Benzodiazepines

Alpha 1 subtype

Sedation

Alpha 2&5

Anxiolytic

Alpha 1,2,3

Anticonvulsants

Which position are EWG needed

#7 position

Examples of EWG

Cl, Br,F,CN,CF3,NO2

What are the most potent groups

Trifluromethyl and nitro

At which positions is activity decreased

6,8,9

The aromatic ring at what position is necessary

5

Which substitutions on the aromatic ring increases potency

Ortho or di-ortho

Which substitution decreases potency

Para

What substitution causes antagonist activity

No aromatic ring on the five position

Reduction of which double bond or shift decreases potency

4,5 double bond or shift to 3,4 double bond

Alkyl sub at which positions decreases potency

3

Which sub on the 3 position does not affect potency but causes a shorter half life

Hydroxyl

Hydroxyl subs on the 3 position are eliminated how

Glucaronidation and excreted

What happens to esters at the 3 position

Easily hydrolyzed

How do you get a benzo prodrug

Carboxylic acid on the 3 position

Decarboxylation occurs under what conditions

Acidic environments in stomach

Which 2 position has optimum activity

2-carbonyl

The N-1 sub should be big or small

Small

What’s the difference between a triazole vs imidazole

Imidazole does not have a nitrogen on the 3

Which compounds usually have a short half life and do not accumulate

Triazole and imidazole

What is usually the final product before glucuronidation

Oxazepam

Which non-benzo has rapid absorption food delays, metabolized by 3A4, and can cause amnesia

Ambien

Which non-benzo is metabolized by aldehyde oxidase, 30% bioavailability, and can cause amnesia

Which non-benzo is a S-isomer of zopiclone, metabolized by 3A4 and 2E1 to one active metabolite and one non active, and can cause HA, hallucinations, unpleasant taste

Lunesta

Which drug is best for sleep onset problems, agonists at melatonin receptors, bioavailable 1.8%, metabolized by 1A2, can cause HA, depression, and worsened insomnia

Ramelton