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flurazepam (Dalmane)
Tradename: Dalmane. DEA-controlled substance: class 4.
Indications: short-term management of insomnia
Contraindications:
1) pregnancy
2) pre-existing CNS depression
3) respiratory depression
4) narrow-angle glaucoma
Caution:
1) use with caution in patients receiving other CNS depressants
2) safety in children not yet established
Dosage: 15-30 mg PO QHS [1,2].
Tabs: 15, 30 mg.
Pharmacokinetics:
1) prodrug for active metabolite desalkylflurazepam
2) t1/2 of 74 +/- 24 hours for active metabolite
Adverse effects:
1) common (> 10%)
- drowsiness, fatigue, impaired coordination, lightheadedness, memory impairment, insomnia, dysarthria, anxiety, decreased libido, depression, headache, dry mouth, constipation, decreased salivation, nausea/vomiting, diarrhea, tachycardia, chest pain, blurred vision, sweating, rash, increased or decreased appetite
2) less common (1-10%)
- confusion, nervousness, syncope, dizziness, akathisia, hypotension, rigidity, tremor, dermatitis, nasal congestion, weight gain or weight loss, increased salivation, hyperventilation, tinnitus, muscle cramps
3) uncommon (< 1%)
- muscle irregularities, blood dyscrasias, reflex slowing, dependence
Drug interactions:
1) additive effects with other CNS depressants
2) carbamazepine may increase hepatic metabolism
3) agents which decrease hepatic metabolism of flurazepam
a) cimetidine
b) estrogens
c) disulfiram
d) erythromycin
Laboratory:
1) specimen: serum, plasma (EDTA)
2) methods: GC, HPLC, RIA
3) labs with Loincs
- flurazepam in specimen
- flurazepam in hair
- flurazepam in tissue
- flurazepam in body fluid
- flurazepam in gastric fluid
- flurazepam in stool
- flurazepam in meconium
- flurazepam in blood
- flurazepam in serum/plasma
- flurazepam in urine
- flurazepam in vitreous fluid
Mechanism of action: benzodiazepine
Interactions
drug interactions
drug adverse effects (more general classes)
Specific
N-desalkylflurazepam
General
benzodiazepine
Properties
MISC-INFO: elimination route KIDNEY
1/2life 50-100 HOURS
toxic-range >0.2 UG/ML
protein-binding 96-98%
elimination by hemodialysis -
pregnancy-category X
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996.
- Manual of Medical Therapeutics, 28th ed, Ewald &
McKenzie (eds), Little, Brown & Co, Boston, 1995,
pg 7
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995