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L2 pharmacology > Anti-inflammatories > Flashcards

Anti-inflammatories Flashcards

1
Q

What are NSAIDs?

A

Non Steroidal Anti Inflammatory Drugs

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2
Q

What is the active chemical in willow tree bark?

A

Salicylic acid

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3
Q

What is ASA?

A
  • Acetylsalicylic acid
  • Aspirin
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4
Q

What are examples of NSAIDs? (3)

A
  • Aspirin
  • Paracetamol (acetaminophen)
  • Ibuprofen
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5
Q

How do NSAIDs work?

A

Inhibit the production of inflammatory mediators (prostaglandins and thromboxanes) by inhibiting COX enzymes

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6
Q

What kind of signalling do prostaglandins and thromboxanes do?

A

Paracrine

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7
Q

Which enzymes are found in cells which make lipid inflammatory mediators?

A

Cyclooxygenases (COX enzymes)

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8
Q

How are lipid inflammatory mediators made?

A
  • Phospholipase A2 acts on plasma membrane lipids and generates the precursor (arachidonate)
  • COX enzyme converts arachidonate into inflammatory mediators
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9
Q

What does PGF (prostaglandin F) cause?

A

Myometrial contraction (initiation of labour)

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10
Q

What does PGD2 (prostaglandin D2) cause? (2)

A
  • Inhibits platelet aggregation
  • Vasodilation (swelling and redness)
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11
Q

What does PGE2 (prostaglandin F) cause? (2)

A
  • Vasodilator
  • Hyperalgesia (increased pain perception)
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12
Q

What does TXA2 (thromboxane A2) cause? (2)

A
  • Blood clotting
  • Vasoconstriction
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13
Q

Why is increased bleeding a side effect of NSAIDs?

A
  • Thromboxane A2 causes blood clotting
  • NSAIDs block the production of TXA2
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14
Q

What do prostaglandins do?

A

Attract immune cells

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15
Q

What are NSAIDs used for? (4)

A
  • Anti-inflammatory
  • Analgesic
  • Antipyretic
  • Antithrombotic
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16
Q

How do NSAIDs relieve headache pain?

A

Decrease vasodilation of blood vessels on the surface of the skull

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17
Q

What does antipyretic mean?

A

Lower raised temperature

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18
Q

Are NSAIDs used for chronic conditions?

A

No because different mediators are associated with chronic inflammatory conditions and NSAIDs are ineffective against them

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19
Q

How many COX enzymes are there?

A
  • COX 1,2 and 3
  • 3 is actually a variant of 1
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20
Q

What is the function of COX 1?

A

Normal constant production of prostaglandins with homeostatic functions in the body

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21
Q

What is the function of COX 2?

A
  • Inducible enzyme
  • Made in response to injury and inflammation
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22
Q

What is the function of COX 3?

A
  • Expressed in the brain and the kidneys
  • Paracetamol exerts action through COX 3 (headaches)
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23
Q

What is the general structure of COX enzymes? (3)

A
  • Dimer (2 identical subunits)
  • Embedded into endoplasmic reticulum membrane
  • Pore leading to cyclooxygenase site
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24
Q

How are COX 1 and 2 different? (2)

A
  • Pore of COX 1 has isoleucine but COX 2 has valine (smaller) so COX 2 has a wider channel
  • Allows for selectivity of COX 2, bigger drugs can enter COX 2
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25
Q

What is the main side effect issue with NSAIDs?

A

GI irritation

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26
Q

Why do NSAIDs cause GI irritation?

A
  • Prostaglandins play a role in maintaining the protective mucus in the GI tract
  • Ulcers can form in severe cases
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27
Q

What are the homeostatic functions of mediators made by COX 1? (3)

A
  • Production of GI mucus
  • Maintenance of blood flow through the kidneys
  • Control of blood clot formation (TXA2)
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28
Q

What is a suicide inhibitor?

A

A drug that covalently binds to its target and causes a permanent inactivation

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29
Q

Why is the duration of aspirin action 3/4 hours? (2)

A
  • Aspirin is a suicide inhibitor so permanently blocks COX enzyme site
  • Aspirin must be metabolised and excreted and new COX enzymes synthesised for action to wear off
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30
Q

Which NSAIDs are COX 1 selective? (2)

A
  • Aspirin
  • Ibuprofen
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31
Q

Which NSAIDs are COX 2 selective?

A

Coxibs

32
Q

What are the unwanted side effects of NSAIDs? (4)

A
  • Gut problems
  • Impacts on renal function
  • Liver damage
  • Allergic reactions (rashes, asthma attacks)
33
Q

Why doesn’t paracetamol cause gut problems?

A

Selective for COX 3

34
Q

How can gut side effects of NSAIDs be reduced?

A

Co-administer a PG analogue (misoprostol)

35
Q

Why can paracetamol cause liver damage?

A

First phase of metabolism of paracetamol generates a dangerous chemical which can kill cells

36
Q

What are the advantages of COX 1 selective drugs?

A

Anti-thrombotic effects can be useful for patients at risk of strokes

37
Q

What are the advantages of COX 2 selective drugs?

A

Don’t cause gut problems

38
Q

What are the disadvantages of COX 2 selective drugs?

A

Role in kidney function means that inhibition of COX 2 causes increase in blood pressure and salt retention

39
Q

Why was the coxib drug Vioxx withdrawn?

A
  • COX 2 selective
  • Caused death of patients with underlying cardiovascular disease due to increase in blood pressure and salt retention
40
Q

What are the properties of aspirin? (3)

A
  • Anti-platelet action
  • Reduces risk of colon/rectal cancer and Alzheimer’s
  • Suicide inhibitor
41
Q

Why might aspirin reduce the risk of Alzheimer’s?

