PA30325 2. Medicines Design Flashcards
1
Q
What are the Pro-drugs and Soft-drugs?
A
Pro-drugs
- compounds that are inactive until activated by metabolism
Soft-drugs
- active species that are deactivated by metabolism
2
Q
Why do we use soft-drugs?
A
- to reduce duration of action
- to reduce side effects/toxicity by limiting how broadly distributed the drug is
- by having predictable metabolism to inactive species you reduce the risk of metabolism leading to multiple metabolites with varying biological activities
3
Q
What are the ideal soft-drugs compounds?
A
- cannot modify the known active molecule too much, or you risk losing activity
- introduction of the metabolically sensitive group should not overly change the physical, steric and electronic properties of the lead
- ideally looking for a metabolisable isostere (similar shape and often electronic properties)
- most often used are esters, carbamates, and less often quaternary nitrogens
4
Q
Describe local anaesthetic action
A
- reversible binding to, and inactivation of, sodium ion channels
- highest affinity for the open state of the channel
5
Q
How do sedative-hypnotics act?
A
- act by enhancing the inhibitory actions of GABA.a receptors