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Pharm Quiz 4
Endocrine
122
Medical
Graduate
04/05/2012

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Term
cirticotropin releasing hormone (CRH) has a positive effect on what target organ to release what hormone
Definition
CRH has a positive effect on the anterior pituitary to secrete adrenocorticotropin hormone
Term
growth hormone releasing hormone has a positive effect on what target organ to release what hormone
Definition
GHRH has a positive effect on the anterior pituitary to release growth hormone (aka - somatotropin)
Term
somatostatin has a positive or negative effect on the anterior pituitary?
Definition
has a negative effect on the anterior pituitary
Term
somatostatin has a negative effect on what target organ, causing the inhibition of what hormone
Definition
somatostatin inhibits the release of GH from the anterior pituitary
Term
gonadotropin releasing hormone has a positive effect on what target organ to release what hormone
Definition
GnRH has a positive effect on the anterior pituitary to release FSH and LH
Term
thyrotropin releasing hormone has a positive effect on what target organ to release what hormone
Definition
TRH has a positive effect on the anterior pituitary to release TSH
Term
dopamine has a negative effect on what target organ to cause the inhibition of what hormone
Definition
dopamine has a negative effect on the anterior pituitary inhibiting the release of prolactin
Term
which pituitary gland is connected to the hypothalamus via a portal system
Definition
the anterior pituitary is connected to the hypothalamus via a special portal system, allowing for direct communication between both glands
Term
the target organ hormone of growth hormone
Definition
insulin like growth factor 1
Term
the target organ hormone of TSH
Definition
thyroixine (T4) and thriiodothyronin (T3)
Term
the target organ hormone of ACTH
Definition
glucocorticoids, mineralocorticoids, and androgens
Term
the target organ hormone of FSH
Definition
estrogen, testosterone, and progesterone
Term
the target organ hormone of LH
Definition
estrogen, testosterone, and progesterone
Term
the target organ hormone of prolactin
Definition
none, it does not target an organ
Term
treatment of GH deficiency
Definition

somatropin

 

somatrem

 

sermorelin

Term
side effects to the treatment of GH deficiency
Definition

treating with somatropin, somatrem or sermorelin can cause:

 

muscle or joint pain, swelling, pain or numbness in hands

 

indicates the GH replacement levels are too high for the pt

Term
what are the differences in the manifestation of gonadotropin deficiency depending on whether the deficiency occured before or after puberty
Definition

deficiency prior to puberty -> prevents normal sexual maturity causing a lack in secondary sex characteristics

 

deficiency after puberty -> early menopause in women or sexual dysfunction in men

Term
treatment of gonodotropin deficiency
Definition

menotropins

 

human chorionic gonadotropin

 

urofollitropin (uFHS)

 

follitropin alpha and beta

 

lutropin alpha (rLH)

 

GnRH agonists

 

estrogen receptor agonist-antagonists

Term
which class of drugs, used for the treatment of gonadotropin deficiency, is formed from human menopausal gonadotropin, from the urine of menopausal women, and contains both FSH and LH
Definition
menotropins (repronex, pergonal humegon)
Term
which drug, used for the treatment of gonadotropin deficiency, is formed from the placenta and isolated from urine of pregnant women, and contains primarily LH
Definition
human chorionic gonadotropin
Term
which drug, used for the treatment of gonadotropin deficiency, is purified FSH extracted from urine of postmenopausal women and has the LH removed
Definition
urofollitropin (uFHS)
Term
which drug, used for the treatment of gonadotropin deficiency, is recombinant forms of FSH (and not from the urine of women)
Definition
follitropin alpha and beta (rFHS)
Term
which drug, used for the treatment of gonadotropin deficiency, is the recombinant form of LH, and is approved only for use in combination with follitropin alpha to stimulate follicular development in infertile women with profound LH deficiency
Definition
lutropin alpha (rLH) 
Term
pulsatile or nonpulsatile release of GnRH leads to hypogonadism
Definition
NONpulsatile release/secretion leads to hypogonadism
Term
pulsatile or nonpulsatile release of GnRH leads to stimulation of FSH and LH release
Definition
pulsatile release of GnRH leads to the stimulation of FSH and LH release
Term
which drug, used for the treatment of FSH and LH deficiency, must be administered in such a manner, that it mimics a pulsatile secretion of FSH and LH, and is acetate salt of human GnRH
Definition
gonadorelin
Term
what are the synthetic analogs of GnRH that are used in the treatment of FSH and LH deficiency/gonadotropin deficiency
Definition
goserelin, histrelin, leuprolide, nafarelin, triptorelin
Term
which drug is an estrogen receptor agonist-antagonist used in the treatment of gonadotropin deficiency/FHS and LH deficiency
Definition
clomiphene - actos on estrogen receptors in the hypothalamus to increase the release of FSH and LH
Term
a somatotrope adenoma (of the anterior pituitary) that develops during adulthood results in what condition
Definition
acromegaly
Term
a somatotrope adenoma (of the anterior pituitary) that develops before the closing of the long bone epiphyses results in what condition
Definition
gigantism
Term
what are the different possible lines of treatment for hypersecretion of GH (hyperpituitartism)
Definition

