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Flashcards in Pharm 37 Objectives Deck (44)
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1

What is the rationale for the replacement use of estrogen and estrogen/progestin in postmenopausal osteoporosis and for menopausal symptoms?

-prevention of accelerated bone loss after menopause who cannot take non-estrogen medications
-relief of menopausal symptoms: hot flashes, depression, insomnia, symptoms of vulvar, vaginal, and urethral atrophy
-take the lowest dose for the shortest duration needed

2

What are the effects of estrogens on clotting factors?

enhance blood coagulation by increasing synths of coagulation factors

3

What are the effects of estrogen on cholesterol tests?

decrease LDL while increasing HDL

4

What are the effects of estrogen on thyroid hormone disposition?

high levels of exogenous estrogen increase thyroxine binding globulin
-cause hypothyroidism in those taking thyroid replacement

5

What are the effects of estrogen on FSH and LH?

high levels suppress FSH and LH in menstrual cycle

6

What are the types of estrogens used therapeutically?

-ethinyl estradiol
-estradiol valerate
-mestranol

7

What is the therapeutic action of estrogen?

suppress ovulation

8

What is the therapeutic action of progestin?

create a hostile environment

9

What are the adverse effects of estrogen?

nausea, breast tenderness, hypertension, melisma, headache

10

What are the adverse effects of progestin?

breast tenderness, headache, fatigue, mood changes

11

What are the contradictions of estrogen?

-DVT, PE or history of
-Stroke or history of
-Breast cancer or history of
-Coagulopathy
-Pregnancy
-Breastfeeding <21 days
-Age >35 + >15 cigarettes/day
-Ischemic heart disease/cardiomyopathy
-Severe hypertension
-Major surgery with prolonged immobilization
-Migraine with aura
-Liver cancer or severe cirrhosis

12

What are the potential mechanism of action of combined oral contraceptives?

-Feedback inhabitation of -GnRH section from the hypothalamus leading to decreased gonadotropic secretion and inhabitation of ovulation
-Reduce FSH secretion and maturation of follicle (estrogen component)
-Inhibit the midcycle LH surge required for ovulation (progestin component)

13

What are the most common drug interactions with combined oral contraceptives?

-antibiotics: cause N/V/D and forgetfulness during illness
-penicillins and tetracylines
-rifampin and griseofulvin

14

What is the rational for the various dosage schedules?

-personal preference
-cost

15

What estrogen is most commonly found in combined oral contraceptives?

ethinyl estradiol

16

What is the starting dose of EE?

start low at 20 mcg and titrate up to 30 to 35 mcg

17

When do you increase estrogen dose?

if there is early or mid-cycle spotting/BTB, vasomotor symptoms, atrophic vaginitis

18

When do you decrease the estrogen dose?

if there is nausea, breast tenderness, hypertension, melisma, headache

19

What is a low estrogen dose?

10 mcg

20

What are the most common progestins used in contraception?

-progesterone
-testosterone/notestosterone
-spironolactone

21

Rank each by relative androgenic potencies (most to least androgenic)

evonorgestrel/norgestrel > norethindrone > desogestrel/norgestimate > dosperinone/dienogest (anti-adrogenic)

22

List the other type of hormonal contraceptive agents other than COCs

-progestin-only
-patch (Xulane or Evra)
-vaginal ring (NuvaRing or Annovera)
-implant (nexplanon)

23

Limitations/CI of Xulane, Evra - Patch

higher incidence of thrombosis d/t higher estrogen level
- less effective in pts over 198 Ibs (90 kg)

24

Limitations/CI of NuvaRing, Annovera - Vaginal Ring

Nuva: no need for back up methods if out for less than 48 hours
Anno: if out for >2 hours need 7 days of back up method and unknown effectiveness in pts BMI >29

25

Limitations/CI of Nexplanon - Implant

-liver disease or liver tumor
-unexplained vaginal bleeding
-breast cancer

26

What is progestin-only contraception place in therapy?

-Premenstrual dysphoric disorder (PMDD)-Yaz
-Contraception
-Dysmenorrhea
-Endometriosis
-Post-coital contraception

27

What are the advantages of progestin-only contraception?

-Less interface w/breast feeding
-Less risk of thrombosis
-No estrogenic SEs

28

What are the disadvantages of progestin-only contraception?

-Must be taken at the same time every day, within 3 hrs
-Taken every day, not cyclically: NO placebo pills
-Less effective contraceptive

29

What is the MOA of Levonorgestrel (Plan-B One-Step)?

a progestin that prevents ovulation and fertilization by altering tubal transport of sperm and/or ova

30

What is the MOA of Ulipristal -selective progesterone receptor modulator

not completely known
-block rise in LH, represses progesterone, blocks ovulation
-interacts with hormonal contraceptives: wait 5 days before restarting