Exam 2 Study Guide Flashcards
Sevoflurane (Ultane)
-MAC %
-B/G Partition Coefficient
-O/G Partition Coefficient
2%
0.6
50 -potent
Isoflurane (Forane)
-MAC %
-B/G Partition Coefficient
-O/G Partition Coefficient
1.15%
1.4
99 -very potent
Nitrous Oxide
-MAC%
-B/G Partition Coefficient
-O/G Partition Coefficient
105%
0.47
1.4 -not potent at all
Desflurane (Suprane)
-MAC%
-B/G Partition Coeffficient
-O/G Partition Coefficient
5.8%
0.42
18.7 -not very potent
Halothane (Fluothane)
-MAC%
-B/G Partition Coefficient
-O/G Partition Coefficient
0.75%
2.3
224 -very potent
MAC and potency is _ proportional
inversely
How blood/gas solubility of drug influences uptake/distribution:
lower the coefficient= faster anesthetic rises in lungs; faster induction + emergence
higher the coefficient= slower anesthetic rises in lungs; slower induction + emergence
How CO influences uptake/distribution:
If CO increases, onset of all anesthetics SLOW (Palv)
-affects SLOW drugs more than FAST drugs bc of Fa/Fi ratio-increased CO removes drug at quicker rate
-ISO uptake is affected the most
How oil/gas solubility influences uptake/distribution:
describes potency; if highly potent it is slow to go in, slow to come out; halothane most potent, N20 least
-high OG solubility = more potent
-low OG solubility = less potent
How V/Q deficits influence uptake/distribution: which drugs are effected most?(3)
less than normal lungs go to sleep slower than normal lungs
-there is a decrease in onset rate especially for LOW blood/gas coefficient or more INSOLUBLE drugs-N2O, SEVO, DES
-sports car slows down much faster than old beater can
All volatile anesthetics are _ _ . The _ protects the compound making it more stable and _ being added prevents the molecule from being metabolized into toxic byproducts
halogenated ethers
Halogen
Fluorine
The only inorganic anesthetic gas is _
Nitrous oxide (no carbon group)
Amnesia is the loss of memory and acts on the _ and _
hippocampus
amygdala
Unconsciousness is controlled through the _, _, and _.
cortex
thalamus
brainstem
Analgesia is the loss of pain and occurs through the _ _
spinothalamic tract
Immobility is the loss of motor control and occurs thru the _ _ and the _ _ _
spinal cord
central pattern generators
CNS effects of anesthesia are _ -dependent with _ requiring the lowest dose (MAC) followed by sedation, unconsciousness, and immobility.
dose dependent
amnesia
In general, CNS and ANS are _ with volatile anesthetics
depressed
T/F Volatile anesthetics are cerebral-protective with antioxidant effects that prevent damage to cells
True
5 effects of anesthesia gases on neuological system
- ICP
- Autoregulation of CBF and cerebral reactivity to CO2
- Cerebral metabolic rate of O2 (CMRO2)
- CSF Pressure
- Neuro assessments (obviously)
The brain’s ability to autoregulate cerebral perfusion pressure depends heavily on the MAP being in the range of _ to _.
60-180
CPP = MAP - ICP
Volatile anesthetics _ the capacity of the brain to autoregulate CPP.
REDUCE
-it does this REGARDLESS of if the MAP is within the window of 60-180
When trying to compensate for increased ICP, cerebral vasodilation, and increased CBF we can _ the dose/MAC and/or hyperventilate the pt to achieve goal of PaCO2 _ - _ to prevent further vasodilation.
reduce
30-35 PaCO2
All inhaled anesthetics (and most IV anesthetics) will _ MEPs, but _ will do so the most.
decrease
Isoflurane
Almost all inhaled and IV anesthetics decrease SSEPs except _ and _ which increase them
Etomidate
Ketamine
Of the IV anesthetics, only _ increases CBF, CMRO2, ICP, SSEPs, and CPP/MAP
ketamine
Unlike the other inhaled anesthetics, _ doesn’t have a large affect on CMRO2 and ICP
N2O
Increasing the dose of anesthetics will typically cause decreased BP EXCEPT in which 4 anesthetics(usually)?
N20
Ketamine
Etomidate
Precedex
The 5 factors that cause BP to fall during anesthesia are:
1.CNS depression
2. Direct Cardiac Depression
3. Dose dependent decrease of SVR leading to vasodilation
4. Baroreceptor Depression (aortic arch, carotids)
5. Hormonal changes (decreased renin, vasopressin release)
-all anesthetics do this EXCEPT N2O
When giving epinephrine, doses should be no stronger than:
1: _ = _ mg/mL
No more than _ mL (or _ mg) in a 10 minute period.
