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Endocrine
N/A
124
Pharmacology
Professional
04/27/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
goals of pharmacotherapy in endocrinology
Definition
-replacement for hormone deficiency states
-antagonists for diseases that result in excess production
-diagnostic tools for identification of endocrine abnormalities
Term
TSH
Definition
thyroid stimulating hormone
thyrotropin
released by anterior pituitary
Term
TRH
Definition
thyrotropin releasing hormone
released by hypothalamus
Term
FSH
Definition
follicle stimulating hormone
released by anterior pituitary
Term
GnRH
Definition
gonadotropin releasing hormone
released by hypothalamus
Term
LH
Definition
leutenizing hormone
released by anterior pituitary
Term
ACTH
Definition
adrenocorticotropic hormone
released by anterior pituitary
Term
CRH
Definition
corticotropin releasing hormone
released by hypothalamus
Term
release of TRH causes release of ___
Definition
TSH
Term
release of GnRH causes release of...
Definition
LH and FSH
Term
release of CRH causes release of...
Definition
ACTH
Term
GH
Definition
growth hormone
released by anterior pituitary
Term
GHRH
Definition
growth hormone releasing hormone
released by hypothalamus
Term
SST
Definition
somatostatin
released by hypothalamus
Term
GH is released when _______ is released.
Definition
GHRH
Term
GH stops being released when _____ is released.
Definition
SST (somatostatin)
Term
prolactin
Definition
released by pituitary
Term
Prolactin is inhibited by ________.
Definition
dopamine
Term
What is an absolue requirement in childhood and early adulthood for normal adult size and is involved in lipid metabolism and lean body mass?
Definition
somatostatin
Term
sermorelin
Definition
shortened analog of GHRH with full biological activity

does not work if GH deficiency is secondary to anterior pituitary defect

cheaper than GH, but may not be as effective
Term
side effects of GH and sermorelin
Definition
very few in children (scoliosis, rarely intracranial HTN)

more in adults (peripheral edema, myalgias, arthralgias, carpal tunnel)
Term
GH contraindication
Definition
malignancy

(although no definitive link to increase in cancer risk)
Term
For children with GH deficiency, the supplemented GH dose is ____________ than adults.
Definition
5-10 times higher
Term
excess GH before end of puberty
Definition
gigantism
Term
excess GH after end of puberty
Definition
acromegaly
Term
cause of excess GH
Definition
hypersecretion of GH by pituitary tumor
Term
definitive treatment for excess GH
Definition
surgical removal of pituitary tumor
Term
pharmacologic treatment of excess GH
Definition
GHRH antagonists (somatostatin analog--octreotide)

D2 receptor agonist--bromocriptine
Term
octreotide use
Definition
treatment of acromegaly as well as other hormone secreting tumors
Term
side effects of octreotide
Definition
GI problems
gall stones
bradycardia
conduction disturbances
vitamin B12 deficiency
Term
How does prolactin exerts a negative feedback control?
Definition
enhances dopamine synthesis in the hypothalamus which acts on the D2 receptors in the pituitary and stops production of more prolactin
Term
release of prolactin is stimulated by...
Definition
TRH
oxytocin
5-HT
suckling
Term
After birth, what hormones stimulate milk synthesis?
Definition
prolactin
insulin
cortisol
Term
During the nursing period, what hormones maintain milk secretion?
Definition
prolactin
oxytocin
Term
causes of hyperprolactinemia
Definition
-hypothalamic or pituitary disease that interferes with dopamine
-renal failure
-primary hypothyroidism (increased TRH)
-pituitary adenoma
Term
effects of hyperprolactinemia
Definition
galactorrhea in women

negative feedback of the H-P-G axis
-amenorrhea and infertility in women
-loss of libido and infertility in men
Term
prototype agent used to treat hyperprolactinemia
Definition
bromocriptine (D2 receptor agonist)
Term
side effects of bromocriptine
Definition
headache, nausea, vomiting, orthostatic hypotension, psychiatric problems
Term
What drugs can cause hyperprolactinemia?
Definition
anti-psychotics that act on D2 receptors
(chlopromazine, haloperidol, resperidone)
Term
D2 receptor agonists are discontinued in what population due to CV toxicity risk?
Definition
post-partum women who do not want to nurse
Term
oxytocin mechanism of action
Definition
direct contraction of uterine muscle via increase in Ca2+

increased production of prostaglandins and leukotrienes
Term
two primary physiological actions of oxytocin
Definition
stimulation of frequency and force of uterine contractions during labor

