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CHHD > Anti-inflammatory and immunosuppressant drugs > Flashcards

Anti-inflammatory and immunosuppressant drugs Flashcards

1
Q

What classes of Anti-inflammatory drugs are there

A
  • Steroidal anti-inflammatory drugs
  • Non-steroidal anti-inflammatory drugs (NSAIDs)
  • Traditional or “non-selective” NSAIDS
  • COX-2 inhibitors
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2
Q

Give an example of steroidal anti-inflammatory drugs

A

Corticosteroids - prednisolone

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3
Q

Give an example of NSAIDs

A

Acetyl salicylic acid - aspirin

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4
Q

Give an example of Traditional or “non-selective” NSAIDs

A
  • Ibuprofen
  • Naproxen
  • Diclofenac
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5
Q

Give an example of COX-2 inhibitors

A
  • Celecoxib
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6
Q

What is the general mechanism of NSAIDs

A

They inhibit the production of Prostaglandins from arachidonic acid by COX enzymes

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7
Q

What effects does aspirin have

A

Analgesic, anti-inflammatory and anti-thrombotic effects

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8
Q

Where is aspirin metabolised and excreted

A

Metabolised in Liver

Excreted in Kidneys

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9
Q

In which patients should you avoid using aspirin

A

In patients with severe liver disease and on dialysis

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10
Q

What does aspirin act on

A

Permanently affects platelet cohesiveness for the entire life span of the platelets

Affects primary homeostasis ~ prolonged bleeding time

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11
Q

What is aspirin’s effect on platelet count, PT/INR and APTT

A

Nothing

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12
Q

What general effects do traditional/non-selective NSAIDs have

A

Analgesic, anti-inflammatory and antipyretic actions

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13
Q

What do traditional/non-selective NSAIDs inhibit

A

COX-1 and COX-2

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14
Q

What does the inhibition of COX-1 and COX-2 result in

A
  • Inhibition of COX-1 = accounts for NSAIDs side effects and toxicity
  • Inhibition of COX-2 = accounts for anti-inflammatory actions
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15
Q

What are the side effects of traditional/non-selective NSAIDs

A
  • Gastric irritability
  • Platelet dysfunction ~ temporarily affect platelet cohsiveness
  • Acute renal failure ~ short term, low dose use does not cause this effect
  • Leukotriene overproduction ~ bronchoconstriction ~ avoid in asthmatic patients
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16
Q

What general effects do selective NSAIDs or COX-2 inhibitors have

A
  • Analgesic
  • Anti-inflammatory
  • Anti-pyretic
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17
Q

Give examples of selective NSAIDs or COX-2 inhibitors

A

Celecoxib

Etoricoxib

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18
Q

What do selective NSAIDs or COX-2 inhibitors affect

A

Promotes platelet aggregation - avoid use in patients with significant history of atherosclerosis

