Anxiolytics

Question 1

What is mainstay short term and long term treatment for anxiety disorders

Answer 1

short term- benzodiazapenes

long term- SSRI

Question 2

Why are benzos used more than barbiturates for anxiety disorders?

Answer 2

Both classes augment the action of GABA but benzos have a “ceiling effect” which in high doses, barbiturates are direct agonists (can lead to full CNS depressions and death)

Question 3

What are the 7 benzodiazepines?

Answer 3

Diazepam, Lorazepam, Flurazepam, Alprazolam, Midazolam, Triazolam and Chlordiazepoxide

Question 4

What are some side effects of benzodiazepines?

Answer 4

Daytime sedation and drowsiness, anterograde amnesia, synergistic depression of CNS with other drugs, pyschologic and physiologic dependence (chronic use)

Question 5

Which benzo is used for amnesia (i.e. during colonoscopy)?

Answer 5

Midazolam- only given IV

Anesthesia (calming effects, production of anterograde amnesia)

Question 6

What are benzos used to treat? Which one is also a muscle relaxant and anti-convulsant? Which 2 produces sedation? Which is used for alcohol withdrawal symptoms? Which induces sleep?

Answer 6

• Short-term depression treatment; maintenance of bipolar; severe bipolar
• diazepam- muscle relaxant, anti-convulsant
• Lorazepam, Alprazolam (Xanax)- sedation
• Lorazepam- EtOH withdrawal
• Triazolam

Question 7

What is the half life of the 7 benzos from shortest to longest?

Answer 7

Midazolam (2hrs) –> Triazolam (3hrs) –> Alprazolam (12hrs) –> Lorazepam (14hrs) –> Chlordiaxepoxide(10hrs), Diazepam(43hrs) and Flurazepam(74hrs) have active metabolites up to 100hrs

Question 8

What is the mechanism, therapeutics and side effects of zolpidem?

Answer 8

(Ambien)
BDZ-1 selective agonist
Sedation and hypnosis without muscle relaxation or anticonvulsant activity (sleeping pill)
Sleep-walking; next morning impairment

Question 9

What drug can be given for a benzo overdose?

Answer 9

Flumazenil

Competitive non-selective GABAa antagonist

Question 10

What are some side effects of barbiturates?

Answer 10

Daytime sedation and drowsiness, dose-dependent depression of CNS, pyschologic and physiologic dependence (chronic use)
Abrupt withdrawal life-threatening

Question 11

What is the mechanism of Thiopental and Phenobarbital? What is the difference between them? Use?

Answer 11

GABAa agonist (binds a or b subunit); 
Thiopental- highly lipid soluble, fast-on, fast-off (very short acting) --> used to induce anesthesia
Phenobarbital- less lipid soluble (t1/2 4-5days) --> used as antiepileptic, anticonvulsant

Question 12

Which 2 drugs are used for sedation (calming) effects?

Answer 12

alprazolam and lorazepam

Question 13

Which 2 drugs induce sleep?

Answer 13

triazolam and zolpidem

Question 14

which 2 drugs are used for anesthesia

Answer 14

Thiopental, midazolam

Question 15

which 3 drugs are used as anti-convulsants?

Answer 15

lorazepam, diazepam, phenobarbital

Question 16

which drug is used for muscle relaxation?

Answer 16

diazepam