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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
what happens to females with not a lot of progesterone
miscarriages early in pregnancy used to have a vaginal suppository of progesterone to help solve this issue
26
how can progestins be used for birth control
in pharmacologic doses (big doses) can inhibit releases of FSH and LH aka birth control effect
27
how are progestins absorbed/distributed
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)
28
how are progestins excreted
undergoes glucuronidation and excreted in urine on slides, but didnt mention
29
what are the two conjugated estorgens | oral estrogens for hormone replacement therapy
both are oral estrogens premarin - horse source cenestin - plant source
30
what is unique about premarin
premarin stands for pregnant mare estrogen made from pregnant horse urine - take out the conjugated estrogen- pill form oral estrogen - specifically conjugated estrogen
31
what are the types of oral estrogens
conjugated estrogens (premarin and cenestin) estradiol (estrace) for hormone replacement therapy
32
estradiol what is it commonly prescribed for
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
what are the various formulations of hormone replacement therapy
1. oral forms (conjugated and estradiol) 2. vaginal estrogens (tablets, creams, rings) 3. IM estrogens (depoestradiol) 4. progestins
34
what are the types of progestins for hormone replacement therapy
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
SERMS
means selective estrogen receptor modulators
36
what do estrogen SERMS do when do you use them
essentially an estrogen antagonist or partial agonist use when trying to block estrogen
37
what are the types of Estrogen SERMS
tamoxifen !!!! raloxifene (evista) - osteoporosis
38
Tamoxifen | what is unique
a form of estrogen SERMS blocks estrogen prescribed for women who estrogen sensitive breast cancer - starving cancer cells to keep them from proliferating
39
how long is the menstrual cycle
28 days long
40
what is day one of menstrual cycle
when menses starts
41
what day is ovulation in the menstrual cycle what causes ovulation
day 14 sharp surge in LH with simultaneous increase in FSH causes ovulation
42
what is estrogens role in the menstrual cycle
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
what happens with progesterone during the menstrual cycle what phase
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
what happens to progesterone if no implantation of egg what does the answer to above signal
progesterone will plateau and eventually drops it dropping signals for mensuration
45
what are the different forms of hormonal contraception available
birth control pills vaginal rings birth control patch depo shots
46
what aspect of contraceptive hormones worsen acne
ones with high androgenic this is just supp info`
47
what are the different oral formulations of hormone drugs | not formulations of Hormone replacement therapy
monophasic biphasic triphasic
48
what is described as the following fixed dosage of estrogen to progestin throughout cycle
monophasic formulation
49
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
biphasic formulation progestin dose changes only once during cycle usually estrogen stays the same
50
what is described as the following usually estrogen amount stays same while progestin dose changes through cycle
triphasic formulation
51
progesterone used as birth control in nursing women
often favored by the mom over estrogen (reduce breast milk maybe) may cause depression
52
what are the side effects of oral contraceptives
- 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
what are the oral contraceptive formulations
1. progestins only - tablet 2. transdermal 3. depo injection 4. Vaginal ring
54
what are the two types of depo contraceptives we know
depoestradiol - IM estrogen depoprovera (medroxyprogesterone) - also comes in non depo form
55
what are the transdermal formulations for oral contraceptives
Norelgestromin/EE (Xulane)- not on quiz list estradiol transdermal systems (vivelle, climara, estraderm)
56
what is an example of a vaginal ring
etonogestetrel/EE (nuvaring) inserted 3 weeks and removed one week break
57
when acne is a problem what is the solution
increase estrogen, decrease androgens
58
if someone is experiencing breakthrough bleeding, what is the solution
increase estrogen, and increase progestin (aka just increase hormones)
59
for someone experiencing ovarian cysts what is a solution
decrease the hormones (decrease androgen, decrease estrogen)
60
if someone is experiencing breast soreness, what is the solution
decrease estrogen possibly go progestin only
61
if someone is experiencing depression / moodiness, what is the solution
decrease progestin
62
if someone is experiencing headaches what is the solution
decrease estrogen, decrease progestin avoid hormone fluctuations (ex: seasonale, seasonique)
63
if someone is experiencing severe cramps, what is the solution
increase progestin avoid periods through most birth control pills will help cramps
64
if someone is experiencing weight gain, what is the solution
decrease estrogen and progestin
65
if someone is experiencing poly cystic ovarian syndrome (PCOS), what is the solution
decrease androgen
66
if a women is breast feeding and wants to be on birth control what hormone do you avoid
estrogens should be avoided have progestin only
67
what do bc called seasonale and seasonique do what are they good for
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
what happens if a 2 year old female eats an entire pack of birth control pills
little girl will have vaginal bleeding may get breast tissue hypertrophy for a little while will return to normal
69
testosterone CIII what are the different formulations
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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