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134 Cards in this Set
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Somatropin (fxn, adverse effects, drug/drug)
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GH
A - hyperglycemia d/d - glucocoriticoids |
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Octreotide (fxn, adverse effects)
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somatostatin analog (GH-RH antagonist, GH release inhibitor) --> decreases GH release from the anterior pituitary
A - GI |
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Pegvisomant (fxn, adverse effects)
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GH receptor antagonist --> normalizes IGF-1
A - flu-like |
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Sermorelin (fxn)
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Dx only, GH-RH
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Cabergoline (fxn, adverse effects)
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DA agonist --> decreases prolactin
A - pregnancy |
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corticotrophin (fxn)
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more antigenic ACTH analog for Dx only
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cosyntropin (fxn)
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ACTH analog Dx only
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Bromocryptine (fxn)
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DA agonist for pituitary adenoma --> decreases prolactin and tumor size
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Leuprolide (fxn, adverse effects)
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GnRH agonist for the androgen tumor and endometriosis treatment --> flare --> constant pit. receptor binding leads to receptor downregulation --> decreased testosterone, estrogen, and progesterone
A - decreased libido, muscle mass, and osteoporosis |
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Nafarelin
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GnRH in infertility
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Gonadorelin
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GnRH used to test pituitary function
Nafarelin is for infertility Leuprolide for Ca |
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vasopression (fxn, adverse effects)
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ADH --> vasoconstriction, increases flow to brain and heart in emergency
A - excess to benefits |
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Desopressin
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ADH --> nasal spray --> increased flow with less vasoconstriction than vasopressin
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Oxytocin (fxn, adverse effects)
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labor, milk letdown
A - hypotension |
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Hydrocortisone fxn and adverse event
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short acting cortisol analog with mixed gluco/mineralcorticoid function
A-few |
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cortisone
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changes in vivo to hydrocortisone
short acting cortisol analog with mixed gluco/mineralcorticoid function |
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prednisone
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intermediate acting cortisol agonist, used for RA and SLE
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Dexamethasone
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long acting cortisol agonist, suppresses ACTH
Used for Dx, IBD/Crohn's Tx |
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Fludrocortisone fxn and side effects
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chronic mineralcorticoid tx, more mineral than glucocorticoid
A- increased NaCl and H20, K loss --> blood volume increase... |
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What are two drugs to test adrenal function?
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Dex supression test (for Cushings)
Corticotrophin/cosyntrophin (for adrenal insufficiency) |
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Administration of corticoids does what to the adrenal gland?
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system suppression and atrophy
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What are the adverse effects of corticoids?
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osteoporosis, infection, increased glucose, myopathy, mineral disturbance
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Hypothalmus releases CRH --> anterior pituitary releases ACTH --> adrenal cortex releases glucocorticoids. What function do glucocorticoids have on the body?
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decreased PG, leukotriene and histamine production via decreased DNA --> mRNA
decreased phagocytic infiltration decreased lymphocyte proliferation |
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What hormone has the following effects:
decreased PG, leukotriene and histamine production via decreased DNA --> mRNA decreased phagocytic infiltration decreased lymphocyte proliferation |
glucocorticoids
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What is the GH-RH drug used only for testing the pituitary function?
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Sermorelin
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What hormones regulates metabolic fuctions?
What are the metabolic effects (not immune effects)? |
Glucocorticoids (cortisol) and synthetics such as Dex, Pred, and Hydro
regulates carbohydrate metabolism and increases glucose availability, protein and fat metabolism |
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What hormones regulate electrolytes?
What electrolyte effects does it have? |
mineralcorticoids (aldosterone) and synthetics such as fludrocortisone.
renal regulation of sodium, potassium, and hydrogen |
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What are the androgens?
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testosterone, androstenedione, and dehydoepiandrosterone
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What hormone is essential the opposite of insulin?
