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D&T3 Exam 1 > Estrogens, Progestestins, And Spermicides-santanam > Flashcards

Estrogens, Progestestins, And Spermicides-santanam Flashcards

1
Q

Estrogen

Premenopausal

A

Made by granulosa cells of ovary

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2
Q

Estrogen

During pregnancy

A

It is the fetoplacental unit

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3
Q

Estrogen

Men and postmenopausal women

A

Synthesis in adipose and hepatic tissue

Androstenedione and testosterone converted to estrone

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4
Q

Most potent endogenous estrogen

A

17 beta-estradiol

Estriol weakest

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5
Q

Estrogen

Synthesis and metabolism

Made from

A

All gonadal hormones synthesized from cholesterol

Steroidal estrogens arise from androstenedione or testosterone by aromatization

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6
Q

Estrogen

Synthesis and metabolism

Placenta

A

Uses fetal dehydroepiandrosterone (DHEA) to make lots of estrone and estriol

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7
Q

Estrogens

Excretion

A

All 3 excreted in urine

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8
Q

Progesterone

Synthesis

A

Ovary (corpus luteum), placenta, adrenal cortex and Testis

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9
Q

Physiological actions of estrogen on sex organs

Ovaries

A

Stimulate follicular growth, large doses cause atrophy

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10
Q

Physiological actions of estrogen on sex organs

Uterus

A

Endometrial growth

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11
Q

Physiological actions of estrogen on sex organs

Vagina

A

Cornification of epithelial cells with thickening and stratification of epithelium

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12
Q

Physiological actions of estrogen on sex organs

Cervix

A

Inc of cervical mucous with a lowered viscosity (favoring sperm access)

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13
Q

Physiological actions of estrogen on sex organs

Other

A

Development and maintenance of internal and external genitalia

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14
Q

Physiological actions of estrogen on sex organs

Skin

A

Inc vascularization, development of soft, textured and smooth skin

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15
Q

Physiological actions of estrogen on sex organs

Bone

A

Inc osteoblastic activity

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16
Q

Physiological actions of estrogen on sex organs

Kidney

A

Retention of na, cl, and water

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17
Q

Physiological actions of estrogen on sex organs

Cholesterol

A

Hypocholesterolemic effect

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18
Q

Progesterone

Physiological action

A

Important intermediate in steroid biogenesis

Development of secretory endometrium

Endocervical glandular fluid: inc viscosity and dec amount

Abrupt decline of progesterone initiates menstruation

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19
Q

Menstrual cycle

Follicular phase

Release

A

Gonadotropin-releasing hormone (GnRH) released into hypothalamic-pituitary portal vasculature in intervals

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20
Q

Menstrual cycle

Follicular phase

GnRH stimulates

A

Pulsation secretion of gonadotropins- FSH and LH from pituitary

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21
Q

Menstrual cycle

Follicular phase

LH and FSH function

A

Regulate the growth and maturation of the Graafian follicle in the ovary

And

Ovarian production of estradiol and progesterone

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22
Q

Menstrual cycle

Follicular phase

Estradiol effects

A

Effects on pituitary are inhibitory and this time

Cause amount of LH and FSH released from pituitary to decline (dec in LH pulse amplitude)

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23
Q

Menstrual cycle

Mid cycle surge

A

Serum estradiol rises above threshold for about 36 hrs.

Exerts brief positive feedback effect on pituitary to trigger preovulatory surge of LH and FSH

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24
Q

Menstrual cycle

Mid cycle surge

Surge in gonadotropins stimulates

A

Follicular rupture and ovulation within 1 to 2 days

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25
Q

Menstrual cycle

Luteal phase

A

Ruptured follicle develops into corpus luteum

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26
Q

Menstrual cycle

Luteal phase

Corpus luteum

A

Produces large amounts of progesterone and less estradiol (due to LH influence during 2nd half of cycle)

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27
Q

Menstrual cycle

Luteal phase

Progesterone

A

Controls the frequency and amplitude of LH

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28
Q

Menstrual cycle

Luteal phase

Effect on endometrium

A

Elevated progesterone limits the proliferative effect of estradiol on endometrium by stimulating differentiation

