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228 Cards in this Set
- Front
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major responses to alpha1 agonists
|
direct vascular contraction (increases BP)
indirect slow HR mydriasis (contracts radial muscles) |
|
clinical uses of alpha1 agonists
|
1.hypotension
2. paroxysmal supraventricular tachycardia 3. nasal decongestant 4. mydriasis to dilate eyes for observation |
|
adverse effects of alpha1 agonists
|
1. hypertension
2. ischemic organ diseases 3. rebound nasal and sinus hyperemia |
|
contraindications of alpha1 agonists
|
1. agents that increase in NE
2. MAOI 3. indirect acting sympathomimetics |
|
example of alpha1 agonist
second messenger? |
phenylephrine
increase IP3 and DAG |
|
clinical use of phenylephrine
|
opthalmological to produce mydriasis
|
|
adverse effect of phenylephrine
|
rebound nasal and sinus hyperemia
|
|
contraindications of phenylephrine
|
drug sensitivity
|
|
response of alpha2 agonist
|
1. vasodilation
2. decrease in aqueous humor production |
|
clinical uses of alpha2 agonist
|
found in brain
1. antihypertensive 2. lower IOP in open angle glaucoma 3. minimize withdrawal effects |
|
adverse effects of alpha2 agonist
|
1. bradycardia
2. CNS effect: dry mouth and sedation 3. sexual dysfunction |
|
contraindications of alpha2 agonist
|
drug hypersensitivity
|
|
example of alpha2 agonist
|
clonidine
|
|
clinical use of clonidine
|
mild to moderate hypertension
use alone or in combination |
|
side effects of clonidine
|
drowsiness
dry mouth GI disturbance muscle weakness withdrawal symptoms |
|
contraindications of clonidine
|
drug sensitivity
|
|
major responses of beta1 agonist
|
increase in Ca2+ influex
increase in rate and force |
|
clinical use of beta1
|
cardiogenic shock
|
|
side effects of beta1
|
CV effects
|
|
contraindications of beta1
|
drug sensitivity
|
|
adverse effects of alpha2 agonist
|
1. bradycardia
2. CNS effect: dry mouth and sedation 3. sexual dysfunction |
|
contraindications of alpha2 agonist
|
drug hypersensitivity
|
|
example of alpha2 agonist
|
clonidine
|
|
clinical use of clonidine
|
mild to moderate hypertension
use alone or in combination |
|
side effects of clonidine
|
drowsiness
dry mouth GI disturbance muscle weakness withdrawal symptoms |
|
contraindications of clonidine
|
drug sensitivity
|
|
major responses of beta1 agonist
|
increase in Ca2+ influex
increase in rate and force |
|
clinical use of beta1
|
cardiogenic shock
|
|
side effects of beta1
|
CV effects
|
|
contraindications of beta1
|
drug sensitivity
|
|
ex of beta1
|
dobutamine
|
|
clinical use of dobutamine
|
cardiac stimulant
used for acute cardiac failure NOT chronic must be given by IV cardiogenic shock |
|
adverse effects of dobutamine
|
arrhythmias
tolerance develops with use |
|
response to beta2 agonist
|
bronchodilation: short or long half life
uterine dilation (ritodrine) |
|
clinical use of beta2 agonist
|
bronchodilators
1.asthma 2. COPD Tocolytic agents used to inhibit labor in late term gestation |
|
adverse effects of beta 2 agonists
|
1. uncommon when administered as an inhalant
2. beta1 tachycardia/widening pulse pressure 3.beta2 widening pulse pressure, decrease K+, skeletal muscle tremors |
|
contraindications of beta2 agonists
|
1. coronary artery disease
2. arrhythmias 3. diabetes 4. hyperthyroidism 5. co-administered with MAO inhibitor 6. indirect acting sympathomimetics |
