Anti-anxiety & Anti-insomnia (exam 2)

Question 1

Chrlodiazepoxide (librium)
Diazepam (valium)
Oxazepam (serax) not metabolized
Alprazolam (xanex) active metabolite

Answer 1

• BZD’s indirectly enhance the inhibitory activity of GABA at the receptor. Site is not on the GABA receptor
• BZD binding will increase activity of the GABA/receptor complex, and open the Cl- channel, hyperpolarizing the cell
• onset is fairly quick; long halflife is sometimes a problem
• BZD act to depress REM stage and 3/4

Question 2

Flumazenil

Answer 2

-benzodiazepine antagonist used to treat BZD overdose symptoms

Question 3

Buspirone (Buspar)

Answer 3

-non-BZD antianxiety; days to weeks until onset
-acts on 5HT receptor as a partial agonist (no GABA influence)
-good for longterm treatment of anxiety, no sedative or incoordination effect
TOX: nausea dizziness, headache

Question 4

Lorazepam (Ativan)

Answer 4

BZD used exclusively for sleep aid
no active metabolite
least likely next day hangover
TOX: retrograde amnesia

Question 5

Tamazepam (Restoril)

Answer 5

metabolized to oxazepam; longer half life
higher chance of next day hangover
TOX: retrograde amnesia

Question 6

Secobarbital (Seconal)
Butabarbital (Butisol)
Phenobarbital

Answer 6

• act to enhance GABA activity at the receptor
• at high doses, can activate the Cl- channel on their own without GABA
• act to decrease sleep latency, increase sleep time
• decrease REM and slow wave sleep
• rebound occurs!
• overdosing can be fatal with barbs, especially when mixed with other CNS depressants (alcohol, BZD)

Question 7

Ambien
Lunesta
Sonata

Answer 7

-Non-benzodiazepines
still act with GABA, much more selective
-mainly acting as sleep agents, as they have increased sedation, but less anti-anxiety/convulsant activity
-minimal disruption to sleep stages
-unlikely to cause withdrawal
-duration of action very short
-should not be used with other CNS depressants

Question 8

Chloral hydrate (Somnote)

Answer 8

• non-barbiturate sleep aid

- quick onset; tolerance and dependence common

Question 9

Rohypnol

Answer 9

• BZD with very fast onset; date rape drug

- amnesia

Question 10

GHB (gamma hydroxy buturante)

Answer 10

date rape drug
precursor to GABA
treats cataplexy and narcolepsy

Question 11

Hydroxyzine (Atarax)

Answer 11

anti histamine used as anti-anxiety

causes sedation, may depress sub-corticol areas

Question 12

Diphenhydramine (Benadryl)

Answer 12

anti-histamine sleep aid

available OTC

Question 13

Ramelteon (Rozerem)

Answer 13

melatonin agonist

headache, nausea, somnolence, dizzy, nausea

Question 14

Alcohol

Answer 14

CNS depressant, disrupts sleep pattern

results in tolerance, dependance, rebound