L34- Thyroid and Antithyroid Drugs (hyperthyroid) Flashcards
describe the management hierarchy for hyperthyroidism
1) pharmacotherapy
2) radioactive iodine (RAI) destruction of thyroid
3) surgical thyroidectomy
list the pharmacological agents for hyperthyroidism
- thioamides
- iodides
- β-blockers
- glucocorticoids
- bile acid sequestrants
Thioamides:
- (1) agents
- (2) MOA
1- methimazole, PTU (propylthiouracil)
2- inhibits thyroid peroxidase enzyme –> prevents iodide oxidation to iodine (+ –> interferes with iodination of tyrosyl groups on thyroglobulin –> inhibits coupling of iodotyrosyl residues –> inhibits TH formation)
Thioamide:
- (1) is preferred agent because of (2) and except for in (3) situations
- (3) drug has (4) as additional MOA
1- methimazole > propylthiouracil (PTU)
2- less toxic (liver injury), longer 1/2 life and duration (once daily)
3- (PTU) severe hyperthyroid, thyroid storms, 1st trimester
4- inhibits peripheral deiodination (T4 –> T3)
list the therapeutic uses of Thioamides
- definitive Tx for hyperthyroidism
- conjunction w/ radioative iodine (quickens recovery)
- control hyperthyroid in preparation for surgery
describe the role and regimen of iodides for hyperthyroidism
Iodides inhibit hormone release via thyroglobulin proteolysis inhibition and transient iodine organification inhibition
-NOT used alone b/c thyroid escapes iodide block in 2-8wks
list the clinical applications of iodides
- Thyroid Storm: rapid improvement of Sxs
- preop for surgery –> dec thyroid size, vascularity of hyperplastic thyroids
- radiation emergencies involving release of radioactive iodine isotropes
iodides AEs
(uncommon)
-precipitates hyperthyroidism (Jod-Basedow phenomenon) or hypothyroidism (no escape from Wolff-Chaikoff)
- delays onset of thioamide therapy – prevents use of radioactive iodine therapy for several weeks
- fetal goiter if used in pregnancy
describe the use of β-blockers in hyperthyroidism
- alleviate the SNS / catecholamine Sxs precipitated by TH inc sensitivity to SNS
- Propanolol inhibits T4 –> T3
- CCBs to control tachycardia if β-blockers are contraindicated
describe the use of glucocorticoids in hyperthyroidism
- inhibits peripheral T4 –> T3
- promotes vasomotor stability
- treats possible associated adrenal insufficiency Sxs
Manages Grave’s ophthalmopathy and dermopathy
describe the use of bile acid sequestrants in hyperthyroidism
binds to TH metabolites to inhibit enterohepatic cycling of TH
_____ is generally the preferred hyperthyroidism Tx
RAI- radioactive iodine (I-131)
-destroy thyroid parenchyma
list RAI AEs
- hypothyroidism
- radiation thyroiditis
- exacerbates Grave’s ophthalmopathy
-destroys fetal thyroid in pregnancy
Thyroid storms are triggered by….
infection trauma surgery physical illness severe emotional distress
thyroid storm management
- supportive therapy
- treat underlying disease process / trigger
-PTU (propylthiouracil), iodides, propanolol, corticosteroids, bile acid seqesterants