Kaplan Section 7 - Endocrine 1
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| GnRH | Gonadotropin releasing hormone; from hypothalamus; stimulates LH and FSH release from anterior pituitary
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| TRH | thyrotropin releasing hormone; from hypothalamus; stimulates TSH and prolactin release from anterior pituitary
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| Dopamine | from hypothalamus; inhibits prolactin release from anterior pituitary
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| GHRH | growth hormone releasing hormone; from hypothalamus; stimulates growth hormone (GH) release from anterior pituitary
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| Somatostatin | from hypothalamus; inhibits GH and TSH release from anterior pituitary
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| CRH | corticotropin releasing hormone; from hypothalamus; stimulates ACTH release from anterior pituitary
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| 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
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| Name the 6 Anterior Pituitary hormones | FLAT PiG: FSH, LH, ACTH, TSH, Prolactin, GH
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| Somatrem. What is it? What is it used for? | Is Growth Hormone; Used for Pituitary dwarfism and osteoporosis.
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| Somatropin. What is it? What is it used for? | Is Growth Hormone; Used for Pituitary dwarfism and osteoporosis.
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| Octreotide. What is it? What is it used for? | Somatostatin; Used for acromegaly, carcinoid and secretory GI tumors.
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| Cosyntropin. What is it? What is it used for? | Is ACTH; Used for infantile spasms.
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| Leuprolide. What is it? What is it used for? | Is GnRH; Used for endometriosis and prostate carcinoma (repository form)
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| Nafarelin. What is it? What is it used for? | Is GnRH; Used for endometriosis and prostate carcinoma (repository form)
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| Urofollitropin. What is it? What is it used for? | Is FSH; Used for hypogonadal states
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| Placental HCG. What is it? What is it used for? | Is LH; Used for hypogonadal states
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| Menotropins. What is it? What is it used for? | Is LH and FSH; Used for hypogonadal states
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| Pergolide. What is it? What is it used for? | is dopamine; Used for hyperprolactinemia
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| Bromocritpine. What is it? What is it used for? | Dopamine receptor antagonist; Used for hyperprolactinemia
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| Oxytocin. What is it used for? | Used for labor induction
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| 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)
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| What is the mechanism of PTU and Methimazole? | inhibits iodination of the tyrosine residues on thyroglobulin
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| What is thyroglobulin? | the storage form of thyroid hormones
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| 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
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| 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)
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| 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
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| PTU and methimazole: which drug crosses the placental barrier? | both do
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| What is Lugol's solution? | KI + Iodine --> Iodide. Possible use in thyrotoxicosis (hypermetabolic clinical syndrome resulting from serum elevations in thyroid hormone levels)
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| 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)
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| Prednisone and dexamethasone are what? | glucocorticoids
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| Fludrocortisone is what? | mineralocorticoid
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| Are infection, shock, and trauma adrenal-rich or adrenal-insufficient states? | adrenal insufficiency -- need supplementation
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| What is the treatment for adrenal hyperplasia? | Give steroids --> negative feedback on the anterior pituitary --> inhibition of ACTH release
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| 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
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| Spironolactone | blocks Aldosterone and androgen receptors
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| Mifepristone | RU 486 - blocks glucocorticoid and progestin receptors
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| Metyrapone | blocks 11-hydroxylation to make the glucocorticosteroids (corticosterone and cortisol)
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| 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)
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| Premarin | conjugated estrogens from horses
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| Ethinyl estradiol | estrogen - steroid
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| mestranol | estrogen - steroid
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| diethylstilbestrol | DES - nonsteroidal
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| 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)
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| Discuss uterine bleeding and estrogen. | Give estrogen to control acute, uncontrolled, heavy uterine bleeding
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| 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.
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| Discuss prostate cancer and estrogen. | Estrogen is therapy for postate cancer
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| 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
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| How does estrogen therapy affect coagulation? | dec antithrombin III --> more coagulation; at high dose, increases the hepatic synthesis of factors 2, 7, 9, 10
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| 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
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| What if a breastfeeding woman takes DES while breastfeeding? | Inc vaginal adenocarcinoma in offspring
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| anastrozole | aromatast inhibitor --> decrease estrogen synthesis
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| What is anastrozole used for? | Breast cancer
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| Danazole | inhibits ovarian steroid synthesis --> dec estrogen
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| What is danazole used for? | endometriosis and breast fibrocystic disease
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| Clomifene | Decreases feedback inhibition --> inc FSH and LH --> inc ovulation --> pregnancy; used as a fertility drug
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| What is adverse effect of clomifene? | Multiple births
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| What are SERMs? | selective estrogen receptor modulators
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| Name 2 SERMs | Tamoxifen and Raloxifene
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| Describe tamoxifen effects on bone, breast, and endometrium. | Agonist at bone; antagonist at breast; partial agonist at endometrium
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| People taking tamoxifen are at increased risk of what cancer? | increased risk of endometrial cancer
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| Describe raloxifene effects on bone, breast, and uterus. | agonist at bone; antagonist at breast and uterus
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| People taking raloxifene are at increased risk of what cancer? | when used in menopause, no increase cancer risk
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| What is medroxyprogesterone? | Progesterone used in depot contraception (intramuscular every 3 months)
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| What is norethindrone? | Progesterone with some androgenic activity (hirsutism - inc hair growth - and acne)
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| What is norgestrel? | Progesterone with some androgenic activity (hirsutism - inc hair growth - and acne); implant - 5 years
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| T or F: hormone replacement therapy of progesterone + estrogen decreases the risk of endometrial cancer | TRUE
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| 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)
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| What effect does estrogen have on lipids? | increases serum HDL and decreases LDL
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| What drug is a progesterone receptor antagonist? | Mifepristone - abortifacient, used with prostaglandins (causes contraction of uterine smooth muscle to expel trophoblast)
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| How do oral contraceptives work? | suppress the mid-cycle LH surge
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| 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
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| 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
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| 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
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| What is dysmenorrhea? | severe uterine pain during menstruation that limits nl activities
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| 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
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| 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!)
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| 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"
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| What is Flutamide? | androgen receptor blocker; used for prostate cancer
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| 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
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| 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.
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| 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.
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| 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
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| 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.
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| 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.
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| Talk about ketoconazole use in prostate cancer | ketoconazole blocks testosterone made by the testicles, as well as androgens made by the adrenal gland.
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