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Pharm > Analgesics and NSAIDs > Flashcards

Analgesics and NSAIDs Flashcards

1
Q

Which drugs are used for pain? (3)

A

-narcotic / opioid analgesics
Non opioid:
-paracetamol
-NSAIDs

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2
Q

Which drugs are anti-inflammatory? (2)

A
  • NSAIDs

- Steroids

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3
Q

cellular mediators of inflammation, pain and thermoregulation can…: (6)

A
  • promote microcirculation blood flow
  • increase permeability
  • enhance action of other mediators
  • sensitize nerve endings
  • promote leukocyte infiltration
  • pro-platelet aggreagtion
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4
Q

What is the mechanism of action for NSAIDs?

A

-nonselective inhibitor for COX-1 and COX-2 isoenzymes

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5
Q

Is the mechanism of action for NSAIDs reversible?

A
  • competitively reversible
  • varying degrees of reversibility
  • EXCEPT asprin (irreversible)
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6
Q

Which NSAID is irreversible?

A

aspirin

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7
Q

What does the COX enzyme do? (3)

A

arachidonic acid–> prostaglandins + thromboxane

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8
Q

Where is arachidonic acid derived from? with what enzyme?

A

From phospholipid bilayer

-enzyme: phospholipase A2

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9
Q

What do prostaglandins do?(2)

A
  • messenger in process of inflammation

- protection of stomach lining

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10
Q

What do steroids inhibit?

A

ENZ phospholipase A2

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11
Q

What do NSAIDs inhibit?

A

ENZ Cyclooxygenase (COX)

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12
Q

What are the derivatives of arachidonic acid? What enzymes produce them? (5)

A

COX enz:

  • prostaglandins + thromboxane
  • collectively called cyclic endoperoxides

5-lipooxygenase ENZ:
-leukotrienes

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13
Q

What are prostaglandins + thromboxane collectively called?

A

cyclic endoperoxides

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14
Q

inhibiting COX produces what therapeutic effects? (2)

A
  • reduces inflammation

- reduces pain

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15
Q

What is the COX-1 expression?

A

constitutively (always) expressed

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16
Q

What are the derivatives of arachidonic acid called?

A

eicosanoids

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17
Q

what functions do COX-1 facilitate? (3)

A
  • protection of stomach lining
  • maintenance of renal function
  • differentiation of marcophages
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18
Q

What is the COX-1 expression?

A

facultatively (when needed)

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19
Q

COX-1 inhibition produces..

A

side effects

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20
Q

COX-2 inhibition produces…

A

desirable NSAID effects

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21
Q

COX-2 functions facilitated? (4)

A
  • inflammation
  • pain
  • fever
  • normal/pathologic cell proliferation
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22
Q

COX-2 inhibition effects?

A

anti-inflammatory

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23
Q

discovery of COX2 led to the research of…

A

development of selective COX-2 inhibitors without gastric problems (characteristic of older NSAIDs)

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24
Q

What are the drug classes of the analgesics and antipyretics that are not NSAIDS?

A
  • paraaminophenols

- pyraolones

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25
Q

What are the classes of drugs that are NSAIDs (10)

A
  • pyrazolones
  • salycilates
  • propionic acid derivatives
  • acetic acid derivatives
  • antranilic acid derivatives
  • oxicams
  • nicotinics
  • others
  • selective cox-2 inhibitors
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26
Q

which COX drugs do NOT produce gastric problems?

A

COX-2 (?)

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27
Q

What are the ParaAminoPhenol drugs?(2)

A
  • acetaminophen (paracetamol)

- propacetamol

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28
Q

What are the pyrazolones? (3)

A
  • propyphenazone
  • metamizole (dypirone)
  • phenylbutazone
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29
Q

What do the non-selective COX-2 inhibitors inhibit?

A
  • cox 1

- cox 2

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30
Q

Which are the non-selective COX 2 inhibitors?

