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240 Cards in this Set
- Front
- Back
thyroid big picture purpose
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"metabolism, oxygen consumption, cardiac contractility"
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thyroxine
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"T4; 3, 5, 3', 5'; main form;
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triiodothyroine
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"T3; 3, 5, 3'; less common form; biologically active thyroid hormone with only 3 iodine"
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reverse triiodothyronine
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"rT3; 3, 3', 5'; biologically inactive form"
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protirelin
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"TRH; tests TSH release from pituitary; SE: diaphoresis, anxiety"
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thyrotropin
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TSH; stimulates thyroid gland; used to test thyroid function; SE: same as protirelin
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hashimoto's disease
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"autoimmune, hypothyroidism"
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cretinism
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"low thyroid function since birth; short, stocky, thyroid treatment helps, if not done within first 2 months mental retardation results"
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myxedema
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hypothyroidism in adults
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grave's disease
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"hyperthyroidism, eyes protude because of edema in eye sockets (exophthalmic goiter), treat by removal or destruction of some thyroid tissue by surgery or radiation."
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iodine transport
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high concentration in thyroid is due to Na/I symporter in basolateral membrane
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thyroxin production
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"iodine combines with tyrosine to form mono and di-iodotyrosine (MIT/DIT), incorporated into thyroglobulin, TSH stimulates proteolysis of thyroglobulin and exocytosis."
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thyroid binding globulin
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binds 99% of circulating T3/T4
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T3 mech of action
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"enters cell, migrates to nucleus, interacts with receptor to induce gene transcription"
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hyperthyroidism symptoms
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"warm, sweating, exophthalmus, diplopia, hyperactivity, weakness, hypercalcemia, polyuria, increased erythropoiesis, anemia, increased sex hormones, infertility, menstrual abnormality, dyspnea, hunger, "
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hypothyroidism symptoms
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"pale, cold intolerance, drooping eyelids, puffy tongue, bradycardia, pleural effusion, hypoventilation, decreased appetite, constipation, lethargy, slowed mental process, oliguria, decreased erythropoiesis, anemia, hypermenorhea, hypogonadism, infertility, decreased libido, "
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thyroid agonists
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"desiccated thyroid, liotrix, liothyronine(T3), levothyroxine(T4); well absorbed"
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thyroid replacement SE
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"decreased bone density, cardiovascular, CNS, GI, misc"
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iodide uptake inhibitors
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"perchlorate, thiocynanate, pertechnetate; SE: aplastic anemia, methamoglobinemia, uncoupling of oxidative phosphorylation"
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iodine organification inhibitors
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"iodides, thioamines(propylthiouracil, methimazole); SE: rash, lupus-like syndrome, agranulocytosis; propylthiouracil prefered in pregnancy"
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iodides
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"saturated solution, Lugol's solution, decreases organification and release of T3/T4; used for short term thyroid inhibition; SE: iodine toxicity, swollen salivary glands and mucous membanes"
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gonadal hormone classes
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estrogens; progestins; androgens
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progesterone production
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released by corpus luteum during 2nd part of cycle
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androgen production
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"primarily produced by testes, small amount by adrenal cortex"
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big picture feedbcak cycle
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"HYPOTHALAMUS[GnRH (pulsatile)]-> ANT PITUITARY[LH/FSH]-->ovaries/testes [ estrogen/testosterone] --> inhibits ANT PIT and HypoThal; inhibin inhibits FSH production, activin opposite"
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leydig cell
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LH stimulated testes cell which produces testosterone
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sertoli cell
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"FSH stimulated testes cell, makes androgen binding protein"
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thecal cell
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"LH stimulated ovary cell, androgen synthesis"
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granulosa cell
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"FSH stimulated ovary cell, increased aromatase production which converts androgen to estrogen"
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androstenetione
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precursor to estradiaol (which goes to estrogen) and testosterone
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aromatase
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converts testosterone to estrogen
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cholesterol
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starting molecule for steroid synthesis pathways
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estrogens
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"estrone, estriol, estradiol; released into blood bound to SHBG; mechanism is through steroid receptors, bind to DNA to increase transcription; maturation in females; growth, closure of epiphyses of long bones; uterine, endometrial, hair growth; decrease rate of bone resorption; hepatic-increase SHBG release, increase clotting factors, increase HDL VLDL, decrease LDL"
