NSAIDs Flashcards

(43 cards)

1
Q

COX-1

A

Enzyme that produce prostaglandins that are important for general housekeeping function of gastric protection and hemostasis

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2
Q

COX-2

A

Inducible form of the enzyme

Prostaglandins that mediate pain, inflammation, fever and carcinogenesis

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3
Q

Key mediator of both peripheral and central pain sensitization

A

PG-E2

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4
Q

Effect of PG

A

Increase release of Sub. P and glutamate (1ON)
Increase sensitivity of 2ON
Decrease NT from descending pain modulating pathways

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5
Q

NSAID general MoA

A

Competitive inhibitor of COX

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6
Q

Duration of NSAID relates directly to

A

Metabolism of the drug

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7
Q

Hyperalgesia

A

Exaggerated pain response to normally painful stimulus

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8
Q

Allodynia

A

Painful response to a typically non-painful stimulus

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9
Q

Areas where COX-2 is constitutively expressed

A

Kidney
Bone
Brain
Reproductive organ

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10
Q

Side effect of NSAIDs

A

Platelet dysfunction
GI ulceration
Risk of nephrotoxicity
Hypertension

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11
Q

Contraindications of NSAIDs and COX-2 selective inhibitor

A

Hypersensitivity

Triad of Asthma, aspirin and nasal polyposis

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12
Q

Contraindications for COX-2 inhibitors

A

Allergy to sulfonamides

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13
Q

NSAID with no/little anti inflammatory and anti platelets effect

A

Paracetamol

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14
Q

MoA of Paracetamol

A

Inhibition of central COX-3 in CNS
Modulation of descending inhibitory serotonergic pathway
Act on opioid and NMDA receptor

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15
Q

Effect of Salicylates on Respiration

A

Increase O2 consumption
Increase CO2 production
Increase respiration

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16
Q

MDD of Paracetamol

A

4gm

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17
Q

DOA of Paracetamol

A

2 hours

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18
Q

Dosage of Paracetamol

A

0.5-1 gm/4-6 hrs

19
Q

Dosage of Salicylate

A

0.5-1 gm/4-6 hrs

20
Q

DOA of Salicylates

21
Q

MDD of Salicylates

22
Q

Effect of Salicylates on CVS

A

Cardioprotective effect <100mg

Salt and water retention&raquo_space; increased CO

23
Q

Contraindications of Salicylates against bleeding time

A

Hypoprothrombinemia
Severe hepatic damage
Vit K deficiency
Haemophilia

24
Q

Contraindications of Salicylates in third trimester because

A

Prolonged gestation
Complicated deliveries
Premature closure of ductus arteriosus

25
Excretion of Salicylates
Free salicylates 10% | Metabolites 90%
26
Urine pH dependecy of Salicylates excretion
Alkaline urine - 30% | Acidic urine - 2%
27
Toxicity of Salicylates
Hearing impairment Blurred vision Light-headedness
28
Use of Ketrolac
Short-term pain management | Immediate postop period
29
Ketorolac (Vs Morphine)
Less dosage Similar onset to morphine Longer DOA
30
Use of Ketorolac
Patient at high risk for postoperative respiratory depression or emesis
31
Pre-admission of Ketorolac
Hypovolemia should be corrected
32
Effect of Ketorolac on CNS
Minimal effect | Does not cross BBB to significant degree
33
Side effect of Ketorolac
Inhibit platelet aggregation Prolong bleeding Long term use may lead to renal toxicity
34
Contraindication of Ketorolac
Aspirin or NSAID allergy | Triad (AAP)
35
Most commonly used NSAID in Europe
Diclofenac
36
DOA of Diclofenac
8hrs
37
Property of Diclofenac
Preferentially COX-2 inhibitor High first pass effect Accumulate in synovial fluid
38
Use of Diclofenac
Long-term symptomatic treatment of RA and OA Short-term treatment of acute musculoskeletal pain, post-op pain, dysmenorrhea Cataract Extraction
39
Side effect of Diclofenac
Modest, reversible elevation of hepatic transaminase
40
Property of Indomethacin
More potent inhibitor of COX than aspirin Central and peripheral anti-inflammatory action Excellent oral bioavailability
41
Use of Indomethacin
Acute gouty arthritis RA OA Closure of PDA
42
Side effect of Indomethacin
Diarrhea PUD Acute pancreatitis Hepatitis
43
Which NSAID has inhibitory effect on leukocyte function
Ibuprofen