Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Therapeutics > Lecture 14: Progestins > Flashcards

Lecture 14: Progestins Flashcards

1
Q

Progesterone

A

-most important progestin
-functions as hormone and precursor to estrogens, androgens, corticosteroids
-bind progesterone receptor
-alter rate of transcription

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Progesterone synthesis

A

-ovary, testis, adrenal glands
-corpus luteum in luteal phase
-placenta during pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Progesterone metabolism

A

-rapidly absorbed
-5 min half life
-almost completely first-passed metabolized
-converted to pregnanediol
-conjugated with glucaronic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Progesterone excretion

A

-urine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Physiological effects of progesterone

A

-menstruation cycle
-metabolic effects
-interference with aldosterone
-deppressant/hypnotic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

progesterone effect on menstrual cycle

A

-cause maturation and secretory changes in endometrium after ovulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

progesterone effect on metabolism

A

-inc insulin and insulin response to glucose
-promote glycogen storage in liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

progesterone interference with aldosterone

A

-compete for mineralcorticoid receptor
-dec Na+ reabsorption
=inc aldosterone secretion by adrenal cortex in pregnancy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Clinical uses of progesteron

A

-contraception
-hormonal replacement therapy
-endometriosis
-dysmenorrhea
-bleeding disorders

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Progesterone effect in hormone replacement therapy

A

-reduce adverse effects of estrogen
-uterine bleeding and carcinoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Progestin effect on endometriosis

A

-suppress growth of endometrial cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

endometriosis

A

-growth of endometrial cells outside uterine cavity
-cells respond to hormonal changes
=cause pain from inflammation during period

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Progestin structure requirements

A

-ketone at C-3
-C-18 Me group
-C-19 Me, H, or double bond
-C-17a and B

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

19-nor, 17-ethynyl steroids

A

-1st gen progestins
-oral contraceptives
-norethindrone
-ethynodiol diacetate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

17-ethynyl group

A

-triple bond
-inc oral availability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

19-methyl group

A

-not necessary for activity
-replace with H enhances activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

17-acetyl

A

-replace with OH to inc oral bioavailability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Levonorgestrel

A

-2nd gen progestin
-levo isomer
-active form
-high oral bioavailability
-iud and mirena

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Norgestimate

A

-prodrug
-converted to levonorgestrel oxime then to levonorgestrel

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

2nd gen progestins

A

-levonorgesterel (active)
-norgestimate (prodrug)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

3rd gen progestins

A

-desogestrel (prodrug)
-etonogestrel (active)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Desogestrel

A

-3rd gen
-prodrug
-metabolized to etonogestrel
-high oral bioavailability

23
Q

Etonogestrel

A

-active
-analog to levonorgestrel
-used in nexplanon implant or nuvaring

24
Q

Drospirenone

A

-4th gen
-weak activity (10% of levo)
-antimineralocorticoid activity
-negate side effects of estradiol in combination therapy

25
Q

Medroxyprogesterone acetate

A

-1st gen
-used for depot injection

26
Q

Optimal hormonal activities of progestins

A

-minimize androgenic and antiestrogenic effects

27
Q

Types of hormonal contraceptive

A

-combinations of estrogens and progestins (phasic)
-progestin w/o estrogen

28
Q

Hormonal contraceptive routes of admin

A

-mostly oral
-implantable, injection

29
Q

adherence to bc schedule more critical for

A

progestin-only therapies

30
Q

Effects of oral bc on ovulation

A

-selectively inhibited by combo estrogen and progestins (inhibit pituitary)
-not always inhibited by progestin-only

31
Q

effects of oral bc on ovary

A

-suppress function
-return to normal cycle in 1-2 months after discontinued use

32
Q

effect of oral bc on uterus

A

-change in mucus and endometrium
-dec chance of conception and implantation

33
Q

Effect of oral bc on breasts (combo only)

A

-stimulation of breasts
-enlargement
-suppress lactation

34
Q

estrogen and progestin combo therapy

A

-ethinyl estradiol + norethindrone (usually)

35
Q

mild adverse effects of oral bc

A

-nausea, HTN, edema, breast fullness due to estrogens
-appetite, datigue, breast regression due to progestins

36
Q

Moderate adverse effects of oral bc

A

-irregularities in menstruation (~progestin-only)
-weight gain, acne, hirsutism (~combos w/ androgen-like progestins)
-ammenorrhea

37
Q

severe adverse effects of oral bc

A

-venous thromboembolic disease (estrogens)
-MI (androgenic progestins)
-not for women over 35 who smoke

38
Q

Interactions with other steroids

A

-may inc blood levels of other steroids by interfering with their metabolism

39
Q

interactions with anticonvulsants

A

-phenytoin
-induces drug-metabolizing enzymes in liver

40
Q

Interactions with rifampin (antibiotic)

A

-induce drug metabolizing enzymes in liver
-inc rate of metabolism of many drugs

41
Q

interactions with tetracyclines (antibiotic)

A

-suppress gut flora that participate in enterohepatic recycling

42
Q

emergency contraceptives

A

-99% effective within 72 hours
-higher doses than bc

43
Q

types of emergency contraceptives

A

-combo (ethinyl estradiol + norgestrel)
-progestin only (planB (levonorgestrel)

44
Q
A
45
Q

side effects of emergncy contraceptive

A

-nausea and vomiting (~combo)

46
Q

Ulipristal acetate

A

-SPRM
-emergency contraceptive
-upto 5 days after sex

47
Q

Ulipristal acete side effects

A

-nausea
-abdominal pain

48
Q

SPRM

A

selective progesterone receptor modulator

49
Q

Mifepristone

A

-RU-486
-progesterone ANTAgonist
-abortifacient up to 70 days (combo with misopristol)

50
Q

Mifepristone side effects

A

-nausea, vomitting
-bleeding (5%)

-requires intervention/admin by physician

51
Q

Danazol

A

-weak adrogen, weak progestin, antiestrogen
-effective for endometriosis
-inhibit LH and FSH surge
-suppress ovarian function
-atrophy of endometrium

52
Q

Adverse effects of Danazol

A

-mostly from weak androgenic activity
-weight gain
-little bitties
-acne, oily skin, hirsutism

53
Q

Danazol contraindications

A

-hepatic dysfunction
-pregnancy and breast feeding

Therapeutics (78 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions