Exam 4 Endocrine Pharmacology Flashcards

1
Q

Ovine corticorelin (Acthrel)

A

CRH analog. helps release ACTH. Used for dx Cushings

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2
Q

Corticotropin (Acthar)

A

porcine ACTH. used for adrenal insuff dx (by stim adrenals), symptoms of MS (by immunosupp) and infantile spasms

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3
Q

Cosyntropin (Cortrosyn)

A

synthetic ACTH. used for adrenal insuff dx (by stim adrenals)

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4
Q

hydrocortisone, cortisone, prednisone, prednisolone, methylprednisolone, mometasone furoate (topical)

A

short acting and low potency glucocorticoids

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5
Q

traimcinolone (+nystatin)

A

intermediate acting and potency glucocorticoid

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6
Q

betamethasone, dexamethasone, clobetasol prop (topical)

A

long-acting with high potency glucocorticoid

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7
Q

dexamethasone sod phos, fluorometholone, medrysone, prenisolone acetate, difluprednate

A

opthalmic GC for allergic conjunctivitis, post-op inflammation

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8
Q

fludrocortisone

A

only MINERALCORTICOID. for hypoaldosteronism or adrenal insuff.

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9
Q

adrenal insuff use MOA

A

replacement addisons disease

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10
Q

anti-inflammatory general MOA

A

inhibits and decreases PLA2 expression

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11
Q

anti-inflamm for asthma MOA

A

decrease COX2 exp

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12
Q

anti-inflamm for arthritis MOA

A

decrease leuk count

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13
Q

anti-inflamm for GI

A

decrease leuk function

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14
Q

anti-inflamm for post sx

A

decrease macrophage function

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15
Q

uses of GC *5 As

A

adrenal insuff, anti-inflamm, allergies, auto-immune and anti-neoplastic

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16
Q

SE of GC general

A

cushings like

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17
Q

SE of GC adrenicortical insuff d/t

A

adrenal suppression

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18
Q

SE of GC hyperglycemia d/t

A

decrease glucose uptake and increased glycogen

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19
Q

SE of GC muscle wasting d/t

A

increase GNG

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20
Q

SE of GC hyperNa, edema, HTN, hypoK, alkalosis d/t

A

increase NA, decrease K and decrease H reabs.

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21
Q

SE of GC ammenorrhea/hirsutism d/t

A

decrease LH (and thus estrogen)

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22
Q

SE of GC stunted growth d/t

A

decrease GH

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23
Q

SE of GC peptic ulcers d/t

A

decrease PLA2 and COX2

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24
Q

SE of GC immunosupp/infection d/t

A

decrease leuk, decreased PLA2 and COX

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25
Q

SE of GC myopathy d/t

A

decrease K reabs

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26
Q

SE of GC osteoporosis d/t

A

inhibits osteoblast and decrease Ca from gut which leads to increase PTH (pulling Ca from bone)

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27
Q

SE of GC cataracts d/t

A

oxidative stress induced by GCs depletes GSH

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28
Q

GC contraindicated in

A

DM, hypothyroid, ulcers, inf (esp TB), preg, COPD

29
Q

GC interactions with

A

P450 inducers, NSAIDs, K depleting diuretics and vaccines

30
Q

pasireotide (signifor LAR)

A

anticorticosteriod which inhibits release of ACTH via SST5. used for cushings or acromegaly (extra GH) when sx fails. analog of SST and is selective for SST2 and 5.

31
Q

metyrapone (metopirone)

A

anticorticosteroid that inhibits 11beta-hydroxylase (synthesis inhibitor). inhibits cortisol and aldosterone synthesis. used to dx HPA axis or tx tumors. if give should see low cortisol causing increase in CRH/ACTH release and increase in 11-deoxycortisol so hypo/pit okay!

32
Q

mitotane (lysodren)

A

anticorticoid binds mitochondria proteins to cause atrophy in zona fasc and reticularis of adrenal cortex (synthesis inhibitor). only effects GC. used for adrenal tumor.

33
Q

mifepristone (korlym) aka mifeprex

A

anticorticosteroid antagonizes progesterone and GC receptors at higher conc (receptor antag-tx excess cortisol) used for abortion, cushings from ectopic ACTH.

34
Q

spironolactone

A

anticorticosteroid that antagonizes MC receptors (excess aldosterone). used for primary or secondary aldosteronism, edema, hypoK, HTN and HF.

35
Q

androgen general MOA

A

activation of nuclear androgen receptor. used for breast tumors, anabolics, anemia, osteoporosis, reverse male aging.

36
Q

goserelin, nafarelin, triptorelin, histrelin, leuprolide

A

GnRH analogs, receptors agonists (antiandrogen). long-acting analogs suppress FSH/LH. for prostate CA or BPH in males and for breast CA, endomet…in women.

37
Q

degarelix (firmagon)

A

GnRH antagonist (antiandrogen)

38
Q

abiraterone acetate (zytiga)

A

testosterone and estrogen synthesis inhibitors (antiandrogen). inhibits CYP17 to inhibit synthesis of test/estrogen. used for AR + prostate tumors.

39
Q

finasteride and dutasteride

A

DHT synthesis inhibitors (antiandrogen). inhibits 5alpha reductase (esp type2). used for BPH, alopecia and hirsutism in women. dutasteride-type 1 and 2.

40
Q

flutamide, bicalutamide, nilutamide, enzalutamide and spironolactone

A

androgen receptor antagonists (antiandrogen). competitive antagonism of androgen receptors. uses for prostate CA and XS androgen in women.

41
Q

gonadotropins

A

FSH and LH

42
Q

Menotropins, hMG

A

FSH and LH like drug for infertility

43
Q

Urofollitropin, hFSH

Follitropin alfa, r-hFSH

A

FSH like drugs for infertility

44
Q

Lutropin alfa, r-hLH:LH

hCG

A

LH/LH like drugs for infertility

45
Q

ganirelix acetate, cetrorelix

A

long acting analogs suppress FSH/LH. these are antagonists!

46
Q

hypogonadotropic hypogonadism

A

lutropin alfa with follitropin alfa one day then hCG day later

47
Q

controlled ovarian hyperstimulation

A

urofollitropin on day 2/3 of cycle then GnRH antagonist from day 7/8, then give hCG

48
Q

infertility d/t anovulation/irregular

A

clomiphene (estrogen antagonist) for 5 days

49
Q

estrogen drugs

A

activate estrogen receptors. for OC, replacement, menses issues, osteoporosis, acne

50
Q

tamoxifen and toremifene (SERM)

A

selective estrogen receptor modulator. antagonizes E2 induced proliferation of breast CA cells. used for breast CA or prophylaxis for recurrence. reloxifene-works in same way but doesn’t stimulate uterine growth.

51
Q

bazedoxifene + conj estrogens (SERM)

A

estrogen effect on bone, antagonism of estrogen effect on uterine cells. uses to prevent menopause and related osteoporosis.

52
Q

ospemifene

A

estrogen agonist effect in vag endometrium, not breast. for dispareunia

53
Q

fulvestrant (faslodex)

A

estrogen receptor antagonist. antagonizes and degrades ERs. for breast CA.

54
Q

clomiphene (clomid)

A

estrogen receptor antagonist. blocks estrogen inhibition of GnRH at hypothalamus. used for induction of ovulation.

55
Q

danazol

A

antagonizes progestin and GC receptors and activates androgren receptors. inhibits many steroid enzymes. used for endometriosis.

56
Q

anastrozole, letrozole, exemestane

A

estrogen synthesis inhibitors. reversible or irrev inhibition of aromatase. used for breast CA in post menopausal women.

57
Q

progestin MOA general

A

activation of receptor, replace with smaller periodic doses, large dose causes long term supp. used for replacement, contraception, menses issues, endomet.

58
Q

ullipristal

A

progestin receptor antagonist. antagonizes progestin receptor. for post-coital contraception.

59
Q

mifepristone

A

progestin and GR antagonist. antagonizes progestin receptors ad GC receptors. for post-coital contraception.

60
Q

korlym

A

anti-progetin that can be used for hyperglycemia.

61
Q

hormonal contraception MOA

A

estrogen and progestin activate negative feedback to prevent GnRH, FSH and LH secretion. progestins-delay ovum transport, thicken mucus.

62
Q

estrogens and LDL/HDL

A

decrease LDL and increase HDL. progestin works opposite.

63
Q

progestin BC: desogestrel, norgestimate, ethynodiol, norgestrel, norethindrone, drospirinone, dienogest.

A

same dose or increasing during cycle.

64
Q

norgestimate, norgestrel, levonorgestrel, drospirenone

A

monophasic

65
Q

desogestriel (mircette)

A

biphasic

66
Q

norgestimate, norethindrone

A

triphasic

67
Q

dienogest + estradiol (natazia)

A

four-phasic

68
Q

emergency contraception P or E+P

A

plan B (levonorgestrel), next choice. MOA feedback inhibition prevents GnRH, LH, FSH which prevents or delays ovulation and implantation

69
Q

emergency contraception P agonist/antagonist

A

Ulipristal-comp antagonist of progestin receptor which prevents or delays ovulation/implant. Mifepristone-comp antagonist of progestin receptor, stimulation of uterine contraction