It stimulates gluconeogenesis in the liver reduces peripheral glucose utilization and uptake (esp muscle and adipose) Promotes storage as glycogen |
glucocorticoid (cortisol) and synthetics such as dex, pred, and hydrocortisone
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What drugs decrease capillary permeability, vasoconstriction, increase blood pressure (these effects are going to change metabolism, mood, and immune cell opportunity)?
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Glucocorticoids such as cortisol, pred, dex, or hydrocortisone
They have immune effects (reduced phagocytic and lymphocytic effects, reduced histamine/leukotriene/PG production) and CV effects (decreased capillary permeability, increased vasoconstriction) |
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What drugs inhibit steroid synthesis?
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Ketoconazole inhibits steroid synthesis in the liver.
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What is cushings disease?
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increased ACTH concentration released from anterior pituitary
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Primary increased glucocorticoid concentration is from what?
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adenoma
compared to decrease which is from Addisons or acute adrenal insufficiency |
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How do you treat Addison's disease (decreased glucocorticoid concentration from a primary cause)?
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Fludrocortisone (to cover mineralcorticoids) and hydrocordisone (to cover more of the glucocorticoids)
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What is addison's disease?
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adrenal insufficiency
The opposit of cushings disease weakness, emaciation hypoglycemia, increased skin pigmentation, hyperkalemia, hyponatremia, hypotension |
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What disease has the following characteristics?
weakness, emaciation hypoglycemia, increased skin pigmentation, hyperkalemia, hyponatremia, hypotension |
Addison's disease
adrenal insufficiency |
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Why do glucocorticoids such as hydrocortisone, prednisone, Dex, and natural cortisol, cause osteoporosis
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They suppress osteoblasts
ribs and vertebrae are most effected |
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How is half-life, minerocorticoid potency, and anti-inflammatory potency affected by the duration of actaion of various glucocorticoids?
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Short acting (hydrocortisone) have short half-lives, little anti-inflammatory action, and more mineralcorticoid crossover.
Long acting (Dex) have more anti-inflammatory and less mineralcorticoid action. |
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What "G"rowth hormone drug interacts with "G"lucocorticoids?
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somatropin
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You have a patient with low corisol levels (Addison's or acute symptoms). What drugs are used to test adrenal insufficiency? Why would you chose 1 drug over the other?
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ACTH agonists cosyntrophin (synthetic and thus less antigenic) or corticotrophin (animal pituitary)
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What is the cause of nephrogenic diabetes insipidus?
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failure of the kidney to produce concentrated urine despite adequate levels of ADH from:
Blockage in the urinary tract High calcium levels Low potassium levels Use of certain drugs (lithium, demeclocycline, amphotericin B) |
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What is the effect when the kidneys fail to concentrate urine despite adequate ADH form the posterior pituitary?
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nephrogenic diabetes insipidus
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What is the effect of inadequate ADH from the posterior pituitary?
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hypothalamic diabetes insipidus (similar effect/presentation to nephrogenic diabetes insipidus)
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When taking OC's what may cause breakthrough bleeding?
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drug interractions that induce haptaic enzymes (lower OC plasma levels)
I think multiphasic OC's are more likely. |
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What are 3 primary functions of estrogen/progestin?
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bone, metabolism, and reproductive control
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Clomiphene function
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SERM (selective estrogen receptor modulator)
infertility tx; inhibits negative Estrogen feedback |
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Tamoxiphen function
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SERM (selective estrogen receptor modulator)
breast cancer treatment; estrogen-like --> therefore endometrial effects Ralozifen has no endometrial effects Anastrozole has no endometrial or thromboembolysm effects but is for post-menopausal |
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Raloxifene function and benefits
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SERM (selective estrogen receptor modulator)
osteoporosis, decreases breast Ca, no change in endometrium Anastrozole is used for post menopausal breast Ca and doesn't have the endometrial effects or thromboemolysm effects wherease Tamoxiphen has the endometrial effects |
ya, breast cancer, but what else
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Anastrozole MOA and benefits over ralozifene
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aromataste inhibitor, post-menopause Breast Ca tx; does not have endometrium or
thromboembolysm effects aromatase changes androgen into estrogen |
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Mifepristone MOA, use, adverse events
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week agonist/competative antagonist of progesterone and glucocorticoids; therefore, local estrogen synthesis inhibitor
used for 1st trimester abortions in conjunction with misoprostol (pg analog) A - excessive bleeding/pain (antagonist effect), weakness, HA, dizziness, fever/chills (these side effects are due to the agonist effects of mifepristone) |
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Dinoprostone MOA, use, adverse events
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PGE2 --> uterine contraction and oxytocin augmentation --> labor or 2nd/3rd trimester abortion
A - uterine hyperstimulation, nausea/vomiting, diarrhea, fever, HA (basically though mifepristone has a different MOA, they have the same side effects) |
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Misoprostol MOA and use
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PGE1 --> progesterone antagonist --> uterine stimulant for labor or used with mifepristone for abortions
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What are the unique adverse effects of estrogen?
