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Pharmacology > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

Function of NSAIDs

A

decr. production of prostaglandins= decr. inflammation, decr. fever, relieve pain

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2
Q

Which are the irreversible COX inhibitors?

A

Aspirin (ASA)

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3
Q

Aspirin is a

A

irreversible inhibitor of COX 1 and COX 2

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4
Q

How is aspirin administered

A

Orally

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5
Q

What kind of enzyme is COX 1

A

is a constitutive enzyme- its always in its active form

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6
Q

What kind of enzyme is COX 2

A

is an inducible enzyme–> it needs to be triggered/turned on in order to perform its function

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7
Q

Prostaglandin responsible for vasodilation

A

PGE2

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8
Q

MOA of aspirin as antiplatelet

A

inhibits COX 1 in platelets
decr. production of thrmboxane A2
Inhibits platelet production of new COX 1=new platelets
decr. COX 1 enzymes
Increased bleeding time w/o affecting PT

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9
Q

MOA of aspirin as anti-inflammatory

A

In liver, aspirin is metabolised into salicylate(anti-inflammatory; no antiplatelet effect)
Salicylate inhibits COX 2
decr. prostaglandin production
decr. inflammation, pain, fever

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10
Q

Indications of aspirin

A

Headaches
Musculoskeletal pain
Short term treatment of chronic pain (e.g. osteoarthritis, rheumatoid arthritis)

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11
Q

Different doses of aspirin cause

A

<300mg/day: antiplatelet
300-2400mg/day: antipyretic and analgesic
>2400mg/day: anti-inflammatory

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12
Q

A/E of aspirin

A

Angioedema
bronchospasm
GI ulceration/bleeding
Hepatotoxicity
Hearing loss
Platelet aggregation inhibition
Pulmonary oedema (non-cardiogenic)

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13
Q

CI of aspirin

A

Aspirin-associated hypersensitivity
Bleeding GI ulcers, PUD; ulcerative collitis
Hemolyic aneamia
Haemophilia
Hemorrhoids
Asthma
Lactation
Chronic diarhoea

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14
Q

PK of aspirirn
Absorption
Distribution
Metabolism
Excretion

A

A: 80-100% (mostly absorbed in ileum)
D: 90-95% protein bound
Metabolism: Liver
E: urine (80-100%), sweat, saliva, feces

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15
Q

Non-selective COX inhibitors function

A

Reversibly inhibits both COX 1 and 2

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16
Q

Name the Non-selective COX inhibitors

A

Ibuprofen
Diclofenac
Indomethacin
Naproxen
Lornoxicam
Flurbiprofen
Ketoprofen
Piroxicam
Mefanamic acid
Fetorolac
Phenazone(antipyrine)

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17
Q

Administration of Non-selective COX inhibitors

A

All taken orally
Parenterally: ketorolac, ibuprofen
Rectal susp: indomethacin
Eye drops: Ketorolac
Ear drops: Phenazone

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18
Q

MOA of Non-selective COX inhibitors

A

Reversibly inhibit COX 1: decr. thromboxane production–> inhibition of platelet aggregation;transient
Reversibly inhibit COX 2: decr. prostaglandin production–> decr. inflammation, pain, fever

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19
Q

Indications of Ibuprofen

A

Analgesia
Inflammation (high dose required)
Ductus arteriosus in premature babies (IV)

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20
Q

CI of Ibuprofen

A

Hypersensitivity to aspirin/other NSAIDs
Active peptic ulceration
3rd trim of pregnancy
Proctitis, haemorrhoids (suspositories)

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21
Q

A/E of Ibuprofen

A

Epigastric pain
Heartburn
Dizziness
Nausea
Rash
Tinnitus

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22
Q

PK of Ibuprofen
Absorption
Distribution
Metabolism
Excretion

A

A: rapid (85%) reduced by food, bio:80-100%
D: 90-99% protein bound
M: rapidly in liver by CYP2C9; CYP2C19 substrate

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23
Q

What is the T1/2 of Ibuprofen

A

2-4hrs in adults
1.6hrs in children (0.25-1yr)

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24
Q

Onset of Ibuprofen

A

30-60mins

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25
Q

DOA of Ibuprofen

A

4-6hrs

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26
Q

Indication of Naproxen

A

Analgesia
Inflammation in rheumatoid disease
Gout
Dysmenorrhea

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27
Q

CI of Naproxen

A

Hypersensitivity to aspirin/other NSAIDs
Active peptic ulceration
3rd trim of pregnancy
Proctitis, haemorrhoids

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28
Q

A/E of Naproxen

A

Epigastric pain
Peptic ulceration
Headache
Dizziness
Rash
Tinnitus
Nephrotoxicity
Hepatic Dysfunction

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29
Q

PK of Naproxen
Absorption
Distribution
Metabolism
Excretion

A

A: rapid, 95% bio
D: 99% protein bound
M: liver via conjugation
E: 95% in urine as metabolites

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30
Q

Half life of Naproxen

A

12-15hrs

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31
Q

Indications of Diclofenac

A

Pain
Inflammation in rheumatoid disease
Gout

32
Q

CI of Diclofenac

A

Hypersensitivity to aspirin/other NSAIDs
Active peptic ulceration
3rd trim of pregnancy
Proctitis, haemorrhoids (suspositories)

33
Q

A/E of Diclofenac

A

Epigastric pain
Peptic ulceration
Headache
Dizziness
Rash
Tinnitus
Nephrotoxicity
Hepatic Dysfunction

34
Q

PK of Diclofenac
Absorption
Distribution
Metabolism
Excretion

A

A: absolte bioav. 55%
D: diffuses into/out synovial fluid,
99% protein bound
M: in liver via glucuronidation
E: in bile

