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bms 420 > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

semiantagonism

A

the idea that partial agonists can act as antagonists because they can bind and reduce the Emax of the endogenous drug

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2
Q

inverse agonists

A

they bind to the receptor site preferentially in the inactivate state to lower basal activity
THESE ARE NOT ANTAGONISTS

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3
Q

spare receptors

A

the idea that only a fraction of the total receptors are needed to yield a 100% response. EC50<Kd HERE. think of insulin

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4
Q

therapeutic index

A

calculated by ld50/ed50

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5
Q

downregulation

A

a decrease in the number of receptors typically when they are overstimulated

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6
Q

tachyphylaxis

A

acute tolerance build up

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7
Q

competitive agonist

A

type of agonist that shifts curve right

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8
Q

noncompetetive antagonists

A

type of agonist that shift curve down

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9
Q

mdr1

A

the most important drug transporter

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10
Q

first pass effects

A

in oral consumption of drugs, it causes a loss of much of the dose

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11
Q

bioavailability

A

auc(drug given as tablet)/auc(drug given as IV)

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12
Q

loading dose equation

A

Co(plasma drug concentration at time 0)= X(total amount of drug in body)/[volume of distribution *patient weight]

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13
Q

target mediated drug disposition

A

the process of eliminating monoclonal antibodies(fast, mAb specific)

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14
Q

half time for drug elimination

A

T1/2=.693/first order elimination rate constant

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15
Q

hepatic metabolism

A

the dominant elimination mechanism for lipophilic drugs

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16
Q

phase 1 of hepatic metabolism

A

the oxidization of lipophilic drugs into polar molecules by cytochrome p450

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17
Q

phase 2 of hepatic metabolism

A

the addition of groups to a drug to make it more water soluble and therefore more easy to excrete in urine

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18
Q

renal elimination

A

the primary mechanism of elimination for hydrophilic drugs. filtration secretion reabsorption and excretion in the nephron

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19
Q

bile excretion

A

main elimination mechanism for large hydrophilic molecules (can be slow because some drugs may go through enterohepatic circulation)

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20
Q

maintenance dose

A

Css(steady state plasma drug concentration)= infusion rate/ CI(drug clearance total)

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21
Q

beta lactam antibiotics

A

penicillins and cephalosporins

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22
Q

penicillin prototype drugs

A

G, V and amoxicillin. cell wall moa. treats otitis media, bronchitis, and pneumonia. can cause anyphlyacti shock but its very rare

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23
Q

cephalosporins

A

proto drug= cephalexin. cell wall moa. crosses bbb. treats meningitis. can cause anaphylactic shock but rare

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24
Q

cell membrane antibiotics

A

daptomycin. cell membrane moa. interactions with statins cause muscle toxicity

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25
Q

ribosomal antibiotics

A

tetracyclines, aminoglycosides, microlides, chloramphenicol

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26
Q

tetracyclines

A

doxycycline. mechanism through 30 s ribosome. reversible. impaired by food. tooth coloration bone deposition and growth inhibition. no children or pregos. interacts negatively with dairy and antacids

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27
Q

aminoglycosides

A

tobramycin, 30s ribosome irreversible, treats eye infection, but is ototoxic(hearing/balance)

28
Q

macrolides

A

azithromycin, 50s ribosome, treats gram positive and negative bacteria, disturbed by food, interactions inhibit CYP450

29
Q

Chloramphenicol

A

proto drug same, 50 s reversible, causes bone marrow bad and gray baby syndrome. interactions inhibit cyp 450

30
Q

folic acid antibiotics (antimetabolites)

A

sulfonamides

31
Q

sulfonamides(trimethoprim)

A

synergistic with trimethoprim, sulfamethizole, inhibit folate synthesis, cause photosensitivity and stevens johnson syndrome

32
Q

dna gyrase inhibitors

A

ciprofloxacin

33
Q

ciprofloxacin

A

dna gyrase topoisomerase 2 inhibition, damage growing cartilage, no kids or pregos

34
Q

antimycobacterial antibiotics

A

isoniazid and rifampin

35
Q

isoniazid

A

cell wall moa of mycolic acids, treats tb (mycobacteria)

36
Q

rifampin

A

inhibits rna synthesis, treats tb, orange urine sweat and tears (harmless) cyp inducer

37
Q

ergosterol synthesis antifungals

A

Imidazoles: ketoconazole, moa disrupts ergosterol synthesis by binding to fungal cyt p450, fungistatic

38
Q

antimitotic antifungals

A

griseofulvin: slowly disrupts mitosis, only effective when used against dermatophytes, fungistatic

39
Q

antiinfluenza antiviral

A

oseltamivir: for influenza a and b and avian flu. Neuraminidase inhibitor

40
Q

antihepatitis antivirals

A

sofosbuvir(harvoni), boceprevir, entecavir

41
Q

sofosbuvir

A

hep c drug. (eradication)

42
Q

boceprevir

A

for hep c(eradication) protease inhibitor

43
Q

entecavir

A

hep b (suppression) dna polymerase inhibitor

44
Q

antihiv antiviral

A

abacavir, rilpivirine, darunavir

45
Q

abacavir

A

Nucleoside reverse transcriptase inhibitor. competitive inhibition of hiv reverse trasncriptase and acts to block dna chain elongation

46
Q

rilpivirine

A

nonnucleoside rti. allosteric inhibition of reverse transcriptase

47
Q

darunavir

A

protease inhibitor that blocks post translational modificatio of viral proteins. cyp3a4 inhibitor

48
Q

non cell cycle specific chemo

A

cyclophosphamide: transfers alkyl groups to dna

49
Q

s phase chemo

A

methotrexate, 5-fluorouacil, hydroxyurea, etopside

50
Q

methotrexate

A

inhibits dihydrofolate reductase

51
Q

5-fluorouracil

A

inhibits pyrimidine synthesis

52
Q

hydroxyurea

A

inhibits dna (not RNA) synthesis by blocking ribonucleotide reductase

53
Q

etoposide

A

blocks topoisomerase II

54
Q

g2/m phase chemo

A

bleomycin: causes oxidative damage to dna

55
Q

m phase chemo

A

vincristine, paclitaxel, ixabepilone

56
Q

vincristine

A

vinca alkaloid that inhibits tubulin polymerization, preventing mitosis

57
Q

paclitaxel

A

taxane that targets microtubules and stabilizes them, preventing mitosis

58
Q

ixabepilone

A

antimicrotubule inhibitor. like taxanes they stabilize microtubules to prevent mitosis

59
Q

hormone chemo

A

tamoxifen, letrozole, leuprolide, degarelix, flutamide

60
Q

tamoxifen

A

binds to estrogen binding site on hormone binding receptor. antagonist in breast tissue, agonist in bone and endometrium. cancer must be er positive

61
Q

letrozole

A

inhibits aromatase

62
Q

leuprolide

A

GnRH agonist, overstimulates and desensitizes the anterior pituitary

63
Q

degarelix

A

GnRH antagonist, prevents pituitary response to GnRH

64
Q

flutamide

A

Blocks androgen receptor to prevent testosterone effect

65
Q

receptor tyrosine kinaseinhibitor chemo

A

nilotinib and erlotinib

66
Q

nilotinib

A

inhibits tyrosine kinase domane of bcr abl oncroprotein and prevents phosphorylation by atp

67
Q

erlotinib

A

inhibits tyrosine kinase domane of edfr rtk oncroprotein and prevents phosphorylation by atp

bms 420 (2 decks)

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