Anxiolytic, Sedative, and Hypnotic Drugs

Question 1

Phenobarbital

Answer 1

Barbiturate class
MOA: bind to GABA channels to increase the duration of channel opening, thus leading to hyper hyperpolarization
ADRs: tolerance, sedation via GABA channel, addiction
Uses: less used for partial and tonic clonic SZ, but more effective in children

Question 2

Thiopental

Answer 2

Barbiturate class
MOA: enhance GABA-A via increased duration and block sodium channels
ADRs: respiratory distress and low TI
Uses: induction agent to bring patients to phase III

Question 3

Benzo

Answer 3

MOA: increase the rate of firing of GABA-A channels
ADRs: tolerance (1-2 wks), sedation, addiction, should not be used in combination with other anxiolytics or CNS depressants. Should not be used with alcohol because alcohol more readily binds to CYP enzymes = slower breakdown of BDZ
Uses: partial and tonic clonic SZ, acute panic attacks, insomnia

Question 4

Flumazenil

Answer 4

agent used for BDZ / zolpidem / eszoplicone OD because they all bind to the GABA-A receptor

Question 5

Zolpidem & Eszoplicone

Answer 5

Non-BDZ hypnotics
MOA: act as agonists for BDZ site on the GABA-A channel
ADRs: Drug-Drug interactions via CYP3A, sedation via GABA channel
Uses: insomnia and sedation without the tolerance and addiction

Question 6

Buspirone

Answer 6

Non-sedating anxiolytic
MOA: agonist for the 5-HT1 receptor pre-/post-synaptically
ADRs: metabolized by CYP3A, so can be either induced or inhibited based on drug interactions. Overall, non-sedating and non-addictive because no effect on GABA
Uses: chronic GAD