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nonsteroidal estrogenic compounds
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"diethylstilbestrol, bisphenol A, genistein"
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alpha2globulin
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sex hormone binding globulin (SHBG)
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estradiaol
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"simplest estrogen, only H on side chains"
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progestins
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"progesterone is predominant form; catabolic, increase lipoprotein lipase activity, fat deposition; increased insulin release and efficiency; increased protein breakdown; antagonism of mineralocorticoid receptors; hyperthermia; secreted by corpus luteum in 2nd pahse of menstruation; density of progestin receptors is controlled by estrogen"
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progesterone analogs
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"medroxyprogesterone(Oac and CH3 group added), norethindrone, norgestrel, desogestrel, ethylnodiol, hydroxyprogesterone, levonorgestrel, megestrol, norethynodrel, norgestimate, "
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androgens
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produced by testes(95%) and adrenal glands; 98% plasma protein bound (SHBG and albumin); hormone receptor mech of action; scrotal growth and decent; increased bone growth and closure of epiphyses; decrease HDL increase LDL; increase clotting factors; anabolic - positive nitrogen balance
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androgen uses
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"hypogonadal/hypogonadism; in females-breast engorgement, endometriosis, osteoporosis, breast cancer; muscle wasting(AIDS, cancer, burn victim), athletes"
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androgen side effects
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"acne, gynemastia, aggression, edema, benign prostatic hyperplasia, prostate cancer, liver/heart?"
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testosterone analogs
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"methyltestosterone, fluoxymesterone, methandrostenolone, oxymethalone, ethylestrenol, oxandrolone, nandrolone, stanozolol, dromostanolone"
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17alpha-alkylated androgens
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"greater anabolic effects than androgen effects; SE - suppress gonadotropic secretion, decreases endogenous testosterone, testicular size diminish, high doses of testost converted to estrogen; hepatoxicity; increase LDL decrease HDL"
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testosterone ester group
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"slows absorption; testosterone enanthate, t. cypionate, t. undecanoate"
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testosterone administration
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injection (t. enanthate) - highest peaks; testosterone patch - intermediate peak; testosterone gel - most constant
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17alpha group
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"more androgenic, more hepatotoxic; methyltestosterone, oxandrolone, stanozolol, fluoxymesterone, danazol"
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finasteride
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"proscar/propecia; inhibits 5alpha reductase, for treating BPH; SE decrease libido, decreased ejaculate volume, impotence, breast tenderness; also low dose can be used for male pattern baldness (propecia); can be absorbed through skin-teratogenic"
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5alpha reductase
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converts cellular testosterone to dihydroxytestosterone which activates cellular androgen receptors; androgen receptors act at DNA promoter regions
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dihydrotestosterone
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"produced from testosterone by 5alpha-reductase; acts on androgen receptors for differentiation of external genitalia, maturation, prostatic diseases, hair follicle growth and baldness"
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testosterone
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"produced by conversion from androstenedione by 17beta HSD; differntiation of internal genitalia, wolffian development, muscle mass, erythropoiesis, bone"
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BPH
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"benign prostate hypertrophy, too high testosterone"
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estrogen replacement therapy
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"used to treat vasomotor disturbances (hot flashes) in post menopausal women; alleviates effects of urogenital atrophy, decreased incidence of colon cancer, prevention of bone loss; SE-breast cancer, stroke, heart disease, cancer"
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oral contraception therapy
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"mono/bi/triphasic; differentiated by form, dose, and time of progestin admin and estrogen dose; mechanism - try to mimic what is normally happening in the body; pharmacodynamic response - 1. changes endometrium, preventing implantation; 2. increases mucous viscosity preventing sperm from entering; 3. altering times; OCT reduces overall ovarian function - returns after stopping drug"
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OCT side effects
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"anatomy changes (breast enlargement, uterine hypertrophy, decreased lactation); edema (has aldosterone like effects of water retention, however, progestin as an aldosterone antagonist slightly offsets effect); hematological (increased thromboembolism, especially in hypertensive, smoking, over 35) "
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progesterone only contraceptive
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"available as a shot which lasts three months; mechanism- blocks ovulation in 60-80% of the cycle; effectiveness also though to thickening of mucous-prevent implantation, slows down sperm; SE 1. breakthrough bleeding 2. amenorhea(no menstruation), longer bleeding, longer menstrual cycle "
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SERM
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"selective estrogen receptor modifiers; tamoxifen, raloxifene; bind to estrogen receptor which controls gene transcription; do not allow cofactor Y to take part in gene transcription like estrogen does; can both inhibit and promote gene expression"
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mifepristone