somatostatin analogues (octreotide acetate, lanreotide)

 

GH receptor antagonists (pegvisomant)

 

dopamine agonists (bromocriptine, cabergoline)

Term
what drug is most often used in the treatment of GH excess
Definition
octreotide
Term
which drugs must be used in combination with octreotide for the treatment of GH, because if used by themselves would require extremely large doses
Definition

the dopamine agonists:

 

bromocriptine

cabergoline

Term
which pegilated drug is used for the treatment of GH excess
Definition

GH receptor antagonist: 

 

pegvisomant

Term
treatments for GnRH excess
Definition

GnRH antagonists (ganirelix, centrorelix, abarelix, degarelix)

 

continual administration of GnRH (gonadotropin, goserelin, leuprolide, nafarelin)

Term
what drugs are approved for the treatment of controlled ovarian hyperstimulation
Definition
genirelix and centrorelix (GnRH antagonists) are approved for controlled ovarian hyperstimulation
Term
what drugs are approved for men with advanced prostate cancer
Definition
abarelix and degarelix (GnRH antagonists)
Term
which drugs can be used as continual administration for the treatment of GnRH hyperpituitarism
Definition

GnRH agonists:

 

gonadorelin

goserelin

leuprolide

nafarelin

Term
what is the most common pituitary hormone hypersecretion in both males and females
Definition
prolactin
Term
what are the treatments for hypersecretion of prolactin
Definition
dopoamine agonists (cabergoline, bromocriptine, and others: pergolide, mesylate, lisuride, quinagolide
Term
which hormone is released in response to elevated tonicity or falling blood pressure
Definition
vasopressin (antidiuretic hormone/ADH)
Term
which vasopression receptors are found on vascular smooth muscle cells and mediate vasoconstriction (the vasopressor property of the hormone) - V1 or V2 receptors?
Definition
V1 receptors
Term
which vasopressin receptors are found on tuble cells and reduce diuresis by increasing water permeability and resorption in collecting tubules (the antidiuretic property of ADH) - V1 or V2 receptors?
Definition
V2 receptors
Term
what are the treatments for vasopressin deficiency
Definition

vasopressin

 

desmopressin

 

 

Term
what is the treatment for diabetes insipidus
Definition

vasopressin

 

desmopressin

Term
which drug is used for the treatment of nocturnal enuresis
Definition
desmopressin
Term
what are the treatments for vasopressin excess
Definition

conivaptan

 

tolvaptam

Term
which drug, used for the treatment of vasopressin excess, has an affinity for both V1alpha and V2 receptors
Definition

conivaptan

 

(tolvaptan - has an affinity for V2 receptors only)

Term

what drugs can be given to induce labor 

 

what are the differences in clinical manifestations between giving low doses and high doses of these drugs

Definition

oxytocin and pitocin

 

low doses: increase frequency and force of uterine contractions

 

high doses: provide for sustained contraction

Term
what is the treatment of choice for hypothyroidism
Definition

replacement therapy:

 