|
ex of beta2 agonists
|
albuterol -short half life
salmetol -long formoterol -long ritodrine for uterine contractions |
|
clinical use of albuterol
|
relax bronchial SM with little effect on heart rate
1. asthma 2. COPD |
|
adverse effects of albuterol
|
1. angina
2. CNS stimulant 3. GI disturbances 4. muscle cramps |
|
contraindications for albuterol
|
1. drug sensitivity
2. tachyarrhythmias 3. pregnancy |
|
major response of EPI
|
1. increase CO, increase VR, cardiac stimulant
WIDEN PULSE PRESSURE 2. vasoconstriction 3. bronchodilation |
|
clinical uses of EPI
|
1. vasoconstriction - alpha1
2. bronchodilation - beta2 3. cardiac stimulant - beta1 4. lower intraocular pressure- wide angle glaucoma |
|
adverse effect of EPI
|
1. ARRYTHMIAS beta1
2. headache alpha1 3. cerebral hemorrhae 4. anxiety symptoms (somatic) |
|
responses of NE
|
endogenous CV effects
1. direct alpha1 casoconstriction 2. beta1 cardiac stimulation 3. increase in TPR + CP |
|
clinical use of NE
|
vasoconstriction
|
|
adverse effects of NE
|
1. arrhythmias
2. cerebral hemorrhage |
|
response of dopamine
|
1. vascular relaxation
2. cardiac stimulant 3. BP DOSE DEPENDENT |
|
clinical uses of dopamine
|
1. increase renal blood flow: shock and cardiac failure
2. cardiac stimulant: for cardiac failure Must be given IV |
|
contraindication
|
arrythmias
|
|
response to isoproterenol
|
direct beta2 vasodilation/decrease TPR
force rate + reflex cardiac, increase CO widen pulse pressure bronchodilation (beta2) GI/bladder relaxation (beta2) uterine dilation in late gestation (beta2) |
|
clinical use of isoproterenol
|
cardiac stimulant beta1
bronchodilation beta2 dromotropic agent beta1 AV node stimulant in heat block and bradycardia |
|
response to fenoldopam
|
D1 agonist
vasodilation will cause increase in cAMP |
|
clinical use of fenoldopam
|
severe hypertensioon
short halflife, not absorbed by gut IV only |
|
adverse effects of fenoldopam
|
hypotension
tachycardia |
|
response to isoproterenol
|
direct beta2 vasodilation/decrease TPR
force rate + reflex cardiac, increase CO widen pulse pressure bronchodilation (beta2) GI/bladder relaxation (beta2) uterine dilation in late gestation (beta2) |
|
response to bromocriptine
|
D2 agonist
suppresses prolactin release from adenoma and shrinks tumor, improve motor function will decrease cAMP |
|
clinical use of isoproterenol
|
cardiac stimulant beta1
bronchodilation beta2 dromotropic agent beta1 AV node stimulant in heat block and bradycardia |
|
clinical use of bromocriptine
|
hyperprolactinemia
Parkinson's |
|
response to fenoldopam
|
D1 agonist
vasodilation will cause increase in cAMP |
|
adverse effects of bromocriptine
|
CNS, CV, GI
|
|
clinical use of fenoldopam
|
severe hypertensioon
short halflife, not absorbed by gut IV only |
|
what drugs will stimulate NE release?
|
tyramine
ephedrine amphetamines |
|
adverse effects of fenoldopam
|
hypotension
tachycardia |
|
what drugs will inhibit NE release?
|
cocaine
tricyclic antidepressant |
|
response to bromocriptine
|
D2 agonist
suppresses prolactin release from adenoma and shrinks tumor, improve motor function will decrease cAMP |
|
clinical use of bromocriptine
|
hyperprolactinemia
Parkinson's |
|
adverse effects of bromocriptine
|
CNS, CV, GI
|
|
what drugs will stimulate NE release?
|
tyramine
ephedrine amphetamines |
|
what drugs will inhibit NE release?
