Oral Contraceptives

Indications (other uses) for oral contraceptives include what?

- Acne - Dysmenorrhea - Polycystic ovary syndrome - Endometriosis - Irregular menstrual cycles

These COCs have an official acne indication:

- Alesse - Tri-cyclen - Yasmin - Yaz - Diane-35/Cyestra-35

What cancers are contraindicated?

- Breast cancer - Endometrial cancer

Contraindications of oral contraceptives

- Certain cancer - Abnormal clotting - Severe or uncontrolled hypertension - Smoking and over 35 years old

Oral Contraceptives include what three types of pills?

- Combination pills - Progesterone pills - Estrogen pills

What is the composition of Diane-35, and what is its indication?

- EE 35mcg - Cyproterone acetate 2mg for acne treatment

What are the menstrual cycle phases?

- Follicular phase - Ovulation - Luteal phase

What are the oral contraceptives phasic types (3)?

- Monophasic - Multiphasic/Triphasic - Extended cycle

What are side effects of COC pills?

- Nausea - Vomiting - Breast tenderness - Spotting - Edema - Weight gain - Blood clots

Give examples of Progesterone pills (medications)

- Norethindrone - Norgestimate - Levonorgestrel - Desogestrel - Drospirenone

Who should not use COCs due to increased risk of MI/stroke?

- Smokers over 35yo - Women with hypertension

What are the side effects of progesterone only pills?

- Spotting - Acne - Nausea

What are the more common SE of COCs?

1) BTB, spotting 2) Amenorrhea 3) N&V 4) Breast tenderness 5) Cyclic weight gain (water retention) 6) Hyperpigmentation of face 7) Mood change 8) Acne, oily scalp

What are the 8 contraindications for COCs?

1) History or current thromboembolic disorder, or CAD 2) Uncontrolled hypertension 3) Liver disease 4) Breast cancer, or estrogen-dependent cancer 5) Undiagnosed abnormal vaginal bleeding 6) Known or suspected pregnancy 7) Smoking in women >35 yo 8) Lactation (until 6 weeks post partum)

Name some monophasic OCs with sub-50mcg EE, and give composition and %BTB.

1) Marvelon (EE 30mcg/Desogestrel 0.15mg) - 9.9%BTB 2) Seasonale (EE 30mcg/Levonorgestrel 0.15mg) - 15.0%BTB 3) Yasimn (EE 30mcg/Drospirenone 3mg) - 13.3%BTB 4) Alesse (EE 20mcg/Levenorgestrel 0.1mg) - 20-29%BTB

What are some other mechanism of COC due to the progestin component?

1. Contractions uncoordinated - sperm and ovum transport impaired 2. Thickens cervical mucus 3. Endometrium atrophy - impairs implanation

MOA for oral contraceptives

1. Estrogen suppresses FSH release from pituitary gland 2. Leads to follicle maturation 3. Progesterone (major player) blocks LH surge, thickens cervical mucus 4. Induces endometrial atrophy leads to ovulation

What is the % of women who ovulate while on Micronor?

30-40%

What is the pregnancy rate of micronor with typical use?

5-10%

When do you discontinue oral contraceptives? (acronym)

ACHES

What is A in ACHES?

Abdominal pain (severe)

What does extended cycle dosing mean?

Active pills taken for more than 21 days

What is LH surge for?

Blocking is necessary for ovulation

Of the side effects, which is rare?

Blood clots (due to estrogen component)

Combination pills are have what type of hormones?

Both estrogen and progesterone like hormones

What are 3 serious increased risks of COCs?

CVD Venous thromboembolism MI and stroke

What is an anti-seizure medication that has a drug interaction with oral contraceptives ?

Carbamazepine

General class of drug interactions that occur include what?

Certain antibiotics Certain natural supplements Anti seizure medications

What is C in ACHES?

Chest pain (severe), SOB

Why is abnormal clotting a contraindication?

Clotting risk increases due to estrogen component

Luteal phase involves what?

Corpus luteum maturation

Ovulation phase begins when?

Day 14

What happens in the drug interactions listed earlier?

Decreases OC (oral contraceptive) plasma concentration and effectiveness

Which 2 monophasic OCs have the highest %BTB?

Demulen 30 - 37.4% Minestrin 1/20 - 29.7%

What does multiphasic/triphasic dosing mean?

Different dosing each week for 21 active pills, mainly for *progesterone* changes

What is the composition, and dose/regime of Evra?

EE 0.60mg (average 35mcg/day) Norelgestromin 6mg (average 200mcg/day) - 1 patch/week for 3 weeks - followed by 1 week off

What is the mechanism by which OC induced increased blood pressure? Which OC can counter this effect?

