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Pharmacology > Endocrine and Metabolic Agents > Flashcards

Endocrine and Metabolic Agents Flashcards

1
Q

3 medical applications to hormone use

A
  1. replacement of hormones that are not produced anymore
  2. pharmacological doses that will elicit a response that is not present at physiologic levels
  3. diagnostic tools
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2
Q

chemical causes uterus to contract

also calming

also excretion of breast milk

also psychological bonding

A

oxytocin

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3
Q

without this hormone incontinence is common

A

ADH

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4
Q

ovulation and spermatogeneissi hormone

A

FSH/ LH

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5
Q

which hormone makes breast milk

A

prolactin

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6
Q

what are the different classes of hormones

A

peptide hormones- receptor on surface of cell

steriod hormones- lipophilic so receptor within cell

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7
Q

what is the molecular mechanism for extracellular binding

What molecule = ex

A

exerts an internal conformation change then cascade of events

plasma membrane receptor mediated response

happens in seconds to minutes!!!

INSULIN= peptide hormones

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8
Q

what is the molecular mechanism following intracellular binding

What molecule = ex

A

binds to receptor in the nucleus causing conformational change which promotes synthesis of specific mRNA

intracellular receptor mediated response

takes hours to days !!

STERIODS hormones

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9
Q

What is GnRH and what does it cause

A

gonadotropin releasing hormone (GnRH)

stimulates the release of follicle stimulating hormone (FSH) and leutinizing hormone (LH) from the anterior pituitary

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10
Q

what is the role of FSH in men vs women

A

women= to stimulate follicular development

men= stimulate spermatogenesis

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11
Q

what does FSH convert androgens into

A

estrogen

both male and female

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12
Q

What is the role of LH in men vs women

A

in general= responsible for regulation of gonadal steriod production

men= acts on testicular leydig cells to stimulate testosterone production

women= works in conjunction with FSH to stimulate corpus luteum during menstruation to produce progesterone

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13
Q

what is the normal levels of estrogen in body

A

huge range of secretion by people is normal (70-500 mcg)

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14
Q

main actions of estrogen

A

maintain female repro system

promote growth /development of vagina/uterus/fallopian tubes

involved other hormones (esp. progesterone) in regulation of menstrual cycle

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15
Q

menopause

A

reduction of estrogen and progesterone levels as women age

physiologic changes result

  • mood
  • hot flashes
  • dryness

estrogen is still higher than progesterone

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16
Q

how does estrogen act as inhibitor and then stimulator

A
  • negative feedback at low doses for FSH and LH= inhibit them= no ovulation

increased doses of estrogen= positive feedback = large spike in LH and FSH= ovulation

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17
Q

another name for progesterone

A

progestin

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18
Q

what do we use estrogens for

A

contraceptives

hormone replacement therapy or menopause symptom control

abnormal uterine bleeding

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19
Q

for contraceptive use of estrogen what is it commonly combined with

and what are the results!!!!!!

A

combined with progestin (progesterone)

Results:

  • thicken cervical mucus
  • inhibit sperm penetration
  • lower mid-cycle FSH/LH peaks (negative feedback)
  • slows the follicule movement in fallopian tubes (estrogen)
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20
Q

where is estrogen absorbed best

A

absorbed fairly well through all routes

  • best absorption via skin

in order of
skin» mucus membranes» GI tract !!!!!!!!!!

aka transdermal patch of estrogen requires much smaller doses !!!!

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21
Q

metabolism/ excretion of estrogen

A

natural estrogens have a HIGH FIRST PASS EFFECT
- circulates as estrone sulfate

conjugated estrogens (EE) are degraded at much slower rates= lower doses needed - aka from another animal so already digested once (horse)

some estrogen excreted into bile and reabsorbed!!!!!!!!!!!!!!!!