|
cocaine
tricyclic antidepressant |
|
clinical uses of nonselective alpha blocker
|
1. phreochromocytoma
2. benign prostatic obstruction 3. migraine headaches (ergot alkaloids) |
|
mechanism of nonselective alpha blockers
|
affect prejunctional alpha2 receptor --> reflex tachycardia
|
|
adverse effects of alpha antagonists
|
1. tachycardia (due to alpha2)
2. orthostatic hypotension 3. nasal congestion |
|
clinical use of selective alpha1 blocker
|
1. benign prostatic hyperplasia
2. hypertension 3. congestive heart failure 4. pheochromocytoma |
|
what is the advantage of selective alpha 1 vs nonselective alpha blockers?
|
less reflex tachycardia
|
|
adverse effect of selective alpha1
|
orthostatic hypotension usually becomes tolerated
|
|
uroselective alpha1A blockers -ex
|
tamsulosin
|
|
nonselective alpha blocker -ex
|
phentolamine
phenoxybenzamine ergot alkaloids |
|
selective alpha1 blocker ex
|
prazocin
|
|
clinical use of alpha1A blocker
|
BEST TX for benign prostatic hyperplasia
|
|
clinical uses of nonselective alpha blocker
|
1. phreochromocytoma
2. benign prostatic obstruction 3. migraine headaches (ergot alkaloids) |
|
mechanism of nonselective alpha blockers
|
affect prejunctional alpha2 receptor --> reflex tachycardia
|
|
adverse effects of alpha antagonists
|
1. tachycardia (due to alpha2)
2. orthostatic hypotension 3. nasal congestion |
|
clinical use of selective alpha1 blocker
|
1. benign prostatic hyperplasia
2. hypertension 3. congestive heart failure 4. pheochromocytoma |
|
what is the advantage of selective alpha 1 vs nonselective alpha blockers?
|
less reflex tachycardia
|
|
adverse effect of selective alpha1
|
orthostatic hypotension usually becomes tolerated
|
|
uroselective alpha1A blockers -ex
|
tamsulosin
|
|
nonselective alpha blocker -ex
|
phentolamine
phenoxybenzamine ergot alkaloids |
|
selective alpha1 blocker ex
|
prazocin
|
|
clinical use of alpha1A blocker
|
BEST TX for benign prostatic hyperplasia
|
|
clinical uses of nonselective alpha blocker
|
1. phreochromocytoma
2. benign prostatic obstruction 3. migraine headaches (ergot alkaloids) |
|
mechanism of nonselective alpha blockers
|
affect prejunctional alpha2 receptor --> reflex tachycardia
|
|
adverse effects of alpha antagonists
|
1. tachycardia (due to alpha2)
2. orthostatic hypotension 3. nasal congestion |
|
clinical use of selective alpha1 blocker
|
1. benign prostatic hyperplasia
2. hypertension 3. congestive heart failure 4. pheochromocytoma |
|
what is the advantage of selective alpha 1 vs nonselective alpha blockers?
|
less reflex tachycardia
|
|
adverse effect of selective alpha1
|
orthostatic hypotension usually becomes tolerated
|
|
uroselective alpha1A blockers -ex
|
tamsulosin
|
|
nonselective alpha blocker -ex
|
phentolamine
phenoxybenzamine ergot alkaloids |
|
selective alpha1 blocker ex
|
prazocin
|
|
clinical use of alpha1A blocker
|
BEST TX for benign prostatic hyperplasia
|
|
adverse effect of alpha1a blocker
|
retrograde ejaculation
secondary to relaxation of bladder neck but able to AVOID orthostatic hypotension |
|
ex of nonselective beta blockers
|
propanolol
nadolol timolol pindolol |
|
nonselective alpha-beta blockers
|
labetalol
carvedilol |
|
beta1-selective blockers
|
metoprolol
esmolol: short half life atenolol: low lipid solubility betaxolol: opthal |
|
clinical uses of nonselective beta blockers
|
1. hypertension if stable angina present
2. angina 3. heart failure decreases heart work and protects against arrythmias 4. decreases eye humor production |
|
mechanism of nonselective beta blockers
|
high lipid solubility
enters guts and CNS high first pass metabolism has membrane-stabilizing activity |
|
adverse effects of beta blockers
|
1. induce CHF or bradycardial arrythmias
2. sudden withdrawal in angina pt--> death 3. bronchospasms 4. sleep disturbance, depression 5. endocrine: insulin-induce hypoglycemia in diabetic patients 6. mask hypoglycemia in diabetics |