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"mifeprex, RU 486; antagonist at progestin receptor; blocks gene transcription effects from progesterone; used as post-coital contraceptive or aborticient, up to 49 days past last menstruation; SE: nausea, diarhea, headache, bleeding, cramping"
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aromatase inhibitors
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"exemestane, formestane, anastozole, letrozole, aminogluthimide"
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aminoglutethimide
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"cytadren; aromatase inhibitor, also inhibits adrenal steroid hormone synthesis, depression of glucocorticoid and aldosterone synthesis; used to treat Cushing's"
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anastrazole
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arimidex; selective aromatase inhibitor through competitive inhibition
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letrozole
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femara; selective aromatase inhibitor; competitive
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exemestane
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"aromasin; selective aromatase inhibitor; suicide inhibitor (others are competitive); used for metastatic breast cancer, hot flashes, rash"
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tamoxifen
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"nolvadex; SERM; breast cancer, adjuvant treatment, prophylaxis in high risk women; SE-hot flahses, blood clots, uterine cancer"
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raloxifene
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"SERM; osteoporosis; SE: hot flashes, thromboembolism, NOT uterine cancer"
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fulvestrant
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faslodex; pure estrogen antagonist; breast cancer for P resistant to tamoxifen; SE hot flashes
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clomiphene
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"clomid; inhibits estrogen binding in the anterior pituitary -> causes increased secretion of GNRH, increased estrogen and ovulation; used to treat infertility; SE: hot flashes, twins"
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androgen receptor antagonists
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"flutamine, bicalutamide, nilutamide, spironolactone"
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flutamide
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eulexin; androgen receptor antagonist
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bicalutamide
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casodex; androgen receptor antagonist
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nilutamide
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"nilandron; androgen antagonist; potent; SE: alcohol intolerance, loss of sexual desire/performance, constipation, visual changes,diziness, insomnia, loss of body hair, gynecomastia, liver failure"
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spironolactone
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diuretic/antiandrogen; SE: gynecomastia
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testosterone for women
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"high dose in female causes masculinization, low dose for sexual disfunction; SE air growth, acne, salt and water retention"
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abarelix
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plenaxis; GnRH antagonist; used for prostrate cancer; does not cause a transient increase in sex steroid production
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ketoconazole
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"nizoral; blocks synthesis of steroid hormones; SE: hepatotoxic, "
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danazol
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"danocrine; GnRH secretion inhibitor; lowers FSH LH; used for endometriosis, fibrocystic breast disease; SE: acne, weight gain, edema, hair growth, flushing, sweating, depression, vaginal, amenorrhea, spotting"
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vasomotor disturbance
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hot flash in postmenopausal women; treated with estrogen replacement therapy
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estrogen replacement therapy benefits and SE
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"lessens effects of urogenital atrophy, decreases colon cancer, prevents bone loss; SE: increase in breast cancer, stroke, coronary heart disease, endometrium cancer;"
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difference in Estrogen Replacement Therapy for women with uterus and women without
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progestin is included in women with a uterus to lower incidence of endometrium cancer
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osteoclast
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breaks down bone; increases PO4 and Ca2 plasma levels; dissolving bone - resorption
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osteoblast
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forms new bone
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epiphyseal plate
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"place where growth occurs on proximal epiphysis, plate fuses in adulthood and bone growth no longer"
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calcium physiological importance
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"membrane current, release of storage vessicles, muscle contraction, blood coagulation, 2nd messenger"
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menopause & Ca
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increased Ca intake necessary in women because of loss of estrogen
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parathyroid hormone (PTH)
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stimulates both mainly resorption (break down) and accretion(build) of bone; increases reabsorbtion of Ca in the kidneys; increases conversion of vitamin D to active form (dihydroxy)
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tetany
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disease state in which body shakes from continuous muscle contraction; increased excitability of cells; low Ca levels in blood
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calcitonin
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polypeptide; released from thyroid; inhibits break down of Ca in bone by osteoclasts; Ca and PO4 homeostasis
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vitamin D
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"synthesized from cholesterol by reactions in skin liver and kidneys; calcitriol(1,25 dihydroxy vitamin D) is the active form"
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TGF-beta
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"together with shear stress and PTH, makes precursor osteoblast express RANKL receptor"
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phosphate physiological importance