No more than _mL (or _ mg) in an hour total.
1:100,000 ~ 0.01mg/mL
10mL (0.1mg)
30mL (0.3mg)
-volume administered can be adjusted by changing concentration of the dose
Which (main) inhaled anesthetic can cause tachycardia due to respiratory irritation and what is a first line intervention for this?
Desflurane
Fentanyl IV
The inhaled anesthetics all lower MAP and SVR EXCEPT
N2O
-can increase SVR, no effect on MAP
The inhaled anesthetics all increase HR EXCEPT
Sevoflurane
Which 2 inhaled anesthetics are known to lower CO?
Isoflurane and N2O
All inhaled anesthetics bronchodilate and cause dose dependent respiratory depression EXCEPT
N2O
Which 2 inhaled anesthetics are respiratory irritants?
Desflurane and Isoflurane
Unlike opiates, the respiratory depressant nature of inhaled anesthetics (except N2O) causes _ to decrease before _.
Vt
RR
All inhaled anesthetics (besides N2O) decrease _, which decreases renal _ _, decreasing _, which then will cause decreased _
BP
renal blood flow
GFR
UOP
Which inhaled anesthetic has the highest rate of toxic metabolites?
Sevoflurane 5-8%
-don’t give to renal pts
-lasts longer in obese pts
Which inhaled anesthetic is known to cause hepatotoxicity?
Halothane
Which inhaled anesthetics can trigger MH and therefore are contraindicated in pts at risk?
ALL EXCEPT N2O
-Succinylcholine too!
N2O oxidizes the cobalt atom on _ _, inhibiting _ _ which disrupts DNA/RNA synthesis.
Vitamin B 12
Methionine Synthetase
Which inhaled anesthetic can cause immunosuppression in at risk pts?
N2O
What are 3 absolute contraindications for giving N2O?
- Known B12 deficiency
- Toxicity from expansion of gas in space
- Increased ICP
-others include: 1st Tri pregnancy, pulm HTN, high risk PONV, risk of MI, PROLONGED CASE (>6hr)
CO2 absorbers can get dry and produce _ during a case if the machine hasn’t been used in a while
CO
In regards to CO2 absorbers, Compound A can form when “low flow _” is given usually at flow rates < _L/min
low flow Sevo
<2L/min
-newer CO2 absorbers don’t react with Sevo
Which anesthetics/OR drugs can worsen cancer/ risks?
Volatile anesthetics
Opiates
Supplemental O2
Which 3 anesthetics are helpful against cancer risks/growth?
Local Anesthetics
NSAIDs
Propofol
The only inhaled anesthetic proven as teratogenic is _ and it is contraindicated in pregnancy (not delivery) due to its risk for spontaneous abortion
N2O
Chance of miscarriage is highest within first _ days postop and inhaled anesthetics are known to make the uterus _ (although N2O is the only confirmed teratogenic drug)
7
boggy
Kids between the ages of _ _ and _ years of age can experience neurotoxicity from inhaled anesthetics and should have cases kept short if possible.
third trimester
3yo
Pediatric Emergency Delirium (ED) is a short term condition that is seen usually after _ or _ is used during a case and can be treated by small doses of other IV anesthetics (midazolam, fentanyl, ketamine, etc.)
sevoflurane
desflurane
Female CRNAs can experience higher likelihood of miscarriage or birth defects when exposed to cases involving: (3 items)
- N2O
- Xray imaging (ortho cases)
- peds cases (mask induction often)
Male CRNAs are more likely to produce children who are _.
female
T/F Inhaled anesthetics don’t pass the placental-fetal barrier.
false, they ALL do
Non-urgent surgeries should occur during the _ trimester in pregnant women.
2nd
Most IV anesthetics (EXCEPT _) pose significant neurodevelopmental risk.
precedex
GA during emergent CS has no association with learning disability but it does with _.
Autism
In addition to N2O, two main drug classes that are considered teratogenic are:
Anticonvulsants and Antipsychotics
If given close to delivery, sedatives and hypnotics can cause _ _ in the newborn.
respiratory depression
Exposure to opioids in early pregnancy can cause congenital _ _
heart defects
T/F Muscle relaxants can cross the placental barrier.
False
NAIDs are contraindicated during pregnancy and have different negative outcomes for different trimesters:
1.
2.
3.
1.spontaneous abortion
2.congenital cryptoracism
3. renal injury and constriction of ductus arteriosus
The vasopressor of choice for pregnant patients is _
Ephedrine
Ionizing radiation is considered teratogenic and can cause _ _ thru gestational weeks 8-15 and childhood _
mental retardation
leukemia :(
T/F Heparin and Abx are ok in pregnancy
true
T/F quinolone, tetracycline, and codeine are ok in pregnancy
false
Age of viability of a fetus:
24 wks
Fast recovery of anesthesia is _ proportional to the solubility of the med
inversely
T/F A longer case will cause a longer emergence
true
Which inhaled anesthetic can cause seizure on EEG?
Sevoflurane = Seizurflurane
MAC peaks at _ months old
6
Sevo
-Boiling point
-Vapor Pressure
58*C
157
Des
-boiling point
-vapor pressure
24*C
669
Iso
-boiling point
-vapor pressure
49*C
238
N2O
-boiling point
-vapor pressure
-88*C
38,770
Which inhaled anesthetic boils at room temp and is easiest to vaporize?
Desflurane
-vapor pressure is close to 760
It takes _ half lives to get rid of a drug.
4
How much of a drug is gone after 3 half lives?
87.5% is gone
12.5% is left
Common drugs in benzo class:
diazepam (vallium)
lorazepam (ativan)
midazolam (versed)
flumazenil (romazicon)
Common drug in butyrophynone class:
Droperidol (Inapsine)
Common induction drugs in miscellaneous classes:
Propofol (Diprivan)
Etomidate (Amidate)
Ketamine (Ketalar)
Dexmedetomidine (Precedex)
Common drugs in barbiturate class:
Thiopental (Petothal)
Metohexital (Brevital)
Phenobarbital (Luminal)
Pentobarbital
Secobarbital
Alpha half life is how long it takes from drug to go from _ to _ and is due to drug _
blood to tissue
distribution
Beta half life is how long drug takes after distribution to be 50% _ and is due to drug _.
eliminated
metabolism
_ of _ is a number that indicates how widely a drug is distributed in the body
Volume of Distribution (Vd)
Normal Vd for a 70kg pt is about _L or _L/kg
42L or 0.6L/kg
A smaller Vd (<0.4L/kg) means the drug is mainly contained in the _ and is _ solube
plasma
water
A larger Vd (>0.6L/kg) means the drug is mainly contained in the _ and is _ soluble
body
lipid
_ has the longest elimination half life out of the IV anesthetics at 20-50hrs.
Diazepam (Valium)
Common heavily (>90%) protein bound IV anesthetics include: (5 items)
Diazepam, Lorazepam, Midazolam, Propofol, and Dexmedetomidine
Zero Order kinetic drugs are eliminated at a certain _ per hour and examples of this would be _ and _.
amount
alcohol and dilantin
First Order kinetic drugs are eliminated from the body at a certain _ per hour.
rate
The reason pts go to sleep so fast with propofol is due to _ _ of the drug from the blood to the brain and the reason they wake up so fast is because of _ _ from the brain to vital organs, muscle, and fat.
rapid DISTRIBUTION
rapid REDISTRIBUTION
A drug’s protein binding of _% or more is considered significant
90%
Acidic drugs primarily bind to _ and basic drugs primarily bind to _ _ _ _ in the plasma.
Albumin
Alpha 2 Acid Glycoprotein
T/F When more than one heavily protein bound drug is given together they will compete for receptors and cause one of the drug’s blood level to increase.
False, they DO compete but BOTH drugs blood levels will increase
If a drug is 99% protein bound and the free fraction is 1% and the free fraction is the active drug, and it enters a more protein deficient body where only 97% of it binds to protein, the active unbound drug is _ % higher than intended.
300%
Pts at risk for protein deficiency:
Malnutrition
Severe CKD
Severe liver disease
Last Tri Pregnancy
Most IV anesthetics’ mechanism of action is __ and they _ chloride ion flow into the cell causing it to become _.
GABA-mimetic
increase
hyperpolarized
Ketamine’s mechanism of action is that it acts as a _ _ on _ receptors.
Glutamate (Excitatory) Antagonist
NMDA receptors
Dexmedetomidine’s mechanism of action is that it is an highly selective alpha 2 adrenergic receptor _ and is _ and _ the release of catecholamines and acting on the alpha 2 _.
Alpha 2 Adrenergic Receptor AGONIST
sympathoLYTIC
decreases
autoreceptor
One of the major disadvantages within scope of anesthesia with benzos are their _ being longer than other drugs
half lives
Benzos are indicated for: (list a few indications)
sleep aid
anxiety
sedation
induction and/or maintenance of anesthesia
What is the brand name for Flumazenil and what class of drugs does it reverse?
