Shared Flashcard Set

Details

Pharmacology Exam 2 Opioids
Pharm Exam 2: Opioids
94
Anatomy
Graduate
02/17/2011

Additional Anatomy Flashcards

 


 

Cards

Term
Analgesia is the ___ of pain perception without the loss of ____.
Definition
- attenuation of pain perception
- without the loss of consciousness
Term
Pain has a ___ and a ___ component.
Definition
- sensory
- reactive
Term
Sensory component of pain means that pain is perceived as a result of ___ ___ of pain receptors and/or by the ___ of __ __ from the periphery.
Definition
- direct stimulation
- pattern of neural input
Term
Reactive component means that the ___ of the pain is dramatically altered by the level of __ and the ___ __ related to the original insult.
Definition
- intensity
- anxiety
- stress response
Term
methods of pain treatment:
Definition
Pharmacologic interventions
Non-pharmacologic interventions
Physical modalities
Psychosocial interventions
Spiritual care
Disruption of nerve pathways
Neuromodulation
Neurodestructive
Term
Pharmacotherapy is the cornerstone of treatment for the management of pain

The majority of pain can be controlled with simple, non-invasive therapeutic modalities
Definition
Term
Pain intensity
Greater severity can be relieved by combining therapies.
Adjuvants may be useful.
More severe pain may require the addition of an opioid preparation.
Definition
Term
Pain intensity
Greater severity can be relieved by combining therapies.
Adjuvants may be useful.
More severe pain may require the addition of an opioid preparation.
Definition
Term
opiods are very effective with ___ ___ pain like a __ __. But not very effective with __ ___ pains like a ___.
Definition
- effective with dull ongoing pains like a tooth ache
- not with sharp stabbing pains like a knife
Term
opioids good for chronic back pain, not sharp back pain that occurs with movements.
Definition
Term
Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Widely used drugs for treatment of mild to moderate pain.
NSAIDs inhibit the enzyme cyclooxygenase (COX) thus decreasing levels of mediators that cause pain, and inflammation (prostaglandin).
Definition
Term
A TCA used in chronic pain management is ____. It blocks the reputake of ___ and ___. It is ___ ___ __ and normalizes ___ ___.
Definition
- Amitriptyline
- 5-HT and NE
- non-habit forming
- normalizes sleep pattern
Term
Amitriptyline, a TCA, is ____ in doses considered non-therapeutic for depression.
Definition
- analgesic
Term
Amitriptyline:
Definition
- TCA that blocks reuptake of 5-HT and NE
- baseline drug for chronic pain
Term
what do you need to be aware of with Amatriptyline?
Definition
- HIGHLY ANTI-CHOLINERGIC /ANTI-MUSCARINIC
Term
Doxepin is another ___ used for __ ___. It is also highly _____.
Definition
- TCA
- chronic pain
- anti-cholinergic
Term
The term "narcotic" is a bit archaic. It is more legal than medical. It refers to substances producing ____ associated with ___, usually associated with derivatives of ___.
Definition
- stupor
- analgesia
- opium
Term
Opiates are ___ __ and ___ from the __ ___. Examples include ___, ___, ___, and ___.
Definition
- natural products
- derivatives
- opium poppy
- opium, morphine, heroin, codeine
Term
Opiods are a class of compounds that bind to __ ___. This includes __, ____, partial agonists, and mixed agonists/antagonists. This is the preferred term.
Definition
- opioid receptors
- agonists, antagonists
Term
Drugs have varying specificity and efficacy at various opioid receptor subtypes. These subtypes are:
Definition
- mu opioid receptors
- kappa opioid receptors
- delta opioid receptors
Term
The ___ ___ ___ are the most important receptor for most drugs. Sometimes ___ is also targeted.
Definition
- mu opioid receptors
- kappa
Term
Some endogenous ligands act as opioid antagonists. For example, ___ ___ is attributed to be the euporic agent in a runner's high.
Definition
- beta endorphin
Term
Even though we know there are endogenous ligands that act as opioid agonists, research has failed to produce meaningful drugs from these peptides. This is a case where we know a great deal about these peptides, but it has not translated into clinical impact. (Boards, particularly USMLE, stress knowledge of this material.)
Definition
Term
3 main endogenous ligands and their receptors and effect:
Definition
- Endorphins: mu activation> euphoria

- Enkephalins (methionine and leucine containing peptides): mu activation> euphoria

