Sedative, Hypnotic, Anxiolytic Use Disorders Medication

Updated: Feb 10, 2017
  • Author: Stephen P Erlach, JD, MD; Chief Editor: Randon S Welton, MD  more...
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Medication

Medication Summary

A variety of drugs are used both in the acute and the long-term setting for the treatment of sedative, hypnotic, and anxiolytic use disorders. Drug selection depends upon whether toxicity or withdrawal symptoms are being targeted.

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Benzodiazepines

Class Summary

In dependent patients, these are used in a manner similar to phenobarbital to wean patients from short-acting benzodiazepines. The general principle is that sedatives with longer half-lives have less severe withdrawal symptoms. Various patient-specific dosing strategies are used. If symptoms are severe enough to require inpatient treatment, IV lorazepam or diazepam is used.

Diazepam (Valium, Diastat Acudial)

Depresses all levels of CNS (eg, limbic, reticular formation), possibly by increasing activity of GABA. Individualize the dosage and increase cautiously to avoid adverse effects.

Lorazepam (Ativan)

Sedative-hypnotic with short onset of effects and relatively long half-life.

By increasing the action of GABA, which is the major inhibitory neurotransmitter in the brain, may depress all levels of CNS, including limbic and reticular formation.

Important to monitor patient's blood pressure after administering dose. Adjust dose as necessary.

Clonazepam (Klonopin)

Suppresses muscle contractions by facilitating neurotransmission of GABA and other inhibitory transmitters.

Chlordiazepoxide

Has a wide therapeutic window and is “self-tapering” because of its long half-life. Longer acting than diazepam and lorazepam and thus is more commonly used, especially in outpatient tapers.

Temazepam (Restoril)

Temazepam is a short- to intermediate-acting benzodiazepine with longer latency to onset and half-life. It depresses all levels of the CNS (eg, limbic and reticular formation), possibly by increasing activity of GABA.

Oxazepam

Binds to benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system. This causes an increase in the inhibitory activity of GABA on neuronal excitability, which in turn makes the neuronal membranes less excitable and more stable.

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Benzodiazepine antagonist

Class Summary

These agents are used in reversing the CNS depressant effects of benzodiazepine overdose. Its ability to reverse the benzodiazepine-induced respiratory depression is difficult to predict.

Flumazenil

This benzodiazepine antagonist has a high affinity for the benzodiazepine receptor, making it a competitive antagonist. Flumazenil is short-acting, with a half-life of 0.7-1.3 h. Because most benzodiazepines have longer half-lives, multiple doses of flumazenil may be required to avoid relapse back into a sedative state. However, it is not typically used due to the fact that the risks of inducing life-threatening withdrawal in chronic users outweighs the potential benefits.

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Barbiturates

Class Summary

These agents are used in some cases to facilitate smooth withdrawals in patients with benzodiazepine and barbiturate dependence.

Phenobarbital

Chosen for withdrawal because of long half-life and wide therapeutic index. General principle is that sedatives with longer half-lives have less severe withdrawal symptoms. Since there is no reversal agent and these agents can accumulate in the system due to their long half-lives, this class is less favored in general.

Pentobarbital (Nembutal)

Pentobarbital is a short-acting barbiturate that interferes with transmission of impulses from the thalamus to the cortex. It has sedative, hypnotic, and anticonvulsant properties. It is a second-line drug for treatment of drug-induced seizures.

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Anticonvulsants, Other

Class Summary

Some agents in this class have been used successfully in the treatment of mild sedative-hypnotic withdrawal.

Carbamazepine (Carbatrol, Tegretol, Epitol)

Carbamazepine is a sodium-channel blocker that typically provides substantial or complete relief of pain. It reduces sustained high-frequency repetitive neural firing and is a potent enzyme inducer that can induce own metabolism. Initially used as an antiseizure medication and mood stabilizer, carbamazepine is also used for explosive outbursts. Carbamazepine is metabolized in the liver to its active metabolite (ie, epoxide derivative) with a half-life of 5-8 hours.

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