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148 Cards in this Set

  • Front
  • Back
Meperidine
Demerol
Fentanyl
Sublimaze
Sufentanil
Sufenta
Alfentanil
Alfenta
Remifentanil
Ultiva
Naloxone
Narcan
Naltrexone
Narcan
Nalmafene
Revex
Enkephalins
Leu
Met
4 groups of chemicals in the body that relieve pain
Enkephalins
Beta Endorphins
Dynorphins
Endomorphins
Precursor for enkephalins
proenkephalin A
Precursor for beta-endorphins
pro-opiomelanocortin
precursor for dynorphins
prodynorphin
precursor for endomorphin
unknown
How many amino acids are in enkephalins?
pentapeptide (5 amino acids long)
Tyr-gly-gly-phe-leu (met)
What is pro-opioimelanocortin (precursor for beta-endorphin) broken down into?
ACTH (which is further broken down to alpha MSH)
and
Beta-Lipotropin (which is further broken down to Beta Endorphin and Beta MSH)
What is prodynorphin broken down into?
alpha neoendorphin, dynorphin A, dynorphin B
Name for pain receptors.
nociceptors
What is another name for pain relievers/narcotics?
antinociceptors
What is the goal of multimodal therapy for pain relief?
-decrease the dose of a single agent
-improve nociception
-reduce side effects
-avoid sedation and respiratory depression
highest concentration of mu receptors are found where?
thalamus
How do you feel pain?
Electrical signal travels down the neuron must signal for the release of the neurotransmitter that produces pain. Neurotransmitter travels across the synapse between neurons and attaches to the appropriate receptor. A pain signal is then sent up the spinalthalamic tract.
What spinal tract sends pain signals up the spinal cord to the brain?
spinothalamic tract
How is pain block by endorphins, etc.?
Opiate receptors on the presynaptic neuron are activated, a conformational change takes place that prevents the release of the pain neurotransmitter.
Opiates work as...
a presynaptic agonist on the pain neuron by stimulating the opiate receptor
What is the difference between mu1 and mu2 receptors in humans?
there is none
The amount of analgesic a narcotic produces is equal to ...
the amount of respiratory depression and the amount of addiction.
The 3 primary subtypes of opiate receptors.
mu
kappa
delta
What is the main receptor for producing anything to do with a narcotic?
mu receptors
what ligands work at the mu receptors?
endomorphin 1 & 2
met-enkephalin
dynorphin A and B
What ligands work on the kappa receptors?
dynorphin A and B
Beta endorphin
What ligands work on the delta receptors?
Leu and met-enkephalins
beta endorphin
What receptors does Narcan reverse?
all of the opiate receptors
Partial agonists will give you 100% efficacy for analgesia but not respiratory depression. T/F
False. No matter how high the dose partial agonist will never reach 100% efficacy.
Why would you give a partial agonist knowing that it won't reach 100% efficacy?
to decrease the amount of respiratory depression experienced
What are the natural occurring phenanthrene alkaloids?
Morphine
Codeine
Thebaine
What are the semi synthetic phenanthrene alkaloids?
Heroin
Vicoden
Dilaudid
Oxycontin
Oxymorphone
What are the synthetic opioids?
Levorphanol
What are the phenylpiperidine derivatives?
Meperidine
Fentanyl
Sufentanil
Alfentanil
Remifentanil
What are the propionilide derivatives?
Methadone
Propoxyphene (Darvon)
If someone is truly allergic to Dilaudid, can you give them Morphine?
No; because they fall within the same class of phenanthrene alkaloids
If someone tells you they are allergic to morphine because they experienced severe nausea and vomiting the last time they were given a dose, is this a correct statement?
No; they experienced the normal effects of opioid drugs
There is a cross allergy _____ chemical classes but not _____ chemical classes.
within; between
What are all opioids compared to when determining their potency?
Morphine
Opioids are have a high degree of anesthetic potency. T/F
False. They do not provide any anesthesia only analgesia
Analgesia goes hand in hand with what other effects when discussing opioids?
analgesia, respiratory depression, and addiction
Where are opiates metabolized?
in the liver by the cytochrome enzymes in the endoplasmic reticulum
What happens to opiate levels when someone is enzyme inhibited?
will have prolonged response to the opiates because they are not being metabolized as quickly
What happens to opiate levels when someone is enzyme induced?
levels drop very quickly because of excessive metabolism. Patient requires higher doses of opiate.
What happens to opiate levels in a liver disease patient?
unable to metabolize the drug so the drug effect stays around longer
What is the only opiate that is not metabolized in the liver?
Remifentenil
Where is Remifentenil metabolized? by what?
Remifentenil is hydrolized in the plasma by nonestherase dependent enzymes
What happens when Demerol is metabolized?
It is metabolized to active/toxic metabolite normeperidine
What is the problem with the metabolite normeperidine?
It is toxic with prolonged administration. Increased levels can cause seizures.
What demographic of patients are at higher risk for toxic levels of metabolite when given demerol?
