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What is the major estrogen produced and what part of the body produces it in women?
What happens to estradiol in the periphery? How is estradiol metabolized and eliminated?
(What happens in the periphery to estradiol)
It's converted into ESTRIOL and ESTRONE
(Metabolism & Elimination of Estradiol)
What effect do estrogens have on the body?
Primary & Secondary Sex Characteristics
Processes related to reproduction
What are the metabolic effects of estrogen?
(Metabolic Effects of Estrogens)
Block bone Resorption (Saving Bone Mass)
Enhance Bone Mineralization (Possibly)
Affect Clotting Factors
What are the non contraceptive used of estrogen?
(Non Contraceptive Uses)
Post Menopausal Hormone Therapy
Female Hypogonadism (Induces Puberty)
Acne + Contraception (@ Least 15 Yrs Old)
When estrogen is used as Post Menopausal Hormone Therapy, what are the things it's treating (7)?
(Post Menopausal Hormone Therapy used for...)
Severe Vasomotor Symptoms Relief
Vulvar & Vaginal Atrophy (Urogenital Atrophy)
Osteoporosis Prevention (Alt Treatments Preferred)
+ Effect on Wound Healing
What are the routes of administration for estrogen therapy?
(Routes of Estrogen Administration)
Intravaginal (Tablets/Creams/Vaginal Rings)
Parenteral (IV/IM) - For heavy uterine bleeding ctrl
What are progestins? What are their physiological effects (6)? Where is progesterone produced in the body?
Compounds that act/mimic progesterones
(Progestin's Effects on Body)
Converts the endometrium from a proliferative to a secretory state.
Drop of progesterone triggers menses
Affect endometrium making secretions scant and viscous
Prepare uterus for implantation
Suppress uterine contractions (During Pregnancy)
Suppress release of LH & FSH preventing follicular maturation
(Where it's made)
When is progesterone given during postmenopausal hormone replacement therapy?
Given during the second half of the cycle. (Starting on day 16 and going for 12-14 days for example)
What are the non contraceptive uses of progesterone(6)?
(Non Contraceptive Uses of Progesterone)
Counteract adverse effects of estrogen during hormone replacement therapy.
Helps regulate monthly cycle for pt's experiencing dysfunctional uterine bleeding
Can induce menstrual flow (For Amenorrhea)
Support early pregnancy for (IVF)
Induce beneficial responses (Women with Metastatic Endrometrial Carcinoma)
Megestrol (Progesterone Derivative) given to increase appetite & weight in AIDS or cancer cachexia.
What are the routes of administration for progesterone?
(Routes of Admin. Progesterone)
Topically (Transdermal, Intravaginal)
Implant Intrauterine Device
What are the regimens available for postmenopausal hormone replacement therapy? What is the purpose of estrogen replacement? Why give progestin as during replacement therapy? When would you NOT NEED to give Progestin?
(Hormone Regimens Available)
Estrogen (For Replacement)
Estrogen + Progestin
(Why give Progestin?)
Counterbalances the estrogen stimulation of the endometrium (Prevents Uterine Cancer)
(When not to give Progestin)
When someone doesn't have a UTERUS
What are the RISKS associated with hormone replacement therapy (9)? What should be done to reduce the risk of CA?
(Risks of HT)
Endometrial Cancer Risk (Unopposed Estrogen Tx)
Invasive Breast Cancer & Breast Tenderness
Dementia Risk (Azh)(>65 yrs) (Estrogen + Progestin)
GI Disturbances (Nausea/Gall Bladder Disease/Jaundice with Liver Pts)
(Reducing Risk of CA)
What is the pregnancy category for estrogens and progestins? What are the effects specifically?
Both are (Category X)
Progestins during 1st 4 months associated with birth defects
What are SERMS and what is their MOA? What tissues will SERMS Block their target receptors? What tissues will SERMS activate their target receptors? Which SERM does NOT activate estrogen receptors in the endometrium?
(SERMS and their MOA)
Selective Estrogen Receptor Modulators that bind to estrogen receptors producing both estrogenic & antiestrogenic effects.
(SERMS as BLOCKERS act on)
Breast tissue estrogen receptors
(SERMS as ACTIVATORS act on)
(SERM that does NOT activate endometrium)
What do SERMS do when they BLOCK estrogen receptors? What about when they act as agonists? What is an important RULE to remember about prescribing SERMS?
(SERMS as Blockers)
In breast tissue, SERMS block estrogen receptors thus inhibiting cell growth.
Produce vasomotor symptoms (Hot Flushes)
(SERMS as Activators)
BONE - SERMS protect against osteoporosis
LIVER - Favorable effects on serum lipids
Don't prescribe SERMS with ESTROGEN
What are the adverse effects of the SERMS? What is special about Raloxifene?
Endometrial Cancer (Some SERMS)
Thromboembolisms (bc of ALL SERMS effects on clotting factors)
Does not activate estrogen receptors in endometrium so it does NOT pose a risk for uterine cancer or endometrial effects
What are the SERMS?
What is Raloxifene indicated for? What is its MOA?
