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Analgesics and NSAIDs Flashcards

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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
What are the classes of drugs that are NSAIDs (10)
- pyrazolones - salycilates - propionic acid derivatives - acetic acid derivatives - antranilic acid derivatives - oxicams - nicotinics - others - selective cox-2 inhibitors
26
which COX drugs do NOT produce gastric problems?
COX-2 (?)
27
What are the ParaAminoPhenol drugs?(2)
- acetaminophen (paracetamol) | - propacetamol
28
What are the pyrazolones? (3)
- propyphenazone - metamizole (dypirone) - phenylbutazone
29
What do the non-selective COX-2 inhibitors inhibit?
- cox 1 | - cox 2
30
Which are the non-selective COX 2 inhibitors?
- 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)
31
What are the selective cox-2 inhibitors? (4)
* only inhibit COX-2 - CELECOXIB (Celebrex®) - ROFECOXIB (Vioxx ®) - ETORICOXIB (Arcoxia®, Exxiv®) - PARECOXIB (Dynastat®)
32
What are the classes of anti-inflammatory drugs? (3)
- steroids - nonselective cox inhibitors - selective cox inhibitors
33
What are the types of salicylate drugs? (2)
1. acetylsalicyclic acid | 2. Salicyclic acid derivatives
34
What are the acetylsalicyclic acid drugs? (2)
- ASA aspirin | - Lysine acetylsalicylate (IV)
35
which acetylsalicyclic acid is used with IV?
Lysine acetylsalicylate
36
What are the salicyclic acid derivatives? (4)
- Diflunisal - Sulfasalazine (Rheumatoid arthritis, Inflammatory bowel disease) - Fosfosal - Salsalate
37
Which salicyclic acid derivative is used for rheumatoid arthritis?
Sulfasalazine
38
Which salicyclic acid derivative is used forInflammatory bowel disease?
Sulfasalazine
39
SALICYLATES indications? (4)
- analgesic - antipyretic - anti-inflamatory - anti-platelet
40
Are people allergic to salicylates?
yes
41
Side effects of salicylates? (3)
- 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
42
SALICYLATES interactions?
-oral anticoagulants (incr. bleeding)
43
Why do oral anticoagulants increase risk of bleeding with salicylates? (3)
- ulcerogenic properties - competition of plasma protein binding (both have high affinity) - inhibition of platelet aggregation
44
When a patient is taking oral anticoagulants, what is the analgesic of choice?
acetaminophen/paracetamol
45
Conraindications for salicylates?
- 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
46
What happens if children under age 12 with a viral infection take salicylates?
-reye syndrome
47
In which trimester of pregnancy is it esp. risky to take salicylates?
third
48
Para-aminophenols have which 2 effects? what do they NOT do? (4)
- analgesic - antipyretic NO anti-inflammatory NO antiplatelet
49
What is the difference between paraceatamol and propacetamol?
propacetamole is: - prodrug (inactive needs to be metabolized) - IV
50
Para-aminophenols are toxic at what dose? what type of toxicity?
- hepatotoxic | - 15 grams
51
What is the antidote for Para-aminophenols poisoning?
Acetylcysteine IV
52
What drug can cause fulminant acute hepatitis? what dose?
paracetamol | -150-250mg/kg in a few hours
53
Para-aminophenols are used for:
- children - patients w/ gastroduodenal ulcer - when ASA produces gastric distress - patients with allergies (esp. ASA) - anti-coagulated patients or w/bleeding disorders - pregnancy
54
Para-aminophenols side effects at normal doses?
none
55
What pyrazolones have analgesic and antipyretic effects?
-DIPYRONE=METAMIZOL -PROPYPHENAZONE
56
What is the specific analgesic effect for DIPYRONE + PROPYPHENAZONE
-moderate and visceral pain
57
define URICOSURIC
increase the excretion of uric acid in the urine
58
What pyrazolone has analgesic, antiinflamatory and uricosuric effects?
phenylbutazone
59
What effects does phenylbutazone have? what type of drug is it? (4)
* is a pyrazolone - analgesic - anti-inflam - uricosuric
60
What is the benefit of pyrazolones?
- less harmful effects to the GI mucosa | - no bleeding complications
61
Which analgesic is useful in colic pain? how? (5)
- metamizol - relaxation of smooth muscle - can be used alone or with anticholinergics or spasmolytic drugs
62
What drugs can metamizol be used with to help with colic pain? (3)
- alone - anticholinergics - spasmolytic drugs ex. Nolotil compositum® = metamizol + butylscopolamine
63
Adverse reactions of dipyrone-metamizol? (2)
- agranulocytosis | - aplastic anemia
64
Which analgesic is not commercially available in most countries but used widely in spain?
-dipyrone-metamizol
65
Which drugs are the propionic acid derivatives? (6)
- Ibuprofen - Dexibuprofen - Naproxen - Ketoprofen - Dexketoprofen - Flurbiprofen
66
What are the pharmacological effects of acetic acid derivatives? (3)
- potent anti-inflam - analgesic (moderate pain) - antipyretic
67
What type of analgesic effect do acetic acid derivatives have?
moderate pain
68
What are the three types of acetic acid derivatives?