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nausea
fibroid, uterine growth hyperpigmentation (like Addison's) galbladder disease HTN |
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What is the hormone of the follicular phase?
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estrogen
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what is the hormoone of the luteal phase?
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progestin
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What are the unique adverse effects of progestin?
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mood change
acne dizziness fatigue dyslipidemia |
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What is the pre-menopausal estrogen?
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estradiol
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what is the estrogen of pregnancy?
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estrone
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What is the benefit to conjugated estrogens?
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absorbed better less first pass
same benefit as synthetic |
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Progesterone has high or low first pass?
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high
precursor to androgen, estrogen, adrenocortical steroids |
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Medroxyprogesterone type and adverse effect
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synthetic, decreased first pass,
A-decreased bone density |
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name some uterine stimulants.
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oxytocin
dinoprostone (PGE2) misoprostol (PGE1) Ergot alkaloids |
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What are some drugs of delivery?
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oxytocin (uterine stimulant)
dinoprostone (PGE2 uterine stimulant) misoprostol (PGE1 uterine stimulant) mifepristone (progesterone/glucocorticoid receptor partial agonist/competative antagonist) |
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What cells make testosterone?
What hormone stimulates the production? |
Leydig cells with LH stimulation
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What stimulates spermatogenesis?
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FSH and Testosterone
"S" for FSH and Spermatogenesis |
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FSH production in the male leads to what?
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spermatogenesis
along with testosterone |
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ketocoonazole treatment can cause what side effects in men?
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gynecomastia and hepatotoxicity
remember ketoconazole may interrupt steroid production |
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what effect does testosterone have on the body?
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increased muscle mass
increased EPO spermatogenesis pubertal growth increased BPH decreased HDL and increased LDL |
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17 alpha alkylated androgens: effects and adverse effect
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orally available, increased anabolic/decreased androgenic
A - hepatotoxic |
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Finasteride: type of drug, MOA, and clinical use
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5 alpha-reductase inhibitor (Type I and II, but more Type II) for BPH and alopecia
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Flutamide MOA, use, adverse effect
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androgen receptor antagonist used to prevent androgen flare
A - gyencomastia |
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Dagarelix MOA, use, adverse effect
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GnRH antagonist in pituitary
used in prostate Ca, A- in women causes hirsutism |
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Androgen definition, effect, adverse effects
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male sex hormone
increases development and maintenance of sex characteristics A-premature epiphyseal closure, decreased HDL/increased LDL, hynecomastia, edema, virilization |
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Name 2 progesterone antagonists.
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PGE1 Misoprostol
Mifepristone week ag/competative antag |
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Tobutamide (MOA and type of drug)
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Sulfonylurea
block K channel --> membrane depolarizes --> Ca++ influx --> insulin release from Beta cells |
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What are the adverse effect of tobutamine?
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sulfonylureas can cause hypoglycemia
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What drugs increase the adverse effect of tobutamine (sulfonylurea)?
