Hormonal Contraceptives Flashcards
Pharmacologic Effects of HCs
- suppress fxn of hypothalamic-pit-ovarian axis- dec secretion of GnRH
- diminish ovarian H prod
- inhibit maturation/release of dominant ovule
- modify mid-cycle surges of LH and FSH
- inc viscosity of cervical mucus to impede sperm transit
- produce endometrial changes unfavorable or ovum implantation
Hormonal Contraceptive Choices
- daily use
- non-daily use
- emergency use
Hormonal Contraceptive Choices- daily use
oral tablets
- combination (COC)
- progestin-only (POP)
- extended cycle
Hormonal Contraceptive Choices- non-daily use
- patch
- vaginal ring
- injectable- LARC (long-acting reversible contraceptive)
- implantable- LARC
- IUS (intrauterine device)- LARC
Hormonal Contraceptive Choices- emergency use
-oral tablets- progestin-only
estrogens in COCs
- ethinyl estradiol (EE)- most common
- estradiol valerate
- mestranol
progestins in COCs
19-Nortestosterone analog -Estranes -Gonanes Spironolactone-analog -Drospirenone
progestins in COCs- 19-Nortestosterone analog
- Estranes- Ethynodiol, Norethindrone
- Gonanes- desogestrel, dienogest, levonorgestrel, norgestrel, norgestimate
Phasic Combination of COC’s- monophasic
(H’s taken for 21 days)
-fixed dose of estrogen and progestin thruout cycle
Phasic Combination of COC’s- biphasic
- fixed dose of estrogen thruout,
- lower progestin amt in 1st half allowing endometrial prolif, inc amt in 2nd half provides adequate secretory development
Phasic Combination of COC’s- triphasic
inc dose of estrogen 3 times during cycle
Phasic Combination of COC’s- quadriphasic
dec dose of estrogen and inc dose of progestin 4x during cycle
Non-Oral Progestins
-Norelgestromin
-Etonogestrel
-Medroxyprogesterone
-Levonorgestrel
(NEML)
Norelgestromin
patch with EE- 7 day duration
Etonogestrel
- vaginal ring with EE- 3 wks
- available in progestin-only implantable rods- 3 yrs
Medroxyprogesterone
-progestin-only long acting IM or SQ injections- 3 months
Levonorgestrel
-progestin-only IUS- 5 yrs or 3 yrs
Non-Oral Non-Hormonal
Copper- non-hormonal IUD- 10 yrs
Estradiol and progesterone effects- cellular moa impacting SE’s
-bind to Rs in various tissues- transferred into nucleus resulting in gene and protein expression
Non-contraceptive effects of estrogens- dec what?
- chol
- osteoclastic activity
- anti-thrombin III
- bile acid levels
Non-contraceptive effects of estrogens- inc what?
- triglycerides, HDL-C
- clotting factors
- platelet aggregation
- renin/aldosterone secretion/activity (Na/fluid retention)
- thyroid, corticosteroid, sex-hormone binding globulins
- iron/TIBC, prolactin
- folate metabolism/excretion
estrogens- adverse effects
- irregular bleeding
- breast tenderness
- fluid retention (wt gain)
- mood changes
- headaches, GI distress
- hyperkalemia (drospirenone-containing agents)
estrogens- serious adverse effects
- systemic thromboembolism
- HTN
- gallbladder dz
Non-contraceptive benefits of combination HCs (COCs)
Improvement in H-related events -irregular menstrual cycles -dysmenorrhea -fxnal ovarian cysts -acne -anemia -PMDD -peri-menopausal sx's -hirsutism REduction in some cancers -ovary, endometrium, colon/rectum *HCs do NOT prevent/reduce risk of STIs and HIV!!!!!
COC- contraindications
- pregnancy or < 21 d postpartum
- vascular-related dz
- valvular HD
- peripartum cardiomyopathy
- rheumatic HD
- hepatic adenoma or malignant hepatoma
- decompensated cirrhosis
- solid organ transplant rejection or organ failure
- major surgery with prolonged immobilization
- uncontrolled severe HTN
- diabetes > 20 yrs with pathy’s
- migraine HA’s with aura
- acute/flare viral hepatitis
- smoking > 15 cigs/day and > 35 yo
IUD- contraindications
- pregnancy
- postpartum sepsis
- immediate post-sepsis abortion
- distorted uterine cavity
- unexplained vaginal bleeding
- cervical cancer
- current PID
- pelvic TB
- current purulent cervicitis
- current STI
- gestational trophoblastic dz with persistently elevated B-HCG
- malignant gestational trophoblastic dz with intrauterine dz
Drug interactions- inducers
- antimicrobial agents
- antiviral agents
- anti-seizure agents
how to be certain a woman is not pregnant
- < 7 days after start of normal menses
- not had sex since start of last normal menses
- uses a method of contraceptive (correctly, consistently)
- <7 days after spontaneous or induced AB
- within 4 wks postpartum
- fully or nearly bresat feeding
emergency contraception- can be admin:
- after unprotected intercouse (up to 72 hrs)
- concern of contraceptive failure
- sexual assault/rape
- exposure to teratogens
emergency contraception- moa of progestin
(levonorgestrel)
- inhibition of ovulation (primary)!!!
- available in 1 and 2-dose tx’s
Levonorgestrel-Only, 2-dose- emergency contraception
Plan B
- first dose- take 1 (0.75 mg) tablet ASAP (within 72 hrs of unprotected sex!!!)
- second dose- take 0.75 mg 12 hrs after 1st dose
Levonorgestrel-Only, 1-dose- emergency contraception
take tablet (1.5 mg) ASAP (within 72 hrs!!!)
Ulipristal (non-pregestin), 1-dose- emergency contraception
- only dose- take tablet ASAP (within 72 hrs)
- progesterone-R modulator: main action is inhibition of ovulation!!!
- initiation of COC’s after EC: start COC no sooner than 5 days of ulipristal use AND use barrier method until next menstrual cycle