[PHARM] Opioids [Iszard] Flashcards
What is the general MOA of Opioids?
Bind to Opioid Receptors in the CNS –> inhibits ascending pain pathways –> alters perception of pain –> CNS Depression
What is the onset of action of the following?
Oral Opioids (Immediate Release)
IV
Oral –> 30 mins
IV –> 5-10 mins
What is the intended duration of action for the following:
Immediate Release –>
Extended Release –>
Epidural/Intrathecal –>
Suppository –>
Immediate Release –> 3-5 hrs
Extended Release –> 8-24 hrs
Epidural/Intrathecal –> 24 hrs
Suppository –> 3-7 hrs
What are some adverse effects of Opioids?
CNS Depression
Constipation
Hypotension
What is the black box warning of Opioids?
Fatal Respiratory Depression
What is the correct order of Opioid Potency from least to greatest?
Oxycodone, Hydrocodone,Methadone, Fentanyl
LEAST: Hydrocodone
Oxycodone
Methadone
Fentanyl: GREATEST
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What are some of the clinical uses of Opioid use in clinical settings to help reduce pain?
MI
Sickle Cell Crisis
Post OP
Trauma
Cancer
Kidney Stones
Back Pain
What are the 3 Opioid Receptors?
What are their endogenous opioid peptide affinities?
Mu –> Endorphins > Enkephalins > Dynorphins
Delta –> Enkephalins > Endorphins > Dynorphins
Kappa –> Dynorphins >> Endorphins - Enkephalins
Which of the opioid receptors functions as a supraspinal and spinal analgesia, psychotomimetic effects, and slow gastrointestinal transit?
Kappa
Which of the Opioid Receptors functions as a supraspinal and spinal analgesia, modulation of hormone and NT release?
Delta
Which of the opioid receptors functions as a supraspinal and spinal analgesia, sedation, inhibition of respiration, slowed GI transit, modulation of hormone and NT release?
Mu
List what type of functional class each of the drugs are:
Methadone
Buprenorphine
Naloxone
Methadone –> Full Agonist
Buprenorphine –> Parial Agonist
Naloxone –> Antagonist
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If you have a patient that comes in while taking Opioids who complains of Respiratory Depression, Pruritis, N/V, Delirium, Sedation, Constipation, or Seizures – what sort of adverse effects to opioids are these?
Acute Adverse Effects
If a patient comes in while taking an opioid and they have increased CNS depression, and respiratory depression – what sort of drug interaction must you be worried about?
Opioid interactions with SEDATIVE-HYPNOTICS
If a patient comes in while taking an Opioid and complains of Increased Sedation, and accentuation of cardiovascular effects, and some variable respiratory depression – what sort of drug interaction are you thinking of?
Opioid interactions with Anti-Psychotic Agents
If you have a patient come in while taking an Opioid and they have hyperpyrexic coma and HTN – what sort of Opioid drug interactions should you think about?
Opioid interactions with MAOI
If someone comes in with an Opioid Overdose what drug should you give them?
Naloxone (Narcan)
–Pure opioid antagonist (releasing catecholamines)
What is the indicated use of Naltrexone (an Opioid Antagonist)?
(Works on Mu Receptors)
acts as a competitive antagonist at opioid receptor sites
Tx of Alcohol use disorder***
blocks effects of exogenously administered opioids
***he basically said this would be a test question
If a patient was recently given Naltrexone, what warning or precaution should you let them know about?
They may respond to lower opioid doses than previously used – watch out for opioid intoxication
Also watch out for Acute Opioid Withdrawl
What are the 9 Opioid Agonists?
Morphine
Hydromorphine
Methadone
Meperidine
Fentanyl
Codeine
Oxycodone
Hydrocodone
Propoxyphene
What are the 4 mixed agonist/antagonist (partial agonist) Opioids?
Pentazocine
Nalbuphine
Buprenorphine
Butorphanol
What are the 2 Opioid Antagonists?
Naloxone
Naltrexone
Morphine, Hydromorphone, Hydrocodone, Oxycodone are what type of chemical class of Opioids?
Phenanthrenes
Fentanyl, Meperidine are what type of chemical class of Opioids?
Phenylpiperidines
Pentazocine and Loperamide are what chemical class of Opioids?
Benzomorphans
Methadone and Propoxyphene are what chemical class of Opioids?
Diphenylheptanes
Morphine Sulfate is a what type of opioid?
What are its contraindications?
What warnings are involved?
What are some adverese reactions?
Opioid Agonist – tx pain not responsive to non-narcotic analgesics
Hypersensitivity to morphine, Asthma
Dosing Errors, Resp Depression, CNS Toxicitiy, CNS Depressants
Sedation, N/V/Lightheadedness, Constipation
What is the drug Buprenorphine used for?
What is a warning for using this drug?
It has the same adverse effects as regular opioids.
What drug interactions does it have?
Tx of Opioid Dependence
Can be abused like opioids, Resp Depression,
CYP3A4 inhibitors/inducers
Fentanyl is what type of opioid?
When is Fentanyl indicated?
- Full Opioid Agonist
- Indicated for management of persistent, moderate to severe chronic pain
Methadone is what type of opiate?
When is Methadone indicated?
Methadone is a synthetic full agonist opioid
-most appropriate drug to manage abstinence symptoms and treat opioid use disorder in an outpatient rehabilitation setting ***
***he basically said this was going to be a test question
Hydrocodone is what type of opioid?
When is it indicated?
Hydrocodone is a semi-synthetic full opioid agonist
for relief of moderate to moderately severe pain and for antitussive properties
Hydrocodone is often combined with what?
What is important to keep in mind about this?
Hydrocodone is often combined with acetaminophen
not to be used for a long time as this could lead to hepatotoxicity
Pentazocine is what type of opioid?
When is it indicated?
Pentazocine is a mixed opioid agonist/antagonist
used in the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate
does not work well for treating addiction
What is an adverse effect observed in pregnant patients using pentazocine?
prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome
Meperidine is what type of opioid?
Drug interactions?
Likely to be abused?
Full opioid agonist
Avoid mixed agonist/antagonist analgesics use with meperidine because the analgesic effect may be reduced or may precipitate withdrawal symptoms
the anesthesiologist is the key abuser for meperidine bc they have direct access***
***he basically said this would be a test question
Codeine is what type of opioid?
What is an important property about Codeine to remember?
Codeine is classified as a moderate full opioid agonist
Compared to fentanyl, hydromorphone, meperidine, and morphine, codeine contains the least opioid analgesic activity***
***He basically said this would be a test question
What is the trade name for Loperamide?
What is an off-label use of loperamide?
imodium A-D
loperamide is used when you don’t have morphine around