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Unit 3 Pharm II > MOAs > Flashcards

MOAs Flashcards

1
Q

Long acting GnRH agonists

A

Continuous administration suppresses release of LH and FSH (after initial surge)

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2
Q

GnRH antagonists

A

Suppress LH and FSH

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3
Q

hMG

A 
Used for FSH effects:
Induces spermatogenesis (takes months) 
IVF: 9-12 days stimulates ovaries→ estrogen
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4
Q

hCG

A

Used for LH effects:

Increases testosterone (for up to a year)

IVF: single dose to induce ovulation

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5
Q

Estrogens act on

A

Nuclear Receptors

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6
Q

Estrogen + uterus

A

endometrial growth

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7
Q

Estrogen + vaginal epithelium

A

proliferation, maintenance

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8
Q

Estrogen + endocervical glands

A

mucus

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9
Q

Estrogen + breasts

A

Breast growth in puberty and pregnancy

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10
Q

Estrogen + bones

A

Bone maintenance
osteoclast apoptosis.
Osteoblast: decreased IL-6 and RANKL, increased OPG

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11
Q

Estrogen + blood

A

Increased synthesis of blood clotting proteins

Increased platelet adhesiveness

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12
Q

Estrogen + lipids

A

Increased HDL

Decreased LDL

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13
Q

Estrogen + Liver

A

clotting factors, hormone binding proteins: SHBG, CBG, TBG

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14
Q

Estrogen + kidney

A

Na+ and H2O retention

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15
Q

Estrogen + ovary

A

prepare for ovulation

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16
Q

Clomiphene

A

Anti-estrogen at the hypothalamus

Agonist in other tissues

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17
Q

Tamoxifen

A

Selective estrogen receptor modulator:
Agonist: uterus, bone
Antagonist: breast

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18
Q

Raloxifene

A

Selective estrogen receptor modulator:
Antagonist: breast, uterus
Agonist: bone, liver

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19
Q

Fulvestrant

A

Pure estrogen antagonist

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20
Q

Toremifene

A

Selective estrogen receptor agonist similar to tamoxifen

Increases HDL

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21
Q

Anastrozole

A

Nonsteroidal competitive inhibitor of aromatase

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22
Q

Exemestane

A

Steroid, irreversible aromatase inhibitor

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23
Q

Letrozole

A

Nonsteroidal competitive inhibitor of aromatase

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24
Q

19-Nortestosterones

A

Progestin

Derived from testosterone→ also have androgenic activity

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25
Q

Mifepristone

A

Antiprogestin

Blocks binding to progesterone receptors and glucocorticoid receptor

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26
Q

Danazol

A

Antiprogestin

Weak progestin, androgen, and glucocorticoid that suppresses ovarian function

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27
Q

Progesterone acts on

A

Acts on nuclear protein receptors→ DNA→ mRNA synthesis→ protein synthesis

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28
Q

Progesterone + uterus

A

converts endometrium to secretory state→ maintains pregnancy by suppressing uterine contractility

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29
Q

Progesterone + endocervical glands

A

regulates composition of cervical mucus

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30
Q

Progesterone + body temp

A

Increases body temperature (thermogenic)

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31
Q

Progesterone + breasts

A

lobuloalveolar development in mammary ducts, pregnancy, puberty

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32
Q

Oral combination pill: estrogen + progesterone

A

Inhibit LH surge→ no ovulation
Cause changes in cervical mucosa and endometrium that decrease implantation
Discontinuation→ bleeding at the end of the cycle
Low level estrogens reduce mid-cycle bleeding

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33
Q

Anabolic effects of androgens

A

Increased bone density, amino acid incorporation into muscle, red blood cell mass
Antagonize catabolic effects of glucocorticoids

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34
Q

Flutamide

A

Androgen receptor antagonist

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35
Q

High doses of spironolactone

A

Mineralocorticoid antagonist, Androgen receptor antagonist

36
Q

Finasteride, Dutasteride

A

5 alpha reductase inhibitors→ no DHT→ suppresses male sex accessory organs without affecting libido

