Pharmacology of inflammation Flashcards

1
Q

What do NSAIDs stand for?

A

Non-steroidal anti-inflammatory drugs

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2
Q

How do NSAIDs work?

A

Inhibiting the activity of cyclooxygenase enzymes (COX-1 or COX-2).

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3
Q

What is the role of COX enzyme?

A

COX catalyzes the formation of prostaglandins and thromboxane from arachidonic acid

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4
Q

What is arachidonic acid generated from?

A

Phosphatidylinositol

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5
Q

How is arachidonic converted from phosphatidylinositol?

A

Via phospholipase A2

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6
Q

What are prostaglandins involved in?

A

Inflammation

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7
Q

What are thromboxane’s involved in?

A

Haemostasis

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8
Q

What are non-selective NSAIDs?

A

Ibuprofen, Naproxen, Diclofenac, Aspirin

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9
Q

What are COX2 selective NSAIDs?

A

Celecoxib, Rofecoxib

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10
Q

What coverts arachidonic acid to the leukotriene pathway?

A

Lipoxygenase

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11
Q

Why is aspirin taken by stroke vulnerable patients?

A

Reduced blood clotting

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12
Q

What is the role of thromboxane A2?

A

Thromboxane that is produced by activated platelets during haemostasis and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation.

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13
Q

What steroid drugs are used for inflammation?

A

Glucocoticosteroids

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14
Q

Why are glucocorticosteroids the most powerful anti-inflammatories?

A

Capable of inhibiting virtually all the components of inflammation.

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15
Q

What do glucocorticosteriods upregulate?

A

Annexin-1

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16
Q

What does annexin-1 do?

A

Suppresses phospholipase A2, thereby blocking eicosanoid production, and inhibits various leukocyte inflammatory events (epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst).

17
Q

Why are glucocorticosteroids good for treating asthma but NSAIDs don’t have a huge effect?

A

Steroids target earlier in the AA pathway, inhibit prostaglandin and leukotriene production

18
Q

What are the most prominent glucocorticoids?

A

Cortisol (hydrocortisone), Cortisone, Prednisone, Prednisolone, Methylprednisolone and Dexamethasone.

19
Q

Side effects of glucocorticoids?

A

Immunodeficiency is the main side effect: increasing susceptibility to viral infection

Hyperglycemia due to increased gluconeogenesis, insulin resistance, and impaired glucose tolerance (“steroid diabetes”); caution in those with diabetes mellitus

Increased skin fragility, easy bruising

Steroid-induced osteoporosis: reduced bone density (osteoporosis, osteonecrosis, higher fracture risk, slower fracture repair)

Weight gain due to increased visceral and truncal fat deposition (central obesity) and appetite stimulation; see corticosteroid-induced lipodystrophy

Hypertension through effects of fluid and electrolyte balance.

20
Q

What is histamine synthesised from?

A

Decarboxylation of histidine

21
Q

First generation antihistamines are..

A

Not specific to the H1 receptor, inverse agonists

22
Q

Second generation antihistamines, are…, they were synthesised because..

A

Modifications of the First Generation Antihistamines to eliminate side effects resulted in the Second Generation Antihistamines

More selective for peripheral H1 receptors

23
Q

What are side effects of first generation anti-histamines?

A

Because they can cross the BBB, they cause drowsiness, as H1 receptors are also involved in the CNS in the sleep-wake cycle.

24
Q

Types of first generation anti-histamine

A

Ethylenediamines, Ethanolamines, Alkylamines - Chlorphenamine, Piperazines and Tricyclics.

25
Q

Examples of second generation anti-histamines

A

Terfenadine, loratadine and cetirizine

26
Q

What are DMARDs

A

Disease-modifying antirheumatic drugs

27
Q

What is does methotrexate do?

A

Stimulates adenosine release from fibroblasts, reduces neutrophil adhesion, inhibits leukotriene B4 synthesis by neutrophils, inhibits local IL-1 production, reduces levels of IL-6 and IL-8, suppresses cell-mediated immunity, and inhibits synovial collagenase gene expression.

28
Q

What are biological DMARDs?

A

Biologic DMARDs are highly specific and target a specific pathway of the immune system

29
Q

Biological DMARD examples

A

Some biologic agents include infliximab (TNFalpha), adalimumab, etanercept, rituximab, abatacept, rituximab, tocilizumab (IL-6), tofacitinib, among others.