EE activates RAAS (increases angiotensinogen) Drospirenone blocks aldosterone action.

What pills are rarely used?

Estrogen pills

What is E in ACHES?

Eye problems : blurred vision, flashing lights

What hormones are involved?

FSH, LH, estrogen, progesterone

Follicular phase involves what?

Follicle maturation

How is drospirenone different than other progestins in terms of its actions?

Has anti-androgenic activity Has anti-mineralocorticoid activity

What is H in ACHES?

Headaches (severe)

What increased SE are associated with Evra when compared to COC?

Increased breast tenderness Increased dysmennorhea

When may the use of Micronor be a benefit over COC?

Lactation When estrogen is contraindicated

What is the composition, dose/regimen SE of plan B?

Levonorgestrel 2 pills of 0.75mg within 5 days of unprotected sex. *SE*: - N&V - Spotting - Cramping - Fatigue - Breast tendernes

Monophasic oral contraceptives includes (what drugs)?

Loestrin, Minestrin, Alesse, Yasmin

What is the dose/regimen for depo-provera?

Medroxyprogesterone acetate susp. 150 mg IM q90d

What is followed after the luteal phase?

Menstruation or pregnancy

Name a progestin-only pill and the composition

Micronor Norethindrone 0.35mg

What are progesterone pills also known as?

Mini pills

What are the main mechanisms of COCs?

Negative feedback suppression of Gn secretion: - Decrease FSH production to <70% - No LH surge - Minimal follicular development and no ovulation

Overall, what is the effect of COC on cancer?

No increase in risk.

What are the 4 common progestins used in OCs?

Norethindrone Levonorgestrel Desogestrel Drospirenone

What is the risk of VTE for OC users and non-user. What is the risk in pregnancy?

OC users - 9-10/10000 Non users - 4-5/10000 Preganacy - 29/10000

Why is hypertension a contraindication?

Oral contraceptives tend to increase blood pressure

What kind of feed back is contraception?

Orchestrated through negative feedback that tricks the body into thinking it is pregnant

Name an Triphasic OC and its composition

Ortho 7/7/7 - EE 35mcg X 21 days - Norethindrone 0.5mg X 7days, 0.75mg X7days, 1mg X7days

Multiphase oral contraceptives includes (what drugs)?

Ortho 7/7/7, Tri-cyclen, Triquilar

Name a monophasic OC with 50mcg estrogen

Ovral - EE 50mcg - norgestrel 0.25mg Has been discontinued in Canada. There are no COCs with >35mcg EE.

Counseling Points SUPPS, first P

P for potential, POTENTIAL** side effects and what to do if they persist, STDs possibility

Counseling Points SUPPS, second P

P for potential, discuss POTENTIAL** drug interactions

Why is smoking and 35 years older a contraindication?

Predisposes to more cardiovascular risks such as strokes, heart attacks

What is estrogen important for?

Prevents continuous endometrial atrophy

What are some non-contraceptive risks that are reduced with OC use?

Reduced risk of: - Iron-deficiency anemia - Dysmenorrhea - Functional ovarian cysts - Endometrial and ovarian cancer - Pelvic inflammatory disease - Benign breast disease - Colorectal cancer

Which antibiotic has a drug interaction with oral contraceptives ?

Rifampin

What drugs may interact with OCs?

Rifampin Anticonvulsants (Phenytoin, Carbemazepine) Antibiotics

Counseling Points SUPPS, first S

S for same, take medication at SAME** time every day

Counseling Points SUPPS, last S

S for skipped, what about SKIPPED** dose?

What are the SE of Depo-provera, and the disadvantage?

SE: - Nausea - Weight gain - Menstrual irregularities *Delay in return of fertility longer than other hormone contraceptives* - up to 1 year

What does monophasic dosing mean?

Same dosing for all 21 pills

Extended oral contraceptives includes (what drugs)?

Seasonale, Seasonique

What is S in ACHES?

Severe leg pain

What is an natural supplement that has a drug interaction with oral contraceptives ?

St Johns Wort

What is the signifiance of placebo pills?

To keep patient continually taking the product for adherence so they do not forget to take them

Counseling Points SUPPS, U

U for use, USE** back up methods until at least 7 days have passed since start of regimen

What are the effects of OC on blood lipids in general (in terms of estrogen and progestin)?

Vary with dose and androgenicity of progestin, but HDL, LDL still in normal range: - Estrogens increase HDL, decrease LDL - The more androgenic the progestin, the more estrogen effects are opposed.

When can spotting occur as a side effect?

Within many months after initial onset of therapy; should resolve after 3 months

Which monophasic OC does not have androgenic activity?

Yasmin