Romazicon
benzos
Shorter acting benzos used for sleep aid:
Zolpidem (Ambien)
Zaleplon (Sonata)
Eszoplicone (Lunesta)
Non-benzo sleep aid with anesthesia implications:
Dual Orexin Receptor Antagonists (DORAs) -> Almorexant (Restora)
block orexin receptors which are involved in emergence “wake up”
IV induction drugs that cause pain on injection:
Diazepam **
Lorazepam *
Etomidate **
Propofol (both formulations) **
Which IV induction benzo drug does NOT cause pain on injection?
Midazolam (Versed)
Which 3 IV induction drugs’ solutions are water soluble?
Midazolam
Ketamine
Dexmedetomidine
Which IV induction drug should be avoided in asthmatics due to its sulfite component?
Generic formulation of propofol
-Diprivan formulation should be ok despite eggs, soy, and glycerol components
Which 3 IV induction drugs are considered excitatory?
Etomidate ***
Propofol *
Ketamine **
Which IV induction drugs are classified as analgesic?
Ketamine
Dexmedetomidine
Which IV induction drugs have the quickest onset?
Etomidate <30sec
Propofol <30sec
Midazolam 30-60sec
~Ketamine 45-60sec
Which IV induction drug has the longest onset of action?
Dexmedetomidine 2-5min
Which IV induction drug have the shortest durations?
Etomidate 5-10min
Propofol 3-8min
Which IV induction drug has the longest duration?
Lorazepam (60-120min)
GABA-mimetic agents possess _ and _ mechanisms
antiseizure
neuroprotective
Retrograde amnesia:
erases previous memory
Anterograde amnesia:
erase future memory
-used during anesthesia
_ are the best drug class typically for IV induction because they cover sedation, anxiolysis, amnesia with minimal side effects.
Benzos -mainly midazolam
Order of IV admin for induction:
Propofol (most cardiac and respiratory depressive)
Less propofol
Etomidate (less cardiac and respiratory depressive)
Ketamine (give in shock, NO cardiac or respiratory depression)
The ONLY IV induction drug that is a bronchodilator and maintains reflexes (after initial apnea from injection) is _
ketamine
A pt experiencing an asthma attack is hypotensive and needs to be intubated for an emergent surgery. Which IV induction drug would be ideal?
Ketamine
Which IV induction drug inhibits BOTH autoregulation and CO2 reactivity?
Dexmedetomidine
Which inhaled anesthetic inhibits autoregulation?
N2O
Which IV induction drug is the only drug to excite the CNS?
Ketamine
In terms of the cardiovascular effect, Ketamine will raise:
MAP
HR
CO
Venous Dilation
In terms of the cardiovascular effects, Propofol will lower:
MAP
HR
CO
SVR
-it will INCREASE venous dilation
Lorazepam and midazolam have no effect on _ but they cause venous dilation which can lead to _ _.
MAP
orthostatic (postural) hypotension
Etomidate can induce _ _ in porphyria patients, leading to a porphyria attack from _ hemoglobin
ALA synthetase
excess
Porphyria attacks can be brought on by _, _, _, _, and _.
(2 are induction IV drugs)
etomidate
toradol
propofol
CCBs
amiodarone
Etomidate suppresses _ _ _, which helps body synthesize cortisol and aldosterone needed to tolerate stressors, and should especially be avoided in _ ill patients
11 beta hydroxylase
critically
Propofol Infusion Syndrome can occur over _ hrs of a propofol infusion, causing severe _ acidosis, refractory _ failure, persistent and refractory _ , _, and _ and _ disturbances
48
metabolic
heart
bradycardia
fever
renal and heptatic
Which IV induction drug is a phencyclidine derivative (LSD) and causes dissociative anesthesia?
Ketamine
Ketamine can cause _ and _ IOP.
nystagmus
increased
Ketamine _ salivation and secretions.
increases
Ketamine _ muscle tone.
increases
Ketamine should be cautiously used in pts with:
HTN, angina, CHF, increased ICP and IOP, psychological conditions, airway problems
Ketamine can cause _ and _ which can be disturbing to patients and their familes.
hallucinations and delerium
Ketamine is ideal for pts experiencing:
severe dehydration
shock
bronchospasm
severe anemia
one-lung anesthesia
On emergence, pts who received Etomidate may experience _ hangover sensation and _ risk for emesis.
mild
high
On emergence, pts who received Ketamine can experience _ and _ , and _ risk for emesis.
hallucinations and delirium
moderate/high
On emergence, pts who received Propofol can experience _ hangover effect, _, and _ risk for emesis.
mild
euphoria
low
Of the IV induction drugs _ is considered anti-emetic.
propofol
The 3 IV induction drugs most likely to cause emesis on emergence are:
Etomidate *
Opioids
Ketamine*
Which IV induction agent can cause myoclonus and hiccups after injection?
Etomidate
Which IV induction drug causes the most severe recovery restlessness and PONV?