levothyroxine

liothyronine

liotrix

Term
which drug, used for the treatment of hypothyroidism, is more potent and consists of only T3
Definition
liothyronin
Term
which drug, used for the treatment of hypothyroidism, is synthetic T4
Definition
levothyroxine
Term
which drug, used for the treatment of hypothyroidism, is a mixture of T3 and T4
Definition
liotrix
Term
what is the first line of treatment for thyrotoxicosis in the US
Definition
radioiodine (131I)
Term
what are all the possible treatments for thyrotoxicosis
Definition
radioiodine, propylthiouracil (PTU), carbimazole, and methimazole
Term
which drug, used for the treatment of hyperthyroidism, inhibits the converson of T4 to T3
Definition
beta-adrenoceptor antagonists (propanolol)
Term
which drugs, used for the treatment of hyperthyroidism, inhibit the organification and hormone release and reduce size and vasculatiry of thyroid
Definition
lugol's solution, potassium iodide
Term
the zona glomerulosa, of the adrenal gland, produces what molecule
Definition
mineralocorticoids (aldosterone)
Term
the zona fasciculata produces what compounds
Definition
glucocorticoids (cortisol)
Term
the zona reticularis produces what molecule
Definition
androgens (DHEA and testosterone, and others)
Term
treatments of adrenal insufficiency
Definition
hydrocortisone, cortisone, prednisone, prednisolone, methylprednisolone, meprednisone, triamcinolone, paramethasone, fluprednisone, (betamethasone, dexamethasone), fludrocortisone, desoxycorticosterone acetate
Term
pharmacologic treatments for secondary and tertiary adrenal insufficiency
Definition
hormone replacement therapy for glucocorticoids, but not usually for mineralocorticoids as aldosterone secretion is preserved.  however, replacement of other pituitary hormones may be necessary
Term
treatment of hyperaldosteronism
Definition

aldosterone antagonist (spironolactone)

MR antagonist (eplerenone)

Term
treatment of virilization and hirsutism because of adrenal hypersecretion
Definition

oral contraceptives

 

glucocorticoids (dexamethasone, prednisone)

 

antiandrogens (spironolacton, flutamide)

Term
treatment of cushing's syndrome
Definition

glucocorticoid synthesis inhibitors:

aminoglutethimide

ketoconazole

metyrapone

 

receptor antagonists:

mifepristone

spironolactone

Term
which drug, used for the treatment of adrenal hypersecretion, blocks conversion of cholesterol to pregnenolone, which is rate limiting step in all hormonaly active steroids
Definition
aminoglutethimide
Term
in the pancreatic beta cell, the presence of glucose (aka - after a meal) causes an an increase in intracellular ATP which leads to what
Definition
the closing of K+ channels, from the increased levels of ATP kinding to the SUR1 receptor on the K+ channel
Term
in the pancreatic beta cell, after a meal, the binding of ATP to the K+ channel causes a hyperpolarization or a depolarization of the cell
Definition
ATP binds to the SUR1 receptor on the K+ channel, causing the channels to close, which leads to depolarization of the beta cell
Term
in the pancreatic beta cell, after a meal, the closure of the K+ channels causes a depolarization of the cell which leads to what
Definition
the depolarization of the beta cell causes the Ca2+ channels to open, causing an influx of Ca into the cell, which results in the movement of vesicles from the golgi to move to the membrane, fuse, and release insulin into circulation
Term
when insulin binds to the insulin receptor on the muscle cell, it causes an increase in what type of glucose transporter
Definition

GLUT4

 

(the insulin binding to the insuline receptor, causes autophosphorylation of the receptor which causes a signal cascade, that results in GLUT4-containing vesicles to fuse with with membrane, increasing the numer of glucose transporters in the cell membrane)

Term
one international unit of insulin (IU) = 
Definition
1 IU is the "biological equivalent" of about 45.5 mcg of insulin
Term
list the different drugs used as insulin therapy that have the fastest onset and duration of action, and are typically taken as boluses with food
Definition

insulin aspart (novolog)

 

lispro (humalog)

 

insulin glulisine (apidra)

Term
list the different drugs used as insulin therapy that have the longest onset and duration of action, and are typically taken as basal insulin therapy
Definition

insulin detemir (levemir)

 

insulin glargine (lantus)

Term
what is the MOA of the sulfonylureas
Definition
the sulfonylureas close the K+ channels on the beta cell plasma membrane causing depolarization of the cell, resulting in release of insulin
Term
list the 2nd generatoin sulfonylureas
Definition

glyburide (diabeta)

 

glipizide (glucotrol)

 

glimepiride (amaryl)

Term
what drug can you use as an "antidote" for the overdose of a sulfonylurea or meglitinide
Definition
octreotide (sandostatin)
Term
what are the disadvantages of using sulfonylureas for the treatment of DM
Definition

they cause:

weight gain

hypoglycemia

 

they do NOT preserve the beta cells of the pancreas

 

cannot be used in pts with sulfonamide allergy

 

Term
list the meglitinide drugs used for the treatment of DM
Definition

nateglinide (starlix)

 

repaglinide (prandin)

Term
what is the MOA of the meglitinides and how is their MOA different from the sulfonylureas
Definition

(nateglindine and repaglinide)