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"metabolism, enzyme regulation, tissue component (80% in bone); not absorbed well thrgouh GI - acts as a mild laxative"
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hypercalcemia
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"saline diuresis (IV to flush calcium out of system), biphosphonates inhibit break down of bone, gallium nitrate (may be nephrotoxic), glucocorticoids (may cause osteoporosis over long term)"
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hypocalcemia
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"two forms: hypomagnesemia (treat with magnesium), unknown with normal Mg (treat with oral calcium and vitamin D)"
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hyperphosphotemia
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occurs in renal failure; treat with aluminum hyrdoxide antacids
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osteoporosis fractures
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"hip, neck of femur, weak spots "
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rickets
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lack of vitamin D; must determine which step of vitamin D is deficient
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pagat's disease
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"uncontrolled osteoclastic bone resorption, etiology unknown leads to osteoporosis; treat with resorption inhibitors"
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chronic renal failure
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"increased phosphate retention, and reduced Ca as secondary effect from vit D reduction; which leads to hyperparathyroidism"
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calcitriol
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"1,25 dihydroxy vitamin D; active form; activation of osteoblasts; Ca and PO4 homeostatis promotes resorbtion in kidney; prodcution stimulated by PTH"
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calcifediol
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25 hydroxy vitamin D3; converted from Vit D3 in liver
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cholecalciferol
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"Vit D3, produced in skin by UV light converting cholesterol"
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hyperparathyroidism
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"response to renal failure; decreased vit D production (leading to decreased Ca) and increased phosphate retention activates parathyroid, increase in PTH, which can lead to osteomalacia"
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osteoporosis
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"low bone mass; low sex hormone level induced; long term use of glucocorticoids and some anticonvulsants can cause; affects 44 million americans; excessive alcohol intake, smoking, risk factors"
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pathologic basis of osteoporosis
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increased production of cytokines; longer lifespan of osteoclasts; shrter lifespan of osteoblasts; shorter life span of osteocytes; --> fragile bone
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antiresorptive agents
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"biphosphonates, calcitonin, estrogen/SERMs"
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biphosphonates
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"the -dronates; mech: inhibit osteoclast resorption; postmenopausal women, elderly men, vertebral/hip fractures, hypercalcemia; SE: hypocalcemia, GI irritation, esophageal ulceration, osteomalacia"
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etidronate
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"didronel; biphosphanate, for osteoporosis; SE: osteomalacia, hyperphaosphatemia"
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osteomalacia
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"defective bone mineralization; pain, weakness, fragile bones; rickets, caused by vitamin D deficiency"
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ibandronate
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boniva; biphosphanate; more potent because of amine group (given once a month)
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alendronate
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fosamax; biphosphanate
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risedronate
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actonel; biphosphanate
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zoledronate
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zometa; biphosphanate
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pamidronate
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aredia; biphophanate
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estrogen
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"does not increase bone mass; prevents bone loss; inhibit cytokines which recruit osteoclasts; SERMS also work (raloxifene - estrogen agonist in bone, antagonist in breast)"
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calcitonin
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"miacalcin, fortical; from salmon; inhibits resorption (break down) of bone; mech: G-protein receptor on osteoclasts, decreasing resorptive activity; use: paget's disease, osteoporosis, hypercalcemia: SE: allergy, flushing of face, frequent urination, nasal version gives runny nose"
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bone anabolic agents
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"vitamin D, calcium, fluoride, PTH"
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fluoride
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"mitogen for osteoblasts; increase dense of bone, but more brittle; increase trabecular bone; not used"
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teriparatide
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"forteo;injectable PTH; mech: increases bone formation in spine and hip; only use for 2 years; SE: nausea disiness, leg cramps"
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plicamycin
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"mithramycin; chemo drug; mech: decreases protein synthesis, decreases bone loss; used for testicular cancer, paget's disease, hypercalcemia; SE: antineoplastic"
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pancreas cell types
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alpha - glucagon; beta - insulin; delta - somatostatin; phi - pancreatic polypeptide
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ketoacidosis
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metabolic acidosis by high concentration of ketone bodies; common in type I diabetes due to breakdown of fat and protein
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type I diabetes
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"disease in which almost no pancreatic beta cells; possibly autoimmune; leads to hyperglycemia, ketoacidosis; sugar in urine is not a good indicator because very high levels are needed."