|
clinical uses of phenoxybenzamine
|
symptomatic management of pheochromocytoma
hypertensive crisis caused by sympathomimetic amindes micturition problems |
|
adverse effects of phenoxybenzamine
|
decreases BP
GI postural hypotension reflex stimulation pupil constriction partial agonist/antagonist of 5HT2A |
|
mechanism of phenoxybenzamine
|
irreversible and noncompetitive
decreases vasoconstriction by EPI and NE |
|
contraindications of phenoxybenzamine
|
drug sensitivity
|
|
clinical use of prazocin -
|
hypertension
PTSD benign prostatic hyperplasia scorpion stings |
|
prazocin mechanism
|
alpha1 antagonist
relaxes SM lower BP PDE inhibition decrease SM contraction in bladder sphincter |
|
adverse effects of prazocin
|
orthostatic hypotension
postural syncope |
|
clinical uses of yohimbine
|
limited clinical use
sexual dysfunction diabetic neuropathy postural hypotension |
|
mechanism of yohimbine
|
alpha2 blocker
increases SNS outflow, increase BP/HR |
|
side effects of yohimbine
|
increase motor activity
tremors antagonist of 5HT R anxiety insomnia |
|
clinical use of propranolol
|
hypertension
angina arrhythmias tachycardia pheochromocytoma prophylaxis of migraine tremor (parkinson/alcohol withdrawal) decrease eye humor production --> wide-angle glaucoma FINE MUSCLE TREMORS anxiety migraine headaches |
|
mechanism of propranolol
|
nonselective beta angtagonist
constrict bronchial SM! |
|
adverse effects of propranolol
|
induce CHF and bradycardial arrhythmias
withdrawal from anginal pt--> sudden death bronchospasms sleep disturbances and depression insulin-induce hypoglycemia |
|
atenolol -uses
|
beta1 selective blocker
hypertension elderly patients with isolated systolic HT ANGINA post MI treatment *no beta2 means eliminate bronchoconstrictor effect |
|
betaxolol - uses
|
beta1 selective blocker
CHRONIC OPEN ANGLE GLAUCOMA hypertension |
|
butoxamine - uses
|
beta2 blocker
used for research only |
|
clozapine - uses
|
refractory schizophrenia
D4 antagonist weak action on other receptors |
|
labetalol
|
beta and alpha1 antagonist
partial beta2 agonist |
|
carvedilol
|
beta and alpha1 antagonist
antioxidant anti-ishemic agent improves survival in chronic heart failure |
|
pheochromocytoma
|
neuroendocrine tumor located off the medulla of the adrenal glands
causes large amounts of secretion of catecholamines |
|
how do you tx pheochromocytoma?
|
prazocin (alpha1)
phenoxybenzamine (alpha) metyrosine for inoperable tumors |
|
priapism
|
erection for more than 4 hrs
use alpha1 agonist to vasoconstrict penile arterial spplu |
|
ADHD
|
use alpha2 agonist like clonidine or methylphenidate (Ritalin)
|
|
BPH
|
1. watch if mild
2. surgery if severe 3. pharmacological tx: 5-alpha reductase to shrink prostate alpha1 adrenergic antagonists like Prazocin and Tamsulosin (better bc no orthostatic hypotension but get retrograde ejaculation) |
|
Angina
|
beta blockers:
propranolol atenolol |
|
arrhythmias
|
beta blockers
propranolol |
|
congestive heart failure
|
alpha1 angatonist such as prazosin
beta blockers such as propranolol, metroprolol, carvedilol |
|
glaucoma
|
beta blockers, timolol is the preferred drug
betaxolol (beta1) selective antagonist |
|
hypertension
|
beta blockers propranolol
alpha1 blockers prazocin atenolol (beta1) reserpine (many side effects) betaxolol (beta1) |
|
ischemic heart disease
|
beta blockers can be used
timolol propranolol metoprolol (beta1) |
|
timolol
|
low local anesthetic action
used in glaucoma |
|
. Dr. Blowhard, an anesthesiologist, reviews the chart of Mrs. Schmidt, who is scheduled for a lumpectomy the next day. Because of her underlying medical conditions, he wishes to use a combination of agents that will give rapid induction and rapid recovery. Which agent is commonly used to increase the absorption and decrease the MAC of other agents?