- Dynorphins: kappa activation> dyshporia, shown to cause hyperalgesia
Term
Mu receptors are responsible for most of the classical effects described for opioid use, including: ____, ___, ___, ___ ___, ___ ___, and ___ ___ __ .
Definition
- analgesia
- euphoria
- miosis
- respiratory depression
- physiological dependence
- reduced GI motility (constipation)
Term
With opioids tremendous ___develops to the ____- faster than to respiratory depression or analgesia.
Definition
- tolerance
- euphoria
Term
Opiod dependence is its own category. It is not the same as ___ ___ dependence.
Definition
NOT same as sedative hypnotic dependence
Term
2 aspects of opiods have no tolerance. What are they?
Definition
- miosis (pin-point pupil)
- constipation
Term
Kappa receptors have less involvement with ___ ___ and ___ ___. These receptors are important for the effects of ___ ___ and some of the ___ ___ ___ opioids including:
Definition
- abuse potential
- physical dependence
- non-selective and mixed agonist/antagonist drugs
- dysphoria
- pscychomimetic responses (disoriented or depersonalized feelings)
- analgesia
- sedation
- vasodiation
- increased urinary output
Term
The Kappa receptor causes less ___ and ___ ___ than the mu receptor.
Definition
- less miosis
- less respiratory distress
Term
Effects of the kappa receptor:
Definition
- dysphoria
- analgesia
- pscychomimetic responses (depersonalization and disorientation)
- vasodilation
- increased urinary output
Term
Opioid therapeutic uses and side-effects are confined to actions in the ___, ___, __, and ____.
Definition
- CNS
- vasculature
- GI
- kidney
Term
Opioids in the kidney are ____ ___.
Definition
kappa agonists
Term
Morphine causes more ___ than other opioids.
Definition
vasodilation
Term
Analgesia is produced by the __ and __ receptors. They diminish the ___ and ___ component of pain, though the ___ component is much more diminished than the ___ component.
Definition
- mu and kappa
- reactive and sensory
- reactive is more diminished than sensory

"It doesn't hurt as much"/"It still hurts, but it doesn't bother me"
Term
euphoria is associated with __ receptors, while dysphoria is associated with ___ receptors.
Definition
- mu
- kappa
Term
Pscychomietic effects of opiods are from the ___ receptors.
Definition
kappa
Term
CNS opioid effects:
Definition
- analgesia
- euphoria
- dysphoria
- psychomimetic effects
- sedation
- respiratory depression
- cough suppression
- miosis
- nausea/vomiting
Term
The cause of death with opioid overdose is __ ___ b/c the brain stem has ___ response to ___.
Definition
- respiratory depression
- decreased response to CO2
Term
Not really clear on this but:

If pt has overdosed on opioids do NOT give them oxygen b/c decreases CO2 and already they aren't sensitve enough to CO2.

Also don't give brain trauma patient opioids b/c could lead to swelling
Definition
Term
Opioids cause miosis b/c of the increased ___ stimulation to the ___ ___ nucleus. Tolerance does not develop to this.
Definition
- parasympathetic
- Edinger-Westphal
Term
Opioids cause nausea and vomiting b/c they stimulate the ___ ___ ___ in the ___.
Definition
- chemoreceptor trigger zone
- brainstem
Term
Opioids causing vasodilation, especially ___, is mediated by __ __ __ ___ receptors.
Definition
- morphine
- non-mu
-non-kappa
Term
vascular effect of opiods:
Definition
vasodiation
Term
In what condition is the vascular effect of opiodis useful?
Definition
- Pulmonary edema
Term
Opioids are usuefl in pulmonary edema b/c morphine-induced ___shifts fluid from the central to peripheral compartment. Also Opioids make the brainstem less responsive to ___, which reduces the ___ ___. Thus the patients are more relaxed so fluid moves off lungs easier.
Definition
- vasodilation
- pCO2
- reduces the sympathetic tone
Term
Opiods cause ___ b/c they decrease ___ due to increased ___. The tone is sometimes described as a ___ b/c it is not coordinated. Little or no tolerance develops.
Definition
- constipation
- decrease motility
- increased tone
- spasm
Term
Opioids are usually classified as having high, intermediate or low efficacy
Their spectrum of therapeutic use is essentially identical to their abuse potential. The greater the ___ of the opioid, the greater the ___ ___.
Definition
- efficacy
- abuse potential
Term
High efficacy mu opioids:

(used in patient, unless terminal cancer)
Definition
- Morphine
- Meperidine
- Methadone
- Fentanyl
- Heroin (schedule I)
Term
With opioids the faster the drug comes on to the receptor, the greater the effect.
Definition
Term
the prototypic opioid analgesic:
Definition
Morphine
Term
Morphine binds to ___ opioid receptor subtypes. It has the highest affinity for the __ receptor. It has a low oral:parenteral potency ratio, meaning that it is ___ and ___ absorbed b/c it is ___ ___. Thus, it is less potent by the __ __. It has ___ efficacy for analgesia.
Definition
- all
- mu
- slowly and incompletely absorbed
- highly polar
- less potent by oral route
- high efficacy for analgesia
Term
Meperidine is another opioid with ___ ___. It has a ___ elmination half life, and has a metabolite that can cause ___. It causes less ___ ___ and thus is good for ___.
Definition
- high efficacy (mu)
- shorter
- seizures
- less respiratory depression
- labor
Term
Methadone is a ___ ___ opoiod with a very ___ half life of __ hours. It also blocks ___ receptors and ___ ___ pumps ( a mechanism of typical antidepressants). For these reasons it can be more efficious in pain that is difficult to treat. It is also used to treat ___ ____.
Definition
- highly efficacious (mu)
- long
- 24
- NMDA
- monamine reputake pumps
- opioid abuse
Term
__ is actively oral, which is rare for opioids.
Definition
Methadone
Term
Fentanyl and Sufentanil are ___ ___ opiods. These are the most ___ ___ and ___ opiods. Very low doses are required.
Definition
- highly efficacious (mu)
- most lipid soluble
- most potent
Term
Uses of Fentanyl and Sufentanil:
Definition
- transdermal patch for vomiting patients
- cardiovascular surgery to obtain analgesia with minimal cardiodepressant effects
Term
what you need to be awrae of with fentanil and sufantenil:
Definition
- highly lipid soluble opioids such as these given i.v. can cause trunchal rigidity (bad for surgery)
Term
What are the high efficacy kappa opioids:
Definition
- Butorphanol
- Nalbuphine
Term
Butorphanol is a relatively pure ___ ___. It is often used __ ___ for pain control with much less risk of __ ___. It produces ___.
Definition
- kappa agonist
- post-surgery
- less risk of respiratory depression
- dysphoria
Term
Nalbuphine is a highly efficacious ___ ___ and __ ___. This is used __ ___ when patients are having ___ ___. This drug removes the __ ___ effects of __ ___given prior to or during surgery, while maintaining ____. Dysphoria is a problem.
Definition
- kappa agonist
- mu ANTagonist
- post surgery
- respiratory depression
- removes the mu agonist
- maintaining analgesia
Term
Opioids with intermediate efficacy:
Definition
- Hydrocodone- abuse potential
- Oxycodone
- Pentazocine- acts at kappa, dysphoria
Term
As a general rule, addition of an __ to an ___ gives much better ___ than the same dose of either agent alone. This combination has been used with good success for all ___ opioids.
Definition
- NSAIDs
- opioid
- analgesia
- intermediate
Term
Hydrocodone efficacy is enhanced by adding ___ , __, __ , or ___.
Definition
- acetaminophine
- aspirin
- Vicodin
- Lortab