(Raloxifene indications and MOA)
BLOCKS estrogen receptors in BREAST & therefore given to PM women at risk for invasive breast cancer.
AGONIZES estrogen receptors in LIVER & BONE thereby reducing LDL and OSTEOPOROSIS and CLOTTING
What is Tamoxifen indicated for? What is it's MOA?
(Tamoxifen indications and MOA)
Used for treatment of metastatic breast cancer or as adjuvant treatment for CA post mastectomy, axillary dissection, or radiation. Also preventative treatment of breast CA in high risk patients.
Does all of the above by BLOCKING estrogen receptors in breast tissue
What is Toremifene indicated for?
Treatment of advanced breast cancer
What are the adverse effects of Raloxifene? What is the BLACK BOX WARNING for this drug? What is the pregnancy category?
N/V & Dyspepsia
(Black BOX Warning)
Venous Thromboembolism (VTE)
Fatal Stroke risk for women with CAD or risk factors for coronary events
What are the 3 drug interactions for the SERMS? Explain
(Drug Interactions with Explanations)
Drugs that are Protein Bound - Competes with SERMS
Bile Acid Resins - Combo decreases [Raloxifene]
Thyroid Hormones - Separate Admin. by 12 Hours
What is the ROLE of birth control? What does it NOT prevent? What are the types of BC?
Interfere the reproductive process at any step from gametogenesis to Nidation
(BC DOesn't Prevent)
STD's so use a condom
(Types of BC)
What is the MOA for estrogen/progesterone contraceptives? What are the 2 classifications for these drugs?
Decrease fertility by inhibiting ovulation
Estrogen + Progestin Combiniations
What are the 4 main subgroups of combination contraceptives? What does each group do?
Monophasic - Hormone doses CONSTANT thru cycle
Biphasic - Estrogen = Constant & Progestin increases @ 2nd half of cycle
Triphasic - Cycle is in 3 phases with progestin dose changing during each phase
Four Phasic - Estrogen & Progestin doses change through entire cycle
What are the 8 main adverse effects of the combination contraceptives? Which part of the combo is responsible for most of the ADR's? What is the black box warning for these drugs? What diseases DO NOT happen with the COMBO's and why?
Thromboembolic Events (Venous & Arterial/PE/DVT/MI/Stroke)
Hypertension (bc drugs increase Angiotensin & Aldosterone levels)
Benign Hepatic Adenoma
Pregnancy Category X
Glucose Intolerance (From Progestin)
Abnormal Uterine Bleeding (See Next Few Cards)
Estrogen/Progestin Imbalance Effects (See Next Cards)
(Part of the drug responsible)
(Black Box Warning)
SMOKING causes Cardiovascular events (Age>35) +(#Cigs>15/day)
(Diseases that DO NOT occur with CC's)
Ovarian, Breast, Cervical, and Endometrial Cancer bc Progestin BLOCKS the Estrogen
Can women with existing breast carcinomas use the COMBO oral contraceptives?
Who should not take (Contraindicated) the Oral Contraceptive Combos(10)?
Surgical Pt's (BC of DVT Risk) - D/C 4 weeks Prior
Cardiovascular Patients (CAD)
Cerebrovascular Disease (HA's/Focal Neurological SS)
Cancer (Liver Tumors, benign or malignant)
Cancer (Breast or estrogen dep. carcinomas)
Liver Disease (Active)
Smokers (Age > 35)
Pregnant Women (Teratogenic Effects if COMBO's taken at high levels)
What happens to uterine bleeding for women taking combination oral contraceptives (CC's)? When may breakthrough bleeding occur? What may bleeding irregularities suggest & What should be done?
CC's decrease or eliminate menstrual flow initially. Breakthrough bleeding &/or spotting may occur.
Caused by CC's that contain low doses of Estrogen & Progestin.
(Bleeding is a sign)
Irregular bleeding may be a sign of malignancy and should be investigated.
If bleeding stops for 2 consecutive months, what should the clinician do? Once CC's are D/C'd, how long before normal menstruation occurs again?
Determine whether the patient is pregnant.
(How long before normal menstruation occurs)
1 - 3 months
What happens to a patient with an imbalance between estrogen and progestin where there is more estrogen? What about if there is more progestin?
(More Estrogen = B.E.N.)
(More Progestin = F.A.D.)
What must be ruled out before starting someone on Combination Contraceptives (CC's)? Can you give CC's to a breastfeeding patient?
Pregnancy Category X
Don't give to patients unless pregnancy is ruled out
Don't give to breastfeeding patients bc CC's enter breast milk and REDUCE PRODUCTION
What are the drug interactions of the Combination Oral Contraceptives (OC's) which LOWER their effect? Which drugs effects are LOWERED by OC's and why? Which drugs effects are INCREASED by taking OC's? What should be done for patients taking OC's who are Nauseous?
(Drugs that LOWER OC's efficacy through P450 Induct.)
