Opioid Analgesics and Antagonists Flashcards
Triad of Opioid Overdose
Pupillary Constriction
Comatose State
Respiratory Depression
Opioid with shortest half-life
REMIFENTANIL
3-4 MINS.
Opioid with longest half-life
BUPRENORPHINE
4-8 HRS.
Opioid effects that does not diminish with continuous opioid use
Mioisis
Constipation
Convulsions
Opioid Side effects not mediated by opioid receptors
Nausea, Vomiting, Hypotension, Pruritus
OPIOID RECEPTORS
mu1, mu2, kappa, delta
Mu receptors agonists
Synthetic opioids
Endorphine
Morphine
Kappa receptor agonist
Dynorphins
Delta receptor agonist
Enkephalins
Opioids Partial Agonists
DOH
Dihydrocodeine
Oxycodone
Hydrocodone
CO-DEX
Codeine
Dextrometorphan
Opioid Weak Agonists
Propoxyphene
Levopropoxyphene
Dextropropoxyphene
Opioid Mixed Agonist-Antagonist
Buprenorphine Nalbuphine Butorphanol Pentazocine Levallorphan
Use: Dextrometorphan, Codeine
Cough suppression
May cause fatal arrhythmia
Weak agonists
Propoxyphene
Levopropoxyphene
Deltapropoxyphene
strong agonists of mu and kappa receptors
DOH
Dihydrocodeine
Oxycodone
Hydrocodone
Meperidine (Pethidine)
partial mu receptor agonists and antagonist at kappa and delta receptors
mixed
Butorphanol Nalbuphine Buprenorphine Pentazocine Levallorphan
used in alcohol dependence
mixed
commonly used in suicides
weak agonists
weak agonist that can be used as anti-tussive
levopropoxyphene
Strong kappa agonist and partial mu antagonist
Nalbuphine
kappa agonist and weak mu antagonist
Pentazocine
Effects resistant to Naloxone reversal
Mixed
Used in opioid withdrawal states
Buprenorphine
Receptor for marked constipation
mu 2
Used in postoperative shivering
Butorphanol
FULL AGONIST
phenanthrenes
phenylpiperidine
Meperidine (Pethidine)
phenylheptylamines
PHENANTHRENES
morphine
hydromorphone
oxymorphone
Heroin
PHENYLPIPERIDINE
fentanyl sufentanil alfentanil remifentanil ohmefentanyl
PHENYLHEPTYLAMINES
methadone
levomethadyl acetate
levorphanol
Used in opioid dependence
phenylheptylamines
Normeperidine is contraindicated in patients with
seizure
lowers seizure threshold
May be given transdermally or via lollipop
Phenylpiperidine
TRUE OR FALSE.
MEPERIDINE CAUSES MIOSIS.
False.
MEPERIDINE causes MYDRIASIS.
has the most pronounced anti-shivering effect
MEPERIDINE
May cause QT prolongation as a side effect
METHADONE
OPIOID ANTAGONIST
NALOXONE NALTREXONE NALMEFENE ALVIMOPAN METHYLNALTREXONE
DOC for opioid overdose
NALOXONE
DOC for opioid and alcohol dependence
NALTREXONE
DUAL ACTING
TRAMADOL
TAPENTADOL
MOA: TRAMADOL, TAPENTADOL
weak mu receptor agonist
inhibits neuronal reuptake of serotonin and norepinephrine
inhibits pain neurotransmission