CH 61 Drugs for Thyroid Disorders Flashcards
Drug: Levothyroxine (Synthroid)
Class: Synthetic thyroid hormone (T4)
MOA: Replaces endogenous thyroxine (T4), which is converted to triiodothyronine (T3); regulates metabolism, growth, and development.
Dosing:
* Adults: 1.6mcg/kg/day; increase by 25mcg/day every 4-6weeks until TSH in normal range
* 60+ years: 1.1mcg/kg/day (2/3 of that needed in younger adult)
Note:
* Different brands are not considered interchangeable due to variable bioavailability
Drug: Armour Thyroid
Class: Natural thyroid hormone (T3/T4 combination)
MOA: Provides both T3 and T4 derived from porcine thyroid glands; mimics endogenous thyroid hormone effects.
Note:
* Has a strong, characteristic odor due to its animal origin.
* Prescribed in grains
Drug: Methimazole (MMI)
Class: Thioamide antithyroid agent
MOA: Inhibits thyroid peroxidase, preventing synthesis of new thyroid hormones by blocking iodination of tyrosine residues.
AE:
* agranulocytosis
* teratogenicity
Note: First-line therapy for hyperthyroidism
Drug: Propylthiouracil (PTU)
Class: Thioamide antithyroid agent
MOA: Inhibits thyroid hormone synthesis and also blocks peripheral conversion of T4 to T3.
AE:
* liver injury
* agranulocytosis
Note: Preferred during the first trimester of pregnancy due to lower teratogenic risk
Drug: Radioactive Iodine (¹³¹I)
Class: Radiopharmaceutical
MOA: Selectively taken up by the thyroid and destroys thyroid tissue via beta-emission.
Note: Contraindicated in pregnancy (Category X); does not emit systemic radiation.
Drug: Propranolol
Class: Non-selective beta-adrenergic blocker
MOA: Reduces sympathetic symptoms of hyperthyroidism and may inhibit peripheral conversion of T4 to T3.
Note: Used in thyroid storm for both symptom control and hormone suppression.
Drug: Iodides (e.g., Lugol’s solution, potassium iodide)
Class: Iodine preparation
MOA: Inhibits the release of preformed thyroid hormone from the gland and decreases vascularity of the thyroid.
Note: Given after a thioamide in thyroid storm to prevent release of stored hormone.
Function of thyroid hormone
- Regulates metabolism
- Affects growth & development
- Controls energy, body temp, heart rate
- Essential for brain development
Hypothalamic-pituitary-thyroid feedback loop
- Hypothalamus → TRH → Anterior Pituitary → TSH
- TSH stimulates thyroid to release T3 & T4
- High T3 & T4 inhibit TRH and TSH release
Signs of hyperthyroidism
- Weight loss
- heat intolerance
- Increased heart rate
- tremors
- Anxiety
- bulging eyes (exophthalmos)
- Goiter
Signs of hypothyroidism
- Weight gain
- cold intolerance
- Fatigue
- constipation
- Dry skin
- slow heart rate
- Coarse skin
- slow reflexes
Triiodothyronine (T3)
- the active thyroid hormone
- more potent thyroid hormone replacement therapy
- shorter half-life
Synthetic (T3): Liothyronine
Thyroxine (T4)
- the precursor to triiodothyronine (T3)
- more common; preferred thyroid hormone replacement therapy
- stable half-life
Synthetic (T4): Levothyroxine
overt primary HYPERthyroidism
TSH: ↓↓ | Total T4: ↑↑ | Free T4: ↑↑ | Total T3: ↑↑
Causes: Graves’ Disease, toxic multinodular goiter, toxic adenoma, thyroditis (virual, postpartum), drugs, hyperemesis gravidarum, gestational throphoblastic disease, excess thryoxine ingestion
sublclinical primary HYPERthyroidism
TSH: ↓ or ↓↓ | Total T4: NL | Free T4: NL | Total T3: NL
Causes: Recent treatement for hyperthyroidism, steroids, dopamine, non-thyroid illness
overt primary HYPOthyroidism
TSH: ↑↑ | Total T4: ↓↓ | Free T4: ↓↓ | Total T3: ↓↓
Causes: Hashimoto’s thyroiditis, thyroidectomy, post-radioiodine therapy, amyloidosis, neck irradiation
subclinical primary HYPOthyroidism
TSH: ↑ or ↑↑ | Total T4: NL | Free T4: NL | Total T3: NL
Causes: Poor compliance with thyroxine, drugs (amiodarone), assay difficulties; non-thyroid illness (including acute psychiatric disorders)
central (secondary) HYPERthyroidism
TSH: ↑↑ | Total T4: ↑↑ | Free T4: ↑↑ | Total T3: ↑↑
Causes: TSH-secreting pititary adenoma, hypothalamic dysfunction
central (secondary) HYPOthyroidism
TSH: ↓↓ | Total T4: ↓↓ | Free T4: ↓↓ | Total T3: ↓↓
Causes: Pituitary dysfunction, non-thyroid illness, assay difficulties, hypothalamic dysfunction
Drugs that decrease levothyroxine absorption
- histamine blockers
- proton pump inhibitors (PPI)
- sucralfate
- cholestyramine
- antacids (aluminum-containing)
- iron supplements
- magnesium salts
Drugs that increase levothyroxine metabolism
These drugs would require an increased levothyroxine dose
* phenytoin
* carbamazepine
* rifampin
* sertraline
* phenobarbital
Drugs needing monitoring with levothyroxine
- warfarin - ↑INR; ↓ warfarin dose
- insulin - ↑ insulin dose
- digoxin
- corticosteroids
Changes in thyroid dosing during pregnancy
- thyroid binding globulin (TBG) increases throughout pregnancy
- ↑TBG = ↓ free T4
- Increase levothyroxin (Synthroid) by 50% during pregnancy
- Return to pre-pregnancy levels following delivery
Thyroid Storm treatment
- propylthiouracil (PTU) OR methimazole (Tapazole) - direct antithyroid (prevent synthesis of new T3/T4)
- Lugol’s solution OR sodium iodide - prevent stored T3/T4 from being secreted
- propranolol - will decrease thyroid hormone production
- hydrocortisone - will decrese inflammatory processes
Avoid aspirin