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Oral Contraception
Dr. Prinster 2/6/13
38
Pharmacology
Post-Graduate
02/06/2013

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Cards

Term
What are the three main estrogens produced by the female body?
Definition
Estradiol
Estrone
Estriol
Term
Which of these estrogens is the principal secretory product of the ovary?
Definition
Estradiol (it is the most potent)
Estradiol > Estrone > Estriol
Term
What does the combined pill contain?
What does the mini-pill contain?
Definition
Combined pill? Estrogen & progestin
Mini-pill? Progestin only
Term
Specifically, what estrogen is contained in the combined pill?
Definition
Ethinyl estradiol (EE), a synthetic estrogen
(It is combined with C-19 steroids)
Term
What is the difference in Monophasic, Biphasic, and Triphasic formulation?
Definition
Monophasic has a single dose of EE and progestins throughout 21 days of pills.
Biphasic has a single dose of EE but two different doses of progestins.
Triphasic has a single dose of EE but three different doses of progestins.
(In all cases, there is a single dose of EE and it is named for the number or doses of progestins)
Term
Common adverse effects of oral contraceptives?
Definition
Weight gain (fluid retention or anabolic effect)
Nausea
Flushing
Dizziness
Depression/irritability
Skin changes (acne, increased pigmentation)
Amenorrhea of variable duration after the pill is stopped
Term
Serious adverse effects of oral contraceptives mnemonic?
Definition
ACHES
Abdominal pain
Chest pain, SOB, coughing blood
Headaches
Eye problems
Severe leg pain
Term
For patients taking oral contraceptives, for who is the risk of cardiovascular disease increased?
Definition
Smokers
Obese women
Hypertensive women
Term
In what preparation of contraceptive is DVT a risk?
Definition
Transdermal preparations
Term
What type of pills should heavy smokers use?
Definition
Progestin-only pills may be used. Oral contraceptives containing estrogen are CI (unless very low dose estrogen).
Term
What oral contraceptive causes problems for women on certain types of anti-hypertensives (ACE inhibitors, K+ sparing diuretics)?
Definition
Drosperinone (Yasmin)
It increases serum K+ levels
Term
MOA of Drosperinone (Yasmin)?
Definition
Drosperinone (Yasmin) is a progesterone with a mineralocorticoid antagonist action
Term
What pill should be used in patients with high levels of LDL cholesterol?
Definition
Use pills with more estrogen than progesterone in individuals with high levels of LDL. The progestins in oral contraceptives cause an increase in LDL and decrease in HDL levels. (side effect of progestin-only mini-pill!)
Term
What component of oral contraceptives is thought to increase risk of certain cancers?
Definition
Estrogen component, particularly in breast cancers (although decreased risk of endometrial and ovarian cancers with oral contraceptive use)
Term
What are alternative formulations of the combined pill?
Definition
Transdermal patch
Vaginal ring (Nuvaring)
Term
Advantages of transdermal patches?
Definition
Applied once/week (better patient compliance
Term
MOA of the mini-pill?
Definition
Similar to the combined pill (suppresses FSH and LH to prevent follicle maturation and ovulation, but not as effective as the combination pill)
Promotes thick cervical mucus that impedes the sperm's progress
Term
Advantages of the mini-pill?
Definition
Avoids estrogen-mediated side effects such as headaches, hyperpigmentation, and changes in clotting factors.
Useful in smokers with history of cardiovascular disease.
Used in breast feeding women.
Non-contraceptive benefits: decreased dysmenorrhea and bleeding, protection against PID and endometrial cancer.
Term
Disadvantages of the mini-pill?
Definition
Less effective than combined pill.
Strict compliance (no missed doses) is necessary.
Chance of ovulatory cycles (back up contraception may be necessary).
More frequent breakthrough bleeding.
Term
Who is the mini-pill CI for?
Definition
Women with history of breast cancer, undiagnosed vaginal bleeding, hepatic diseases.
Term
What contraceptive is long-acting, progestin-only, and administered IM?
Definition
Depot medroxyprogesterone acetate (DMPA)(Depo-Provera)
Term
What contraceptive is long-acting, progestin-only, and administered as subdermal capsules? What does it contain?
Definition
Progestin implants
They are subdermal capsules containing Etonorgestrel (Nexplanon).
Term
Advantages of Progestin implants?
Definition
Cheaper than oral contraceptives.
No reliance on patient compliance.
Last for over 3 years.
Return of fertility after removal of implant.
Term
How are contraceptive metabolized?
Definition
Metabolized by hepatic cytochrome P450 enzymes
Term
What drugs can cause contraceptive failure?
Definition
Enzyme-inducing drugs cause contraceptive failure.
Antibiotics - Rifampin
Antiepileptics - Carbamazepine, Phenytoin
Term
What hormone is present in forms of post-coital contraception?
Definition
High doses of progesterone (prevents implantation)
Term
Menopause and Hormone Replacement Therapy (move to next slide)
Definition
Menopause and Hormone Replacement Therapy (move to next slide)
Term
Symptoms of menopause?
Definition
Hot flashes ("resetting" of the central thermostat leading to increased sympathetic outflow)
Vaginal dryness
Arthralgia & Myalgia
Sleep pattern disturbances
Wrinkling of skin
Thinning of hair
Osteoporosis
Coronary artery disease (leading cause of morbidity and mortality in postmenopausal women)
Term
What is the natural version of HRT (hormone replacement therapy)?
Definition
Conjugated equine estrogens (CEE)
(short-acting estrogen mixture of conjugated estrogens)
Term
What is the synthetic version of HRT (hormone replacement therapy)?
Definition
Esterified estrogens
Term
What drug regimen is recommended for women with intact uterus? What about for those that have undergone hysterectomy?
Definition
Include PROGESTIN in the regimen to lower the risk of endometrial cancer.

CEE alone
Term
Does HRT increase the risk of coronary heart disease? Does HRT increase the risk of cancers? Does HRT increase the risk of other cardiovascular diseases?
Definition
No to CHD.
Yes to breast cancer.
Yes to venous thromboembolism & stroke (dose dependent).
Term
What two other drugs are beneficial for reducing hot flashes?
Definition
Clonidine (reduces sympathetic outflow, the cause of hot flashes)
Desvenlaflaxine
Term
What drugs are used to treat endometriosis (5)?
Definition
Oral contraceptives (combined pills)
Progestins
Danazol*
GnRH analogs
Aromatase inhibitors
Term
MOA of Danazol*?
Definition
Acts as a partial agonist at progesterone, androgen, and glucocorticoid receptors.
Term
What GnRH analog is often used?
Definition
Leuprolide*
Term
What aromatase inhibitor is often used to treat endometriosis?
Definition
Anastrozole*
Term
Patient is a 29 yo woman who is requesting prescription for contraception. She has a 10 yr history of smoking 1 pack/day and has recently been diagnosed with endometriosis. The most appropriate and effective contraceptive would be?
Definition
Depo-provera (Medroxyprogesterone acetate); it is progestin-only and is indicated in patients who need contraceptives and smoke and in the treatment of endometriosis.
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