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Class progestrogens and antiprogestrogens
This document discusses progestogens and antiprogestogens, including their mechanisms of action, physiological targets, uses, and side effects. It focuses on several classes of progestogens used in oral contraceptives and hormone replacement therapy. It also describes mifepristone (RU-486) as an antiprogestogen used to terminate early pregnancies by antagonizing progesterone receptors and inducing uterine contractions. Precautions and contraindications for its use are outlined.
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Class progestrogens and antiprogestrogens
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- 3. Medroxyprogesterone acetate Megestrol acetate Dydrogesterone Hydroxyprogesterone caproate Newer –Nomegestrol acetate 19-nor testosterone derivatives a) Older Norethindrone Levonorgestrel Lynesternol-Ethinylesternol, Allylesternol b)Newer compounds Gonanes Desogestrel Norgestimate Gestodene
- 4. OH O HH H 19-NORTESTOSTERONE OH C CH O HH H NORETHINDRONE O C CH O HH H ETHYNODIOLDIACETATE AC AC Progestins • 19-NOR Steroids :Progestins Removal of 19-carbon changed major hormonal effect from an androgen to progestin while maintaining oral activity •Estranes: have some androgenic activity as well as estrogenic/anti- estrogenic actions. Rapidly absorbed (Norethindrone)
- 5. OH CH 2 CCH O H3C HH H DESOGESTREL OCOCH3 CH2 C CH HON H3C HH H NORGESTIMATE OH CH2 C CH O H3C HH H NORGESTREL H2C • Gonanes: More potent than estranes and less androgenic activity and are now used in the 3rd generation combination oral contraceptives (Norgestrel, Norgestimate, Desogestrel) Progestins
- 6. Mechanism ofAction: Interacts with PR to mimic the stimulatory affects of progesterone Physiological Target: Reproductive Tract - Decreases estrogen-driven endometrial proliferation - Establishment and maintenance of pregnancy P/K- usually inactive orally T1/2- short-5-7 min High first pass metb
- 8. Uterus –secretory changes Cervix- viscid scanty secrtn Vagina-leukocyte infiltrtn Breast-cause proliferation of acini CNS-sedative Body temp-increased respiration- stimulation Metabolism-OCPs-prolonged use- glucose tolerance Pituitary-inhibit Gn sectrn negetive feed back Natural progesterone-micronised oral
- 9. 1. Oral contraceptives 2.HRT to limit estrogen’s effects on the endometrium 3. Uterine Bleeding disorders -DUB 4. Premature labor (decrease uterine contractions) 5. Stimulate Appetite in AIDS or cancer patients 6. Endometriosis-danazol(non-progestrogenic, non- estrogenic, but exhibits hypoestrogenic, hyperandrogenic, cause atropy of endometrium) 7. Premenstrual syndrome 8. Threatened abortion 9. Endometrial Carcinoma
- 10. Mild-Nausea, mastalgia,breakthrough bleeding, edema, headache Moderate-break through bleeding, weight gain, skin pigmentation, hirsuitism, bacteruria, vaginal infections and amenorrhoea Severe –venous thromboembolism, myocardial infarction, cerebrovascular disease, GI disorders- cholestatic jaundice, depression, cancer
- 11. Anti-Progesterones Mifepristone (RU 486)PR agonist ,antagonist Used in first trimester to terminate pregnancy (along with prostaglandins to increase uterine contractions) Post-coital contraceptive (prevent implantation) Investigational: induction of labor after fetal death and treatment of endometriosis. Promotes shedding of endometrium, softening of the cervix, and uterine contractions leading to spontaneous abortion Often used in conjunction with misoprostol prostoglandin
- 12. 12 Effects of abortionprocess Cramping-Often described as similar to menstrual cramps Vaginal bleeding-Median bleeding time 9-13 days Often described as similar to a heavy period or spontaneous miscarriage Common side effects Nausea Vomiting Diarrhea Headache Dizziness Fever, chills, hot flashes, warmth
- 13. 13 Non-ectopic pregnancyof ≤63 days’ gestation Absence of contraindications Willingness to undergo vacuum aspiration or dilation and curettage (D&C), if indicated
- 14. 14 Confirmed orsuspected ectopic (extra-uterine) pregnancy Allergy to either mifepristone or misoprostol Presence of an intrauterine device (IUD) Chronic systemic use of corticosteroids Chronic adrenal failure Coagulopathy or current therapy with anticoagulants Inherited porphyria
- 15. ▪ Interactions: ▪ Decreasesefficacy of anticoagulants. ▪ Inhibits hepatic metabolism by CYP3A4 (eg.anti- retroviral protease inhibitors, calcium-channel blockers, carbamazepine)