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Pharmocolgy > P8: Allergies and Anti-inflammatories > Flashcards

P8: Allergies and Anti-inflammatories Flashcards

1
Q

What are the main categories of anti-inflammatory drugs?

A
  • NSAIDs
  • Glucocorticoids
  • Anti-histamines
  • Anti-rheumatics
  • Biologics
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2
Q

Name some NSAIDs (3)

A
  • Aspirin
  • Ibuprofen
  • Diclofenac
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3
Q

Name some Glucocorticoids (3)

A
  • Betamethasone
  • Hydrocortisone
  • Prednisolone
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4
Q

Name some Anti-histamines (2)

A
  • Loratidine

- Acrivastine

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5
Q

Name some Anti-rheumatics (3)

A
  • Methotrexate
  • Azathioprine
  • Ciclosporin
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6
Q

Etanerecpt is an example of which type of anti-inflammatory drug

A

Biologics

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7
Q

NSAID mechanism of action

A

Primary mechanism of action is through inhibition of cyclo-oxygenase (COX)

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8
Q

COX breaks down Arachidonic Acid into which 3 metabolites?

A
  • Thromboxanes
  • Prostacylin
  • Prostaglandins
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9
Q

Role of Thromboxanes

A

Promote thrombosis and vasoconstriction

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10
Q

Role of Prostacyclin

A
  • Limits thrombosis

- Promotes vasodilation

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11
Q

Role of Prostaglandins

A
  • Vasodilators

- Stimulate bronchial, GI tract, uterine smooth muscles

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12
Q

Where are COX-1 expressed?

A

COX-1 expressed in virtually all tissues

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13
Q

Where are COX-2 expressed?

A

COX-2 has very limited constitutive expression

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14
Q

When are COX-2 upregulated?

A

Rapidly upregulated during inflammation by cytokine stimulation

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15
Q

Name some of the many actions of Glucocorticoids (7)

Many actions but bottom line is that these all work together to stop inflammation

A
  • Induction of neutrophil apoptosis
  • Promotion of macrophage phagocytosis
  • Suppression of T cell activity
  • Direct small vessel vasoconstriction
  • Suppression of cytokine release
  • Decreased production of prostanoids and leukotrienes
  • Reduced production of ROS from neutrophils and macrophages
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16
Q

What are the two isoforms of Glucocorticoid Receptors?

Which binds to cortisol?

A
  • GRα and GRβ

- Only GRα binds cortisol

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17
Q

What are the 5 major side effects of Glucocorticoid

A
  • Osteoporosis
  • Hypertension
  • Mood disorders
  • Hyperglycaemia
  • Adrenal suppression
18
Q

Give an example of Type I hypersensitivity

only Type I is an allergy

A

Asthma/Atopy/Anaphylaxis

19
Q

Give an example of Type II hypersensitivity

A

Myasthenia gravis

20
Q

Give an example of Type III hypersensitivity

A

Lupus

inflammation in joints

21
Q

Give an example of Type IV hypersensitivity

A

Contact dermatitis/rheumatoid arthritis/coeliac disease/MS

22
Q

What is a major effector of Type I hypersensitivity

A

Histamine acting on H1 receptors

23
Q

What is Anaphylaxis?

A
  • Severe, life-threatening systemic allergic reaction
  • Systemic release of histamine and cytokines
  • Bronchoconstriction and vasodilation causing hypotension
24
Q

What is Rheumatoid Arthritis?

A

Chronic autoimmune disease affecting the joints

25
Q

What are the two therapies for Rheumatoid Arthritis

A
  • Disease modifying anti-rheumatic drugs (DMARDs)

- Biologic therapies (antibodies)

26
Q

What does the COX1 cyclo oxygenase do

A
  • Produces prostaglandins responsible for homeostatic function as well as during inflammation
  • Maintains gastric mucosa integrity
  • Regulates renal blood flow
27
Q

What inhibits COX1 and COX2 enzymes and what side effects do they have?

A

Older NSAIDs like aspirin, ibuprofen and diclofenac

GI side effects - gastric ulcers, duodenal bleeding

28
Q

Name some selective COX2 inhibitors and what side effects they have

A

Celecoxib and etoricoxib

Fewer effects on gastric mucosa
Cardiovascular damage - block of protective PGI2

29
Q

What are the most powerful anti-inflammatory agents

A

Glucocorticoids, lots of side effects

30
Q

What happens after glucocorticoid receptors bind to cortisol

A

They translocate to the nucleus to activate and repress gene transcription

31
Q

Steroids that activate the glucocorticoid receptor are commonly also mineralocorticoid receptor agonists, name some GR selective steroids

A

Prednisolone - orally active, high potency

Betamethasone + dexamethasone - long action duration, high potency insignificant MR effects

Hydrocortisone - moderate effectiveness, topical administration due to weak MR effects

32
Q

Give examples of histamines and their characteristics

A

Acrivastine, Cetirizine, loratadine - orally active, long half life, no sedation

33
Q

Name some older anti histamines and their characteristics

A

Promethazine - strong sedative effect due to CNS actions

Diphenhydramine - sedative, anti muscarinic effects used for motion sickness

Mepyramine - topical cream for insect bites, marginally effective

34
Q

What are some treatments for anaphylaxis

A
  • Administration of adrenaline, i.m., at 5 min intervals
  • administration of oxygen
  • administration of anti histamines, slow i.v. or i.m. injection
35
Q

What is the purpose of DMARDs and where are they usually used

A

Diverse collection of drugs that target aspects of the inflammatory response in arthritis, used in many autoimmune diseases Egypt, lupus, crohn’s, myasthenia gravis

36
Q

How does Azathioprine work and what are its side effects

A

Orally active prodrug, converted to mercaptopurine
Integrates into DNA, halts replication, preventing immune cell proliferation

Side effects: nausea/vomiting, carcinogen, birth defects

37
Q

How does Methotrexate work and what are its side effects

A

Inhibits enzymes in purine metabolism, preventing immune cell activation
Prevents expression of T cell adhesion molecules, limiting access to tissue

Side effects: hepatotoxic, leukopenia, teratogen, abortifacient

38
Q

How does Ciclosporin work and what are its side effects

A

Blocks activity of calcineurin, an enzyme required for cytokine production

Side effects: kidney damage, mild hepatotoxicity, gum hypertrophy

39
Q

What are Anti-TNFalpha therapies used for and how do they work

A

Highly effective in treating rheumatoid arthritis, Crohn’s disease, ulcerative colitis

Humanised antibodies, or antibody components that target the cytokine TNFα

40
Q

name some anti TNFalpha therapies and their mechanisms

A

Bind TNF and prevent its activity

Etanercept
TNF receptor fused to an antibody stem

Infliximab, adalimumab
Anti-TNFα antibodies

Pharmocolgy (22 decks)

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