Trade Names:Doral- Tablets 7.5 mg- Tablets 15 mg
Potentiates action of GABA, an inhibitory neurotransmitter, resulting in increased neuronal inhibition and CNS depression, especially in limbic system and reticular formation.
Well absorbed from GI tract. The t ½ is 30 min; C max is about 20 ng/mL; T max is about 2 h.
Protein binding is 95%. Quazepam is present in breast milk (less than 0.1% of dose).
It is extensively metabolized in the liver to 2 active metabolites, 2-oxoquazepam and N-desalkyl-2-oxoquazepam.
Eliminated in the urine (31%) and feces (23%) as trace amounts of unchanged drug. The t ½ for parent and 2-oxoquazepam is 39 h and 73 h for N-desalkyl-2-oxoquazepam.
The potential for excessive sedation or impaired coordination exists.Elderly
Elimination t ½ of N-desalkyl-2-oxoquazepam is increased 2-fold that of young adults.Alcoholism
The potential for excessive sedation or impaired coordination exists.
Short-term management of insomnia.
Hypersensitivity to benzodiazepines; pregnancy; sleep apnea.
PO 15 mg at bedtime initially; may reduce to 7.5 mg once individual response is determined. Administer 30 min to 1 h before bedtime with full glass of water. If GI upset occurs, administer with snack.Elderly or debilitated patients
Attempt dosage reduction after 1 to 2 nights.
May cause additive CNS depressant effects.Cimetidine, disulfiram, omeprazole
May increase quazepam effects.Digoxin
May increase serum digoxin concentrations.Theophylline
May antagonize sedative effects.
None well documented.
Daytime drowsiness; dizziness; lethargy; confusion; memory impairment; euphoria; relaxed feeling; falling; ataxia; hallucinations; paradoxical reactions (eg, anger, hostility, mania); headache.
Blurred vision; difficulty focusing.
Anorexia; diarrhea; abdominal cramping; constipation; nausea and vomiting.
Hepatic function impairment.
Tolerance; physical and psychological dependence; weakness; slurred speech.
Category X .
Excreted in breast milk.
Contraindicated in children younger than 18 yr of age.
Use drug with caution in patients with renal or hepatic function impairment, depression or suicidal tendencies, drug abuse and dependence, chronic pulmonary insufficiency, seizure disorders.
Prolonged use can lead to psychologic or physical dependence. Withdrawal syndrome may occur; dose must be tapered gradually.
Somnolence, confusion with reduced or absent reflexes, respiratory depression, apnea, hypotension, impaired coordination, slurred speech, seizures, coma.
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