EXAM 1 PQ Flashcards
Mu opiod receptor activation leads to supraspinal analgesia via
Decrease release of GABA from periaqueductal gray matter
Activatoin of opiod receptors leads to activation of which intracellular transduction mechanism
G protein
most hydrophillic opioid
Morphine
Altered duration and potency with reduced renal function due to this metabolite
Morphine 6 glucuronide
Clinical effect of fentanyl terminated by
Redistribution
OPIOD with LONGEST CONTEXT sensitive half time
FENTANYL
OPIOD with longest duration after EPIDURAL
MORPHINE
Fentanyl to a low dose bupivacaine decrease
Failed block incidence
Best opiods for patient with combined hepatic and renal impairment
REMIFENTANYL
Converted from product to active
CODEINE
OPIOD that cause TACHYCARDIA
MEPERIDINE
Decrease the risk of respiratory depression
CLONIDINE
Biliary spasm side effect of
MORPHINE
OPIOD metabolite to cause seizure
Normeperidine ( from meperidine)
Prolonged administraton lead to loss of drug effect
tolerance
Best choice for patients taking MAOI
Morphine to prevent serotonin syndrome
OPIOD for surgery requiring quick recovery
REMIFENTANYL
Primary mechanism of waking following induction dose of thiopental
Redistribution of drug to lean tissues
Compared to thio, the reason patient awakens more rapidly form IV methohexital is
Metho has higher rate of hepatic clearance
Short acting barbiturate to accelerate elimination of for exmple phenobarbital give
SODIUM BICARBONATE
Following administration CV effect of thiopental
PERIPHERAL VENODILATION
Barbiturates on pulmonary
brief apnea lasting 30-45 sec
Uremia increases free fraction of thiopental by
100%
Thiopental cannot reduce the CMRO2 below 50% because
it only affects the neuron’s functional cellular processes
Barbiturates are the classic anesthetic trigger agent for
PORPHYRIA
PROPOFOL rapid termination of action due to
Redistribution to the periphery
Organ responsible for extra hepatic metabolism of propofol is
Kidneys
Propofol increase elimination half time in elderly due to
age related
Which hemodynamic decreases the most after induction of anesthesia with propofol
Systolic BP
Which IV anesthetic , causes the greatest decrease in mean BP
Propofol
After propofol most frequent effect on Resp system
APNEA
IV anesthetics causing EPILEPTOGENIC ACTIVITY
Methohexital
Most common side effect of propofol during induction
HYPOTENSION
PROPOFOL infusion syndrome is characterized by
Rhabdomyolysis
Causes ADRENOCORTICAL SUPPRESION
ETOMIDATE
Not associated with ETOMIDATE
increase IOP
ETOMIDATE on CNS
Decrease CMRO2, decrease CBF, Increase CPP
To increase water solubility of ETOMIDATE formulated with
PROPYLENE GLYCOL
Metabolism of etomidate
Liver by ester hydrolysis
Not a pharmacological effect of benzo
ANALGESIA
MOA of midazolam
allosteric modulation of GABA binding to GABAa receptor
Significantly increase metabolism of midazolam
Chronic alcohol consumptino
Benzo with inactive metabolite
Lorazepam
Midazolam hemodynamic changes
Decrease CIFm
Flumazenil reverse effects of
benzo
competitive antagonists
elimination directly proportional to drug clearance, and concentration
1st order elimination
HIGHLY lipid soluble
ETOMIDATE
ETOMIDATE INDUCTION DOSE
0.2-0.3 mg/kg
May attenuate CV stimulating effects of ketamine
Benzos
Net effect of ketamine induction is
Increase BP, HR, CO and Myocardial oxygen consumption.
Ketamine in critically ill patient
decrease in BP and CO , who have depleted their catecholamines stores and lack ability to compensate via the SNS
Catalepsy
Ketamine
Dissociative anesthesia
Ketamine
Contraindicated in brain injury
KETAMINE (increase ICP)
Potent stimulator of bronchial secretion______give?
Ketamine; give with glycopyrrolate
Emergence Delirium
Ketamine
Prolong effect of ketamine
Diazepam
Change in hepatic blood flow affect
KETAMINE metabolism
Use in burn patients
KETAMINE
What is emergence delirium attenuated by
Benzodiazepines
Ketamine IV dose
1-2mg/kg
Ketamine redistribution is
WITHIN 10 MIN
Minimal effect of RR, mV
Ketamine
Use to induce seizures
Methohexital
Allergic to propofol use
Barbiturates
Decrease BP and Increase HR
Barbiturates
Dose dependent respiratory Depression
Barbiturates
Decrease ICP aand CBF
Barbiturates
Lack histamine release
ETOMIDATE
NO alteration in HR, CO CVP or PWCP
ETOMIDATE
Benzo with perfusion limited clearance (high hepatic ratio)
Midazolam
Capacity limited clearance
Lorazepam and diazepam
Benzo containing propylene glycol
Diazepam and lorazepam
Dose related reduction in CMRO2
Benzos
Relatively safe drug
Benzo
Depress swallowing reflex and upper airway reflex
Benzos
Most likely to be un-ionized (uncharged) at physiological pH
Alfentanyl
swallow and corneal reflexes present with this med
Ketamine
Morphine vs fentanyl solubility
Morphine is LOW lipid solubility
Thrombophlebitis associated with
Etomidate
myoclonus associated with
Etomidate
nausea and vomiting associated with
ETOMIDATE
inhibition of steroid synthesis
ETOMIDATE
not approved in the U.S. for sedation of pediatric ICU patients
PROPOFOL
______administration may increase intraoperative wheezing in patients with asthma (causes bronchodilation)
Propofol (Diprivan)
EEG activation, consistent with possible epileptogenic activity
ETOMIDATE
More likely to require fentanyl (Sublimaze) to reduce hemodynamic effects caused by direct laryngoscopy
ETOMIDATE
More likely to cause anterograde amnesia
Midazolam
Suppression of recall for events before amnestic drugs are administered:
Retrograde amnesia
Suppression of recall for events after amnestic drugs are administered:
Anterograde amnesia
Reduction the cerebral edema following surgery; useful in head injury cases and management of cerebral ischemia:
barbiturates
Main tissue reservoir for opiods
SKELEtAL MUSCLE
Anatomical sites of opioid action: pain-modulating descending pathways –
rostral ventral medulla
locus ceruleus
periaqueductal gray
Principal alkaloid in opium (derived from opium poppy)
morphine
Most reliable indicator of opioid-mediated respiratory depression:
depressed patient response to a carbon dioxide challenge
Opioid direct action on neurons:
may close a voltage-gated calcium channel on presynaptic nerve terminals, resulting in reduced transmitter release
Contraindications/caution for opioid use:
Addison’s disease
impaired pulmonary function
patients with head injury
Morphine effect/effects on bronchomotor status.
Bronchoconstrictive secondary to histamine release.
Worsening of asthmatic attacks
Meperidine administration results in effects generally similar to those caused by
morphine
Analgesic effects associated with codeine occurs because of its
conversion of morphine.
Morphine, principally as morphine-3-glucuronide, is eliminated by
renal glomerular filtration
2 are examples of drugs that increase meperidine induced respiratory depression.
Chlorpromazine and tricyclic antidepressant medications (first-generation agents)
Opiods exhibits local anesthetic properties which can be observed following epidural administration.
Meperidine
Increased cerebral blood flow with increased cerebrospinal fluid pressure secondary to drug-induced respiratory depression leading to increased carbon dioxide levels.
meperidine
IV administration of _________is likely to produce a notable elevation in heart rate.
meperidine
OPioids may induce delayed resp depression
Fentanyl or sufentanil administration may induce delayed respiratory depression
principal, primary anesthetic in cardiac surgery or for patients with pre-existing poor cardiac status because of LIMITED CARDIOVASCULAR ACTIVITY
Fentanyl or sufentanil
Slowest time to peak analgesic effect following IV administration:
MEPERIDINE
Administration of nonsteroidal anti-inflammatory drugs may induce pain relief comparable to that provided by about
60 mg codeine.
The major ion channel affected by benzodiazepine sedative-hypnotics is:
Chloride
T/F Benzodiazepine administration results in comparable degrees of neuronal depression as barbiturates.
false
T/F Benzodiazepines are not GABA type A receptor activators but rather modulate GABA effects at the receptor.
True
T/F Benzodiazepine sedative hypnotic drugs are examples of patients which even at high doses do not induce by themselves surgical anesthesia.
True
T/F Benzodiazepines at higher doses appropriately qualify as anaesthetics.
False
Midazolam has been associated with
both decreased respiratory rate in tidal volume, even given without accompanying CNS depressant agents.
The major receptor system targeted by clinically used benzodiazepines is:
GABA
T/F At normal benzodiazepine doses cardiovascular effects are usually minor in normal individuals.
TRUE
Highly plasma protein bound
Benzo
Which one of the following benzodiazepines is classified as an intermediate-acting drugs
Lorazepam
Refers to drug concentration producing 50% of that drug’s maximal effect:
EC50
This type of drug, even at doses that fully saturate the receptor, does not elicit a response as great as that seen with a full agonist
partial agonist
TI
TD50/ED50
In women, morphine associated with
Greater analgesic potency
Greatest amount of ROSTRAL SPREAD into intrathecal space (cephalad migration into the CSF)
Morphine
Most common side effect of opioids
Pruritus
Route associated with the reactivation of the HSV
Epidural
Mu receptor activation associated with
Bradycardia
Morphine does not
Cause MYOCARDIAL DEPRESSION
2 medications that are most effective at reducing OPIOID INDUCED HYPERANALGESIA caused by REMIFENTANYL?
Ketamine
Magnesium
Which benzodiazepine is more effective in preventing emergence delirium?
Midazolam is more effective than diazepam
Which barbiturate has a greater lipid solubility and what does it result in?
Thiobarbiturates, results in greater hypnotic potency, faster onset and shorter duration of action.
Which agent produces modest decreases in hepatic blood flow?
Thiopental.
Which agent is useful for induction of anesthesia in patients with increased ICP?
Thiopental
What is the opioid receptor activity of ketamine?
