Autonomic Nervous System Drugs Flashcards
acetylcholine category?
parasympathomimetic
acetylcholine MOA?
muscarinic & nicotinic agonist
bethancehol category?
parasympathomimetic
bethanechol MOA?
muscarinic agonist
pilocarpine category?
parasympathomimetic
pilocarpine MOA?
muscarinic agonist
neostigmine category?
parasympathomimetic
neostigmine MOA?
reversible cholinesterase inhibitor
malathione category?
parasympathomimetic
malathione MOA?
irreversible cholinesterase inhibitor
atropine category?
parasympatholytic
atropine MOA?
muscarinic receptor antagonist
scopolamine category?
parasympatholytic
scopolamine MOA?
muscarinic receptor antagonist
ipratropium (atrovent) category?
parasympatholytic
ipratropium (atrovent) MOA?
muscarinic receptor antagonist
EPI category?
sympathomimetic
EPI MOA?
stimulates alpha & beta receptors
phenylephrine category?
sympathomimetic
phenylephrine MOA?
alpha 1 receptor agonist
clonidine (catapres) category?
sympathomimetic
clonidine (catapres) MOA?
alpha 2 receptor agonist
isoproterenol category?
sympathomimetic
isoproterenol MOA?
beta 1 and 2 receptor agonist
albuterol category?
sympathomimetic
albuterol MOA?
beta 2 receptor agonist
amphetamine category?
sympathomimetic
amphetamine MOA?
stimulates the release of NE and dopamine
phenelzine category?
sympathomimetic
phenelzine MOA?
MAO inhibitor
prazocin (minipress) category?
sympatholytic
prazocin (minipress) MOA?
alpha 1 receptor antagonist
propranolol category?
sympatholytic
propranolol MOA?
beta 1 & 2 receptor antagonist
metoprolol category?
sympatholytic
metoprolol MOA?
beta 1 receptor antagonist
reserpine category?
sympatholytic
reserpine MOA?
promotes release of NE and reduces re-uptake resulting in depletion of NE stores
distinguishing characteristics: Rapidly hydrolyzed by esterases; acts on both muscarinic and nicotinic receptors; quaternary ammonium group invokes a polarity
predicted actions: Short half-life (sec); diffuse activity; limited distribution
uses: local opthalmic use if other options aren’t available
acetylcholine
distinguishing characteristics: Not metabolized by esterase enzymes; quaternary ammonium compound; particular affinity for the gut and bladder smooth muscle; oral administration is preferred
predicted actions: Longer half-life allows for distribution to areas of low perfusion; no CNS effect
uses: post-op gastroparesis, urinary retention, xerostomia, ocular diagnostics
bethanechol
distinguishing characteristics: Resistant to esterases; plant origin, tertiary ammonium compound; preferential activity on sweat glands
predicted actions: Will cause accomodation; may cause CNS effects at high plasma levels; duration of action is up to 8 hours
uses: glaucoma, xerostomia
SEs: diaphoresis
pilocarpine
distinguishing characteristics: Contains an ester group - slowly hydrolyzed (half-life is 1-2hrs); quaternary ammonium compound; poorly absorbed orally
predicted actions: Elevates Ach levels; causes both muscarinic and nicotinic stimulation
uses: miosis, glaucoma, myasthenia gravis, antidote to atropine, atonic gut or bladder
neostigmine
distinguishing characteristics: Not hydrolyzed by esterase enzymes; binds covalently to esterase enzymes; tertiary ammonium compound; rapidly absorbed through multiple routes
predicted actions: causes SLUD & other ANS activities, causes CNS distribution, chemical weapon
uses: insecticide, chemical warfare, not used medically
atropine is antidote
malathione
distinguishing characteristics: Resistant to hydrolysis by esterases; plant origin, tertiary ammonium compound; metabolized in liver with a half-life of 4hrs
predicted actions: Inhibits SLUD and other parasympathetic activities
uses: mydiasis, cycloplegia, antidote to parasympathomimetics, diarrhea, historical asthma tx
atropine
distinguishing characteristics: Greater CNS distribution than atropine; similar to atropine otherwise; plant source - Hyocyamus niger
predicted actions: Greater CNS effects/abuse potential than atropine; used less frequently
uses: Motion sickness
scopolamine
distinguishing characteristics: Quaternary ammonium compound; minimal inhibition of mucociliary clearance
predicted actions: No CNS effects; bronchodilation; limited mucous accumulation
muscarinic antagonist
ipratropium
distinguishing characteristics: Metabolized in many tissues; more Beta and Alpha activity; ineffective orally
predicated actions: Very short half-life (min)
uses: Cardiac emergencies; bronchospasm; adjunct to local anesthesia
ephinephrine
distinguishing characteristics: Limited access to CNS; effective orally
uses: Nasal decongestant; mydriatic
SEs: rebound congestion, increased peripheral resistance, reflex bradycardia
phenylephrine
distinguishing characteristics: Crosses BBB; prefers alpha receptors in the brainstem; long half-life and duration of action; diminish discharge from medular vasomotor center; effective orally
uses: Antihypertensive
SEs: Dry mouth; sedation; sexual dysfunction
clonidine
distinguishing characteristics: Metabolized by COMT; short duration of action
predicted actions: Tachycardia; bronchodilation; replaced by more selective beta agonists
uses: Cardiac arrest
isoproterenol
distinguishing characteristics: Limited CV effects; duration of action is several hours; effective orally or by inhalation
uses: Bronchodilator
SEs: weak and ocassional tachycardia, vasodilation
albuterol
distinguishing characteristics: Enters the CNS; Inhibits MAO
predicted actions: Vasoconstriction, cardiac stimulation, inc. BP; mydriasis - NE; CNS stimulation: euphoria, insomnia, anxiety, loss of appetite, hyperthermia
uses: narcolepsy, obesity, ADHD
highly abused, controlled substance
amphetamine
distinguishing characteristics: Readily absorbed; crosses BBB; increases synaptic catecholamine levels
uses: antidepressant
phenelzine
distinguishing characteristics: Highly protein bound (only 5% free); effective orally
uses: HTN
prazocin
distinguishing characteristics: Very lipid soluble; significant 1st pass metabolism; highly variable plasma levels
uses: Antihypertensive; antiangina; antiarrythmic
propranolol
distinguishing characteristics: Similar to propranolol
uses: Antihypertensive without risk to asthma and diabetic patients
metoprolol
distinguishing characteristics: Derived from plant; transitory sympathomimetic followed by prolonged sympatholytic effect; Antiquated for therapeutic use - more for research
uses: anti-HTN
reserpine