Ketamine
Which IV induction drug has many routes of administration (ROA) making it great for use in kids?
-think Nagelhout peds dentist case example
Ketamine
-IV, IM, PO, liquid syrup mix, lollipop, etc.
Along with dexmedetomidine, what drug is a highly selective alpha 2 adrenergic receptor agonist?
catapres/ clonidine
Which IV anesthetic causes lighter sedation and easier arousal?
Dexmedetomidine
Dexmedetomidine is highly _ and highly bound to plasma proteins
lipophilic
Which IV anesthetic can be useful for postop shivering?
Dexmedetomidine
Merperidine (Demerol)
Dexmedetomidine reduces sympathetic outflow by reducing release of _
norepinephrine
Dexmedetomidine causes increased cardiac vagal activity with alpha 2 antagonism of the dorsal motor nucleus at _ doses by causing _ outflow.
lower
parasympathomimetic
Dexmedetomidine is _ compared to other IV anesthetics.
expensive
Dexmedetomidine’s cardiac side effects include _ and _.
bradycardia and hypotension
Droperidol (Butyrophenone) is a tranquilizer that blocks _ receptors to prevent emesis
dopamine
Droperidol has a black box warning for _ _
QT prolongation
T/F IV anesthetics have faster emergence than inhaled anesthetics
false
Barbiturates involve _ and _ GABA inhibitory pathways leading to loss of consciousness and respiratory and cardiac depression
cortical and brainstem
Which IV anesthetic is used for amnesia and conscious sedation?
Midazolam
Which IV anesthetic’s sympathomimetic effects completely preserve cardiac function?
Ketamine
Which IV anesthetic causes inhibition of adrenocortical synthesis?
Etomidate
Which IV anesthetic has both parasympathomimetic and sympatholytic properties that cause dose dependent decrease in HR and CO?
Dexmedetomidine
T/F flumazenil has a longer half life than the benzos it typically reverses and will be adequate even for Valium.
False
-half life is shorter than benzos typically and will sometimes need more than one dose o a continuous infusion to reverse pt again after initial dose wears off (esp. with Valium).
Which benzo is in acid form in its vial, then changes shape and transitions from pro-drug to active drug in the plasma pH?
Midazolam
Speed of recovery is inversely proportional to _
solubility (B/G)
The most expensive inhaled anesthetic is _
Sevo
Sevo is used mainly in cases with _ patients, _ patients, _ surgery, or cases < _ in duration
obese
pediatric
ambulatory
1hr
If hospital short on propofol, can give _ instead as they work interchangeably except for its ability to suppress seizures.
Methohexital
ECT cases:
-induction
-NMB
Induction: Methohexital, Propofol, Thiopental, Etomidate, Ketamine, Benzos, Sevo
NMB: Succinylcholine, Mivacurium, Atracurium, Rocuronium, Rapacurium
When using thiopental for ECT, it has the cardiac effect of increased _ and _s
bradycardia and PVCs
When using Etomidate for ECT, it causes _ seizure duration, _ recovery from post-ECT confusion and _ N/V compared to other drugs.
longer
delayed
more
When using Ketamine for ECT, it can cause _ ICP leading to less than desirable _ properties.
increased
analgesic
Drug of choice in ECT is _ because it is an ultra short barbiturate and cleared rapidly.
Methohexital
2nd drug of choice in ECT is _ because of its rapid emergence and elimination, but it can increase the risk of a missed seizure.
propofol
Haloperidol is in the butyrophenone class and if given in low doses has a high affinity for _ receptors and can produce an _ effect.
dopamine (D2)
antiemetic
Haldol, like Droperidol, has the negative cardiac effect of _ _.
QT prolongation
Which of the benzos are highly protein bound and problematic for elderly patients?
Diazepam
The inhaled anesthetic that offers the best bronchodilator properties is _
Sevoflurane
The inhaled anesthetic that lasts long and is ideal for cases with patients who will be intubated following the procedure is _
Isoflurane
MH is also called:
Neuroleptic Malignant Syndrome
Serotonin Syndrome
Symptoms of MH include:
muscle rigidity ***
EtCO2 increase (50-80)
Tachycardic
Tachypneic
High BP
Hyperkalemia
MH treatment drugs:
Methylene Blue or Dantrolene
Fluids (not LR)
K Cocktail
Albuterol
Kayexalate
hyperventilation
Don’t use flows less than _ L/min of Sevo because it causes _
2L/min
hypoxemia
3 chemicals in body used for analgesia:
Enkephalins
Endorphins
Dynorphins
3 greek named opioid receptors (ORL1 receptor)
Mu
Delta
Kappa
When opiate receptors on the _-synaptic neuron are _, it prevents the release of Substance P, inhibiting the pain signal.
