焦慮、失眠、肌肉痙攣、癲癇重積狀態
Acute alcohol withdrawal syndrome; Anxiety; Muscle spasm; Status epilepticus
藥理
Anticonvulsant, Benzodiazepine
Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system. Enhancement of the inhibitory effect of GABA on neuronal excitability results by increased neuronal membrane permeability to chloride ions. This shift in chloride ions results in hyperpolarization (a less excitable state) and stabilization. Benzodiazepine receptors and effects appear to be linked to the GABA-A receptors. Benzodiazepines do not bind to GABA-B receptors.
藥動學
Onset of action:
1. Sedation: (Pediatric) 4-5 minutes
2. Status epilepticus: 1-3 minutesz Duration of action:
1. Sedation: (Pediatric) 60-120 minutes
2. Status epilepticus: 15-30 minutes Distribution:
Vd: 1.2 L/kg (range: 0.6 to 2 L/kg) Metabolism:
Hepatic; diazepam is N-demethylated by CYP3A4 and 2C19 to the active metabolite N-desmethyldiazepam, and is hydroxylated by CYP3A4 to the active metabolite temazepam. N-desmethyldiazepam and temazepam are both further metabolized to oxazepam. Excretion:
Urine (predominantly as glucuronide conjugates)
Anxiety:
1. Anxiety, acute/severe: 2-10 mg every 3-6 hours as needed up to 40 mg/day
2. Anxiety disorders: Initial 2-5 mg once or twice daily; increase gradually up to 40 mg/day in 2-4 divided doses Seizure:
Initial 5-10 mg every 10-15 minutes; increase gradually up to a total dose of 30mg Muscle spasm:
Initial 5-10 mg every 3-4 hours (if necessary)
小兒調整劑量
腎功能調整劑量
1. Kidney Impairment: There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
2. Hemodialysis: Not dialyzable (0% to 5%); supplemental dose is not necessary.
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling; use with caution because distribution and half-life may increase, and clearance may decrease significantly.
安定性
Do not mix IV product with other medications. To administer directly IV, inject slowly through infusion tubing as close as possible to the vein insertion.