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USMLE - Pharm

Kaplan Section 7 - Endocrine 1

GnRH Gonadotropin releasing hormone; from hypothalamus; stimulates LH and FSH release from anterior pituitary
TRH thyrotropin releasing hormone; from hypothalamus; stimulates TSH and prolactin release from anterior pituitary
Dopamine from hypothalamus; inhibits prolactin release from anterior pituitary
GHRH growth hormone releasing hormone; from hypothalamus; stimulates growth hormone (GH) release from anterior pituitary
Somatostatin from hypothalamus; inhibits GH and TSH release from anterior pituitary
CRH corticotropin releasing hormone; from hypothalamus; stimulates ACTH release from anterior pituitary
Name the 8 Hypothalamic hormones GGC has STDs Out his Ass. To ANTERIOR PIT: GnRH, GHRH, CRH, Somatostatin, TRH, Dopamine. To distant tissues: Oxytocin, ADH
Name the 6 Anterior Pituitary hormones FLAT PiG: FSH, LH, ACTH, TSH, Prolactin, GH
Somatrem. What is it? What is it used for? Is Growth Hormone; Used for Pituitary dwarfism and osteoporosis.
Somatropin. What is it? What is it used for? Is Growth Hormone; Used for Pituitary dwarfism and osteoporosis.
Octreotide. What is it? What is it used for? Somatostatin; Used for acromegaly, carcinoid and secretory GI tumors.
Cosyntropin. What is it? What is it used for? Is ACTH; Used for infantile spasms.
Leuprolide. What is it? What is it used for? Is GnRH; Used for endometriosis and prostate carcinoma (repository form)
Nafarelin. What is it? What is it used for? Is GnRH; Used for endometriosis and prostate carcinoma (repository form)
Urofollitropin. What is it? What is it used for? Is FSH; Used for hypogonadal states
Placental HCG. What is it? What is it used for? Is LH; Used for hypogonadal states
Menotropins. What is it? What is it used for? Is LH and FSH; Used for hypogonadal states
Pergolide. What is it? What is it used for? is dopamine; Used for hyperprolactinemia
Bromocritpine. What is it? What is it used for? Dopamine receptor antagonist; Used for hyperprolactinemia
Oxytocin. What is it used for? Used for labor induction
Desmopressin. What is it? What is it used for? Vasopressin (ADH); V2 selective; Used for neurogenic (pituitary) diabetes insipidus, Hemophilia A (inc factor 8 from liver), von Willebrand dz (inc vWF from endothelium)
What is the mechanism of PTU and Methimazole? inhibits iodination of the tyrosine residues on thyroglobulin
What is thyroglobulin? the storage form of thyroid hormones
What is the effect of high levels of iodide on thyroid synthesis? High levels of iodide will inhibit the formation of DIT, T3 (DIT + monoIT), and T4 (DIT + DIT); will also inhibit the proteolytic release of T4 nd T3 from thyroglobulin
What does high-dose ipodate do? Inhibits the proteolytic release of T3 and T4 from thyroglobulin; in peripheral tissues, inhibits the conversion: T4 --(5'deiodinase)--> T3 (much more active than T4)
What are some side effects of PTU and methimazole? 1. common: maculopapular rash, 2. dec prothrombin (anti-platelet actions) 3. hypersensitivity, 4. immune-based arthralgia, 5. jaundice, 6. lupus, 7. vasculitis
PTU and methimazole: which drug crosses the placental barrier? both do
What is Lugol's solution? KI + Iodine --> Iodide. Possible use in thyrotoxicosis (hypermetabolic clinical syndrome resulting from serum elevations in thyroid hormone levels)
Can you use Iodide as a long term therapy for hyperthyroidism? No because the thyroid gland "escapes" from the effects of increased iodide after 1 to 14 days (hi iodide inhibits the proteolytic release of T3 and T4 from thyroglobulin as well as inhibits the coupling rxns to form DIT)
Prednisone and dexamethasone are what? glucocorticoids
Fludrocortisone is what? mineralocorticoid
Are infection, shock, and trauma adrenal-rich or adrenal-insufficient states? adrenal insufficiency -- need supplementation
What is the treatment for adrenal hyperplasia? Give steroids --> negative feedback on the anterior pituitary --> inhibition of ACTH release
What is Addison disease and how to treat? Addison - adrenal insufficiency - not enough cortisol and/or aldosterone (weight loss, muscle weakness, fatigue, low blood pressure, and sometimes darkening of the skin in both exposed and nonexposed parts of the body); treat by giving steroids -- whateve
Spironolactone blocks Aldosterone and androgen receptors
Mifepristone RU 486 - blocks glucocorticoid and progestin receptors
Metyrapone blocks 11-hydroxylation to make the glucocorticosteroids (corticosterone and cortisol)
ketoconazole Interferes with synthesis of some enzymes that make the glucocorticoids (interferes with the fungal synthesis of ergosterol, a constituent of cell membranes and some enzymes)
Premarin conjugated estrogens from horses
Ethinyl estradiol estrogen - steroid
mestranol estrogen - steroid
diethylstilbestrol DES - nonsteroidal
What happens to bone resorption and parathyroid hormone in hormone replacement therapy? decreases bone resorption (halts bone loss) and decreases release of parathyroid hormone (decreases bone resorption and osteoclasts' breaking down of bone)
Discuss uterine bleeding and estrogen. Give estrogen to control acute, uncontrolled, heavy uterine bleeding
Discuss acne and estrogen. Monthly surges of estrogen --> oily skin and acne. Give OCPs with estrogen to balance out the estrogen levels and prevent surges that would cause acne.