Interacts with mu, delta, and kappa receptors. May be an antagonist at mu receptors and an agonist at kappa receptors.
Which agent is the only barbiturate with actions sufficiently different from the thiobarbiturates to offer an alternative to other IV induction agents?
Methohexital.
What is the modest fall in renal blood flow and glomerular filtration rate due to?
Decrease in BP and CO.
Which agent is the most potent enzyme inducer of the barbiturates?
Phenobarbital
Which agent is contraindicated in hypovolemic
patients?
Thiopental
Which agent causes anaphylaxis in 1:30,000 patients?
Thiopental
Which agent can be mixed with propofol for production of TIVA and has more stable hemodynamics than propofol and fentanyl without incidence of emergence reactions?
Ketamine
What is the metabolism of thiopental dependent on?
Thiopental has a low hepatic extraction ratio so metabolism is dependent on hepatic enzyme activity not hepatic blood flow.
What is the metabolism of methohexital dependent on?
CO and hepatic blood flow
Where is methohexital metabolized?
Liver
What side effect occurs with thiopental and thiamylal (1:30,000)
histamine release
Etomidate
Use cautiously in patients with focal seizures. Can cause hypotension if given to hypovolemic patients
Pain occuring during IV injection is frequent (80%).
Use with caution or avoid in patients that may require an intact cortisol response (sepsis or hemorrhage patients).
Etomidate
What is the side effect with overdose or large doses of barbiturates required to lower ICP?
Direct mYocardial depression
Disadvantage of mEthohexital
Increased incidence of excitatory phenomena such as involuntary skeletal muscle movements (myoclonus) and hiccough.
Between barbiturates and isofulrane which agent is preferable if profound EEG is desired?
Barbiturates
How are thiobarbiturates metabolized?
Break down in extra hepatic sites such as the kidneys
What are the risk factors of emergence delirium associated with ketamine?
Age >15, females, doses >2 mg/kg, history of personality disorders or frequent dreaming.
What beneficial effect does propofol have on the lungs?
Causes bronchodilation and decreases the incidence of intra-operative wheezing in patients with asthma.
What beneficial effect does ketamine have on the lungs?
Has bronchodilatory activity (successful in treatment of status asthmaticus).
May increase ICP placing patients with intracranial pathology at risk. Increases salivary secretions necessitating protection of airway.
Ketamine
What agent can impair neutrophil functions?
Thiopental.
How much of thiopental and methohexital is excreted unchanged in the urine?
Less than 1%.
How can venous thrombosis be prevented with barbiturate use?
By using diluted concentrations: methohexital 1%, thiopental 2.5%.
What agents may increase the incidence of emergence delirium?
Atropine or droperidol, and scopolamine.
What agents may decrease the incidence of emergence delirium?
Thiopental or inhalation agents.
Sufentanyl vs morphine
1000 times more potent than morphine
Meperidine vs morphine
0.1 times more potent than morphine
Remifentanyl vs morphine
100 times more potent than morphine
Alfentanyl vs morphine
10 times more potent than morphine
Hydromorphone vs morphine
8 times more potent than morphine
Opiods with active metabolites
Morphine
Meperidine
Opioids with anticholinergic effects
Meperidine
Demythlation in the liver metabolism of
Meperidine
Can lead to SEROTONIN SYNDROME
Meperidine with MAOI
What is the effect equillibration of ALfentanyl
1.4 min
Why is the effect equilibration time so fast in ALFENTALY
Low degree of ionization
90 % unionized in Physiologic pH
Alfentanyl
For short but INTENSE periods of stimulation used
Alfentanyl
Dose of remi
0.1 to 1mcg/kg/min
Mu agonist rapid on and off
Remifentanyl
Context sensitive half life of remifentanyl
4 minutes
Is Bradycardia a side effect of Narcan
No
AMnesia associated with Midazolam
ANTEROGRADE
Clearance directly related to
blood flow to organ
Extraction ratio
Steady state is achieved after
5 half lives
Circumstance for Ion trapping
Maternal ALKALOSIS
Fetal ACIDOSIS
Constant AMOUNT per unit of time (ZA)
ZERO
Constant FRACTION per unit of time (FF)
FIRST order
Perfusion dependent HEPATIC elimination meds
Fentanyl
Lidocaine
Propofol
CAPACITY dependent HEPATIC elimination meds
Rocuronium
DIAZEPAM
Acidic drugs
better ABSORBED in ACIDIC
Basic drugs
BASIC Better ABSORBED in BASIC
Drugs dose and plasma concentration is PHARMD or PHARK
PHARMACOKINETICS
Effect site and clinical effect is PHARMD or P ARK
Pharmacodynamics
Dose response curve x axis is (PX)
potency
Dose response curve y axis is
Efficacy
From top to bottom dose response curve
Agonist
Partial agonist
Antagonist
Inverse Agonist
TI formula
LD50/ ED 50
Chiral molecules non-superimposable
Enantiomers
Levorototary rotaes
counterclockwise
WK ACIDS ph and pKa
if ph < pka NON-IONIZED
if ph>pka IONIZED
WK Bases pH and pKa
If ph PKA IONIZED
