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Autonomic Pharmacology 3
n/a
119
Pharmacology
Graduate
03/01/2010

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Cards

Term
what kind of drug is pirenzapine?
Definition
M1 muscarinic antagonist
Term
what kind of drug is atropine?
Definition
muscarinic antagonist
Term
what kind of drug is scopolamine?
Definition
muscarinic antagonist
Term
what kind of drug is propantheline?
Definition
muscarinic antagonist
Term
what kind of drug is ipratropium?
Definition
muscarinic antagonist
Term
what kind of drug is tiotropium?
Definition
muscarinic antagonist
Term
what kind of drug is hexamethonium
Definition
nicotinic ganglionic antagonist
Term
what kind of drug is tubocurarine?
Definition
motor end plate nicotinic antagonist
Term
what kind of drug is pancuronium?
Definition
motor end plate nicotinic antagonist
Term
what kind of drug is atracurium?
Definition
motor end plate antagonist
Term
what kind of drug is succinylcholine?
Definition
motor end plate depolarizer
Term
what kind of drug is botulinum toxin?
Definition
blocks Ach release
Term
general action of muscarinic receptor antagonist
Definition

compete with Ach for binding

effect cell muscarinic cholinergic receptors

Term
side effects of muscarinic receptor antagonists
Definition
dry mouth
constipation
decreased sweating
mydriasis (dilated pupil)
urinary retention
tachycardia
decreased lacrimation
precipitation of glaucoma
decreased resp secretions

tachycardia - M2 receptors
rest - M3 receptors
Term
mechanism of tachycardia side effects of muscarinic receptor antagonists
Definition
mediated via M2 receptors - decreases cAMP normally
Term
mechanism of side effects of muscarinic receptor antagonists?

what side effect is different and why?
Definition
mediated through M3 receptors - increase Ca

tachycardia is different - M2 receptors
Term
sensitivity of innervated organs to muscarinic receptor antagonists
Definition
differ depending on organ

salivary, bronchial, and sweat secretions - very sensitive; most frequent side effects
Term
atropine type
Definition
blocking agent
muscarinic receptor antagonist
prototype drug
Term
atropine origin
Definition
natural plant alkaloid from belladonna plant
contained in Jimson weed
Term
atropine structure
Definition
uncharged, tertiary amine
Term
atropine action
Definition
blocks all subtypes of muscarinic receptors (M1-M5)
used in urgent situation
Term
effects of atropine in the eye
Definition
blocks contraction of the iris circular (constrictor) muscle - produce mydriasis
blocks contraction of ciliary muscle - produce cycloplegia (loss of accommodation)
Term
effects of atropine in the GI tract
Definition
reduces both secretion and motility
inhibits stomach, small bowel and large bowel contractions - decrease transit time
Term
effects of atropine on sweating
Definition
decreases thermoregulatory sweating
Term
effects of atropine on heart
Definition
induces tachycardia
Term
effects of atropine on lungs
Definition
bronchodilation
Term
effects of atropine on CNS
Definition
almost no effect at therapeutic doses although it crosses BBB

muscarinic receptor blocker and not a nicotinic receptor blocker
Term
does atropine cross BBB?
Definition
YES
Term
pharmacological effects expected of atropine (muscarinic receptor antagonist)?
Definition
mydriasis
cycloplegia
reduce GI secretion and motility
decrease thermoregulatory sweating
tachycardia
bronchodilation
no CNS effects
Term
mechanism of atropine poisoning
Definition
results from overdose - including atropine or smoke from Jimson weed
Term
effects of atropine poisoning
Definition
parasympathetic blockade:
dilated pupils
decreased bowel sounds
tachycardia
dry mouth
dry skin
flushing
fever (inhibition of sweat)
delirium
hallucinations
restlessness that may convert to coma
Term
treatment of atropine poisoning
Definition
symptomatic
may include administration of physostigmine (penetrates into CNS)
Term
scopolamine type
Definition
blocking agent
muscarinic receptor antagonist
Term
scopolamine structure
Definition
naturally occuring belladonna alkaloid
pharmacologically and structurally similar to atropine
Term
effects of scopolamine
Definition
drowsiness
amnesia
blocks receptors in vestibular apparatus and prevents motion sickness
Term
how does scopolamine differ from atropine?
Definition
exerts more CNS actions
Term
side effects of scopolamine?
Definition
similar to atropine - parasympathetic blockade
Term
propantheline type
Definition
blocking agent
muscarinic receptor antagonist
synthetic blocker
Term
propantheline structure
Definition
quarternary amine
Term
does propantheline cross the BBB?
Definition
NO; not effectively
Term
selectivity of propantheline?
Definition
gastric acid secretion and GI motility