Discuss prostate cancer and estrogen. Estrogen is therapy for postate cancer
What are general adverse effects of being on estrogen therapy? nausea, breast tenderness, endometrial hyperplasia, inc in gall bladder disease, cholestasis (dec bile formation or flow), migraine
How does estrogen therapy affect coagulation? dec antithrombin III --> more coagulation; at high dose, increases the hepatic synthesis of factors 2, 7, 9, 10
How does estrogen therapy affect risk of cancer in women? increases risk for endometrial and breast cancers. Can decrease risk for endometrial cancer by adding progestins
What if a breastfeeding woman takes DES while breastfeeding? Inc vaginal adenocarcinoma in offspring
anastrozole aromatast inhibitor --> decrease estrogen synthesis
What is anastrozole used for? Breast cancer
Danazole inhibits ovarian steroid synthesis --> dec estrogen
What is danazole used for? endometriosis and breast fibrocystic disease
Clomifene Decreases feedback inhibition --> inc FSH and LH --> inc ovulation --> pregnancy; used as a fertility drug
What is adverse effect of clomifene? Multiple births
What are SERMs? selective estrogen receptor modulators
Name 2 SERMs Tamoxifen and Raloxifene
Describe tamoxifen effects on bone, breast, and endometrium. Agonist at bone; antagonist at breast; partial agonist at endometrium
People taking tamoxifen are at increased risk of what cancer? increased risk of endometrial cancer
Describe raloxifene effects on bone, breast, and uterus. agonist at bone; antagonist at breast and uterus
People taking raloxifene are at increased risk of what cancer? when used in menopause, no increase cancer risk
What is medroxyprogesterone? Progesterone used in depot contraception (intramuscular every 3 months)
What is norethindrone? Progesterone with some androgenic activity (hirsutism - inc hair growth - and acne)
What is norgestrel? Progesterone with some androgenic activity (hirsutism - inc hair growth - and acne); implant - 5 years
T or F: hormone replacement therapy of progesterone + estrogen decreases the risk of endometrial cancer TRUE
What are some adverse effects of using progesterone? 1. lipids: dec HDL & inc LDL, 2. glucose intolerance (some resistance to insulin --> higher blood glucose), 3. breakthrough bleeding, 4. androgenic (hirsutism & acne), 5. antiestrogenic (beneficial effects of estrogen on lipids are reduced w progestins)
What effect does estrogen have on lipids? increases serum HDL and decreases LDL
What drug is a progesterone receptor antagonist? Mifepristone - abortifacient, used with prostaglandins (causes contraction of uterine smooth muscle to expel trophoblast)
How do oral contraceptives work? suppress the mid-cycle LH surge
People on what types of meds should be advised that their OCPs will be less effective? Those on antimicrobials or any other drug that induces the CYP450 system --> increase OCP metabolism --> OCPs less effective
Name some of the benefits of taking OCPs 1. dec risk of endometrial and ovarian cancer, 2. dec dysmenorrhea, 3. dec endometriosis, 4. dec PID, 5. dec osteoporosis
What is endometriosis? tissue that looks and acts like the lining of the uterus grows outside of the uterus in other areas; this "misplaced" tissue can cause pain, infertility (not being able to get pregnant), and very heavy periods
What is dysmenorrhea? severe uterine pain during menstruation that limits nl activities
What is PID? Pelvic Inflammatory Disease; generic term for inflammation of the female uterus, fallopian tubes, and/or ovaries as it progresses to scar formation with adhesions to nearby tissues and organs
What are the effects of using testosterone or other androgens? 1. inc muscle mass, 2. inc RBC's, 3. dec nitrogen excretion (keep to build more muscle mass!)
What are the adverse effects of using testosterone or other androgens? 1 excessive masculinization, 2. premature closure of epiphysis, 3. cholestatic jaundice, 4. aggression, 5. dependence, 6. "roid rage"
What is Flutamide? androgen receptor blocker; used for prostate cancer
What is Leuprolide? GnRH analog -- stimulates increased release of LH and FSH initially; then the non-pulsatile presence of GnRH suppresses release of both LH and FSH; used in repository form for prostate cancer
What is Finasteride? 5-alpha reductase inhibitor -- used for BPH and male pattern baldness. Inhibition of 5-alpha reductase results in decreased production of DHT and increased levels of testosterone.
What is 5-alpha reductase? the enzyme that converts testosterone to dihydrotestosterone (DHT) -- more potent form of testosterone. DHT is produced only in skin, seminal vesicles, prostate and epididymis.
Why use Finasteride in BPH? In benign prostatic hyperplasia, dihydrotestosterone acts as a potent cellular androgen and promotes prostate growth - inhibiting the enzyme reduces the excessive prostate growth
Why use Finasteride in male pattern balding? In alopecia, pattern-baldness is one of the effects of androgenic receptor activation. Reducing the levels of dihydrotestosterone thus reduces alopecia.
What is Ketoconazole? inhibits synthesis of ergosterol -- component of fungal cell walls and enzymes that make androgens. Used in prostate cancers that are positive for androgen receptors.
Talk about ketoconazole use in prostate cancer ketoconazole blocks testosterone made by the testicles, as well as androgens made by the adrenal gland.
Created by: christinapham
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