milk ejection: contraction of myoepithelium that surrounds areolar channels in breast
Term
oxytocin therapeutic uses
Definition
induction of labor
augmentation of labor
reduction of bleeding postpartum
Term
oxytocin diagnostic use
Definition
challenge test to determine fetal heart rate
Term
oxytocin half life
Definition
short
3-5 min
Term
Oxytocin is eliminated by...
Definition
liver and kidney
Term
Explain the concentration dependent effect of oxytocin.
Definition
Low dose increases force and frequency of contractions.
High dose causes a sustained contraction.
Term
oxytocin contraindications
Definition
fetal distress
prematurity
abnormal fetal presentation
any predisposition for uterine rupture
Term
What happens if the oxytocin dose is too high or the patient has an exaggerated response to a typical dose?
Definition
excessive uterine contraction
Term
High dose of oxytocin stimulates...
Definition
vasopressin receptors
Term
What results from a high dose of oxytocin as a result of vasopressin receptor stimulation?
Definition
water intoxication
hyponatremia
Term
oxytocin is released by...
Definition
posterior pituitary
Term
vasopressin (ADH) is released by...
Definition
posterior pituitary
Term
What causes the release of vasopressin (ADH)?
Definition
hyperosmolality
hypovolemia/hypotension
Term
primary site of action for vasopressin (ADH)
Definition
V2 receptors in renal collecting duct
Term
vasoconstrictor receptor subtype found in the heart and vascular smooth muscle that acts as a vasopressin receptor
Definition
V1a
Term
receptor subtype that releases ACTH from anterior pituitary and vasopressin (ADH) from posterior pituitary
Definition
V1b
Term
drugs that enhance vasopressin's anti-diuretic response
Definition
chloropropramide
carbamazepine
NSAIDs, especially indomethacin
Term
diabetes insipidus (DI)
Definition
impaired renal conservation of water

large volume of urine
thirst, polydipsia
Term
2 types of DI
Definition
neurogenic: inadequate secretion of ADH

nephrogenic: inadequate renal response to ADH
Term
causes of neurogenic DI
Definition
head injury
pituitary tumors
infections
genetics
Term
treatment for neurogenic DI
Definition
replacement therapy (desmopressin)
Term
Why is desmopressin preferred to vasopressin in the treatment of neurogenic DI?
Definition
3000x more selective at V2 than V1 receptors
Term
What distinguishes between neurogenic and nephrogenic DI?
Definition
response to desmopressin
Term
causes of nephrogenic DI
Definition
genetics
drug-related
Term
What drugs can cause nephrogenic DI?
Definition
lithium (33% of patients)
demeclocycline
Term
treatment of nephrogenic DI
Definition
adequate water intake
amiloride for lithium-induced
thiazide diuretics
Term
syndrome of inappropriate secretion of ADH (SIADH)
Definition
too much secretion
water intoxication, hyponatremia, hypoosmolality

fatigue and lethargy--convulsions and death
Term
treatment of SIADH
Definition
demeclocycline
loop diuretics
water restriction
Term
What is demeclocycline used to treat SIADH instead of lithium?
Definition
lithium has a low therapeutic efficacy and is more toxic
Term
What happens if vasopressin is given PO?
Definition
completely inactivated
Term
drug of choice for V1 receptor mediated therapeutic applications
Definition
vasopressin
Term
drug of choice for bleeding esophageal varices (vasoconstriction of splanchnic arterial vessels to the portal system)
Definition
vasopressin
Term
vasopressin half life
Definition
short
15 min
Term
Vasopressin is given IV/IM for esophageal varices.
Definition
IV
Term
Why must large doses of PO and intranasal desmopressin be given?
Definition
low bioavailability
Term
desmopressin half life
Definition
2 hours
Term
drug of choice for anti-diuretic related disorders
Definition
desmopressin
Term
drug of choice for neurogenic DI
Definition
desmopressin
Term
drug of choice for type I von Willebrand's disease
Definition
desmopressin

