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Molecules and cells in human disease > Lecture 4- Therapeutics for inflammation > Flashcards

Lecture 4- Therapeutics for inflammation Flashcards

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Organic Chemistry 101 flashcards
1
Q

what are H1 receptor antagonists commonly known as?

A

Anti-histamines

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2
Q

what do histamines do?

A
  • increase vascular permeability

- release pro-inflammatory mediators- eosinophils, adhesion molecules etc.

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3
Q

how many classes of histamine receptor are there?

A

2 (H1 and H2)

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4
Q

how many generations of anti-histamines have there been?

A

3

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5
Q

what was a major side-effect of anti-histamine generation 1?

A

sedation (drowsy)

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6
Q

what changed from generation 1 to generation 2 of anti-histamine side-effects?

A

no sedating effects but could react with other chemical such as grapefruit juice to give cardiotoxic effects

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7
Q

what changed from generation 2 to generation 3 of anti-histamines?

A

non sedating and non-cardio toxic

however they still bind to muscarinic receptors which can cause blurred vision and dry mouth

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8
Q

what are the 3 actions of NSAIDs?

A

1) anti-inflammatory
2) analgesic
3) anti-pyretic (reduce fever)

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9
Q

how do NSAIDs have an anti-inflammatory effect?

A

decrease in PGE2 and PGI1 to inhibit oedema

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10
Q

how do NSAIDs have an analgesic effect?

A

decrease prostaglandin sythesis, less sensitisation of nociceptors to bradykinin and 5-HT

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11
Q

how do NSAIDs have an anti-pyretic effect?

A

prevents IL-1 from releasing prostaglandins in te CNS so doesn’t elevate the hypothalamic set point for body temp

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12
Q

what’s the worst anti-inflammatory NSAID?

A

salicylic acid

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13
Q

what’s the best anti-inflammatory NSAID?

A

flurbiprofen

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14
Q

is paracetamol anti-inflammatory?

A

unknown/ contraversial subject

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15
Q

what 2 important enzyme families do NSAIDs have an effect on to cause side-effects?

A

COX-1

COX-2

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16
Q

by what mechanism do NSAIDs inhibit COX enzymes?

A

they prevent the binding of arachidenate to the active site of the COX enzyme

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17
Q

how are NSAIDs distinguished?

A

by their Cox selectivity, rather than chemical class

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18
Q

what are the 4 classes of NSAIDs with examples?

A

Selective COX-1 inhibitor- low dose aspirin
Non- selective COX inhibitors- ibuprofen and high dose aspirin
Selective COX-2 inhibitors- meloxicam
Highly selective COX-2 inhibitors- celeboxib

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19
Q

where does most of the knowledge about steroidal anti-inflammatory drugs come from?

A

observation of naturally produced steroids in the body

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20
Q

is natural cortisol produced at a steady speed or does it fluctuate?

A

it fluctuates throughout the day

however, it increases in stressful situations like illness

21
Q

what chemical to anti-inflammatory steroids mimic?

A

cortisol

22
Q

show the natural glucocorticoid production and feedback

A

CRH (corticotropin releasing hormone)–>anterior pituitary –> releases ACTH (adrenocorticotropic hormone) –> adrenal glands (on kidney) –> circulating glucocorticoids –> stops CRH poduction from hypothalamus

23
Q

what type of feedback is there in natural glucocorticoid production?

A

negative

24
Q

what are the 3 actions of exogenous glucocorticoids (steroid anti-inflammatories)?

A
  • suppress immune system (intended, therefore not side effect)
  • increase blood glucose
  • reduce bone formation
25
Q

give 2 examples of exogenous glucocorticoids

A
  • hydrocortisol (external)- excema

- prednisolone

26
Q

what’s the mechanism of actions of steroid anti-inflammatories on cells?

A
  • they’re lipophilic, so can enter cells
  • bind to cytoplasmic receptors
  • causes dimerisation
  • receptor-steroid dimer moves into nucleus
  • it interacts with HRE (hormone response element)
  • will lead to either up or down- regulation of mRNA production to either increase anti-inflammatory agents or decrease pro-inflammatory agents
27
Q

what effects do anti-inflammatory drugs have on immune cells?

A
  • reduced migration of neutrophils into tissue from BVs
  • reduced activation of WBCs
  • reduced T-helper proliferation and fibroblasts e.g. collagen
28
Q

what effects do anti-inflammatory drugs have on immune chemical mediators?

A

reduced production of mediatiors such as- cytokines, TNF, cell-adhesion molecules, histamine, NO synthase, complement proteins
increased synthesis of IL-10 and annexin-1 which are anti-inflammatory chemicals

29
Q

give some side-effects of steroid anti-inflammatories:

A 
candidas 
bruising
weight changes/ fat redistibution
osteoporosis 
adrenal suppression
30
Q

what effect do steroid hormones have on HPA axis?

A

negative effect

31
Q

why can’t patients come straight off most steroid drugs?

A

takes a while before the HPA axis returns to normal so need to come of slowly to prevent dangerous withdrawal symptoms

32
Q

what’s the difference between NSAIDs and DMARDs?

A

NSAIDs only reduce symptoms caused by inflammation, whereas DMARDs can affect the progression of an inflammatory disease over several months

33
Q

what type of drugs do DMARDs include?

A

immunosuppressants
antimalarials
gold salts

34
Q

what’s an important example of an immunosuppressant DMARD?

A

Methotrexate

35
Q

what does methotrexate do to cells?

A

pauses them in S-phase

36
Q

overall, what negative thing is happening in gout?

A

increased plasma urate/uric acid which deposits as crystals in synovial joints to cause pain and stiffness

37
Q

what, immune-system wise is uric acid?

A

a DAMP which stimulates the production of IL-1

38
Q

what’s the acute treatment for gout?

A
  • NSAIDs
  • corticosteroids
  • colchicine- reduces neutrophil mobility
39
Q

what’s the long-term treatment for gout?

A
  • uricosuric agents- act on kidney to increase uric acid secretion
  • xanthine oxidase inhibitors- increase uric acid levels in urine, therefore less in plasma
40
Q

what are anti-cytokine drugs used to treat?

A

rheumatoid arthiritis/ other inflammatory arthritis’

41
Q

what do anti-cytokine drugs target?

A

TNF and ILs (cytokines)

42
Q

why are anti-cytokine drugs expensive?

A

they are biologics (come from a living organism)

43
Q

what’s a negative long-term effect of anti-cytokine drugs?

A

increased risk of infection

44
Q

what does PPAR stand for?

A

Peroxisome Proliferator Activated Receptor (agonist)

45
Q

give 2 examples of PPARs

A
  • fibrates

- thiazolidinediones

46
Q

what do PPARs do?

A

reduce expression of cytokines, chemokines, cell adhesion molecules, TLRs etc.

47
Q

what are the 3 subtypes of PPARs?

A

alpha
beta/delta
gamma

48
Q

what’s a major pathology PPARs are used to treat?

A

atherosclerosis

49
Q

what is it important to balance when treating inflammatory diseases?

A

the anti-inflammatory effects of drugs with the host’s need for inflammation for immune system function

Molecules and cells in human disease (7 decks)

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