lecture 6 Flashcards
(30 cards)
direct acting parasympathomimetic drugs
immediately active, agonist
indirect acting parasympathomimetic drugs
requires additional steps (cholinesterase inhibitors)
botulinum toxin
blocks release of ACh from the vesicle it is stored in
Snap 25 proteins
can bind vesicle but this is calcium dependent
N1 receptor
neuronal type, on demand of ACh
N2 receptor
muscle type, muscular end plate
depolarisation block
done by desensitization of the nicotinic receptor. only postsynaptic stimulation will cause an action potential
M1,3,5 receptor
coupled to Gq, stimulation of PLC causing IP3 release, causing calcium release
M1 receptor
nerve cell stimulation, CNS tremor
M3 receptor
smooth muscle contraction and exocrine glands secretion
M2,4 receptors
inhibitory receptors, Gi, inhibition of AC causing decrease in cAMP.
GIRK
stimulated by inhibitory receptors, causing outflux of K+
M2 receptor
heart inhibition
M4 receptor
striatum and lungs
carbachol
charged, indicator for postoperative intestine function and glaucoma
pilocarpine
uncharged, indicator for glaucoma
non-esterificating inhibitors
competitive inhibition
carbamylating inhibitors
enzyme is restored
phosphorylating inhibitors
irreversible inhibition
pralidoxime
used to treat patients that are exposed to toxins or insecticides
neostigmine
can increase ACh concentrations to treat e.g. glaucoma
glaucoma
increased pressure in the eye due to weakening of the muscle in the eye
myasthenia gravis
antibodies against muscular nicotinic receptors are produced, treated with neostigmine
tiotropium
indicator of spasmolysis, poor absorption, doesnt cross blood brain barrier