pharmacology of the ANS Flashcards
sympathetic pregangilionic neurons
short
sympathetic postganglionic neurons
long
cholinergic preganglionics
sympathetic and parasympathetics
postganglionics are adrenergic
sympathetics
postganglionics are cholinergic
parasympathetics
postganglionic parasympathetics stimulate what?
muscarinic receptors
What do sympathetic post ganglionics stimulate?
alpha and beta receptors
Muscarinic stimulation causes
SLUD: salivation, lacrimation, urination, diarrhea
miosis, vasodilation, bronchoconstriction, negative chronotropic and inotropic heart changes
What does beta 1 sympathetic stimulation cause?
+ionotropic
+chronotropic
responses in the heart
What does beta 2 sympathetic stimulation cause?
bronchodilation
relaxation of myometrium
insulin release
What does alpha 1 sympathetic stimulation cause?
vasoconstriction
mydriasis
What does alpha 2 sympathetic stimulation cause?
reduces norepinephrine release
Parasympathomimetics include:
muscarinic receptor agonists
cholinesterase inhibitors
What does muscarinic stimulation cause?
stimulates sphincter muscle of iris-->miosis vasodilation of arterioles -chronotropic and -inotropic heart bronchoconstriction SLUD
What category is acetylcholine?
parasympathomimetic
What is the MOA of acetylcholine?
muscarinic and nicotinic agonist
What are the characteristics of acetylcholine?
rapidly hydrolyzed by esterases
acts on both muscarinic and nicotinic receptors
quaternary ammonium group invokes polarity (not lipid soluble, not go to brain)
What category is bethanechol?
parasympathomimetic
What is the MOA of bethanechol?
muscarinic agonist
What are the distinguishing characteristics of bethanechol?
not metabolized by esterase enzymes
quaternary ammonium compound
affinity for gut and bladder smooth muscle
oral route preferred
What are the predictable characteristics of bethanechol?
no CNS effect
T1/2 allows distribution to areas of low blood flow
What are the predictable uses of behanechol?
gastroparesis
urinary retention
xerostomia
ocular diagnostics
What is category is pilocarpine?
parasympathomimetic
What is the MOA of pilocarpine?
muscarinic receptor agonist
What are the distinguishing characteristics of pilocarpine?
preferential activity on sweat glands
resistant to esterases
What are the predictable characteristics of pilocarpine?
miotic and treatment of glaucoma causes accomodation treats xerostomia may cause CNS at high plasma levels diaphoresis is common side effect duration up to 8 hours
What category is neostigmine?
parasympathomimetic
What is the MOA of neostigmine?
reversible cholinesterase inhibitor
What are the distinctive characteristics of neostigmine?
slowly hydrolyzed
poorly absorbed following oral Rx
What are the predictable activities of neostigmine?
elevates Ach levels
causes both muscarinic and nicotinic stimulation
numerous peripheral side effects but not CNS
What are the predictable uses of neostigmine?
miosis and Rx glaucoma
Rx myasthenia gravis
antidote to some drugs (atropine)
atonic gut and bladder
What category is malathione?
parasympathomimetic
What is the MOA of malathione?
irreversible cholinesterase inhibitor
What are the distinguishing characteristics of malathione?
tertiary ammonium compound
binds covalently to esterase enzymes
not hydrolyzed by esterase enzymes
rapidly absorbed through multiple routes
What are the predictable characteristics of malathione?
SLUD and other ANS CNS disturbances no therapeutic use used as insecticide chemical weapons atropine=antidote
What category is atropine?
parasympatholytic
What is the MOA of atropine?
muscarinic receptor antagonist
What are the distinguishing characteristics of atropine?
tertiary ammonium (lipid soluble, crosses BBB)
ester group required for activity
resistant to hydrolysis by esterases
metabolized in liver with T1/2 of about 4 hr
What are the predictable activities of atropine?
inhibits SLUD
used in opthalmology-mydriasis and cycloplegia
used as antidote to parasympathomimetics
used to treat diarrhea
What category is Ipratropium?
parasympatholytic