NSAIDs

Question 1

NSAIDs; two classes & mechanism of action

Answer 1

COX 1 i and Non-selectove (COX 1i and COX2i) -> reduce PGL, responsible for pain, fever and inflammation

Question 2

What’s the deal with COX 1 & COX 2 & what does their inhibition result in?

Answer 2

free COX 1 = protects stomach & platelet glue (pro-coagulates) [risk of MI, stroke etc]

COX 1inhibition: GI bleed: no protection, no platelet coagulation

COX 2inhibition = anti-inflammatory effect

Question 3

First line NSAIDS include:

Answer 3

buprofen:
low incidence of side-effects
good for pain
less anti-inflammatory

naproxen and diclofenac:
more anti-inflammatory effects
relatively low incidence of side-effects

Question 4

T or F?
All NSAID use (including COX-2 selective inhibitors) associated with a small increased risk of thrombotic events (e.g. myocardial infarction and stroke) independent of baseline cardiovascular risk factors or duration of NSAID use; however, the greatest risk may be in those receiving high doses long term.

Answer 4

T

Question 5

Which iii areassociated with an increased risk of thrombotic events.

Answer 5

COX-2 selective inhibitors: -coxibs
Diclofenac (150 mg daily)
Ibuprofen (2.4 g daily)

Question 6

Why are NSAIDs a problem in heart failure?

Answer 6

Sodium and water retention: antagonize & increase toxicity of diuretics
Vasocontriction: antagonise diuretics & increase toxicity
Clotting risk: MI, stroke
Overall increased mortality and CV morbidity risk

Question 7

For severe HF, mild - moderate HF how should NSAIDs be prescribed?

Answer 7

○ Severe heart failure — NSAIDsshould be avoided.
○ Mild, moderate, or severe heart failure —COX-2 inhibitors, diclofenac, andhigh-dose ibuprofen (2400 mg or more daily) should be avoided.

Question 8

Mild - moderate heart failure, which NSAIDs are best to prescribe?

Answer 8

Ibuprofen up to 1200mg daily

Naproxen up to 100mg daily

Question 9

For people with ischaemic heart disease, cerebrovascular disease, or peripheral arterial disease, what are NSAID first line options?

Answer 9

Ibuprofen up to 1200mg/day

Naproxen up to 100mg daily

Question 10

For people with ischaemic heart disease, cerebrovascular disease, or peripheral arterial disease, what are NSAIDs are contraindicated?

Answer 10

○ COX-2 inhibitors, diclofenac, and high-dose ibuprofenare contraindicated.

Question 11

For people with risk factors for cardiovascular disease and all elderly people what NSAIDs should be prescribed?

Answer 11

Ibuprofen max 1200mg

Naproxen max 1000mg

Question 12

For people with uncontrolled hypertension(blood pressure persistently above 140/90 mmHg) what NSAIDs should be avoided?

Answer 12

Eterocoxib and high dose ibuprofen

Question 13

Ibuprofen dose

Contraindications (VIII)

Answer 13

Any NSAID hypersensitivity
Hx GI bleed
Active/Hx recurrent ulcer/hae
Severe RF/HF
Severe HF
Last trimester pregnancy
Dehydration
CVD/active bleeding

Question 14

General risks of Cardiovascular events?

Answer 14

. hypertension, hyperlipidaemia, diabetes mellitus, smoking)

Question 15

State the interaction:

NSAIDs + Acetylsalicyclic acid:

Other NSAIDs:

Answer 15

antagonise antiplateletet properties and reduce cardioprotective effects: avoid

GI ulcer & haemorrhage risk: avoid

Question 16

State the interaction: NSAIDS + SSRIs:

Answer 16

increased bleeding risk

Question 17

State the interaction: NSAIDS +
Corticosteroids:

Quinolones:

Answer 17

i) GI bleeding and ulceration

ii) seizure risk

Question 18

State the interaction: NSAIDS +
Amionoglycosides:

Captopril:

Answer 18

i) reduced excretion of aminoglcosises

ii) increased sodium retention

Question 19

State the interaction:
NSAIDs +
Antihypertensives: Duiretics, betablockers, ACE-I., ARB

ii) Potassium-sparing duiretics & ACEI/ARB

Answer 19

Reduced effectiveness
Impaired renal function

Elevated K+ - monitor K+

Question 20

State the interaction: 
NSAIDs + 
Ciclosporin, Tacrolimus
Ritonavir
Zidovudine

Answer 20

i) nephrotoxicity
ii) increased plasma concentration
iii) haemotological toxicity in HIV

Question 21

State the interaction:
NSAID + 
lithium:
phenytoin:
digoxin:

Answer 21

i) increased levels due to reduced excretion - necessary monitor
ii) increased levels - rec monitor
iii) increased levels - rec monitor

Question 22

State the interaction:

NSAID + Alcohol, bisphosphonates and oxpentifylline (pentoxyflline):

Answer 22

potential GI SE and risk of GI ulceration

Question 23

State the interaction:

NSAID + METHOTREXATE

Answer 23

Inhibition of renal tubular secretion especially given 24hours before and 24 hours after.

D not use high doses
Monitor renal function

Question 24

Topical NSAID: pt advice

Answer 24

For topical preparations, patients or their carers should be advised against excessive exposure to sunlight of area treated in order to avoid possibility of photosensitivity