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13 Cards in this Set

  • Front
  • Back
anterior pituitary
Hypothalamic neurons secrete releasing/inhibiting factors into a portal vessel system that carries the factors to the cells of the anterior pituitary via Growth-Hormone Releasing Hormone (GHRH), Somatostatin (SST), and Dopamine (DA).
The pituicytes of the anterior pituitary produce various hormone products:Growth Hormone (GH) and Prolactin (PRL), Thyroid-Stimulating Hormone (TSH), etc
posterior pituitary
Hypothalamic neurons from the Supraoptic Nucleus and the Paraventricular Nucleus project directly into the posterior pituitary

secrete Arginine Vasopressin (ADH) and Oxytocin directly into the bloodstream
Growth Hormone (GH)
large peptide hormone (anterior pituitary)
physiological effects include:
1. Increasing the growth and metabolic activity of all tissue
2. Stimulating protein synthesis in muscle and adipose tissue
3. Stimulating lipolysis in adipose tissue
* often via Insulin-like Growth Factor-1 (aka IGF-1, aka Somatomedin)
*negative feedback.
Mechanism: stimulating the JAK/STAT kinase pathway, while IGF-1 acts mainly by stimulating the MAP kinase pathway.
Prolactin (PRL)
peptide hormone(anterior pituitary)
tonically inhibited by dopamine from the hypothalamus
- to be lifted during pregnancy to increase milk production in breast lobules
Mechanism: activating the JAK/STAT kinase pathway
Arginine Vasopressin (AVP)
posterior pituitary
plasma osmoregulation and BP Regulated by:
1. Serum osmolarity (salt concentration)-osmoreceptors
2. Systemic blood pressure- baroreceptors

Mechanism: G-protein receptors
1. V1 receptors- on vascular smooth muscle. They utilize Gq/Calcium – Protein Kinase C to stimulate vasoconstriction.
2. V2 receptors- renal tubules Use Gs/cAMP – Protein Kinase A to allow for increased renal water resorption. *major action
small peptide hormone (posterior pituitary)
Uterine contractions during labor, infants’ suckling stimulates oxytocin

Oxytocin causes contraction of the uterine myometrium and the myoepithelium of mammary glands
Mechanism: via a G protein- the Gq/Calcium – Protein Kinase C pathway
GH drugs
1. Somatropin (Humatrope)- recombinant human GH
2. Somatrem (Protropin)- recombinant human GH with an extra methionine group added

given 3X weekly via IM or SC injection for dwarfism, Turner’s Syndrome, chronic renal failure
* Normal adults and children- increase muscle mass and reduce adipose tissue
Side Effects- autoimmune anti-GH antibodies

3. Growth Hormone Releasing Hormone (GHRH)- recombinant peptide Sermorelin acetate, or GHRH-29
*no clinical use and is only used for investigation
Somatostatin drugs
Octreotide (Sandostatin)- selective SST2R agonist
45 times more effective than SST at inhibiting GH release

uses: GH secreting tumors (acromegaly)
Side effects: GI distress, gallstones, and hyperglycemia
Given by SC injection 3X/day
Prolactin inhibiting drugs
dopamine (DA) receptor agonists- selective for D2

1. Bromocriptine (Parlodel)- a semi-selective D2 agonist, given orally 2-3X a day
2. Pergolide (Permax)- a cheap, long-lasting D2 agonist, given orally once a day
3. Cabergoline (Dostinex)- newer, more potent, and more selective than the previous two drugs. It shows fewer side effects and is only administered once every 2-3 days.
Uses: hyperprolactinemia by a prolactin-secreting pituitary tumor, pregnancy, or lactation
Side effects: nausea, orthostatic hypotension, and dyskinesia
Oxytocin drugs
Pitocin and Syntocin
Uses: Induce uterine contractions and maintain labor, Control postpartum bleeding, Stimulate milk letdown
Given IV, IM, or as a vaginal suppository during labor- short half-life (1-6 min)
Side effects: uterine hypertonus or rupture at high doses, fetal hypoxia
vasopressin drugs
1. Pitressin- natural 9 amino acid AVP peptide- activity at both V1 and V2 receptors *limited clinical use: temporarily control GI bleeding (vasoconstrictor) given IM and SC with a 10 min half-life
Side effects: skin blanching, abdominal cramps, and hypertension

2. Desmopressin acetate (DDAVP)- a synthetic AVP analogue- selective for V2 receptors
Uses: Diabetes Insipidus, and von Willebrand’s Disease (V2 stimulation of Factor VIII synthesis)
Given orally, IV, SC, or intranasally
Side effects: water retention
Hypothyroidism drugs
underproduction of thyroid hormones- Hashimoto or dietary iodine deficiency, goiter (myxedema in adults), cretinism (infants)

Tx= simple replacement
1. Levothyroxine (Synthroid, L-T4) * drug of choice (body can regulate T3 levels)
2. Liothyroxine (Cytomel, L-T3) *myxedema coma only (severe/acute)
3. Liotrix (Euthroid, Thyrola) - mixture of T4 and T3 ratio (4:1)
4. Thyroid (USP) and Thyroglobulin (Proloid)- extracts of animal thyroid glands- *first used drugs not recommended for use now
Hyperthyroidism drugs
overproduction of thyroid hormones- - Graves’ Disease, goiter, tumor
Treatments include:
1. Blocking iodide uptake at the membrane of follicular epithelial cells- Thiocyanate, Perchlorate * drugs of choice
2. Blocking iodination of tyrosine residues on Tg- Thiourelyenes
2. Blocking coupling of MIT/DIT- Thiourelyenes, Iodide
3. Blocking peripheral conversion of T4 to T3- Propylthiouracil
4. Blocking sympathetic pathways by blocking beta-adrenergic receptors- Propanolol- used for "thyroid storm" Sx
5. Iodide or KI (Lugol’s) solution/tablets- replace deficiency or if radioactive (Iodine-131) used for tumor destruction

Side Effects- esp sythesis blockers- agranulocytosis, aplastic anemia