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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
bupivacaine
infiltration
nerve block
spinal
epidural
what is the utility of vasoconstrictors
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
cocaine has inherent vasoconstriction
bc of its sympathomimetics effects