|
nitrous oxide
|
|
. Mr. Flowmax undergoes prostate surgery. The tumor has spread to neighboring lymph nodes and the procedure takes much longer than planned. The patient develops renal failure post-operatively with an elevated fluoride concentration. Which agent was most probably used?
|
methoxyflurane
metabolism of methoxyflurane results in F- ion which is nephrotoxic |
|
Mrs. Schmidt is undergoing a mastectomy for breast cancer. As her anesthesiologist, you notice a sudden increase in temperature and muscular rigidity three hours into the surgery. You promptly notify the surgeon, turn off the flow of the anesthetic agent, administer dantrolene IV and place a cooling device under the patient. Which agent most commonly causes this adverse reaction to anesthesia?
|
Halothane
|
|
As the anesthesiologist for Miss. Doe, you are conducting a pre-surgical interview to determine appropriate anesthetic agents. She discloses an allergy to peanuts and eggs. Which agent do you decide may cause anaphylaxis in this patient?
|
propofol, commonly emulsified in egg lecithin
|
|
. Grandpa Jones has a 20-year history of coronary artery disease. He will be undergoing a short surgical procedure to implant a pacemaker. Which IV agent is most appropriate for him?
|
Etomidate (lowest risk of adverse CV effects and commonly used for short procedures)
|
|
Little Betsy suffers from partial seizures. She presents with a simple break of the radius and ulna. Which IV agent would be preferred for procedural anesthesia in this patient?
|
benzodiazepines reduces seizures
MIdazolam |
|
Diethyl ether, cyclopropane, and ethylene were effective and widely used anesthetics. What is the primary reason they were discontinued?
|
ethylene - explosive
diethyl ether - flammable cyclopropane - very explosive |
|
mechanism of action of IV anesthetics is most probably
|
a) potentiating the action of an inhibitory ionophore (the GABAA receptor).
b) blocking the action of excitatory ionophores (Nicotinic ACh & NMDA receptors). |
|
Jerry, a 3 year old, is scheduled for surgery to repair a fractured left humerus. The anesthesiologist selected Midazolam from the other benzodiazepines diazepam or lorazepam primarily because:
|
Midazolam (Versed) – Water Soluble
Diazepam and Lorazepam – not water soluble and slow to onset |
|
John Doe is scheduled to undergo coronary bypass surgery. The surgeon wishes to use a short acting opioid during initial stages of the procedure due to concerns of chest wall rigidity. The opioid analgesic with the shortest duration of action is:
|
Remifentanil
Duration of analgesia: Morphine (hours)> Demerol > Fentanyl > Sufentanil > Alfentanil > Remifentanil (minutes) |
|
Agent with highest risk of nephrotoxicity and the metabolite responsible for damage
|
methoxyflurane
|
|
IV agent that has CNS excitatory effects but produces the least adverse cardiovascular effects
|
etomidate
|
|
IV agent that requires a lipid diluent (emulsificant/use egg) because its not water soluble
|
propofol
|
|
IV agent that causes cardiac stimulation, leading to increased blood pressure, heart rate and cardiac output
|
ketamine
|
|
Agent that in large doses produces general anesthesia requiring mechanical ventilation but frequently used to provide analgesia with other anesthetics
|
fentanyl
|
|
Agent that is associated with emergence phenomena of hallucinations and vivid dreams
|
ketamine
|
|
Agent causing vasodilation resulting in a decline in blood pressure
|
propofol
|
|
agent used to treat malignant hypothermia
|
dantrolene
|
|
agent used to reverse Versad (midazolam)
|
flumazenil
|
|
Agent that can be used for mask induction due to not being pungent
|
sevoflurane
|
|
Agent associated with Compound A generation at low flow rates
|
sevoflurane
|
|
agent associated with the highest risk of hepatitis
|
halothane
|
|
agent associated with tonic-clonic seizures
|
enflurane
|
|
Agent that maintains cardiac output, systemic and coronary vasodilation and has reduced risk of catecholamine-dependent arrythmias
|
isoflurane
|
|
ALL CNS drugs must be______to cross the BBB?
