Cholinergic Flashcards
Cholinergic agents - direct acting cholinomimetics
Cholinergic agonist, express the same symptoms of parasympathetic nervous system
Bethanenchol & pilocarpine
Muscarinic cholinergic receptor agonist. Direct acting
Bethanechol- treatment of gi/urinary bladder paralysis
Pilocarpine- treatment of glaucoma
Nicotine
Nicotinic cholinergic receptor agonist.
Glaucoma treatment (pilocarpine)
Muscarinic cholinergic receptor on ciliary muscle in eye. If you’re using a cholinergic agonist you relax the ciliary muscle, allow schlemms canal to open and allows pressure to go down.
Why are antimuscarinic drugs contraindicated in patients with glaucoma
There is a Muscarinic cholinergic receptor on the iris that relaxes the muscle so the pressure in the eye can be reduced. If you block it with an antimuscarinic drug, you won’t get the relaxation
Varenicline (chantix)
Reduced craving for and decreases pleasure effects from cigarettes PARTIAL AGONIST
Indirect acting cholinomimetics (cholinergics)
PNS neostigmine (doesn’t pass bbb) - myasthenia gravis
Donepazil (passes bb and produces central effects) Alzheimer’s
Indirect acting cholinomimetics mechanism of action
Acetylcholinesterase (achase) inhibitors - ACH accumulates in synapse and produces cholinergic response
Neostigmine
Used to treat gi and urinary paralysis, glaucoma, myesthenia gravis , treatment of anticholinergic effects produced by other drugs like phenothiazines
Donepezil
Used to treat systems of Alzheimer’s disease associated with loss of cholinergic control of short term memory. Not curative
Memory foundation
Sensory inputs activate memory circuits “acquisition”, cholinergic pathways form short term memories, through repetition you develop new synaptic connections “consolidation” and that makes long term memories.
Alzheimer’s is associated with neuro degeneration of cholinergic pathways
Myesthenia gravis Is an autoimmune disorder associated with destruction of what receptors ?
Nicotinic Cholinergic receptors at the neuromuscular junction of skeletal muscle
Sarin nerve gas and parathione is an insecticide. What is the antidote for these ?
Pralidoxime (Pam) breaks chemical bonds between drugs and a chase (acetylcholinesterase)
Describe causes and strategies that are used to treat life threatening state of cholinergic poisoning
If you give too much of a cholinergic agent the receptors are too saturated so they won’t produce a response. Cholinergic crisis Too much drug is, occurs soon after dose. treatment is give an anticholinergic agent. Myesthenic crisis is not enough drug. Occurs at the end of doseage. Treatment for myesthenic crisis is give more drug. Same symptoms but can tell the different around dosing times.
Cholinergic crisis
Too much drug, receptors are too saturated and can’t receive nerve impulse. give an anticholinergic agent. Occurs soon after dose of cholinergic meds
Myesthenic crisis
Need more drug, happens at the end of a dosage, treatment is giving a cholinergic agonist
CholinoLYTIC mechanism of action
Cholinergic antagonist, anticholinergic agents, Muscarinic cholinergic receptor antagonists
Muscarnic cholinergic receptor antagonist
They bind to the Muscarinic cholinergic receptor and block it so nothing else can bind to it resulting in decreased parasympathetic response
Atropine uses
Induces mydriasis (dilation), reduces secretions (preop for anesthesia ), treatment of ventricular Bradycardias, treatment of severe diarrhea & urinary incontinence
Why is atropine not an ideal med?
Has a lot of side effects and isn’t as targeted to one symptoms
Scopolamine
Used in treatment of motion sickness, inhibits cholinergic activation of emesis center
Solifenacin (vesicare)
Selective m3 Muscarinic cholinergic receptor antagonist , helps with bladder incontinence
Detrusor muscle
Muscle that controls the urinary bladder
Where are m1, m2, and m3 receptors
M1- salivary glands
M2- heart
M3- smooth muscle of bladder, gi tract and eyes
Cholinolytic toxicology (anticholinergic )
Extreme dry mouth, hallucinations, not sweating when hot
Mechanism of action of baclofen
gaba receptor agonist that suppresses motor neuron activity and nerve conduction
Skeletal muscle relaxation meds
Baclofen, botulism, pancuronium
Pancuronium MOA
nicotinic receptor antagonist on skeletal muscle. Non depolarizing relation because it blocks excitation contraction coupling (depolization)
Succinylcholine
Activates the ach receptor and causes depolization but remains bound to the receptor for a prolonged period of time.
Botulism neurotoxin
Inhibit membrane fusion proteins (synaptin and snap25) necessary for exocytosis of ach by motor neurons, blocks excitation secretion coupling. This effect causes skeletal muscle paralysis
Atropine treats what ?
Cholinergic crisis with ingestion of poisonous mushroom
What med is a depolarizing skeletal muscle relaxant
Succinylcholine
