Pharmacology I: Block 1 Cholinergic Agonists and Antagonists

Bethanechol

MOA: Muscarinic receptor agonist

Location: Bladder

Indication/Why It’s Given: Urinary Retention

Side Effects: Cholinergic Side Effects (Parasympathetic)

Pilocarpine

MOA: Muscarinic receptor agonist

Location: Eye and Salivary Glands

Indication/Why It’s Given: Glaucoma, Dry Mouth

Side Effects: Cholinergic Side Effects (Parasympathetic)

Edrophonium

MOA: Acetylcholinesterase Inhibitor (AChEi)

Location: ACh Receptors in Skeletal Muscles

Indication/Why It’s Given: Myasthenia Gravis (tx and dx), reversal of NMBs

Side Effects: Cholinergic Side Effects (when given in excess)

Pralidoxime

MOA: Reactivates Acetylcholinesterase (AChE)

Location: Skeletal Muscles

Indication/Why It’s Given: Organophosphate poisoning

Side Effects: -

Donepezil

MOA: Acetylcholinesterase Inhibitor (AChEi)

Location: CNS

Indication/Why It’s Given: Alzheimers’s

Side Effects: Cholinergic Side Effects

Atropine

MOA: Muscarinic Receptor Antagonist

Location: Heart and other organs

Indication/Why It’s Given: Treat bradycardia, Organophosphate Poisoning

Side Effects: Anticholinergic side effects (sympathetic)

Hycosamine

MOA: Muscarinic Antagonist

Location: Stomach and Lungs

Indication/Why It’s Given: To reduce bronchial and pharyngeal secretions, reduces HCl production (Tx of peptic ulcer disease) —> stop rest and digest

Side Effects: Anticholinergic side effects (sympathetic)

Scopolamine

MOA: Muscarinic antagonist

Location: Salivary Glands and Bronchi

Indication/Why It’s Given: Motion Sickness, drooling (prevents excessive salivation)

Side Effects: Anticholinergic side effects (sympathetic)

Glycopyrrolate

MOA: Muscarinic antagonist

Location: Salivary Glands

Indication/Why It’s Given: Drooling (prevents excessive salivation)

Side Effects: Anticholinergic side effects (sympathetic)

Ipratropium

MOA: Muscarinic antagonist

Location: Lungs

Indication/Why It’s Given: Treat wheezing from COPD/Asthma

Side Effects: Anticholinergic side effects (sympathetic)

Oxybutynin

MOA: Muscarinic antagonist

Location: Bladder

Indication/Why It’s Given: Urinary incontinence/overactive bladder

Side Effects: Anticholinergic Side Effects (sympathetic)

Pancuronium and Cistracurium

MOA: Non-depolarizing Neuromuscular Blocker (NMB), nicotinic receptor competitive antagonist

Location: Skeletal Muscle

Indication/Why It’s Given: For relaxation during surgery, mechanical ventilation

Side Effects: Can be reversed by AChEi

Succinylcholine

MOA: Depolarizing NMB at nicotinic receptors, technically ACh receptor agonist

Location: Skeletal muscle

Indication/Why It’s Given: For relaxation during surgery, mechanical ventilation

Side Effects: cannot be reversed by AChEi