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29
Q

Menstrual cycle

Luteal phase

If no implantation

A

Dec in progesterone and estradiol

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30
Q

Menstrual cycle

Luteal phase

Drop in progesterone levels

A

Signals onset of menses

Pulse generator resets and new ovarian cycle occurs

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31
Q

Menstrual cycle

Luteal phase

If implantation occurs

A

Embryo secretes hCG which maintains elevated estradiol and progesterone

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32
Q

Therapeutic use of estrogens and progestins

A

Contraception (E&P)

Postmenopausal Hormone therapy (E&P)

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33
Q

Oral contraceptives

MC hormonal contraceptives

A

Combined estrogen and progesterone

34
Q

Oral contraceptives

Monophasic

A

Constant amount of estrogen and progesterone for 21 days

35
Q

Oral contraceptives

Biphasic or triphasic

A

Lower levels of hormones reduce ADR

Bi: 2 levels of progesterone, constant estrogen

Tri: 3 levels of progesterone and estradiol

36
Q

Mircette

A

EE for 21 days, 2 days placebo then 5 days low EE

Fewer estrogen withdrawal headaches

37
Q

YAZ

A

24 days (EE and drospirenone), 4 days placebo

Improve premenstrual dysphoric disorder (PMDD)

38
Q

Seasonale

A

Levonorgestral-EE

Take for 84 days, 7 days placebo

Reduces menstrual bleeding to once every 13 wks

39
Q

Lybrel

A

EE and levonorgestrel

365 days without placebo

40
Q

Patch

Xulane

A

EE and norelgestromin

Once weekly for 3 weeks with 1 week free

Rash at patch site

41
Q

Vaginal ring

A

EE and etonogestrel daily

Inserted for 3 wks with 1 wk break

42
Q

Estrogen component

A

Mestranol and Ethynyl estradiol

(80 ug mestranol same as 50 ug EE)

Mestranol metabolized to EE to be active

43
Q

Progestin component

A 
Norethindrone
Levonorgestrel
Norgestimate
Norelgestromin (metabolite of norgestimate)
Desogestrel
Ethynodiol diacetate
Gestodene
Norgestrel 
Drospirenone (YAZ)
44
Q

Progestin component

Drospirenone

A

Antiandrogen activity and antimineralocorticoid (unique)

3 mg drospirenone comparable to 25 mg spironolactone

Must monitor K

Beneficial for acne

45
Q

Androgenic activity

Side effects

A

Acne and hirsutism

46
Q

Progestin component

Androgenic activity

Highest androgenic activity

A

Norgestrel and levonorgestrel

47
Q

Mechanism of action for combination pills

A

Inhibit ovulation through a negative feedback on hypothalamus prevents mid cycle surge of FSH and LH

Thicken cervical mucus

Endometrium unsuitable for nidation

48
Q

Dosing and effectiveness

A

Req for 7 days to become effective for tricyclics (ortho tri-cycles) and 21 days for monophasics (ortho cyclen)

49
Q

Adverse effects

General

A

Migraines, depression

Nausea, ha, weight gain

50
Q

Adverse effects

Metabolic

A

Dec HDL

Inc gall stones

51
Q

Adverse effects

CV

A

Inc coagulation factors, platelet aggregation

Inc hypertension and thromboembolism

52
Q

Contraindications

A

Pregnancy
Thrombophlebitis or thromboembolic disease
Breast or estrogen dependent carcinoma (current)

Cerebrovascular or coronary artery disease
Liver disease
Cholestatic jaundice during pregnancy
Estrogen ass benign or malignant hepatic tumors
Diabetes with vascular disease
Cigarette smoker (>15/day >35y/o)

53
Q

Risks

A

Venous thromboembolism

MI (w EE)

Stroke (EE)

Gall bladder disease

Breast cancer

54
Q

Non-contraceptive benefits

A

Inc bone mineral density

Dec acne

55
Q

Adjustment of oral contraceptive dose

ADR due to estrogen xs (lower E2)