35
Q

T1/2 of Diclofenac

A

12-15hr

36
Q

Indication of Indomethacin

A

Pain
Inflammation in rheumatological disorders

37
Q

CI of Indomethacin

A

Hypersensitivity to aspirin/other NSAIDs
Active peptic ulceration
3rd trim of pregnancy
Proctitis, haemorrhoids (suspositories)

38
Q

A/E of indomethacin

A

Epigastric pain(more than in diclofenac)
Peptic ulceration(more than in diclofenac)
Headache
Dizziness
Rash
Tinnitus
Nephrotoxicity
Hepatic Dysfunction
Drowsiness
Retinal disturbance(prolonged use)

39
Q

PK of Indomethacin

A

A: 100% bioav.
D: 99% protein bound
M: in liver
E: 60% in urine, >33% in faeces

40
Q

Onset of Indomethacin

A

30 min

41
Q

DOA of indomethacin

A

4-6hrs

42
Q

Indications of Ketorolac

A

Short-term management of moderate postoperative pain

43
Q

CI of Ketorolac

A

duration >5days
chronic pain
Hypersensitvity to NSAIDs
PUD

44
Q

AE of Ketorolac

A

Dizziness
drowsiness
Headaches
GI pain
nausea
dyspepsia (indigestion)
somnolence (drowsiness)

45
Q

PK of Ketorolac

A

A: 100% bioav.
D: 99% protein bound
M: in liver
E: 91% in urine, 6% in feces

46
Q

Onset of Ketorolac

A

10 min: IM
30-60 PO

47
Q

DOA of Ketorolac

A

4-6hrs

48
Q

Indication of Lornoxicam

A

short-term management of mild to moderate pain
Osteoarthritis
Rheumatoid arthritis

49
Q

CI of Lornixcam

A

GI bleeding
Active peptic ulceration
Coagulation disorders
Children <18
Hypersensitivity to NSAIDs

50
Q

AE of Lornoxicam

A

Dizziness
Insomnia
Migraines
Gastritis
Nausea
Vomiting
Gastro-eophageal reflux
Dyspepsia
Somnolence

51
Q

Half-life of Lornoxicam

A

3-4hrs

52
Q

Indications of Meloxicam

A

Painful osteoarthritis
Rheumatoid arthritis
Ankylosing Spondylitis
Acute Sciatica

53
Q

CI of Meloxicam

A

GI bleeding/perforation/ulceration
IBD
HF
Hypersensitivity to NSAIDs

54
Q

AE of Meloxicam

A

Light-headedness
Dizziness
Insomnia
Headache
Gastritis
Bronchospasm
Rash
Renal Failure

55
Q

T1/2 of Meloxicam

A

20hrs

56
Q

Indications of Piroxicam

A

Rheumatic disorders
Acute musculoskeletal disorders
Acute gout
Dysmenorrhea

57
Q

CI of Piroxicam

A

GI bleeding/perforation/ulceration
IBD
HF
Hypersensitivity to NSAIDs

58
Q

AE of Piroxicam

A

Light-headedness
Dizziness
Insomnia
Headache
Gastritis
Bronchospasm
Rash
Renal Failure

59
Q

T1/2 of Piroxicam

A

50hrs

60
Q

Indications of Mefenamic acid

A

Post-traumatic conditions
Dysmenorrhea

61
Q

CI of Mefenamic acid

A

GI bleeding/perforation/ulceration
IBD
HF
Hypersensitivity to NSAIDs

62
Q

AE of Mefenamic acid

A

Light-headedness
Dizziness
Insomnia
Headache
Gastritis
Bronchospasm
Rash
Renal Failure

63
Q

PK of Mefenamic acid

A

A; Extensive bioav.
D: Highly protein bound
M: in liver via oxidation/conjugation
E: 66% urine, 20-25% feces

64
Q

Onset of Mefenamic acid

A

Rapid

65
Q

T1/2 of Mefenamic acid

A

2hrs; dialysable

66
Q

Which are the Selective COX inhibitors

A

Celecoxib
Etoricoxib
Parecoxib

67
Q

MOA of selective COX inhibitors

A

Reversibly inhibit COX 2–> decr. prostaglandin synthesis= decr. pain and inflammation

68
Q

Effects of Selective COX 2 inhibitors

A

Decr. risk of peptic ulceration
decr. risk of renal failure(or other NSAID AE)
incr. risk of Heart Attacks, Strokes and thrombosis by relative incr. in thromboxane

69
Q

Indications of Celecoxib

A

Symptomatic treatment of inflammation and pain in osteoarthritis and Rheumatoid arthritis
Pain after dental surgery

70
Q

CI of Celecoxib

A

Hypersensitivity to sulphonamides
Severe renal/hepatic impairment
Asthma
Allergy to NSAID
Risk to CVS disease
Pregnancy

71
Q

AE of Celecoxib

A

Dyspepsia
Abd. pain
Diarrhea
Nausea and vomiting
Flatulence
SJS

72
Q

PK of Celecoxib

A

A: undetermined bioav.
D: 97% protein bound
M: in liver via CYP2C9
E: inactive metabolites in urine and feces

73
Q

T1/2 of Celecoxib

A

11hrs

74
Q

Indications of Etorocoxib

A

Osteoarthritis
Rheumatoid arthritis
Gouty arthritis
Primary dysmenorrhea

75
Q

CI of Etoricoxib

A

Hypersensitivity to sulphonamides
Severe renal/hepatic impairment
Asthma
Allergy to NSAID
Risk to CVS disease
Pregnancy

76
Q

AE of Etoricoxib

A

Dizziness
Headache
Palptations
Bronchospasm
Gastritis
SJS
Tinnitus

77
Q

Indications of Parecoxib

A

Preoperative pain

Pharmacology (50 decks)

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