Cholinergic Receptor Inhibitors Flashcards
Cholinergic Receptor MOA
Drugs that bind to cholinergic receptors, but do not trigger usual receptor mediated response
Types:
- Muscarinic receptor antagonists
- Ganglionic antagonists
- Neuromuscular blockers
Muscarinic Receptor Antagonist MOA
- Inhibits muscarinic functions
- Primarily affects the parasympathetic NS
excp. salivary and sweat glands
Ganglionic Blockers MOA
Block nicotinic receptors for both the sympathetic and parasympathetic ganglia. Rarely used clinically bc response is wide and unpredictable
Neuromuscular Junction Blockers MOA
- Block cholinergic transmission between motor nerve endings and nicotinic receptors on the neuromuscular end plate of skeletal muscle
- May be an agonist or antagonist
- Clinically useful during surgery as a muscle relaxant
Common Side Effects of Muscarinic Receptor Antagonists
- Blurred vision
- Confusion
- Constipation
- Urinary Retention
- Mydriasis
Atropine MOA
Muscarinic receptor antagonist via competitive inhibition
Atropine Clinical Indications
- Bradycardia
- AV Block
- IBS
- Antisecretory agent
- Ocular inflammation
- Antidote for AChesterase inhibitor poisoning
Atropine Effects on the Eye
- Eye exam relaxant
- Blocks all cholinergic activity in the eye
- Results in mydriasis, unresponsiveness to light and cycloplegia (inability to focus near vision)
Atropine Effects on the GI System
- Used as an antispasmodic to reduce activity of GI tract (relax GI)
Atropine Effects on the Urinary System
- Reduces hypermotility states of the bladder (relaxes bladder)
Atropine Effects on the Cardiovascular System
- Increase heart rate and conduction velocity
2. Causes smooth muscle relaxation
Atropine Effects on Secretory Activity
- Blocks salivary glands, decreasing secretion (used to dry secretions in upper and lower respiratory tracts prior to surgery)
- Produces xerostomia: dryness of mucous membranes
- Decreases activity of sweat and lacrimal glands
Atropine Overdose Mnemonic
- Dry as a bone: decreased secretions, sweat, and tears
- Blind as a bat: blockade of pupillary accommodation, and excessive dilation
- Red as a beet: Dilation of cutaneous vessels in upper body
- Mad as a Hatter: Inhibition of CNS muscarinic receptors with confusion and hallucinations
Benzetropine (Cogentin) MOA
Muscarinic receptor antagonist
Benzetropine (Cogentin) Treatments
- Parkinson’s Disease: blockage of muscarinic receptors may restore neurotransmitter balance in basal ganglia