L43- Contraceptives (general + oral) Flashcards
(1) = most common goal of contraception
(2) are the other goals
-*prevention of pregnancy
- menstrual cycle regulation
- reduction of premenstrual symptoms
- Acne Tx
- Hirsutism (excess androgens)
(1) types of OCPs
(2) and (3) are the major general approaches
1- combined OR progestin-only
2- preventing ovulation
3- impairing implantation
describe mechanism of preventing ovulation
1) give estrogen
2) stabilize (prevent fluctuations) of estrogen levels
3) suppress FSH, LH release
describe mechanism of impairing implantation
give progestin –> maintains elevate progesterone levels:
- thickens cervical mucus –> prevents sperm penetration
- induces changes in endometrium –> impairs implantation
list estrogen oral contraceptives
- ethinyl estradiol
- mestranol (prodrug –> ethinyl estradiol)
list progestins
norethindrone norgestrel levonorgestrel desogestrel norgestimate drospirenone
describe the non-progesterone activity of progestin
variable Androgenic activity:
- levonorgestrel, norgestrel: highest
- norethindrone: 2nd
- desogestrel, norgestimate: 3rd gen.
- drospirenone: antiandrogenic
describe oral contraceptive preparations
Monophasic: fixed dose estrogen and progestin in each active pill
Biphasic, Triphasic: variable proportions one or both hormones
Biphasic and Triphasic OCP preparations have the following advantages over Monophasic:
- (T/F) more efficacious
- (T/F) less amount and monthly dosing
- (T/F) less AEs
- (T/F) hormone levels more closely related to changes in menstrual cycle
1- F
2- T, reduced progestins
3- T, related to dec amount / dose
4- T
name most common combined OCP and discuss most common dosing
35 µg ethinyl estradiol (or less, aka ‘low dose’) + progestin
One mo: 21 hormonal pills, 7 pill placebo (consecutive- allows withdrawal from bleeding)
describe the type of combined OCP dosing regimens
Common: 21 hormonal days, 7 placebos
Extended Cycle: 84 hormonal days, 7 placebo –> only 4 menstrual cycles per year
Continuous: 21 hormonal days, then 4-7 reduced dose days
list the many benefits of combined OCPs
- reduced risk endometrial, ovarian cancer
- improve menstruation regulation
- breast disease relief
- ovarian cyst prevention
- reduced risk of symptomatic PID
- acne control
OCPs have many AEs, (1) are the main concern limiting long-term use. (2) is an adjustment that have greatly reduced AEs.
1- CVS toxicity
2- reduced dosage
________ OCP AEs can improve spontaneously by the third cycle
- nausea
- bloating
- breakthrough bleeding
________ most common OCP AE
breakthrough bleeding (vaginal spotting)- more w/ low estrogen doses –> stabilizes endometrium
describe HAs as an OCP AE
-usually mild, transient
- migraine maybe associated with CVA
- -> indication to stop OCP
OCP AEs:
- (1) positive hormone effects
- (2) negative hormone effects
- inc (3) production
- (4), an over effect of hormones administered
- decreases the incidences of (5)
- a few patients with (6) disease may need to stop
1- Androgenic progestins –> acne, oily skin, hirsutism –> switch to less or non-androgenic progestin
2- progestins –> insulin resistance (competes for receptor) –> therefore low progestin content to avoid hyperglycemia
3- estrogen –> melanocyte production–> melasma
4- amenorrhea
5- endometrial and ovarian cancer
6- depression
OCP cardiac AEs:
- increases (1) production –> increasing risk of (2) events in general
- (3) name the (2) events
- (4) are the precipitating risk factors
1- Estrogen –> inc factor VII, factor X, fibrinogen
2- thromboembolic events
3- thromboembolism, thrombophlebitis, HTN, MI, cerebral thrombosis
4- obesity, smoking, HTN, DM, >35 y/o
OCP AEs: Liver Enzyme (induction/inhibition) is the main concern, explain
drugs that induce CYP450:
- *inc estrogen metabolism
- rifampin mainly (+ the others you known)
OCP AEs effect on Antibacterials
Ethinyl estradiol –> undergoes bile excretion –> hydrolyzed by intestinal bacteria –> active drug reabsorption
- if given Antibiotic –> dec estrogen levels may occur
- some antibiotics dec OCP efficacy
list the ABSOLUTE OCP contraindications
- pregnancy
- > 35 + smoking (15 cigs)
- surgery or immobilization injury
- thrombophlebitis, thromboembolic disorders
- stroke, CAD
-breast CA, estrogen dependent CA, benign/malignant liver tumor
- vaginal bleeding, uncontrolled HTN, DM + vascular disease
- migrains w/ aura
- active hepatitis
list the RELATIVE OCP contraindications
- migraine w/o aura
- lactation
- HTN, DM
- Heart and Kidney disease
- gallbladder disease, cholestasis during pregnancy
- SCD
Progestin Only Pills:
- (1) formulation
- (2) efficacy compared to combined OCP
- (3) benefits
- (4) disadvantages
(impairs implantation)
1- norethindrone, norgestrel (not used in US)
2- less –> only blocks 60-80% of cycles
3- NO thromboembolic events + dec dysmenorrhea, des blood in menstruation, dec PMS Sxs
4- bleeding / spotting
