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DT4-Exam 1 > Pharm-OCP/MRT- Melissa *** > Flashcards

Pharm-OCP/MRT- Melissa *** Flashcards

1
Q

List the three estrogens in order of most to least potent:

A

17-B Estradiol –> Estrone–> Estriol

*estrione tri’s to be a good estrogen, but it just cant.

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2
Q

Where are the different types of estrogen formed in the body?
(Premenopausal women/ preggos/ men and post menopausal women…)

A

Premenopausal Women:
-Ovary, estradiol mainly

Pregnancy:
Placenta: Estrone, Estriol

Men and Postmenopausal women:

  • Liver
  • Adipose tissue
  • Primarily Estrone
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3
Q

Describe the synthesis of 17-B Estradiol.

By which enzyme is the reaction catalyzed?

A

Cholesterol is the basis for ALL steroid hormones…

Androstenedione –>Testosterone–> 17B-Estradiol
*requires aromatase

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4
Q

Describe how the placenta forms Estrone and Estriol:

A

DHEA–> Estrone + Estriol

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5
Q

How are all three estrogens excreted?

A

Renal excretion as estrogens or glucuronide/ sulfate conjugates

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6
Q

Describe the effect of estrogens on female sexual organs (4):

  • follicles?
  • endomertrium?
  • vaginal epi?
  • cervical mucous?
A
  • ^ follicular growth (ovarian atrophy in large doses)
  • ^ endometrial growth
  • cornify, thicken, stratify vaginal epi
  • decrease viscosity and ^ amount of cervical mucous
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7
Q

Describe 5 roles of estrogen outside the female reproductive system:

  • skin
  • bone
  • blood
  • cholesterol
A
  • ^ vascularization, softness, and suppleness of skin
  • ^ osteoblastic activity
  • ^ renal retention of Na, Cl, H2O (bloating)
  • maintain HDL/LDL balance = low CVD risk
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8
Q

What are the three physiological effects of estrogen on men?

A
  • manage bone density
  • spermatogenesis
  • behavior
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9
Q

What stimulates the production of progesterone in females?

Where is it produced?

A
  • LH –> corpus luteum production in 2nd half cycle
  • HCG –> corpus luteum production in early pregnany
  • HCG –> placenta + fetal adrenal gland production of P/E in late pregnancy

Also produced in adrenal cortex and testis (important intermediate in steroid synthesis)

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10
Q

How is progesterone important in promoting pregnancy (2)?
What is the role of progesterone in endometrial cycle?
How does it affect cervical mucous?

A

-*Progesterone promotes IMPLANTATION/ Maintain pregnancy
by:
- ^ development of secretory endometrium
- Decrease amount and ^ viscosity of cervical mucous

(opposite of estrogen in terms of effects on endometrium/ cervical mucous)

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11
Q

Events of menstrual cycle follicular phase: (3)

A
  • Pulsatile: GnRH–> LH + FSH
  • follicle growth, granulosa cells secrete estrogen
  • Estrogen–> (-) feedback on hypothal.-> keeps FSH + LH in check.
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12
Q

Events of mid menstrual cycle surge:

What is required to maintain surge?

A

-^ Estradiol for 36hrs –> (+) Feedback on Hypothalamus–>
^ GnRH–> LH SURGE–> Follicle rupture + ovulation
-*Progesterone required to maintain LH surge

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13
Q

Events of menstrual cycle: luteal phase
What happens if implantation occurs?
No implantation?

A

Ruptured follicle–> Corpus luteum–> P + E released

  • No implantation–> DECREASE P + E–> menstruation
  • Implantation–> Embryo–> HCG–> P + E stay high
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14
Q

What type of synthetic estrogen is used in combination oral contraceptives (COCs)?
How common are these drugs and what is one issue with their use?

A
  • Ethinyl estradiol
  • # 1 contraceptive in US
  • Strict oral dosing regimin= poor compliance
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15
Q

What type of synthetic estrogen is used in post-menopausal hormone replacement therapy (MHT)?
How does the dosing compare to that in COCs?

A

conjugated estrogens–dosing is much LOWER than that in COCs

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16
Q

Monophasic COCs:
Dosing regimin?
What dose EE is considered low dose?

A
  • 21 days active hormone + 7 days placebo (Fe or nothing)
  • Take same amount EE + prog. for 21 days
  • Must be less than 35 ug EE to be considered low dose
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17
Q

Multiphasic COCs:
How do these work?
Why are they good?
What are the two types?

