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Pharm Sex drugs

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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