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alpha glucosidase
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"enzymes which break down complex carbohydrates; amylase, maltase"
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alpha glucosidase inhibitors
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"acarbose, miglitol;drugs which block starch binding to prevent digestion of complex carbs; used with type II diabetics; SE: GI effects, flatulence; treat hypoglycemia with ingestion of monosacharides; no chance of hypoglycemia"
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B cell metabolism
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"glucose enters cell, increases metabolism, increase in ATP, induces insulin secretion; sulfonylureas, melitinides promote secretion; diazoxide inhibits secretion"
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insulin effects on cells
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promotes cell absorption of glucose; adipose cell - also promotes glucose converstion to triglyceride; liver cell - promotes glucose conversion to glycogen
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thiazolidinediones
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"insulin sensitizer; pioglitazone, rosiglitazone; promotes glucose conversion to triglyceride in adipose cells by bonding to PPARgamma; promotes glucose transport; hepatotoxic, increase BP; chance of hypoglycemia"
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biguanides
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insulin sensitizer; metformin (glucophage); inhibit gluconeogenesis in liver cells and thus lower blood glucose levels; SE: increases BP; inhibits folic acid and B12 absorption
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insulin molecule activation
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activated by cleavage of polypeptide proinsulin at two points leaving an A and B chain connected only by two disulfide bonds.
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insulin secretagogues
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"sulfonylurea & meglitinide - antidiabetic drugs that increase insulin release from beta cells; act by inhibiting K+ channel influx, depolarizing membrane, which opens voltage gated Ca2+ channels, Ca induces insulin granulae to fuse with external membrane."
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diazoxide
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"opposite of sulfonylurea, inhibits insulin release; K+ channel activator, primarily for treating hypertension; also decreases insulin release by decreasing depolarization in pancreatic beta cells, which in turn reduces Ca2+ influx which reduces insulin release; SE: nausea, vomiting, fluid retention"
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insulin receptor structure
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2 alpha and 2 beta subunits;
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insulin effects
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"glucose transport, increased glucose intake (glut4), glucose storage, mitogenesis, protein synthesis, glycogen synthesis, VLDL formation, increase lipoprotein lipase (freeing TG for uptake and storage), decrease conversion to ketoacids; store energy, prevent utilization of stored energy"
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hyperglycemia effects
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"peripheral vascular disease, retinopathy, nephropath, neuropathy"
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hypoglycemia effects
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"sympathetic discharge- tachycardia, sweating, convulsions, confusin, coma; treat conscious with sugar, unconscious with glucagon/glucose IV."
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insulin resistance
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"when normal amounts of insulin no longer produce sufficient response in fats, muscle, and liver cells"
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lipodystrophy
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abnormal or degenerative condition of adipose tissue; can occur at site insulin is repeatedly injected
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glucagon
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"~opposite of insulin; 29 AA peptide; produced in pancreas; normally released in response to hypoglycemia; binds to G-protein receptor, causes liver to convert glycogen to glucose and release it; SE: nausea; also used for beta blocker overdose; structure similar to secretin"
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HbA1c
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"glycosylated hemoglobin, gives measure of average blood glucose concentration over time, "
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sulfonylureas
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inculin secretagogue; mech: inhibits beta cell Mg/ATP pump; increases insulin; supresses glucose release from liver; increases insulin receptor #; increases glucose uptake; do not work on type I diabetics
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1st generation sulfonylureas drugs
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"tolbutamide, acetohexamide, tolazamide, chlorpropamide"
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2nd generation sulfonylureas drugs
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"glyburide, glypizide, glimepiride"
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glimepiride
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amaryl; insulin secretagogue; has different binding site but similar action
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sulfonylureas SE
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todo
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chlorpropamide
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insulin secretor; longest acting sulfonylrurea with distinctive renal only clearance
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repaglinide
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"prandin; short acting meglitinide insulin releaser; has unique binding site on K+/ATP channel (diff than sulfonylurea), closes channel and induces beta cell depolarization; fast onset; reduced hypoglycemia"
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nateglidine
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starlix; D-phenyalanine class of hypoglycemic agent; inhibits K+/ATP channel in beta cells; fast on off; increases insulin release when glucose available; low hypoglycemia
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incretin
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"Incretins are a type of gastrointestinal hormone that cause an increase in the amount of insulin released from the beta cells of the islets of Langerhans after eating, even before blood glucose levels become elevated. "
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exenatide
