Contraceptives

Levonorgestrel Plan B & Next Choice has two pills, one that should be taken within 72 hours of unprotected intercourse and the next that is taken 12 hours later. Plan B One-Step contains one tablet that should be taken within 72 hours after unprotected intercourse.

Both Plan B, Next Choice, and Plan B One-Step, emergency postcoital contraceptives, contain what? What is the difference between these contraceptives?

1. Progestin 2. Used in contraception

Desogestrel 1. Mechanism of action 2. Use

1. Progestin 2. Used in contraception

Norethindrone 1. Mechanism of action 2. Use

1. Progestin 2. Used in contraception

Norgestimate 1. Mechanism of action 2. Use

1. Progestin 2. Used in contraception

Norgestrel 1. Mechanism of action 2. Use

Hormonal and non-hormonal Oral and non-oral Combination estrogen and progestin and progestin-only oral contraceptives

What are the two big groups in contraceptive method? Hormonal contraceptives fall into two groups as well. What are they? What are the two types of oral contraceptives?

Heavy smokers (≥15 cigarettes per day) who are older than 35 years of age.

What is the most important absolute contraindication for the use of oral contraceptives?

The low hormone content has decreased adverse effects and risks associated with oral contraceptive pills. They are more likely to result in contraceptive failure if doses are missed.

Combined oral contraceptives most commonly used today are called low dose and contain 35 µg of ethinyl estradiol or less. How is this beneficial? How can this cause complications?

1. 21 hormonally active pills are given followed by a 7-day placebo phase to allow for withdrawal bleeding. 2. Hormone containing pills are given for 84 days and are then followed by a 7-day placebo phase which results in 4 menstrual cycles per year 3. Continuous combination regimens are given with 21 days of hormone containing pills and then very low-dose estrogen and progestin for an additional 4-7 days so that no menstrual cycles occur

Describe the 3 types of combined oral contraceptives: 1. 21 hormonally active pills 2. Extended-cycle formulations 3. Continuous combination regimens

1. Progestin 2. Used in contraception

Drospirenone 1. Mechanism of action 2. Use

1. Contains ulipristal acetate which acts as a progesterone antagonist to inhibit or delay ovulation. 2. Emergency postcoital contraception No, it is by prescription only. Within 5 days.

ELLA 1. Mechanism of action 2. Use Is this available over the counter? How long after unprotected intercourse should this be taken?

1. Both ethinyl estradiol and progestin 2. Both ethinyl estradiol and progestin 3. Progestin-only injection that contains depot medroxyprogesterone acetate (DMPA). 4. Progestin 5. Levonorgestrel Every 3 months, IM. It can cause significant loss of bone minerally density that can be irreversible. 3 years.

What do the following non-oral hormonal contraceptives contain? 1. The patch 2. The ring 3. Depo-provera 4. Implanon 5. Mirena How often does Depo-provera need to be given? What is a complication of Depo-provera? How long is implanon effective?

Oral contraceptive pills Daily administration is required and inconsistent use of oral contraceptive pills may increase failure rate.

What is the most widely used form of hormonal contraception? What is a major disadvantage of these drugs?

Leave No Notes Don't Nestimate Drugs Levonorgestrel & Norgestrel: highest Norethindrone: lower Desogestrel & Norgestimate: even lower Drospirenone: anti-androgenic

Almost all currently available progestins have some androgenic activity but each drug varies in their androgenic activity. Rank the progestin drugs from highest to lowest in their androgenic activity. Norethindrone, norgestrel, desogestrel, drospirenone, norgestimate, & levonorgestrel.

Nausea, bloating, and breakthrough bleeding can occur but this typically improves spontaneously by the third cycle. Cerebrovascular accidents so women who develop migraines when taking oral contraceptives should stop taking the contraceptive. Progestins compete with insulin for its receptor but current oral contraceptive have a low progestin content and they rarely cause hyperglycemic events. Some of the progestins act as androgenic activators that can lead to acne, oily skin, and hirsutism. These patients should be switched to a contraceptive that has less androgenic effect.

Although the reduction in estrogen and progestin content has led to a reduction in adverse effects, adverse effects still exist. What are the adverse effects that typically resolve and when do they resolve by? Headaches are another adverse effect of oral contraceptives and it can lead to migraine. What can be associated with this complications? How do oral contraceptives lead to insulin resistance? How do oral contraceptives lead to hirsutism? How should these patients be treated?

