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

Estrogens, Progestestins, And Spermicides-santanam Flashcards

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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
Menstrual cycle Luteal phase
Ruptured follicle develops into corpus luteum
26
Menstrual cycle Luteal phase Corpus luteum
Produces large amounts of progesterone and less estradiol (due to LH influence during 2nd half of cycle)
27
Menstrual cycle Luteal phase Progesterone
Controls the frequency and amplitude of LH
28
Menstrual cycle Luteal phase Effect on endometrium
Elevated progesterone limits the proliferative effect of estradiol on endometrium by stimulating differentiation
29
Menstrual cycle Luteal phase If no implantation
Dec in progesterone and estradiol
30
Menstrual cycle Luteal phase Drop in progesterone levels
Signals onset of menses Pulse generator resets and new ovarian cycle occurs
31
Menstrual cycle Luteal phase If implantation occurs
Embryo secretes hCG which maintains elevated estradiol and progesterone
32
Therapeutic use of estrogens and progestins
Contraception (E&P) Postmenopausal Hormone therapy (E&P)
33
Oral contraceptives MC hormonal contraceptives
Combined estrogen and progesterone
34
Oral contraceptives Monophasic
Constant amount of estrogen and progesterone for 21 days
35
Oral contraceptives Biphasic or triphasic
Lower levels of hormones reduce ADR Bi: 2 levels of progesterone, constant estrogen Tri: 3 levels of progesterone and estradiol
36
Mircette
EE for 21 days, 2 days placebo then 5 days low EE Fewer estrogen withdrawal headaches
37
YAZ
24 days (EE and drospirenone), 4 days placebo Improve premenstrual dysphoric disorder (PMDD)
38
Seasonale
Levonorgestral-EE Take for 84 days, 7 days placebo Reduces menstrual bleeding to once every 13 wks
39
Lybrel
EE and levonorgestrel 365 days without placebo
40
Patch Xulane
EE and norelgestromin Once weekly for 3 weeks with 1 week free Rash at patch site
41
Vaginal ring
EE and etonogestrel daily Inserted for 3 wks with 1 wk break
42
Estrogen component
Mestranol and Ethynyl estradiol (80 ug mestranol same as 50 ug EE) Mestranol metabolized to EE to be active
43
Progestin component
``` Norethindrone Levonorgestrel Norgestimate Norelgestromin (metabolite of norgestimate) Desogestrel Ethynodiol diacetate Gestodene Norgestrel Drospirenone (YAZ) ```
44
Progestin component Drospirenone
Antiandrogen activity and antimineralocorticoid (unique) 3 mg drospirenone comparable to 25 mg spironolactone Must monitor K Beneficial for acne
45
Androgenic activity Side effects
Acne and hirsutism
46
Progestin component Androgenic activity Highest androgenic activity
Norgestrel and levonorgestrel
47
Mechanism of action for combination pills
Inhibit ovulation through a negative feedback on hypothalamus prevents mid cycle surge of FSH and LH Thicken cervical mucus Endometrium unsuitable for nidation
48
Dosing and effectiveness
Req for 7 days to become effective for tricyclics (ortho tri-cycles) and 21 days for monophasics (ortho cyclen)
49
Adverse effects General
Migraines, depression Nausea, ha, weight gain
50
Adverse effects Metabolic
Dec HDL Inc gall stones
51
Adverse effects CV
Inc coagulation factors, platelet aggregation Inc hypertension and thromboembolism
52
Contraindications
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
Risks
Venous thromboembolism MI (w EE) Stroke (EE) Gall bladder disease Breast cancer
54
Non-contraceptive benefits
Inc bone mineral density Dec acne
55
Adjustment of oral contraceptive dose ADR due to estrogen xs (lower E2)
Nausea, bloating Ha Hypermenorrhea
56
Adjustment of oral contraceptive dose ADR due to Too little estrogen (inc E2 dose)
Early spotting and bleeding (days 1-14)
57
Adjustment of oral contraceptive dose ADR due to progestin xs (dec P dose)
Depression, fatigue | Hirsutism
58
Adjustment of oral contraceptive dose ADR due to too little progestin
Late-cycle bleeding (days 15-21)
59
Adjustment of oral contraceptive dose ADR due to xs adrogenic activity (switch to P with less adrogenic activity)
Noncyclic weight gain Acne
60
Special considerations Missed pills
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
Special considerations Cigarette smoking and some drugs
Inc OC's clearance Inc risk of therapeutic failure
62
Special considerations Things that inc risk of therapeutic failure
Cigarette smoking Some drugs Antibiotics Use other method with tetracyclin, penicillin, erythromycin, ampicillin (dec GI flora)
63
Progesterone only minipills Mechanism
Dec frequency of GnRH and LH release Dec volume and inc viscosity for cervical fluid
64
Progesterone only minipills Special considerations
Used primarily in women who cannot take estrogen CV disease Migraines
65
Progesterone only minipills Agents
Norethindrone Norgestrel
66
Depot preparations Medroxyprogesterone acetate (DMPA) MOA
Inhibits ovulation, suppresses midcycle LH surge Thicken cervical mucus Atrophy of endometrium
67
Depot preparations Medroxyprogesterone acetate (DMPA) ADR
Delay in fertility (1 yr) Weight gain, insomnia Risk of loss of bone mineral density
68
Depot preparations Nexplanon
Progestin based single rod formulated for 3 years continuous use Etonogestrel
69
Depot preparations Progesterone containing IUD
Dec gradually over 5 years. Effective for 5 yrs.
70
Depot preparations Paragard T380A
Copper containing IUD. 10 yrs
71
Depot preparations Skyla
T shaped polyethylene with levonorgestrel. Smallest IUD 3 yrs
72
Depot preparations Liletta
3 yrs Levonorgestrel
73
Emergency contraceptive
Drugs used for prevention of pregnancy following unprotected intercourse or known contraceptive failure
74
Emergency contraceptive Plan B
Levonorgestrel
75
Emergency contraceptive Plan B one Step OTC
Single tablet taken once ADR: HA, abdominal pain Efficacy dec with inc BMI
76
Emergency contraceptive Copper IUD
Up to 5 days after intercourse Most effective
77
Emergency contraceptive Antiprogestin
Selective progesterone receptor modulator Prescription 5 days after
78
Vaginal spermicides
Active ingredient is octoxynol-9 or nonoxynol-9 Permeabilizes the cell wall of sperm
79
Menopausal replacement therapy Goal
Delay and/or prevent osteoporosis Reduce risk of cv disease Reduce vasomotor disturbances
80
Menopausal replacement therapy Drug regimen
Estrogen combined with progesterone Unopposed estrogen ass with inc risk of endometrial cancer
81
Menopausal replacement therapy Bazedoxifene
Selective estrogen receptor modulator Antiestrogen on uterus Estrogen agonist on bone
82
Menopausal replacement therapy Conjugated estrogens/selective estrogen receptor modulator
Tx of mod to severe vasomotor sx

D&T3 Exam 1 (19 decks)

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