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USMLE - Pharm
Kaplan Section 7 - Endocrine 1
Question | Answer |
---|---|
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. |