Arthritis Drugs

Question 1

What is osteoarthritis?

Answer 1

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

Question 2

What is rheumatoid arthritis?

Answer 2

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

Question 3

Where is the site of action for NSAIDs?

Answer 3

COX

Question 4

What is the difference between COX 1 and COX 2?

Answer 4

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

Question 5

List the actions of NSAIDs

Answer 5

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

Question 6

What are the actions of aspirin?

Answer 6

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

Question 7

How many patients respond to aspirin?

Answer 7

60%

Question 8

What are the side effects of aspirin?

Answer 8

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

Question 9

Why does aspirin produce side effects?

Answer 9

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

Question 10

Name the COX2 selectivity drugs:

Answer 10

Meloxicam, Rofecoxib, Celecoxib, Etoricoxib

Question 11

What is an alternative strategy to using aspirin?

Answer 11

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!!

Question 12

Paracetamol…

Answer 12

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

Question 13

Side effects of paracetamol

Answer 13

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

Question 14

What type of drugs are use to control Osetoarthritis?

Answer 14

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

Question 15

What is Strontium Ranetate?

Answer 15

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

Question 16

What is Glucosamine Sulphate?

Answer 16

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

Question 17

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

Answer 17

NSAIDS/Opioid Analgesics
Glucocorticoids 
Immunosuppresants 
DMARDs
Anticytokines

Question 18

What are the main actions of glucocorticoids?

Answer 18

Metabolic effects
Anti-inflammatory
Immunosuppressive

Question 19

What are the actions of mineralocorticoids?

Answer 19

Water and electrolyte balance

Question 20

Hydrocortisone/Corticosterone…

Answer 20

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

Question 21

Aldosterone

Answer 21

MC only

Question 22

Prednisolone

Answer 22

GC and MC activity

Question 23

GC activity only…

Answer 23

Dexamethasone, betamethasone, beclomethasone, budesonide

Question 24

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

Answer 24

Prednisolone, daily oral or IM injection

Question 25

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

Answer 25

Dexamethasone - Injection every 3-21 days

Question 26

What are the actions of glucocorticoids in RA?

Answer 26

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

Question 27

Side effects of oral corticosteroids?

Answer 27

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

Question 28

What are Disease Modifying Antirheumatoid Drugs? (DMARDs)

Answer 28

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

Question 29

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

Answer 29

Sulfasalazine.

Question 30

How does Sulfasalazine work?

Answer 30

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

Question 31

What are the side effects of Sulfasalazine?

Answer 31

GI upset, headache, skin reactions, leukopenia.

Question 32

What is Penicillamine?

Answer 32

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

Question 33

Side effects of Penicillamine?

Answer 33

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

Question 34

What are Gold Compounds and give the names of 2?

Answer 34

Type of DMARD. Sodium aurothiomalate and Auranofin

Question 35

What does Auranofin do given orally?

Answer 35

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

Question 36

Side effects of gold compounds?

Answer 36

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

Question 37

Types of Anti-Malarials?

Answer 37

Chloroquine/Hydroxychloroquine

Question 38

What do anti-malarials do?

Answer 38

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

Question 39

Side effects of anti-malarials?

Answer 39

N&V, dizziness, blurring of vision

Question 40

What are Anticytokine drugs?

Answer 40

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

Question 41

Types of anticytokine drugs?

Answer 41

Etenercept, infliximab, rituximab, abatacept

Question 42

Side effects of anticytokine drugs?

Answer 42

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

Question 43

Ciclosporin...

Answer 43

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

Question 44

Side effects of Ciclosporin?

Answer 44

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

Question 45

Azathioprine...

Answer 45

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

Question 46

Methotrexate...

Answer 46

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

Question 47

Side effects of Methotrexate?

Answer 47

Blood dyscrasias, liver cirrhosis, folate deficiency.

Question 48

Leflunomide...

Answer 48

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

Question 49

Side effects of Leflunomide?

Answer 49

Diarrhoea, alopecia, increased liver enzymes.

Question 50

What is cyclophosphamide?

Answer 50

Immunosuppressant. Prodrug.