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42 Cards in this Set
- Front
- Back
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Phenobarbituric acid
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Barbiturate
LA (Saturated, aromatic) anticonvulsant, anxiety sodium salt, oral/inj moderate PPB aromatic hydroxylation |
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Methylbarbital
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Barbiturate (LA saturated)
insomnia, anxiety aromatic hydrox |
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Thiopental
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Barbiturate
(intermediate --> SA) saturated + branched |
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Diazepam (Valium)
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BDZ LA (active metabolites)
1. N-dealkylation 2. Aliphatic hydrox 3. Aromatic hydrox Glucuronidation Preanesthetic, anticonvulsant PO/inj |
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Flurazepam
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LA BDZ
Basic for oral use 1. N-dealkylation 2. Aliphatic hydrox 3. Aromatic hydrox Glucuronidation |
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Clorazepate
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LA BDZ
PO salt Decarboxylation, aliphatic hydrox |
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Chlordiazepoxide (Librium)
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LA BDZ
HCL salt, NCH3 at c3 PO/inj with solubilizing factors |
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Lorazepam
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Intermediate BDZ
OH at c3 *glucuronidation |
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Oxazepam
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Intermediate BDZ
OH at c3 *glucuronidation |
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Temazepam
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Intermediate BDZ
OH at c3 *glucuronidation |
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Triazolam
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short --> ultrashort BDZ
Additional triazole ring fast hydroxylation of CH3 DOC for preanesthesia HCL salt, inj |
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Alprazolam
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short --> ultrashort BDZ
Additional triazole ring fast hydroxylation of CH3 DOC for preanesthesia HCL salt, inj |
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Midazolam
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short --> ultrashort BDZ
Additional triazole ring fast hydroxylation of CH3 DOC for preanesthesia HCL salt, inj |
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Zolpidem
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BDZ like
6/5 fusion SA, Aliphatic hydroxylation for insomnia |
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Zopiclone/Eszopiclone
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BDZ like
6/5 fusion SA, N-dealkylation Insomnia Chiral enatiomers |
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Dexomedetormidine
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Hypnosedative for insomnia
Alpha2 agonist |
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Chloralhydrate
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Hypnosedative for insomnia
Alcohol dehydrogenase prolongs effect of alcohol |
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Triclofos
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Hypnosedative for insomnia
similar to choloralhydrate but no effect w/ alcohol |
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Inhibitory NT
(2) |
GABA
Glycine |
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Excitatory NT
(3) |
Glutamate
Sodium Calcium |
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Morphine
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Mu agonist
N-demethylation PO/inj |
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Codeine
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Mu agonist, antitussive
Morphine analog O-demethylation to yield morphine |
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Hydromorphone
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Mu agonist
Morphine analog 10x more potent than morphine (metabolite of hydrocodone) |
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Oxymorphone
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Mu agonist
Morphine analog 100x more potent metabolite of oxycodone |
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Hydrocodone
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Mu agonist antitussive
Morphine analog O-demethylation--> hydromorphone |
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Oxycodone
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Mu agonist, potent antitussive
Morphine analog O-demethylation --> oxymorphone |
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Nalorphine
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• µ antagonist
• κ, δ agonist |
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Nalbuphine
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• µ antagonist
• κ, δ agonist |
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Naloxone
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Mu antagonist
injection/PO |
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Naltrexone
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Mu antagonist
injection |
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Buprenorphine
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Mu antagonist Kappa agonist
decreased euphoria, dependence Oripavines- additional ring |
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Levorphanol
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Morphinans
5x potency as morphine |
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Dextromethorphan
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Morphinans
Antitussive Some analgesia after O-demethylation |
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Butorphanol
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Morphinans
Mu antag/ Kappa agonist treat migraines |
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Pentazocine
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Benzomorphan (no C or D)
Mu antagonist mild analgesia at Kappa |
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Meperidine
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Phenylpiperidines (A-E)
weak analgesic PO |
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Diphenoxylate
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Phenylpiperidines (A-E)
Weak analgesic antidiarrheal |
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Loperamide
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Phenylpiperidines (A-E)
no analgesia antidiarrheal |
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Fentanyl
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Anilinopiperidines
100x as potent Amidases, N-dealkylation, aromatic hydrox |
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Sulfentanyl
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Anilinopiperidines
1000x as potent |
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Methadone
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Phenylpropylamines
Weak µ agonist N-demethylation active metabolites |
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Propoxyphene
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Phenylpropylamines
Weak analgesic |
