Anti-inflammatories (year 2)

Question 1

name the drugs that can be used as anti-inflammtories

Answer 1

NSAIDs
glucocorticoids
anticytokines
immunosuppressants
antihistamine

Question 2

what is the mode of action of NSAIDs?

Answer 2

inhibit COX enzyme

Question 3

what does the COX enzyme do?

Answer 3

forms prostanoids from arachidonic acid

Question 4

what does the prostanoid group contain?

Answer 4

prostaglandins and thromboxanes

Question 5

what three effects do NSAIDs have?

Answer 5

anti-inflammatory
analgesic
antipyretic

Question 6

what prostaglandin do NSAIDs reduce that reduces inflammation?

Answer 6

prostaglandin E2 and prostacyclin

Question 7

what does a decrease in prostaglandin E2 and prostacyclin causes?

Answer 7

reduced vasodilation and oedema

Question 8

how does a decrease in prostaglandins result in analgesia?

Answer 8

decrease in sensitisation of nociceptive nerve endings to inflammatory mediators

Question 9

why do NSAIDs have a lot of adverse effects?

Answer 9

prostaglandins are important in normal homeostatic function

Question 10

what are some of the normal functions prostaglandins?

Answer 10

gastric protection - mucus production and proton pump inhibitor
platelet aggregation
renal blood flow autoregulation

Question 11

which of the COX enzymes is a constitutive enzyme and which is an induced enzyme?

Answer 11

constitutive - 1

induced - 2

Question 12

what is a constitutive enzyme?

Answer 12

one found in most tissues with a role in homeostasis

Question 13

which COX is mainly responsible for the mediators of inflammation?

Answer 13

COX-2

Question 14

inhibition of which COX enzyme are most of the side effects of NSAIDs due to?

Answer 14

1

Question 15

describe the absorption of NSAIDs

Answer 15

weak acids that are readily absorbed from the GI tract

Question 16

how are NSAIDs transported in blood?

Answer 16

bound to albumin

Question 17

why is the fact NSAIDs are distributed bound to albumin important?

Answer 17

changes in protein alters the transport and efficacy of the drug
if given with another drug that is bound to albumin then they compete

Question 18

how are NSAIDs eliminated from the body?

Answer 18

hepatic phase I and II metabolism

excreted in urine/faeces

Question 19

what species should NSAIDs be given sparingly and why?

Answer 19

cats - insufficient cytochrome P450 and glucoronidation conjugation

Question 20

what species should you not give paracetamol?

Answer 20

cats

Question 21

when might NSAIDs be used?

Answer 21

infectious disease
pain
osteoarthritis

Question 22

what is the main side effects of reduced prostaglandins?

Answer 22

GI ulceration and erosion leading to gastric bleeding

Question 23

other than GI ulceration what are other side effects of NSAIDs?

Answer 23

vomiting, diarrhoea, renal toxicity, hepatotoxicity, CNS depression, circulatory disturbance

Question 24

when should NSAIDs not be used?

Answer 24

with other NSAIDs or glucocorticoids
pregnancy
with renal, liver or cardiac impairment

Question 25

what are some examples of NSAIDs?

Answer 25

phenylbutazone, meloxicam, firocoxib, paracetamol, aspirin,

Question 26

what are the advantages of phenylbutazone?

Answer 26

long duration of action (intense protein binding) | cheap

Question 27

what animals is phenylbutazone not licensed in?

Answer 27

food producing animals

Question 28

what is the therapeutic use of meloxicam?

Answer 28

acute/chronic pain and inflammation

Question 29

which COX enzyme does meloxicam preferentially bind to?

Answer 29

2 - meaning less side effects

Question 30

where does paracetamol act in the body?

Answer 30

specific effect in CNS so has poor local inflammatory action - don't get peripheral adverse effects

Question 31

what animals is paracetamol licensed in?

Answer 31

pigs and dogs

Question 32

where is paracetamol metabolised?

Answer 32

liver - highly toxic to cats

Question 33

which COX enzyme does aspirin inhibit?

Answer 33

1 - significant side effects

Question 34

aspirin inhibits platelet aggregation, what does this mean it can be used as?

Answer 34

an anti clotting agent

Question 35

what effects do glucocorticoids have on neutrophils?

Answer 35

reduce extravasation and activation

Question 36

what effects do glucocorticoids have on fibroblasts?

Answer 36

reduce the function so reduce collagen production and hence reduce wound healing

Question 37

what chemical mediators do glucocorticoids reduce the production of?

Answer 37

prostanoids, cytokines, IgG, complement components, nitric oxide

Question 38

what chemical mediators do glucocorticoids increase the synthesis of?

Answer 38

anti-inflammatory mediators such as IL1

Question 39

what do large doses of glucocorticoids for extended periods of time cause?

Answer 39

iatrogenic cushings

Question 40

what are the adverse effects of glucocorticoids?

Answer 40

GI ulceration, decrease wound healing, myopathy, osteoporosis, oedema, thrombosis, abortion, diabetes, laminitis

Question 41

what are cytokines?

Answer 41

soluble protein or polypeptides released from a cell

Question 42

cytokines are important in the control of what system?

Answer 42

immune

Question 43

what are the 4 main classes of cytokines?

Answer 43

chemokine interferons interleukins colony stimulating factors

Question 44

what is colchicine?

Answer 44

an anti fibrotic drug

Question 45

what is colchicine used for?

Answer 45

treat liver fibrosis