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22
Q

what happens if give a drug that is estrogenic or blocks androgens and allows estrogen to predominate in males what happens

A

men who get gynecomastia

both genders can see hypertrophy of the gums in the mouth (because tissue in mouth is similar to vaginal tissue and estrogen sensitive

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23
Q

what is primary progestin

A

progesterone

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24
Q

what are progestins necessary for / what do they do

A

progesterone is necessary for implantation of the embryo and to be viable

once embryo in place, progesterone maintains pregnancy

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25
Q

what happens to females with not a lot of progesterone

A

miscarriages early in pregnancy

used to have a vaginal suppository of progesterone to help solve this issue

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26
Q

how can progestins be used for birth control

A

in pharmacologic doses (big doses) can inhibit releases of FSH and LH

aka birth control effect

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27
Q

how are progestins absorbed/distributed

A

absorbed well orally

unique: IM absorption can take place over 3-6 months (aka takes that long to reach steady state- depo shot long acting progestin)

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28
Q

how are progestins excreted

A

undergoes glucuronidation and excreted in urine

on slides, but didnt mention

29
Q

what are the two conjugated estorgens

oral estrogens for hormone replacement therapy

A

both are oral estrogens

premarin - horse source

cenestin - plant source

30
Q

what is unique about premarin

A

premarin stands for pregnant mare estrogen

made from pregnant horse urine - take out the conjugated estrogen- pill form

oral estrogen - specifically conjugated estrogen

31
Q

what are the types of oral estrogens

A

conjugated estrogens (premarin and cenestin)

estradiol (estrace)

for hormone replacement therapy

32
Q

estradiol

what is it commonly prescribed for

A

form of oral estrogen

natural estrogen (human)

1 of 3 estrogens in the body

prescribed for hormone replacement (pill, vag cream, patches no first pass metabolism through skin)

33
Q

what are the various formulations of hormone replacement therapy

A
  1. oral forms (conjugated and estradiol)
  2. vaginal estrogens (tablets, creams, rings)
  3. IM estrogens (depoestradiol)
  4. progestins
34
Q

what are the types of progestins for hormone replacement therapy

A

Medroxyprogesterone (provera) !!!!

  • depo version
  • can come in tablet form
  • this is usually given 5-10 days starting on either the 16h or 21st day of cycle
35
Q

SERMS

A

means

selective estrogen receptor modulators

36
Q

what do estrogen SERMS do

when do you use them

A

essentially an estrogen antagonist or partial agonist

use when trying to block estrogen

37
Q

what are the types of Estrogen SERMS

A

tamoxifen !!!!

raloxifene (evista) - osteoporosis

38
Q

Tamoxifen

what is unique

A

a form of estrogen SERMS

blocks estrogen

prescribed for women who estrogen sensitive breast cancer - starving cancer cells to keep them from proliferating

39
Q

how long is the menstrual cycle

A

28 days long

40
Q

what is day one of menstrual cycle

A

when menses starts

41
Q

what day is ovulation in the menstrual cycle

what causes ovulation

A

day 14

sharp surge in LH with simultaneous increase in FSH causes ovulation

42
Q

what is estrogens role in the menstrual cycle

A

initially is negative feedback to LH and FSH during follicular phase of the cycle

then positive feedback to FSH and LH causing spike -=ovulation

the increase in estrogen is what causes PMS symptoms

FSH and LH have a negative feedback on estrogen once they spike= decrease in estrogen

43
Q

what happens with progesterone during the menstrual cycle

what phase

A

when ovulation occurs, FSH and LH spike is a negative feedback to estrogen= decrease in estrogen

as estrogen drops, there is an increase in progesterone (second half of cycle = luteal phase)

REMEMBER: progesterone= to prepare for implantation of egg and sustaining pregnancy
progesterone= PRO pregnancy