PRE-synaptic
ACTIVATED
Opioid mechanism of action: once ligand or drug bind to receptor, activates the -, causing multiple effects that are primarily _. The activity of adenylyl cyclase and voltage dependent CA++ is _.
G-protein
inhibitory
depressed
3 factors about Opiate drugs that always are associated (due to the mu receptor):
Potency
Amount of Resp. Depression
Addiction Liability
Mu receptor effects:
Analgesia (supra/spinal)
EUPHORIA/sedation
physical dependence
resp. depression
miosis
constipation - major
urine rtn
bradycardia
itch
skel musc. rigidity
biliary spasm
-there’s a lot!!!
Mu receptor:
-agonist
-antagonist
Agonist: endorphins, morphine, synthetic opioids
Antagonist: Naltrexone, Naloxone, and Nalmefene
Kappa Receptor effects:
Analgesia (supra/spinal)
DYSPHORIA/sedation
low abuse potential
miosis
ANTISHIVERING
Kappa receptor:
-agonist
-antagonist
Agonist: Dynorphins
Antagonist: Naloxone, Naltrexone, Nalmefene
Delta receptor effects:
Analgesia (supra/spinal)
Physical dependence
resp. depression
constipation - minor
urine rtn
Delta
-agonist
-antagonist
Agonist: Enkephalins
Antagonist: Naloxone, Naltrexone, Nalmefene
Most opioid effects occur on the _ receptor
Mu
Which 2 opioid receptors cause physical dependence?
Mu and Delta
-Kappa has least abuse potential
What do each opioid receptor have in common?
Common effect of analgesia at the spinal and supraspinal level
Same antagonists
Which opioid receptor has anti-shivering and dysphoric effects?
Kappa receptor
Most common way to classify opioids:
chemical structure
T/F If a pt is allergic to an opioid, they will be allergic to all opioids regardless of subclass.
false, pt will be allergic to all other drugs in that class most likely
Asthma patients should avoid opioid classes that have a histamine release effect such as _ and _. The _ subclass should be safe, however.
Phenanthrenes and Demerol
Phenylperidines
Other than chemical structure, opioids have subclasses that are classified by their _.
efficacy
-full agonist, partial agonist (has a ceiling effect), antagonist, etc.
Phenanthrene Alkaloid Naturally Occurring Agonists:
Morphine
Codeine
Thebaine
Phenanthrene Alkaloid Semisynthetic Agonists:
Diacetylmorphine (Heroin)
Hydrocodone (Vicodin)
Hydromorphone (Dilaudid)
Oxycodone (Oxycontin)
Tramadol
Naltrexone
Naloxone
Nalmefene
-**most common
Phenanthrene Alkaloid Synthetic Agonists:
-morphine derivatives
-benzmorphans
Morphine derivatives:
Levorphanol
Butorphanol
Nalbuphine
Benzmorphan:
Pentazocine
What is the most common subclass of opiates used?
Phenanthrene Alkaloid Semisynthetic Agonists
Peridine Derivative Agonists (synthetic)- Phenylpiperidines:
Meperidine (Demerol)
Loperamide
Peridine Derivative Agonists (synthetic)- 4-Anilidopiperidines:
Fentanyl
Sufentanyl
Alfentanyl
Remifentanyl
Diphenylheptane (synthetic methadone derivative) Agonists:
Methadone
Subclasses of Opioids (based on chem structure):
Phenanthrenes (natural, semisynth, synthetic-morphine and benzmorphan derviatives)
Piperidine Derivatives (Phenylpiperidines and 4-Anilidopiperidines)
Diphenyheptanes (methadone derivatives)
T/F Someone allergic to fentanyl will also be allergic to Meperidine
true
T/F Someone allergic to codeine can have oxycodone because they’re in different classes
false, they’re under the same umbrella of phenanthrene alkaloids
The potency of opioids is variable due to the _ _ associated with pain
emotional response
The opiate with the highest potency ratio is _
Sufentanyl
The opiate with the weakest potency ratio is _
Codeine
Fentanyl is in which subclass of opioids?
Piperidine Derivatives- 4-Anilidoperidine
Hydromorphone is in which subclass of opioids?
Phenanthrene Alkaloids-semisynthetic
Methadone is in which subclass of opioids?
Diphenylheptanes
Naltrexone is in which subclass of opioids?
Phenanthrene Alkaloids-semisynthetic
Why could demerol and codeine be harmful to asthmatics?
Release histamines
T/F If a pt has liver disease you can expect pt to need higher doses of opioids to work and last longer.