 

close the K+ channels on the beta cell plasma membrane, causing depolarization of the cell, resulting in the release of insulin

 

they require glucose present in order to bind to the K+ channel to cause the conformation change of the K+ channel, and they do not bond as tightly to the channel and therefore have a shorter duration of action

Term
what are the disadvantages of using a meglitinide for the treatment of DM
Definition

(nateglinide and repaglinide)

 

weight gain

hypoglycemia

dosing frequency

medium cost

pts with hepatic and renal insufficiency

no beta-cell protection

Term
list the biguanide used for the treatment of DM
Definition
metformin (glucophage)
Term
what is the MOA of metformin
Definition

it is an insulin sensitizer, by activating the AMP kinase which stimulates/favors catabolic pathways:

 

decreasing hepatic glucose production, decreasing intestinal glucose absorption, increasing insulin action, reduces visceral fat depots

Term
what are the disadvantages of taking metformin for the treatment of DM
Definition

GI side effects (diarrhea)

contraindicated in reduced kidney function

can result in lactic acidosis

no beta cell preservation

Term
which drug, normally used for the treatment of DM, can also be used for the treatment of polycystic ovarian syndrome as well as improving acne by decreasing androgen levels
Definition
metformin
Term
list the thiazolidinediones (TZDs)
Definition

rosiglitazone (avandia)

 

pioglitazone (actos)

Term
what is the MOA of TZDs
Definition

(rosiglitazone and pioglitazone)

 

activate the nuclear transcription factor PPAR-y modulating transcription for the GLUT4 transporter, resulting in an increase in peripheral insulin sensitivity

Term
which drug, used for the treatment of DM, is metabolized by CYP2C8 and CYP2C9, and which one is metabolized by CYP 2C8 and CYP3A4
Definition

rosiglitazone

 

pioglitazone

Term
which drug, used for the treatment of DM, weakly induces CYP3A4
Definition
pioglitazone
Term
which drug, used for the treatment of DM, has the adverse effects of possibly causing heart failure, bone fractures, and liver toxicity, but does NOT cause hypoglycemia when taken
Definition
rosiglitazone
Term
which class of drugs, used for the treatment of DM, takes approx 8 - 12 weeks to see see maximal effects
Definition
thiazolidinediones (TZDs)
Term
list the GLP-1 receptor agonists
Definition

exenatide (byetta)

 

liraglutide (victoza)

Term
list the different effects of GLP-1 receptor agonists
Definition

(exanatide and liraglutide)

 

increases insulin biosynthesis and preserved beta-cell function

 

decreases appetite

 

decreases hepatic glucose production

 

slows gastric emptying

 

increases muscle insulin sensitivity

Term
what are the disadvantages to taking GLP-1 receptor agonists (incretin mimetics)
Definition

(exanatide and liraglutide)

 

GI side effects (N/V/D)

acute pancreatitis

injectable

hypoglycemia

long term effects unknown - pancreatic CA

 

Term
list the DDP 4 inhibitors and its MOA
Definition

sitagliptan (januvia)

 

saxagliptan (onglyza)

 

inhibits DDP 4 activity and prolongs endogenously released incretin hormones; GLP1 is not degraded as fast and has a longer duraction of action, increasing insulin secretion

Term
what are the disadvantages to using DPP4 inhibitors for the treatment of DM
Definition

pancreatitis observed

long term safety unkown (pancreatic CA)

expensive/high cost

Term
list the alpha-glucosidase inhibitors
Definition

acarbose (precose)

 

miglitol (glyset)

 

voglibose (basen)

Term
what is the MOA of the alpha-glucosidase inhibitors
Definition

(acarbose, miglitol, voglibose)

 

competitively inhibit intestinal alpha-glucosidase and delay hydrolysis and absorption of sugars

Term
what are the disadvantages to alpha-glucosidase inhibitors
Definition

GI side effects (gas, flatulence, diarrhea)

 

dosing frequency

 

medium cost

Term
list the dopamine-2 agonists used for the treatment of DM
Definition
bromocriptine (cycloset)
Term
what is the MOA of the dopamine-2 agonists that are used for the treatment of DM
Definition
activates dopaminergic receptors and resets the circadian organization/biological clock (which alters the hypothalamic regulation of metabolism and increases insulin sensitivity)
Term
what are the disadvantaged to dopamine-2 agonists for the treatment of DM
Definition

(bromocriptine)

