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1.11

progestins

TermDefinition
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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