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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
tyrosine transmem enzyme
tyrosine residues kinase each other -> cascade
26
JAK-STAT
JAKs dimerize -> bind STAT -> kinase activity -> cascade
27
GPCR
7 transmem domains alpha subunit = specificity alpha dissociates when ligand binds --> binds GTP -> adenyl cyclase -> cAMP
28
Gs subunit of GPCR
beta adrenergic, glucagon, histamine, serotonin | AC-->cAMP
29
Gq subunit of GPCR
ACh muscarinic receptor | PLC-> IP3 and DAG -> inc intracell Ca
30
short term GPCR desensitization
GRK phosphorylate Ser and Thr residues, inhibiting interaction with G proteins -> bind to b-arrestin -> dec signal
31
long term receptor desensitization
lysosomal degradation (clathrin coating)
32
Kd
small Kd= tight binding/high affinity | drug concentration at which 50% of receptors are occupied
33
EC50
concentration at which drug is giving 50% response
34
ED50
dose at which drug gives 50% response
35
Quantal response
all or nothing response
36
Graded response
continuous variable
37
Spare receptors (EC50 vs Kd)
when there's spare receptors, EC50 is less than kD
38
Therapeutic index
TI = TD50/ED50 = toxicity/efficacy | want a HIGH number
39
Certain Safety factor
CSF = TD1/ED99 | want HIGH number
40
antagonists
no intrinsic efficacy (but can have biologic effects) | blunts effects of agonists
41
physiologic antagonist
drugs produce opposing responses by acting on different systems
42
chemical antagonist
antag. chemically alters the agonist
43
inverse agonist
does have intrinsic activity | can reduce response below baseline
44
competitive antagonism
reversible, surmountable | ED50 inc, but max response doesnt change
45
noncompetitive antagonism
insurmountable | ED 50 unchanged, but max effect decreases
46
Enteric routes of drug admin
PO, SL, PR
47
Parenteral routes of drug admin
SC, Pulmonary, IV, Intra-arterial, IM, Intra-thecal, topical bypass GI and liver rapid, predictable $$(sterile), painful, hard to self-admin
48
SL administration
lipophilic fast avoids first pass
49
PO adminstration
safe, easy, cheap | slow, variable, 1st pass phenom.
50
PR admin
good for vom/unconscious | 50% goes 1st pass
51
Pulmonary admin
``` gas and volatile drugs, aerosols rapid alveoli 1-5 --> GI >5 --> upper airway ```
52
Intra-thecal admin
spinal anesthesia | bypass BBB
53
SC admin
not good for irritating or large volumes | slow absorption can give sustained effect
54
IM admin
rapid, allows for more irritating drugs | painful
55
IV admin
accurate, fast (depends on infusion rate), large vol/irritating substances not for oily/insol. drugs
56
ABC transporters
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
apparent volume of distribution
Amt/Concen = Vol of dist
58
2 most common drug binding proteins
Albumin --> weak acids | a1-acid glycoprotein --> weak bases
59
Blood-organ barriers
brain testes *only one that uses occluding instead of TJs thymus ocular
60
Phase I rxns
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
Phase II rxns
``` 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
Drugs that induce CYPs
glucocorticoids anticonvulsants HIV drugs St. John's wart
63
Drugs that inhibit enz induction
antibiotics azole antifungals grapefruit jice
64
drugs affected by CYP polymorphisms
``` antipsychotics warfarin omeprazole codine SSRIs ```

FM1, Block 1 (2 decks)

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