A
  • acetylsalicyclic acid (aspirin)
  • salycilates (sulfasalazine + salicylamide)
  • pyrazolones (phenylbutazone)
  • proionic acid derivatives (ibuprofen. sulindac, ketrolac, diclofenac, aceclofenac)
  • PHENAMATES-ANTHRANILIC ACID
  • oxicams (piroxicam, meloxicam, lornoxicam)
  • nicotinic (Clonixinate lysine, niflumic aicd)
  • other (nabumetone, nimesulide)
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31
Q

What are the selective cox-2 inhibitors? (4)

A
  • only inhibit COX-2
  • CELECOXIB (Celebrex®)
  • ROFECOXIB (Vioxx ®)
  • ETORICOXIB (Arcoxia®, Exxiv®)
  • PARECOXIB (Dynastat®)
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32
Q

What are the classes of anti-inflammatory drugs? (3)

A
  • steroids
  • nonselective cox inhibitors
  • selective cox inhibitors
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33
Q

What are the types of salicylate drugs? (2)

A
  1. acetylsalicyclic acid

2. Salicyclic acid derivatives

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34
Q

What are the acetylsalicyclic acid drugs? (2)

A
  • ASA aspirin

- Lysine acetylsalicylate (IV)

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35
Q

which acetylsalicyclic acid is used with IV?

A

Lysine acetylsalicylate

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36
Q

What are the salicyclic acid derivatives? (4)

A
  • Diflunisal
  • Sulfasalazine (Rheumatoid arthritis, Inflammatory bowel disease)
  • Fosfosal
  • Salsalate
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37
Q

Which salicyclic acid derivative is used for rheumatoid arthritis?

A

Sulfasalazine

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38
Q

Which salicyclic acid derivative is used forInflammatory bowel disease?

A

Sulfasalazine

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39
Q

SALICYLATES indications? (4)

A
  • analgesic
  • antipyretic
  • anti-inflamatory
  • anti-platelet
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40
Q

Are people allergic to salicylates?

A

yes

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41
Q

Side effects of salicylates? (3)

A
  • Gastric irritation-peptic ulcer
  • Hypersensitivity or allergic reactions
  • Increased risk of bleeding
  • Reye syndrome (in children younger than 12 years old with fever) + Liver disease + Encephalopathy
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42
Q

SALICYLATES interactions?

A

-oral anticoagulants (incr. bleeding)

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43
Q

Why do oral anticoagulants increase risk of bleeding with salicylates? (3)

A
  • ulcerogenic properties
  • competition of plasma protein binding (both have high affinity)
  • inhibition of platelet aggregation
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44
Q

When a patient is taking oral anticoagulants, what is the analgesic of choice?

A

acetaminophen/paracetamol

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45
Q

Conraindications for salicylates?

A
  • allergic to them
  • asthmatics
  • patients w/anticoagulants
  • pregnancy (esp. 3rd trimester)
  • patients w/peptic ulcer disease
  • patients w/ chronic renal failure
  • children under 12 with viral infections
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46
Q

What happens if children under age 12 with a viral infection take salicylates?

A

-reye syndrome

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47
Q

In which trimester of pregnancy is it esp. risky to take salicylates?

A

third

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48
Q

Para-aminophenols have which 2 effects? what do they NOT do? (4)

A
  • analgesic
  • antipyretic

NO anti-inflammatory
NO antiplatelet

49
Q

What is the difference between paraceatamol and propacetamol?

A

propacetamole is:

  • prodrug (inactive needs to be metabolized)
  • IV
50
Q

Para-aminophenols are toxic at what dose? what type of toxicity?

A
  • hepatotoxic

- 15 grams

51
Q

What is the antidote for Para-aminophenols poisoning?

A

Acetylcysteine IV

52
Q

What drug can cause fulminant acute hepatitis? what dose?

A

paracetamol

-150-250mg/kg in a few hours

53
Q

Para-aminophenols are used for:

A
  • children
  • patients w/ gastroduodenal ulcer
  • when ASA produces gastric distress
  • patients with allergies (esp. ASA)
  • anti-coagulated patients or w/bleeding disorders
  • pregnancy
54
Q

Para-aminophenols side effects at normal doses?

A

none

55
Q

What pyrazolones have analgesic and antipyretic effects?

A

-DIPYRONE=METAMIZOL -PROPYPHENAZONE

56
Q

What is the specific analgesic effect for DIPYRONE + PROPYPHENAZONE

A

-moderate and visceral pain

57
Q

define URICOSURIC

A

increase the excretion of uric acid in the urine

58
Q

What pyrazolone has analgesic, antiinflamatory and uricosuric effects?