|
lipid soluble
|
|
drugs with __________ result in rapid induction and recovery
|
low blood solubility
|
|
what is the only dissociative anesthetic in current use
|
ketamine
|
|
drugs with high ______ are the most potent and are effective at low mac
|
lipid solubility
|
|
what has low blood and lipid solubility?
what does it offer? |
nitrous oxide
rapid induction and recovery but low potency |
|
what has high lipid and blood solubility
|
halothane
high potency but slow induction |
|
MAC
|
minimum alveolar concentration
minimum conc of an anesthetic gas required to eliminate mvmt or other response to noxious stimuli in 50% if patients |
|
representative MACs
Nitrous oxide Methoxyflurane |
Nitrous oxide has high MAC
methoxyflurane has low MAC |
|
MAC is increased by
|
sympathoadrenal stimulation
chronic alcohol and opiod abuse decreasing age |
|
MAC is decreased by
|
nitrous oxide
hypothermia increasing age pregnancy acute alcohol abuse (drunk) |
|
what has high lipid and blood solubility
|
halothane
high potency but slow induction |
|
MAC
|
minimum alveolar concentration
minimum conc of an anesthetic gas required to eliminate mvmt or other response to noxious stimuli in 50% if patients |
|
representative MACs
Nitrous oxide Methoxyflurane |
Nitrous oxide has high MAC
methoxyflurane has low MAC |
|
MAC is increased by
|
sympathoadrenal stimulation
chronic alcohol and opiod abuse decreasing age |
|
MAC is decreased by
|
nitrous oxide
hypothermia increasing age pregnancy acute alcohol abuse (drunk) |
|
what has high lipid and blood solubility
|
halothane
high potency but slow induction |
|
MAC
|
minimum alveolar concentration
minimum conc of an anesthetic gas required to eliminate mvmt or other response to noxious stimuli in 50% if patients |
|
representative MACs
Nitrous oxide Methoxyflurane |
Nitrous oxide has high MAC
methoxyflurane has low MAC |
|
MAC is increased by
|
sympathoadrenal stimulation
chronic alcohol and opiod abuse decreasing age |
|
MAC is decreased by
|
nitrous oxide
hypothermia increasing age pregnancy acute alcohol abuse (drunk) |
|
Oswald coefficient = blood: gas partition coefficient
|
anesthetic concentration in blood divided by concentration of anesthetic in gas phase in contact with it at EQ
measures the solubiltity of anesthetic in blood |
|
higher oswald coefficient means
|
slower speed of induction
|
|
nitrous oxide has ____oswald coefficient
|
low
|
|
methoxyflurane has ____ ostwald coefficient
|
high
|
|
________ is defined as surgical anesthesia
|
Stage III plane III
|
|
what stage is medullary paralysis
|
Stage IV
|
|
stage III
|
surgical anesthesia with regular respiration skeletal muscle relaxation and decreased eye reflexes
|
|
stage III plane III
|
surgical anesthesia patietn begins to lose the ability to use chest and abdominal muscle for breathing
requires assisted ventilaion |
|
Stage IV
|
medullary paralysis with severe depression of respiratory and vasomotor center
|
|
halothane is metabolized to
|
triflouroacetyl chloride and hydrogen bromide by CYP450 and then triflouroacetic acid
|
|
what drug has the highest fraction metabolized?
