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NSAIDs Flashcards

(108 cards)

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1
Q

What does NSAID stand for

A

Non steroidal anti-inflammatory drugs

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2
Q

Define NSAIDs

A

class of drugs that relieve pain, reduce inflammation, redness and swelling and bring down high temperature (fever)

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3
Q

What conditions require NSAIDs

A

Headaches
painful periods
toothaches
sprains and strains inf
common cold /flu
inflammation of the joints (arthritis)

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4
Q

How do NSAIDs work

A

blocking the production of prostaglandins, which are chemical messengers that are responsible for pain / swelling of inflammatory conditions

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5
Q

What is the difference between narcotic analgesics and non-narcotic analgesics

A

Narcotic -> CNS effect
Non-narcotic -> no CNS effect

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6
Q

Most NSAIDs are reversible or irreversible COX inhibitors

A

Most NSAIDs are irreversible cyclooxyrgenase inhibitors
-> prevent formation of prostaglandins -> lowering signs and symptoms of inflammation

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7
Q

What are prostaglandins

A

family of chemicals that are produced by the cells 1. in response to injury/illness
2. prostaglandins promote inflammation/pain/fever
3. Prostaglandins support blood clotting func of platelets
4. prostaglandins protect the lining of the stomach from the effects of acid

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8
Q

What is the chemical structure of prostaglandins

A

Unsaturated carboxylic acids
20 carbon skeleton
+ 5 member ring

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9
Q

Where are prostaglandin biochemically synthesized from

A

Fatty acids, arachidonic acid

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10
Q

Prostaglandins in COX 1 ARE

A

Thromboxane A2

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11
Q

Prostaglandins in COX2 are

A

Prostacyclin PG12

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12
Q

COX 1 is called

A

Constitutive

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13
Q

COX 2 is called

A

inducibile

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14
Q

Salicylates are derived from

A

Salicylic acid (monohydroxybenzoic acid

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15
Q

Salicylic acid is also known as

A

2-hydroxybenzoic acid

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16
Q

Does salicylamide have analgesic and inflammatory action

A

No,
Salicylamide has analgesic but not inflammatory action

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17
Q

In salicylates, the hydroxyl group should be on the ______ position

A

Ortho

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18
Q

T/F: Halogen substitution enhances activity however makes them toxic as well

A

True

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19
Q

In salicylates, substitution with a hydrophobic aryl group at 5 position improves anti inflammatory activity

A

True

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20
Q

Phenacetin is available in united states

A

No

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21
Q

Acetaminophen is an effective analgesic and antipyretic

A

True

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22
Q

Is acetaminophen an anti-inflammatory?

A

No, due to its weak inhibition of cyclooxygenase -> weak inhibition of prostaglandin synthesis

