Term
| Codeine: Class, Potency, Metabolism |
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Definition
Phenanthrene
Low potency
Great for antitussive
Must be converted to morphine by CYP 2D6
One of the most constipating opioids |
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Term
| Hydrocodone: Class, Metabolism |
|
Definition
Phenanthrene
Parent and metabolite active
Hydrocodone to hydromorphone by CYP 2D6
Little effect of metabolite on analgesia |
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Term
| Hydromorphone: Class, Metabolism |
|
Definition
Phenanthrene
Glucuronidated to similar metabolites as morphine (H3G and H6G)
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Term
| Levorphanol: Class, Activity |
|
Definition
Phenanthrene
Opioid + NMDA activity |
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Term
| Oxycodone: Class, Metabolism |
|
Definition
Phenanthrene
Active parent drug
Metabolized to oxymorphone via CYP 2D6
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Term
| Oxymorphone: Class, Metabolism |
|
Definition
Phenanthrene
Active metabolite of oxycodone
Undergoes glucuronidation and reduction |
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Term
|
Definition
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Term
| Nalbuphine: Class, Metabolism, Activity |
|
Definition
Phenanthrene
Metabolized to inactive metabolites hepatically
Stimulates kappa
Antagonizes Mu receptors |
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Term
| Butorphanol: Class, Metabolism, Receptor Activity |
|
Definition
Phenanthrene
Metabolized primarily to hydroxybutorphanol (inactive) hepatically
Kappa agonist
Sigma agonist
Mu antagonist |
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Term
| Naloxone: Class, Receptor Activity, Uses |
|
Definition
Phenanthrene
Pure opioid antagonist
Used for opioid overdose reversal |
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Term
|
Definition
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Term
| Pentazocine: Class, Activity |
|
Definition
Benzomorphan
Agonist at Kappa
Antagonist at Mu |
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Term
| Morphine: Class, Metabolism |
|
Definition
Phenanthrene
Undergoes glucuronidation
- M3G = neurotoxicity
- M6G = analgesia
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Term
|
Definition
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Term
|
Definition
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Term
| Meperidine: Class, Cautions |
|
Definition
Phenylpiperidine
Currently being phased out due to ceiliing dose as a result of toxic metabolite (normeperidine)
Accumulaiton in renal insufficiency
Caution reversing overdose with naloxone (seizures may result) |
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Term
| Fentanyl: Class, Metabolism |
|
Definition
Phenylpiperidine
Metabolized via CYP 3A4 to inactive metabolites |
|
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Term
|
Definition
Phenylpiperidine
Rarely used in pain mgmt
Used in extremely opioid tolerant patients |
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Term
|
Definition
Phenylpiperidine
Rarely used |
|
|
Term
|
Definition
Phenylpiperidine
Rarely used |
|
|
Term
| Methadone: Class, Receptor Activity, Metabolism, ADRs |
|
Definition
Diphenylheptane
Opioidergic
NMDA Antagonism
NE/5-HT Reuptake Inhibition
Metabolism via N-demethylation
May cause QTc prolongation, Torsades de Pointes
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Term
| Propoxyphene: Class, Receptor ActivityUses, ADRs |
|
Definition
Diphenylheptane
Opioid and NMDA activity
Usually combined with APAP
Rarely used alone
Constipating
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Term
| Tramadol: Metabolism, Activity, Caution |
|
Definition
- O-demethylated to active metabolite
- Weak Mu-opioid agonist
- Weak NE/5HT reuptake inhibition
- Analgesia NOT reversed by naloxone in studies
- Caution for seizures and serotonin syndrome
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Term
| Fentanyl Patches: Which can you cut? |
|
Definition
Mylan patch you can cut
J&J patch you cannot
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|
|
Term
|
Definition
Fentanyl - 100
Methadone - 10
Hydromorphone - 5
Oxymorphone - 4
Oxycodone - 2
Morphine - 1
Meperidine - 0.1
Codeine - 1/30
Propoxyphene - 0.01 |
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