Module Test 3 Set 1

Front 1

APAP major structural feature

Back 1

fxnal amide

Front 2

ASA mechanism

Back 2

NSAID that inhibits COX1/2 irreversibly (only drug that inhibits irreversibly)

Front 3

ASA major structural feature and significance of this

Back 3

has an ester; so metabolized by esterases (Phase I)

Front 4

Main structural feature of Ibuprofen and metabolism

Back 4

1)isobutyl
2)Phase 2 rxns

Front 5

Indomethacin is a ___ derivative

Back 5

indo derivative

Front 6

Etodolac is a ___ derivative

Back 6

perro derivative

Front 7

Nabumetone is a ___ drug...

Back 7

prodrug, activated by CYP450

Front 8

...induce COX-2 gene transcription (6)

Back 8

1)oxidative stress
2)injury
3)inflammation/pain
4)ischemia
5)seizures
6)neurodegenerative diseases

Front 9

NSAIDS dual insult of GI

Back 9

1)primary insult is via direct acid damage due to their free hydroxyl
2)secondary insult via PG inhibition

Front 10

Celebrex
a)has a ___ structure
b)dosing for OA/RA
c)Does it GI side effects
d)main structural feature

Back 10

a)sulfonamide structure
b)200mg for OA, 400mg for RA
c)YES, only 90% selective for COX-2
d)diaryl substituted pyrazole

Front 11

First NSAID

Back 11

Quinine

Front 12

How do NSAIDs reduce fever?

Back 12

decr PG's in the hypothalamus, which is the body's thermostat

Front 13

Precursor to PG

Back 13

arachidonic acid

Front 14

3 sources of arachidonic acid and what is main source

Back 14

1)CELL MEMBRANE PHOSPHOLIPID ESTERS**
2)cholesterol esters
3)triglyceride esters

Front 15

Arachidonic acid is created by what enzyme?

Back 15

phospholipase A2

Front 16

Arachidonic acid interacts w/ 2 enzymes to make 2 products what are they?

Back 16

1)lipoxygenase = LK
2)cyclooxygenase = PG

Front 17

COX 1 fxn (2)

Back 17

1)CONSTITUTIVE FORM
2)found in blood vessels, stomach, tissues where PG is synthesized

Front 18

ADR's of COX non-specific NSAIDS (5)

Back 18

1)GI irritation
2)block platelet aggregation
3)inhibit uterine motility
4)prolong pregnancy
5)hypersensitivity rxns (seen mostly w/ ASA)

Front 19

Salicylates ex (4)

Back 19

1)ASA (prototype)
2)salsalate
3)diflunisal
4)Choline salicylate

Front 20

Effects of salicylates (3)

Back 20

1)analgesic
2)antipyretic
3)anti-inflamm

Front 21

Salicylates absorption

Back 21

rapidly absorbed in stomach, upper intestine, and skin by passive diffusion

Front 22

Antipyretic effect of salicylates (3)

Back 22

1)lowers abnormally high body temp, wont alter normal temp
2)heat production not altered
3)heat dissipation is enhanced by peripheral blood flow and sweating (notice red face)

Front 23

ASA toxicity (3)

Back 23

1)hypersensitivity
2)acute toxicity (lethal dose is 10-30g, but can survive 100g)
3)leads to metaboic acidosis

Front 24

Treatment of acute ASA toxicity (5)

Back 24

1)induce vomiting
2)oral admin of charcoal
3)if acidotic, Na bicarb is administered to incr blood pH
4)exchange transfusion (infants)
5)hemodialysis (adults)

Front 25

Chronic ASA toxicity? (7)

Back 25

SALICYLISM
a)HA
b)dizziness
c)ringing ears/hard hearing
d)dim vision
e)confusion
f)n/v
g)hyperventilation

Front 26

Pharmacologic Axn of Sulindac (2)

Back 26

1)is a sulfoxide prodrug, metabolized to active sulfide metabolite
2)major axn is anti-inflamm, more potent than ASA

Front 27

Sulindac
a)PK (2)
b)ADR (3)

Back 27

a)rapidly absorbed, half-life is 8hrs
b)thrombocytopenia, agranulocytosis, nephritic syndrome

Front 28

Sulindac therapeutic use (3)

Back 28

1)arthritic conditions
2)inhibits intestinal polyposis
3)inhibit colon cancer

Front 29

Ketorolac pharmacologic effects (3)

Back 29

a)anti-inflamm like other NSAIDs
b)greater analgesic potency
3)can be used w/ opoid and reduces opoid requriement by 25-50%

Front 30

Etodolac pharmacologic effects (3)

Back 30

1)GREATER COX2 SELECTIVITY THAN MOST OTHER NON-SPECIFIC NSAIDS***
2)analgesic and anti-inflamm
3)some uricosuric activity

Front 31

Proprionic Derivatives (6)

