Benzodiazepines

Question 1

Benzodiazepines (General Class Info)

Answer 1

Prototype: Diazepam (Valium)

Uses: Anxiolytic, Hypnotic, Anti-convulsant, Muscle Relaxant, Pre-methetic

Similar but NOT a non-selective CNS Depressant

Binding site on GABAa receptors (alpha and gamma subunit)…more SELECTIVE so it works at fewer GABAa receptors (and is safer)

*All are anxiolytic, hypnotic, SAFER THAN BARBITUATES

Question 2

Diazepam (Valium)

Answer 2

Uses: Anxiolytic, anticonvulsant, muscle relaxant, pre-anesthetic

Mechanism: See Benzodiazepines card (selective GABAa receptor)

*Has complex metabolism; 3 active metabolites

Question 3

***Flumazenil (Romazicon)

Answer 3

Uses: Reversal of BZ used for conscious sedation, reversal of BZ used for anesthetic induction, treat BZ overdose

Mechanism: COMPETITIVE BZ ANTAGONIST at GABAa BZ binding site

No action of its own

Short half-life

Question 4

Clonazepam (Klonopin)

Answer 4

Uses: Anticonvulsant
Mechanism: BZ
Complex metabolism; active metabolites
**Used for CHRONIC EPILEPSY

Question 5

Lorazepam (Ativan)

Answer 5

• Uses: anxiolytic, anticonvulsant
• Mechanism: BZ
• Conjugated directly to inactive metabolites

Question 6

Alprazolam (Xanax)

Answer 6

• Uses: *anxiolytic for panic disorder
• Mechanism: BZ
• *Hydroxylation then conjugation to inactive metabolites

Question 7

Midazolam (Versed)

Answer 7

• Uses: Pre-anesthetic
• Mechanism: BZ
• *Hydroxylation then conjugation to inactive metabolites

Question 8

Eszopiclone (Lunesta)

Answer 8

Uses: Hypnotic
Mechanism: BZ

Question 9

Zolpidem (Ambien)

Answer 9

Uses: selective hypnotic
Mechanism: BZ

Question 10

Buspirone (Buspar)

Answer 10

Uses: anxiolytic, treat anxiety disorder (similar to BZs)

Mechanism: Unclear? GABA receptors NOT involved

Onset of clinical effects is very gradual
No other effects of sedation, anticonvulsant/psychomotor impairment

Drug interactions
-Hypertension with MAO inhibitors

Question 11

Ramelteon (Rozerem)

Answer 11

Uses: Hypnotic, mild sedative,
Mechanism: Melatonin agonist (acts like melatonin)
Little abuse potential but hormonal effect
Little interactions with CNS depressants
Induces DSPS (circadian rythm disorder)
Rapid absorption/elimination
Decreases testosterone/increases prolactin

Question 12

Suvorexant (Belsomia)

Answer 12

Uses: Insomnia, shortens sleep latency and reduce awakenings

***Mechanism: Antagonist at orexin receptors in lateral hypothalamus involved in wakefulness and apetite

Major adverse effect is somnolence (strong desire for sleep or sleeping for unusually long periods of time)