Note: although hydrocodone is classified as an intermediate efficacy agent, experimental literature suggests its efficacy is nearly that of morphine.
Term
Pentazocine:
Definition
Moderate kappa agonist with either very weak partial agonist (or pure antagonist) actions at mu receptors.
Developed as oral analgesic with limited abuse potential. In general, it hasn’t worked out that way (T’s and Blues).
Term
Opioids with low efficacy:
Definition
Buprenorphine (Buprenex)
Codeine
Term
Buprenorphine has high ___ but not efficacy.
Definition
potency
Term
Buprenophrine, a low efficacious opioid, has __ duration and is __ to disocciate from mu receptors. Thus it is difficult to reverse respiratory depresion.
Definition
- long
- slow
Term
ideal drug for preventing access to receptors by high efficacy compounds. Used in narcotic treatment programs.
Definition
Buprenorphine
Term
___ is a opioid with low effiacy and is opioid of choice for cough.
Definition
Codeine
Term
Codeine: Ceiling on analgesia effect is not limited by efficacy per se. Rather, at high doses codeine is an agonist at non-mu receptors (sigma ??) that mediate psychotomimetic effects that are unpleasant. This may limit the abuse potential of this agent
Definition
Term
Codeine has interesting biotransformation. The analgesic effects of the drug come from __ conversion of drug to ___ by ___ via the ___ cytochrome.
Definition
- slow
- morphine
- demethylation
- CYP2d6 cytochrome
Term
CYP2D6 is repsonsible for ___ of codeine to ___, and responsible for ___ __ metabolism. This is missing in 5-10% of caucasians, these people get unexpectedly high levels of codeine with no efficacy and increased likelhood of sympathhomimetic effects.
Definition
- demethylation
- morphine
- beta blocker
Term
codeine cough suppressant effects:
Definition
As with most opioids, suppression of cough appears to be by action at mu receptors. Note: all opioids are efficacious cough suppressants. The ceiling on abuse liability, or perhaps historical use, has resulted in codeine usually selected as the first agent of the opioid drugs that is prescribed if OTC meds are ineffective.
Term
Opioid Antagonists:
Definition
- Naloxone
- Naltrexone
Term
Nalaxone:
Definition
- opioid antagonist
- must be injected
- not active orally
Term
Naltrexone:
Definition
- opioid antagonist
- long acting
- oral route only
Term
prototype of opioid antagonist:
Definition
Naloxone
Term
Naloxone:
Definition
Naloxone is the prototype.
useful in opioid overdose
reverses the action or blocks the action of agonists
precipitates withdrawal syndrome in chronic users of opioids
useful in treating some drug-free addicts
Term
opioid overdose triad:
Definition
- pin-point pupils
- low respirations
- coma
Term
if treat person who is not dependent on opiods but it is ER for overdose and give them Naloxone, what happens?
Definition
- save their life
- pushes opioids off mu receptors
- respirations come back up
- recover consciousness
Term
what happens if you give pt who is dependent on opioids and has opioid overdosed naloxone?
Definition
- go into withdrawal
- angry patient
- respirations back up
- diarrhea everywhere
Term
Opioid abuse:
Definition
Euphoria
Tolerance- becomes issue at 2-3 weeks
Occurs even with the lowest therapeutic doses and increases as dose and duration of treatment increase
Dependence/Withdrawal
Overdose
Maintenance Treatment
Term
Is withdrawal from opioids life threatening?
Definition
NO
Term
Opioid tolerance:
Definition
Tolerance, with cross-tolerance, can develop to all opioid agonists
rate of development varies among agents but generally develops faster with more potent drugs and/or higher doses
starts with first dose but doesn’t become clinically relevant for 2-3 weeks (@ normal therapeutic doses)
there is specificity of tolerance development
tolerance can be profound (as great as 35-fold)
Term
Opioid dependence:
Definition
accompanies tolerance development
may include both physical and psychological dependence
withdrawal syndrome is seen upon cessation of drug use or upon treatment with opioid antagonists or mixed agonist/antagonists (precipitated withdrawal).
Term
Opioid withdrawal symptoms:
Definition
- diarrhea
- sweating
- dilated pupils
- sympathetics are activated
Term
primary opioid overdose symptoms:
Definition
Primary (triad)
lethargy or coma
depressed respiration
pinpoint pupils (normoxic)
Term
secondary opioid overdose symptoms:
Definition
hypotension
hypothermia with cold or clammy skin (goose flesh)
pulmonary edema
convulsions (primarily in children)
hypoxia with dilated pupils right before death
Term
opioid overdose treatment:
Definition
administer opioid antagonist (naloxone is drug of choice)
support of respiration and other vital functions
identify most likely drug
if determined that other drugs were also ingested, treat for the overdose of these drugs accordingly
Term
notes on opioid use with pulmonary edema:
Definition
Relief from dyspnea associated with left
ventricular failure is due to:
reduced perception of shortness of breath
anxiolytic effects (this effect is noted in many texts, but the evidence for direct anti-anxiety effects of opioids is nearly non-existent. By reducing the perception of shortness of breath, the anxiety accompanying that perception is reduced. This is a very different phenomenon than anti-anxiety effects per se.)
reduction in cardiac preload and afterload
Term
Dextromethorphan is a non-opioid availabe OTC that enhances cough suppression of opioids. but do not give this to kids.
Definition
Term
relief of cough with codeine needs lower dose than if it was for analgesia.
Definition
Term
opioids can be used to treat diarrhea. Don't need as high of dose to treat diarrhea as you would for analgesia. Use ones that aren't well absorbed to decrease liability.
Definition
loperamide (Imodium)
diphenoxylate (+ atropine) (Lomotril)
difenoxin (+ atropine) (Motofen)
Supporting users have an ad free experience!