Cholinergic mexhanism Flashcards
(19 cards)
Semisynthetic conjugate of Anisotropine
Clinidium
Synthetic conjugate of Glycopyrrolate
Dicyclomine
Synthetic conjugate of Homatropine
Hexocyclium
Semisynthetic conjugate of ipatropium
Isopropamide
Synthetic conjugate of propantheline
Oxybutynin
Semisynthetic conjugate of tolterodine
Tridihexethyl
Antihistamines are known to antagonize cholinergic agents T/F
T
Natural group of alkaloids
- Atropine
- Scopolamine
Small diesel if cholinergic antagonists cause
Decreased heart rate
Decreased tremors
Large doses of cholinergic antagonists cause
- Increased heart rate
- Drowsiness, hallucinations, Dilated pupils (mydriasis)
Cholinergic antagonists are used in the treatment of Parkinson’s disease by
Decreasing muscle rigidity
Decreasing power tremors
Atropine is used primarily for
Cardiovascular disorders
Cholinergic antagonists are used to treat (respiratory)
Chronic bronchitis
Asthma
Cholinergic antagonists are used to treat (gastrointestinal/urinal)
Peptic ulcer
Irritable bowel disease
GI hypersecretory states
Choline esters act at all sites, like acetylcholine but are resistant to degradation by
ACETYLCHOLINESTERASES
Functional groups that make up Acetycholine
Acyl group
Ethylene Bridge
Omium group
What groups can be substituted into the acyl group to form a more potent compound
Primary amine
Ether/Ketone
Aromatic
Modifications of ethylene bridge
- Replacement of H with methyl group increases cholinergic activity (with larger group than methyl decreases activity)
- Substitution of methyl group at beta carbon acts selectively on muscarinic receptors
Modifications in omium group
- Primary,Secondary and Tertiary amines are less active than quaternary amines
- If methyl group is replaced by ethyl group or larger ethyl group it produces INACTIVE compounds
- Nitrogen can be replaced by arsenic, antimony, phosphorus or sulphur atom
