LAB_Anti-Inflam and Analgesics Flashcards

1
Q

a response intended to eliminate the initial cause of cell injury,
remove the damaged tissue, and generate new tissue

A

Inflammation

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2
Q

Cardinal signs of inflammation:

A
  • rubor (redness)
  • tumor (swelling)
  • calor (heat)
  • dolor (pain)
  • functio laesa (loss of function)
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3
Q

Materials needed for inflammatory activity

A
  • Plethysmometer
  • Tuberculin syringes
  • Intubation needles
  • Individual Observation Cages
  • 24 or 26 gauge 1” syringes
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4
Q

Anti-inflamm drugs

A

Diclofenac
Carrageenan

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5
Q

It is a highly sensitive and reproducible test for nonsteroidal antiinflammatory drugs and has long been established as a valid model to
study new anti-inflammatory drugs

A

Carrageenan-Induced Paw Edema

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6
Q

The development of edema induced by carrageenan injection causes
an _____ and ______ inflammatory response

A

acute and local

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7
Q

In the early phase (0-1h), ________, ________, and _________ are
the first mediators involved

A

histamine, serotonin, and bradykinin

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8
Q

In the second phase - ________ and various _______ such as
IL-1β, IL-6, IL-10, and TNF-α are implicated

A

Prostaglandins ; cytokines

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9
Q

Used to suppress the symptoms of inflammation and relieve pain
(analgesic action) and fever (antipyretic action)

A

Non-Steroidal Anti-inflammatory Drugs
(NSAIDS)

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10
Q

Anti-inflammatory effect of nsaids:

A

inhibition of COX-1 and COX-2

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11
Q

NSAID that inhibits COX-1 and COX-2

A

Aspirin

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12
Q

Inhibit COX-2>COX-1

A

COX-2 selective agents

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13
Q

_____ reduce the inflammatory response and pain but not the cytoprotective action of
prostaglandins in the stomach

A

COX-2

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14
Q

Analgesic effect of NSAIDs

A

Inhibition of PGE2 and PGI2

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15
Q

: inhibition of production of prostaglandins induced by IL1 and IL-6 in the hypothalamus and the ‘resetting’ of the thermoregulatory
system leading to vasodilation and increased heat loss

A

Antipyretic effect of NSAIDs

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16
Q

First-line drugs to arrest inflammation and accompanying pain of
rheumatic and non-rheumatic diseases

A

NSAIDs

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17
Q

NSAIDs alleviate __________ pain

A

mild-moderate

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18
Q

T/F: NSAIDs reduce elevated body temperature

A

T

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19
Q

Ibuprofen, fenoprofen, ketoprofen flurbiprofen, oxaprozin, naproxen

A

Propionic acid derivatives

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20
Q

Indomethacin, tolemtin, sulindac, ketorolac

A

Acetic acid derivatives

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21
Q

Piroxicam, tenoxicam

A

Oxicam

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22
Q

Celecoxib, parecoxib etoricoxib

A

Selective Cox-2 Inhibitors

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23
Q

better tolerated than ASA

A

Ibuprofen

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24
Q

Analgesic, antipyretic, anti-inflammatory efficacy less than ASA

A

Ibuprofen

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25
Q

T/F: Ibuprofen is well-absorbed, >90% bound to plasma proteins and cross BBB

A

T

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26
Q

Ibuprofen is metabolized in the ______, excreted in ________

A

liver; bile and kidneys

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27
Q

Ibuprofen dosage forms

A

Oral, parenteral, topical use (gel, cream)

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28
Q

available as patch, capsule, tablet

A

Ketoprofen

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29
Q

used in the eye for anti-inflammatory property

A

Flurbiprofen

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30
Q

longer acting

A

Naproxen

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31
Q

Propionic Acid ADR

A

nausea, vomiting, GI discomfort, fluid retention

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32
Q

This Acetic Acid derivative has analgesic property to relieve postoperative pain

A

Ketorolac

33
Q

Acetic Acid derivative that is a potent anti-inflammatory, agent, antipyretic,
analgesic effect

A

Indomethacin

34
Q

ADR of Indomethacin:

A

headache, dizziness, ataxia, confusion, hallucinations, psychosis,
hypersensitivity reaction

