Anti-Inflammatory agents Flashcards

1
Q

What is an NSAID?

A

Non-Steroidal Anti-Inflammatory Drug

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2
Q

How are membrane phospholipids converted into leukotrienes?

A

Membrane phospholipids get converted into arachidonic acid by phospholipase A2
Arachidonic acid is then broken down into leukotrienes by Lipoxygenase

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3
Q

How are membrane phospholipids converted into prostaglandins?

A

Membrane phospholipids get converted into arachidonic acid by phospholipase A2
Arachidonic acid is then broken down into different prostaglandin classes by Cyclo-oxygenase (COX) enzyme

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4
Q

Which enzyme is targeted by corticosteroids?

A

Phospholipase A2 preventing the formation of arachidonic acid

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5
Q

What are some examples of glucocorticosteroids?

A

Hydrocortisone
Betamethasone
Prednisolone

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6
Q

Which enzyme is targeted by NSAIDs?

A

The Cyclo-oxygenase enzyme (COX)

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7
Q

What are some examples of NSAIDs?

A

Aspirin, Ibuprofen, Naproxen and celecoxib

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8
Q

Where are steroid hormones produced?

A

In the adrenal gland that sit on the kidneys

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9
Q

What are the 2 types of corticosteroid receptors?

A

Glucocorticoid receptors
Mineralocorticoid receptors

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10
Q

How do steroid drugs affect the cell?

A

Drugs pass through the plasma membrane
Here, they bind to glucocorticoid receptors
These allow passage into the nucleus where they bind to GRE (Glucocorticoid Response Elements) on DNA

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11
Q

What are the main therapeutic effects of glucocorticoid drugs?

A

Pain relief
Anti-allergy
Immunosupression
Anti-inflammatory
Decreased blood vessel permeability

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12
Q

What side effects can glucocorticoid drugs have on muscles?

A

Increased risk of myopathies causing muscle weakness

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13
Q

What side effects can glucocorticoid drugs have on bone?

A

Can cause osteoporosis
Can cause aseptic necrosis of the femur

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14
Q

What side effects can glucocorticoid drugs have on the skin?

A

Causes skin thinning

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15
Q

What side effects can glucocorticoid drugs have on metabolism?

A

Hyperglycaemia
Weight gain
Fluid retention
Cushingoid appearance - fat build up on the sides of the face

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16
Q

What side effects can glucocorticoid drugs have on the CNS and adrenal system?

A

HPA insufficiency
Neuropsychiatric disorders

17
Q

What side effects can glucocorticoid drugs have on the eyes?

A

Cataracts
Glaucoma

18
Q

What side effects can glucocorticoid drugs have on the cardiovascular system?

A

Hypertension

19
Q

What side effects can glucocorticoid drugs have on the gastrointestinal system?

A

Increased stomach acid production

20
Q

What do inhaled steroids increase the risk of thrush?

A

Steroids can be deposited in the oropharynx causing local immunosuppression, allowing the growth of Candida albicans

21
Q

What is CRH?

A

Corticotrophin Releasing Hormone

22
Q

What causes the release of CRH and where is it released from?

A

The hypothalamus, stimulated by stress or the Circadian rhythm

23
Q

What does CRH do?

A

It stimulates the anterior pituitary gland to release ACTH

24
Q

What is ACTH?

A

AdrenoCorticoTrophic Hormone

25
Q

What does ACTH do?

A

It stimulates the release of glucocorticoids from the adrenal glands

26
Q

What is the HPA axis?

A

Stress/circadian rhythm
Stimulates hypothalamus
Releases CRH
Stimulates anterior pituitary gland
Releases ACTH
Stimulates adrenal glands
Releases glucocorticoid steroids
Stimulates hypothalamus to reduce CRH production
Regulates steroid hormone levels

27
Q

How do glucocorticoid drugs cause HPA insufficiency?

A

Addition of glucocorticoid steroids into the blood stream stimulates the hypothalamus to reduce CRH levels
After prolonged use (3 weeks) the adrenal glands no longer produce glucocorticoids on their own, leading to adrenal insufficiency

28
Q

What would happen if steroids were stopped instantly, instead of slowly decreased?

A

The adrenal glands would no longer produce endogenous glucocorticoids, so the person would fall into a coma

29
Q

What are the 2 types of COX enzyme?

A

COX-1 and COX-2

30
Q

What is the function of COX-1?

A

COX-1 is always present in low levels , within the body and involved in platelet regulation, kidney function and regulation of stomach acid

31
Q

What is the function of COX-2?

A

COX-2 is an inducible enzyme that, when activated, causes inflammation, leading to pain, heat and swelling

32
Q

What are some common side effects of NSAIDs?

A

Adverse GI effects (Abdominal bleeding)
Reduced renal function in predisposed patients)
Hypertension

33
Q

What is misoprostol and why is it combined with NSAIDs?

A

Misoprostol is a synthetic prostaglandin medication
When bound to an NSAID, it can prevent gastric bleeding and discomfort by regulating the stomach lining which can be prevented by the NSAID alone

34
Q

What is a DMARD?

A

Disease Modifying Anti-Rheumatic Drug

35
Q

What are some examples of DMARDs?

A

Methotrexate
Sulfasalazine

36
Q

What are the advantages of DMARDs over NSAIDs?

A

They can be used for longer periods of time

37
Q

What are some examples of immunosuppressant drugs?

A

Ciclosporin
Azathioprine
Tacrolimus
Mycophenolate mofetil

38
Q

What are some examples of biological immunosuppressant?

A

Infliximab
Rituximab

39
Q

What are the 2 types of antihistamines and what are some examples of each?

A

1st generation (Sedating) - Promethazine, Cyclizine, Chlorphenamine

2nd generation (Non-sedating) - Fexofenadine, loratadine