37
Q

GLUT1

A

brain

38
Q

GLUT2

A

beta cells of pancreas, Km=15-20 (highest Km=lowest affinity)

39
Q

GLUT3

A

brain

40
Q

GLUT4

A

Muscle, adipose tissue, Km=5, insulin-mediated

41
Q

Glucagon

A

Hormone produced by alpha cells of pancreas→ regulates glucose, amino acids, +/- free fatty acid homeostasis
→ Increases blood glucose levels by mobilizing hepatic glycogen when available

42
Q

Diazoxide

A

Non-diuretic thiazide, vasodilator, hyperglycemic
→ directly inhibiting insulin secretion
→ decreasing peripheral glucose utilization
→ stimulating hepatic glucose production

43
Q

Metformin

A

Decreases glucose levels, insulin-independent
Increased: glucose removal from blood: AMPK, secretion of GLP-1
Decreased: glucose absorption from GI, glucagon levels, gluconeogenesis (mitochondrial enzyme inhibtion)

44
Q

GLP1 and GIP

A

increase release of insulin

released from bowel in response to glucose

45
Q

GLP 1

A

inhibits glucagon release → decreased hepatic gluconeogenesis

46
Q

DDP-4 (dipeptidyl peptidase)

A

binds to and degrades GLP-1 and GIP

47
Q

GLP-1 agonists

“tides”

A

GLP-1 agonists resistant to DPP-4 degradation

48
Q

DPP-4 inhibitors

“gliptins”

A

DDP-4 inhibition potentiates the effect of endogenous incretin hormones

49
Q

SGLT-2 inhibitors

“flozins”

A

inhibit sodium-glucose co-transporter 2 (SGLT-2) in the kidney

50
Q

Thiazolidinediones

“glitazones”

A

Insulin sensitizers→ specifically target insulin resistance
Ligand of the nuclear PPAR-gamma receptor→ post-receptor insulin mimetic action:
Increased glucose transporter synthesis in adipose
Decreased hepatic glucose production

51
Q

Alpha glucosidase inhibitors
Acarbose
Miglitol

A

Inhibition of alpha glucosidases in small intestine→ delayed carbohydrate digestion and absorption

52
Q

Sulfonylureas

A

Binding to and blocking ATP-sensitive K+ channel→ depolarization→ Ca++ influx in beta cells→ insulin exocytosis

53
Q

Meglitinides

“Glinide”

A

Binding to and blocking ATP-sensitive K+ channel→ depolarization→ Ca++ influx in beta cells→ insulin exocytosis

54
Q

Colesevelam

A

Bile acid binding resin

MOA for glycemic effect unknown

55
Q

Bromocriptine

A

Quick acting dopamine agonist
Augments low hypothalamic dopamine levels→ inhibition of excessive sympathetic tone in CNS→ decreased post meal plasma glucose levels due to enhanced suppression of hepatic glucose production

56
Q

Pramlintide

A

Synthetic analog of amylin, a hormone co-secreted with insulin
→ regulation of postprandial glucose:
Decreased gastric emptying
Suppression of postprandial glucagon secretion
Centrally mediated modulation of appetite→ decreased caloric intake

57
Q

Oxytocin

A

Cyclic octapeptide stored in posterior pituitary

Suckling/cervical pressure→ release

58
Q

Ergot alkaloids

A

Activation of serotonin receptors and alpha receptors→ contraction of uterine smooth muscle

59
Q

Synthetic prostaglandin E2 (Dinoprostone)

A

causes:
expulsion of uterine contents
Cervical ripening prior to delivery at term

60
Q

Prostaglandin: PGF2 alpha derivative (15 methyl) (caboprost tromethamine)

A

Induce abortion in 13th and 20th week

3rd line: postpartum bleeding due to uterine atony

61
Q

Tranexamic acid

A

Inhibits plasminogen activation→ antifibrinolytic

62
Q

Magnesium Sulfate (MgSO4)