modest use in peptic ulcer disease
Term
propantheline use
Definition
antispasmodic in urinary incontinence
rhinitis
treatment of ulcers
Term
ipratropium type
Definition
blocking agent
muscarinic receptor antagonist
Term
ipratropium structure
Definition
quarternary derivative from atropine
Term
does ipratropium cross the BBB?
Definition
NO
Term
ipratropium action
Definition
blocks all subtypes of muscarinic receptors
Term
ipratropium use
Definition
reversible airway disease - primarily asthma, COPD as well

slower acting, longer action than B2 agonists (like albuterol)
Term
tiotropium type
Definition
blocking agent
muscarinic receptor antagonist
Term
tiotroprium structure
Definition
quaternary derivative from atropine
Term
how does tiotroprium compare to ipratroprium?
Definition
longer duration of action
Term
selectivity of tiotroprium?
Definition
some selectivity for M1 and M3 over M2

use as inhaler - less likely to get side effects in heart; localize delivery of drug
Term
tiotroprium use
Definition
reversible airway disease
Term
what drugs are used as pre-anesthetic meds to reduce salivary and resp secretions and induce amnesia?
Definition
atropine and scopolamine
Term
what drug is used as an effective anti-motion sickness agent?
Definition
scopolamine
Term
what drugs are used in Parkinson's Disease?
Definition
muscarinic receptor antagonists

PD - striatal cholinergic neurotransmission is not adequately balanced by dopamine neurotransmission
Term
what drugs are used to decrease secretions of the nasopharynx for treatment of the common cold?
Definition
atropine, scopolamione, and synthetic muscarinic receptor antagonists (ipratropium)
Term
what drugs are used for management of peptic ulcers?
Definition
synthetic muscarinic receptor antagonist agents
Term
what is used as an intestinal antispasmodic agent to inhibit contractions contributing to cramping abdominal pain?
Definition
muscarinic receptor antagonists
Term
what drug is applied topically to the eye to induce cycloplegia for retinal exams and treat acute iritis?
Definition
atropine and related compounds
Term
what is used to reverse poisoning from irreversible organophosphate inhibitors?
Definition
atropine
Term
what drugs are used for reversible airway disease?
Definition
ipratropium and tiotroprium
Term
why are ganglionic blocking drugs rarely used in medicine?
Definition
because of severe side effects resulting from non-selective blockade of Ng receptors in sympathetic and parasympathetic ganglia
Term
what are the prototype ganglionic blocking drugs?
Definition
hexamethonium and trimethaphan

do not have specificity over nicotinic or muscarinic receptors; lack specificity
Term
what do the side effects of ganglionic blocking drugs depend on?
Definition
depend on whether sympathetic or parasympathetic systems predominate in any given tissue
Term
what are the side effects of ganglionic blocking drugs?
Definition
constipation - caused by blockade of enteric ganglia
atony of the urinary bladder - caused by parasympathetic blockade
decreased sweating
vasodilation - due to blockade of a1 receptor (sympathetic control) of arteries
Term
what does neuromuscular transmission rely on?
Definition
Ach release at the motor end plate
Term
botulinus toxin class of blocking agent?
Definition
poison the nerve terminal
Term
mechanism of botulinus toxin?
Definition
prevents vesicle docking and release at nerve terminal
thus prevents Ach release and initiation of signal
Term
selectivity of boulinus toxin
Definition
non-selective
blocks release from all cholinergic nerves
Term
botulinus toxin use
Definition
directly applied to certain involuntary muscles of eye for treatment of stabismus (wandering eye)
Term
what are the 3 classes of neuromuscular blocking agents?
Definition
1. poison the nerve terminal - botulism
2. competitive (non-depolarizing) motor end plate blockade
3. depolarizing motor end plate blockade
Term
what class of drugs are used for skeletal muscle relaxation during surgery?
Definition
competitive (non-depolarizing) motor end plate blocking agents
Term
who is very sensitive to competitive (non-depolarizing) motor end plate blocking agents?

what are they used for in these patients?
Definition
patients with myasthenia gravis are very sensitive