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NSAIDS, cimetidine (H2 blocker), ramantidine (parkinsons and antiviral), sulfonamide abx, ethanol, and BB's increase hypoglycemia
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What is the MOA of Repaglinide?
type of drug |
meglitamide with the same MOA as sulfonylureas
blocks K+ --> depol --> Ca++ influx --> insulin release |
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What is the adverse effect and drug/drug interaction of repaglinide?
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hypolgycemia
gemfibrozil (TG tx) inhibits repaglinide metabolism and makes hypoglycemia worse |
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Metformin (class and MOA)
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biguanide class
suppresses gluconeogenesis by liver enhances glucose uptake by muscle --> increases krebs cycle --> uses O2 to produce ATP |
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What are the adverse effects and contraindications of metformin (biguanide)?
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A-GI, lactic acidosis
contraindications-renal dz (cleared unchanged by kidneys) and cardiac problems |
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Rosiglitizone (Avandia) MOA
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Thiazolidinedione activates peroxisome proliferator-activated receptor gamma genes that respond to insulin
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What are the adverse effects and drug/drug interractions of rosiglitazone (thiazolidinedione)?
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A-fluid retention/edema/exacerbate CHF, angina/MI
gemfibrozil (just like Repaglinide (meglitamide) |
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Acarbose MOA and class
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alpha-glucosidase inhibitor --> decreased breakdown of carbohydrates --> delays absorption from GI
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Glucagon function, secreted from where?
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increases blood glucose
secreted from alpha cells in pancreas |
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Sitagliptin phosphate MOA
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DDP-4 inhibition --> inhibits Incretin (increases insulin synthesis, lower glucagon secretion) inactivation
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what drug inhibits DDP-4 which inhibits incretin deactivation?
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Sitagliptin phosphate
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What drugs may be combined with metformin?
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sitagliptin phosphate
sulfonulureas (glipizide, glyburide) rosiglitazone |
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Glucagon function, secreted from where?
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increases blood glucose
secreted from alpha cells in pancreas |
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What drug should NOT be combined with metformin?
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acarbose (carb absorption inhibitor) because of additive GI effects
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Sitagliptin phosphate MOA
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DDP-4 inhibition --> inhibits Incretin (increases insulin synthesis, lower glucagon secretion) inactivation
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what drug inhibits DDP-4 which inhibits incretin deactivation?
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Sitagliptin phosphate
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What drugs may be combined with metformin?
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sitagliptin phosphate
sulfonulureas (glipizide, glyburide) rosiglitazone |
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What drug should NOT be combined with metformin?
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acarbose (carb absorption inhibitor) because of additive GI effects
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effects of insulin deficiency are?
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diabetic ketoacidosis
increased lipolysis --> glycerol increased glucose production and decreased glucose use furthers hyperglycemia --> encourages diuresis --> leads to dehydration --> shock |
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how is ketoacidosis treated?
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insulin
saline solution monitor K and glucose (insulin may cause hypokalemia and hypoglycemia) bicarb in serious situations |
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short or long duration
insulin lispro when is it used |
short
rapid acting used any time |
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regular insulin, short or long duration?
when is it used? |
short
slow acting used before meals for basal control |
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insulin aspartate, short or long duration?
when is it used? |
short, rapid
any time |
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insulin glulisine, short or long duration?
when is it used? |
short, rapid
used any time or with NPH |
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NPH insulin
when is it used? how is it used? |
intermediate duration 16-24hr, b/c conjugated w/protamine
used with insulin aspartate, glulisine, or lispro BID |
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Insulin detemir
how, when is it used? |
intermediate duration 12-24 hr bc conjugated w/FA
use SID or BID |
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Insulin glargine
when and how is it used? |
long duration, 24hr
decreased solubility adn physiologic pH |
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which insulin has the fastest onset of action
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insulin lispro 15 min
insulin aspartate 10 min insulin glulisine 10 min |
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What do alpha-glucosidase inhibitors do and what is an example?
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acarbose inhibits carbohydrate breakdown and decreased absorption
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What cells secrete stomach acid?
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parietal cells
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what receptors are stimulated to release acid into the stomach?
