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FM1, Block 1 > Pharm > Flashcards

Pharm Flashcards

1
Q

pharmacokinetics

A

body’s affect on drug

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2
Q

pharmacodynamics

A

drug’s affect on body

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3
Q

summation

A

simple additive effect of 2 drugs

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4
Q

synergism

A

greater than simple addition

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5
Q

latency

A

delayed onset

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6
Q

tolerance

A

acq. insensitivity

requires >/=1 exposure

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7
Q

tachyphylaxis

A

rapid tolerance

single dose followed by another dose leads to no response

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8
Q

bradyphylaxis

A

slow tolerance
built up over time
ex: opioids

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9
Q

drug resistance

A

lack of responsiveness

no previous exposure

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10
Q

drug sensitivity

A

exaggerated response

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11
Q

ideal drug characteristics

A 
efficacy
safety
selectivity (no side effects)
reversible
ease of admin
predictable
no drug interactions
cheap
chemical stability
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12
Q

phase 1 trial

A

healthy people - is it safe

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13
Q

phase 2 trial

A

sick people, does it work

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14
Q

phase 3 trial

A

more sick people, does it work/do we see toxicities

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15
Q

phase 4 trial

A

post-marketing surveilance

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16
Q

1906 federal pure food and drug act

A

labeling law

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17
Q

1938 food, drug, cosmetic act

A

required safety, not efficacy

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18
Q

1962 harris-kefauver amend.

A

required efficacy

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19
Q

pregnancy risk categories

A

A,B,C ok
D - risks don’t outweigh benefits
X - risks do outweigh benefits -DON’T PRESCRIBE

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20
Q

characteristics of drugs that cause allergy

A

previous exposure
molecule >1Kd
covalently linked to macromolecule
can lead to anaphylactic shock (histamine)

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21
Q

common sx of drug allergy

A 
angioedema
urticaria
swelling mucous mem
cough, wheeze, SOB
hypotension
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22
Q

non-specific drug action mech

A

physiochemical process
needs high concentration
varied structures work the same way
slight structural changes ok

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23
Q

specific drug action mech

A

act on receptors, enz, transporters (macromolecules)
low concentration
changing structure has big impact

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24
Q

ligand-regulated transmem enzymes

A

ligand binding causes dimerization of transmem. regions

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25
Q

tyrosine transmem enzyme

A

tyrosine residues kinase each other -> cascade

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26
Q

JAK-STAT

A

JAKs dimerize -> bind STAT -> kinase activity -> cascade

27
Q

GPCR

A

7 transmem domains
alpha subunit = specificity
alpha dissociates when ligand binds –> binds GTP -> adenyl cyclase -> cAMP

28
Q

Gs subunit of GPCR

A

beta adrenergic, glucagon, histamine, serotonin

AC–>cAMP

29
Q

Gq subunit of GPCR

A

ACh muscarinic receptor

PLC-> IP3 and DAG -> inc intracell Ca

30
Q

short term GPCR desensitization

A

GRK phosphorylate Ser and Thr residues, inhibiting interaction with G proteins -> bind to b-arrestin -> dec signal

31
Q

long term receptor desensitization

A

lysosomal degradation (clathrin coating)

32
Q

Kd

A

small Kd= tight binding/high affinity

drug concentration at which 50% of receptors are occupied

33
Q

EC50

A

concentration at which drug is giving 50% response

34
Q

ED50

A

dose at which drug gives 50% response

35
Q

Quantal response

A

all or nothing response

36
Q

Graded response

A

continuous variable

37
Q

Spare receptors (EC50 vs Kd)

A

when there’s spare receptors, EC50 is less than kD

38
Q

Therapeutic index

A

TI = TD50/ED50 = toxicity/efficacy

want a HIGH number

39
Q

Certain Safety factor

A

CSF = TD1/ED99

want HIGH number

40
Q

antagonists

A

no intrinsic efficacy (but can have biologic effects)

blunts effects of agonists

41
Q

physiologic antagonist

A

drugs produce opposing responses by acting on different systems

42
Q

chemical antagonist

A

antag. chemically alters the agonist

43
Q

inverse agonist

A

does have intrinsic activity

can reduce response below baseline

44
Q

competitive antagonism

A

reversible, surmountable

ED50 inc, but max response doesnt change

45
Q

noncompetitive antagonism

A

insurmountable

ED 50 unchanged, but max effect decreases

46
Q

Enteric routes of drug admin

A

PO, SL, PR

47
Q

Parenteral routes of drug admin

A

SC, Pulmonary, IV, Intra-arterial, IM, Intra-thecal, topical
bypass GI and liver
rapid, predictable
$$(sterile), painful, hard to self-admin

48
Q

SL administration

A

lipophilic
fast
avoids first pass

49
Q

PO adminstration

A

safe, easy, cheap

slow, variable, 1st pass phenom.

50
Q

PR admin

A

good for vom/unconscious

50% goes 1st pass

51
Q

Pulmonary admin

A 
gas and volatile drugs, aerosols
rapid
 alveoli
1-5 --> GI 
>5 --> upper airway
52
Q

Intra-thecal admin

A

spinal anesthesia

bypass BBB

53
Q

SC admin

A

not good for irritating or large volumes

slow absorption can give sustained effect

54
Q

IM admin

A

rapid, allows for more irritating drugs

painful

55
Q

IV admin

A

accurate, fast (depends on infusion rate), large vol/irritating substances
not for oily/insol. drugs

56
Q

ABC transporters

A

transmem proteins that actively extrude cmpds from cells
liver, kidney, intestine, brain, testes, placenta
C1 and C3 –> into blood
PGP, C2, G2 –> into “outside”

57
Q

apparent volume of distribution

A

Amt/Concen = Vol of dist

58
Q

2 most common drug binding proteins

A

Albumin –> weak acids

a1-acid glycoprotein –> weak bases

59
Q

Blood-organ barriers

A

brain
testes *only one that uses occluding instead of TJs
thymus
ocular

60
Q

Phase I rxns

A

oxidative - redox or hydrolytic
Enz: CYP: 1a2, 2c9, 2c19, 2d6*, 3a4
req: NADPH (activates enz), O2 (oxidized drug)
Other enz: FAD mono, MAO, ADH, ald DH, XO

61
Q

Phase II rxns

A 
congugation - couple polar grps to fxnl substrates
5 types
1. glucuronidation
2. sulfation
3. mercapturic acid formation
4. NOS methylation
5. arylamine n-acetyltransferase
62
Q

Drugs that induce CYPs

A

glucocorticoids
anticonvulsants
HIV drugs
St. John’s wart

63
Q

Drugs that inhibit enz induction

A

antibiotics
azole antifungals
grapefruit jice

64
Q

drugs affected by CYP polymorphisms

A 
antipsychotics
warfarin
omeprazole
codine
SSRIs

FM1, Block 1 (2 decks)

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