A

Hormone dose increases for 21 days (prevent ADRs)

Biphasic- prog varies.
-2 doses progesterone + constant E

Triphasic- either prog or EE vary

  • 3 doses progesterone + constant E
  • 3 doses E + constant progesterone
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18
Q

Extended COCs:
How do they work?
How long is the cycle always?

A

Dosing regimen alters # of pill free days –>
Decrease hypoestrogenism–> Fewer menstrual sx.

*Cycle always 28 days, so 2 placebo days = 26 days hormone, 4 placebo days = 24 days hormone. Don’t memorize # of hormone days!!!!! Just know placebo and count.

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19
Q

Mircette: class + dosing regimen

A

Extended COC:

20 ug EE + desogestrel–>2 days placebo–>5 days 10ugEE

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20
Q

Yaz:
Dosing regimen
In addition to contraception, what was its clinical use? (2)
Salient ADR?

A

Extended COC:

  • EE + Drospiredone–> 4 placebo pills/ cycle
  • TREATS PMDD, reduces bloating (diuretic)
  • Worry about HYPERKALEMIA (dros= spiro derivative)
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21
Q

Yasmin: class + dosing regimen
How does it differ from Yaz?
Salient ADR?

A

Extended COC:

  • EE + Drospiredone–> 4 days placebo pills
  • Uses 10+ ug (30ug total) E to decrease w/drawal sx
  • Worry about HYPERKALEMIA
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22
Q

Drospirenone: What is it? Why is it important?

A
  • Derivative of spironolactone
  • Anti-mineralicorticoid activity (Hyperkalemia!)
  • Anti-androgen activity (prevent Progesterone ADRs like bloating)
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23
Q

Seasonale: class + dosing regimen

A

Extended COC:
Levonogestral + EE for 84 days–> 7 days placebo
*Bleed every 13 wks (3mos)

*Seasonal periods

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24
Q

Seasonique: class + dosing regimen

Advantages to this drug over seasonale?

A

Extended COC:
(Seasonale) but 10ug EE for 10 days instead of the 7 day placebo every three months