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"byetta, amylin; incretin mimetic; lizard saliva protein, increases cAMP in beta cells and stimulates insulin secretion, inhibits glucagon secretion, and slows gastric emptying, weight loss. 2x daily injection; used together with metformin or sulfonylurea"
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chromium
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trace element necessary for glucose utilization;
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lispro
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"humalog; rapid acting insulin analog; two AA order switched (B28,29) allows for faster absorption"
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aspart
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novolog; single AA substitution; rapid acting insulin analog
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glusine
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apidra; rapid acting insulin analog; 2 AA substitutions
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detemir
|
"levemir; insulin analog, has fatty acid inserted; long acting insulin analog (up to 24hrs)"
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rapid acting insulin analogs
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"lispro, aspart, glusine"
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intermediate acting insulin analogs
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"NPH, lente"
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long acting insulin analogs
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"ultralente, lantus, detimir"
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premixed insulins
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for both long and short effects; novo- hum-
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hypothalamus
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"regulates drives for hunger, sex, thirst, sleep; thermoregulation; controls release of pituitary hormones"
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anterior pituitary
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"derived from buccal ectoderm; portal system; synthesize and stores ACTH, TSH, prolactin, growth hormone, endorphins, FSH, and LH"
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posterior pituitary
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derived from neural ectoderm; stores antidiuretic hormone and oxytocin made by the hypothalamus
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superior hypophyseal artery
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goes top down from hypothalamus then anterior pit
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paraventricular/supraoptic nuclei
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hypothalamic neurons which connect to posterior pituitary and control hormone release
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inferior hypophyseal arterior
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goes top down through posterior pituitary
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GnRH
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released from hypothalamus to ant. Pituitary; pulsatile GnRH release causes LH/FSH secretion; continuous GnRH release inhibits LH/FSH secretion
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hypothalamus releasing hormones
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"corticotropin RF, thyrotropin RH (TRH, protirelin), GH RF (somatorelin), GH inhibitory (somatostatin, octreotide), prolactin RH, prolactin inhibitory (PRH, Dopamine), melanocyte stimulating hormone RF and IF."
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somatotropic hormones
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"monomeric proteins, GH, prolactin"
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glycoprotein hormones
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"LH, FSH, TSH"
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Pro-opiomelanocortin
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"ACTH, MSH"
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somatostatin
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"hypothalmic factor; inhibits GH, TSH, prolactin release from ant pit"
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TSH
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"induces thyroid to release thyroxin, triiodothyronine"
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ACTH
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induces adrenal gland to release cortisol and adrenal androgens
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LH/FSH
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"induces release of estrogen, testosterone, progesterone"
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adrenal gland
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"medulla - catecholamines(adrenalins), cortex - corticosteroids (cortisol, androgens, aldosterone)"
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growth hormone (GH)
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"peptide - amall and large forms due to alternative splicing; a protein binding to half GH increases half life 10x; affects liver, adipose, bone, muscles; release induced by GHRH and ghrelin, inhibited by SST and indirectly by IGF-1"
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ghrelin
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"produced in stomach and other organs; stimulates GH release, gastric emptying, hunger;suppresses fat utilization; increased cardiac output"
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GH release stimulators
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"dopamine, 5HT, alpha2adrenergic agonists, exercise, stress, hypoglycemia, protein meals; and of course GhRH and ghrelin"
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GH release inhibitors
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"beta adrenergic agonists, free fatty acids, IGF-1, somatostatin"
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primary deficiency/disease
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problem with target tisue
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secondary deficiency/disease
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problem with pituitary secretion
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tertiary deficiency/disease
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problem with tissues that act on pituitary (ie: hypothalamus)
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GH effects
|
"bone development/growth; increases bone mineral density; increase muscle mass; anti-insulin actions in adipocytes and muscle, increase lipolysis"
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GH deficiency effect
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"in children leads to short stature; in adults leads to cardiovascular problems, decreased muscle mass, decreased bone density, increased inflamation"
