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TOPIC DISCUSSION

CONTRACEPTION
For NAPLEX Study

Objectives

 Describe reproductive hormones


 Define and list contraception options
 Compare and contrast the major advantages and disadvantages of each class of
contraception
 Recognize counseling pearls for each class of contraception

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THE HORMONES

 In humans, all steroid hormones are derived from cholesterol


 Steroid hormones are then modified into sex hormones for both female and male
o Different modifications for different hormones
o Each set of alterations to the steroid backbone alters the affinity of the
steroid for a give steroid receptor

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GnRH FSH & LH
Hypothalamus Anterior Pituitary Ovaries (estrogen, progesterone)
 Gonadotropin releasing hormone (GnRH)
o Stimulates FSH and LH
o Made in the hypothalamus
Synthesis and secretion controlled by estrogen feedback mechanisms

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The Cycle (AKA “the confusing stuff”)

 Normal menstrual cycle ranges from 23 – 35 days


 The start of menses is the beginning of the cycle and is counted as day 1
o Occurs during the follicular phase
o Estrogen and progesterone levels are low
 Estrogen steadily increases and peaks right before the luteal phase
o Estrogen and progesterone cause the endometrium to thicken
(proliferative phase)
o The increase in estrogen leads to a surge in LH
 LH surge triggers ovulation (release of the egg) and the luteal phase

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Summary
 Menses occurs during follicular phase and is counted as
day one
o Estrogen and progesterone levels start off low
o FSH causes estrogen to surge
o Surge in estrogen causes LH and FSH to spike
 LH triggers ovulation
 Start of luteal phase is the start of ovulation

HORMONAL CONTRACEPTIVES
Inhibiting the production of FSH and LH, which prevents ovulation

 Inhibits sperm penetration by altering cervical mucus


 Estrogen + progestin OR progestin alone
o Combined Oral Contraceptives (COC); Progestin Only Pills (POPs);
Transdermal Patch; Vaginal Contraceptive Ring; Injection; Long-Acting
Reversible Contraception (implants, IUD)

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 NOTE: If implantation of the fertilized egg in the uterus has already taken place,
hormonal contraceptives are not effective, and pregnancy will proceed normally

ESTROGENS AND PROGESTINS

 Estrogens
o Ethinyl estradiol (EE)
 Most commonly used for contraception
o Mestranol
 Converted to EE by liver
 50% less potent than EE
o Estradiol valerate
 Used in some COC’s and in the injectable contraception
 Progestins
o First generations
 Norethindrone, norethindrone acetate, ethyndiol
o Second generation
 Norgestrel, levonorgestrel
 More potent and longer half-life than 1 st gen, more androgenic
activity
o Third generation
 Desogestrel, norgestimate
 Less androgenic activity than 2nd gen, increased risk of
thrombosis
o Fourth generation
 Drospirenone (Yaz, Yasmin, Beyaz, Ocella)
 Anti-androgenic and mineralocorticoid activity
 Possibly increased risk of thrombosis

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COMBINED HORMONAL CONTRACEPTIVES
MOA
 Progestin: Thickens cervical mucus, inhibits sperm passage through the uterus
and sperm survival; inhibits ovulation (negative feedback on hypothalamus)
 Estrogen: Suppresses FSH release from the pituitary (blocks LH surge);
stabilizes the endometrial lining

COC type Pearls Formulations


Monophasic  Consistent level of 21/7: Junel Fe 1/20,
estrogen and progestin in Microgestin Fe
all active pills 1/20, Sprintec,
Loestrin, Yasmin
 21/7 regimen; can be
(and many more)
used for extended or
continuous cycles 24/4: Loestrin 24
Fe, Yaz, Beyaz

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24/2/2 (24 active, 2
EE only, 2 inactive):
Loestrin Fe
Biphasic and  Varying amounts of  Ortho Tri-
Triphasic progestin and estrogen Cyclen, Tri-
from week to week Sprintec, TriNessa
 21/7 regimen
 If “phasic” in the name,
hormones are delivered in
phases
Four-phasic  Four different phases,  Natazia
(quadraphasic) each containing different
doses of estrogen and
progestin
 26/2 regimen
Extended/Continu  Extended: fewer  Seasonique, Lo-
ous Cycle periods; Continuous: No Loestrin, Natazia,
periods Yaz, Beyaz (off-
label, extended
 Reduced risk of
cycle)
pregnancy with missed
pills (highest when 7 or  Amethyst
more are missed) (continuous)
 More convenient
menstruation (or none at
all)
 Increased
breakthrough
bleeding/spotting

 Yasmin, Yaz
o Has mild K+ sparing diuretic to reduce bloating and other side effects
o Contraindicated in renal or liver disease; monitor kidney function while
using
 Seasonique
o 84 days of EE + levonorgestrel followed by 7 days of low dose EE

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COC Counseling Pearls
 Take pill at the same time every day (any time during the day)
o Helpful to coordinate it with another daily task
 Missed period is somewhat common, does not mean pregnancy
o If 2 consecutive missed periods, consider pregnancy test
 Missed doses
o <24 hours: ‘late’ >/= 24 hours: ‘missed’
o May take 2 pills in one day

