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Pharm Sex drugs
| Question | Answer |
|---|---|
| Estrogen (Estradiol and Estrone) | follicular phase-maturation of follicle, proliferation of endometrium, breast enlargement. luteal phase: synthesized by corpus luteum, maintain endometrium hypertrophy, lowered levels = mestruation, endometrial restoration after menstruation |
| Estrogen during pregnancy | large amount produced by placenta, stimulates uterine blood flow and growth of uterine muscle, acts on breast to continue ductal proliferation |
| Estrogen- MOA (receptors) | binds to estrogen receptors in nucleus, estrogen- ER complexes bind to estrogen response element on target gene and alter rate of gene txn |
| ER alpha | ER alpha (vagina, uterus, ovaries, mammary glands, vascular epithelium, hypothalamus) |
| ER beta | expressed in ovary, prostate, and to lesser extent the lungs, brain, bones, blood vessels |
| effects of estrogens on primary and secondary sex characteristics in females | maturation of reproductive organs, development of 2ndary sex characteristics, physiologic processes related to reproduction, positive effect on bone mass (protective aginast osteoporosis) |
| Metabolic actions of estrogens | favorable effects on cholesterol levels; increases HDL and decreases LDL |
| Therapeutic Uses of estrogen | contraception, hormone replacement, female hypogonadism, acne |
| adverse effects of estrogens | CV events, cancers |
| Progestins (progesterone) | production by corpus luteum under influence of LH, np implantation= cease of progesterone and menstruation, implantation= continue to produce progesterone, secretory phase of endometrium, menstruation |
| Progesterones during pregnancy | Increases, suppress contraction of uterus to sustain pregnancy |
| Therapeutic Uses of Progestins | Contraception, postmenopausal hormone replacement therapy |
| Progestins (drugs) | Medroxyprogesterone (Provera), Norgestrel (Ovrette), Norethindrone (Micronor) |
| Adverse Effects of Progestins | teratogenic effects, gynecologic effects (bleeding, amenorrhea, breast tenderness), depression, cancers |
| Risks of HRT | CV events (MI,stroke, pulmonary embolism DVT), endometrial cancer, breast cancer, ovarian cancer, urinary incontinence |
| Benefits if HRT | relief of vasomotor symptoms of menopause, management of urogenital atrophy, prevention of osteoporosis, prevention of colorectal cancer |
| absolute Contraindications of HRT | undiagnosed vaginal bleeding, active thrombophlebitis, endometrial adenocarcinoma, breast cancer, acute liver disease |
| Conjugated Estrogens (Premarin) | isolated from pregnant mares, contain equine estrogen (equilin) that is converted to testosterone, then to estradiol (combo with progesterone-Prempro) |
| Estrogens (drugs) | Estradiol, Estrone, Estratab |
| Soy products | contain soy protein and hormone like substances called isoflavones. Bind to estrogen and testosterone receptors |
| Estrogen/Progestin Combinations | estradiol + norethindrone (Activella) |
| Regimens for HRT | every woman receives an estrogen every day, women with a uterus also receive progestin |
| Continuous HRT regimen | estrogen and progestin administered continuously, no monthly bleeding |
| Sequential HRT regimen | estrogen day 1-28 and progestin added from day 14-28 (estrogen every day and progestin cycle 3 days on and 3 days off) |
| Antiresportive Therapy drugs | Estrogen, raloxifene (Evista), biphosphates, calcitonin-salmon (Miacalcin) |
| Raloxifene (evista) - SERM | activates estrogen receptors and protects against osteoporosis, blocks estrogen receptors in breast (protects against breast cancer). Promotes thromboembolism, estrogen blockade produces hot flashes |
| Biphosphates | kill osteoclasts, which break down bone. Alendronate (Fosamax) and Ibandronate (Boniva) |
| Calcitonin-Salmon (Miacalcin) | same metabolic effects as human calcitonin (inhibits activation of osteoclasts, reduces amount of blood calcium) |
| Teriparatide (Forteo) | increases activity of osteoblasts |
| Oral contraceptives- MOA | inhibits ovulation |
| 2 categories of OC | Combination OC (estrogen and progestin) and Progestin only OC (minipills) |
| Adverse Effects of Combination OC | thromboembolic disorders, hypertension, cancer, teratogenic effects, abnormal uterine bleeding, effects related to estrogen or progestin imbalance, use in pregnancy and lactation contraindicated |
| Progestin Only OC (minipill) Adverse Effects | less thromboembolic effects, but cause more menstrual irregularity |
| Transdermal Contraceptive Patch (Ortho-Evra) | Ethniylestradiol + norelgestromin |
| Vaginal Contraceptive Ring (Nuva ring) | ethinylestradiol + etonogestrel |
| Subdermal Levonogesrel Implants | surgically implanted, removed and replaced after 5 years |
| Depot Medroxyprogesterone Acetate (MPA) | Injected IM or SubQ, protection 3 months or longer (fertility returns after 12 months) |
| Intrauterine Devices | Copper T 380A (Paragard), Progesterone Intrauterine System (Progestasert), Levonorgestrel-releasing intrauterine system (Mirena) |