35
Q

CI of Indomethacin

A

renal failure, thrombocytopenia, elevated bilirubin

36
Q

used as closure of PDA, pain in laminectomy, eye drops for inflammation

A

Indomethacin

37
Q

Indomethacin _________ action of furosemide, thiazides, beta blockers, and ACE
inhibitors by salt and water retention ; ____________ bleeding with warfarin

A

decreases; increases

38
Q

weaker actions than others but less toxic, not antagonize
diuretic and antihypertensive actions of thiazides

A

Sulindac

39
Q

are more toxic, contraindicated in children, and not
to be used for more than one week

A

Mefenamic Acid

40
Q

Mefenamic Acid ADR

A

GI side effects (diarrhea)

41
Q

used in analgesic in myalgias, dysmenorrhea

A

Mefenamic Acid

42
Q

good anti-inflammatory activity, more potent,
poorer analgesic and antipyretic activity

A

Phenylbutazone

43
Q

less likely to cause agranulocytosis

A

Azapropazone

44
Q

poor anti-inflammatory agent

A

Metamizol

45
Q

good anti-inflammatory, analgesic and antipyretic
activit

A

Piroxicam

46
Q

similar to Metamizol

A

Propiphenazone

47
Q

significant effect on RA and OA

A

Nabumetone

48
Q

less gastric irritation than piroxicam; preferentially
binds to COX-2

A

Meloxicam

49
Q

preferentially inhibits COX-2, antihistaminic and antallergic properties

A

Nimesulide

50
Q

Acetic acid derivative that is relatively
nonselective COX inhibitor

A

DICLOFENAC

51
Q

DICLOFENAC has a half life of _______;

A

1.9 to 2.3 hours

52
Q

Co-administration of
____________ may increase the toxicity of diclofenac.

A

voriconazole

53
Q

Diclofenac ADE

A

GI ulceration
Elevation of serum aminotransferases

54
Q

Selective COX-2 Inhibitors prototype

A

Celecoxib

55
Q

Celecoxib can cause

A

HTN and edema

56
Q

ADR of Selective Cox 2 inhibitors

A

increase risk for cardiovascular and cerebrovascular thrombotic
events -> increase risk for MI and stroke

57
Q

highly selective for COX-2 and longer acting (given once a day)

A

Etoricoxib

58
Q

Materials included in analgesic activity

A

Hot plate analgesia apparatus
* Weighing scale
* Stopwatches
* Tuberculin syringe

59
Q

a condition of enhanced sensitivity to painful stimu

A

Hyperalgesia

60
Q

Mice treated with test compound -> ______________ latencies to respond
to thermal stimulation compared to mice treated with vehicle.

A

increased

61
Q

Pharmacological test for evaluating the analgesic potential of test
compounds

A

Hot Plate Method

62
Q

Acts peripherally (inhibit COX1 or
COX2)

A

Non- Opioid Analgesics

63
Q

Has ceiling effect

A

Non- Opioid Analgesics

64
Q

Used as analgesic, anti-inflammatory,
antipyretic and antiplatelet

A

Non- Opioid Analgesics

65
Q

Interact with mu, delta, kappa opioid
receptors, act mostly on SC and brain

A

Opioid Analgesics

66
Q

May have a capacity for dependence,
withdrawal and abuse

A

Opioid Analgesics

67
Q

Used as analgesic

A

Opioid Analgesics

68
Q

Does not have analgesic ceiling
effect; dose escalation is limited by
incidence and severity of ADRS

A

Opioid Analgesics

69
Q

Used in moderate to severe pain,
neuropathic pain

A

Opioid Analgesics

70
Q

SE: constipation, nausea, vomiting,
respiratory depression, urinary
retention, withdrawal symptoms

A

Opioid Analgesics

71
Q

SE: GI, renal, cardiovascular (see
previous slides)

A

Non- Opioid Analgesics

72
Q

acute and chronic inflammatory
diseases (eg. RA, OA, gout)

A

Non- Opioid Analgesics

73
Q

relieves pain without loss of consciousness

A

Analgesia

74
Q

T/F: Analgesia alters both perception and reaction to pain

A

T

75
Q

presynaptic inhibition of the reuptake of serotonin
and NE in pain inhibitory pathways

A

Antidepressants

76
Q

: deplete local neurons of Substance P, which is required in
the transmission of nociceptive inpu

A

Capsaicin

77
Q

lowering NT release or reducing neuronal firing

A

Anticonvulsants

78
Q

clock nerve signals that send the feeling of pain
from site of injury to the brain

A

Topical lidocaine