used as a diagnostic procedure
Term
what antagonizes competitive blockade of the motor end plate?
Definition
administration of cholinesterase inhibitor
Term
d-Tubocurarine type
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker
Term
is d-tubocurarine absorbed orally?
Definition
NO
Term
why is d-tubocurarine not absorbed orally?
Definition
because it contains 2 quarternary nitrogen functions
Term
half life of d-tubocurarine?
Definition
long; 80-120 min
Term
problems (side effects) with d-tubocurarine
Definition
**releases histamine
may reduce BP
increases resp secretions
produces some degree of bronchospasm
increases salivary secretions
Term
what is a possible complication for all drugs that generate neuromuscular block?
Definition
release of histamine
Term
selectivity of d-tubocurarine
Definition
not completely selective
can induce some degree of ganglionic blockade - may contribute to hypotensive effects due to cross reaction and non-specific reactions with Ng receptors
Term
atracurium type
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker
Term
atracurium duration of action
Definition
intermediate; 30-40 mins
Term
pancuronium type
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker
Term
pancuronium duration of action
Definition
long; 120-180 min
Term
mivacurium type
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker
Term
mivacurium duration of action
Definition
short; 12-18 min
Term
metabolism of mivacurium
Definition
plasma cholinesterases
bolus admin has to occur within 18 mins after initial admin due to short half life
Term
newer competitive (non-depolarizing) motor end plate blocking agents end in...
Definition
-urium or -onium
Term
newer competitive (non-depolarizing) motor end plate blocking agents work as
Definition
competitive antagonists at Nm receptors
Term
newer competitive (non-depolarizing) motor end plate blocking agents differ in
Definition
duration of action
Term
newer competitive (non-depolarizing) motor end plate blocking agents have less
Definition
**histamine releasing properties
Term
newer competitive (non-depolarizing) motor end plate blocking agents are more
Definition
**selective for Nm receptors
Term
newer competitive (non-depolarizing) motor end plate blocking agents are more
Definition
potent
can get desired effect at lower concentrations
Term
what 2 drugs combine with cholinergic receptors to produce persistent depolarization?
Definition
succinylcholine and decamethonium (nicotinic agonists)
Term
succinylcholine and decamethonium type
Definition
nicotinic agonists
depolarizing motor end plate blocking agents
Term
depolarizing motor end plate agents action
Definition
prevent repolarization of the motor end plate
Term
depolarizing motor end plate blocking agents produce ____ before relaxation
Definition
transient contraction of skeletal muscle
Term
what intensifies blockade by depolarizing motor end plate blocking agents?
Definition

cholinesterase inhibitors - both are targeting the same receptor on cholinesterase

 

succinylcholine and decamethonium are metabolized by plasma cholinesterases

Term
succinylcholine and decamethonium are metabolized by
Definition
plasma cholinesterases
Term
depolarizing motor end plate blocking agents use
Definition
short-lasting neuromuscular blockade
e.g. tracheal intubation
Term
succinylcholine type
Definition
depolarizing motor end plate blocking agent
Term
succinylcholine structure
Definition
ester of 2 choline residues with succinic acid
Term
succinylcholine duration of action
Definition
short; 6-8 min
Term
succinylcholine inactivation
Definition
relatively rapid
by plasma cholinesterases
Term
possible side effects of succinylcholine
Definition
malignant hyperthermia
histamine release
Term
what is malignant hyperthermia?
Definition
persistent release of Ca from SR - cause skeletal muscle contraction
patients stiffen and temp increasingly rises to over 105 degrees
can be fatal
Term
who is susceptible to malignant hyperthermia?
Definition
patients with a mutation in the rhyanidine receptor (incidental target of inhalation anesthetics)
commonly mutation/susceptibility is not known in a patient
Term
how do you treat malignant hyperthermia?
Definition
dantrolene - inhibits Ca release from the SR
Term
decamethonium type
Definition
depolarizing motor end plate blocking agent
Term
decamethonium action
Definition
produces neuromuscular block of moderate duration
Term
decamethonium duration
Definition
moderate
Term
decamethonium side effects
Definition
does not cause histamine release
Term
healthy 25 yo man undergoes surgery requiring general anesthesia
unremarkable intubation and induction of anesthesia using IV succinylcholine and inhaled halothane
during surgery - develops muscle rigidity, tachycardia, and temp rapidly rises
what is the mechanism of action of succinycholine?
Definition
depolarization (sustained) of the motor end plate
Term
healthy 25 yo man undergoes surgery requiring general anesthesia
unremarkable intubation and induction of anesthesia using IV succinylcholine and inhaled halothane
during surgery - develops muscle rigidity, tachycardia, and temp rapidly rises
what reaction is occurring in the patient?
Definition
malignant hyperthermia
Term
healthy 25 yo man undergoes surgery requiring general anesthesia
unremarkable intubation and induction of anesthesia using IV succinylcholine and inhaled halothane
during surgery - develops muscle rigidity, tachycardia, and temp rapidly rises
what drug should be given?
Definition
dantrolene
interfere with Ca release from SR
Term
use of succinylcholine as an adjunct to general anesthetics during surgery is based on its ability to?
Definition
act like Ach - cause depolarization of muscle end plate
Term
continued exposure of muscle end plates to succinylcholine results in their
Definition
desensitization (repolarization) - end plate repolarizes but cannot readily be depolarized
receptor can no longer be the target of Ach
Term
35 yo man has surgery to for hernia repair
after - complains of diffuse muscle aches; most likely caused by skeletal muscle relaxant
temp - 100F
what is likely about the muscle relaxant?
Definition
agent causes persistent end plate depolarization and desensitization

myalgia - common adverse reaction of depolarizing agents like succinylcholine; can also cause hyperkalemia and malignant hyperthermia
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