Inhibition Flashcards
4 forms of inhibition
Competitive
Non-competitive
Uncompetitive
Irreversible (suicide)
3 types of competitive inhibition and examples
Non substrate (quinidine for 2D6)
Other substrate (diazepam for 2C19)
Mixed (reacts with Fe in haem group)
What is ketaconozole inhibition
Mixed competitive
Replaces with triazoles - more anti fungal activity, less inhibition
Mechanism of non-competitive and example
Allosteric site binding
St John’s wort on 2D6 in vitro
Mechanism of uncompetitive
Rare
Binds ES complex
Increase affinity of binding but inhibitor makes nonfunctional
Mechanism of irreversible and example
Bind active site for long time
Can change shape of active site
Grapefruit juice on 3A4
Use of inhibitor for alcoholism
Disulphiram
Clinical consequence of inhibitor
Grapefruit juice causes build up of terfenadine
- cardiac arrhythmias