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bms 420 > Exam 1 > Flashcards

Exam 1 Flashcards

(67 cards)

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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
ribosomal antibiotics
tetracyclines, aminoglycosides, microlides, chloramphenicol
26
tetracyclines
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
27
aminoglycosides
tobramycin, 30s ribosome irreversible, treats eye infection, but is ototoxic(hearing/balance)
28
macrolides
azithromycin, 50s ribosome, treats gram positive and negative bacteria, disturbed by food, interactions inhibit CYP450
29
Chloramphenicol
proto drug same, 50 s reversible, causes bone marrow bad and gray baby syndrome. interactions inhibit cyp 450
30
folic acid antibiotics (antimetabolites)
sulfonamides
31
sulfonamides(trimethoprim)
synergistic with trimethoprim, sulfamethizole, inhibit folate synthesis, cause photosensitivity and stevens johnson syndrome
32
dna gyrase inhibitors
ciprofloxacin
33
ciprofloxacin
dna gyrase topoisomerase 2 inhibition, damage growing cartilage, no kids or pregos
34
antimycobacterial antibiotics
isoniazid and rifampin
35
isoniazid
cell wall moa of mycolic acids, treats tb (mycobacteria)
36
rifampin
inhibits rna synthesis, treats tb, orange urine sweat and tears (harmless) cyp inducer
37
ergosterol synthesis antifungals
Imidazoles: ketoconazole, moa disrupts ergosterol synthesis by binding to fungal cyt p450, fungistatic
38
antimitotic antifungals
griseofulvin: slowly disrupts mitosis, only effective when used against dermatophytes, fungistatic
39
antiinfluenza antiviral
oseltamivir: for influenza a and b and avian flu. Neuraminidase inhibitor
40
antihepatitis antivirals
sofosbuvir(harvoni), boceprevir, entecavir
41
sofosbuvir
hep c drug. (eradication)
42
boceprevir
for hep c(eradication) protease inhibitor
43
entecavir
hep b (suppression) dna polymerase inhibitor
44
antihiv antiviral
abacavir, rilpivirine, darunavir
45
abacavir
Nucleoside reverse transcriptase inhibitor. competitive inhibition of hiv reverse trasncriptase and acts to block dna chain elongation
46
rilpivirine
nonnucleoside rti. allosteric inhibition of reverse transcriptase
47
darunavir
protease inhibitor that blocks post translational modificatio of viral proteins. cyp3a4 inhibitor
48
non cell cycle specific chemo
cyclophosphamide: transfers alkyl groups to dna
49
s phase chemo
methotrexate, 5-fluorouacil, hydroxyurea, etopside
50
methotrexate
inhibits dihydrofolate reductase
51
5-fluorouracil
inhibits pyrimidine synthesis
52
hydroxyurea
inhibits dna (not RNA) synthesis by blocking ribonucleotide reductase
53
etoposide
blocks topoisomerase II
54
g2/m phase chemo
bleomycin: causes oxidative damage to dna
55
m phase chemo
vincristine, paclitaxel, ixabepilone
56
vincristine
vinca alkaloid that inhibits tubulin polymerization, preventing mitosis
57
paclitaxel
taxane that targets microtubules and stabilizes them, preventing mitosis
58
ixabepilone
antimicrotubule inhibitor. like taxanes they stabilize microtubules to prevent mitosis
59
hormone chemo
tamoxifen, letrozole, leuprolide, degarelix, flutamide
60
tamoxifen
binds to estrogen binding site on hormone binding receptor. antagonist in breast tissue, agonist in bone and endometrium. cancer must be er positive
61
letrozole
inhibits aromatase
62
leuprolide
GnRH agonist, overstimulates and desensitizes the anterior pituitary
63
degarelix
GnRH antagonist, prevents pituitary response to GnRH
64
flutamide
Blocks androgen receptor to prevent testosterone effect
65
receptor tyrosine kinaseinhibitor chemo
nilotinib and erlotinib
66
nilotinib
inhibits tyrosine kinase domane of bcr abl oncroprotein and prevents phosphorylation by atp
67
erlotinib
inhibits tyrosine kinase domane of edfr rtk oncroprotein and prevents phosphorylation by atp

bms 420 (2 decks)

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