Pharmacology Exam Opioids Flashcards

Terms Definitions
meperidine, fentanyl
phenylpiperidines
Opioid Antagonists:
- Naloxone- Naltrexone
the prototypic opioid analgesic:
Morphine
Morphine, hydromorphone, oxymorphone, heroin
phenanthrenes
Opioids with low efficacy:
Buprenorphine (Buprenex)Codeine
methods of pain treatment:
Pharmacologic interventionsNon-pharmacologic interventionsPhysical modalitiesPsychosocial interventionsSpiritual careDisruption of nerve pathwaysNeuromodulationNeurodestructive
Which opioid treats pulmonary edema?
morphine
What is heroin metabolized to?
morphine
Is withdrawal from opioids life threatening?
NO
Pentazocine:
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).
Pscychomietic effects of opiods are from the ___ receptors.
kappa
Pain intensityGreater severity can be relieved by combining therapies.Adjuvants may be useful.More severe pain may require the addition of an opioid preparation.
Pharmacotherapy is the cornerstone of treatment for the management of painThe majority of pain can be controlled with simple, non-invasive therapeutic modalities
How is morphine given?
orally or IV
What potency does hydromorphone have with respect to morphine?
higher
opioids good for chronic back pain, not sharp back pain that occurs with movements.
opioid overdose treatment:
administer opioid antagonist (naloxone is drug of choice)support of respiration and other vital functionsidentify most likely drugif determined that other drugs were also ingested, treat for the overdose of these drugs accordingly
CNS opioid effects:
- analgesia- euphoria- dysphoria- psychomimetic effects- sedation- respiratory depression- cough suppression- miosis- nausea/vomiting
ideal drug for preventing access to receptors by high efficacy compounds. Used in narcotic treatment programs.
Buprenorphine
Nalaxone:
- opioid antagonist- must be injected- not active orally
What is the only oral mixed agonist-antagonist opioid?
pentazocine
Name two analogs of codeine.
oxycodone and hydrocodone
Opioids with intermediate efficacy:
- Hydrocodone- abuse potential- Oxycodone- Pentazocine- acts at kappa, dysphoria
Opioid withdrawal symptoms:
- diarrhea- sweating- dilated pupils- sympathetics are activated
Opioids in the kidney are ____ ___.
kappa agonists
How is naloxone administered? How is it metabolized?
IV, liver
If meperidine is given IV it can cause what dangerous side effect?
tachycardia
Buprenorphine is a partial agonist at which receptor? It is a more potent analgesic than which opioid?
mu; morphine
Opioids cause miosis b/c of the increased ___ stimulation to the ___ ___ nucleus. Tolerance does not develop to this.
- parasympathetic- Edinger-Westphal
In what condition is the vascular effect of opiodis useful?
- Pulmonary edema
euphoria is associated with __ receptors, while dysphoria is associated with ___ receptors.
- mu - kappa
Amitriptyline, a TCA, is ____ in doses considered non-therapeutic for depression.
- analgesic
Some endogenous ligands act as opioid antagonists. For example, ___ ___ is attributed to be the euporic agent in a runner's high.
- beta endorphin
__ is actively oral, which is rare for opioids.
Methadone
What is methadone for?
sever chronic pain and opioid addiction
Pain has a ___ and a ___ component.
- sensory- reactive
Opioid therapeutic uses and side-effects are confined to actions in the ___, ___, __, and ____.
- CNS- vasculature- GI - kidney
Hydrocodone efficacy is enhanced by adding ___ , __, __ , or ___.
- acetaminophine- aspirin- Vicodin- LortabNote: although hydrocodone is classified as an intermediate efficacy agent, experimental literature suggests its efficacy is nearly that of morphine.
How is naltrexone administered? What makes it different from naloxone? What about nalmefene?
orally, longer action; longer half-life
What are the effects of delta receptor agonism?
spinal and supraspinal analgesia
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.
loperamide (Imodium)diphenoxylate (+ atropine) (Lomotril)difenoxin (+ atropine) (Motofen)
Mu receptors are responsible for most of the classical effects described for opioid use, including: ____, ___, ___, ___ ___, ___ ___, and ___ ___ __ .
- analgesia- euphoria- miosis- respiratory depression- physiological dependence- reduced GI motility (constipation)
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 ___.
- stupor- analgesia- opium
High efficacy mu opioids: (used in patient, unless terminal cancer)
- Morphine- Meperidine- Methadone- Fentanyl- Heroin (schedule I)
What are the effects of kappa receptor agonism?
spinal analgesia; sedation, some dysphoric and psychotomimetic effects
What are the effects of mu receptor agonism?
supraspinal analgesia; spinal analgesia, respiratory depression, euphoria, physical dependence
What are the main side effects of opioids?
respiratory depression, constipation, N/V, dysphoria, hypotension, urinary retention, increase in ICP, pruritus
Drugs have varying specificity and efficacy at various opioid receptor subtypes. These subtypes are:
- mu opioid receptors- kappa opioid receptors- delta opioid receptors
Butorphanol is a relatively pure ___ ___. It is often used __ ___ for pain control with much less risk of __ ___. It produces ___.
- kappa agonist- post-surgery- less risk of respiratory depression- dysphoria
Doxepin is another ___ used for __ ___. It is also highly _____.
- TCA- chronic pain- anti-cholinergic
Opiod dependence is its own category. It is not the same as ___ ___ dependence.
NOT same as sedative hypnotic dependence
Which drugs do opioids interact with and how?
+ sedatives increases CNS and respiratory depression; + antipsychotics increases sedation, antimuscarinic effects, and alpha block; + MAOI is contraindicated because it will lead to hypertension and hyperpyrexic coma
Opiods are a class of compounds that bind to __ ___. This includes __, ____, partial agonists, and mixed agonists/antagonists. This is the preferred term.
- opioid receptors- agonists, antagonists
The ___ ___ ___ are the most important receptor for most drugs. Sometimes ___ is also targeted.
- mu opioid receptors- kappa
Tramadol is a weak agonist of which opioid receptor? What does it inhibit? What are its side effects?
mu; reuptake of norepinephrine and serotonin; seizures, dependence, withdrawal symptoms
if treat person who is not dependent on opiods but it is ER for overdose and give them Naloxone, what happens?
- save their life- pushes opioids off mu receptors- respirations come back up- recover consciousness
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