Sedative Hypnotics

Question 1

Classification of sedatives and hypnotics.

Answer 1

1. Benzodiazepines - diazepam, alprazolam, lorazepam, nitrazepam, clobazam
2. Barbiturates - phenobarbitone, secobarbitone, thiopentone, meohobarbitone
3. Non-benzodiazepines - Zolpidem, zipiclone, zaleplon, eszopiclone.
4. Melatonin receptor agonists-ramelteon
5. Miscellaneous - chloro hydrate, promethazine, opioids, neuroleptics, etc.

Question 2

Name the clinical uses of sedatives and hypnotics?

Answer 2

1. Anxiety
2. Sleep disorders
3. Bipolar disorders
4. Seizure management
5. Muscle spasticity
6. Management of withdrawal states

Question 3

Which drugs when added with sedative hypnotics causes additive CNS depression?

Answer 3

1. Alcoholic beverages
2. Anti-histamines
3. Anti-psychotic drugs
4. Opioid analgesics
5. Tricyclic antidepressants

Question 4

What are the toxicities of sedatives and hypnotics?

Answer 4

1. Psychomotor dysfunction
2. Overdose
3. Additive CNS depression (cardiac and respiratory depression)
4. increase anticoagulant effect
5. acute porphyria
6. formation of liver microsomal enzymes that metabolize drugs

Question 5

What peptide is found in the hypothalamus and involved in wakefulness?
What’s it’s antagonist?

Answer 5

Orexin
Suvorexant

Question 6

Flumanzenil is used for the overdose of which drugs?

Answer 6

Benzodiazepines, eszopiclone, zaleplon

Question 7

Clinical applications of benzodiazepines?

Answer 7

1. Anxiety states and anxiety disorder
2. Panic attacks
3. Insomnia
4. Skeletal muscle relaxation
5. Seizure control

Question 8

Mechanism of action of benzodiazepines

Answer 8

Bind GABA(A) receptors to facilitate chloride channel opening and increase frequency.

Question 9

Mechanism of action of barbiturates

Answer 9

Bind to GABA(A) receptor sites (different from benzodiazepines) and facilitate chloride channel opening and increase duration.

Question 10

Clinical applications of barbiturates

Answer 10

1. Anesthesia
2. Insomnia and sedation
3. Seizure disorders

Question 11

Which hypnotic drug causes endocrine changes?

Answer 11

Ramelteon (melatonin receptor agonist)

Question 12

Name 5-HT agonist for anxiety state?

Answer 12

Buspirone

Question 13

Name newer hypnotics used for sleep disorders.

Answer 13

1. Eszopiclone
2. Zaleplon
3. Zolpidem