Anti-inflammatory drugs Flashcards
How is hereditary angioedema (HAE) treated?
- B2 antagonists
- Kallikrein antagonists
What is a selective bradykinin B2 receptor inhibitor?
Icatibant
What is a kallikrein inhibitor?
Ecallantide
What is the purpose of TrkA inhibition?
Treatment of inflammatory pain by NGF.
What is a TrkA antagonist?
Tanezumab
What is the mechanism of action of tanezumab?
- Monoclonal antibody that binds to and inhibits TrkA
- Prevents NGF mediated pain sensitisation
What is the mechanism of action of bufexamac?
Inhibition of LTA4 hydrolase
What is the therapeutic use of bufexamac?
Anti-inflammatory
What is the mechanism of action of zafirlukast?
CysLT1 receptor antagonist
What is the mechanism of action of zileuton?
5-lipoxygenase inhibitor
What is the therapeutic use of zafirlukast and zileuton?
Treatment of asthma
What is the function and mechanism of action of lexipafant?
- Function: Treatment of inflammatory conditions
- Mechanism: PAF receptor inhibitor
What is the function and mechanism of action of rupatadine?
- Function: Treatment of fever and urticaria
- Mechanism: Recombinant histamine H1 and PAF receptor antagonist
What is the mechanism of action of most NSAIDs?
Enters hydrophobic tunnel and forms H-bond with Arg120 to prevent entry of arachidonic acid (reversible inhibition)
What are COX-2 selective drugs?
- Etoricoxib
- Rofecoxib
What are the actions of aspirin on platelets?
- Irreversibly inhibits COX 1 in both platelets and endothelial cells.
- Prevents platelet production of TXA2 (promotes platelet aggregation and vasoconstriction).
- Prevents endothelial cell production of PGI2 (inhibits platelet aggregation and promotes vasodilation).
- Endothelial cells can re-synthesise COX1 but platelets can’t.
What is the mechanism of action of eicosapentanoic acid in fish oil in decreasing heart attacks?
- Eicosapentanoic acid results in production of TXA3 and PGI3.
- TXA3 has much less potent pro-platelet aggregation effect compared to TXA2.
- PGI3 has only slightly less potent anti-platelet aggregation effect compared to PGI2.
- Balance tipped in favour of anti-aggregation PGI3 and thus risk of thrombo-embolism decreased.
How can gastric side effects of NSAIDs by countered?
- Use in combination with synthetic PGE2 analogue such as misoprostol
- Use with proton pump inhibitor such as omeprazole
How can paracetamol overdose be treated?
Acetylcysteine and methionine to increase hepatic glutathione production