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GH deficiency diagnosis
|
inject hypothalmic releasing factors to see if GH released from pituitary
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somatropin
|
"recombinant GH; serostim, genotropin, humatrope, nutrophin"
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somatrem
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protropin; GH with an extra methionine
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uses of GH supplementation
|
"GH deficiency, turner's syndrome, praderwillie syndrome, short stature"
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excess GH effects
|
"leads to gigantism in children, acromegaly in adults - arthropathy, carpal tunnel synd., visceromegaly, glucose intolerance"
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oral glucose test
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tests GH excess; glucose challenge is supposed to suppress GH level
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somatostatin
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peptide cleaved to form two types; binds to Gi to inhibit cAMP accumulation; SST 14 and SST28 show specificity only to the SSTR 5 receptor subtype
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SST analogs
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show SSTR specificity; octreotide
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octreotide
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"sandostatin; SST analog; longer half life (1.5hr); SSTR2 & SSTR 5; used to treat acromegaly; SE: gallstones, bradycardia, arrythmia, diarhea, hyper/hypo glycemia, hypothyroidism"
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prolactin
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"ant. pit; promotes breast milk production; nipple suckling increases prolactin production; secretion induced by TRH, inhibited by dopamine; member of somatotropin family"
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excess prolactin syndrome
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"can be caused by hypothalmic, pituitary adenoma, hypothyroidism; renal failure; relatively common; dopamine receptor antagonists; leads to loss of libido and infertility; treat with dopamine agonists"
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bromocriptine
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"parlodel; dopamine agonist, inhibits release of prolactin; ergot alkaloid; SE: postural hypotension, nausea, psychosis"
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pergolide
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"permax; ergot derivative parkinson's drug, off label use for hyperprolactinemia; similar SE to bromocriptine"
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cabergoline
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dostinex; hyperprolactinemia drug; long half life ergot derivative; more specific to D2 receptors; better at reducing prolactin levels.
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quinagolide
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norprolac; hyperprolactinemia drug; non ergot; D2 agonist
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oxytocin production
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"hormone produced in hypothalamus, stored in posterior pituitary; also produced by female reproductive organs;"
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oxytocin structure
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"nonapeptide, differs from vassopressin by 1 AA"
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oxytocin
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"stimulates uterine contractions, and contraction of breast myoepithelium for milk let down; oxytocin release stimulated by dilation of cervix, suckling, estradiol; used to induce labor; "
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oxytocin SE:
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"antidiuretic - can lead to water intoxication; vasodilation - hypotension, tachycardia"
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vasopressin
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ADH; promotes reabsorption of water from collecting duct in kidneys; release is controlled by nerve receptor cells in hypothalamus;
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vasopressin receptors
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"V1a - widespread; V1b - ant pituitary, adrenal medulla; V2 - collecting ducts"
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diabetes insipidus
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"inability of hypothalmic neurons to produce or secrete ADH (neurogenic); or inability of nephron to respond to ADH (nephrogenic); thirst, polydipsia, polyuria"
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desmopressin
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"synthetic ADH; longer half life and little effect on BP; used to treat bedwetting; SE: hyponatremia, water intoxication, rhinitis, abdominal cramps"
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adrenal cortex
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"steroid hormones(glucocorticoids, mineral corticoids, adrenal androgens); salt balance, metabolism, androgenic"
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adrenal medulla
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"adrenalin, noradrenalin"
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ACTH
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more released during times of physical and emotional stress
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zona glomerulosa
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"most superficial layer of adrenal cortex, aldosterone"
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aldosterone
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"mineral corticoid hormone produced in superficial adrenal cortex; causes kidney to conserve sodium and water, secrete potassium; reduced in Addison's disease, increased in Conn syndrome"
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aldosterone mechanism
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"acts on principle cells of distal renal tubules; diffuses through cell membrane, binds to mineralcorticoid receptor in cystol, is transported to nucleus, binds to mineral corticoid response elements on gene promoters, increases Na+/K+ ATPase expression in distal cells"
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angiotensin II
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peptide hormone causes vasoconstriction; encourages release of aldosterone in the adrenal cortex
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ketoconozol
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antifungal that inhibits whole hormone synthesis pathway in the adrenal cortex
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renin-angiotensin-aldosterone system
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"kidney baroreceptors, low pressure causes release of renin, leads to reuptake of water"