Elderly and renal patients
What is the chemical make up of Remifentanil that allows it to be easily hydrolized in the plasma?
has an esther group
Remifentenil is a long acting opioid. T/F
False. It is very short acting. Must be given by continuous infusion with a plan for analgesia to be given as soon as the drip is discontinued.
What procedure takes the most analgesia to block the stress response?
intubation
What cardiac effects are produced by opiates?
-slight bradycardia
-minimal vasodilation w/ phenanthrene drugs
-hypotension will be seen if pt is dehydrated
What cardiac effect is noted with Demerol?
tachycardia
What are the emetic drugs that we have discussed thus far?
opiates
Etomidate
Ketamine
Nitrous Oxide
What are the anti emetic drugs?
Propofol
Droperidol
What is the only affect of narcotics that is not diminished with tolerance?
miosis
What produces the miotic effects of narcotics?
Constriction of the pupil is caused by an exictatory action on the parasympathetic nerve innervating the pupil. Opioids abolish the cortical inhibition of the Edinger-Westphal nucleus
Acute effects of Opioids
analgesia
Ventilatory depression
Sedation
Euphoria
Vasodilation
Bradycardia
Cough Suppression
Miosis
Nausea and Vomiting
Skeletal muscle ridgidity
Smooth muscle spasm
Constipation
Urinary retention
Biliary Spasm
pruritus
Antishivering (meperidine)
Where is the CTZ located?
the area postrema of the brain stem
The CTZ contains opiate receptors as well as what other neurotransmitters?
dopamine, serotonin, histamine, and muscarinic acetylcholine
Opiates stimulate ____ but inhibit _____.
CTZ; vomiting center
The frequency of nausea and vomiting goes ____ after several days of taking opiates.
down; this is due to the inhibition of the vomiting center
What can cause vomiting if released into the CTZ?
histamine; antihistamines can have an antiemetic effect
Where does the vomiting center receive its input from?
the CTZ and peripheral sites via the vagus nerve
Anesthetic Risk factors for PONV
Volatile agents
Nitrous oxide
Opioids
High doses of neostigmine
Ketamine
Etomidate
Patient Risk factors for PONV
Female gender
History of PONV or motion sickness
Pain
High levels of anxiety
Surgical Risk factors for PONV
Long surgical procedures
Certain types of surgery (ie. intra abdominal, major gynecologic, laparoscopic, breast, ears/nose/throat)
What is the CTZ?
Chemoreceptor Trigger Zone
area in one of the ventricles where there is no BBB. It has direct access to the chemicals in the blood. There is an immediate response to vomiting.
What effect do anticholinergic drugs have on the CTZ?
antiemetic effects
What area of the brain is responsible for chronic nausea?
vomiting center
What class of drugs causes the most nausea and vomiting?
opiates
Frequency of nausea and vomiting (increases/decreases) the longer the duration of treatment.
decreases
Nausea and vomiting is worse in patients that are...
ambulatory
Therapy that involves giving more than one drug that acts on different receptors for the same thing.
multimodal
A single dose of what drug can be given for PONV prophylaxis?
dexamethasone
What are the risk factors used for the scale to determine the managment of PONV?
female gender
nonsmoker
history of PONV
postoperative opioids
How do narcotics depress ventilation?
shifts the CO2 response curve to the right (depressing the respiratory center sensitivity to CO2-require a higher CO2 to get the same amt of respirations as a nonanesthetized patient)
What does a PCO2 shift to the right mean?
requires a higher CO2 for increased RR
What combination of circumstances cause chest wall ridgidity?
-dose of narcotic
-speed of administration
-use of nitrous oxide at the same time
-use of narcotics in older patients
-absence of muscle relaxants
What two opiates cause the greatest incidence of rigidity?
alfentanil and remifentanil
When does ridgidity occur?
can be immediately after dose or it can occur several hours after the last dose of narcotics has been given
How do you treat chest wall ridgidity?
succinylcholine or nondepolarizing muscle relaxant
What is primarily responsible for difficulty ventilating a patient that has been given opiates?
vocal chord closure
What is primarily responsible for delayed or postoperative muscle ridgidity?
second peak in plasma opioid concentration after redistribution
What is the pathway that causes miosis with opiates?
abolishing the cortical inhibition of the Edinger Westphal nucleus
Patients can have an allergic reaction to opiates that causes pruritis. T/F
False-pruritis is a normal effect of the medication not an allergic reaction
What opiate can be given to stop post operative shivering?
Demerol
mediated through kappa receptors
Use of what drugs can prevent increases in intraocular pressure during induction of anesthesia?
fentanyl, sufentanil, and alfentanil
What receptors cause constriction of the pupil?
mu and kappa receptors
What receptor mediates itching?
mu receptors
What drugs will reduce pruritis related to opioid use?
naloxone and zofran
What happens in the biliary tree with opiate administration?
they cause constriction of the sphincter in the biliary tree via the vagus nerve
-more potent the narcotic the more pressure produced in the biliary tree
What drugs can reverse the pressure in the biliary tree?