A

phenylbutazone

59
Q

What effects does phenylbutazone have? what type of drug is it? (4)

A
  • is a pyrazolone
  • analgesic
  • anti-inflam
  • uricosuric
60
Q

What is the benefit of pyrazolones?

A
  • less harmful effects to the GI mucosa

- no bleeding complications

61
Q

Which analgesic is useful in colic pain? how? (5)

A
  • metamizol
  • relaxation of smooth muscle
  • can be used alone or with anticholinergics or spasmolytic drugs
62
Q

What drugs can metamizol be used with to help with colic pain? (3)

A
  • alone
  • anticholinergics
  • spasmolytic drugs

ex. Nolotil compositum® = metamizol + butylscopolamine

63
Q

Adverse reactions of dipyrone-metamizol? (2)

A
  • agranulocytosis

- aplastic anemia

64
Q

Which analgesic is not commercially available in most countries but used widely in spain?

A

-dipyrone-metamizol

65
Q

Which drugs are the propionic acid derivatives? (6)

A
  • Ibuprofen
  • Dexibuprofen
  • Naproxen
  • Ketoprofen
  • Dexketoprofen
  • Flurbiprofen
66
Q

What are the pharmacological effects of acetic acid derivatives? (3)

A
  • potent anti-inflam
  • analgesic (moderate pain)
  • antipyretic
67
Q

What type of analgesic effect do acetic acid derivatives have?

A

moderate pain

68
Q

What are the three types of acetic acid derivatives?

A
  • indolacetic
  • pirrolacetic
  • phenyllacetic
69
Q

What are indolacetics acetic acid derivatives? (2)

A
  • acetic acid derivatives

- drug: indomethacin

70
Q

What is indomethacin used for? (2)

A
  • arthritis rheumatoid

- more frequent side effects

71
Q

What are the pirrolacetic acetic acid derivatives?(4)

A
  • ETODOLAC
  • SULINDAC
  • KETOROLAC
  • TOLMETIN
72
Q

describe ketorolac (3)

A
  • acetic acid derivative
  • Significant analgesic potency
  • High risk of gastrointestinal adverse effects
73
Q

What are the phenylacetic acetic acid derivatives? (2)

A
  • DICLOFENAC

- ACECLOFENAC

74
Q

Describe the phenamates-antranilic acid derivatives (3)

A
  • anti-inflam
  • little relevance
  • little use in clinical routine
75
Q

What are the phenamates-antranilic acid derivatives? (4)

A
  • MEFENAMIC ACID
  • FLUFENAMIC ACID
  • MECLOFENAMIC ACID
  • TOLFENAMIC ACID
76
Q

What is another name for enolic acid derivatives?

A

oxicams

77
Q

What is the effect of oxicams?

A
  • anti-inflam
  • analgesic
  • antipyretic
78
Q

What are the oxicam drugs? (4)

A
  • PIROXICAM
  • TENOXICAM
  • MELOXICAM
  • LORNOXICAM
79
Q

Which oxicam has a greater selectivity for inhibiting COX2?

A

MELOXICAM

80
Q

Which oxicam is used as a hospital diagnosis drug?

A

PIROXICAM

81
Q

Side effect of oxicams?

A

Greater risk of gastrointestinal adverse effects

82
Q

What is the dosing for oxicams?

A

Prolonged half-life: single daily dose

83
Q

What drug is classified as other for the NSAIDs?

A

Nabumetone

84
Q

Describe Nabumetone (2)

A

-It is used in musculoskeletal processes of moderate
intensity
-Rarely used in Spain

85
Q

Name the selective cox inhibitor drugs (3)

A

CELECOXIB

PARECOXIB ETORICOXIB

86
Q

What are the selective cox-2 inhibitor indications (3)

A
  • rheumatoid arthritis
  • gouty arthritis
  • osteoarthritis
87
Q

Selective cox-2 inhibitor contraindications? (2)

A
  • ischemic heart disease

- stroke

88
Q

What is the benefit of Cox2 inhibitors?

A

less gastric lesions

89
Q

Side effects of cox 2 inhibitors? (2)

A
  • cardiovascular mortality

- due to thombotic events

90
Q

NSAID administration? (4)

A
  • oral = most common
  • rectal (erractic)
  • parenteral
  • sublingual
91
Q

NSAID bioavailability?

