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
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
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
muscarine
type of alkaloid
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
quaternary
type of NH4 group
-cannot be given orally because it has a short duration of action (easily hydrolyzed because water- loving)
quaternary
type of NH4 group
-no penetrability of CNS because easily hydrolyzed in GIT, cannot reach CNS
quaternary
unlike choline esters, they don’t have parent drugs because most of them are derived from plants
type of direct-acting drug
alkaloids
type of alkaloid – cigarette -isolated as a liquid -easily absorbed across the skin -risk is the same for active and passive smoker
nicotine
type of alkaloid
isolated from mushrooms
Muscarine