Term
what kind of drug is pirenzapine? |
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Definition
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Term
what kind of drug is atropine? |
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Definition
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Term
what kind of drug is scopolamine? |
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Definition
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Term
what kind of drug is propantheline? |
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Definition
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Term
what kind of drug is ipratropium? |
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Definition
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Term
what kind of drug is tiotropium? |
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Definition
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Term
what kind of drug is hexamethonium |
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Definition
nicotinic ganglionic antagonist |
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Term
what kind of drug is tubocurarine? |
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Definition
motor end plate nicotinic antagonist |
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Term
what kind of drug is pancuronium? |
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Definition
motor end plate nicotinic antagonist |
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Term
what kind of drug is atracurium? |
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Definition
motor end plate antagonist |
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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 |
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Definition
compete with Ach for binding
effect cell muscarinic cholinergic receptors |
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Term
side effects of muscarinic receptor antagonists |
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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 |
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Term
mechanism of tachycardia side effects of muscarinic receptor antagonists |
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Definition
mediated via M2 receptors - decreases cAMP normally |
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Term
mechanism of side effects of muscarinic receptor antagonists?
what side effect is different and why? |
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Definition
mediated through M3 receptors - increase Ca
tachycardia is different - M2 receptors |
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Term
sensitivity of innervated organs to muscarinic receptor antagonists |
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Definition
differ depending on organ
salivary, bronchial, and sweat secretions - very sensitive; most frequent side effects |
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Term
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Definition
blocking agent muscarinic receptor antagonist prototype drug |
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Term
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Definition
natural plant alkaloid from belladonna plant contained in Jimson weed |
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Term
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Definition
uncharged, tertiary amine |
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Term
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Definition
blocks all subtypes of muscarinic receptors (M1-M5) used in urgent situation |
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Term
effects of atropine in the eye |
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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
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Term
effects of atropine on lungs |
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Definition
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Term
effects of atropine on CNS |
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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
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Definition
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Term
pharmacological effects expected of atropine (muscarinic receptor antagonist)? |
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Definition
mydriasis cycloplegia reduce GI secretion and motility decrease thermoregulatory sweating tachycardia bronchodilation no CNS effects |
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Term
mechanism of atropine poisoning |
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Definition
results from overdose - including atropine or smoke from Jimson weed |
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Term
effects of atropine poisoning |
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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 |
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Definition
symptomatic may include administration of physostigmine (penetrates into CNS) |
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Term
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Definition
blocking agent muscarinic receptor antagonist |
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Term
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Definition
naturally occuring belladonna alkaloid pharmacologically and structurally similar to atropine |
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Term
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Definition
drowsiness amnesia blocks receptors in vestibular apparatus and prevents motion sickness |
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Term
how does scopolamine differ from atropine? |
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Definition
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Term
side effects of scopolamine? |
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Definition
similar to atropine - parasympathetic blockade |
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Term
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Definition
blocking agent muscarinic receptor antagonist synthetic blocker |
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Term
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Definition
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Term
does propantheline cross the BBB? |
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Definition
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Term
selectivity of propantheline? |
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Definition
gastric acid secretion and GI motility
modest use in peptic ulcer disease |
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Term
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Definition
antispasmodic in urinary incontinence rhinitis treatment of ulcers |
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Term
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Definition
blocking agent muscarinic receptor antagonist |
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Term
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Definition
quarternary derivative from atropine |
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Term
does ipratropium cross the BBB? |
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Definition
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Term
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Definition
blocks all subtypes of muscarinic receptors |
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Term
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Definition
reversible airway disease - primarily asthma, COPD as well
slower acting, longer action than B2 agonists (like albuterol) |
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Term
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Definition
blocking agent muscarinic receptor antagonist |
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Term
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Definition
quaternary derivative from atropine |
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Term
how does tiotroprium compare to ipratroprium? |
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Definition
longer duration of action |
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Term
selectivity of tiotroprium? |
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Definition
some selectivity for M1 and M3 over M2
use as inhaler - less likely to get side effects in heart; localize delivery of drug |
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Term
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Definition
reversible airway disease |
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Term
what drugs are used as pre-anesthetic meds to reduce salivary and resp secretions and induce amnesia? |
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Definition
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Term
what drug is used as an effective anti-motion sickness agent? |
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Definition
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Term
what drugs are used in Parkinson's Disease? |
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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? |
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Definition
atropine, scopolamione, and synthetic muscarinic receptor antagonists (ipratropium) |
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Term
what drugs are used for management of peptic ulcers? |
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Definition
synthetic muscarinic receptor antagonist agents |
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Term
what is used as an intestinal antispasmodic agent to inhibit contractions contributing to cramping abdominal pain? |
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Definition
muscarinic receptor antagonists |
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Term
what drug is applied topically to the eye to induce cycloplegia for retinal exams and treat acute iritis? |
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Definition
atropine and related compounds |
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Term
what is used to reverse poisoning from irreversible organophosphate inhibitors? |
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Definition
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Term
what drugs are used for reversible airway disease? |
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Definition
ipratropium and tiotroprium |
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Term
why are ganglionic blocking drugs rarely used in medicine? |
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Definition
because of severe side effects resulting from non-selective blockade of Ng receptors in sympathetic and parasympathetic ganglia |
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Term
what are the prototype ganglionic blocking drugs? |
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Definition
hexamethonium and trimethaphan
do not have specificity over nicotinic or muscarinic receptors; lack specificity |
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Term
what do the side effects of ganglionic blocking drugs depend on? |
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Definition
depend on whether sympathetic or parasympathetic systems predominate in any given tissue |
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Term
what are the side effects of ganglionic blocking drugs? |
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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 |
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Term
what does neuromuscular transmission rely on? |
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Definition
Ach release at the motor end plate |
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Term
botulinus toxin class of blocking agent? |
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Definition
poison the nerve terminal |
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Term
mechanism of botulinus toxin? |
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Definition
prevents vesicle docking and release at nerve terminal thus prevents Ach release and initiation of signal |
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Term
selectivity of boulinus toxin |
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Definition
non-selective blocks release from all cholinergic nerves |
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Term
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Definition
directly applied to certain involuntary muscles of eye for treatment of stabismus (wandering eye) |
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Term
what are the 3 classes of neuromuscular blocking agents? |
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Definition
1. poison the nerve terminal - botulism 2. competitive (non-depolarizing) motor end plate blockade 3. depolarizing motor end plate blockade |
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Term
what class of drugs are used for skeletal muscle relaxation during surgery? |
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Definition
competitive (non-depolarizing) motor end plate blocking agents |
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Term
who is very sensitive to competitive (non-depolarizing) motor end plate blocking agents?
