Term
| what kind of drug is pirenzapine? |
|
Definition
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|
Term
| what kind of drug is atropine? |
|
Definition
|
|
Term
| what kind of drug is scopolamine? |
|
Definition
|
|
Term
| what kind of drug is propantheline? |
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Definition
|
|
Term
| what kind of drug is ipratropium? |
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Definition
|
|
Term
| what kind of drug is tiotropium? |
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Definition
|
|
Term
| what kind of drug is hexamethonium |
|
Definition
| nicotinic ganglionic antagonist |
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|
Term
| what kind of drug is tubocurarine? |
|
Definition
| motor end plate nicotinic antagonist |
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|
Term
| what kind of drug is pancuronium? |
|
Definition
| motor end plate nicotinic antagonist |
|
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Term
| what kind of drug is atracurium? |
|
Definition
| motor end plate antagonist |
|
|
Term
| what kind of drug is succinylcholine? |
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Definition
| motor end plate depolarizer |
|
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Term
| what kind of drug is botulinum toxin? |
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Definition
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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 |
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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 |
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Term
|
Definition
blocking agent
muscarinic receptor antagonist
prototype drug |
|
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Term
|
Definition
natural plant alkaloid from belladonna plant
contained in Jimson weed |
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Term
|
Definition
| uncharged, tertiary amine |
|
|
Term
|
Definition
blocks all subtypes of muscarinic receptors (M1-M5)
used in urgent situation |
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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) |
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Term
| effects of atropine in the GI tract |
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Definition
reduces both secretion and motility
inhibits stomach, small bowel and large bowel contractions - decrease transit time |
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|
Term
| effects of atropine on sweating |
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Definition
| decreases thermoregulatory sweating |
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|
Term
| effects of atropine on heart |
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Definition
|
|
Term
| effects of atropine on lungs |
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Definition
|
|
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 |
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|
Term
|
Definition
|
|
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 |
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|
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 |
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|
Term
| treatment of atropine poisoning |
|
Definition
symptomatic
may include administration of physostigmine (penetrates into CNS) |
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|
Term
|
Definition
blocking agent
muscarinic receptor antagonist |
|
|
Term
|
Definition
naturally occuring belladonna alkaloid
pharmacologically and structurally similar to atropine |
|
|
Term
|
Definition
drowsiness
amnesia
blocks receptors in vestibular apparatus and prevents motion sickness |
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|
Term
| how does scopolamine differ from atropine? |
|
Definition
|
|
Term
| side effects of scopolamine? |
|
Definition
| similar to atropine - parasympathetic blockade |
|
|
Term
|
Definition
blocking agent
muscarinic receptor antagonist
synthetic blocker |
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|
Term
|
Definition
|
|
Term
| does propantheline cross the BBB? |
|
Definition
|
|
Term
| selectivity of propantheline? |
|
Definition
gastric acid secretion and GI motility
modest use in peptic ulcer disease |
|
|
Term
|
Definition
antispasmodic in urinary incontinence
rhinitis
treatment of ulcers |
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|
Term
|
Definition
blocking agent
muscarinic receptor antagonist |
|
|
Term
|
Definition
| quarternary derivative from atropine |
|
|
Term
| does ipratropium cross the BBB? |
|
Definition
|
|
Term
|
Definition
| blocks all subtypes of muscarinic receptors |
|
|
Term
|
Definition
reversible airway disease - primarily asthma, COPD as well
slower acting, longer action than B2 agonists (like albuterol) |
|
|
Term
|
Definition
blocking agent
muscarinic receptor antagonist |
|
|
Term
|
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
|
Definition
| reversible airway disease |
|
|
Term
| what drugs are used as pre-anesthetic meds to reduce salivary and resp secretions and induce amnesia? |
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Definition
|
|
Term
| what drug is used as an effective anti-motion sickness agent? |
|
Definition
|
|
Term
| what drugs are used in Parkinson's Disease? |
|
Definition
muscarinic receptor antagonists
PD - striatal cholinergic neurotransmission is not adequately balanced by dopamine neurotransmission |
|
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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
|
|
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 |
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|
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
|
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
|
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker |
|
|
Term
| is d-tubocurarine absorbed orally? |
|
Definition
|
|
Term
| why is d-tubocurarine not absorbed orally? |
|
Definition
| because it contains 2 quarternary nitrogen functions |
|
|
Term
| half life of d-tubocurarine? |
|
Definition
|
|
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
|
|
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
|
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker |
|
|
Term
| atracurium duration of action |
|
Definition
|
|
Term
|
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker |
|
|
Term
| pancuronium duration of action |
|
Definition
|
|
Term
|
Definition
neuromuscular blocking agent
competitive (non-depolarizing) motor end plate blocker |
|
|
Term
| mivacurium duration of action |
|
Definition
|
|
Term
|
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
|
|
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
|
|
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
|
|
Term
| depolarizing motor end plate blocking agents use |
|
Definition
short-lasting neuromuscular blockade
e.g. tracheal intubation |
|
|
Term
|
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
|
|
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
|
Definition
| depolarizing motor end plate blocking agent |
|
|
Term
|
Definition
| produces neuromuscular block of moderate duration |
|
|
Term
|
Definition
|
|
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
|
|
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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|