NON-ORAL CHCs

NuvaRing
 Worn for 21 days, removed for 7 days, insert new ring vaginally

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 Can be used as continuous cycle: 28-30 days worn, then insert new ring
immediately
 Stored in refrigerator, stable at RT for 4 months
 Same SE profile as COC plus vaginal irritation and wetness
o Breast tenderness < COCs
o Unscheduled bleeding </= COCs (can use 4-day ring free period to help)
 Can be left in during sex, with tampon use, and while using topical therapies
Xulane
 Transdermal patch
o Worn on the upper outer arm, back, abdomen, or buttock
 Apply weekly for 3 weeks, 7 day patch-free
o Continuous cycle not recommended – increase VTE risk (more estrogen
exposure than other combined hormonal contraceptives)
 SE profile same as COCs + application site reaction
 Less effectiveness in women > 198 lbs.

CHC Monitoring
 SE
o Estrogen
 N/V; bloating; decreased libido; breast tenderness; breakthrough
bleeding
o Progestin
 Nausea; headache; bloating; dizziness; weight gain; breakthrough
bleeding
 Severe adverse events
o ACHES
o Abdominal pain, chest pain, headache, eye problems, severe leg
pain/swelling

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Summary

Boxed Warning
 All estrogen products
 Do not use in women >35 years old and smoke
 Xulane: increased risk of VTE/PE vs COCs

PROGESTIN ONLY CONTRACEPTION


Available options

 Pills; injections; implant; IUD

Progestin Only Pills (POPs; mini-pill)


 Norethindrone
 Preferred in women who have contraindications to estrogen-containing
contraceptives
 No placebo pills
 MOA

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o Thickens cervical mucus inhibiting sperm passage and survival
o Inhibits ovulation with negative feedback on hypothalamus reducing
secretion of FSH and LH
o Alters endometrial lining affecting implantation
o Slows the movement of the ovum through fallopian tubes
 Monitoring
o Nausea; HA; dizziness; bloating; weight gain; breakthrough bleeding; acne
flare
o Increased prevalence of follicular ovarian cysts
 Counseling pearls
o Take pill at the same time every day
o Adherence is more strict vs COCs

INJECTION CONTRACEPTIVES

Depot medroxyprogesterone acetate

 MOA
o Transforms a proliferative endometrium into a secretory endometrium
o Inhibits secretion of pituitary gonadotropins
 May be preferred vs CHC in women who have contraindications to estrogen-
containing contraceptives
 Depo-provera
o 1 injection every 3 months (13 weeks)
 Depo-subQ Provera
 Monitoring
o Same SE as POPs + nervousness and abdominal pain
o Injection-site reaction
o Weight-gain more prevalent

Summary

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LONG-ACTING REVERSIBLE CONTRACEPTIVES
IUDs - Hormonal

 Mirena; Skyla; Kyleena; Liletta


 Most common contraceptive internationally
 3-5 year effectiveness
 Return to fertility within 30 days
 MOA
o Thickens cervical mucus that inhibits sperm passage
o Inhibits ovulation
o Alters endometrial lining
IUD – non-hormonal
 ParaGard
o Effective up to 10 years
o Easily reversible with rapid return to fertility
o MOA: inhibits fertilization via toxic effects of copper on sperm and ovum
o Causes heavier menstrual bleeding and cramping

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Nexplanon
 Implanted in the arm, under the skin
 Used for up to 3 years
 Possible decrease in efficacy in obese patients
 Main SE: irregular menstrual bleeding

Contraception overview

HELPFUL TABLES

TYPE OF PATIENT PRODUCT SELECTION


CONSIDERATIONS
Acne Use COC with lower androgenic (Ortho-Cyclen)
activity or no androgenic activity (Yaz, Yasmin).
Breastfeeding POPs or nonhormonal method

Estrogen contraindication Choose POPs or nonhormonal method


(including clotting risk)
Migraine With aura: POPs or nonhormonal method
W/o aura: any method
Heavy menstrual bleeding Natazia and Mirena are indicated for this. Also
consider extended/continuous regimens
Hypertension If uncontrolled, POPs or nonhormonal methods

Mood changes or disorder Monophasic COC or extended cycle or


continuous with dorspirenone
Nausea Take at night, decrease estrogen dose. Also: ring
or nonhormonal
Overweight Do not use DMPA if trying to avoid further weight
gain
Postpartum POPs or nonhormonal within 3 weeks

Premenstrual dysphoric Yaz (or antidepressant)


disorder
Spotting/breakthrough Common when intiating extended cycles, usually
bleeding resolves in 3-6 months. If early or mid cycle
spotting, increase estrogen dose. If later in cycle,

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increase progestin
Wishes to avoid monthly cycle Extended or continuous formulation. Can
consider monophasic 28 day formulation and skip
placebo pills
Fluid retention/bloating Choose product with drospirenone

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