Week 6: Thyroid and Adrenal Pharmacology

Endocrine System

• Controlled via the pituitary and hypothalamus

o Regulate many body functions via hormones
▪ Unlike the nervous system, hormonal changes may take seconds to days to respond, and results
may last for weeks/months
o Pituitary sends out numerous hormonal messengers
▪ Growth hormone, Adrenocorticotropic hormone, Thyroid stimulating hormone, to name a few

Thyroid Hormones

• TRH, TSH, T3, T4

• T3 (triiodothyronine):
o Most potent thyroid hormone
o Affects body temperature, growth and heart rate
o Four times more potent than T4
o Primarily produced by conversion from T4
• T4 (thyroxine):
o Major hormone secreted from the thyroid
o Converted to T3 by deiodinases
o More abundant than T3 in the body, but less potent

Hypothyroidism

• Cold intolerance
• Weight gain
• Lethargy/somnolence
• Fatigue
• Dry skin/hair
• Due to a lack of adequate T3 and T4 levels

Therapeutic options

• Levothyroxine (Synthroid): L-isomer of thyroxine (T4)

• Armour thyroid (Thyrolar): T3 and T4 synthetic hormones
• Liothyronine (Cytomel): T3 hormone only
• Equivalent dosing:
o 100 mcg (0.1 mg) of levothyroxine = Armour thyroid 65 mg = 25 mcg (0.25 mg) of liothyronine

Hyperthyroidism

• Heat intolerance
• Weight loss despite increased appetite
• Increased activity, sweating, palpitations
• Insomnia and shortened sleep cycles
• Hair loss
• May present with a goiter
• Due to incr. levels of T3 and T4

Therapeutic optics

• Thioamides:
 o Propylthiouracil (PTU) or Methimazole (Tapazole)
o MOA: inhibits peripheral conversion of T4 to T3
▪ Typically utilized for long-term management as both are oral tablets
• Iodines:
o Lugol’s solution or SSKI (Super saturated potassium iodide)
o MOA: inhibits release of thyroid hormone
▪ Typically utilized in preparation for thyroidectomy

Adrenal gland functions

• Adrenal Medulla:
o Secretion of:
▪ Epinephrine
▪ Norepinephrine
• Adrenal Cortex:
o Secretion of:
▪ Adrenocorticosteroids
▪ Aldosterone hormones
▪ Androgenic steroids

Adrenocorticosteroids

• Two types: glucocorticoids & mineralocorticoids

o Glucocorticoid receptors are found throughout the body, whereas mineralo- receptors are found in
excretory organs e.g. colon, kidney and saliva/sweat glands
▪ Given differences in receptors, effects within the body differ greatly
o Cortisol is the primary human glucocorticoid
▪ Synthetic versions also exist
▪ Promotes metabolism, combat stress, and decrease inflammation
o Mineralocorticoids regulate electrolyte concentrations and water volume

Glucocorticoids

• Our bodies typically produce between 7.5-10 mg of prednisone equivalent per day as cortisol
• Typical measuring point is relative to prednisone
o Prednisone (pred) 5 mg =
o Dex 0.75 mg (highest potency)
o Methylpred 4 mg
o Hydrocortisone 20 mg (lowest potency)

Clinical uses

• Glucocorticoids:
o Aerosolized forms are utilized for asthmatics chronically
o Oral forms are utilized for acute asthma/COPD exacerbations, inflammation (muscoskeletal,
respiratory, etc.)
▪ IV forms are utilized for the same reasons as above but for patients who cannot tolerate oral
agents
• Mineralocorticoids:
o Primarily used to regulate electrolytes/water volume in patients with hypotension
▪ Fludrocortisone (Florinef)

Adverse drug events

 • ADRs Inhaled:
o Oral thrush, coughing, hoarseness
• ADRs systemic (oral):
o Short-term:
▪ Hyperglycemia,  BP
o Long-term:
▪ Osteoporosis, cataracts/glaucoma, atherosclerosis, electrolyte imbalances, weight gain

Summary

• For thyroid disorders, the primary modulation is increased/decreased levels of T3/T4/TSH

• For adrenal disorders, the primary modulation is via glucocorticoid/mineralocorticoid pathways