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