Hormonal contraceptives: Segars Flashcards
what are the pharmacologic effects of HCs
- suppress function o hypthalamic pituitary ovarian axis; decrease secretion of GnRH
- Diminish ovarian hormone production
- inhibit maturation/release of dominant ovule
- modify mid-cycle surges of LH and FSH
- increase viscosity of cervical mucus to impede sperm transit
- produce endometrial changes unfavorable for ovum implantation
What are the 3 broad categories of HCs
- Daily use (oral tablets)
- Non Daily use
- emergency use
what are the daily oral HC options
- Combination (COC)
- Progestin only (POP
- Extended cycle
what are the non daily HC options
- patch
- Vaginal ring
- Injectable (LARC): long acting reversible contraceptive
- Implantable (LARC)
- IUS/IUD (LARC)
what is the emergancy use contraceptive option
progestin only oral tablet
what are the different estrogen in COCs (comination oral contraceptives)
- Ethinyl estradiol (EE): most common; longer half life and more active than estradiol
- Estradiol valerate: synthetic pro-drug of 17-beta estradiol
- Mestranol: gets metabolized to ethinyl estradiol
what are the broad different progestins in COCs
- 19-Nortestosterone analogs: Estranes and Gonanes
- Spironolactone-analog
what are the Estanes in COCs
- Ethynodiol
- Norethindrone
what are the Gonanes in COCs
- Desogestrel
- Dienogest
- Levonorgestrel
- Norgestrel
- Norgestimate
what is the spironolactone analog in COCs
Drospirenone
What progestins have the most progestinic activity
- Desogestrel
- Levonorgestrel
What progestins have the most estrogenic activity
- Ethynodiol (most)
- Norethindrone (2nd)
what progestins have the most androgenic activity
-Levonorgestrel
Describe a monophasic combination of HCs
fixed dose of estrogen and progestin throughout cycle
describe Biphasic combination of HCs
- fixed dose estrogen throughout cycle
- lower progestin amount in 1st half, allowing endometrial proliferation
- increased amount in 2nd half provides adequate secretory development
Describe triphasic HCs
increasing dose of estrogen (or progestin and estrogen) 3 times during the cycle
Describe Quadriphasic HCs
-DECREASING dose of estrogen and increasing dose of progestin 4 times during cycle
Describe non oral progestin: Norelgestromin
- gonane family: “Gest”
- metabolite of norgestimate
- available in PATCH with EE (ethynyl estradiol)
- 7 day duration *****
Describe non oral progestin: Etonogestrel
- a vaginal ring with EE (3 weeks duration ***)or
- implantable rod with progestin only (3 YEARS duration)**
Describe non oral progestin: mydroxyprogesterone
- progestin only
- long acting IM injections (3 month duration)
Desribe the non oral progestin: Levonorgestrel
- Progestin only IUD
- Kyleena adn Mirena (5 years)
- Skyla and Liletta (3 years)
what is the non oral non hormonal contraceptive
-copper: non hormonal IUD (10 years)
what is the long list of non contraceptive effects of estrogens
decrease in:
- cholesterol
- Osteoclastic activity
- Anti-thrombin III
- Bile acid levels
increase in:
- Triglycerides and HDL-C
- clotting factors
- platelet aggregation
- renin/aldosterone activity (Na/fluid retnention)
- thyroid, corticosteroid, sex hormone binding globuline
- Iron/TIBC and prolactin
- Folate metabolism/excretion
what are common adverse effects of HCs
- irregular bleeding
- breast tenderness
- fluid retention (weight gain)
- mood changes
- headache and GI distress
- Hyperkalemia
- Acne/hirsutism/wt. gain: progestinic and androgenic effect . . . so choose a product without these effects