Sedative-hypnotic Drugs

Question 1

Benzos

Answer 1

Acute toxicity
• Treatment with flumazenil
• Competitive benzodiazepine receptor antagonist
• Reverses the sedative effects of benzodiazepines but may not
reverse respiratory depression
• Approved for benzodiazepine overdose and for reversing the effects of benzodiazepines after general anesthesia

General treatment measures
• Oral: Gastric lavage, activated charcoal, saline cathartic, and dialysis

Question 2

Zolpidem [Ambien]

BENZODIAZEPINE-LIKE DRUGS

Answer 2

Sedative-hypnotic
• Most widely used hypnotic
• Short-term management of insomnia
• Long term use: No apparent tolerance or increase in adverse effects
• Side effects: Daytime drowsiness and dizziness

Question 3

BENZODIAZEPINE-LIKE DRUGS

Zaleplon [Sonata]

Answer 3

• New class of hypnotics, pyrazolopyrimidines
• Short-term management of insomnia
• Prolonged use does not appear to cause tolerance
• Most common side effects: Headache, nausea, drowsiness, dizziness, myalgia, and abdominal pain

Question 4

BENZODIAZEPINE-LIKE DRUGS

Eszopiclone [Lunesta]

Answer 4

• The S-isomer of zopiclone
• For treatment of insomnia
• No limitation on how long it can be used
• Most common adverse effect: Bitter aftertaste
• Other common side effects: Headache, somnolence, dizziness, and dry mouth

Question 5

RAMELTEON: MELATONIN AGONIS T

Answer 5

• Brand name: Rozerem
• Relatively new hypnotic
• Not a controlled substance
• Activation of melatonin receptors
• Approvedforchronicinsomnia:Difficultywithsleeponset but not with sleep maintenance
• Rapid onset (about 30 min)

Question 6

BARBITURATES

Answer 6

Cause tolerance and dependence
• High abuse potential
• Multiple drug interactions
• Powerful respiratory depressants that can be fatal with overdose
• Barbiturates are used much less than they were in the past because they have been replaced by newer and safer drugs, primarily the benzodiazepines and the benzodiazepine-like drugs (such as zolpidem)

Threeclassifications
• Ultrashort-acting (thiopental)
• Short- to intermediate-acting (secobarbital)
• Long-acting (phenobarbital)
• Mechanism of action
• Binds to the GABA receptor–chloride channel complex

Drug interactions
• CNS depressants
• Interactions that result from the induction of drug-metabolizing enzymes
• Chloral hydrate
• Meprobamate

Adverse effects
• Respiratory depression
• Suicide • Abuse

Acute toxicity
• Symptoms
• Respiratory depression
• Coma
• Pinpoint pupils • Treatment
• Maintain body heat
• Support blood pressure
• Removal of barbiturate from the body: Activated charcoal
• Maintenance of an adequate oxygen supply to the brain

Question 7

DRUGS USED FOR TREATMENT OF INSOMNIA

Antidepressants

Answer 7

Trazodone [Oleptro]
• Atypical antidepressant with strong sedative actions
• Can decrease sleep latency and prolong sleep duration
• Does not cause tolerance or physical dependence
• Doxepin
• Old tricyclic antidepressant with strong sedative actions
• Used to treat patients who have trouble staying asleep