will increase the factor and shorten bleeding time
Term
sex steroid critical for development of fetal male genital tract
Definition
testosterone
Term
sex steroids cricial for growth and development during puberty
Definition
testosterone and estrogen
Term
sex steroids critical for reproduction
Definition
estrogen, testosterone, and progesterone
Term
GnRH stimulates the release of ____ and _____, which in turn stimulate _____ _________ production and release at the level of the gonad.
Definition
FSH; LH
sex steroid
Term
areas of hypothalamus that produce GnRH
Definition
arcuate nuclei
preoptic acrea
Term
What hormone is responsible for stimulation of immature follicle and estrogen synthesis?
Definition
FSH
Term
What hormone(s) surge at ovulation?
Definition
FSH and LH
Term
What secretes progesterone for implantation?
Definition
corpus luteum
Term
What directs progesterone and estrogen production if implantation occurs?
Definition
human chorionic gonadotropin (hCG)

hCG is very similar to LH
Term
What drives progesterone and estrogen production if implantation does not occur?
Definition
LH (luteal phase)
Term
LH acts on _______ cells in the ovaries.
Definition
theca
Term
FSH acts on ________ cells in the ovaries.
Definition
granulosa
Term
LH acts on ______ cells in the testes to release ________.
Definition
Leydig; testosterone
Term
FSH acts on _______ cells in the testes to release _________.
Definition
sertoli; growth factors
Term
GnRH release is increased by...
Definition
norepinephrine and pheromones
Term
GnRH release is inhibited by...
Definition
dopamine, endorphins, and stress
Term
H-P-G axis has a _________ type of secretion.
Definition
pulsatile
Term
There are greater concentrations of LH and FSH in women/men.
Definition
women
Term
Is the concentration of LH or FSH higher?
Definition
LH, but they track together
Term
During the menstrual cycle, LH and FSH are greater in the first/second half.
Definition
first
Term
When do LH and FSH make a sharp peak in a woman's menstrual cycle?
Definition
ovulation
Term
treatment of infertility in women
Definition
simulate ovulation

controlled ovulation hyperstimulation for assisted reproductive techniques (IVF)
Term
causes of infertility in women
Definition
hypogonadotropic hypogonadism
polycystic ovary syndrome (PCOS)
obesity
Term
treatment of infertility in men
Definition
stimulate spermatogenesis
Term
Hypogonadal men require treatment with ____ and _____.
Definition
LH (hCG) and FSH
Term
Lutropin
Definition
LH (recombinant), given with recombinant FSH
Term
Which hormones have both extracted and recombinant forms?
Definition
FSH and hCG
Term
side effects of LH, FSH, and hCG
Definition
ovarian overstimulation
multiple pregnancies
ovarian cancer risk increases
men--gynecomastia
Term
hyperstimulation syndrome
Definition
ovarian overstimulation, causing ovarian enlargement, rupture, hypovolemia, shock, arterial thromboembolism
Term
What risks do multiple pregnancies raise?
Definition
pre-eclampsia
diabetes
pre-term labor
Term
gonadorelin
Definition
GnRH agonist
Term
leuprolide
Definition
GnRH agonist
Term
How is GnRH agonist therapy administered?
Definition
IV pump (intermittent administration)

about 6 months of treatment for men
Term
Which infertility treatment is less likely to cause multiple ova to be released?
Definition
GnRH agonists (gonadorelin, leuprolide)
Term
What happens with continuous administration of GnRH agonists?
Definition
suppression of gonadotropin formation
Term
What is continuously administered GnRH agnoist used to treat?
Definition
endometriosis (suppression of cyclical hormone changes reduces symtpoms)

uterine fibroid reduction

precocious puberty (rule out tumors first!)
Term
treatment of prostate cancer
Definition
GnRH agonist and androgen antagonist (flutamide)

reduces testosterone levels to hypogonadal levels within two weeks
Term
other androgen antagonists
Definition
spironalactone (competitive inhibitor)

finasteride (reduces dihydrotestosterone production)
Term
side effects of GnRH agonists
Definition
hot flashes, sweating, HA, loss of libido
reduced bone density, osteoporosis
headaches
depression
vaginal dryness and breast atrophy in women
gynecomastia in men
Term
Where is testosterone and dihydrotestosterone produced?
Definition
Leydig cells in testes (95%) and adrenals (5%)
Term
What is the major form of testosterone in the prostate, seminal vesicles, and epididymis?
Definition
dihydrotestosterone
Term
various forms of testosterone
Definition
androgens
Term
What is androgen therapy not useful in?
Definition
anemia
catabolic states
Term
side effects of androgen therapy
Definition
masculinization in women

synthetic agents:
-hepatic dysfunction
-prostatic hyperplasia

supraphysiologic doses
-azoospermia
-decreased testicular size
-hepatic failure/cancer
-aggressiveness/psychosis
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