Pharmacologic Class: Benzodiazepine; GABAA receptor agonist
ACTIONS AND USES: Diazepam binds to the GABA receptor–chloride channels throughout the CNS. It produces its effects by suppressing neuronal activity in the limbic system and subsequent impulses that might be transmitted to the reticular activating system. Effects of this drug are suppression of abnormal neuronal foci that may cause seizures, calming without strong sedation, and skeletal muscle relaxation. When used orally, maximum therapeutic effects may take from 1 to 2 weeks. Tolerance may develop after about 4 weeks. When given IV, effects occur in minutes, and its anticonvulsant effects last about 20 minutes.
ADMINISTRATION ALERTS: When administering IV, monitor respirations every 5 to 15 minutes. Have airway and resuscitative equipment accessible. The drug is pregnancy category D.
ADVERSE EFFECTS: Because of tolerance and dependency, use of diazepam is reserved for short term seizure control or for status epilepticus. When given IV, hypotension, muscular weakness, tachycardia, and respiratory depression are common.
Contraindications: When administered in injectable form, this medication should be avoided under the following conditions: shock, coma, depressed vital signs, obstetrical patients, and infants less than 30 days of age. In tablet form, the medication should not be administered to infants less than 6 months of age, to patients with acute narrow-angle glaucoma or untreated open-angle glaucoma, or within 14 days of monoamine oxidase inhibitor (MAOI) therapy.
INTERACTIONS: Drug–Drug: Diazepam should not be taken with alcohol or other CNS depressants because of combined sedation effects. Other drug interactions include cimetidine, oral contraceptives, valproic acid, and metoprolol, which potentiate diazepam’s action; and levodopa and barbiturates, which decrease diazepam’s action. Diazepam increases the levels of phenytoin in the bloodstream and may cause phenytoin toxicity.
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