False, their disease will make meds last longer and they will require smaller doses
Remifentanyl is metabolized by - _ enzymes via _.
non-specific esterase
hydrolysis
Remifentanyl lasts about _ minutes and must be given as an infusion with another med ready to give when pt wakes up.
5 mins
The 3 most highly protein bound opiates are:
Sufentanyl
Alfentanyl
Methadone
The opiate with the smallest volume of distribution is _.
Remifentanyl ( hardly leaves the plasma bc so water soluble)
~0.3-0.4L/kg
Which opiate has the longest elimination half life?
Methadone ~15-20hrs
Which opiate has the shortest elimination half life?
Remifentanyl 0.1-0.2hrs
Which opiate has the shortest duration?
Remifentanyl ~2-5mins
It’s better to - opiates during a case.
front-load
Acute effects of opiates:
analgesia
resp. depression
sedation
euphoria
vasodilation
bradycardia
cough suppression
miosis
N/V
skel. musc. rigidity
smooth musc. spasm
constipation
urine rtn
biliary spasm
itch
antishivering (meperidine only)
-a lot!
Chronic effects of opiates:
tolerance
physical dependence
constipation
Which subclass of opiates can cause postural hypotension/ orthostatic hypotension?
histamine-releasing opiates: Phenanthrenes and demerol!
Every time an opiate is given to a pt, their _ will increase.
CO2
-eventually pt will stop breathing
At end of case, if pt not breathing and CO2 is at or above _ mmHg, either call APCU for a vent or give _.
50mmHg
Narcan
Pt’s can’t develop a tolerance for _ and _ in opiates
miosis and constipation
Which drug class can suppress cough which helps with tolerating ETT and emergence?
opiates
Pupils constrict with opiates due to a _ or _ effect.
parasympathomimetic or vagal
The vomiting center receives input from the chemotactic trigger zone via the _ _
vagus nerve
The _ _ _ (_) is an area in postrema of brain that senses the O2 level in blood and causes N/V.
chemotactic trigger zone
CTZ
Anyone who receives a _ is at higher risk for N/V and this typically occurs _ because eventually drug has an inhibiting effect on the _ _ _
narcotic
initially
CTZ chemotactic trigger zone
Narcotics are resp. depressors because they shift the CO2 response curve to the _, meaning it takes a _ CO2 to drive up respirations
right
higher
PONV risk factos:
female
<50yo
hx PONV (#1)
high dose intra/postop opiates
surg > 1hr
laproscopic procedures`
PDNV risk factors:
female
<50 yo
hx PONV
PONV in PACU
Best prophylaxis/treatment for PONV:
multimodal antiemetic therapy
Things that stimulate CTZ which then stimulates vomit center:
Opioids (initially)
Vestibular part of CN VIII
Things that inhibit CTZ and therefore inhibit vomit center:
Benzos/Propofol
Dopamine ANTAgonists
Serotonin ANTAgonists
Histamine ANTAgonists
Acetylcholine (muscarinic) ANTAgonists
Opioids (after initial dose)
Most widely used/gold standard antiemetic:
Ondansetron (Zofran)
Preferred drug for PDNV:
Palonosetron (Axoli)
Drug classes indicated for PONV:
Glucocorticoids
5HT3 Receptor Antagonists
Neurokinin 1 Receptor Antagonists
Antihistamines
Transdermal Scopolamine(anticholinergic)
+Metoclopramide(Reglan)
Dexamethasone (and methylprednisolone) for PONV should be given _ induction and _ surgery
after
before
Dexamethasone is thought to act as a _ antagonist on the CTZ
serotonin
A diabetic pt is at risk for PONV, which antiemetic drug class should be avoided in this population? Why?
glucocorticoids
-spikes BG for 6-12 hrs following admin, not nice
What negative effect could come with using dexamethasone or methylprednisolone for PONV?
can mask infection, delay wound healing :(
Your pt with a hx of 2nd degree type 2 block and LBBB is complaining of nausea prior to a case. Which antiemetic drug class should be avoided if possible and why?
5-HT3 Receptor Antagonists like Zofran
-prolongs QT interval leading to torsades
Which antiemetic can lead to serotonin syndrome with concurrent use with zofran?
Palonosetron for PDNV
What time is zofran typically given for a case?
beginning
-works better with dexamethasone added
How does Emend work as an antiemetic?
