Anticholinesterases
Blocking acetylcholinesterase, so acetylcholine builds up at synapses.
Also called cholinesterase inhibitors and acetylcholinesterase inhibitors.
Class card
- Drugs
- Neostigmine and Pyridostigmine
- Used for
- Myasthenia gravis
- Reversing non-depolarizing muscle relaxants after surgery
- Urinary retention after surgery
- Known for
- Slow heart rate
- Cholinergic crisis: weakness from too much drug
- Name stems
- -stigmine
3 cards: the class, and each drug in it.
Mechanism of action
How do anticholinesterases work?
They bind reversibly to acetylcholinesterase and block it, so acetylcholine is broken down more slowly and builds up at synapses. At the neuromuscular junction the extra acetylcholine strengthens weak muscles in myasthenia gravis and outcompetes non-depolarizing blockers. It also boosts muscarinic effects on the gut, glands, airways and heart, which cause most side effects.
The drugs
Anticholinesterases with a card
Uses
What are anticholinesterases used for?
- Myasthenia gravis
- Reversing non-depolarizing muscle relaxants after surgery
- Urinary retention after surgery
Side effects
Side effects of anticholinesterases
- Slow heart rateKnown forSerious
- Cholinergic crisis: weakness from too much drugKnown forSerious
- Diarrhea and abdominal cramps
- Passing urine often, or incontinence
- Small pupils (miosis)
- Bronchospasm and extra bronchial secretionsSerious
- Nausea and vomiting
- Watery eyes
- Excess saliva
- Sweating
What the class has in common. Each drug's card has its own, and Known for marks what an exam expects you to know.
Watch for
Cautions
- Contraindicated in mechanical obstruction of the gut or urinary tract.
- Asthma: they can trigger bronchospasm.
- Slow heart rate or arrhythmia: risk of marked slowing; atropine or glycopyrrolate is given with them when reversing blockade.
- They prolong, rather than reverse, a depolarizing block such as suxamethonium's.
Remember them
A way to remember them
DUMBBELSS
- D
- Diarrhea
- U
- Urination
- M
- Miosis
- B
- Bradycardia
- B
- Bronchospasm and bronchial secretions
- E
- Emesis (vomiting)
- L
- Lacrimation (watery eyes)
- S
- Salivation
- S
- Sweating
A mnemonic widely used in teaching
Name stems
-stigmine means cholinesterase inhibitor
Neostigmine reverses non-depolarizing muscle relaxants and rivastigmine treats dementia. Donepezil, a cholinesterase inhibitor used for dementia, doesn't carry the stem.
- Every drug name stem
Don't mix them up
Classes easily confused with these
Sources
Checked against
Written for biofideX in plain words, after checking these references:
- Neostigmine methylsulfate injection: label (DailyMed)
- Pyridostigmine bromide tablets: label (DailyMed)
- Neostigmine methylsulfate injection: SmPC (emc)
- Acetylcholinesterase inhibitor (NCI Thesaurus)
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Autonomic nervous system
Practice anticholinesterases with the other classes in this group: what each drug is, how it works, what it treats and what it's known for.
Start Practicing