Natural product derived drug for pain

Question 1

What class do cocaine belongs to?

Answer 1

Tropane alkaloid

Question 2

Removal of carbomethoxy group in cocaine gives? What is eliminated?

Answer 2

Benzoltropine (tropacocaine)
Eliminated addiction liability

Question 3

How is procaine synthesised?

Answer 3

Replacement of tropine with amine
- Lacked local and systemic toxicity

Question 4

Lidocaine is the ___________ of local anaesthetic agent.

Answer 4

First amide-type

Question 5

Lidocaine is less _____ than isogramine.

Answer 5

Allergenic

Question 6

Lidocaine is more ______ than isogramine.

Answer 6

Stable in water

Question 7

Which SAR strategy was adopted to give lidocaine from isogramine?

Answer 7

Structural simplification

Question 8

SAR of cocaine-derived local anaesthetic must have which 3 portions?

Answer 8

1. Lipophilic/aromatic part
2. Intermediate chain should carry ester or amide, followed by 1-3 C chain
3. Hydrophilic portion (secondary or tertiary amine or N is part of heterocycle)