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19
Q

Where are selective NSAIDs or COX-2 inhibitors metabolised and excreted

A

Metabolised in the liver

Excreted in the kidneys

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20
Q

Name some types of anti-inflammatory/immunosuppressive drugs

A

Antimitotic agents
Calcineurin inhibitors
Biological response modifiers

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21
Q

Name some kinds of anti-inflammatory drugs

A

Corticosteroids

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22
Q

Name some kinds of anti-mitotic agents

A
  • Azathioprine
  • Cyclophoshphamide
  • Chlorambucil
23
Q

Name some types of calcineurin inhibitors

A
  • Ciclosporin

- Tacrolimus

24
Q

Name some types of biological response modifiers

A
  • Adalimumab
  • Infliximab
  • Etanercept
25
What actions do corticosteroids carry out in order to reduce inflammatory reaction
- Limiting capillary dilation and permeability of the vascular structures - Restricts accumulation of polymorphonuclear leukocytes and macrophages and reduces the release of vasoactive kinins
26
What are the indications for use of corticosteroids
- Primary and secondary arden-cortical insufficiency - Psoriatic arthritis - Rheumatoid arthritis - Ankylosing spondylitis - Bursitis - Acute gouty arthritis - Systemic lupus erythematosus - Leukaemias, lymphomas, thrombocytopenia purpura and autoimmune haemolytic anaemia - Coeliac, UC and liver disorders
27
What are the potential endocrine side effects of corticosteroid use
Adrenal insufficiency weight gain diabetes mellitus
28
What are the potential gastrointestinal side effects of corticosteroid use
Peptic ulceration with perforation and haemorrhage Dyspepsia Abdominal distension Oesophageal ulceration
29
What are the potential psychiatric side effects of corticosteroid use
Confusion Irritability Delusions and suicidal thoughts
30
What are the potential musculoskeletal side effects of corticosteroid use
Osteoporosis | Proximal myopathy
31
What are the potential ophthalmic side effects of corticosteroid use
Glaucoma Cataract Blurred vision
32
What are the potential skin related side effects of corticosteroid use
Thinning of the skin Easy bruising Delayed wound healing
33
What recommendation are there for minimise the side effects of corticosteroids
- Prescribe low effective dose for the minimum time possible - Take corticosteroids in the morning and on alternate days - Provide a steroid treatment card - Prescribe a proton pump inhibitor for GI protection in patients with high risk of GI bleed - Withdrawal from long-term treatment, must be gradual - Be alert to signs and symptoms of adrenal insufficiency and prescribe steroid cover if needed
34
What are some withdrawal strategies for corticosteroids
- Short courses can be stopped abruptly Gradual withdrawal for people: - whose disease is unlikely to relapse and who have received more than 3 weeks of corticosteroid treatment - history of previous long term therapy - other possible causes of adrenal suppression, alcohol, stress - Had more than 40mg of prednisolone daily or equivalent for more than a week
35
What kind of drug is azathioprine
Immunosuppressive and antimetabolite drug
36
What is azathioprine converted into in the body
6-mercaptopurine
37
Describe the basic mechanism of azathioprine
Inhibits purine and DNA synthesis needed for the proliferation of cells, especially leukocytes and lymphocytes
38
What disease is azathioprine used to manage
- Rheumatoid arthritis - Preventing renal transplant rejection - Crohn's disease - Recurrent oral ulceration - Behcet's disease - Colitis
39
What are the side effects of azathioprine
- Myelosuppression - Hepatotoxicity - Leukopenia - Thrombocytopenia - Infections - Lymphoproliferative disorders - Teratogenicity
40
What are the clinical signs of toxicity
- Rash - Oral ulceration - Abnormal bruising - Severe sore throat
41
What kind of drug is cyclosporin and what does it act on
- Immunosuppressant with specific action on T-lymphocytes
42
Describe the mechanism of cyclosporin
- Binds to immunophilins, inhibits calcineurin that is normally responsible for activating transcription of IL-2 - Inhibits lymphokine production and interleukin release and preferentially inhibits t-helper and killer t-cells
43
Where is cyclosporin metabolised
Liver
44
When is cyclosporin used
Used in immunosuppression for prophylactic treatment of: - organ transplant - rheumatoid arthritis - severe psoriasis
45
What are the potential side effects of ciclosporin
- Hypertension - Nephrotoxicity - Neurotoxicity - Gingival hypertrophy/hyperplasia - Lymphoproliferative disorders - Malignancies - Teratogenicity
46
What possible drug interactions are there for ciclosporin
- Antibiotics: Macrolides increases toxicity - Antifungal: Fluconazole, Miconazole increase toxicity - Analgesic: avoid use of NSAIDs with ciclosporin because they promote nephrotoxicity
47
What kind of drug is mycophenolate mofetil
Antibiotic substance | Immunosuppressive agent
48
Describe the basic mechanism of mycophenolate mofetil
- Blocks de novo biosynthesis of purine nucleotides by inhibiting inosine monophosphate dehydrogenase - Prevents the proliferation of T cells, lymphocytes and the formation of antibodies from B cells
49
How is mycophenolate mofetil usually used
Prophylaxis of organ rejection, often used in combination with ciclosporin and prednisolone
50
What are the potential side effects of mycophenolate mofetil
- Fever - Chills - Hyperglycaemia - Hypertension - Easy bruising/bleeding - Skin reactions - Abdominal pain; nausea and vomiting; dyspepsia; diarrhoea; oesophagitis; gastritis; GI bleed - Increased risk of infection - Leukopenia, thrombocytopenia - Depression
51
What do biological response modifiers
- Block inflammation and immune responses - Act directly to neutralise specific target immune components - Less immunosuppressive compared to conventional therapy that broadly cause immunosuppression
52
What are biological response modifiers used for in the treatment of
- Rheumatoid arthritis - Ankylosing spondylitis - Psoriasis - Crohn's disease - Ulcerative colitis - Malignancies - Vesciulo-bullous disease - Lichen planus - Behcets disease
53
How are biological response modifiers administered
Injection or infusion
54
What are the most commonly used biologics and give examples
TNF-alpha inhibitors | Adalimumab, Infliximab, Etanercept

CHHD (27 decks)

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