- indolacetic - pirrolacetic - phenyllacetic
69
What are indolacetics acetic acid derivatives? (2)
- acetic acid derivatives | - drug: indomethacin
70
What is indomethacin used for? (2)
- arthritis rheumatoid | - more frequent side effects
71
What are the pirrolacetic acetic acid derivatives?(4)
- ETODOLAC - SULINDAC - KETOROLAC - TOLMETIN
72
describe ketorolac (3)
- acetic acid derivative - Significant analgesic potency - High risk of gastrointestinal adverse effects
73
What are the phenylacetic acetic acid derivatives? (2)
- DICLOFENAC | - ACECLOFENAC
74
Describe the phenamates-antranilic acid derivatives (3)
- anti-inflam - little relevance - little use in clinical routine
75
What are the phenamates-antranilic acid derivatives? (4)
- MEFENAMIC ACID - FLUFENAMIC ACID - MECLOFENAMIC ACID - TOLFENAMIC ACID
76
What is another name for enolic acid derivatives?
oxicams
77
What is the effect of oxicams?
- anti-inflam - analgesic - antipyretic
78
What are the oxicam drugs? (4)
- PIROXICAM - TENOXICAM - MELOXICAM - LORNOXICAM
79
Which oxicam has a greater selectivity for inhibiting COX2?
MELOXICAM
80
Which oxicam is used as a hospital diagnosis drug?
PIROXICAM
81
Side effect of oxicams?
Greater risk of gastrointestinal adverse effects
82
What is the dosing for oxicams?
Prolonged half-life: single daily dose
83
What drug is classified as other for the NSAIDs?
Nabumetone
84
Describe Nabumetone (2)
-It is used in musculoskeletal processes of moderate intensity -Rarely used in Spain
85
Name the selective cox inhibitor drugs (3)
CELECOXIB | PARECOXIB ETORICOXIB
86
What are the selective cox-2 inhibitor indications (3)
- rheumatoid arthritis - gouty arthritis - osteoarthritis
87
Selective cox-2 inhibitor contraindications? (2)
- ischemic heart disease | - stroke
88
What is the benefit of Cox2 inhibitors?
less gastric lesions
89
Side effects of cox 2 inhibitors? (2)
- cardiovascular mortality | - due to thombotic events
90
NSAID administration? (4)
- oral = most common - rectal (erractic) - parenteral - sublingual
91
NSAID bioavailability?
80-100%
92
NSAID half life? (2)
2-5 hrs | exception: oxicams 24hrs
93
Which NSAID has a longer half life than normal?
oxicams -24hrs
94
What is the plasma protein binding percentage for NSAIDs
99%
95
NSAIDs metabolism?
hepatic preferably
96
NSAID excretion? (2)
- renal | - non-acitve form
97
What causes the anti-inflam effect with NSAIDs?
decrease of Thromboxane & prostaglandin
98
What causes the analgesic effect with NSAIDs?
decrease of prostaglandins for moderate pain
99
What causes the antipyretic effect with NSAIDs?
prostaglandin decrease in CNS
100
What causes antiplatelet action in NSAIDs? (3)
- Not shared by all NSAIDs - IRREVERSIBLE INHIBITION (ASA) - Decrease of platelet TXA2
101
What causes uricosuric action in NSAIDs? (3)
- Not shared by all NSAIDs - high dose of aspirin + phenylbutazone - Inhibition uric acid reabsoption
102
NSAIDs local effect on the GI mucosa depends on...? (2)
- ph | - varies with the preparation used
103
NSAIDs systemic effect depends on?
- less specific of the preparation used - inhibiting COX = decrease PG - PGE2 - protecting gastric mucosa
104
What do NSAIDs do to the kidney? (4)
- synthesis of PGE2 and PGI2 in kidney - regulate glomerular filtration & renal plasmatic flow - vasodilation - incr. PG synthesis when renal perfusion compromised
105
What do NSAIDs do to the uterus? (3)
- decrease of PG synthesis - Decrease the contractility - Reduce the pain in the uterus
106
NSAID indications (8)
``` 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
Which drug produces the greatest number of adverse reactions?
NSAIDs
108
Which drugs represent over 20% of adverse drug reactions?
NSAIDs
109
NSAID adverse reactions (7)
1. Gastrointestinal 2. Hepatic 3. Renal 4. Hematological 5. Skin 6. Hypersensitivity 7. Cardiovascular
110
The most frequent adverse reactions with NSAIDs is... why?
- GASTROINTESTINAL | - decrease in PG synthesis
111
What are the GI adverse effects? (7)
Mild: - dyspepsia - epigastralgia - vomiting Severe: - gastric/duodenal erosion - gastric ulcer - GI bleeding - gastric perforation
112
How frequent is it to get gastric peptic ulcers with NSAIDs?
5-25%
113
Which NSAIDs are the most ulcerogenic? (4)
ASA OXICAMS KETOROLAC INDOMETHACIN
114
Which analgesic is not ulcerogenic?
paracetamol
115
Risk factors for GI adverse effects with nsaids (5)
- nsaids or steroids - women - tobacco - caffiene - alcohol
116
GI NSAID prophylaxis (3)
- omeprazole - anti H2 - low doses of paracetamol or ibuprofen instead of other NSAIDs
117
NSAIDs and cardiovascular adverse effects: (3)
- incr. bp - thrombotic events (myocardial infarction, angina, stroke) - HF (palpitations, edema of lower limbs)
118
What causes NSAIDs cardiovascular adverse effects?
COX 2 inhibition
119
Which NSAIDs produce more cardiovascular side effects? (4)
- coxibs - diclofenac - aceclofenac - high doses of ibuprofen

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