WK8- Cholinergic Medchem

what is a non selective drug

it means its acts on multiple receptors, rather than target 1 receptor

• this means an increase in side effects because the drug effects more than just the intended side effect

what is the biosynthesis of acetylcholine

1. acetyl-COA+ Choline is converted to acetylcholine using the enzyme choline acetyl transferase

why cant we use ACh directly as a drug

1. it is hydrolysed in the stomach

2. It is broken down in the blood by AChE

3. it is also non selective - meaning it binds to both muscarinic + nicotinic which increases side effects

what are natural muscarinic antagonist

they are plant derived compounds that block muscarinic receptors

what is atropine

it is a muscarinic antagonist used for pupil dilation before an exam

what is hyoscyamine

it is a muscarinic antagonist which is an active form of atropine

what is hyoscine

it is a muscarinic antagonist which is used for motion sickness

what is scopolamine

it is a muscarinic antagonist used to treat motion nausea & vomiting

why are antagonist much larger than agonist

1. because muscarinic agonist MUST fit into the active site to activate

2. Antagonist hare larger as they have bulky groups that clog the receptor which prevents activation

what is a semi-synthetic antagonist

it is a natural molecule which is modified to improve drug action

what is hyoscine butylbromide

it is a semisynthetic antagonist used for gut spasm

what is ipratropium bromide

an semi-synthetic antagonist used for bronchodilator in asthma(short-acting)

what is tiotropium bromide

it is a semi-synthetic antagonist used as a bronchodilator in COPD (long-lasting)

what is propantheline bromide

it is a antagonist used for urinary incontinence

what is procyclidine chloride

an antagonist used for Parkinson disease