*Better follicular suppression + less breakthrough bleeding

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25
Lybrel: class + dosing regimen
Extended COC: Levonogestral + EE for 365 days! No bleeding! *Not a coincidence that drug name is a play on the word "liberation"!
26
``` *Patch (Xulane): Dosing regimin? ADRs (2)? Advantages? In which population may Xulane not be as effective? ```
EE (more) + Norelgestromin (less) for 3 weeks--> 1 wk off - ADRs: ^ risk rash + thrombosis - Avoids hepatic first pass elimination - May not be as effective in obese patients
27
*Vaginal Nuvaring: Dosing regimin? Advantages? Disadvantages?
EE (more) + Etonogestrel (less) for 3 weeks--> 1 week off - Avoids hepatic first pass elimination - Better than patch for obese patients - Uterine first pass elimination instead!
28
What are the two synthetic estrogens? How are they used?
- Mestranol: metabolized to *active* Ethinyl Estradiol (80ug M--> 50ug EE) - Ethinyl Estradiol: used in 2nd gen low dose COCs (more potent, more frequently used)
29
What are the 4 synthetic progesterone types?
- Pregnanes - Estranes - Gonanes - Drospirenone *These are altered in COCs while EE remains constant
30
Pregnanes: how are they used?
Injectable contraceptives
31
Estranes: how are they used?
- Similar to 19-Norestosterone - hepatic metabolism - activity similar to E - used in COCs; shorter t 1/2
32
Gonanes: how are they used?
- Similar to 19-Norestosterone but w ethyl vs. methyl group - Used in COCs - ^^^ t1/2 + bioavailability compared to estranes
33
Which progesterones have the MOST progestational and androgenic activity?
Levonorgestrel + Norgestrel | Norgestrel is in the name levonorgestrel!
34
Which progesterones have the LOWEST progestational and androgenic activity? What population are these hormones good for?
Desogestrel + Norgestimate Gestrodene + Drosperinone *Good for patients with acne and PCOS (just remember the progs are generally weak except levo*norgestrel* and norgestrel)
35
Which progesterone has anti-androgen + anti-mineralocorticoid activity and can be used to reduce acne and weight gain?
Drosperinone-- don't forget hyperkalemia risk!
36
What is the MOA for COCs? How do the estrogen and progesterone influence ovulation? (3) What are two effects of progesterone on the cervix and uterus that prevent pregnancy?
- Negaitve FB on hypothalamus--> no LH/FSH surge - Estrogen--> Inhibit FSH - Progesterone--> Inhibit LH, also GnRH Additional Progesterone Effects (prevail over estrogen) Thicken cervical mucous--> Inhibit sperm entry Endometrial atrophy--> Prevent implantation
37
What are 3 factors leading to decreased contraceptive efficacy?
- ADRs = non-compliance - ^ body weight - Drug interactions
38
How long does it take for monophonic and triphasic drugs to become effective? When do patients start a pack?
Pack started on 5th day of menses or first Sunday after Monophonic: 21 days Triphasic: 7 day
39
When is failure more common--at the start or end of a pack?
Failure is higher at beginning of pack and associated with varying time between doses
40
What are two things that can happen if patients inappropriately vary time between doses?
- failure | - ^ ADRs due to hormone flux
41
List 5 ADRs associated with OCPs:
- N/V/ HA (~migraine) / weight gain - ^ cholesterol sat in bile--> ^ Gall stones - ^ platelet agg + ^ clotting factor synth--> thrombosis - ^ RAAS activation--> ^ HTN - Breast cancer (controversial!!)
42
What type of OCP would be safe for breastfeeding woman to take less than 6wks postpartum?
Progestin only formulation--NO E! | mini pill
43
Contraindications to OCP use (5):
- Hepatic/ Biliary Diseases - Cardiovascular/ clotting disorders - pregnancy/ breastfeeding - estrogen dependent cancers - HTN/ Diabetes/ Cigarette smokers over 35***
44
When is the risk for venous thromboembolism on OCPs highest?
During first year of treatment
45
At what dose is the risk for MI/Stroke highest on OCPs? | Which patient population is at highest risk?
50+ug ethinyl estradiol; women with HTN at highest risk
46
What are some non-contraceptive benefits associated with OCP use?
- ^ bone mineral density | - Decreased acne + hirsutism
47
How do OCPs decrease acne and hirsutism? What condition are these drugs good to treat?
^ serum hormone binding globulins--> androgen sequestration | *Good to treat PCOS
48
What are three ways we can adjust OCPs to manage ADRs?
- Dose of E and P - Ratio of E:P - Type of P
49
Which ADRs mandate adjustment to LOWER dose of estrogen? (5)
- N/V/HA/ Migraine*** (you get sick) - CYCLIC weight gain, leg cramps, edema*** (you retain water) - HYPERmenorrhea - HTN
50
Which ADRs mandate adjustment to HIGHER dose of estrogen? (3)
- Vasomotor sx. (Hot flashes)*** - EARLY Breakthrough bleeding - HYPOmenorrhea
51
Which ADRs mandate adjustment to LOWER progesterone? | Aka what are the ADRs of progesterone?
Depression: of both your mood and your boobies. | You get sad about your small boobs. Like Leah and Stacee.
52
Which ADRs mandate adjustment to LESS ANGROGENIC progesterone?
- Acne/ oily skin | - consistent (non cyclic) weight gain
53
Which ADRs mandate adjustment to HIGHER progesterone?
- LATE breakthrough bleeding - HYPERMENORRHEA (low prog effects are similar to estrogen effects) *Switch from norgestimate--> norgestrel
