Term
| Benzodiazepines - 1st Generation |
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Definition
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Term
| Benzodiazepines - 2nd Generation |
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Definition
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Term
| Benzodiazepines - 2nd Generation |
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Definition
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Term
| only _____substitutions on aromatic ring are active |
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Definition
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Term
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Definition
O or N
(S decreases potency) |
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Term
| Substituents at 2' that are meta or para ______activity of BDZ |
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Definition
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Term
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Definition
Chlordiazepoxide-----Diazepam
Oxazepam----Clorazepate
Lorazepam----Clonazepam
Temazepam----Quazepam |
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Term
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Definition
| Chlordiazepoxide (Librium®) |
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Definition
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Definition
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Definition
Clorazepate (Tranxene®)
PRODRUG!!! |
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Definition
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Definition
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Term
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Definition
Flunitrazepam (Rohypnol®)
10x as potent as Valium |
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Term
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Definition
Flurazepam (Dalmane®)
PRODRUG!! |
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Definition
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Definition
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Definition
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Definition
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Definition
Flumazenil (Romazicon®)
BZR Competitive antagonist
ANTIDOTE |
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Term
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Definition
Buspirone
Full agonist at presynaptic 5HT1A receptors
Functional Antagonist at postsynaptic 5HT1A receptors
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Definition
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Definition
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Definition
ZOLPIDEM (Ambien, Intermezzo)
GABAA receptor BZ-1 site
(Induces Physiological Sleep)
Imidazopyridine |
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Term
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Definition
Zaleplon (Sonata)
Interacts with BZ-1 site
Pyrazolopyrimidine |
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Term
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Definition
• Eszopiclone (Lunesta®)
GABAa agonist binds both BZ-1 and BZ-2 sites with no selectivity
Pyrrolopyrazine |
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Definition
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Term
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Definition
Ramelteon (Rozerem)
Melatonin receptor agonist |
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Term
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Definition
Tasimelteon (Hetlioz®)
MOA:MT1 and MT2 ) receptor agonist in the suprachiasmatic nucleus
non-24-hour sleep-wake disorder in totally blind people
Can elevate liver enzymes (ALT |
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Term
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Definition
Suvorexant (Belsomra®)
Orexin receptor antagonist to treat difficulties with sleep onset and/or maintenance |
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Term
| Melatonin Receptors are GPCRs and ____ |
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Definition
| are coupled to adenylyl cyclase inhibition thus inhibiting cAMP synthesis |
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Term
| 1st Gen BDZ Metabolized how? |
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Definition
N-dealkylation at N-1
Alicyclic oxidation at C-3
Both ACTIVE |
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Term
| 2nd Gen BDZ Metabolized how? |
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Definition
Alicyclic Oxidation at C-3 = Active
-CH3 oxidation on triazole or imidazole ring = inactive |
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Term
short acting barbs
intermediate
long acting |
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Definition
pentobarbital, secobarbital
amobarb
barb and phenobarbital |
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