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X Pharmacological Treatment Of Disease > NSAIDs and Coxibs > Flashcards

NSAIDs and Coxibs Flashcards

1
Q

what are eicosanoids?

A

inflammatory mediators

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2
Q

how are eicosanoids made?

A

synthesised from membrane phospholipids via intermediate arachidonic acid

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3
Q

what are the main groups of eicosanoids?

A

prostaglandins
leukotrienes
thromboxanes

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4
Q

what are prostanoids?

A

prostaglandins and thromboxanes

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5
Q

what are the two classes of drugs for prostanoids?

A

non steroidal anti-inflammatory drugs (NSAIDS)

anti-inflammatory steroids (glucocorticoids)

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6
Q

what do steroidal anti-inflammatories do?

A

block the synthetic pathway

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7
Q

what do non-steroidal anti-inflammatories do?

A

block prostaglandin pathway

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8
Q

what is an example of a non-steroidal anti-inflammatory?

A

aspirin (NSAIDS)

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9
Q

what is an example of a steroidal anti-inflammatory?

A

predisolone

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10
Q

how are prostanoids synthesised?

A
  1. arachidonic acid is released from membrane phospholipids by phospholipase A2
  2. arachidonic acid has to fates
    i) conversion to prostanoids (prostaglandins and thromboxanes) via COX pathway (cyclooxygenase)
    ii) conversion to leukotrienes via 5-lipoxygenase pathway
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11
Q

what is the synthesis of prostanoids via the COX pathway?

A
  1. phospholipids -> arachidonic acid via phospholipase A2
  2. arachidonic acid -> PGH2 via COX
  3. PGH2 -> PGI2, PGE2, PGD2, PGF2alpha, TXA2
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12
Q

what are the 5 classes of prostanoids and what are their corresponding G-coupled receptors?

A
  1. Prostaglandin D2 (PGD2), DP G-coupled receptor
  2. Prostaglandin E2 (PGE2), EP G-coupled receptor
  3. Prostaglandin F2alpha (PGF2alpha), FP G-coupled receptor
  4. Prostaglandin i2 (PGI2), IP G-coupled receptor
  5. Thromboxane A2 (TXA2), TP G-coupled receptor
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13
Q

what produces PGI2?

A

vascular endothelium

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14
Q

what produces TXA2?

A

platelets

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15
Q

what produces PGE2?

A

macrophages

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16
Q

what produces PGD2?

A

mast cells

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17
Q

what is the action of PGI2?

A

vasodilation

inhibition of platelet aggregation

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18
Q

what is the action of PGE2?

A 
vasodilation
hyperalgesia
fever
bronchoconstriction
mucus secretion
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19
Q

what is the action of PGD2?

A

vasodilation

inhibition of platelet aggregation

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20
Q

what is the action of PGF2alpha?

A

bronchoconstriction

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21
Q

what is the action of TXA2?

A

vasoconstriction

promotion of platelet aggregation

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22
Q

how are leukotrienes synthesised?

A

phospholipids —-PLA2—> arachidonic acid —5-lipoxygenase—> leukotrienes

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23
Q

what are the 4 kinds of leukotrienes?

A

LTB4
LTC4
LTD4
LTE4

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24
Q

what does LTB4 do?

A

chemotaxis - attracts neutrophils and eosinophils

25
Q

what does LTC4, LTD4 and LTE4 do?

A

bronchoconstriction, increase vascular permeability, promote mucus secretion

26
Q

what conditions are leukotrienes used to treat?

A

asthma

27
Q

what kind of NSAID is aspirin?

A

salicylicates

28
Q

what kind of NSAID is ibuprofen?

A

propionic acid

29
Q

what are the clinical uses of NSAIDs?

A

diseases associated with pain and inflammation e.g. rheumatoid arthritis and musculoskeletal disorders

somatic pain e.g. headaches, toothache, menstrual pain

febrile conditions e.g. fever

30
Q

what are the 3 main effects of NSAIDs?

A

anti-inflammatory
analgesic
antipyretic

31
Q

how are the 3 main effects of NSAIDs produced?

