ANS Flashcards
What does muscarinic stimulation in sphincter muscle of the iris of the eye cause?
Miosis
What does muscarinic stimulation in arterioles cause?
Vasodilation
What does muscarinic stimulation in heart cause?
Negative chronotropic and inotropic respnses
What does muscarinic stimulation in bronchial smooth muscle cause?
Bronchoconstriction
What does muscarinic stimulation in GI and GU systems cause?
Salivation
Lacrimation
Urination
Diarrhea
What kind of stimulation of the heart causes +inotropic and +chronotropic response?
Beta 1
What kind of stimulation of the bronchus causes bronchodilation?
Beta 2
What kind of stimulation of the myometrium causes relaxation?
Beta 2
What kind of stimulation of the pancreas causes insulin release?
Beta 2
What kind of stimulation of arterioles causes vasoconstriction?
Alpha 1
What kind of stimulation of radial muscles of the iris causes mydriasis?
Alpha 1
What kind of stimulation reduces norepinephrine release?
Alpha 2
What are the two types of parasympathomimetics?
Muscarinic agonists
Cholinesterase inhibitors
What is the one type of parasympatholytic?
Muscarinic antagonist
Acetylcholine: Category?
ANS - parasympathomimetic
Acetylcholine: MOA?
Muscarinic and nicotinic agonist
Acetylcholine: Distinguishing characteristics?
Rapidly hydrolyzed by esterases
Acts on musc. and nic. receptors
Quaternary ammonium group invokes polarity
Acetylcholine: Predictable characteristics?
Short half life (seconds)
Diffuse activity
Limited distribution
Acetylcholine: Predictable uses?
Local ophthalmic use (but better products available)
Bethanechol (Urecholine): Category?
ANS - parasympathomimetic
Bethanechol (Urecholine): MOA?
Muscarinic agonist
Bethanechol (Urecholine): Distinguishing characteristics?
Not metabolized by esterase enzymes
Quaternary ammonium compound
Particular affinity for gut and bladder smooth muscle
Oral route preferred
Bethanechol (Urecholine): Predictable characteristics?
No CNS effect
T1/2 allows dist. to areas of low blood flow
Bethanechol (Urecholine): Predictables uses?
Postoperative gastroparesis
Urinary retention
Xerostomia
Ocular diagnostics
Bethanechol (Urecholine): Predictable side effects?
Other parasympathomimetic effects especially following parenteral Rx
Neostigmine: Category?
ANS - Parasympathomimetic
Neostigmine: MOA?
Reversible cholinesterase inhibitor
Neostigmine: Distinctive characteristics?
Quaternary ammonium compound
Contains ester group- slowly hydrolyzed
Poorly absorbed following oral Rx
Neostigmine: Predictable activities?
Elevates Ach levels
Causes both muscarinic and nicotinic stimulation
Numerous peripheral side effects but not CNS
Neostigmine: Predictable uses?
Miosis and Rx glaucoma (local)
Rx myasthenia gravis
Antidote to some drugs (atropine)
Atonic gut and bladder
Malathione: Category?
ANS- Parasympathomimetic
Malathione: MOA?
Irreversible cholinesterase inhibitor
Malathione: Distinguishing characteristics?
Tertiary ammonium compound
Binds covalently to esterase enzymes
Not hydrolyzed by esterase enzymes
Rapidly absorbed through multiple routes
Malathione: Predictable characteristics?
Causes SLUD and other ANS activities Causes CNS disturbances No therapeutic use Used as insecticide Similar agent used as chemical weapons Atropine is antidote plus supportive therapy
Atropine: Category?
ANS- parasympatholytic
Atropine: MOA?
Muscarinic receptor antagonist
Atropine: Distinguishing characteristics?
From plant source (atropa belladonna) Tertiary ammonium compound Ester group required for activity Resistant to hydrolysis by esterases Metabolized in liver with t1.2 of ~4hr
Atropine: Predictable activities?
CNS toxicity (especially kids) Inhibit SLUD Used in ophthalmology (mydriasis and cycloplegia) Antidote to parasympathomimetics Used to treat diarrhea
Ipratropium: Category?
Parasympatholytic
Ipratropium: MOA?
Muscarinic antagonist
Ipratropium: Distinguishing characteristics?
Quaternary ammonium compound
Minimal inhibition of mucociliary clearance
Ipratropium: Predictable actions?
No CNS effects
Bronchodilation
Limited mucous accumulation
Scopolamine: Category?
ANS- parasympatholytic
Scopolamine: MOA?
Muscarinic receptor antagonist
Scopolamine: Distinguishing characteristics?
From plant source (Hyocyamus niger)
Greater CNS distribution than atropine
Other char. similar to atropine
Scopolamine: Predictable actions?
Greater CNS side effects and abuse potential than atropine
Used less frequently than atropine
Used to treat motion sickness
Epinephrine: Category?
