Anxiolytic, Sedative and Hypnotic Drugs-part 1

Question 1

What are benzodiazepines mainly used for,Give an example s

Answer 1

Question 2

Why would you want to use oxazepam for anxiety

Answer 2

For patients with hepatic impairment. Thier enzymes do not work as effeciently , increasing th etime for metabolism so the drug becomes even more long acting. So you ewould use this has it is more short acting than other anxiolytics,

Question 3

What would an ideal benzodiazepine or barbiturate do?

Answer 3

• Produce natural sleep , Not depress respiration , Have a wide margin of safety ,Not produce hangovers or dependence , Not interact with other drugs

Question 4

How does GABA binding affect the GABA A receptor complex?

Answer 4

• Linkage of GABA receptor protein and BDZ receptor protein mediated by GABA modulin - Enhances BDZ binding - Momentary opening of Cl- channel

Question 5

Explain the GABA A receptor complex

Answer 5

Cl- ionophores - cause hyperpolarisation: GABA modulin + GABA R protein + Barbiturate R protein + BDZ R protein in ring with Cl- channel protein in middle

Question 6

Why do benzodiazepines and barbiturates have no activity alone?

Answer 6

They are positive allosteric modulators Only increase freq or duration of opening caused by GABA

Question 7

What makes nitrazepam differe from other SEDATIVE / HYPNOTICS Why would you want to use NITRAZEPAM for sedation?

Answer 7

Nitrazepam is long-acting .If you want anxioltyic effect along side the the sedative effect , like particularly in daytime.

Question 8

What do hypnotics do?

Answer 8

Induce sleep

Question 9

What drugs can increase free [plasma] of benzodiazepines?

Answer 9

Aspirin Heparin

Question 10

What are barbiturates mainly used for,Give an example and the specifc case when you would se it with it;s half life information

Answer 10

Question 11

Describe the metabolism of benzodiazepines

Answer 11

Only remember boxed one for now

Question 12

Recall inhibitors of GABA metabolism and the consequences of their actions

Answer 12

•

• INHIBITORS OF GABA METABOLISM causes LARGE increase in ­ BRAIN GABA
• SODIUM VALPROATE (EPILIM)
• VIGABATRIN (SABRIL)

Question 13

What do anxiolytics do?

Answer 13

Remove anxiety without impairing mental or physical activity

Question 14

Why do the pharmacokinetics of benzodiazepines determine clinical use?

Answer 14

• 20+ different benzodiazepines with very small differences in structure (3 rings, differ in R1, R2, R3, R4) - Same mechanisms of action - Similar potency - Tf pharmacokinetics determine clinical use