Cholinergics Flashcards
What is acetylcholinesterase?
An enzyme that breaks down acetylcholine
What is miosis?
Very constricted pupils
What is a cholinergic agonist?
Drugs that mimic the effects of the neurotransmitter acetylcholine (and therefore the parasympathetic nervous system)
agonist = to stimulate/increase the effects
Not limited to a specific site –> many undesired systemic effects
Work either directly or indirectly on ACh receptors
(AKA parasympathomimetic)
What is Myasthenia gravis?
- A chronic autoimmune disorder affecting the muscles
- Patients make antibodies to ACh receptors, causes destruction of them
- Progressive weakness and lack of muscle control with periodic acute episodes
What is Alzheimer’s Disease?
- A progressive disease that causes neural degeneration in the cortex
- Leads to marked loss of memory, decreased ability to perform ADLs
- Believe there is a progressive loss of ACh producing neurons
What are the effects of the parasympathetic nervous system?
REST AND DIGEST
* Pupil constriction
* ⬆️ salivation
* ⬆️ respiratory secretions
* ⬆️ peristalsis
* Vasodilation (in most blood vessels)
* Bronchoconstriction
* ⬇️ heart rate
* ⬇️ blood pressure
* Bile release
* Urination
Lifespan Considerations of Cholinergic Drugs
In Children
- Increased risk of adverse effects
- Dosages should be based off weight
Lifespan Considerations of Cholinergic Drugs
In Adults
- Caution against driving while on medication
- No studies on safety during pregnancy/lactation
- Use alternative method to breastfeeding
Lifespan Considerations of Cholinergic Drugs
In Older Adults
- More likely to have adverse effects
- More likely to have toxic levels
- Start low and go slow
- Institute safety precautions
Direct Acting Cholinergic Agonists
Mechanism of Action
- Mimics acetylcholine at the receptor sites (muscarinic or nicotinic) on the surfaces of the target cells of the postganglionic cholinergic nerves
- Causes an increased stimulation of the cholinergic receptor
Direct-Acting Cholinergic Agonists: 🍄Muscarinic
Indications
- Urinary Retention (Bethanechol)
- To induce miosis (carbachol)
- Treat dry mouth (cevimeline & pilocarpine)
Direct-Acting Cholinergic Agonists: 🍄Muscarinic
Drug Names
- Bethanechol (urinary retention)
- Carbachol (to induce miosis)
- Cevimeline (treats dry mouth)
- Pilocarpine (treats dry mouth)
Direct-Acting Cholinergic Agonists: 🍄Muscarinic
Contraindications
Absolute:
* Allergy
* Any condition that would be exacerbated by parasympathetic effects: Bradycardia, hypotension
* Peptic Ulcer Disease, GI obstruction or recent GI surgery
* Asthma (can cause bronchoconstriction)
* Bladder obstruction
* Epilepsy and parkinsonism (can worsen)
Caution:
* Pregancy and lactation
Direct-Acting Cholinergic Agonists: 🍄 Muscarinic
Adverse Effects
💩 Diarrhea, involuntary defecation, cramps
🤮 Nausea, vomiting, increased salivation
💓 Bradycardia, heart block, hypotension
🫣 Urinary urgency
💦😳 Flushing or increased sweating
Direct-Acting Cholinergic Agonists: 🍄Muscarinic
Drug Interactions
Acetylcholinesterase Inhibitors
(Indirect-Acting Cholinergic Agonists)
Can lead to a cholinergic crisis!