flurazepam DALMANE

Class: Benzodiazepine
FDA Indications: Insomnia
Off-Label Use:
Prescribing
FDA Schedule IV
Forms: 15, 30mg capsule
Dose Range: 15-60 mg/day
Starting: 15-30 mg qhs

NAMI drug fact sheet

Precautions
Contraindications: Acute narrow angle glaucoma, sleep apnea
Serious Side Effects: "Sleep-Driving" and other complex behavior. Overdose can result in hypotension, respiratory depression, and coma
Side Effects: sedation/somnolence, dizziness, ataxia, lightheadedness, falls
Pharmacodynamics
1° MOA: GABAAR PAM
Target: GABAA: α1 (low to moderate), α3 (moderate)
Pharmacokinetics
t½: TMAX: 0.5-1°
Absorption Rate: Fast
Lipid Solubility: High
Substrate of: 3A4
Inhibits: ∅ ; Induces:
Active Metabolites: Hydroxyethylflurazepam (t½ 2-4°) and desalkylflurazepam (t½ 40-250°)
DDIs
Misc
  • - rapid sedative effects (w/in 15-20 min) d/t parent drug's rapid absorption from GI tract, with an intermediate metabolite (hydroxyethylflurazepam) to sustain sleep, & a long-acting metabolite (desalkylflurazepam) that minimizes early morning awakening
  • - slow accumulate of desalkylflurazepam (t½ 40-250°) can cause morning-after cognitive impairment
  • - the 1st benzodiazepine specifically marketed for insomnia—highly successful, especially competing against the major sedative-hypnotics of the 1970s i.e. glutethimide, ethchlorvynol, methaqualone
Special Populations

Category D—Limited reports describing the use of flurazepam in human pregnancy have been located. The effects of this drug on the fetus should be similar to other benzodiazepines, including the risk of malformations after exposure in the 1st trimester. Maternal use near delivery may cause a syndrome of hypothermia, hypotonia, respiratory depression, withdrawal, and difficulty feeding. The manufacturer classifies flurazepam as contraindicated in pregnancy.

Low incidence of infant toxicity and AEs associated with benzodiazepine use during breastfeeding. Benzodiazepines with shorter half-lives (i.e., lorazepam, alprazolam, and oxazepam) have been found to be very low in breast milk

In most elderly patients, the slow accumulate of the desalkyl metabolites causes a morning-after cognitive impairment

Renal insufficiency has a quantitatively small influence on pharmacokinetics; no dosage adjustments provided in the manufacturer's labeling

T½ ↑ ≈ 73% in patients with alcohol liver disease

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Last updated January 22 2018 19:18:05. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.