what are they used for in these patients? |
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Definition
patients with myasthenia gravis are very sensitive
used as a diagnostic procedure |
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Term
what antagonizes competitive blockade of the motor end plate? |
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Definition
administration of cholinesterase inhibitor |
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Term
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Definition
neuromuscular blocking agent competitive (non-depolarizing) motor end plate blocker |
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Term
is d-tubocurarine absorbed orally? |
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Definition
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Term
why is d-tubocurarine not absorbed orally? |
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Definition
because it contains 2 quarternary nitrogen functions |
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Term
half life of d-tubocurarine? |
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Definition
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Term
problems (side effects) with d-tubocurarine |
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Definition
**releases histamine may reduce BP increases resp secretions produces some degree of bronchospasm increases salivary secretions |
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Term
what is a possible complication for all drugs that generate neuromuscular block? |
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Definition
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Term
selectivity of d-tubocurarine |
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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 |
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Term
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Definition
neuromuscular blocking agent competitive (non-depolarizing) motor end plate blocker |
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Term
atracurium duration of action |
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Definition
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Term
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Definition
neuromuscular blocking agent competitive (non-depolarizing) motor end plate blocker |
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Term
pancuronium duration of action |
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Definition
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Term
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Definition
neuromuscular blocking agent competitive (non-depolarizing) motor end plate blocker |
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Term
mivacurium duration of action |
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Definition
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Term
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Definition
plasma cholinesterases bolus admin has to occur within 18 mins after initial admin due to short half life |
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Term
newer competitive (non-depolarizing) motor end plate blocking agents end in... |
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Definition
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Term
newer competitive (non-depolarizing) motor end plate blocking agents work as |
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Definition
competitive antagonists at Nm receptors |
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Term
newer competitive (non-depolarizing) motor end plate blocking agents differ in |
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Definition
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Term
newer competitive (non-depolarizing) motor end plate blocking agents have less |
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Definition
**histamine releasing properties |
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Term
newer competitive (non-depolarizing) motor end plate blocking agents are more |
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Definition
**selective for Nm receptors |
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Term
newer competitive (non-depolarizing) motor end plate blocking agents are more |
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Definition
potent can get desired effect at lower concentrations |
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Term
what 2 drugs combine with cholinergic receptors to produce persistent depolarization? |
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Definition
succinylcholine and decamethonium (nicotinic agonists) |
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Term
succinylcholine and decamethonium type |
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Definition
nicotinic agonists depolarizing motor end plate blocking agents |
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Term
depolarizing motor end plate agents action |
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Definition
prevent repolarization of the motor end plate |
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Term
depolarizing motor end plate blocking agents produce ____ before relaxation |
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Definition
transient contraction of skeletal muscle |
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Term
what intensifies blockade by depolarizing motor end plate blocking agents? |
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Definition
cholinesterase inhibitors - both are targeting the same receptor on cholinesterase
succinylcholine and decamethonium are metabolized by plasma cholinesterases |
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Term
succinylcholine and decamethonium are metabolized by |
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Definition
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Term
depolarizing motor end plate blocking agents use |
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Definition
short-lasting neuromuscular blockade e.g. tracheal intubation |
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Term
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Definition
depolarizing motor end plate blocking agent |
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Term
succinylcholine structure |
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Definition
ester of 2 choline residues with succinic acid |
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Term
succinylcholine duration of action |
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Definition
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Term
succinylcholine inactivation |
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Definition
relatively rapid by plasma cholinesterases |
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Term
possible side effects of succinylcholine |
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Definition
malignant hyperthermia histamine release |
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Term
what is malignant hyperthermia? |
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Definition
persistent release of Ca from SR - cause skeletal muscle contraction patients stiffen and temp increasingly rises to over 105 degrees can be fatal |
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Term
who is susceptible to malignant hyperthermia? |
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Definition
patients with a mutation in the rhyanidine receptor (incidental target of inhalation anesthetics) commonly mutation/susceptibility is not known in a patient |
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Term
how do you treat malignant hyperthermia? |
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Definition
dantrolene - inhibits Ca release from the SR |
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Term
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Definition
depolarizing motor end plate blocking agent |
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Term
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Definition
produces neuromuscular block of moderate duration |
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Term
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Definition
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Term
decamethonium side effects |
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Definition
does not cause histamine release |
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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? |
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Definition
depolarization (sustained) of the motor end plate |
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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? |
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Definition
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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? |
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Definition
dantrolene interfere with Ca release from SR |
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Term
use of succinylcholine as an adjunct to general anesthetics during surgery is based on its ability to? |
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Definition
act like Ach - cause depolarization of muscle end plate |
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Term
continued exposure of muscle end plates to succinylcholine results in their |
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Definition
desensitization (repolarization) - end plate repolarizes but cannot readily be depolarized receptor can no longer be the target of Ach |
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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? |
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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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