1. atropine and glycopyrrolate
(counteracts the vagal effect)
2. nitrolycerine
(NTG is smooth muscle relaxer)
3. glucagon
(also smooth muscle relaxer)
4. naloxone
(reverse narcotic)
What drug is five times more potent than fentanyl?
Sufentanil
What drug is ten times less potent than fentanyl?
Alfentanil
What is the duration of action for Narcan?
30-60 min
What is the name of the opiate antagonist that is 100% soluble at all times in the body?
Alvimopan (Entereg)
Does alvimopan pass the BBB?
no it is not lipid soluble-100% water soluble
What does Alvimopan block?
the GI effects normally caused by opiates but still gives analgesic effects
What is front loading?
giving a bolus dose (highest dose) at the beginning of the case so that the blood level of drug drops by the end of the case to reduce the incidence of respiratory depression
Opioid will (increase/decrease) the MAC of the gas anesthetic.
decrease
What receptors are the classical pharmacologic effects of morphine mediated by?
mu receptors
What drug is contraindicated with MAO inhibitors?
demerol
What is the most potent opiate in the world?
sufentanil
What class of drugs cause amnesia?
benzodiazepines
Is a decrease in ventilatory rate a sensitive indicator of opioid effect?
No a patients drive to breathe may be abnormal despite an apparently normal ventilatory rate and state of consciousness
Does sleep affect the ventilatory response?
yes-sleep further depresses the response to CO2 and potentiates the ventilatory depression caused by opioids
Which opiate produces the most respiratory depression?
They all produce equivalent amounts of ventilatory depression in equivalent doses
How do opiods suppress cough?
by depressing cough centers in the medulla
What is a pathognomonic sign of opioid overdose?
pinpoint pupils
Why is it difficult to reverse respiratory depression without reversing analgesia?
because the same receptor is responsible for both-reverse one you reverse the other
What is stimulated in ambulatory patients that makes them more likely to experience nausea and vomiting than nonambulatory patients?
stimulation of the vestibular apparatus
Hypertonus of the skeletal muscle is most commonly experienced with which drugs?
fentanyl, alfentanil, sufentanil, and remifentanyl
What potent opioids do not release histamine?
fentanyl, alfentanil, sufentanil, and remifentanyl
What effects do opioids have on the GI system?
delay gastric emptying and increase antral tone
What effects do opioids have on the gall bladder?
contraction of smooth muscle in the gall bladder and spasm of the sphincter of Oddi which can precipitate biliary colic
Neonatal withdrawal can occur ____ after delivery.
shortly
When tolerance to an opioid occurs, there is simultaneous development of cross tolerance to all other opioid agonists. T/F
True
What effects caused by opioids do people develop tolerance to most rapidly?
analgesia, ventilatory depression, euphoria
What drug has a low lipid solubility that gives it some of morphine's characteristics as a selective spinal analgesic?
hydromorphone
This drug is a long lasting synthetic mu opioid approximately equipotent with morphine.
Methadone
What accounts for the rapid onset and short duration of fentanyl?
high lipid solubility
Do narcotics increase ICP?
No-the respiratory depression can cause an increase in CO2 that causes vasodilation in the brain increasing blood flow and increasing ICP
Opioids produce a dose related _____ in the need for volatile anesthetics.
decrease
Naloxone acts as a ________ at ___ opioid receptors.
competitive antagonist; all
What two drugs cause the most biliary spasm?
morphine and fentanyl
Are all NSAIDS antiinflammatory?
no acetaminophen is not
All NSAIDS are antipyretic and analgesic. T/F
True
What is the primary mechanism by which NSAIDS exert their analgesic effect?
inhibition of cyclooxygenase and synthesis of prostaglandins
NSAIDS act only as peripheral analgesic agents. T/F
False. They also have analgesic effects through inhibition of spinal COX
What are the functions of the COX 1 enzymes?
they participate in platelet aggregation, hemostatsis, and gastric mucosal protection
What are the functions of the COX 2 enzymes?
they participate in pain, inflammation, and fever
Why is perioperative use of NSAIDS associated with a higher incidence of gastrointestinal bleeding?
inhibition of COX 1 inhibitors that are necessary for the synthesis of cytoprotective gastric mucosal prostaglandins
What major affect can NSAIDS have after surgery?
NSAIDS affect bone osteogenesis during bone repair
What population of patients should you use caution with when giving Toradol?
patients with impaired renal function or history of kidney disease-it is a potent inhibitor of prostaglandin synthesis
How is Toradol and its metabolites eliminated from the body?
primarily by the kidneys
When is Toradol contraindicated?
in patients with serum creatinine concentrations indicating advanced renal impairment
How do you measure the effect of ASA on patients?
check the bleeding time
What is the principal use of ASA?
platelet inhibition-irreversibly inhibits platelet function for 8-10 days
What is the max dose of Tylenol per day?
4 gm
What drug will Tylenol increase the effects of ?
Warfarin-increasing the aticoagulant effect