-St. John's Wart-
*Aprepitant (Anti-emetics) - Reduce OC efficacy
(Drugs whose effects LOWERED by OC's)
Warfarin (OC's Incr. Clotting Factors)
Insulin (Progestin reduces Insulin efficacy)
(Drugs whose effects are INCREASED by OC's)
Theophylline (Increased effect by OC's)
Since anti emetics reduce oral contraceptive efficacy, have pt's use back up methods for contraception for 28 days following anti emetic therapy.
What is the principal estrogen in combination contraceptives? What is the principal progestin in these drugs? Which 2 of the MANY progestin drugs have a lower incidence of side effects? What are the estrogen and progestin components of the Transdermal Contraceptive Patch (Ortho Evra)? WHat are the components of the Vaginal Contraceptive Ring (NuvaRing)
(2 Progestins with reduced side effects)
(Ortho Evra Patch Components)
Ethyl Estradiol + Norelgestromin
Ethyl Estradiol + Etonogestrel
What is a major concern regarding Drospirenone? Who would not be prescribed these drugs? What should periodically checked?
Contains both Progestational + ANTIALDOSTERONE actions causing:
(Who should not take this drug)
Pt's on ACE's
PT's On ArB's
How should Ortho Evra be administered? What are the routes of administration? Where on the body should this drug not be used? What is a risk for this drug?
Patch is applied 1/week for 3 weeks
(Routes of Administration)
(Don't put this drug)
NOT on BREAST
Greater Risk than Oral CC's for serious CLOTS
How is the NuvaRing administered? How is the drug distributed and why?
Inserted vaginally for 3 weeks then removed
*Insert new ring 1 week later
(Distribution of drug)
Systemic due to absorption thru vaginal mucosa
How are progestin only contraceptives taken? What is the pregnancy category for these pills? Do these drugs cause breast cancer or thromboembolic disorders like estrogen?
'Mini Pills' are taken continuously the same time each day.
Safer than Estrogen
More Menstrual Irregularity (Spotting)
(Clots and Cancer???)
No BREAST cancer
How are the long acting contraceptives administered? How is MPA administered? How long does MPA work for?
Subdermal Etonogestrel Implant (Lasts 3 Yrs)
Depot Medroxyprogesterone Acetate (MPA)
(Administration of MPA)
(Duration of MPA)
Upon D/C MPA injections, how long will it take for women to become fertile? What are the ADR's for MPA? What is given to minimize the risk of osteoporosis? What's the max time women take MPA?
About 1 year for fertility to return
Osteoporosis (Used long term)
(Given to minimize osteoporosis)
Calcium (1500 mg)
Vitamin D (400 - 800) IU
(Max Period of Time to take MPA)
What are the 3 common intrauterine devices? What is great about these devices? Common ADR's? What are the risks? Who should NOT use these devices?
(3 Common Intrauterine Devices)
Intrauterine Progesterone System
Levonorgestrel-Releasing Intrauterine System (Mirena)
Reliable form of BC
Infertility (Women with STD's)
Ectopic Pregnancy (If one slips by)
(Don't use these if you are)
Have have STD's
What is the definition of Emergency Contraception? What are the reasons for this intervention?
Use of a drug within 70 to 120 hours after unprotected sex for the purpose of preventing unintended pregnancy.
*No Contraception Used
*Ruptured/Slipped Off Condom
*Forgot to take BC
*Forgot to insert ring/Apply the patch/Injection (2wks)
*Diaphragm slid out of place
*Miscalculation of 'Safe Days'
*Failed Coitus Interruptus
*Forced to have intercourse
What are the choices for the Progestin Only Emergency Contraception? What is the progestin & dosage that is given in both cases? What are the dosing options for NEXT CHOICE? When should these drugs be given?
(Choices For Emergency Contraception)
Plan B (Next Choice) (0.75 mg Levonorgestrel)
Plan B (One-Step) (1.5 mg Levonorgestrel)(1 DOSE)
(Dosing Options NEXT CHOICE)
2 Doses (1 pill Q12 hours)
1 Dose (2 pills)
Within 72 hours unprotected sex
What are the side effects of Progestin Only Emergency Contraception? (9)
Heavier Menstrual Bleeding
How is the Emergency Contraception drug Ulipristal administered? What are the adverse effects? When should this drug be given?
(Give this drug)
Within 120 Hours of Unprotected Sex
*Repeat if vomiting occurs within 3 hours!
What are the other drugs that may be given as Emergency Contraception?
Many Oral Contraceptives used off label!
What is the MOA for Mifepristone or Misoprostol (RU486)? What are the dosages? When is this drug given? What should be monitored? What is the black box warning for this drug? What are the ADR's? What are the drug interactions?
Blocks progesterone receptors in the uterus! Uterine motility increase which aborts the fetus.
600 mg for Early Termination
400 ug of Misoprostol x 2 days unless abortion confirmed
(When Given & Rules for Administration)
Pt < 49 Days from last period
Infection with afebrille presentation
Bleeding and Serious Infection
*Drugs that increase Bleeding
*Prostaglandins (Misoprostol + Mifepristone) (Carboprost)
*Methotrexate + Misoprostol
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