ANS- sympathomimetic
Epinephrine: MOA?
Stimulate alpha and beta receptors (G protein which facilitate 2nd messengers)
Epinephrine: Distinguishing characteristics?
Metabolized in gut, blood and multiple tissues
More beta and less alpha activity than norepinephrine
Epinephrine: Predictable uses?
Ineffective orally Very short t1/2 (minutes) Cardiac emergencies Bronchospasms Adjunct to local anesthesia
Epinephrine: Predictable side effects?
Tachycardia and increased force of contraction BP disturbance (usually HTN)
Phenylephrine: Category?
ANS- Sympathomimetic
Phenylephrine: MOA?
Alpha 1 receptor agonist
Phenylephrine: Distinguishing characteristics?
Effective orally
Limited access to CNS
Phenylephrine: Uses?
Nasal decongestant
Mydratic
Phenylephrine: Side effects?
Rebound congestion
Increased peripheral resistance
Reflex bradycardia
Clonidine: Category?
ANS- sympathomimetic
Clonidine: MOA?
Alpha 2 receptor agonist
Clonidine: Distinguishing characteristics?
Effective orally Crosses blood-brain barrier Prefers alpha receptors in brainstem Long t1/2 and duration of action Diminish discharge from medular vasomotor center
Clonidine: Predictable uses?
Antihypertensive
Clonidine: Side effects?
Dry mouth
Sedation
Sexual dysfunction
Isoproterenol: Category?
ANS- sympathomimetic
Isoproterenol: MOA?
Beta receptor agonist (1 and 2)
Isoproterenol: Distinguishing characteristics?
Metabolized by COMT
Short duration of action
Both beta 1 and 2
Isoproterenol: Predictable uses?
Cardiac arrest
Isoproterenol: Predictable actions?
Tachycardia
Bronchodilation
Replaced often by more selective beta agonists
Albuterol: Category?
ANS- sympathomimetic
Albuterol: MOA?
Beta 2 receptor agonist
Albuterol: Distinguishing characteristics?
Effective orally or by inhalation
Limited cardiovascular effects
Duration of action is several hours
Albuterol: Predictable uses?
Bronchodilator
Albuterol: Side effects?
Weak and occasional tachycardia
Vasodilation
Amphetamine: Category?
ANS sympathomimetic
Amphetamine: MOA?
Stimulate release of norepinephrine and dopamine
Amphetamine: Dist. char.?
Enters CNS
Inhibits MAO
Amphetamine: Actions?
Alpha and beta stim by NorE (vasoconstriction, cardiac stim., increased BP, mydriasis)
CNS stim. (euphoria, insomnia, anxiety, loss of appetite, hyperthermia)
Used to treat narcolepsy, obesity and ADHD
High abuse potential makes it scheduled substance
Name some other substances that increase norepinephrine release?
Cocaine Tyramine Reserpine Ephedrine Pseudoephedrin Methamphetamine
Phenelzine: Category?
ANS- sympathomimetic
Phenelzine: MOA?
Monoamine oxidase inhibitor
Phenelzine: Dist. Char.?
Readily absorbed
Crosses blood-brain barrier
Increases synaptic catecholamine levels
Phenelzine: Uses?
Antidepressant
Phenelzine: Side effects?
Sympathomimetic actions
Prazocin: Category?
ANS- sympatholytic
Prazocin: MOA?
Alpha 1 receptor antagonist
Prazocin: Dist. Char.?
Effective orally
Highly protein bound
Reflex tachycardia
Prazocin: Uses?
Hypertension
Prazocin: Side effects?
Hypotension
Syncope
Propranolol: Category?
ANS- sympatholytic
Propranolol: MOA?
Beta 1 and 2 receptor antagonist
Propranolol: Dist. Char.?
Very lipid soluble
1st pass metabolism
Highly variable plasma levels
Multiple uses
Propranolol: Uses?
Antihypertensive
Antiangina
Antiarrythmic
Propranolol: Side effects?
Place asthma patients at risk
Place diabetics at risk
Metoprolol: Category?
ANS- sympatholytic
Metoprolol: MOA?
Beta 1 receptor antagonist
Metoprolol: Dist. Char.?
Similar to propranolol
Metoprolol: Uses?
Antihypertensive w/o risk to asthmatics and diabetics
Metoprolol: Similar drugs?
Atenolol
Others
Reserpine: Category?
ANS- sympatholytic
Reserpine: MOA?
Promotes release of NorE and reduces reuptake resulting in depletion of NorE stores
Reserpine: Dist. Char.?
Derived from plant
Transitory sympathomimetic followed by prolonged sympatholytic effect
Antiquated for therapeutic use
Reserpine: Uses?
Antihypertensive
Reserpine: Side effects?
Prolonged paralysis of sympathetic nervous system