44
Q

what happens to progesterone if no implantation of egg

what does the answer to above signal

A

progesterone will plateau and eventually drops

it dropping signals for mensuration

45
Q

what are the different forms of hormonal contraception available

A

birth control pills

vaginal rings

birth control patch

depo shots

46
Q

what aspect of contraceptive hormones worsen acne

A

ones with high androgenic

this is just supp info`

47
Q

what are the different oral formulations of hormone drugs

not formulations of Hormone replacement therapy

A

monophasic

biphasic

triphasic

48
Q

what is described as the following

fixed dosage of estrogen to progestin throughout cycle

A

monophasic formulation

49
Q

what is described as the following

Estrogen remains the same dose for the first 21 days

progestin is a lower dose for the first half of cycle allowing for endometrial proliferation

increase in progestin 2nd half of cycle to provide adequate secondary development

A

biphasic formulation

progestin dose changes only once during cycle
usually estrogen stays the same

50
Q

what is described as the following

usually estrogen amount stays same while progestin dose changes through cycle

A

triphasic formulation

51
Q

progesterone used as birth control in nursing women

A

often favored by the mom over estrogen (reduce breast milk maybe)

may cause depression

52
Q

what are the side effects of oral contraceptives

A
  • weight gain
  • sexual desire (androgens- can be increased or decreased)
  • vaginal discharge
  • menstrual flow
  • breast size
  • blood pressure
  • complexion
  • break through bleeding
  • naseua/headaches
  • UTI
  • depression
  • Gum inflammation
53
Q

what are the oral contraceptive formulations

A
  1. progestins only
    - tablet
  2. transdermal
  3. depo injection
  4. Vaginal ring
54
Q

what are the two types of depo contraceptives we know

A

depoestradiol - IM estrogen

depoprovera (medroxyprogesterone) - also comes in non depo form

55
Q

what are the transdermal formulations for oral contraceptives

A

Norelgestromin/EE (Xulane)- not on quiz list

estradiol transdermal systems (vivelle, climara, estraderm)

56
Q

what is an example of a vaginal ring

A

etonogestetrel/EE (nuvaring)

inserted 3 weeks and removed one week break

57
Q

when acne is a problem what is the solution

A

increase estrogen, decrease androgens

58
Q

if someone is experiencing breakthrough bleeding, what is the solution

A

increase estrogen, and increase progestin (aka just increase hormones)

59
Q

for someone experiencing ovarian cysts what is a solution

A

decrease the hormones (decrease androgen, decrease estrogen)

60
Q

if someone is experiencing breast soreness, what is the solution

A

decrease estrogen

possibly go progestin only

61
Q

if someone is experiencing depression / moodiness, what is the solution

A

decrease progestin

62
Q

if someone is experiencing headaches what is the solution

A

decrease estrogen, decrease progestin

avoid hormone fluctuations (ex: seasonale, seasonique)

63
Q

if someone is experiencing severe cramps, what is the solution

A

increase progestin

avoid periods through most birth control pills will help cramps

64
Q

if someone is experiencing weight gain, what is the solution

A

decrease estrogen and progestin

65
Q

if someone is experiencing poly cystic ovarian syndrome (PCOS), what is the solution

A

decrease androgen

66
Q

if a women is breast feeding and wants to be on birth control what hormone do you avoid

A

estrogens should be avoided

have progestin only

67
Q

what do bc called seasonale and seasonique do

what are they good for

A

they extend the cycle

considered continous oral contraceptives

so they may take 91 days worth of pills before placebo week

good for

  • endometriosis, premenstrual dysphoric disorder, lifestyle reasons
  • breakthrough is common
68
Q

what happens if a 2 year old female eats an entire pack of birth control pills

A

little girl will have vaginal bleeding

may get breast tissue hypertrophy for a little while

will return to normal

69
Q

testosterone CIII what are the different formulations

A
  1. transdermal products (patch, gel)
  2. oral products (testosterone, methyltestosterone)
  3. injection

often abused for libido enhancing and weight lifting
side effects
-anger
-testicular atrophy

Pharmacology (13 decks)

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