Flashcards in Opioids / Narcotics Deck (17):
Morphine, codeine, oxycodone, and methadone are all opioid analgesics that act on what receptors, and are they agonists or antagonists?
Mu opioid receptors (agonists)
Name the 2 major metabolites of morphine. Which one is more active / has higher potency?
M3 and M6; M6 is the active and more potent metabolite
Which opioid is commonly used in cough medicine because it is antitussive?
Codeine (morphine is also antitussive; codeine gets metabolized to morphine)
A Caucasian patient takes codeine and suffers dry mouth, delirium, urticaria, pruritis, and urinary incontinence, but their pain doesn't go away. What enzyme might be deficient in this patient, and why is this enzyme needed?
CYP2D6, which converts codeine to morphine (codeine has low receptor affinity so it isn't a great analgesic anyways)
What kind of drugs are tramadol and fentanyl, what receptors do they affect, and are they agonists or antagonists?
Opiods; mu opioid receptor agonists
What synthetic analog of codeine inhibits NE and 5HT reuptake as well as the usual actions on mu receptors?
What kind of drugs are meperidine and propoxyphene, and why are they no longer recommended for use?
Opiods / mu opioid receptor agonists; not recommended for treating pain due to CNS effects
How is fentanyl usualy administered, and what molecular property makes it so potent?
Transdermal patch (long term, long half-life, don't change dose more than 1x/week); very lipid soluble
Which opioid is used to treat heroin addicts? Where does it accumulate in the body?
Methadone; 90% is bound to plasma proteins or accumulates in tissues
Which 2 opioids have the longest half lives and greatest risk of overdose? How often can their doses be adjusted?
Fentanyl and methadone; therefore should not change dose more than once a week
Diphenoxylate and loperamide are safer analogs of what opioid, and what are they used to treat?
Meperidine; treat diarrhea
What 2 effects do diphenoxylate and loperamide have in the body?
They slow peristalsis and decrease intestinal secretions (reduce diarrhea symptoms)
Give 3 important side effects of using any opioid.
Miosis, constipation, and respiratory depression
What receptors does naloxone affect, is it an agonist or antagonist, and competitive or noncompetitive?
Mu, delta, and kappa opioid receptor antagonist, competitive
What receptor does naltrexone affect, is it an agonist or antagonist, and how is the drug used therapeutically?
Mu opioid receptor antagonist; used for alcoholism
Nausea, vomiting, piloerection, and yawning are side effects of what kind of reaction to opioids?
These are all side effects of opioid withdrawal, such as after naloxone or naltrexone administration (although opioids themselves can also cause nausea and vomiting...)