NSAIDs Flashcards

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

A

15-20 min

21
Q

MDD of Salicylates

A

3gm

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
Q

Excretion of Salicylates

A

Free salicylates 10%

Metabolites 90%

26
Q

Urine pH dependecy of Salicylates excretion

A

Alkaline urine - 30%

Acidic urine - 2%

27
Q

Toxicity of Salicylates

A

Hearing impairment
Blurred vision
Light-headedness

28
Q

Use of Ketrolac

A

Short-term pain management

Immediate postop period

29
Q

Ketorolac (Vs Morphine)

A

Less dosage
Similar onset to morphine
Longer DOA

30
Q

Use of Ketorolac

A

Patient at high risk for postoperative respiratory depression or emesis

31
Q

Pre-admission of Ketorolac

A

Hypovolemia should be corrected

32
Q

Effect of Ketorolac on CNS

A

Minimal effect

Does not cross BBB to significant degree

33
Q

Side effect of Ketorolac

A

Inhibit platelet aggregation
Prolong bleeding
Long term use may lead to renal toxicity

34
Q

Contraindication of Ketorolac

A

Aspirin or NSAID allergy

Triad (AAP)

35
Q

Most commonly used NSAID in Europe

A

Diclofenac

36
Q

DOA of Diclofenac

A

8hrs

37
Q

Property of Diclofenac

A

Preferentially COX-2 inhibitor
High first pass effect
Accumulate in synovial fluid

38
Q

Use of Diclofenac

A

Long-term symptomatic treatment of RA and OA
Short-term treatment of acute musculoskeletal pain, post-op pain, dysmenorrhea
Cataract Extraction

39
Q

Side effect of Diclofenac

A

Modest, reversible elevation of hepatic transaminase

40
Q

Property of Indomethacin

A

More potent inhibitor of COX than aspirin
Central and peripheral anti-inflammatory action
Excellent oral bioavailability

41
Q

Use of Indomethacin

A

Acute gouty arthritis
RA
OA
Closure of PDA

42
Q

Side effect of Indomethacin

A

Diarrhea
PUD
Acute pancreatitis
Hepatitis

43
Q

Which NSAID has inhibitory effect on leukocyte function

A

Ibuprofen