A

Nausea, bloating
Ha
Hypermenorrhea

56
Q

Adjustment of oral contraceptive dose

ADR due to Too little estrogen (inc E2 dose)

A

Early spotting and bleeding (days 1-14)

57
Q

Adjustment of oral contraceptive dose

ADR due to progestin xs (dec P dose)

A

Depression, fatigue

Hirsutism

58
Q

Adjustment of oral contraceptive dose

ADR due to too little progestin

A

Late-cycle bleeding (days 15-21)

59
Q

Adjustment of oral contraceptive dose

ADR due to xs adrogenic activity (switch to P with less adrogenic activity)

A

Noncyclic weight gain

Acne

60
Q

Special considerations

Missed pills

A

1 pill: take pill (2 in a day)

2 pills (take extra pill for 2 days) in first 2 weeks

2 pills in week 3 or 3 pills, stop current cycle of pills start new cycles

61
Q

Special considerations

Cigarette smoking and some drugs

A

Inc OC’s clearance

Inc risk of therapeutic failure

62
Q

Special considerations

Things that inc risk of therapeutic failure

A

Cigarette smoking

Some drugs

Antibiotics

Use other method with tetracyclin, penicillin, erythromycin, ampicillin (dec GI flora)

63
Q

Progesterone only minipills

Mechanism

A

Dec frequency of GnRH and LH release

Dec volume and inc viscosity for cervical fluid

64
Q

Progesterone only minipills

Special considerations

A

Used primarily in women who cannot take estrogen

CV disease

Migraines

65
Q

Progesterone only minipills

Agents

A

Norethindrone

Norgestrel

66
Q

Depot preparations

Medroxyprogesterone acetate (DMPA)

MOA

A

Inhibits ovulation, suppresses midcycle LH surge

Thicken cervical mucus

Atrophy of endometrium

67
Q

Depot preparations

Medroxyprogesterone acetate (DMPA)

ADR

A

Delay in fertility (1 yr)

Weight gain, insomnia

Risk of loss of bone mineral density

68
Q

Depot preparations

Nexplanon

A

Progestin based single rod formulated for 3 years continuous use

Etonogestrel

69
Q

Depot preparations

Progesterone containing IUD

A

Dec gradually over 5 years. Effective for 5 yrs.

70
Q

Depot preparations

Paragard T380A

A

Copper containing IUD. 10 yrs

71
Q

Depot preparations

Skyla

A

T shaped polyethylene with levonorgestrel.

Smallest IUD

3 yrs

72
Q

Depot preparations

Liletta

A

3 yrs

Levonorgestrel

73
Q

Emergency contraceptive

A

Drugs used for prevention of pregnancy following unprotected intercourse or known contraceptive failure

74
Q

Emergency contraceptive

Plan B

A

Levonorgestrel

75
Q

Emergency contraceptive

Plan B one Step OTC

A

Single tablet taken once

ADR: HA, abdominal pain

Efficacy dec with inc BMI

76
Q

Emergency contraceptive

Copper IUD

A

Up to 5 days after intercourse

Most effective

77
Q

Emergency contraceptive

Antiprogestin

A

Selective progesterone receptor modulator

Prescription

5 days after

78
Q

Vaginal spermicides

A

Active ingredient is octoxynol-9 or nonoxynol-9

Permeabilizes the cell wall of sperm

79
Q

Menopausal replacement therapy

Goal

A

Delay and/or prevent osteoporosis

Reduce risk of cv disease

Reduce vasomotor disturbances

80
Q

Menopausal replacement therapy

Drug regimen

A

Estrogen combined with progesterone

Unopposed estrogen ass with inc risk of endometrial cancer

81
Q

Menopausal replacement therapy

Bazedoxifene

A

Selective estrogen receptor modulator

Antiestrogen on uterus

Estrogen agonist on bone

82
Q

Menopausal replacement therapy

Conjugated estrogens/selective estrogen receptor modulator

A

Tx of mod to severe vasomotor sx

D&T3 Exam 1 (19 decks)

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