PHRM 825: Pharmacologic Manipulations of the Cholinergic System Flashcards
(35 cards)
What causes botulism and where is it present?
Bacterium clostridium botulinum; soil and water
How does clostridium botulinum cause botulism?
Inhibits release of Ach
What are symptoms of botulism?
- Weakness
- Trouble seeing
- Feeling tired
- Trouble speaking
- NOT NECESSARILY FEVER*
What is the most fatal symptom of neuropathy of the ANS?
Silent ischemic events (painless event)
What are 2 approaches to increase cholinergic stimulation?
Increase endogenous stimulation and use exogenous stimulation
What can reduce symptoms of neuropathic ANS disorders?
Cholinergic stimulation
Would an AchE inhibitor help botulism patients?
No. Patient’s don’t release Ach
What are the 2 types of cholinesterases?
Acetylcholinesterase (AchE) and plasmacholinesterase (Butyrylcholinesterase (BuChE)
Where is AchE located?
In nerve synapses
Where is butyrylcholinesterase (BuChE) located?
In plasma and many organs (liver, skin, GI tract, brain)
What does BuChE metabolize?
Succinylcholine
Where do acetylcholinesterase inhibitors bind?
The same site as acetylcholine
What are the 3 classes of AchE inhibitors?
Quaternary ammonium alcohols, carbamates, and organophosphates
What drug is a tertiary amine that can enter the CNS?
Physostigmine
What can physostigmine be used to treat?
glaucoma and Alzheimer’s disease, and atropine overdose
What is neostigmine used to treat?
myasthenia gravis, reversal of neuromuscular blockers and post-operative ileus
What is pyridostigmine use to treat?
myasthenia gravis, reversal of neuromuscular blockers and post-operative ileus
What is an irreversible, covalent binding AchE inhibitor?
Organophosphates
What are organophosphates used to treat?
Glaucoma (not commonly used)
What are symptoms of acetylcholinesterase inhibitor poisoning?
DUMBBELLSS (all of these are M3 except Bradycardia) -Diarrhea -Urination -Miosis -Bronchospasms -Bradycardia (M2) -Excitation of skeletal muscles and CNS -Lacrimation -Sweating -Salivation
What can be given to treat AchE “poisoning”?
Pralidoxime chloride (2-PAM) and/or Atropine
What drug is usually used for diagnosis of myasthenia gravis?
Edrophonium (tensilon)
Symptoms of myasthenia gravis
- Muscle weakness (visible in eye)
- Trouble chewing/swallowing
- Hard to talk/nasal sound
- Reduced facial expression
What causes myasthenia gravis?
Auto-antibodies that block nicotinic acetylcholine receptors at the postsynaptic neuromuscualr junction
