Term
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Definition
Strong AGONIST (Sched II)
LOW bioavailability (^^1st Pass Effect)
Admin parenterally
Don't give with head injury/asthma/sedatives |
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Term
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Definition
Strong Synthetic Mu AGONIST (Sched II)
85% bioavailable
IDENTICAL to Morphine (+ Cross-tolerance/dependence)
Detoxify morphine/heroin abusers |
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Term
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Definition
Strong Synthetic Mu AGONIST (Sched II)
50% bioavailble
10x weaker than Morphine
LESS miosis, SMC effects
Liver metabolite = Normeperidine -> CONVULSANT properties |
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Term
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Definition
HIGHLY POTENT Mu AGONIST (Sched I)
Lipid soluble -> RAPID CNS penetrance
Robust euphoria |
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Term
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Definition
Strong Mu AGONIST (Sched II)
100x more potent than Morphine
Anaesthesia
Teratogenic
Alfentanil+Remifentanil = FASTER but SHORT duration |
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Term
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Definition
Semi-synthetic Moderate My AGONIST (Sched II)
High bioavailbility
Oxycontin, Percodan, Percocet
Cancer pain |
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Term
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Definition
Synthetic Weak Mu AGONIST (Sched IV)
Low abuse, NOT effective
Irritation at injection site |
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Term
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Definition
Mild-moderate AGONIST (Sched III/V)
Component of Opium
Converted by CYP2D6 to Morphine
Antitussive |
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Term
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Definition
Synthetic Weak Mu AGONIST
GABA, NE, 5-HT Activity
Converted by CYP2D6 for ^ Mu affinity
Don't take with SSRIs |
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Term
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Definition
Kappa AGONIST, Weak Mu Partial AGONIST
(Sched IV)
Dysphoria at high doses
Oral prep has Naloxone -> Prevent abuse via injection |
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Term
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Definition
High affinity Partial Mu AGONIST (Sched III)
LONG t1/2 -> Naloxone ineffective
Methadone -> Buprenorphine for addicts |
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Term
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Definition
*Mu*, Kappa, Delta ANTAGONIST
NOT bioavailable
SHORT t1/2
ONLY reverses receptor-mediated effects |
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Term
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Definition
SAME AS NALOXONE
LONGER t1/2
Bioavailable
Treat alcoholism |
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Term
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Definition
SIMILAR to Naltrexone
ONLY parenteral admin
Reverse effects of LONG-ACTING Mu agonists
Less renarcotization |
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