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30 Cards in this Set
- Front
- Back
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Which part of the opioid molecule dictates agonist/antagonist effects?
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amine (nitrogen substitution)
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Methyl substituent on the opioid amine gives (agonist/antagonist)
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agonist
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3-5 carbons on the opioid amine with a double bond or carbocyclic ring gives (agonists/antagonists/partial agonists) at the mu receptor
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antagonists or partial agonists
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Addition of what specific group to the opioid amine increases the potency as compared to the methyl about 10x?
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phenylethyl
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Addition of a phenylethyl group on the opioid amine (increases/decreases) potency compared to the methyl
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increases (10x)
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Repeat administration of which opioid can lead to accumulation?
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Levorphanol
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Which opioid is the methyl ether of dextrorphan?
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Dextromethorphan
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What is the cause of euphoria, feeling of floating, and hallucinations from dextromethorphan?
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it's metabolite, dextrophan (isomer of Levorphanol)
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Which opioid metabolite can accumulate and lead to toxicity?
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Mepiridine (normepiridine)
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Which opioid causes excitatory symptoms such as hallucinations, tremors, muscle twitch, and convulsions?
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Mepiridine
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Which opioid cannot be abused by the IV route?
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Diphenoxylate
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Which opioid is mixed with atropine in the oral formulation?
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Diphenoxylate
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Which opioid is a substrate for p-glycoprotein?
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Loperamide
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Which full opioid agonist is highly protein and tissue bound?
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Methadone
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Which isomer of methadone has anti-tussive effects?
D or L |
D-isomer
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What is the mechanism of action of tramadol? (2)
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Weak mu agonist
NE and 5HT reuptake inhibition (analgesia) |
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Which tramadol isomer is a mu agonist and inhibits 5HT (serotonin) reuptake?
(+) or (-) |
(+) isomer
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Which tramadol isomer inhibits NE reuptake and is an alpha2 agonist?
(+) or (-) |
(-) isomer
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What is the mechanism of action of tapentadol (Nucynta)? (2)
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Mu agonist
NERI |
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Which opioids produce a ceiling effect on analgesia? (3)
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Pentazocine, Nalbuphine, Butorphanol
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Which opioid is structurally related to levorphanol?
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Butorphanol
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Which opioid is used to maintain addicts due to its long half-life?
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Buprenorphine
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Which opioid antagonist is only used IV because of its short half-life?
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Naloxone
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Which opioid antagonist is used for alcoholism to block the dopamine pathway needed for reward?
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Naltrexone
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Arrange in order from decreasing potency to increasing potency...
(morphine, hydromorphone, oxymorphone) |
morphine < hydromorphone < oxymorphone
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Arrange in order from decreasing potency to increasing potency...
(codeine, oxycodone, hydrocodone) |
codeine < hydrocodone = oxycodone
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Arrange in order from decreasing potency to increasing potency...
(fentanyl, mepiridine, remifentanil, sufentanil, alfentanil) |
mepiridine < fentanyl = remifentanil = alfentanil < sufentanil
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Arrange in order from decreasing potency to increasing potency...
(butorphanol, buprenorphine, nalbuphine) |
nalbuphine < butorphanol < buprenorphine
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Fentanyl has a (fast/slow) onset/recovery
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fast
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Which opioid is not used anymore?
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alfentanil
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