Part II: Anxiety and Sleep

Question 1

Barbiturates prolong the inhibitory effects of GABA and glycine thus depressing neuronal activity in the

Answer 1

midbrain reticular formation

Question 2

How do barbiturates affect GABA-mediated chloride ion channel opening?

Answer 2

Increases the duration of GABA-mediated Cl-channel opening

They may also block Glutamic acid (excitatory) and Na-channels at high concentrations

Question 3

Are Barbiturates antagonized by flumazenil (a BZ receptor antagonist)?

Answer 3

No. Unlike Benzodiazepines which are antagonized by Flumazenil, Barbiturates do not have antagonists

Question 4

CNS drugs are able to reach the CNS based on characteristics including Lipophilicity. The lipophilic nature of drugs allowing them to enter the CNS means that they can also cross the

Answer 4

Placenta

Question 5

Benzodiazepines is an allosteric modulator of the GABAa receptor different from the Barbiturate receptor. How do the diazepines alter GABA’s ability to affect the GABA channel?

Answer 5

When benzos bind, takes less GABA to open the channel

Question 6

Short acting benzos (2-4hours)

Answer 6

Midazolam (IV, anesthesia/pre-anethesia)

Triazolam (hypnotic)

Question 7

Moderate Acting benzos (10-14)

Answer 7

Alprazolam
Chlordiazepoxide
Lorazepam

Question 8

Long acting benzo used for anti-convulsant (24 hour half life)

Answer 8

Clonazepam

Question 9

Very long acting benzos because they have active metabolites

Answer 9

Diazepam (43 hours, can be IV used for status epilepticus, also rectal)
Flurazepam (74 hour half life)

Question 10

Date rape drug that is very fast acting

Answer 10

Flunitrazepam

Question 11

Benzodiazepam antagonist

Answer 11

Flumazinil. Used to reverse overdose of benzodiazepine

Question 12

Benzodiazepines are highly protein bound but counterintuitively have

Answer 12

few drug interactions

Question 13

Benzodiazepine receptor agonists are different than the benzodiazepines because they bind to the receptor but have

Answer 13

non-benzo structure

Question 14

BZ1 selective Agonists:

Answer 14

Zolpidem

Zaleplon

Question 15

Non-selective Non-benzo BZ receptor agonist

Answer 15

Eszopiclone

Question 16

Non-depressant anxiolytic that doesn’t have much abuse liability but people like taking it with benzos and acts on 5-HT1A as a partial agonist but generally unknown activity

Answer 16

Buspirone

Question 17

Buspirone is metabolized by

Answer 17

CYP3A4

Question 18

Buspirone levels are increased by what drugs?

Answer 18

Eythromycin and ketoconazole

Question 19

Benzos and Barbiturates are contraindicated in what sleep disorder?

Answer 19

Obstructive Sleep Apnea (Pickwickian syndrome)

Question 20

What drugs are hypnotics that are not used in seizure or muscle spasticity states but act on the same receptor as benzos?

Answer 20

The non-benzodiazapines:

Eszopiclone
zaleplon
zolpidem