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Pt care 7 Structures
Neuro
35
Chemistry
Graduate
01/30/2019

Additional Chemistry Flashcards

 


 

Cards

Term
Benzodiazepines - 1st Generation
Definition

-azepam

 

[image]

Term
Benzodiazepines - 2nd Generation
Definition

-azolam

 

[image]

 

 

Term
Benzodiazepines - 2nd Generation
Definition

Imidazo-

 

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Term
BDZ inc in e- act at
Definition
2' and 7 positions
Term
only _____substitutions on aromatic ring are active
Definition
C-7 (usually Cl or NO2)
Term
Optimum atoms at C2 BDZ
Definition

O or N

(S decreases potency)

Term
Substituents at 2' that are meta or para ______activity of BDZ
Definition
DECREASE
Term
1st Gen BDZ
Definition

Chlordiazepoxide-----Diazepam

Oxazepam----Clorazepate

Lorazepam----Clonazepam

Temazepam----Quazepam

Term
[image]
Definition
Chlordiazepoxide (Librium®)
Term
[image]
Definition
Diazepam (Valium®)
Term
[image]
Definition
Oxazepam (Serax®)
Term
[image]
Definition

Clorazepate (Tranxene®) 

 

PRODRUG!!!

Term
[image]
Definition
Lorazepam (Ativan®)
Term
[image]
Definition
Temazepam (Restoril®)
Term
[image]
Definition

Flunitrazepam (Rohypnol®)

 

10x as potent as Valium

Term
[image]
Definition

Flurazepam (Dalmane®)

 

PRODRUG!!

Term
[image]
Definition
Alprazolam (Xanax®)
Term
[image]
Definition
Estazolam (ProSom®)
Term
[image]
Definition
Midazolam (Versed®)
Term
[image]
Definition
Triazolam (Halcion®)
Term
[image]
Definition

Flumazenil (Romazicon®)

 

BZR Competitive antagonist

ANTIDOTE

Term
[image]
Definition

Buspirone

 

Full agonist at presynaptic 5HT1A receptors

Functional Antagonist at postsynaptic 5HT1A receptors

 

Term
[image]
Definition
Phenobarbital
Term
[image]
Definition
Methaqualone (QUAALUDE)
Term
[image]
Definition

ZOLPIDEM (Ambien, Intermezzo)

 

GABAA receptor BZ-1 site

(Induces Physiological Sleep)

 

Imidazopyridine

Term
[image]
Definition

Zaleplon (Sonata)

 

Interacts with BZ-1 site 

 

Pyrazolopyrimidine

Term
[image]
Definition

• Eszopiclone (Lunesta®) 

 

GABAa agonist binds both BZ-1 and BZ-2 sites with no selectivity

 

Pyrrolopyrazine

Term
[image]
Definition
melatonin
Term
[image]
Definition

Ramelteon (Rozerem)

 

Melatonin receptor agonist

Term
[image]
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

Term
[image]
Definition

Suvorexant (Belsomra®)

 

Orexin receptor antagonist to treat difficulties with sleep onset and/or maintenance

Term
Melatonin Receptors are GPCRs and ____
Definition
are coupled to adenylyl cyclase inhibition thus inhibiting cAMP synthesis
Term
1st Gen BDZ Metabolized how?
Definition

N-dealkylation at N-1  

Alicyclic oxidation at C-3

 

 Both ACTIVE

Term
2nd Gen BDZ Metabolized how?
Definition

Alicyclic Oxidation at C-3 = Active

 

-CH3 oxidation on triazole or imidazole ring = inactive

Term
short acting barbs
intermediate
long acting
Definition
pentobarbital, secobarbital

amobarb

barb and phenobarbital
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