Benzodiazepines

Question 1

Most frequently encountered benzodiazepines are

Answer 1

Alprazolam

Diazepam

Question 2

Color Tests

Answer 2

Zimmerman-Reinhardt (Janovsky)

Question 3

Analytical Methods

Answer 3

TLC
SPE
GC
LC/MS/MS

Question 4

Benzodiazepines are what schedule type of drug?

Answer 4

Schedule IV

Question 5

Substiuent Effects

Answer 5

Electron withdrawing group binds

• C-7 = enhanced activity
• C-2’ = drug is more potent, increases amnesic effect
• N-1 = greater intrinsic effects
• C-3 = reduces duration of the drug and allows faster excretion
• if ring attaches to N-1 and C-2 = drug is more potent

Question 6

pKa1 –> N-4 position

Answer 6

(+) –> neutral

Question 7

pKa2 –> N-1. Position

Answer 7

Neutral –> (-)

Question 8

Absorption

Answer 8

Highly lipophilic

Rapidly crosses blood-brain barrier and placental barrier

Question 9

Administration

Answer 9

Oral
Intravenously
Intramuscularly

Question 10

Benzodiazepines vary in

Answer 10

Dosage
Onset of action
Duration of action tendency to accumulate
Potency

Question 11

Major binding protein

Answer 11

Albumin

Question 12

Most forms of benzodiazepines are excreted

Answer 12

In urine form of the oxidized and glucuronide-conjugated metabolites

Amount of drug present in urine in elimination process is also dependent on type of benzodiazepine