A

80-100%

92
Q

NSAID half life? (2)

A

2-5 hrs

exception: oxicams 24hrs

93
Q

Which NSAID has a longer half life than normal?

A

oxicams -24hrs

94
Q

What is the plasma protein binding percentage for NSAIDs

A

99%

95
Q

NSAIDs metabolism?

A

hepatic preferably

96
Q

NSAID excretion? (2)

A
  • renal

- non-acitve form

97
Q

What causes the anti-inflam effect with NSAIDs?

A

decrease of Thromboxane & prostaglandin

98
Q

What causes the analgesic effect with NSAIDs?

A

decrease of prostaglandins for moderate pain

99
Q

What causes the antipyretic effect with NSAIDs?

A

prostaglandin decrease in CNS

100
Q

What causes antiplatelet action in NSAIDs? (3)

A
  • Not shared by all NSAIDs
  • IRREVERSIBLE INHIBITION (ASA)
  • Decrease of platelet TXA2
101
Q

What causes uricosuric action in NSAIDs? (3)

A
  • Not shared by all NSAIDs
  • high dose of aspirin + phenylbutazone
  • Inhibition uric acid reabsoption
102
Q

NSAIDs local effect on the GI mucosa depends on…? (2)

A
  • ph

- varies with the preparation used

103
Q

NSAIDs systemic effect depends on?

A
  • less specific of the preparation used
  • inhibiting COX = decrease PG
  • PGE2 - protecting gastric mucosa
104
Q

What do NSAIDs do to the kidney? (4)

A
  • synthesis of PGE2 and PGI2 in kidney
  • regulate glomerular filtration & renal plasmatic flow
  • vasodilation
  • incr. PG synthesis when renal perfusion compromised
105
Q

What do NSAIDs do to the uterus? (3)

A
  • decrease of PG synthesis
  • Decrease the contractility
  • Reduce the pain in the uterus
106
Q

NSAID indications (8)

A 
1.- Inflammatory processes
(E.g. Dental inflammation)
2. - Rheumatic Diseases
3. - Metabolic arthritis (e.g. Gout)
4. - PAIN MILD / MODERATE
(Especially pain + inflammation)
5. - FEVER
6. - Dysmenorrhea
7. - HEADACHE
8. - Antiplatelet (E.g.. After acute myocardial infarction, low doses of ASA)
107
Q

Which drug produces the greatest number of adverse reactions?

A

NSAIDs

108
Q

Which drugs represent over 20% of adverse drug reactions?

A

NSAIDs

109
Q

NSAID adverse reactions (7)

A
  1. Gastrointestinal
  2. Hepatic
  3. Renal
  4. Hematological 5. Skin
  5. Hypersensitivity 7. Cardiovascular
110
Q

The most frequent adverse reactions with NSAIDs is… why?

A
  • GASTROINTESTINAL

- decrease in PG synthesis

111
Q

What are the GI adverse effects? (7)

A

Mild:

  • dyspepsia
  • epigastralgia
  • vomiting

Severe:

  • gastric/duodenal erosion
  • gastric ulcer
  • GI bleeding
  • gastric perforation
112
Q

How frequent is it to get gastric peptic ulcers with NSAIDs?

A

5-25%

113
Q

Which NSAIDs are the most ulcerogenic? (4)

A

ASA
OXICAMS
KETOROLAC
INDOMETHACIN

114
Q

Which analgesic is not ulcerogenic?

A

paracetamol

115
Q

Risk factors for GI adverse effects with nsaids (5)

A
  • nsaids or steroids
  • women
  • tobacco
  • caffiene
  • alcohol
116
Q

GI NSAID prophylaxis (3)

A
  • omeprazole
  • anti H2
  • low doses of paracetamol or ibuprofen instead of other NSAIDs
117
Q

NSAIDs and cardiovascular adverse effects: (3)

A
  • incr. bp
  • thrombotic events (myocardial infarction, angina, stroke)
  • HF (palpitations, edema of lower limbs)
118
Q

What causes NSAIDs cardiovascular adverse effects?

A

COX 2 inhibition

119
Q

Which NSAIDs produce more cardiovascular side effects? (4)

A
  • coxibs
  • diclofenac
  • aceclofenac
  • high doses of ibuprofen

Pharm (14 decks)

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