| Yaz/Yazmin | Drospirenone (synthetic progestin) and ethnyl estradiol (synthetic estrogen)- birht control proven to treat emotional and physical symptoms of premenstrual dysphoric disorder |
| emergency Contraception- MOA | may prevent ovulation, but effectiveness late in cycle suggests other mechanisms |
| Yuzpe Regimen | 2 doses of an OC that contains an estrogen and progestrin. First dose within 72 hours of intercourse and second dose 12 hours after the first dose. (PREVEN) |
| Plan B | progestin only emergency contraceptive (Norgestrel), should be administered within 72 hours of intercourse and second dose 12 hours after the first |
| Mifepristone(Mifeprex)- MOA | partial agonist of progesterone receptro- blocks uterine progesterone receptors and causes medical termination or intrauterine pregnancy through 49 days (detatchment of conceptus) |
| Adverse Effects of Mifepristone (Mifeprex) | vaginal bleeding, abdominal pain, headache |
| Clomiphene Citrate (clomid)- MOA | selective estrogen receptor modulator (SERM)-partial agonist of estrogen receptors- blocks estrogen receptors, inhibits feedback effect of estrogen on pituitary gland, increases FSH and LH which stimulate ovary-promotes follicular maturation and ovulation |
| Clomiphene Citrate (clomid)- uses | promote follicular maturation and ovulation- infertility therpay due to anovulation |
| Clomiphene Citrate (clomid)- adverse effects | hot flashes, n/v, breast enlargement, 10% multiple birth |
| Human Chorionic Gonadotrophin (hHCG) - MOA | promotes follicular maturation and ovulaiton |
| - Human Chorionic Gonadotrophin (hHCG- uses | infertility treatment die to anovulation |
| - Human Chorionic Gonadotrophin (hHCG- adverse effects | ovarian hyperstimulation syndrome, multiple births |
| Testosterone (MOA) | made in leydig cells of testes and converted to dyhdrotestosterone (DHT) which binds to the nuclear androgen receptors |
| Testosterone- physiologic effects | o Pubertal transformation o Spermatogenesis o Anabolic effects: promotes skeletal muscle growth o Erythropoietic effects: promote synthesis of erythropoietin (EPO) → increases red blood cell production |
| Testosterone- uses | o Management of androgen deficiency in males • Male hypogonadism • Delayed puberty o Breast cancer o Catabolic states: loss of muscle mass in AIDs patients • Oxandrolone • ** Use and abuse in athletes → performance enhancing drugs o anemias |
| Testosterone- adverse effects | o Virilization o Hepatotoxicity o Effects on cholesterol levels o Edema o Gynecomastic o Abuse potential (athletic performance) |
| Sildenafil (Viagra) - MOA | phosphodiesterase type 5 inhibitor I - increases cGMP, causes vasodilation, increases erectile response |
| Vardenafil (Levitra) and Tadalafil (Cialis) | phosphodiesterase type 5 inhibitor II - same MOA as viagraa, cialis has longer half life |
| Phosphodiesterase Type 5 inhibitors- adverse effects | hypotension, priapism (erect penis does not return to flaccid state) |
| Antiestrogens- against breast cancer | 1) SERMs, 2) Pure Estrogen Receptor Antagonist 3) Aromatase Inhibitors |
| o Selective Estrogen Receptor Modulators (SERMs)- breast cancer therapy -MOA | partial ER agonists- binds to ER and block in breast tissues (prevent receptor activation by estrogens, blcok cells proliferation and tumor growth) |
| SERMS- adverse effects | hot flashes, fluid retention, N/V, increased risk of endometrial cancer and thrombosis |
| SERMS- drugs | Tamoxifen (Nolvadex), Toremifene (Fareston), Raloxifene (Evista) |
| Fulvestrant (Faslodex) | Pure estrogen receptor antagonist (blocks actions of estrogen on breast tissue) |
| Aromatase Inhibitors -MOA | block conversion of adrenal androgens to estrogen in peripheral tissue (mediated by aromatase)- decreased estrogen production |
| Aromatase Inhibitors- adverse Effects | • Generally well tolerated • Asthenia, N/V • About 25% of females experience musculoskeletal and joint pain → 5% discontinue treatment • Increased risk of osteoporosis and fracture |
| Aromatase Inhibitors- drugs | • Anastrozole (Arimidex) • Letrozole (Femara) • Exemestane (Aromasin) |
| o Trastuzumab (Heceptin) | - Monoclonal Antibody for IV therapy of metastatic breast cancer → anti- HER2 → blocks HER2 receptors |
| 2 drug classes for prostate cancer | GnRH Agonists, Androgen Receptor blockers |
| GnRH Agonists- MOA | mimics GnRH action → direct acting anti-androgen |
| GnRH Agonists- drugs | o Leuprolide (Lupron), IM, subQ o Triptorelin (Trelstar Depot), IM o Goserilin (Zoladex), subQ |
| GnRH Agonists-adverse effects | o Generally well tolerated o Hot flushes o Impotence and loss of libido o Increased risk of osteoporosis and bone fracture |
| Androgen receptor Blockers- MOA | block androgen receptors in tumor cells |
| Androgen receptor Blockers- drugs | o Flutamide (Eulexin) o Bicalutamide (Casodex) o Nilutamide (Nilandron) |
| Androgen receptor Blockers- adverse effects | o Generally well tolerated o Gynecomastia o N/V o Rarely hepatotoxicity |
Created by:
alexadianna
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