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1.11
progestins
| Term | Definition |
|---|---|
| progesterone | major endogenous progestin |
| sources of endogenous progesterone in females | ovary and placenta |
| where is endogenous progesterone synthesized during the luteal phase? | corpus luteum |
| where is endogenous progesterone synthesized during the 1st trimester? | placenta |
| sources of endogenous progesterone in males (2) | 1. produced in testis 2. adrenal cortex |
| progestational agents in clinical use | Desogestrel |
| Progesterone MOA | 1. binds to progesterone receptors in nucleus and cytoplasm 2. receptors are in reproductive tissues, hypothalamus, pituitary, mammary gland |
| Progesterone MOA | 3. progesterone receptors undergo dimerization 4. ligand receptor complex binds to PRE to activate gene transcription |
| feature: secondary females sexual characteristics | effect: maintain (less than estrogen) |
| feature: uterine lining (endometrium) | effect: maintain; when progesterone decreases, shedding/promote loss of endometrium (menses) |
| feature: cholesterol | effect: decrease HDL, increase LDL |
| feature: body fat | effect: fat deposition |
| progestin excess | increased appetite, weight gain, acne, hair loss, hirsutism, oily scalp, breast regression |
| progestin deficiency | late breakthrough bleeding |
| Therapeutic uses (1-5) | 1. hormonal contraception 2. hormonal replacement therapy 3. dysmenorrhea (pain with period) 4. amenorrhea (absence of menstruation) 5. endometriosis |
| therapeutic uses (6-9) | 6. uterine bleeding disorders 7. acne vulgaris 8. progesterone supplementation or replacement for infertile women with progesterone deficiency 9. endometrial carinoma |
| Progesterone preparations: oral micronized capsule drug | PROMETRIUM |
| Progesterone preparations: medroxyprogesterone acetate injectable suspension drug | DEPO-PROVERA |
| Progesterone preparations- drug: Megestrol acetate (MEGACE) | suspension approved for treatment of AIDS and cancer patients with anorexia, cachexia, or unexplained weight loss stimulates appetite and weight gain |
| Progesterone preparations- drug: Norethindrone (MICRONOR) | used alone as "minipill" has some androgenic activity |
| Progesterone preparations- drug: Levonorgestrel | emergency contraceptive (Plan B) |
| Progesterone preparations: drug | Desogestrel |
| Progesterone preparations-drug: Drospirenone | anti-androgenic and anti-mineralocorticoid activity |
| Progesterone preparations-drug: Norelgestromin (ORTHO-EVRA) | transdermal contraceptive patch |
| Progesterone preparations- drug: Etonogestrel (NUVARING) | used in combination with estrogen as a contraceptive vaginal ring |
| Progesterone Adverse effects | 1. Breakthrough bleeding and spotting 2. amenorrhea 3. breast tenderness 4. edema, bloating 5. increased appetite and weight gain 6. abnormal lipid profile (decrease HDL, increase LDL) 7. hirsutism 8. headache |
Created by:
megangodfrey97
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