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spironolactone
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"competitive mineralcorticoid antagonist, also inhibits androgen and progesterone receptors; used as antihypertensive and for heart failure; SE: gynecomastia"
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eplerenone
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specific mineralcorticoid antagonist; used as antihypertensive agent and heart failure
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dehydroepiandrosterone
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DHEA; adrenal cortex androgen; prohormone of testosterone; no research shows it increases testosterone in men; important source of testosterone in females
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steroid 21 hyrdoxylase
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enzyme in both the mineralcorticoid and glucocorticoid adrenal hormone pathways (but not for testosterone);
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adrenal cortex feedback
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ACTH-->adrenal cortex-->glucocorticoid-->reduced pituitary ACTH release
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cortisol
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"hydrocortisone; glucocorticoid; binds tightly to plasma proteins (CBG, albumin)"
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glucocorticoid metabolic effects
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"cortisol; increase gluconeogenesis by increased uptake of AA by liver; decreased utilization of dietary glucose; stimulates storage of glucose as glycogen; increase protein breakdown; activates lipolysis, decreased uptake in adipose (redistribution of fat - buffalo hump, moon face, skinny extremities; gives you energy"
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glucocorticoid CNS effects
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"decreased seizure threshold; pychosis, paranoia, aggression, depression, euphoria"
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glucocorticoid GI effects
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"increase gastric acid and pepsin production-->ulcers, drugs should be given with food; increased dietary fat absorption; decreased Ca absorption"
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cushing's syndrome
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"hypercortisolism; trunk and face obesity; excess sweating, thinning of skin, reduced libido, impotence, infertility"
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addison's disease
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"hypocortisolism; chronic fatigue, muscle weakness, loss of appetite, weight loss, postural hypotension, respond poorly to stress, hyperpigmentation"
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glucocorticoid immune effects
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"antiinflammatory and immunosuppressive; decreases lekocyte adhesion to inflammed areas; decreseases lymphocytes, monocytes, eosinophils, and basophils; decreased responsiveness to antigens; inhibit kinnins and histamine release; "
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glucocorticoid mechanism
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"cortisol is transported primarily bound to blood protien, free cortisol diffuses into cell, glucocorticoid receptor (GR) is normally bound to heat shock proteins (HSP70/HSP90), when cortisol attaches to GR the GR detaches from HSP's, GR-cortisol complex migrates to nucleus where it promotes transcription."
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11beta hydroxysteroid dehydrogenase
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11B-HSDI/II; I converts cortisone to cortisol in the liver; II converts cortisol to cortisone in the kidney
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cortisone/cortisol balance
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at normal levels mostly cortisone; saturation of enzyme system leads to greater cortisol and mineral corticoid effect
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cortisol backbone modifications
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methyl groups and double bond increase glucocorticoid activity; F - increases mineral corticoid activity; dexamethasone has all modifications
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fludrocortisone
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"has greatly increased mineral corticoid activity, and somewhat increased glucocorticoid activity; used when people have a deficiency in both, low BP"
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triamcinolone
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glucocorticoid used in creams
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methprednisolone
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GC used to treat poison ivy
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dexamethasone
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strong GC used in cancer patients
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"fluticasone proprionate, beclomethasone diproprionate, flunisolide, triamsinolone"
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inhaled GC
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adrenal insufficiency
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"nausea, vomiting, abdominal pain, dehydration, hyponatremia, hyperkalemia, lethargy, hypotension; treat primary with hydrocortisone/fludrocortisone and salt; secondary insufficiency (kidney still viable) treat with GC alone"
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adrenal corticalsteroid toxicity
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"myopathy, osteoporosis, peptic ulcers, immune responses, metabolic changes, electrolyte balance, behavioral changes"
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metyropone
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inhibits 11Bhydroxylase (CYP11B1) and thus inhibits synthesis of cortisol; used in Cushing's for short term; causes increase in mineralcorticoid and androgen synthesis
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trilostane
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inhibits 3 beta 27 dehydrogenase; inhibits conversion of pregnenolone to progesterone; SE: GI
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aminoglutethimide
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"cytadren; inhibits CYP11A1, thus inhibiting synthesis of all steroid hormones; used in estrogen dependent breast cancer and Cushing's; SE: lethargy, rash, adrenal insufficiency"
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ketoconozole
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"nizoral; antifungal also used in Cushing's; high doses inhibit 17 alpha hydroxylase (CYP17); SE: hepatic dysfunction, CYP drug interactions; not for excessive steroid"
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