A

Unknown

Relaxes uterus, probably direct effect

63
Q

Nifedipine

A

L-type calcium channel blocker→ inhibits Ca++ influx→ inhibits smooth muscle contraction

64
Q

Indomethacin

A

Inhibits COX enzyme→ reduction of prostaglandin synthesis

65
Q

Prophylactic Progesterone

A

Maintaining length of pregnancy from 16th week-37 weeks/delivery
→ high risk women with a history of preterm birth
→ approved for use in assisted reproductive technology to maintain the luteal phase following IVF or intracytoplasmic sperm injection

66
Q

Nitroglycerin

A

100 ug IV bolus → sudden transient cervicouterine relaxation within 45-90 seconds, lasting about 1 minute

67
Q

Ethanol

A

Direct relaxant effect on myometrium

Inhibits oxytocin release

68
Q

Thioamides

A

Inhibits synthesis of T4

Propylthiouracil: Blocks conversion of T4→ T3

69
Q

Iodide

A

Decreases synthesis and release of T3/T4

Short term effect: 2-8 weeks

70
Q

Radioactive Iodine

I-131

A

Small amounts microCi=diagnostic

Large amounts mCi=destroys gland

71
Q

Propranolol

A

Non-specific beta blocker

Specifically inhibits conversion T4→ T3

72
Q

OPG=osteoprotegerin

A

comes from osteoblasts, blocks RANKL

73
Q

RANKL

A

ligand for receptor for activation of nuclear factor-kB → positive effect on osteoclast, preosteoclast
stimulated by Vit D

74
Q

Calcitonin

A

Decreases bone resorption of calcium

Antagonizes PTH

75
Q

PTH drugs

A

→ more osteoblast activity→ osteoporosis in men/postmenopausal

PTH and PTHrP bind to PTH receptor type 1 (PTHR1) RG conformation on osteoblast→ activation:
Decreased new fractures
Stimulates formation of new bone: ONLY anabolic drugs

rhPTH also binds PTHR1 R0 confirmation→ more osteoclast activity→ hypoparathyroidism tx

76
Q

Denosumab

A

Antibody against receptor activator of nuclear factor kappa-beta ligand (RANKL)
→ inhibits bone resorption
→ inhibits RANKL-mediated osteoclast maturation

77
Q

Bisphosphonates

A

P-C-P bond analogs of pyrophosphate→ substitutes for PO4 in Ca++ binding→ incorporates into bone→ inhibit resorption
Mechanism unclear: inhibition of osteoclasts, bone resorption

78
Q

Fludrocortisone

A

Mimics aldosterone
Has mineralocorticoid and some glucocorticoid activity
Used to treat adrenal insufficiency refractory to glucocorticoids alone: inadequate salt/water retention

79
Q

Hydrocortisone

A

Slow onset and long lasting: Bind to cytoplasmic receptor (nuclear receptor) → simulate gene transcription
Some rapid actions (poorly understood)

80
Q

Prednisone/Prednisolone

A

Glucocorticoid>mineralocorticoid

Prednisone: Must first be activated by liver: converted to prednisolone

81
Q 
Triamcinolone
Methylprednisolone
Betamethasone
Dexamethasone
Fluticasone
A

Newer glucocorticoid drugs→ Virtually no mineralocorticoid activity

82
Q

Ketoconazole

A

Corticosteroid synthesis inhibitor
Antifungal that inhibits steroid synthesis at very high doses
Non-selective

83
Q

Mitolane

A

Corticosteroid synthesis inhibitor

Adrenocrotioclytic→ causes adrenocortical atrophy→ used for primary adrenal carcinoma

84
Q

Metyrapon

A

Corticosteroid synthesis inhibitor

Selective inhibitor of terminal enzyme in cortisol synthesis

85
Q

Mifepristone

A

Antagonist of glucocorticoid and progesterone receptors

Unit 3 Pharm II (8 decks)

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