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1.11
Hormonal Contraceptives
Term | Definition |
---|---|
benefits of hormonal contraceptives (8) | 1. decrease bone resorption (loss = osteopenia) 2. decrease non-cancerous changes 3. few ovarian cysts and benign breast changes 4. decreased cancer 5. ovarian and endometrial 6. prevention of ectopic pregnancy 7. decrease acne 8. decrease PMS |
principles of hormonal contraceptives: constant non-physiological levels of estrogens and progestins suppress _____&_____ secretion | FSH and LH |
Suppressing FSH and LH secretion prevents maturation of ________ | the dominant follicle (FSH) and ovulation (LH surge) |
estrogen provides cycle control by stablilizing: | endometrium |
estrogen and progestin effects prevent: | ovulation |
progestins thicken: | cervical mucus |
progestins prevent proliferative effects of estrogen on the _______________ reducing likelihood of ____________________ | endometrium, implantation |
removal of progestin leads to the loss of the: | functional zone |
Break through bleeding is reduced with: | estrogen |
first generation of combined oral contraceptives | higher concentration of estrogens (>50ug day) and progestins (>1mg) estrogen led to increased risk of thromboembolism |
second generation combined oral contraceptives | because of the side effects associated with higher doses of estrogen and progestin, the "modern pill" has less estrogens (20-35 ug/day) and progestins (levonorgestrel) |
third generation combined oral contraceptives | similar to the 2nd generation except the type of progestin used has minimal androgenic side effects (but slightly higher risk of thromboembolic disease) |
The combined pill contains: a synthetic estrogen | ethinyl estradiol or mestranol( prodrug of ethinyl estradiol) |
The combined pill contains: variety of progestins | -gonanes: norgestrel, levonorgestrel, desogestrel, norgestimate -estranes: ethynodiol diacetate, norethindrone acetate -spironolactone derivative: drospirenone |
The combined pill: monophasic | doses of estrogen and progestin stay approximately in the same throughout 21 days of pill |
the combined pill: multiphasic | -doses of estrogen and progestin change during the menstrual cycle -types: biphasic, triphasic, 4-phasic |
Triphasic combined pill | reduce the total exposure to both hormones and physiologic effects related to progestin component of oral contraceptives |
why cant you just lower the progestin dose? | not an option since contraceptive effect may also be reduced |
OCs common side effects | weight gain, nausea, acne, increased pigmentation (age spots), oily skin |
estrogen excess | nausea, age spots, hypertension, migraine, breast tenderness, edema |
estrogen deficiency | early breakthrough bleeding |
progestin excess | increased appetite, weight gain, acne, oily scalp, hair loss, hirsutism, breast regression |
progestin deficiency | mid-late cycle breakthrough bleeding |
alternative formulations of the combined pill: 2 drugs | 1. transdermal patches (ORTHOEVRA, XULANE, XAFEMY) 2. Vaginal ring (NUVARING) |
serious adverse effects of oral contraception | A.C.H.E.S. A-abdominal pain C-chest pain, shortness of breath, coughing blood H-headaches E- eye problems S- severe leg pain |
symptom: abdominal pain | condition: gallstones, blood clot, pancreatitis |
symptom: chest pain, shortness of breath, coughing blood | condition: blood clot in lung, myocardial infarction |
symptom: headaches | condition: stroke, hypertension, migraine |
symptom: eye problems | condition: stroke, hypertension, vascular occlusion |
symptom: severe leg pain | condition: blood clot |
risk of thromboembolism is small but increases with: | heavy smokers >35 yo obese women hypertensive women |
transdermal preparations: risk of DVT | risk of deep vein thrombosis has been reported with some patch preparations |
oral contraceptives in heavy smokers | -heavy smokers over 35 should not use oral contraceptives containing estrogen (estrogen increased production of pro-thrombotic factors) |
oral contraceptives in light smokers | -light smokers, 20 ug dose estrogen formulations is acceptable since it doesn't appear to impact coagulation/clotting factors |
oral contraceptives in smokers | progestin-only pills may be used when estrogen is contraindicated |
oral contraceptives in hypertensive women | oral contraceptives are NOT acceptable (especially with end-organ damage) |
oral contraceptives in hypertensive women drug | drospirenone-containg oral contraceptives (YASMIN) |
drospirenone-containg oral contraceptives (YASMIN) | increases serum K+ levels in women using anti-hypertensives bc. of anti-aldosterone properties |
patients with high levels of LDL | use pills with more estrogen then progesterone |
Contraindications to COCs use | 1. history/presence of cardiovas. diseases (venous thromboembolism, MI, stroke, congenital hyperlipdidemia) 2.known/suspected carcinoma of breast/reproductive tract 3. known/suspected pregnancy 4. liver tumors/impaired liver function |
progestin only pills: mini pill- is similar to but not as effective as: | the combined pill (suppresses FSH and LH to prevent follicle maturation and ovulation) |
progestin only pills: mini pill- promotes: | thick cervical mucus that impedes sperm's progress |
progestin only pills: mini pill-prevents: | proliferative effects of of estrogen on endometrium reducing likelihood of implantation |
progestin only pills: mini pill- removal of progestin leads to: | the loss of the functional zone |
progestin only pills: mini pill- break through bleeding is __________with estrogen | REDUCED |
the mini-pill: advantages- is able to avoid: | estrogen-mediated side effects (headaches, hyper pigmentation, hypertension and changes in clotting factors) |
the mini-pill: advantages- useful for which group of people: | smokers with history of cardiovascular disease |
the mini-pill: advantages- non-contraceptive benefits: | decreased dysmenorrhea decreased bleeding protection against pelvic inflammatory disease endometrial cancer |
the mini-pill: advantages- used in women who are: | breast feeding |
the mini-pill: disadvantages: | strict compliance- NO MISSED DOSES to avoid failure of contraception (chance of ovulation cycles, need back up contraception) |
long-acting Progestin-only contraceptive DRUG: | Depot medroxyprogesterone acetate (DMPA) |
DMPA (long-acting progestin) common side effects: | menstrual irregularities, cessation of menses, weight gain |
DMPA (long-acting progestin) cavoite of drug after you stop taking it: | infertility persists from months after stopping the drug |
Pharmacokinetics and drug interactions of hormonal contraceptive pills- metabolized by: | hepatic cytochrome p450 enzymes |
Pharmacokinetics and drug interactions of hormonal contraceptive pills- minimum effective doses of estrogen and progesterone are used for contraception, if increases: | CYP450 levels will increase clearance |
Pharmacokinetics and drug interactions of hormonal contraceptive pills- what causes contraceptive failure: | enzyme-inducing drugs (rifampin, antiepileptic drugs: carbamazepine, phenytoin) |
Pharmacokinetics and drug interactions of hormonal contraceptive pills- caused by antibiotic use: | altering enterohepatic recirculation (reabsorbed in intestine rather than being removed from body) |
Emergency contraceptive DRUG | Plan B (levonorgestrel) |
Emergency contraceptive DRUG (progesterone ANTAGONIST) | Mifepristone, Ulipristal |
Termination of pregnancy: Mifepristone MOA | ANTAGONIST of progesterone receptors a prostaglandin (misoprostol) is administered after |
Termination of pregnancy: Methotrexate with Misoprostol | methotrexate is toxic to trophoblastic tissue |