54
When should you be concerned about a SINGLE missed dose and how would you manage it? When is this most likely to cause failure?
Days 1-21 (non-placebo) - Take pill as soon as discovered - Do not take more than 2 per day - Most likely to fail within first 5 days
55
How would you manage missing TWO doses? | How does this vary depending on when doses are missed?
Day 1-14: take extra pill for 2 days + additional method for 7 Day 15-21: stop pack, start new cycle + 7 days additional method
56
What is the protocol for non-nursing new mothers on OCPs? (When can they start and why?)
May begin COC 4 weeks after delivery; must wait because thrombosis risk
57
Describe the influence of smoking on OCP efficacy:
P450 INDUCERS! - Make OCPs LESS EFFECTIVE - Use supplemental method or ^ dose
58
List some P450 inducing drugs that might cause OCP failure/ decrease efficacy:
- Carbamazepine - Phenytoin - Phenobarbital - Pirimidone - Rifampin - St John's wart *Generally Think: Anticonvulsants, Antimicrobials
59
Which ABX decrease OCP efficacy? How do they do this?
Tetracyclines,Erythromycin, PEN V, Ampicillin - *DECREASE GI flora* - Less GI flora = LOWER hormone enterohepatic circulation
60
What is the primary contraceptive MOA for progesterone ONLY drugs?
- Only 70-80% inhibition of ovulation | - Mostly thicken cervical mucous and cause endometrial atrophy
61
Describe how the mini pill works; what is the active component? When do you start the pills? How long until they are effective? How often do they inhibit ovulation?
ONLY norgestrel or norethindrone (progesterone) - Begin first day of menses; same dose throughout cycle - Inhibits ovulation 80% - Requires additional method for 3 weeks
62
Indications for mini pill use: (3)
- Breast feeding - Smokers over 35yoa + other situations w/ CI estrogen - Migraines and depression
63
Disadvantages to mini pill use: (2)
Easy to FAIL!! - Low hormones = miss one dose = FAILURE! - Regimen off by 3 hours = FAILURE * Obviously use additional method if failure suspected
64
Depot Preparation: Active ingredient? Treatment regimen? MOA? (2)
``` Medroxyprogesterone acetate (pregnane) - IM injections every 3 mos ``` MOA - Stops LH surge - Induces endometrial atrophy--> delay fertility
65
ADRs to Depot prep? (3)
- weight gain - insomnia - decrease bone at 2 years +
66
*Nexplanon: | ROA, duration of use
- etonogestrel based implant | - good for 3 years
67
Merena: | ROA, duration of use
- levonogestrel IUD | - good for 5 years
68
ParaGard: | ROA, MOA, duration of use
- copper based IUD - causes inflammation and decreased sperm motility - good for 10 years
69
Skyla: | ROA, duration of use
- T shaped levonorgestrel IUD, smallest of them all | - good for 3 years
70
Liletta: | ROA, duration of use
- levonorgestrel IUD | - good for 3 years
71
Progestin based Emergency Contraceptives: Which synthetic hormone is used? What are the two preparations available and when should they be taken? What are some ADRS and limitations to use (2)?
Levonorgestrel - Plan B (2 doses 12 hours apart Levonorgestrel + EE) - Plan B one Step OTC (single dose levonorgestrel) - Should be taken within *72 hours* of unprotected intercourse - May cause HA and *abdominal cramps* - Decrease efficacy with ^ BMI
72
What is the most effective emergency contraceptive?
Copper IUD inserted within 5 days of unprotected sex
73
Ulipristal acetate/ Ella: | Drug class, MOA, therapeutic regimen
Antiprogestin ECP - Selective progestin reuptake modulator - Take within 5 days unprotected intercourse - Prescription only
74
Octoxynol-9/ Nontoxynol-9 | Drug class, MOA, ADRs
Vaginal spermicide - nonionic detergent--> ^ leakiness in sperm cell wall - additives may cause irritation or allergy
75
What are the goals of MRT? (2)
- reduce vasomotor disturbance (hot flashes) | - reduce osteoporosis
76
What is the most common hormone combo used in MRT? When is a combination MANDATED? What is the risk of using unopposed estrogen?
Estrogen + Progesterone * **Combo mandated in women WITHOUT HYSTERECTOMY * **Unopposed E = ^ risk endometrial cancer
77
MRT Drug Regimens (3):
1. 21 days estrogen + last 10 add progesterone + 1 week off 2. Estrogen + progesterone for first 10-13 days 3. Continuous E+ P
78
Which synthetic estrogens and progesterones are used for MRT?
Estrogen: conjugated estrogen Progesterone: medroxyprogesterone or norethindrone
79
Premarin/ Prempro/ Premphase: | Therapeutic use and hormone constituents
MRT, primarily conjugated estrogen
80
Duavee: What is it? Therapeutic use?
Conjugated estrogen + SERM (bazedoxifene) - SERM acts as estrogen AGONIST (osteoblast^) in bone - SERM acts as estrogen ANTAGONIST in uterus Treats hot flashes and osteoporosis in post menopausal women w/o hysterectomy!
81
What does SERM stand for?
selective estrogen receptor modulator
82
General ADRs of MRT? (2) | CIs? (3)
- ^ risk clots esp in first year - ^ risk HTN + CVD in higher doses CIs: breast cancer, estrogen dependent cancer, thrombophlebitis
83
When is unopposed estrogen mandated for MRT and why?
- Women WITH HYSTERECTOMY should get E ONLY | - P associated with alteration of HDL/LDL ratio

DT4-Exam 1 (17 decks)

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