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1.11

Hormonal Contraceptives

TermDefinition
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
Created by: megangodfrey97
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