They are more common in women who are older than 35 and smoke. The risks are also increased by obesity, HTN, and diabetes. Estrogen increases the production of factor VII, factor X, and fibrinogen which leads to an increased change of a thromboembolic event. The oral contraceptive should be stopped and other contraceptive measures should be used.

Cardiovascular disorders including thromboembolism, thrombophlebitis, HTN, MI, and cerebral and coronary thrombosis can occur in women taking oral contraceptives. What leads to an increased risk of this complication? How do oral contraceptives lead to this complication? Oral contraceptives can lead to depression in about 6% of patients. What is the treatment of these patients?

1. Synthetic estrogen 2. Used in contraception

Ethinyl estadiol 1. Mechanism of action 2. Use

Oral contraceptives are metabolized by CYP450 enzymes. Rifampin induces these enzymes which can lead to an increased metabolism of estrogen and a decrease in effectiveness of the contraceptive. During administration of this drug backup non-hormonal contraceptive methods should be recommended. Carbamazepipne, phenytoin, phenobarbital, and St. John's Wort. Many anti-epileptics can lead to induction of CYP450 enzymes.

How are oral contraceptives affected by cytochromes and how can Rifampin lead to changes in the effectiveness of oral contraceptives? Name some other drugs with a similar effect that can lead to decreased effectiveness of oral contraceptives.

Estrogen leads to suppression of LH and FSH release and ovulation does not occur. Progestin thickens cervical mucus which prevents sperm penetration and induces changes in the endometrium that impair implantation.

How do combination contraceptives work to prevent conception?

Ethinyl estradiol is conjugated in the liver, excreted in the bile, hydrolyzed by intestinal bacteria, and resorbed as active drug. Many broad-spectrum antibiotics reduce the population of intestinal bacteria which can lead to inhibition of the hydrolyzation of the drug which can lead to a decrease in estrogen levels.

How does the administration of antibacterials, such as broad-spectrum antibiotics, lead to a decreased effectiveness of oral contraceptives?

A norgestrel or levonorgestrel containing oral contraceptive in high doses can be used for emergency contraception within 72 hours of unprotected intercourse. The copper IUD, which can be inserted within 5 days of the unprotected intercourse, can act as an emergency contraceptive.

If Plan B, Next choice, etc. are not available for emergency contraception, what can be used? Besides taking a pill, what else has been approved for emergency contraception?

1. Progestin 2. Used in contraception

Levonorgestrel 1. Mechanism of action 2. Use

Monophasic preparations contain fixed doses of estrogen and progestin in each active pill regardless of the time of the month that the drug is taken. Biphasic and triphasic preparations contain varying preparations of one or both hormones during the pill cycle.

Oral contraceptives are available in mono phasic, biphasic, and triphasic preparations. What is the difference?

1. Progestin 2. Used in contraception

Medroxyprogesterone acetate 1. Mechanism of action 2. Use

1. Synthetic estrogen 2. Used in contraception It is a prodrug that is converted to ethinyl estradiol.

Mestranol 1. Mechanism of action 2. Use How is this drug activated?

No risk of thromboembolic events is the major benefit. There is also decreased dysmenorrhea, decreased menstrual blood loss, and decreased premenstrual syndromes. Unscheduled bleeding and spotting. They lead to thickening of the cervical mucus which decreases sperm penetration and lead to endometrial alterations that impair implantation.

Progestin-only pills are not widely used in the US because they are slightly less effective but have some benefits. What are these benefits? What is a common complication? Progestin-only pills only block ovulation in 60-80% of cycles. How are they effective?

It decreases the incidence of endometrial and ovarian cancer but their ability to induce other cancers is controversial. It is a change in pigmentation due to estrogens stimulation of melanocyte production. There can be an impact on HDL, LDL, triglycerides, or total cholesterol but most low-dose oral contraceptives have little impact on the lipid profile.

What affect do oral contraceptives have on the incidence of cancer? Some other complications are melasma, amenorrhea, and changes in lipid profile. What is melasma? What changes can occur in the lipid profile and how common are these changes?