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
|
|
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
|
|
Term
|
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
|
|
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
|
|
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
|
|
Term
| Morphine causes more ___ than other opioids. |
|
Definition
|
|
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
|
|
Term
| Pscychomietic effects of opiods are from the ___ receptors. |
|
Definition
|
|
Term
|
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
|
|
Term
| In what condition is the vascular effect of opiodis useful? |
|
Definition
|
|
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
|
|
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
|
|
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
|
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
|
|
Term
| Buprenophrine, a low efficacious opioid, has __ duration and is __ to disocciate from mu receptors. Thus it is difficult to reverse respiratory depresion. |
|
Definition
|
|
Term
| ideal drug for preventing access to receptors by high efficacy compounds. Used in narcotic treatment programs. |
|
Definition
|
|
Term
| ___ is a opioid with low effiacy and is opioid of choice for cough. |
|
Definition
|
|
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
|
Definition
|
|
Term
|
Definition
- opioid antagonist
- must be injected
- not active orally |
|
|
Term
|
Definition
- opioid antagonist
- long acting
- oral route only |
|
|
Term
| prototype of opioid antagonist: |
|
Definition
|
|
Term
|
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
|
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
|
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
|
|
Term
|
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
|
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) |
|
|