Back 31

1)ibuprofen (prototype)
2)fenoprofen
3)flurbiprofen
4)ketoprofen
5)naproxen
6)oxaprozin

Front 32

Pharmacological effects of proprionics (3)

Back 32

Analgesia, antipyresis, anti-inflamm similar to ASA

Front 33

Proprionic therapeutic uses (3)

Back 33

1)arthritis (general)
2)analgesia
3)dysmenorrhea

Front 34

Oxicams ex (2)

Back 34

1)piroxicam (feldene) (prototype)
2)meloxicam

Front 35

Pharmcological effects of oxicams (3)

Back 35

1)anti-inflamm, analgesia, antipyresis
2)non selective COX inhibitor
3)inhibits WBC migration & inhibits oxygen free radical production = increased anti-inflammatory

Front 36

PK of Oxicams (1)

Back 36

1)45-72hr half-life due to enterohepatic recycling

Front 37

Therapeutic uses of oxicams (4)

Back 37

1)long-term treatment of arthritic conditions
2)postop pain
3)acute muscle pain
4)gout

Front 38

Naphtylalkones ex

Back 38

a)nabumetone (relafen) (prototype)

Front 39

Pharmacological effects of Naphtylalkones (3)

Back 39

1)anti-inflamm, antipyresis, analgesia
2)prodrug (produces a longer half life)
3)no real adv over other NSAIDs

Front 40

Therapeutic uses of Naphtylalkones (2)

Back 40

1)arthritic conditions
2)acute pain

Front 41

Fenamates ex (2)

Back 41

1)meclofenamate (prototype)
2)mefenamic acid

Front 42

Fenamates pharmacological effects (3)

Back 42

1)anti-inflamm, analgesia, antipyretic
2)non-selective COX inhibitor
3)ALSO inhibits PLA2

Front 43

Fenamates therapeutic uses (2)

Back 43

1)short term treatment of arthritis and acute pain
2)should NOT be used for more than 1 week

Front 44

Celecoxib therapeutic uses (2)

Back 44

1)RA/OA if pt experiences GI problems w/ other NSAIDS
2)reduces occurrence of colon polyps

Front 45

T/F?
a)ASA was first drug used therapeutically to treat pain and inflammation
b)COX1 is found primarily in areas of inflammation
c)Sulindac is a prodrug that is metabolized to an active metabolite
d)NSAIDs produce an antipyretic effect by enhancing peripheral blood flow

Back 45

a)F
b)F
c)T
d)T

Front 46

T/F?
a)Morphine has a lower potency and a greater efficacy than ASA
b)APAP is a COX3 inhibitor
c)Etodolac has much longer therapeutic duration of action than Piroxicam
d)Celebrex has been shown to inrease the occurrence of colon polyps

Back 46

a)F
b)T
c)F
d)F

Front 47

Morphine structural features (4)

Back 47

1)A,B,C,D,E rings
2)1 phenolic OH
3)D ring is a piperidine ring making it basic (forming salts)
4)ring C is L-cyclic (one double bond)

Front 48

MorphinAN difference from morphine (2)

Back 48

1)NO E RING
2)loss on NONphenolic OH

Front 49

Morphine is based on...

Back 49

Phenanthrene

Front 50

Narcotic def.

Back 50

binds centrally to relieve constant chronic pain

Front 51

4 different opoid receptors (and which 2 do narcotics bind to)

Back 51

1)mu***
2)kappa***
3)delta
4)sigma

Front 52

Codeine is...

Back 52

3-methoxy morphine

Front 53

DXM is..

Back 53

3-methoxy derivative of (+)dextro-levorphanol

Front 54

4 most important things in opoid structure (and which is not so necessary)

Back 54

1)ring D
2)ring A
3)N
4)phenolic OH (not so necessary)

Front 55

Benzomorphans difference from morphine?

Back 55

NO ring C/E

Front 56

4-phenylpiperidines
a)difference from morphine
b)2 ex

Back 56

a)A/D ring only
b1)axial-4-phenyl
b2)equatorial-4-phenyl

Front 57

Methadone difference from morphine (3)

Back 57

1)no piperidine ring
2)ring folds to make a pseudopiperidine ring
3)has a dimethyl amino

Front 58

What is heroin? and why so addictive

Back 58

3-6 acetyl morphine

nonpolar so goes strait to brain

Front 59

Meperidine
a)difference from morphine
b)typical use

Back 59

a)4-phenyl piperidine ESTER
b)short acting analgesic commonly used in child birth

Front 60

Pentazocine difference from morphine (3)

Back 60

a)benzomorphone
b)A,B,D rings only
c)has dimethylallyl group

Front 61

dimethylallyl group fxn

Back 61

imparts agonist/antagonist effects

Front 62

Fentanyl properties (2)

Back 62

1)anilido/aniline group
2)80x more potent than morphine