|
methoxyflurane
|
|
what ion damages the kidney by inhibiting sodium chloride reabsorption in thick ascending limb of loop of henle
inhibits ADH-dependent reabsorption of water perhaps through inhibition of AC |
Flouride
|
|
malignant hyperthermia
|
very high body temperature and skeletal rigidity
|
|
tx malignant hyperthermia with
|
dantrolene
|
|
action of dantrolene
|
inhibits release of calcium from SR and rapid chilling of patient
|
|
sevoflurane
|
degrades to compound A in anesthesia machines by reacting with CO2 absorbents especially at low flow rates
|
|
general effects of general anesthesia
|
myocardial depression
respiratory depression nausea and emesis increased cerebral blood flow decreased cerebral metabolic demand |
|
Toxicity of general anesthesia
|
halothane is hepatotoxic
methoxyflurane is nephrotoxic enflurane is proconvulsant ALL CAN CAUSE MALIGNANT HYPOERTHERMIA BUT HALTHANE IS MOST COMMONLY INVOLVED |
|
ester or amide
more susceptible to hydrolysis by plasma and liver esterases |
ester
|
|
ester or amide
shorter duration of action |
ester
|
|
ester or amide
widely distributed and taken up by most tissues |
amide
|
|
ester or amide
metabolized so rapidly that their systemic distribution is probably insignificant |
ester
|
|
ester or amide
metabolized by plasma butyrylcholinesterase and secondarily by liver esterases |
ester
|
|
amides are metabolized by
|
hepatic microsomal metabolism
|
|
name the esters
|
procaine
cocaine tetracaine benzocaine |
|
name the amides
|
lidocaine
mepivacaine bupivacaine etidocaine dibucaine prilocaine |
|
local anesthetics are toxic to
|
immune system - allergic response due to primarily ester anesthetic
-triggering IgE and mast cells CV - absorption into bloodstream can block sodium channels in heart nervous system CNS toxicity, IV injection, suppression of inhibitory pathway, convulsion, coma cardio-respiratory arrest |
|
procaine
|
extremely short half life
metabolized by plasma esterases potential for hypersensitivity poorly absorbed from mucous membrane USED FOR INFILTRATION AND NERVE BLOCK OR SPINAL ANESTHESIA NOT TOPICAL |
|
cocaine
|
produce surface anesthesia of respiratory tract
|
|
chloroprocaine
|
extremely short half-life
probably least toxic contraindicated for IV regional block bc induce thrombosis |
|
tetracaine
|
longer duration of action than procaine and chloroprocaine
used topical for eyes, skin, mucous membranes or injectable spinal anesthesia |
|
benzocaine
|
topical in creams and ointments, not absorbed systemically
for denuded areas, poor absorption |
|
short acting local anesthetics
|
procaine and chloroprocaine
|
|
long-acting local anesthetics
|
tetracaine
bupivacaine etidocaine |
|
lidocaine
|
more prompt more intense longer-lasting more extensive than procaine
metabolized by liver microsomal enzymes topical/systemic/injected -just not eyes |
|
bupivacaine
|
more toxic but less will enter infant bc high materal protein binding
chosen for particular use bc longer duration injectable |
|
prilocaine
|
rapid hepatic metabolism
|
|
mepivacaine route of administration
|
infiltration
nerve block epidural |
|
long-acting local anesthetics
|
tetracaine
bupivacaine etidocaine |
|
lidocaine
|
more prompt more intense longer-lasting more extensive than procaine
metabolized by liver microsomal enzymes topical/systemic/injected -just not eyes |
|
bupivacaine
|
more toxic but less will enter infant bc high materal protein binding
chosen for particular use bc longer duration injectable |
|
prilocaine
|
rapid hepatic metabolism
|
|
mepivacaine route of administration
|
infiltration
nerve block epidural |
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bupivacaine
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infiltration
nerve block spinal epidural |
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what is the utility of vasoconstrictors
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retards absorption by decrease blood flow to and away from injection area
increase duration by 50% (procaine and lidocaine) reduces systemic absorption and toxic effects cocaine is the only local anesthetic to produce vasoconstriction varying degrees of vasodilation |
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cocaine has inherent vasoconstriction
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bc of its sympathomimetics effects
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