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ENDO EXAM 2 DRUGS

DRUG MOAUSEADRsNOTES
Cortisol (hydrocortisone) (GC) Glucocorticoids receptor agonist with mineralocorticoid activity many addisons HPA-axis suppression (adrenal cortex) Cushing syndrome Primarily CBG bound, circadian rhythm na retention MR loves cortisol so to prevent this binding, enzyme 11B-HSD2 converts cortisol to inactive cortisone
Dexamethasone (GC) Glucocorticoids receptor agonist little MC activity many HPA-axis suppression (adrenal cortex) Cushing syndrome minimal Na retention primarily albumin bound
(GCs)Methylprednisolone Prednisolone/prednisone Triamcinolone Glucocorticoids receptor agonist with mineralocorticoid activity many HPA-axis suppression (adrenal cortex) Cushing syndrome triam minimal na retention (MC activity)
Aldosterone (MC) MR agonist increases Na/water absorption at collecting duct, increases K excretion sodium retention HPA-axis suppression (adrenal cortex) Cushing syndrome little GR activity
Fludrocortisone (MC) MR agonist increases Na/water absorption at collecting duct, increases K excretion addisions disease, orthostatic hypotension HPA-axis suppression (adrenal cortex) Cushing syndrome high GR activity
Synthesis inhibitors 1-aminoglutethimide 2- ketoconazole 3- metyrapone 1- reversible inhibitor of steroidgenesis enzymes 2-P450 inhibitor 3-inhibits 11B-hydroxylase (decrease cortisol formation) decrease adrenal steroid synthesis cushing syndrome 2- antifungal, advnaced prostate cancer 3-diagnostic test of ACTH addisons, lethary, hypotension, CNS 2- hepatotoxicity, prolonged QT 1-enhances dexmethasone, medroxyprogesterone, tamoxifen meetabolism
GR ANTagonist Mifepristone (RU-486) Competitive GR/PR antagonists cushings, antprogestin activity CV: edem, HTN, prolong QT Abdominal cramps use higher dose for GR effects, lower doses for PR efects
MR ANTagonists Spironolactone Competitive MR antag, block Na reabsoption (K sparring diuretic) PR agonist K sparing diuretic, alsoteronism treatment (high aldosterone) gynecomastia antiandrogenic (blocks androgen) CI in addison disease and hyoerkalemia
Mg Sulfate delays preterm labor seizure prevention in eclampsia
Oxytocin (Pitocin-synthetic) Stimulates contraction and milk ejection hypothalamic hormone labor induction
Dinoprostone PGE2, increase uterine muscle contractions low dose induces labor hugh dose terminates pregnancy dose dependent effects
Misoprostol PGE1, increase contractions pregnancy termination
Estrogens inhibits HPG-axis, limit LH, FSH birth control, menopause, heavy bleeding cancer, breast tenderness, smoking, CV risk, thrombosis, gall bladder disease mestranol is estrdiol prodrug
Levonorgesrel (Opil) OTC and ulipristal pr agonist and selective PR modulator EMERGENCY CONTRACEPTION headaches , weight gain are big
anastrozole, letrozole, exemstane(irreversible) aromatase inhibitors, blocks estrogen synthesis breast cancer therapy, infertility vasodilation, edema, sweating exemestane is irrersible aromatase inhibitor
fulvestrant estrogen receptor antagonist, ER inhibitor breast cancer therapy, infertility fatigue downregulates Er levels
Mifepristone +misoprostol medical pregnancy termination, cushings, hyperglycemia CV, edema, QT, cramps
Ulipristal impedes fllicle development emergency contraception pain, headache
Bazedoxifene and raloxifene can be used for osteoporosis
clomiphene induces ovulation antagonist at hypo and ant pit
SERMS (estrogen receptor modulators) tamoxifen, toremifene, bazedoxifene, raloxifene, ospemifene, clomiphene
Fezolinetant Neurokinin 3 receptor antagonist, and neurokinin B is responsible for heat response stops menopause hot flashes, night sweats reduces VMS , blocks receptrs in the hypothalamus, blocking entire HPG axis
testosterone derivatives: Ar agonist - nadrolene, prasterone, testolactone, oxymetholone, oxadrolone, stanozolol hypogodanism, TRT, osteoporosis, weight gain acnd, sleep apnea, gynenocomastia, clitoral elargement, deep voice, amenorrhea, hirsutism testolactone irreversibly inhibits aromatase
antiadrogen: bicalutamide, flutamide, nilutamide, spironolactone AR antagonist hypergonadism, male pattern baldness, hirsutism gyneno
dutasteride and finasterdide 5a reductase inhibitor prevent test to dihydroxytest hypergonadism, male pattern baldness, hirsutism reduced libido, ED CI in pregnancy
ketoconazole spironolactone P450 inhibitor, inhitts adrenal and gonadal steroid synthesis prostate cancer therapy, inhibit adrenocoricoids
Created by: beezy41
 

 



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