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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
DOA of Ibuprofen
4-6hrs
26
Indication of Naproxen
Analgesia Inflammation in rheumatoid disease Gout Dysmenorrhea
27
CI of Naproxen
Hypersensitivity to aspirin/other NSAIDs Active peptic ulceration 3rd trim of pregnancy Proctitis, haemorrhoids
28
A/E of Naproxen
Epigastric pain Peptic ulceration Headache Dizziness Rash Tinnitus Nephrotoxicity Hepatic Dysfunction
29
PK of Naproxen Absorption Distribution Metabolism Excretion
A: rapid, 95% bio D: 99% protein bound M: liver via conjugation E: 95% in urine as metabolites
30
Half life of Naproxen
12-15hrs
31
Indications of Diclofenac
Pain Inflammation in rheumatoid disease Gout
32
CI of Diclofenac
Hypersensitivity to aspirin/other NSAIDs Active peptic ulceration 3rd trim of pregnancy Proctitis, haemorrhoids (suspositories)
33
A/E of Diclofenac
Epigastric pain Peptic ulceration Headache Dizziness Rash Tinnitus Nephrotoxicity Hepatic Dysfunction
34
PK of Diclofenac Absorption Distribution Metabolism Excretion
A: absolte bioav. 55% D: diffuses into/out synovial fluid, 99% protein bound M: in liver via glucuronidation E: in bile
35
T1/2 of Diclofenac
12-15hr
36
Indication of Indomethacin
Pain Inflammation in rheumatological disorders
37
CI of Indomethacin
Hypersensitivity to aspirin/other NSAIDs Active peptic ulceration 3rd trim of pregnancy Proctitis, haemorrhoids (suspositories)
38
A/E of indomethacin
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
PK of Indomethacin
A: 100% bioav. D: 99% protein bound M: in liver E: 60% in urine, >33% in faeces
40
Onset of Indomethacin
30 min
41
DOA of indomethacin
4-6hrs
42
Indications of Ketorolac
Short-term management of moderate postoperative pain
43
CI of Ketorolac
duration >5days chronic pain Hypersensitvity to NSAIDs PUD
44
AE of Ketorolac
Dizziness drowsiness Headaches GI pain nausea dyspepsia (indigestion) somnolence (drowsiness)
45
PK of Ketorolac
A: 100% bioav. D: 99% protein bound M: in liver E: 91% in urine, 6% in feces
46
Onset of Ketorolac
10 min: IM 30-60 PO
47
DOA of Ketorolac
4-6hrs
48
Indication of Lornoxicam
short-term management of mild to moderate pain Osteoarthritis Rheumatoid arthritis
49
CI of Lornixcam
GI bleeding Active peptic ulceration Coagulation disorders Children <18 Hypersensitivity to NSAIDs
50
AE of Lornoxicam
Dizziness Insomnia Migraines Gastritis Nausea Vomiting Gastro-eophageal reflux Dyspepsia Somnolence
51
Half-life of Lornoxicam
3-4hrs
52
Indications of Meloxicam
Painful osteoarthritis Rheumatoid arthritis Ankylosing Spondylitis Acute Sciatica
53
CI of Meloxicam
GI bleeding/perforation/ulceration IBD HF Hypersensitivity to NSAIDs
54
AE of Meloxicam
Light-headedness Dizziness Insomnia Headache Gastritis Bronchospasm Rash Renal Failure
55
T1/2 of Meloxicam
20hrs
56
Indications of Piroxicam
Rheumatic disorders Acute musculoskeletal disorders Acute gout Dysmenorrhea
57
CI of Piroxicam
GI bleeding/perforation/ulceration IBD HF Hypersensitivity to NSAIDs
58
AE of Piroxicam
Light-headedness Dizziness Insomnia Headache Gastritis Bronchospasm Rash Renal Failure
59
T1/2 of Piroxicam
50hrs
60
Indications of Mefenamic acid
Post-traumatic conditions Dysmenorrhea
61
CI of Mefenamic acid
GI bleeding/perforation/ulceration IBD HF Hypersensitivity to NSAIDs
62
AE of Mefenamic acid
Light-headedness Dizziness Insomnia Headache Gastritis Bronchospasm Rash Renal Failure
63
PK of Mefenamic acid
A; Extensive bioav. D: Highly protein bound M: in liver via oxidation/conjugation E: 66% urine, 20-25% feces
64
Onset of Mefenamic acid
Rapid
65
T1/2 of Mefenamic acid
2hrs; dialysable
66
Which are the Selective COX inhibitors
Celecoxib Etoricoxib Parecoxib
67
MOA of selective COX inhibitors
Reversibly inhibit COX 2--> decr. prostaglandin synthesis= decr. pain and inflammation
68
Effects of Selective COX 2 inhibitors
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
Indications of Celecoxib
Symptomatic treatment of inflammation and pain in osteoarthritis and Rheumatoid arthritis Pain after dental surgery
70
CI of Celecoxib
Hypersensitivity to sulphonamides Severe renal/hepatic impairment Asthma Allergy to NSAID Risk to CVS disease Pregnancy
71
AE of Celecoxib
Dyspepsia Abd. pain Diarrhea Nausea and vomiting Flatulence SJS
72
PK of Celecoxib
A: undetermined bioav. D: 97% protein bound M: in liver via CYP2C9 E: inactive metabolites in urine and feces
73
T1/2 of Celecoxib
11hrs
74
Indications of Etorocoxib
Osteoarthritis Rheumatoid arthritis Gouty arthritis Primary dysmenorrhea
75
CI of Etoricoxib
Hypersensitivity to sulphonamides Severe renal/hepatic impairment Asthma Allergy to NSAID Risk to CVS disease Pregnancy
76
AE of Etoricoxib
Dizziness Headache Palptations Bronchospasm Gastritis SJS Tinnitus
77
Indications of Parecoxib
Preoperative pain

Pharmacology (50 decks)

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