CNS Introduction, and Sedative-Hypnotic and Anxiolytic Drugs 63

TABLE 7-1. Therapeutic Summary of Selected Sedative-Hypnotic drugs

DRUGS CLINICAL APPLICATIONS ADVERSE EFFECTS CONTRAINDICATIONS

Mechanism: Allosteric agonist of GABAA receptors that increase the frequency of chloride channel opening

Short-acting benzodiazepines Triazolam Midazolam

Intermediate-acting benzodiazepines Alprazolam Estazolam Lorazepam Oxazepam Temazepam

Long-acting benzodiazipines

Chlordiazepoxide Clorazepate

Diazepam Flurazepam Prazepam Quazepam

Hypnotic (triazolam and many others)
 Amnesia induction and anesthesia (midazolam) Absence seizures (clorazepate)
 Insomn
especially alprazolam) Alcohol withdrawal (diazepam, chlordiazepoxide) Status epilepticus (diazepam, lorazepam) Muscle relax

Respiratory depression Drowsiness
 Physical and psychological

dependence Blurred vision

Hypersensitivity
 Children <6 months of age

(oral) Pregnancy

Mechanism: Enhance GABAA receptors by increasing duration of chloride channel open time

Ultrashort-acting barbiturates Thiopental Methohexital

Induction and maintenance of anesthesia
 Treatment of elevated intracranial pressure (thiopental)

Respiratory depression Cardiac depression
 CNS depression Hematologic depression

Porphyria Respiratory disease Liver disease

Intermediate-acting barbiturates Secobarbital Pentobarbital

Preanesthetic agent Same as above Same as above Short-term treatment of insomnia
 Treatment of elevated intracranial pressure

(pentobarbital)

Long-acting barbiturates Management of generalized tonic-clonic (grand mal) Same as above Same as above Phenobarbital and p
Sedative

Mechanism: BZ1 benzodiazepine agonists

Zolpidem Insomnia Drowsiness Hypersensitivity Zaleplon Drugged feeling
 Eszopiclone

Mechanism: Central H1 receptor blocker

Diphenhydramine OTC sleeping aid See chapter 20 See chapter 20 Other antihistamines

Mechanism: Selective agonist of melatonin receptors (MT1 and MT2)

Ramelteon Insomnia Drowsiness Hypersensitivity Concurrent use with

fluvoxamine

Mechanism: Partial agonist at 5-HT1A serotonin receptors in the brain

Buspirone Management of generalized anxiety disorder (GAD) Dizziness Hypersensitivity

Mechanism: Benzodiazepine antagonist

Flumazenil Reverse benzodiazepine effects in conscious sedation and general anesthesia

Treatment of benzodiazepine overdose

GI distress CNS agitation Seizures

Serious tricyclic- antidepressant overdoses

Seizure disorders

CNS, central nervous system; GABA, g-aminobutyric acid; GI, gastrointestinal; OTC, over the counter