 

dizziness, nausea, fatigue

rhinitis

long term safety unknown

medium cost

Term
what is the MOA of pramlintide (symlin)
Definition
it is a synthetic analog of amylin that works with insulin to delay gastric empyting and inhibit glucagon release
Term
what are the disadvantages to pramlintide for the treatment of DM
Definition

hypoglycemia

 

nausea and HA

 

can delay absorption of oral drugs

 

don't combine with other drugs that slow GI motility (atropine-like)

 

given by injection before meal and must be given by a syringe different than the one used for injecting insulin

Term
list some drugs that can cause drug induced osteoporosis
Definition

steroids (glucocorticoids)

barbituates, phenytoin

L-thyroxine over-replacement

anticoagulants (warfarin)

PPIs

TZDs

chronic lithium therapy

some drugs to treat HIV

Term
list the possible causes of osteoporosis
Definition

being confined to a bed

chronic RA, CKD, eating disorders

hyperPTH

Vit D deficiency

drug induced osteoporosis

Term
agents used to treat osteoporosis
Definition

calcium and vitamin D

calcitonin

estrogen

raloxifene (SERM)

teriparatide (forteo)

denosumab (prolia)

bisphosphonates

Term
what are the possible calcium agents used to CA supplementation
Definition

calcium carbonate

calcium lactate

calcium gluconate

calcium citrate

calcium phosphate

calcium levulinate

 

these all must be administered with Vit D

Term
what is the calcium recommendation for men, premenopausal women, and postmenopausal women who are also taking estrogen
Definition
1000 mg/day
Term
what is the calcium recommendation for teenagers and young adults 11 - 24 years of age
Definition
1200 mg/day
Term
what is the calcium recommendation for postmenopausal women not taking estrogen
Definition
1500 mg/day
Term
which drug, used for the treatment of osteoporosis, primarily has the effect of inhibiting osteoclastic bone resorption, as well as possibly stimulating osteoblasts, and may be more effective for increasing vertebral density as opposed to hip or femoral density; however this drug is biphasic and should be temporarily be stopped during middle of treatment plan
Definition
calcitonin
Term
which calcitonin agent has a longer half life and comes in the form of injectable or nasal spray
Definition
salmon calcitonin -> calcimar, miracalcic
Term
which drug, used for the treatment of osteoporosis, reduces the bone-resorbing actions of PTH and stimulates osteoblasts, but can increase the risk of MI, stroke, breast cancer, and DVTs, but does decrease vertebral and hip fractures
Definition
estrogen
Term
which drug, used for the treatment of osteoporosis, preserves bone density without increasing breast cancer risk, lowers total and LDL cholesterol, reduces vertebral and nonvertebral fractures, and increases lumbar and femoral bone densities, but will increase the incidence of hot flashes
Definition

raloxifene

 

(acts like estrogen in the bone, but does NOT act like estrogen in uterus and breast, acts as estrogen blocker)

Term
which drug, used for the treatment of osteoporosis, is the first 34 amino acids of the parathyroid hormone, and when given in low and intermittent doses cauess an increase in bone density by stimulating production of cAMP which stimulates osteoblasts, but is limited to only two years of use by the FDA
Definition
teriparatide
Term
which drug, used for the treatment of osteoporosis, has a black box warning for causing osteosarcomas when used in high dosages in rats, and therefore is limited to two years of use
Definition
teriparatide
Term
which drug, used for the treatment of osteoporosis, mimics the effects of osteoprotegerin by binding to the RANK ligand inhibiting osteoclasts from differentiating and decreasing their survival
Definition
denosumab (prolia)
Term
which drug, used for the treatment of osteoporosis, in injected every 6 months, but has has incidences reported of rare osteonecrosis of the jaw
Definition
denosumab
Term
which drugs, used for the treatment of osteoporosis, are absorbed into the bone matrix, and inhibit bone resoprtion, by inhibiting osteoclast function, promoting their apoptosis; some of the drugs in this class have a N in the side chain, making them more potent than the other drugs within this class that do NOT have a N in the side chain
Definition
bisphosphonates
Term
list the bisphosphonates used for the treatment of osteoporosis
Definition

etidronate

pamidronate

alendronate (fosamax)

tiludronate (skelid)

risendronate (actonel)

ibandronate (boniva)

zoledronic acid (reclast) - newest, IV

Term
what are the possible side effects of bisphosphonates
Definition

*esophagitis - upper GI problems*

 

some osteonecrosis of the jaw

 

 

musculoskeletal pain

 

possible nephrotoxicity - only with zoledronic acid

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