Osteoarthritis Case Drugs

Question 1

Glucosamine & Chondroitin

Answer 1

Mechanism:
- Glucosamine encourages chondrocytes to make and secrete ECM components by supplying them with the molecules to produce aggrecan. ​
- Bypasses glucosamine bottleneck.​
- Chondroitin sulphate – terminal metabolite of glucosamine and part of aggrecan. ​
- ‘Chondroprotectives’ - strengthen and restore cartilage.

Effects:
Reduced Pain
Increased Mobility
Reduced risk of joint replacement.

Side Effects:
Not NICE recommended, mixed results, potentially no significant benefit.

Question 2

Rosehip Extract & Circumin

Answer 2

Mechanism:
- Osteoarthritis involves ROS, which induce oxidative stress signalling, leads to breakdown of ECM and death of chondrocytes – joint erosion.
- Rosehip contains a lot of antioxidants, reduces ROS levels.
- Circumin also scavenges ROS.
- Also reduces histamine release and increases cortisol release – anti-inflammatory effects.
- Can also inhibit NFκB (inflammation) and PGE2 production (pain and inflammation).

Effects:
Reduced cartilage breakdown.
Increased Mobility
Anti-Inflammatory

Side Effects:
Constipation/Diarrhoea
Allergic Reactions
Heartburn

Question 3

Non-steroidal anti-inflammatory drugs

Answer 3

3 key properties- analgesic (pain relief), anti-pyretic (reduces fever), anti-inflammatory.

○Non-selective NSAID, inhibits COX1 and COX2 enzymes. Selective inhibits COX2.
○COX2 catalyses production of prostaglandins (esp. PGE2) from arachidonic acid.
○COX1 has various effects and important in homeostasis (e.g. protection of gastric mucosa and haemostasis,) so non-selective NSAIDs can have a lot of unexpected side effects.
○Prostaglandins are normally involved in inflammation and bind to prostaglandin receptors on sensory neurones causing depolarisation.
○Drug binds COX active site, competitively inhibiting arachidonic acid binding = no prostaglandin production = anti-inflammatory effects.

Side Effects:
○GIT Reactions- ppi’s taken with NSAID’s as prostaglandin E2 is inhibited so can’t regulate stomach acid production
○CV Reactions
○Pulmonary Reactions
○Renal Insufficiency