33 - endocrine Flashcards
the endocrine system is made of the _ and _
plus thyroid gland, parathyroid glands, adrenal glands, pancreas, ovaries, testicles
what about skeletal muscle and fat?
hypothalamus and pituitary glands (antieror/posterio)
skeletal muscle - should be considered because muscles secrete things that cause physio change
Hormones of the Anterior Pituitary Gland
_ _ and _ are important for pharm intervention
Others: either very rare usage or better ways accomplish things.
FSH, LH, and GH
TSH, ACTH, Prolactin, MSH - not important pharm wise
GH from anterior pituitary
causes liver to release _, leading to growth of cartliage and bone, and protein synthesis growth in muscle and other organs
what does it do to adipose tissue
most tissues?
insulin-like growth factor 1
adipose - lipolysis, release of fatty acids
most tissues - decreased glucose utilization
Hypothalamus secretes _ and _ , positive and
negative effectors, respectively, of
growth hormone (GH) release by the
anterior pituitary
Growth
hormone releasing hormone (GHRH)
and somatostatin (SST),
_ is a negative regulator of
GHRH secretion.
_, produced in the liver in response to GH, is a negative regulator of GH release by the pituitary and a positive regulator of SST release by the hypothalamus.
GH regs GHRH from hyothalamus
Insulin-like
growth factor 1 (IGF-1) - from liver has positive efffect on somatostatin and negative effect on GH
_ is a peptide hormone released by the stomach in response to hunger
Ghrelin
positive effect on GH
A receptor with associated JAK kinase (as well as
Src kinase) activity mediates the effects of _ hormone
when binds to receptor dimerization and
transphosphorylation occurs
growth hormone
Growth Hormone Therapeutics
Treatment in children with short stature
Treatment of severe catabolic states ( e.g. AIDS)
Anti-aging (benefits controversial)
GH antagonists used to treat _ (too much GH produced)
antagonists used to tx acromegaly
GH has receptor with associated JAK kinase
_ and _ Receptors are G protein coupled
receptors linked to Gαs
FSH and LH
Human Chorionic Gonadotropin-hCG - considered with these two guys (from placenta)
FSH in women and men
women - ovarian follicle development, and ovarian steroidogeneis (LH too)
men - spermatogensis
Follicular stage of menstrual cycle
_ hormone - androgen production
_ hormone - conversion of androgens to estrogens
LH - androgen production
FSH - conversion androgen to estrogens
Luteal stage of menstrual cycle
_ hormonse - Estrogen and progesterone production
LH
hCG
(human chorionic gondadotropin) If pregnancy occurs
the _ is stimulated by LH (or hCG) to produce progesterone and estrogen - required to maintain pregnancy
corpus luteum
LH in males
testosterone production
FSH, LH, hCG therapeutics
Used to induce _ that is secondary to
hypogonadotropic hypogonadism,
Polycystic ovary syndrome, obesity, others
Used to treat male _ in cases not treatable
with androgen alone
ovulation
Complex protocols, requires close monitoring.
Expensive. (use reserved for cases not
treatable with simpler , cheaper alternatives)
—
used to tx male infertility
Hormones of the posterior Pituitary: _ and _
Small peptides synthesized in hypothalamic neurons. Transported down
axon to pituitary, where they are stored and released.
Oxytocin - uterine muscles and mammary glands
and Vasopressin (aka antidiuretic Hormone, ADH) - kidney tubules and vasoconstriction
vassopress/ADH from posterior pituitary
stimulated by angiotensin II, sympathetic stimulation, hyperosomolarity, hypovolemia, hypotension
has 2 receptors and wwhat do they do
V1 - vasoconstriction, increase BP - G protein coupled
receptors on vascular
smooth muscle that
mediate vasoconstriction
V2 - G protein coupled receptors on
kidney tubules that mediate water
retention - renal fluid reabsorption - increased blood volume - increased BP
Clinical Uses of Vasopressin/ADH
Treatment of diabetes insipidous - if defect in ADH just replace it with the drug
Treatment of certain types of bleeding problems
Treatment of nocturnal enuresis (bed wetting)
_ Antagonists
Used to treat hyponatremia (Low Na+ concentration in the blood) Very, Very complex. Perhaps counter-intuitive Limit water retention (Yea, Na+ less dilute). But what about diminishing increased Na+ retention by vasopressin???
Vasopressin
Used to treat low sodium in the blood
Limit water retention
Making Na more concentrated in blood
Also diminished increased sodium retention by vasopressin
_ hormone
Works through G protein coupled receptor (Gαq)
Induces contraction of uterine smooth muscle (Receptor
numbers go up during second half of pregnancy)
Elicits milk ejection in lactating women
oxytocin
AKA the love hormone because of its role in sexual arousal
Oxytocin Physiology
_ dose: increase frequency and force of contractions
_ dose: sustained contractions
Lower dose: increase frequency and force of contractions
Higher dose: sustained contractions
Oxytocin therapeutics
_: If early vaginal delivery required or labor problems
Atosiban: antagonist (of both vasopressin and oxytocin). Used
to halt premature labor.
Induce labor
Increasing metabolism and burning ATP and producing heat
Hyper - too hot
Hypo - cold
thyroid hormone
calorogenic effect - influences tolerance to cold, availability of ATP
increase glc metabolism
increase lipid metabolism
_ deficiency is worlds’ leading cause of goiter
Thyroid gets bigger to try to make more
Tx not usually necessary - often no symptoms
Iodine deficiency is the world’s leading cause of goiter - but this is
rare in North America
usually by autoimmune disease in developed countries
what is a goiter
Enlargement of the Thyroid Gland
T3 or T4
dominant in plasma ?
more active?
T4 in plasma
T3 more active
hyper/hypo thyroidism?
hair thinning, big tongue, dry skin, cold skin, cold intolerance, slow reflexes,
hypothyroidism
not enough thyroid hormone
hyper/hypo thyroidism?
intolerance to heat, fine straight hair, bulging eyes, facial flushing, enlarged thyroid, tachycardia, giner clubbing, muscle wasting, weight loss
hyperthyroidism
too much
Treatment of Hyperthyroidism
_ – Block hormone synthesis
_ – Block I- transport into thyroid
high concentrations of _ inhibit
transport and inhibit hormone biosynthesis)
Thioamides - block hormone synthesis
Anion inhibitors - block iodide transport into thyroid - NIS transporter Na/I symporter) allows thyroid to accumulate
iodide
Iodide - high concentrations inhibit synthesis
treatment of hyperthyroidism
_ prevent hormone synthesis by inhibiting the thyroid peroxidase-catalyzed rxns and blocking iodine organification
block coupling of the iodotyrosines
since synthesis of hormones is affected, their effect requires 4 weeks
thioamides
