Arthritis Drugs Flashcards

1
Q

What is osteoarthritis?

A

Inflammation of the bone, caused by wear and tear, ageing, trauma, disease. Affects synovial joints and involves loss of cartilage and bone.

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2
Q

What is rheumatoid arthritis?

A

An auto-immune disorder, inflammation flowing in a stream, affects other tissues.

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3
Q

Where is the site of action for NSAIDs?

A

COX

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4
Q

What is the difference between COX 1 and COX 2?

A

COX 1 = responsible for the protection of GI mucosa and production of PGs for platelet aggregation.
COX2 = PGE2 causes vasodilation and inflammatory effects

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5
Q

List the actions of NSAIDs

A

Inhibits actions of prostaglandins
Analgesic = reduce sensitivity of neurone
Anti-inflammatory = reduce vasodilation and reduce tissue damage

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6
Q

What are the actions of aspirin?

A

Inhibits NFkB expression - reduces transcription of genes for inflammatory mediators
Pain relief is immediate
Rapidly absorbed in stomach
Displaces warfarin bound to plasma proteins
Increased plasma warfarin = risk of bleeding

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7
Q

How many patients respond to aspirin?

A

60%

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8
Q

What are the side effects of aspirin?

A
Gastric Ulcers
Impaired coagulation
GI bleeds in the elderly 
Risk of CV events 
May induce asthma attacks
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9
Q

Why does aspirin produce side effects?

A

May inhibit COX1 as well as COX2, COX1 is responsible for the protection of GI mucosa and PGs inhibit platelet aggregation

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10
Q

Name the COX2 selectivity drugs:

A

Meloxicam, Rofecoxib, Celecoxib, Etoricoxib

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11
Q

What is an alternative strategy to using aspirin?

A

Misoprostol: synthetic PG. Used alongside NSAIDs, preserves mucous lining of GI tract, protects against ulceration. Side effects = diarrhoea, vaginal bleeding, precautions in women of child bearing age!!

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12
Q

Paracetamol…

A

Not an NSAID!!!
Analgesic and Antipyretic effects
Suppresses PG production
May involve COX1

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13
Q

Side effects of paracetamol

A

Few side effects
Chronic use = kidney damage
Toxic doses = liver damage

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14
Q

What type of drugs are use to control Osetoarthritis?

A
Paracetamol - regular dosing and NSAID 
Topical NSAID or Capsaicin 
Opioid Analgesic 
Corticosteroid injection
Joint replacement surgery
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15
Q

What is Strontium Ranetate?

A

Drug used to treat osteoarthritis, promotes osteoblast differentiation, reduces pain.
Side effects: increased risk of MI and thrombotic events.

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16
Q

What is Glucosamine Sulphate?

A

Drug used to treat osteoarthritis. Constituent of ECM. Present in cartilage and synovial fluid.

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17
Q

What type of drugs are used to treat Rheumatoid arthritis (RA)?

A
NSAIDS/Opioid Analgesics
Glucocorticoids 
Immunosuppresants 
DMARDs
Anticytokines
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18
Q

What are the main actions of glucocorticoids?

A

Metabolic effects
Anti-inflammatory
Immunosuppressive

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19
Q

What are the actions of mineralocorticoids?

A

Water and electrolyte balance

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20
Q

Hydrocortisone/Corticosterone…

A

Show both MC and GC activities
short acting - 1-12 hours
twice daily cream or IM injection

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21
Q

Aldosterone

A

MC only

22
Q

Prednisolone

A

GC and MC activity

23
Q

GC activity only…

A

Dexamethasone, betamethasone, beclomethasone, budesonide

24
Q

Which steroid is intermediate acting (12-36 hours)?

A

Prednisolone, daily oral or IM injection

25
Q

Which steroid is long-acting? (36-55 hours)

A

Dexamethasone - Injection every 3-21 days

26
Q

What are the actions of glucocorticoids in RA?

A

decrease transcription of pro-inflammatory cytokines
decrease circulating lymphocytes
increase synthesis of anti-inflamm. proteins

27
Q

Side effects of oral corticosteroids?

A

buffalo hump, moon face, hypertension, increased abdo fat, thinning of skin, muscle wasting, poor wound healing, osteoporosis

28
Q

What are Disease Modifying Antirheumatoid Drugs? (DMARDs)

A

Drugs with unrelated structures and diff. mechanisms of action
Therapy only started upon definite diagnosis of RA

29
Q

What is the common 1st choice of DMARD in the UK?

A

Sulfasalazine.

30
Q

How does Sulfasalazine work?

A

Thought to act by scavenging free radicals produced by neutrophils.
Causes remission in active RA.
Given as enteric-coated tablets

31
Q

What are the side effects of Sulfasalazine?

A

GI upset, headache, skin reactions, leukopenia.

32
Q

What is Penicillamine?

A

Type of DMARD. 75% of patients respond but effects take weeks. Decreases IL-1 and fibroblast proliferation which decreases the immune response. Given orally.

33
Q

Side effects of Penicillamine?

A

rashes, stomatitis, anorexia, taste disturbance, feve, N and V

34
Q

What are Gold Compounds and give the names of 2?

A

Type of DMARD. Sodium aurothiomalate and Auranofin

35
Q

What does Auranofin do given orally?

A

Inhibits induction of IL-1 and TNF so reduced pain and joint swelling.

36
Q

Side effects of gold compounds?

A

skin rashes, flu-like symptoms, mouth ulcers, blood disorders

37
Q

Types of Anti-Malarials?

A

Chloroquine/Hydroxychloroquine

38
Q

What do anti-malarials do?

A

increase PH of intracellular vacuoles - interferes with antigen-presenting.

39
Q

Side effects of anti-malarials?

A

N&V, dizziness, blurring of vision

40
Q

What are Anticytokine drugs?

A

Treat RA. Engineered recombinant antibodies. Given S/c or IV

41
Q

Types of anticytokine drugs?

A

Etenercept, infliximab, rituximab, abatacept

42
Q

Side effects of anticytokine drugs?

A

TB , Hep B, Herpes, opportunistic infection, nausea, ab pain, worsening heart failure, hypersensitivity

43
Q

Ciclosporin…

A

An immunosuppresant. Inhibits IL-2 gene transcription. Poorly absorbed orally.

44
Q

Side effects of Ciclosporin?

A

Nephrotoxicity, Hepatotoxicity, Hypertension, N&V, GI problems

45
Q

Azathioprine…

A

Immunosuppresant. Interferes with purine metabolism. Depresses immune reactions. Suppression of bone marrow.

46
Q

Methotrexate…

A

Immunosuppresant. Folic acid antagonist - inhibits DNA synthesis. Inhibits T cell activation.

47
Q

Side effects of Methotrexate?

A

Blood dyscrasias, liver cirrhosis, folate deficiency.

48
Q

Leflunomide…

A

Immunosuppresant. Inhibitor of activated T cells. Well absorbed orally.

49
Q

Side effects of Leflunomide?

A

Diarrhoea, alopecia, increased liver enzymes.

50
Q

What is cyclophosphamide?

A

Immunosuppressant. Prodrug.