A

by inhibiting the COX enzyme of prostaglandin synthesis pathway

32
Q

how do NSAIDs produce an analgesic effect?

A

decrease PGs which decrease the sensitisation of nerve endings to BradyKinin and 5-HT

33
Q

how do NSAIDs produce an anti-inflammatory effect?

A

decrease PGE2/PGI2 -> decrease vasodilation -> decrease oedema and redness

34
Q

how do NSAIDs produce an antipyretic effect?

A

decreased PGE2 produced in response to IL-1 (inflammatory pyrogen) -> decreased elevation of hypothalamic set point for temperature control in fever

35
Q

why doesn’t NSAIDs completely abolish inflammation - why does it only decrease it?

A

NSAIDs don’t inhibit other inflammatory mediators such as bradykinin or histamine

36
Q

what synthesis do NSAIDs inhibit to for analgesic action?

A

inhibit synthesis of PGE2 and PGF2alpha in inflamed tissues

37
Q

how does fever occur?

A
  1. infection
  2. leukocytes
  3. IL-1
  4. PGE2
  5. hypothalamus
  6. fever
38
Q

how does aspirin cause antiplatelet action?

A

inhibition of TXA2 synthesis in platelets via inhibiting COX

inhibition of endothelial PGI2 synthesis

39
Q

what are the gastrointestinal effects of aspirin?

A 
nausea
vomitting
diarrhoea
gastric damage:
- irritation
- bleeding
- ulceration due to prostaglandin synthesis inhibition
(prostaglandins protect mucosa)

PGE2 and PGI2 reduce acid secretion and promote mucus secretion

40
Q

except gastrointestinal, what other adverse effects of aspirin are there?

A

hypersensitivity

renal insufficiency

  • due to inhibition of vasodilatory PGE2 and PGI2
  • problematic in elderly/renal patients

effects on the uterus
- delay labour by inhibiting PGE2 and PGF2alpha

Reye’s syndrome

  • associated with aspirin treatment of childrens viral infections
  • hepatitis with cerebral oedema
41
Q

what new versions of COX have been discovered?

A

COX 1

COX 2

42
Q

what are COX 1 and 2?

A

isoenzymes

43
Q

when is COX 1 produced?

A

constitutive- always present

44
Q

when is COX 2 produced?

A

inducible - by inflammatory stimuli

45
Q

where is COX 1 found?

A

platelets, kidney, stomach, other tissues

46
Q

where is COX 2 found?

A

most inflammatory cells

47
Q

Adverse effects of NSAIDs are due to inhibition of which enzyme?

A

COX1

48
Q

therapeutic effects of NSAIDs are due to inhibition of which enzyme?

A

COX2

49
Q

name 2 COX-2 selective drugs

A

celecoxib (celebrex)

rofecoxib (vioxx)

50
Q

how can COX1 and 2 inhibitors be designed to be selective from eachother?

A

structual differences between the substrate-binding channels of COX 1 and COX 2

51
Q

what kind of adverse effects occur with coxibs?

A

serious cardiovascular

52
Q

what do COX1s do in the endothelium?

A

constitutive

53
Q

what do COX2s do in the endothelium?

A

induced by ischaemia and inflammation. generate mostly PGI2 and prevents aggregation

54
Q

what do COX1s do in platelets?

A

constitutive. generate mostly TXA2 and promote aggregation

55
Q

what do tNSAIDs inhibit?

A

COX-1 of platelet aggregation

COX-1 and COX-2 of PGI2 synthesis

56
Q

what do coxibs inhibit?

A

COX-2 of PGI2 synthesis

57
Q

what are celecoxib and etoricoxib used to treat?

A

both- licensed for the relief of pain in osteoarthritis and rheumatoid arthritis

celecoxib- relief of ankylosing spondylitis

etoricoxib - relief of pain from gout

58
Q

what is a condition cause by an adverse effect of aspirin?

A

Reye’s syndrome

aspirin in children with viral infections

fulminating hepatitis with cerebral oedema

X Pharmacological Treatment Of Disease (9 decks)

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