A

Inflammation in the brain is a contributing factor to neurodegenerative disease

42
Q

What are the properties of paracetamol? (5)

A
  • Effective analgesic and antipyretic
  • Weak anti-inflammatory, not good for swelling
  • COX 1/3 selective
  • Can cause liver and kidney damage
  • Competitive inhibitor (binds reversibly)
43
Q

What do formulations sometimes combine with NSAIDs in painkillers?

A
  • Opioids e.g. naproxen = ibuprofen + codeine
  • Combination reduces the amount of opioid needed to achieve the same level of pain relief by 1/3
44
Q

What are 2 examples of chronic inflammatory conditions?

A
  • Asthma
  • Rheumatoid arthritis
45
Q

What is rheumatoid arthritis?

A

An inflammatory autoimmune disease that causes painful swelling in the synovium of joints

46
Q

What causes the symptoms of rheumatoid arthritis?

A
  • Activation of T cells which activate macrophages which release cytokines (IL-1 and TNF-alpha)
  • The cytokines cause inflammation leading to the symptoms
47
Q

What drugs are used to treat rheumatoid arthritis? (5)

A
  • Methotrexate
  • DMARDS (Disease Modifying Anti Rheumatic Drugs) e.g. sulfasalazine
  • Cyclosporin
  • Glucocorticoids e.g. prednisolone
  • Biopharmaceuticals
48
Q

What are the effects of methotrexate? (2)

A
  • Folic acid antagonist
  • Immunosuppressant activity
49
Q

What other condition is sulfasalazine used to treat?

A

Chronic inflammatory bowel disease (e.g. ulcerative colitis, Crohn’s disease)

50
Q

How do cyclosporin and glucocorticoids work?

A

Inhibit transcription of proinflammatory cytokines

51
Q

How does cyclosporin work to treat rheumatoid arthritis? (2)

A
  • Inhibits calcineurin so inhibits activity of NFKB
  • Therefore prevents production of cytokines
52
Q

What is a phosphatase?

A

Enzyme which removes phosphate groups

53
Q

What is calcineurin? (2)

A
  • Phosphatase which targets NFKB
  • NFKB drives transcription of cytokines
54
Q

What is NFKB?

A

Transcription factor which drives production of cytokines (IL-2, IL-1, TNF-alpha)

55
Q

How do glucocorticoids work to treat rheumatoid arthritis?

A

Bind to DNA and repress the transcription of cytokines at the level of the DNA

56
Q

What kind of drug is prednisolone?

A

Glucocorticoid

57
Q

What does it mean if a drug name ends in ‘mab’?

A

It is a monoclonal antibody

58
Q

What is adalimumab?

A

Humanised monoclonal antibody drug which targets and neutralises TNF-alpha to treat inflammation

59
Q

How do soluble receptors work?

A

Inject soluble receptors to the cytokines in order to ‘mop them up’

60
Q

Which drugs are used to treat asthma? (3)

A
  • Salbutamol
  • Steroids e.g. prednisolone
  • Biopharmaceuticals e.g. omalizumab
61
Q

How does salbutamol work?

A
  • Agonist for beta 2 adrenoreceptors in airway smooth muscle
  • Causes bronchodilation
62
Q

Which G protein do beta 2 adrenoreceptors signal via?

A

Gs

63
Q

What are the 2 classes of respiratory allergies?

A
  • Allergic rhinitis
  • Allergic asthma
64
Q

What is the difference between allergic rhinitis and allergic asthma?

A

Allergic rhinitis is restricted to the upper airways (i.e. nose) but allergic asthma affects the lower airways

65
Q

What happens in respiratory allergies?

A

Allergen activates mast cells which release inflammatory mediators

66
Q

What are the 2 phases of respiratory allergy responses?

A
  • Early/immediate phase
  • Late phase
67
Q

What happens during the early phase of respiratory allergy response?

A

The allergen activates mast cells which secrete histamine

68
Q

What is the late phase of respiratory allergy response?

A
  • Doesn’t occur in all patients (genetic component which isn’t understood)
  • Involves cytokines causing an inappropriate inflammatory response hours after coming into contact with an allergen
69
Q

What happens in asthma? (2)

A
  • T cells are activated and cause production of IgE antibodies against the allergen
  • The antibodies are bound to mast cells and eosinophils which cause the inflammation
70
Q

What happens when the IgE antibody receptor on mast cells is activated by the allergen? (2)

A
  • Release of histamine, prostaglandins
  • Increased transcription of cytokines and chemokines which cause the late phase response
71
Q

What are the effects of histamine and prostaglandin release from mast cells in asthma? (4)

A
  • Bronchoconstriction
  • Increased vascular permeability (allows immune cells into the lungs)
  • Mucous secretion
  • Stimulation of nerve endings (coughing)
72
Q

What drugs are used to treat the late phase of the allergic asthma response?

A

Glucocorticoids

73
Q

What is seen in chronic inflammation of the airways from uncontrolled asthma? (3)

A
  • Lots of mucous
  • Thickening of the smooth muscle around the airways
  • More mucous-secreting cells
74
Q

What is caused by long term glucocorticoid use?

A

Cushing’s disease

75
Q

What are the symptoms of Cushing’s disease? (4)

A
  • Buffalo hump
  • Bruising
  • Hypertension
  • Poor wound healing
76
Q

How does omalizumab work?

A

Targets IgE antibodies so prevents inflammatory response

77
Q

What new therapies are being developed for asthma treatment? (2)

A
  • Humanised monoclonal antibodies
  • Prostaglandin receptor antagonists

L2 pharmacology (9 decks)

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