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M3 + Ach or gastrin on enterochromaffin-like cells --> histamine release OR directly on parietal cells
H2 + histamine (H1 is emetic) |
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What is the MOA and use of Omeprazole?
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Prilosec is a PPI, irreversible inhibit H/K ATPase pumps
for peptic ulcers, GERD, dyspepsia, gastrinoma-caused gastric hyersecretion (Zollinger-Ellison syndrome, G-cell hyperplasia, increased parietal-cell mass) |
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What are the adverse effects of Lansoprazole and omeprazole?
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prevacid adn prilosec decreased B12, cause HA, diarrhea, or abd pain
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What drugs do Omeprazole and lansoprozole inhibit?
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ketoconazole and digoxin (by acidity)
coumadin, diazepam, phenytoin (seizure), theophyllin (COPD) by P450 |
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What is the MOA and use of sucralfate?
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forms gel in acid or water sln --> wall coating for peptic ulcer
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What is the MOA and use of bismuth subsalicyte?
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coat gI, antimicrobial, stimulates PG, mucus, and bicarb production
for travelers and for H. pylori peptic ulcer (with Abx and PPI) |
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What are the adverse effects of aluminum antacids?
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constipation
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what are the adverse effects of magnesium antacids
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diarrhea with altered electrolyte balance
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What adverse effects do H2 antagonists (cimetidine, ranitidine) have?
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cimetidine - CNS and endocrine (increases estradiol metabolism --> hynecomastia or impotence or galactorrhea)
do not use in pregnancy |
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Which drugs should not be used in pregnancy: cimetidine, omeprazole, ranitidine, lansoprazole?
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cemtidine and ranitidine
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What drug gives harmless black tongue, black stool and is great for traveler's diarrhea?
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bismuth subsalicylate
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MOA and use of metoclopramide
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DA2 antagonist in GI --> increase esophogeal and stomach motility/emptying in post surgery
at high antagonist to DA1 chemoreceptor trigger in medulla --> antiemetic |
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What are the major adverse effects of metoclopramide?
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D2 antag
oculogyric crisis, HTN/HypoTN, hyperprolactinaemia, depression |
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Laxative MOA
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bulk --> stretches receptors
surfactants --> permits water to penetrate mineral oil --> prevent water absorption --> lubricant osmotic --> draw water out |
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What type of laxatives are used in bowel preparation?
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balanced polyethylene glycol - osmotic
stimulants --> clean entire bowel |
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Loperamide MOA and use
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opiod agonist, doesn't cross BBB, no analgesic effect --> inhibit presynaptic cholinergic action
anti-diarrhea |
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MOA and use of Kaolin & Pectin
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antidiarrhea in kids
coats wall, binds bacteria --> absorbant --> decreases stool liquidity |
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Receptors involved in vomiting
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D2, H1, 5-HT3, M1 and NK1 (neurokinin)
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Ondasetron MOA and use
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block 5-HT3 central and peripheral --> targets vomiting center, chemoreceptor trigger zone, vagas, adn spinal afferents --> antiemetic
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Dolasetron MOA and use
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blocks 5-HT3 --> at chemo trigger center, vomiting center, spinal aferents, and vagas --> antiemetic
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Receptors of the vestibular system are ?
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M1 and H1
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Aprepitant MOA and use
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NK1 antagonist --> antiemetic
CYP3A4 metabolism |
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drugs to treat IBD
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inflammatory suppressors (5-ASA = mesalamine)
Immunomodulators (6-mercaptopurine) Anticytokine (Infliximab) |
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Mesalamine use
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anti-inflammitory for IBD
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6-mercaptopurine use
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immunomodulator reducing T cell in IBD
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infliximab use
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anticytokine for TNF-alpha in refractory IBD
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most antiemetics cause tiredness. One causes prolonged QT interval, which one?
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Metoclopramide (D2 antagonist)
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some antiemetics are used with dexamethasone to enhance their effect, which ones
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Ondansetron (5-HT3 antagonist)
Aprepitant (NK1) |
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