Pathway to thyroid hormones:
Hypothalamus releases TRH → anterior pituitary releases TSH → thyroid secretes T4 > T3 → conversion in periphery
Causes of hyperthyroidism:
Graves’: IgG antibody activates TSH receptor
Toxic multinodular goiter
Iatrogenic (overdose)
Pit tumor, thyroid cancer, testicular cancer (βhCG release)
Examples of thioamides/thioureylenes:
Propylthiouracil
Methimazole (Tapazole)
Indications for thioamides/thioureylenes:
Graves’
Hyperthyroidism
Only useful in overproduction situations
MoA of thioamides/thioureylenes:
Competes with thyroglobulin for iodide and reduces thyroid hormone synthesis
Onset of thioamides/thioureylenes:
1-2 weeks due to thyroid gland stores
A/E of thioamides/thioureylenes:
Goiter d/t ↑ TSH stimulating thyroid hypertrophy Pruritic rash Arthralgias Agranulocytosis Hepatotoxicity Vasculitis/drug-induced lupus
Preferred agent for hyperthyroidism and why:
Methimazole d/t longer half-life, once daily dosing, more potent, less serious A/E
Considerations for PTU:
Inhibits conversion of T4 to T3 in periphery
TID dosing
Preferred in pregnancy and thyroid storm
No IV formulation
A/E of PTU:
Depletes prothrombin so ↑ bleeding time
Additional hyperthyroid therapy beyond thioamides/thioureylenes:
I131 Surgical resection β blockers Corticosteroids Iodide salts (Lugol's)
β blockers for hyperthyroid:
Blocks peripheral conversion of T4 to T3, blocks adrenergic effects
Corticosteroids for hyperthyroid:
Blocks peripheral conversion of T4 to T3, suppresses antibodies and inflammation
Iodide salts for hyperthyroid:
Blocks peripheral conversion of T4 to T3, decreases vascularity of thyroid gland, temporarily blocks TH release due to gland being occupied with iodide uptake
Causes of hypothyroidism:
Hashimoto’s: antibodies against thyroid gland proteins
Thyroid ablation/surgery
Iodine-containing drugs
Pit tumor
PO synthroid:
Synthesized T4
Long half-life (7 days)
Monitor TSH, T4
A/E of synthroid:
Allergic rash
Indications for T3 vs. T4:
Myxedema coma
Drugs that increase levothyroxine metabolism:
Phenobarbital
Phenytoin
Rifampin
Carbamazepine
Drugs that decrease T4 to T3 conversion:
PTU
β blockers
Amiodarone
Glucocorticoids
Drugs that decrease absorption of levothyroxine from the gut:
Cholestyramine FeSO4 Aluminum hydroxide Sucralfate Kayexalate
Drugs that ↑ thyroid binding globulin and bind T4/T3:
Pregnancy
Estrogen
Amiodarone and thyroid status:
Structurally resembles TH, can make hypo or hyperthyroid
Lithium and thyroid status:
Actively concentrates in thyroid gland and can inhibit TH synthesis → hypothyroid
Reglan and thyroid status:
↑ TSH production/release