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149 Cards in this Set
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|
what muscarinic agonist is SHORT ACTING
diagnose bronchial hyperactivity and asthmatic conditions only hydrolyzed by true AChE |
METHACHOLINE (provocholine)
|
|
not broken down by either true or pseudoAChE
PURE MUSCARINIC AGONIST and STIMULATE SM of bladder of GI over the heart TX postoperative distention, gastric atony, urinary retention, reflux esophagitis |
BETHANECHOL (urecholine)
|
|
not broken down by either true or pseudo AChE
Nicotinic AND muscarinic activity --> side effects --> use topically in eye for wide (open) angle glaucoma |
CARBACHOL (iospto carchachol)
|
|
cross BBB --> CNS effects --> drug of choice to treat wide angle glaucoma
not broken down by true or pseudo-AChE |
PILOCARPINE
|
|
what drug is used to treat xerostomia and narrow angle glaucoma until surgery can be performed (combined with physostigmine)?
|
pilocarpine
|
|
what is the drug of choice to treat dry mouth associated with Sjogren's syndrome?
|
more selective than pilocarpine
CEVEMELINE (Evoxac) |
|
what are the side effects of muscarinic receptor agonists?
|
extension of their actions on SM, glands, heart
urinary frequency, diarrhea, bronchiole constriction, salivation use of cholinergic stimulants contraindicated in asthma, hyperthyroidism, peptic ulcers |
|
what drug is the anxiety-competitive antagonist basically causes anxiety (photophobia and blurry vision)? affect ALL muscarinic receptors
|
Atropine
|
|
what drug is long acting and causes anxiety?
|
atropine
|
|
what drug is used as an antidote for organophosphate intoxication?
|
atropine
|
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what drug is used as an adjunct for myasthenia gravis to reduce muscarinic side effects due to AChE inhibition?
|
atropine
|
|
what is atropine flush?
|
increase in body temperature
block sweating treated with AChE inhibitors (physostigmine) |
|
what drug is shorter acting
causes sedation |
SCOPOLAMINE
|
|
treat motion sickness and bedwetting
|
SCOPOLAMINE
|
|
used for retinal examinations
shorter acting than atropine |
homatropine
|
|
used for retinal examinations
shorter acting than atropine and homatropine |
tropicamide
|
|
used to treat peptic ulcers but has numerous side effects
block ganglionic transmission and antagonize ACh at muscarinic receptors |
methantheline (banthine)
propantheline (Pro-banthine) |
|
What are the side effects of muscarinic receptor antagonists?
|
very dangerous in patients with narrow angle gaucoma
antihistamines, phenothiazines, tricyclic antidepressants have enough antimuscarinic receptor activity to cause atropine-like toxicity (atropine flush) |
|
what are the contraindications for muscarinic receptor antagonists?
|
prostatic hypertrophy
achalasaia intestinal atony |
|
what drug is a competitive antagonist at M1 receptors (myenteric plexus and cerebral cortex)?
|
pirenzepine
|
|
where are nicotinic receptors located?
|
autonomic ganglia
adrenal medulla motor endplate region |
|
DMPP (dimethyl 4-phenyl piperazinium)
|
stimulates nicotinic receptors
|
|
classical nicotinic receptor antagonist that acts at GANGLIA, competitively IS
|
hexamethonium
|
|
classical nicotinic receptor antagonist that acts at motor endplate, acts competitively
|
d-tubocurarine
|
|
where are muscarinic receptors located?
|
SM
glands heart |
|
how many types of muscarinic receptors are there?
|
5 distinc gene products
|
|
known AGONISTS do or do not discriminate between muscarinic receptors subtypes
|
DO NOT
|
|
what is used to diagnose achalasia?
|
metacholine
|
|
what are the side effects of bethanecol?
|
best of synthetic drugs but cause gastric distress and bronchial constriction
|
|
what drug has been used to counter atropine but may cause convulsions?
|
physostigmine (AChE inhibitor)
|
|
what drugs are used for irritable bowel syndrome?
|
methantheline
propantheline block ganglionic transmission and antagonist ACh at muscarinic receptor -can be used to treat peptic ulcer numerous side effects |
|
which receptor is quick and short-lived and ALWAYS excitatory?
|
nicotinic receptors
|
|
which receptor is slow, long-lasting and can be excitatory or inhibitory?
|
muscarinic receptors
|
|
what drug can stimulate ganglionic transmission without causing receptor desensitization?
|
DMPP
specific for nictonic receptor on autonomic ganglia and at adrenal medulla not at NMJ |
|
primary pathway of ganglionic transmission is mediated by
|
nicotinic receptors on ganglia--> fast excitatory potential
|
|
secondary pathway of ganglionic transmission
|
slow excitatory produced by ACh on M1 receptors
slow inhibitory potential produced by ACh from preganglionic nerve terminals, activate M2 receptor |
|
what drug blocks dopamine action at ganglia
increase GI tract motility without stimulating HCl secretion? |
metoclopramide
|
|
are ganglionic stimulants used therapeutically?
|
NO
|
|
nicotine in low doses
|
considered a nonselective nicotinic receptor agonist bc it binds a variety of nicotinic receptors on autonomic ganglia
stimulate both parasympathetic and sympathetic ganglia |
|
what are the cardiovascular effects of low dose nicotine (ganglionic stimulate)
|
increase TPR, increase sympathetic ganglia ventricular contraction, increase venous return, increase blood pressure
|
|
low dose nicotine does what to the respiratory system?
|
activate chemoreceptors in aortic arch and carotid body to INCREASE RESPIRATION
some direct action on medulla to INCREASE RESPIRATION |
|
what does nicotine due to the GI tract?
|
has dominant tone on GI tract
can INCREASE GI tract motility and INCREASE HCl release |
|
what are central effects of low dose nicotine?
|
cause emesis at chemoreceptor trigger zone
increase ADH release to cause fluid retention |
|
at high doses, nicotine acts as a
|
ganglionic blocker
rapidly absorbed through skin and can enter placenta readily |
|
nicotine at high doses on respiratory system
|
desensitizes nicotinic receptors at medulla oblongata to stop breathing
desensitizes nicotinic receptor at motor endplate region to cause paralysis of diaphragm and intercostal muscles |
|
WERE used chronically to lower BP but caused too many side effects
|
ganglionic blockers
|
|
what drug is used only chronically to control BP in patients with acute dissecting aortic aneurysm (ideal bc they inhibit sympathetic reflexes, reduce rate of rise of BP at site of tear)
|
ganglionic blockers - can also be used to produce hypotension during surgery to minimize hemorrhage at operative sites
|
|
Tetraethylammonium (TEA)
|
+charged
short duration of action |
|
Hexamethonium
|
+charged
does not cross BBB long duration of action not well absorbed |
|
Trimethaphan
|
+charged
short acting inactive orally MUST BE GIVEN BY IV |
|
mecamylamine
|
long-acting non-charged
can cause CNS effects used chronically for hypertension if pt can tolerate side effects |
|
what are the side effects of ganglionic blockers?
|
interfere with body's ability to maintain homeostasis
abolish autonomic effects such as miosis/accomodation of eye reduce transmission through division of ANS which dominant parasympathetic tone at SA node GI motility is inhibited causing constipation |
|
major side effects of blocking ganglionic blockers
|
1. orthostatic hypotension due to decrease sympathetic tone in veins
2. urinary retention block PNS 3. impotence due to blocking both PNS and SNA that control erection and ejaculation |
|
pseudo-AChE found in what cells?
|
plasma
glial |
|
pseudo or true AChE is more sensitive to organophosphate inhibition?
|
pseudoAChE
|
|
slow excitatory potential in secondary pathway can be blocked by
|
pirezipine (block M1 receptor)
|
|
slow inhibitory potential in secondary pathway can be blocked by
|
Metoclopramide (block M2)
|
|
delay neurotoxicity can be caused by what drugs?
|
echothiophate and DFP
|
|
what are sx of delayed neurotoxicity?
|
ataxia
muscle paralysis demyelination 8-14 days after drug exposure |
|
can be caused by certain general anesthetics such as halothane + succinylcholine
increase Ca2_ causing exaggerated skeletal contraction and INCREASED body temperature |
malignant hyperthermia
|
|
nicotinic receptor antagonists are mainly used to produce what during general anesthesia so that less anesthetic is required?
|
skeletal muscle relaxation
|
|
what drugs release histamine and are dangerous to asthmatic patients?
|
tubocurarine
succinylcholine |
|
what is the antidote for d-tubocurarine overdose?
|
neostigmine and endrophonium
|
|
what are the therapeutic uses for AChE inhibitors?
|
tx for GI tract or bladder atony
glaucoma (narrow and wide angle) myasthenia gravis: diagnosis and treatment antidote for d-tubocurarine overdose terminate attack of supraventricular tachycardia |
|
what drug acts centrally to produce skeletal muscle relaxation?
|
cyclobenzaprine
|
|
cyclobenzaprine is used to treat
what are the side effects? |
muscle spasms
cause dry mouth, drowsiness, tachycardia, blurred vision |
|
what drug acts on skeletal muscle to produce relaxation?
chelate Ca2+ in SR postjunctionally PROVIDE MUSCLE RELAXATION in PATIENTS with stroke, MS, malignant hyperthermia |
dantrolene
|
|
used to treat blepharospasm and to cosmetically reduce facial aging
treat cerebral palsy spasms |
botulinum toxin
|
|
chelates calcium prejunctionally to reduce risk of ACh release
|
aminoglycosides antibiotics (neomycine, kanamycin)
tetracycline |
|
increases histamine release --> rarely used
broken down if given orally blockade of ganglionic transmission through sympathetic divsion of ANS--> decreases TPR only used as a surgical adjunct during general anesthesia |
d-tubocurarine
|
|
long acting
little histamine release INCREASES BP if given rapidly |
pancuronium
|
|
intermediate duration of action
no ganglionic blockade or histamine release can cause tachycardia |
vecuronium
|
|
short acting
breakdown by pseudo-AChE release vasodilator histamine--> decreases BP bradycardia prolong apnea increase plasma K+ levels malignant hyperthermia produce muscle fasciculations prior to muscle relaxation |
depolarizing blocking drugs-succinylcholine
|
|
is there an antidote for succinylcholine overdose?
|
NO
|
|
increases histamine release --> rarely used
broken down if given orally blockade of ganglionic transmission through sympathetic divsion of ANS--> decreases TPR only used as a surgical adjunct during general anesthesia |
d-tubocurarine
|
|
long acting
little histamine release INCREASES BP if given rapidly |
pancuronium
|
|
intermediate duration of action
no ganglionic blockade or histamine release can cause tachycardia |
vecuronium
|
|
short acting
breakdown by pseudo-AChE release vasodilator histamine--> decreases BP bradycardia prolong apnea increase plasma K+ levels malignant hyperthermia produce muscle fasciculations prior to muscle relaxation |
depolarizing blocking drugs-succinylcholine
|
|
is there an antidote for succinylcholine overdose?
|
NO
|
|
increases histamine release --> rarely used
broken down if given orally blockade of ganglionic transmission through sympathetic divsion of ANS--> decreases TPR only used as a surgical adjunct during general anesthesia |
d-tubocurarine
|
|
long acting
little histamine release INCREASES BP if given rapidly |
pancuronium
|
|
intermediate duration of action
no ganglionic blockade or histamine release can cause tachycardia |
vecuronium
|
|
short acting
breakdown by pseudo-AChE release vasodilator histamine--> decreases BP bradycardia prolong apnea increase plasma K+ levels malignant hyperthermia produce muscle fasciculations prior to muscle relaxation |
depolarizing blocking drugs-succinylcholine
|
|
is there an antidote for succinylcholine overdose?
|
NO
|
|
what drug PULLS organophosphates off esteratic site of AChE
must be given rapidly to prevent AGING of AChE? |
pralidoxime
|
|
what are the two irreversible AChE inhibitors?
|
echothiophate
mipafox |
|
long acting and positive charge --> no CNS effect
used topically in eye for wide angle glaucoma |
echothiophate
|
|
what organophosphate insecticide can cause delayed neurotoxicity?
|
Mipafox
|
|
what two drugs can be used to treat Alzheimer's?
|
Tacrine and Donepezil
|
|
what drug is used in eyes only with pilocarpine for narrow angle glaucome
no charge so can cross BBB? |
physostigmine
|
|
what drug is used to dx MG?
|
edrophonium
|
|
what drug is used to treat supraventricular tachycardia and overdose of d-tubocurarine like drugs? improve muscle strength upon IV
|
edrophonium
|
|
what drug of choice is used to treat myasthenia gravis
|
pylidostigmine
|
|
what drug is used to treat paralytic ileus bladder atony wide and narrow angle glaucoma?
|
neostigmine
|
|
what are the side effects of reversible AChE inhibitors?
|
bronchial constriction
GI distress diarrhea |
|
what are the side effects of irreversible AChE inhibitors?
|
respiratory arrest can kill by paralyzing diaphragm and intercostal muscles by building up ACh at nicotinic receptors --> desensitized
delay neurotoxicity involve ataxia, muscle paralysis, demyelination |
|
Agent associated with Compound A generation at low flow rates
|
sevoflurane
|
|
agent that can be used to mask induction due to not being pungent
|
sevoflurane
|
|
agent used to reverse Versed (midazolam) anesthesia
|
Flumazenil
|
|
agent used to treat malignant hyperthermia
|
dantrolene
|
|
agent causing vasodilation resulting in a decline in BP
|
propofol
|
|
agent that is associated with emergence phenomena of hallucinations and vivid dreams
|
ketamine
|
|
agent in large doses produces general anesthesia requiring mechanical ventilation but frequently used to provide analgesia with other anesthetics
|
fentanyl
|
|
agent with highest risk of neprhotoxicity and the metabolite responsible for damage
|
methoxyflurane F-
|
|
iv agent that has CNS excitatory effects but produces the least adverse CV effects
|
etomidate
|
|
iv agent that requires a lipid diluent (emulsificant) because its not water soluble
|
propofol
|
|
iv agent that causes cardiac stimulation leading to increased blood pressure, heart rate, CO
|
ketamine
|
|
agent that maintains CO, systemic and coronary vasodilation, has reduced risk of catecholamin-dependent arrythmias
|
isoflurane
|
|
agent associated with tonic-clonic seizures
|
endlurane
|
|
agent associated with highest risk of HEPATITIS
|
halothane
|
|
only dissociative anesthetic in current use. Its use is limited by emergence phenomena: disorientation, sensory and perceptual illusions, and vivid dreams. Perhaps similar to LSD
|
ketamine
|
|
MAC
|
Defined as minimum concentration of an anesthetic gas required to eliminate movement or other response to noxious stimuli in 50% of patients.
|
|
MAC stands for
|
Minimum alveolar concentration
|
|
representative MACs
highest MAC lowest MAC |
highest - Nitrous oxide
lowest - methoxyflurane |
|
MAC is increased by:
|
sympathoadrenal stimulation
chronic alcohol or opiod abuse decreasing age |
|
esters are broken down by
|
butyrlcholinesterase
|
|
amides are broken down by
|
hepatic microsomal system
|
|
esters
short half-life hypersensitivity reactions injectable not surface |
procaine (very widely used) and chloroprocaine
|
|
longer duration of action
ester topical and injectable opthalmic often used in spinal anesthesia |
tetracaine
|
|
esters
Not widely used -Respiratory Tract Anesthetic -CNS Side Effects -CV Side Effects |
cocaine
|
|
esters
topical use ONLY |
benzocaine
|
|
amide
Longer Lasting than Esters -Efficiently Absorbed from Mucous Membranes -All Routes, except eyes |
lidocaine
|
|
amides
long lasting injectable not effective of surface |
Bupivacaine
|
|
local anesthetics-toxicity
|
immune system--allergy
cardiovascular system nervous system |
|
CV toxicity
|
A. Excessive Absorption
B. Direct Suppression of Heart C. Death to CV Collapse- Arrhythmia, Suppression of Electrical Activity D. Cocaine: Sympathomimetic |
|
esters are broken down by
|
butyrlcholinesterase
|
|
amides are broken down by
|
hepatic microsomal system
|
|
esters
short half-life hypersensitivity reactions injectable not surface |
procaine (very widely used) and chloroprocaine
|
|
longer duration of action
ester topical and injectable opthalmic often used in spinal anesthesia |
tetracaine
|
|
esters
Not widely used -Respiratory Tract Anesthetic -CNS Side Effects -CV Side Effects |
cocaine
|
|
esters
topical use ONLY |
benzocaine
|
|
amide
Longer Lasting than Esters -Efficiently Absorbed from Mucous Membranes -All Routes, except eyes |
lidocaine
|
|
amides
long lasting injectable not effective of surface |
Bupivacaine
|
|
local anesthetics-toxicity
|
immune system--allergy
cardiovascular system nervous system |
|
CV toxicity
|
A. Excessive Absorption
B. Direct Suppression of Heart C. Death to CV Collapse- Arrhythmia, Suppression of Electrical Activity D. Cocaine: Sympathomimetic |
|
CNS toxicity of local anesthetics
|
IV injection
suppression of inhibitory pathways consulsion, coma, cardio-respiratory arrest |
|
chloroprocaine can cause what deficits?
|
motor and sensory
|
|
benzocaine used for
|
surface anesthesia, not much systemic
denuded areas poor absorption |
|
infiltration anesthesia
|
Injection into a region without
regard to cutaneous nerve route B. Superficial Tissues C. Intraabdominal Organs |
|
nerve block
|
injection into or about peripheral nerves or nerve plexuses
sensory and motor block |
|
epidural anesthesia
|
epidural space
sacral hiatus, lumbar, thoracic, cervical regions large doses-diffusion |
|
spinal anesthesia
|
Subarachnoid Space in
Lumbar Region B. Positioning, Specific Gravity of drug- desired height of block C. CV Depression D. Headache |
|
CNS toxicity of local anesthetics
|
IV injection
suppression of inhibitory pathways consulsion, coma, cardio-respiratory arrest |
|
chloroprocaine can cause what deficits?
|
motor and sensory
|
|
benzocaine used for
|
surface anesthesia, not much systemic
denuded areas poor absorption |
|
infiltration anesthesia
|
Injection into a region without
regard to cutaneous nerve route B. Superficial Tissues C. Intraabdominal Organs |
|
nerve block
|
injection into or about peripheral nerves or nerve plexuses
sensory and motor block |
|
epidural anesthesia
|
epidural space
sacral hiatus, lumbar, thoracic, cervical regions large doses-diffusion |
|
spinal anesthesia
|
Subarachnoid Space in
Lumbar Region B. Positioning, Specific Gravity of drug- desired height of block C. CV Depression D. Headache |
