Opioid Drugs Flashcards
What are the strong agonists
Morphine Hydromorphone Oxymorphone Heroin Meperidine Fentanyl Sufentanil Alfentanil Methadone Levorphanol
What are the Mild to Moderate Agonists
Codeine Oxycodone Hydrocodone Propoxyphene Tramadol
What are the Mixed Agonist/Antagonist
Pentazocine
Butorphanol
Nalbuphine
Buprenorphine
What are the Mu, Delta, Kappa Antagonists
Naloxone
Naltrexone
What are the Antitussives
Dextromethorphan
Codeine
What are the Antimotility Agents
Diphenoxylate
Loperamide
What is the standard for Analgesia
Morphine
How is Morphine metabolized
M3G causing neuro-excitation
M6G (10%) more potent
Can Morphine metabolites cross BBB
No
What is a hazard of renal impairment on Morphine metabolites
Increased effect
What is Heroin metabolized to
6-MAM then morphine
What is unique about 6-MAM and Heroin
Can cross BBB
Why does Meperidine have high metabolite toxicity
Normeperidine causes tremor, twitching, mydriasis, hyperreflexia, convulsions
What is a major AE of Meperidine
Serotonin Syndrome
What is seen in Serotonin Syndrome
Delerium
Hyperthermia
HA, rigidity, coma
What do you not give with Meperidine
MAOIs
Pt on Meperidine has seizures
Decreased renal function and Normeperidine accumulation
Does Meperidine or Normeperidine have a longer t1/2
Normeperidine
Which strong agonist has a rapid onset and short duration (100x more potent than morphine)
Fentanyl
Sufentanil
Alfentanil
Remifentanil
What are the Fentanyls metabolized by
3A4
Equal potency to morphine, but less euphoria and longer acting
Methadone
Levorphanol
Opioid withdrawal in Heroin addict
Methadone
Levorphanol
What do Methadone and Levorphanol act on
Mu
NMDA antagonist
5-HT/NE reup inhibitor
What can cause QT prolongation
Methadone
Levorphanol
Which mild/moderate do you combine with Aspirin or Acetaminophen
Codeine
Oxycodone
Hydrocodone
What is metabolized by 2D6
Codeine
Hydroxycodone
Hydrocodone
Affinity of Codeine to opioid receptors
Low
No longer on the market
Propoxyphene
What about Propoxyphene makes it toxic
Metabolite Norpropoxyphene
Good for Neuropathic pain
Tramadol
What does Tramadol act on
Weak Mu
5-HT/NE reup inhibitor
What are the Tramadol AE
Risk of seizures
Serotonin Syndrome
Why are mixed not routine
Ceiling
Which mixed can cause psychotomimetic effects
Pentazocine
Butorphanol
Nalbuphine
Which mixed act on Mu and Kappa
Butorphanol (K ag, Mu anti)
Buprenorphine (Mu ag, K anti)
What were Mixed developed for
Reduce addiction potential esp. Buprenorphine
What is given for acute opioid overdose
Naloxone
What is given to decreased EtOH craving
Naltrexone (also for opioid addicts)
What are the most effect cough suppressors
Dextromethorphan
Codeine
Is the antitussive effect through opioid receptors
No
Diarrhea Tx
Diphenoxylate
Loperadine
What do the Antimotility Agents act on
Mu
Delta