Substance P/ neurokinin1 antagonist
-suppresses activity at nucleus of solitary tract where vagal afferents from GI system interact with inputs from area postrema to the brain that initiate vomiting
Droperidol was used for decades as an antiemetic as a _ receptor blocker in the CNS, making it awful for pts with _ disease by causing EPS. It also has a black box warning for what?
dopamine
Parkinson’s
QT prolongation
Transdermal Scopolamine blocks _ impulses from the vestibular nuclei to high centers in the CNS. Due to its longer onset, when should it be applied for PONV prophylaxis?
cholinergic
Evening prior to case
Scopolamine patches are a great antiemetic for _ due to their effect on the vestibular nuclei but come with side effect including _, _ _, _, and _ _.
motion sickness
dizziness, dry mouth, sedation, blurred vision
-sounds like a bummer on a cruise tbh
Midazolam can be used prophylactically for PONV as a _ inhibitor on the CTZ but should be given _ or _.
dopamine
pre/intraoperatively
Metoclopramide (Reglan) is a weak _ blocker but can cause _ in high doses and has a _ half life
dopamine
dyskinesia/ EPS
short (30-40 mins)
- i get why pt were pissed with this drug, Tigan works better tbh
If PONV occurs within _ hrs postop, do not give the same medication class given prophylactically, use one from another class with another admin method
6
Common 5-HT3 Antagonists used for antiemetics:
Ondansetron (Zofran)**
Granisetron (Kytril)
Palonosetron (Aloxi) **
Common Dopamine Antagonists used for antiemetics:
Droperidol (Inapsine)**
Haloperidol (Haldol)**
Metoclopramide (Reglan)
Prochlorperizine (Compazine)
Common Antihistamines used for antiemetics:
Hydroxazine (Atarax)
Promethazine (Phenergan)
Diphenhydramine (Benadryl)
Common Glucocorticoids used for antiemetics:
Dexamethasone (Decadron)
Methylprednisolone (Prednisone)
Common Anticholinergic used for antiemetics:
Scopolamine transdermal
Common Neurokinin-1 Antagonists used for antiemetics:
Aprepitant (Emend)
Rolapitant (Varubi)
Giving a narcotic too quickly or at a high dose can cause _ _ rigidity AKA _ _, which is treated with a _ _
chest wall rigidity
tight chest
muscle relaxant
-pt can’t be ventilated, too tight
Narcotics have a vagal effect in the sphincter of Oddi in the bile duct causing it to contract, bad if in a choli-angiogram case, give 4 things:
Atropine or glycopyrolate
give SL NTG
give glucagon
give naloxone
To treat epidural-morphine induced pruritis, give _
ondansetron
To prevent pruritis, you can give 3 different meds:
(follow hosp policy tho)
Droperidol
Propofol
Alizapride
_ can be given for antishivering properties and it works on the _ opioid receptors
Merperidine (Demerol)
KAPPA
Fentanyl comes in many routes of administration:
transdermal or iontophoretic transdermal
oral transmucosal (lollipops/tablets)
intranasal
transpulmonary
Tramadol is metabolized into the _ metabolite which is 6x as potent than its parent compound and is metabolized by the _ enzyme
M1
CYP3D6
Hydrocodone has varying effectiveness from genetic status of parents affecting the _ receptor binding and is metabolized by the _ enzyme
mu
CYP3D6
Oxycodone has significant _ and effectiveness depending on the metabolic genotype and is metabolized by the _ enzyme
VARYING
CYP3D6
Codeine is a _ and is metabolized into its active form, morphine and is metabolized by the _ enzyme
prodrug
CYP3D6
CYP3A4 enzyme metabolizes _, _, and _ in varying fashion depending on the enzymatic activity.
fentanyl
buprenorphine
methadone
CYP3B6 metabolizes _ and _ and women typically have higher levels of enzyme activity
propofol
methadone
Opioid antagonists (brand names too):
Naloxone (Narcan)
Naltrexone (Trexane, Vivitrol NT-ER)
Nalmefene (Revex)
Narcan titration:
use 5ml syringe,
draw up the 1ml from the 0.4mg/ml vial
draw up 3ml sterile water
now you have 4ml total with 0.1mg/ml and you can “titrate” it
Tell PACU RN if you gave narcan and that you are concerned with pt _
re-narcotizing
Naltrexone (Vivitrol NT-ER) is used to help alcoholics trying to quit, so may need to give these pts _ narcotics during a case bc drugs will have to _ for receptor sites
more
compete
What are the preferred endogenous ligands for mu receptors:
beta endorphins
met- and leu- enkephalins
What are the preferred endogenous ligands for the delta receptor?
met and leu enkephalins
What are the preferred endogenous ligands for the kappa receptor?
dynorphins
What is the preferred endogenous ligand for the ORL1 receptor?
nociceptin
Droperidol (Inapsine)
-class
-use
-extra info
dopamine blocking antiemetic
-black box warning for QT prolongation (used to be given)
Merperidine (Demerol)
-class
-use
-extra info
phenylpiperidine opiate
anti shivering, weaker than morphine,works on KAPPA receptor
