PHARM: Contraception Flashcards by Rachael Petry

What is the major risk factor in using gonadotropins for infertile women?

multiple pregnancies

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Are gonadotropins first line treatment for male fertility?

NO, not until after androgens have induced sexual development because they are expensive.

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What drug is an IM injection of FSH and LH from the urine of postmenopausal women?

menotropin

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What can be given as an IM injection from urine of pregnant women?

chorionic gonadotropin

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How can exact time of ovulation be predicted?

with LH-specific antibodies (will peak 36 hours before ovulation)

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What estrogens may be used to treat prostate cancer?

DES and clorotrianisene

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What is the difference between the difference between selective estrogen receptor modulators and antiestrogens?

Whereas SERMs have estrogen agonist activity in some tissues and estrogen antagonist activity in other tissues (ex. breast), antiestrogens are pure antagonists in ALL tissues.

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What is the most effective type of birth control (along with progestin implants and sterilization)?

IUD

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What are the indications for an IUD?

birth control; dysmenorrhea

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What are the two types of IUD?

copper containing

progestin releasing

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How do copper IUDs work?

copper is spermicidal

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What drug is used in progestin releasing IUDs?

levonorgestrel is slowly released

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What are the major toxicities of a copper IUD?

copper may cause cramping

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What are the major toxicities of progestin releasing IUDs?

irregular bleeding (6-12 months)

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What is one of the biggest benefits of an IUD?

fertility is quickly restored upon removal

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What is the most popular form of birth control?

hormonal contraceptives

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What are the indications for hormonal contraceptives?

prevent ovulation (birth control)
reduced dysfunctional uterine bleeding and dysmenorrhea
menstrual regulatiry
increased hemoglobin
decrease androgens (so decreases hirsuitism and acne)
PCOS treatment (“off-label”)

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What are some contraindications of hormonal contraceptives?

thromboembolic disease, cerebral vascular disease, MI, CAD, congential hyperlipidemia, known or suspected breast or endometrial cancer.

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List the different forms of hormonal contraceptives.

Combination pill
Mini-Pill
Transdermal Patch
Vaginal contraceptive ring
Injectable contraceptives
implant

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What hormones are found in combination pills?

combination of estrogen and progesterone

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How do combination pills work?

prevent LH and FSH release by feedback inhibition

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Why can combination pills be used to treat PCOS?

Raise SHBG (decrease androgens)

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What are the major side effects of the combination pill?

breakthrough bleeding, HA, bloating, etc.

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What hormones are found in mini pills?

low dose progestin only

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How do mini pills work?

blocks ovulation in only 60-80% of cycles, impairs sperm transport—thickens mucous, decreases motility of ovules in oviduct and alters endometrium to impair implantation

How does the dose scheduling of mini pills differ from most combination pills?

usually with combination pills there are a few days of "placebo" at the end of the package; with mini pills, you take it continuously

The mini pill would be especially good for women of what population?

women who are breastfeeding; women > 35 who smoke

What are the "cons" of the mini pill?

slightly higher failure rate than the combination pill; May actually cause acne (progesterone causes sebaceous gland secretion); may cause weight gain

What hormones are found in a transdermal patch and a transvaginal ring?

combination of ethinyl estradiol and progestin

Which population CANNOT use a transdermal patch?

NOT for women >198 lbs (too much adipose tissue)

What are the major toxicities of a transdermal patch?

skin irritation; break through bleeding in first 2 cycles

What is important to tell women who insert a transvaginal ring?

Not effective until in place for seven days

How long can you remove your vaginal contraceptive ring?

not longer than 3 hours

What hormone is used for injectable contraception?

medroxyprogesterone

What is the dosing schedule for injectable contraception?

injected every 3 months; discontinue after 2 years unless no alternative

What are some adverse effects of injectable contraception?

amenorrhea common; irregular bleeding can occur; weight gain, HA, decreased bone density; delayed return to fertility (6-12 months)

What hormones are in an "implant"?

progesterone only (usually etonogestrel)

How does an "implant" work?

single rod implanted under the skin of the upper arm and is effective for 3 years

How does emergency contraception work?

progestins taken to prevent or delay ovulation

What hormones are found in Plan-B and Preven?

OTC levonorgestrel 2 doses in 12 hours

What is another, non-recommended way to administer emergency contraception?

taking many oral contraceptives with doses equivalent to 1.5 mg levonorgestrel

What can be inserted within 5 days to act as emergency contracption?

copper IUD

When is it best to take emergancy contraception?

within 72 hours of intercourse

If you vomit within 1 hour of taking single-dose 1.5 mg levonorgestrel, what should you do?

take another dose

Who can get emergency contraception?

without prescription for women 17 years or older

When must diaphragms be placed?

6 hours BEFORE sex

What is found in spermacides?

Nonoxynol-9 (surfactant) with 100-150mg dose

How long are spermacides effective?

1 hour

What are some adverse effects of spermacides?

irritation of vaginal mucosa, TSS

What do sponges contain?

Nonoxynol-9

What is a very negative aspect about sponges?

must remain in place 6 hours after intercourse

How does the "calendar method" work?

detect ovulation by increased body temperature (around 1 degree) due to progesterone increase just before LH surge. Avoid intercourse on presumed fertile days.

Where is ERα located?

female reproductive tract

Where is ERβ located?

prostate and ovary

What is the pro-drug that is converted to ethinyl estradiol?

mestranol

What is special about the formulation of ethinyl estradiol?

Native estrogens are rapidly degraded by first-pass so not effective orally. Ethinyl estradiol has ethinyl groups (triple bonds) that greatly decrease hepatic metabolism.

What types of estrogens is long-acting and used for hypogonadism in young girls?

estrogen esters (IM)

What type of estrogen is used in patches and rings?

ethinyl estradiol

What are the toxicities of estrogens?

Increase clotting factor synthesis (stroke, DVT); high dose stimulates growth of endometrial and breast tumors

List progestins used for contraception.

Norethindrone Norgestrel Levonorgestrel

What are some adverse effects of progestins?

Weight gain, reversible decrease in bone mineral density (high doses)

List the anti-estrogens.

Clomiphene | Fulvestrant (IM)

What is the indication for clomiphene?

Used for ovulation induction; antagonist effect in pituitary increases gonadotropins

What is the indication for fulvestrant?

Used in treatment of women with breast cancer that has resistance to tamoxifen

How does clomiphene work?

Act on ERs in the hypothalamus to block feedback inhibition of natural estrogens and stimulate release of GnRH which stimulates the pituitary to increase LH and FSH secretion leading to ovulation

What do anti-progestins do?

Produces abortion by blockage of progesterone binding to receptor

LIst the anti-progestins.

Mifepristone (RU 486) | Onapristone

What are the toxicities of anti-progestins?

Vaginal bleeds, Severe abdominal cramping, GI disturbances, atypical infection

What is the “French Abortion Drug”?

mifepristone - VERY tightly regulated!

Which anti-progestin is a more pure antagonist?

onapristone