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MedChem 2
lecture 2 GH
32
Medical
Graduate
11/30/2008

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Term
GH stimulates:
(somatomedin)
Definition
liver-glucogenesis & IGF (somatomedins)bone
adipose lypolysis (hyerglycemia
muscle- AA uptake and protein syntheis
Term
IGF-1
Definition
Somatomedins: produced in the liver and mediate growth. and have neg feedback on GHRH
Term
GH has a direct relationship with:
Definition
thyroid hormones
Term
GH acts directly on hepatocytes to:
Definition
stimulate gluconeogenesis
Term
cAMP phosphorylation of GH causes:
Definition
GH synthesis and increases Ca++ influx (which helps release GH out of the cell)
Term
Factors increasing Growth Hormone Secretion
Definition
Increase: Sleep, thyroid Hormones, estrogens or androgens (puberty), amino acids
Term
Factors decreasing Growth Hormone Secretion
Definition
Decrease: Corticosteroids (suppress growth), Hypothyroidism, Aging
Term
Growth hormone excess in adults:
Definition
Acromegaly- Connective tissue proliferation; dermal overgrowth; enlarged extremities; skull deformities; insulin resistance
Term
low levels of GH in children cause:
Definition
Children (Dwarfism): Decreased growth velocity and skeletal development, delayed puberty less muscle and more SQ fat exces
Term
IGF-1 deficiency:
Definition
Short stature (more common than GH deficiency)
Igf is needed as a mediator to stimulate growth but not lipoysis
Term
GH recombinant DNA Theraputic agents
Definition
Somatotropin (Serostim, Genotropin) : pituitary dwarfism; short stature (children); GH-deficient adults
Term
Synthetic GHRH
Definition
sermorelin
Use: increase GH to treat dwarfism, short stature)
decreased efficacy and cost vs. GH
Term
Recombinant IGF-1
Definition
somatomdin
Use: ↑ growth in children with GH insensitivity & low IGF-1 levels (stimulate growth in children) (GH resistance)
Term
Dopamine and GH agonists
Definition
Bromocriptine, pergolide, cabergoline,sermorelin
Use: decrease GH secretion in acromegaly
MOA: inhibit GH
“you need more Bros Per Cab”
Term
Somatostatin analog
Definition

Sandostatin (Octreotide) Use: decrease GH in acromegaly

Pegvisomant

“eight men will stop you”

Term
Dopamine and GH receptor antagonists:
Definition
Octreotide (Sandostatin) and pegvisomant
Dopamine antagonist- Domperidone“eight men will stop you”
Term
Side effects of GH analog
Definition
increased glucose (hyperglycermia) diabetes type 2 (insulin resistance)
Bone deformation
Tumor genesis
Term
prolactin function:
Definition
lactation/ milk secretion
-dopamine must be inhibited
Term
prolactin is inhibited by:
Definition
dopamine
Term
Hyperprolactinemia symptoms:
Definition
Cause: pituitary Tumor
Symptoms: gynecomastia, galactorrhea, male hypogonadism, amenorrhea
Term
Dopamine agonist
Definition
bromocriptine (Parlodel)
Use - hyperprolactinemia
MOA: 1 D1 stimulates dopamine
2 D2 is a TRH inhibitor
Side effects: postural hypotension
Term
Dopamine(D2)receptor antagonist
Definition
Domperidone
Use: stimulates lactation
MOA: ↑ prolactin → ↑ milk production
Term
Oxytocin actions:
Definition
Milk ejection, uterine contractions, abortion
Term
Synthetic oxytocin use and contraindications
Definition
Oxytocin citrate
Uses: induce or support labor, stimulate milk ejection, induce abortion
Side effects: uterine rupture
Contraindications: Abnormal fetal position; previous uterine surgery(weakened uterine muscles); fetal distress
Term
Vasopressin (ADH) Actions:
Definition
V1 receptor binding- vasoconstriction
V2 receptor binding-opens H2O channels
Term
ADH secretion increased by:
Definition
high plasma osmolality
decreased blood volume
Term
ADH secretion decreased by:
Definition
ethanol, cold, low blood somolarity and high blood volume
Term
Disorders of ADH Secretion- Diabetes insipidus symptoms:
Definition
decreased ADH secretion (Diabetes increases diuretic effect) Symptoms - polyuria, polydipsia, dehydration Treatment – ADH Nephrogenic diabetes insipidus tissue insensitivity to ADH Higher doses of ADH for treatment
Term
Diabetes insipidus bedwetting treatments:
Definition
1 Natural vasopressin (pitressin) – injection V1 and V2
Vasopressin tannate - longer acting
Lysine vasopressin
Desmopressin acetate – only V2 activity
tablets and nasal spray with prolonged effect
Term
ADH treatment side effects:
Definition
hyponatremia, water intoxication, uterine cramping
Term
ADH V1 versus V2 treatment:
Definition
WE prefer to treat desompressin nasal spray because it does not cause vasoconstriction
Term
other ADH response modifier drugs:
Definition
Chlorpropamide - ­ responsiveness to ADH
Carbamazepine - ­ responsiveness to ADH
Clofibrate - ­ ADH release
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