pharmaco - chapter 6 Flashcards
type of cholinomimetic drug
• Inhibiting the hydrolysis of endogenous Ach
Indirect-acting
type of cholinomimetic drug
• Binding/activate cholinoceptors
Direct-acting
4 impt choline esters
acetycholine
carbachol
betanechol
methacholine
type of direct-acting drug
- Permanently charged quaternary NH4 group
choline ester
type of direct-acting drug
- Relatively insoluble in lipids
- Poorly absorbed
choline ester
type of direct-acting drug
-Hydrolyzed in the GIT
choline ester
type of direct-acting
Hydrophilic
choline ester
type of direct-acting drug
Poorly distributed in the CNS
choline ester
type of choline ester
- Addition of methyl CH3
- 3x more resistant to hydrolysis compared to Ach
METHACHOLINE
TYPE OF DIRECT-ACTING DRUG
- Act mostly with muscarinic receptors
(muscarine, pilocarpine)
- Act with nicotinic receptors(nicotine, lobeline)
ALKALOIDS
4 impt alkaloids
nicotine
pilocarpine
lobeline
muscarine
type of alkaloid
- Liquid
- Sufficiently lipid-soluble to be absorbed across
the skin
NICOTINE
type of alkaloid
- Quaternary amine
- Less completely absorbed from the GIT
- Toxic when ingested
- Eg, in certain mushrooms, it even enters the brain
muscarine
type of alkaloid
- Plant derivative
- Similar to nicotine
LOBELINE
type of Ach
– methyl group at α carbon was changed to amino group
c. Carbachol
type of Ach
– addition of methyl group at β carbon, replacement of methyl group with amino group at α carbon
Betanechol
type of Ach
addition of methyl group at the β carbon
methacholine
type of NH4 group
- no more electrons to share, cannot attach
- becomes insoluble in lipids
quaternary