ANS Drugs Flashcards
NO, 5-HT, ATP, GABA, dopamine, purines, neuropeptides
NANC (noradrenergic, noncholinergic)
Neostigmine, Physostigmine
Medium acting acetylcholinesterase inhibitors
Notes - carbamyl esters. Physostigmine longer acting than neostigmine. Use to reverse neuromuscular block or myasthenia gravis treatment
Hemicholinium
Stops reuptake of choline from synaptic cleft for recycling
Suxamethonium
Depolarizing blocking agent (NMJ agonist)
Notes - nicotinic antagonist. binds receptors and stays there blocking further ACh action - used for transient paralysis ex intubation
Tubocurarine
Non-depolarizing blocking agent (NMJ antagonist)
Notes - nicotinic antagonist. compeptitive antagonist to ACh
Botulinum
Ganglion blocking drug
Notes - nicotinic antagonist. toxin produced by C.diff (toxin BTX-A). local effects causing denervation
Cholinergic receptors
Nm - muscle type - neuron to muscle
Nn - nerve type - neuron to neuron
M1 - increase IP3 - excitation - neurons
M2 - decrease cAMP - inhibition - heart
M3 - increase IP3 - excitation - glands, erectile tissue, eye, bronchi
Cholinergic stimulant
- cholinergic toxidrome - DUMBBELSS
- defecation, urination, miosis, bronchospasm, bradycardia, emesis, lacrimation, sweating, salivation
Anticholinergic effects
- opposite of DUMBBELSS
- dry mouth, blurred vision, constipation, glaucoma
Doneprezil, tacrine
Acetylcholinesterase inhibitor
Notes - for Alzheimer’s disease
Edrophonium
Short acting acetylcholinesterase inhibitor
Notes - Quaternary alcohol. Binds anionic sites only and prevents ACh binding. Used in diagnosis for myasthenia gravis
Echothiopate, Isofluorophate
Irreversible acetylcholinesterase inhibitors
Notes - pentavalent phosphorus compounds that phosphorylate ser203 @ active site forming a stable bond. It is reversible within first few hours if pralidoxime or an “oxime” administered
Adrenoceptors
A1 - increase IP3 - excitatory - BVs
A2 - decrease cAMP - inhibitory - BVs, pancreatic islets
B1 - increase cAMP - excitatory - kidney, heart
B2 - increase cAMP - excitatory - SMC, ciliary muscle
Propanolol
beta adrenoceptor antagonist
Notes - sympatholytic. b1/b2 nonspecific
phentolamine
alpha adrenoceptor antagonist
Notes - sympatholytic. a1/a2 nonspecific
ACh, bethanechol
Direct-acting muscarinic agonists
Notes - choline esters
Pilocarpine
Direct-acting muscarinic agonists
Notes - alkaloid. Used for glaucoma to lower the pressure in the eye