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23
Q

Acetaminophen toxicity

A

Hepatotoxicity -> depletion of glutathione pool

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24
Q

What is the antidote of acetaminophen

A

Acetylcycsteine

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25
When was phenylbutaxone introduced
1949 -> treatment of arthritis although not a first line drug
26
T/F: phenylbutazone is an NSAID effective for treatment of fever, pain and inflammation in the body
True
27
Phenylbutazone has analgesic and antipyretic effects and enhanced antiinflammatory effects -> RA
True
28
Pyrazolone is a drug that has analgesic, anti inflammatory, and anti pyretic properties
True
29
What condition is assosiated with pyrazolone
Leukopenia (low white blood cell count)
30
What is fenamates derived from
N-phenylanthranilic acid
31
What major side effect of fenamates
Diarrhea
32
T/F: Fenamates are N containing analouges of salicylates
True
33
Mefanaic acid is used as
1. Anti-inflammatory 2. arthritis 3. menstrual pain 4. pain after surgical conditions
34
Is mefanamic acid an inhibitor of what type
COX1 AND COX2 competitive inhibitor which are responsibile for the first step of prostaglandin biosynthesis
35
What are heteroaryl acetic acids and propionic acid derivatives used for
RA
36
Is Sulindac a prodrug
Yes
37
In ibuprofen, the S-isomer is more active than the R-isomer
True
38
What was the first member of propionic acid class of NSAIDs to come to general use
Ibuprofen
39
Is naproxen widely used
One of the most widely used NSAIDs
40
Diclofenac is what type of derivative
Phenyl acetic acid derivative
41
Is diclofenac potent?
Yes, it is one of the most potent NSAIDs known clincially
42
What is under the oxicam family
piroxicam meloxicam tenoxicam (under study)
43
Is piroxicam equivalent to aspirin, indomethacin , or naproxen for long term treatment of RA or OA
yes
44
Is there a difference between COX1 AND COX 2
yes, x-ray crystals structure analysis show difference in amino acid sequence
45
What is the difference in structure between COX 1 and COX 2
COX 2 has a smaller valine in the active site COX 1 has a larger isoleucine
46
COX 2 inhibitors lack what
A carbonyl group
47
Simple competitive inhibiton of COX 1 AND COX 2 inhibitors is thought to occur becuase of ...?
Lack of access to the side pocket
48
In COX2 selective drugs, the heterocycles could include
furan pyrrole thiazole oxazole imidazole isoxazole pyrimidine thiophene
49
Coxibs are _______ COX 2 inhibitors
selective
50
What effects do selective COX 2 inhibitors give
antiinflammatory analgesic antipyretic low ulcerogenic potential
51
Primary indication of celecoxib
pt who need long and regular pain relief no advantage for using celecoxib for a short term or acute pain relieve over conventional NSAIDs
52
Prostaglandin inhibition in kidney after using COX2 can affect what
renal blood flow -> retention of water and sodium ( edema) a risk encountered in all NSAIDs except aspirin
53
In order to fight inflammation we either use:
Steroids or NSAIDs
54
Do some NSAIDs target 5-LOX? which ones?
Yes, ibuprofen and indomethacin can inhibit activity of 5-LOX
55
What do we call COX 1 and COX 2
ISOENZYMES identical yet differ in their distripution
56
What is the % identical between COX 1 AND COX 2
99% identical only point mutation -> different selectivity
57
COX 1 is housekeeper which COX 2 is only release in inflammation
True
58
Which has a larger active site? cox 1 or cox 2
COX 2 has a larger active site, due to it containing valine an a.a that is small
59
Since COX 2 has a larger active site, where does large drugs and small drugs fit?
Large drugs -> COX 2 Small drugs -> both COX 1 AND COX 2 (non selective)
60
Salicylic acid is also known as ...?
Vitamin S
61
Is salicylic acid selective?
Non selective because its small
62
Is salicylic acid reversible (not aspirin)
Yes reversibile binding
63
Which is more stable, salicylic acid or ASA
Salicylic acid when ASA degrades -> vinegar smell
64
Which is more acidic, Salicylic acid or ASA
same acidity
65
Is aspirin a prodrug?
No, becuase the ester is active before and after it's broken down
66
Is aspirin reversible
No, Aspirin is irreversible
67
the only NSAID that inhibits clotting of blood for 4-7 days is
Aspirin
68
Why does aspirin have antipyretic activity
because its able to interfere with the production of prostaglandin E1 in the brain
69
At low doses, aspirin is used as
Anti-platelet
70
Does Aspirin reach the brain?
Yes via transporters
71
Aspirin should be stopped how long before surgeries?
A week
72
What are some off-label uses of aspirin
1. shiny hair 2. plant illness (basic soil -> neutralize it)
73
What are side effects of aspirin
1. bleeding 2. stomach ulcer 3. allergy (bronchostriction) 4. reye's syndrome
74
Since all NSAIDs are acids and they must contain COOH, that makes them
irritants
75
What is bufferin
A buffering solution to reduce the COOH irritation to the stomach wall
76
What is Reyes syndrome
if you give a child <16 yr with a viral infection, aspirin Symptoms: 1. swelling of the brain 2. liver dysfunction 3. breathing difficulties 4. fever -> coma
77
Is Aspirin C/I in children with viral infections
Yes, reyes syndrome
78
Is diflunisal reversible
Yes
79
Is diflunisal small/large/selective/nonselective
Small Non selective
80
Which is more potent, aspirin or diflunisal
Aspirin is more potent than diflunisal
81
One of the strongest/most potent NSAIDs
Dicolfenac
82
Is diclofenac used for chronic pain management
NO
83
What is the MAO of diclofenac
blockage of voltage-dependent sodium channels -> freezes the nerve -> no action potential
84
Is diclofenac pure COX 2 inh
no, because its small it can bind to both cox 1 and cox2 bit it prefers cox 2
85
Is diclofenac effective as an antipyretic
Yes
86
Is diclofenac effective against all strains of multi drug resistant E. coli with a MIC of 25 mcg/mL
Yes Drug repurposing
87
The methyl in ibuprofen was orignially an H but they changed it to methyl. why
H -> Hepatotoxic CH3 -> safer
88
What is the painkiller of choice for pregnant woman
Paracetamol avoid in first trimester -> ADHD
89
What is the pain killer of choice for babies
None <3 months 1. no liver dysfunction -> paracetamol 2. ibuprofen
90
Which is more tolerated, ibuprofen or aspirin
Ibuprofen is more tolerated, less GI irritation, reversible COX inhibitor
91
What is the prophylaxic use of ibuprofen
Prophylaxis of alzeheimer and parkinson
92
Is indomethacine reversible?
Yes, reversible COX inhibitor
93
Is indomethacine potent
VERY مرصد
94
What is the indication of using indomethacine
acute gout arthritis (severe pain)
95
Is indomethacine selective
No , least selective among all NSAIDs
96
Is sulindac selective
Not selective. however, more selective than indomethacine
97
Why is naproxen mostly prescribed by dentists
because it distributes to low perfusion tissues like lungs and gum?
98
Is naproxen selective
NO
99
Piroxicam, is it short acting or long acting
Long acting , once daily
100
Does dosing alter selectivity in piroxicam
YES low doses -> COX 2 high doses -> no selectivity
101
How is piroxicam excreted
h.philic -> urine -> dose adjusments in kidney injurt
102
Why does COX 2 have cardiotoxic
inhibiting all COX 2 -> body produced more COX 1 -> INC thromboxane A2 -> INC platelet aggregation
103
What is the black box warning on celecoxib
NOT TO BE GIVEN FOR PATIENTS WITH CARDIOVASCULAR RISK, DM, MI PTS
104
Does acetaminophen have platelet function
No
105
Is acetaminophen an NSAID
NO, but it functions on COX 3 centrally
106
How does acetaminophen reach the CNS knowing that it doesnt have a transporter
it's unionized -> passive diffusion
107
Why does acetaminophen toxicity occur
because acetaminophen already has an OH group, it bypasses phase 1 metabolism in the liver and you suddenly shock the liver with a high amount of acetaminophen ready for phase 2 if the liver does not have enough glucuronic acid needed for conjugation -> acetaminophen accumulation in the liver NAPQI is a very toxic intermediate
108
What is the toxic dose of acetaminophen
up to 4g or up to 1 g in cases of reduced liver function

Medicinal 3 (6 decks)

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