Autonomics III: Cholinergic Receptor-Inhibiting Drugs Flashcards
are muscarinic antagonists selective?
no, they do not discriminate well between the 5 muscarinic receptor subtypes.
emergency uses for muscarinic antagonists
treatment of poisoning with cholinesterase inhibitors (nerve gases and insecticides) and mushrooms. atropine is best for this. tropicamide has a short half life and deals with nicotinic effects
toxicity of muscarinic antagonists
dry as a bone, blind as a bat, red as a beet, mad as a hatter. reduced sweating, lacrimation, and salivation. excessive pupil dilation. dilation of cutaneous vessels in upper body. inhibition of CNS muscarinic receptors
atropine fever
blockade of thermoregulatory sweating. can lead to hyperthermia
ganglionic blockers mechanism
competitively inhibit Nn receptors at both sympathetic and parasymp ganglia. lack of selectivity left them abandoned for clinical use.
NMJ blockers mechanism
interfere with transmission at the axon terminals and are useful as skeletal muscle relaxants. several act by inhibiting Nm receptors. can either be nondepolarizing or depolarizing. used to facilitate surgery and ventilation
toxic efffects of NMJ blockers
respiratory paralysis and disturbance of autonomic function. non-depolarizing blockers are blocked by cholinesterase inhibitors, but nothing can fix depolarizing blockers.
botulinum toxin A
degrades SNAP-25, which mediates fusion of synaptic vesicles with the presynaptic terminal membrane.