Yes

Benzodiazepine

Short-term treatment of insomnia

C-IV

X

Hypersensitivity to this drug or any component of its formulation (cross-sensitivity with other benzodiazepines may exist); narrow-angle glaucoma; pregnancy

Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), or renal impairment. Active metabolites with extended half-lives may lead to delayed accumulation and adverse effects. Use with caution in patients with respiratory disease, or impaired gag reflex. Avoid use in patients with sleep apnea.

Use caution in patients with depression, particularly if suicidal risk may be present. Use with caution in patients with a history of drug dependence. Benzodiazepines have been associated with dependence and acute withdrawal symptoms on discontinuation or reduction in dose. Acute withdrawal, including seizures, may be precipitated in patients after administration of flumazenil to patients receiving long-term benzodiazepine therapy.

As a hypnotic, should be used only after evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric or medical illness. A worsening of insomnia or the emergence of new abnormalities of thought or behavior may represent unrecognized psychiatric or medical illness and requires immediate and careful evaluation.

Benzodiazepines have been associated with anterograde amnesia. Paradoxical reactions, including hyperactive or aggressive behavior have been reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Does not have analgesic, antidepressant, or antipsychotic properties.

Cardiovascular: Palpitations, chest pain

Central nervous system: Drowsiness, ataxia, lightheadedness, memory impairment, depression, headache, hangover, confusion, nervousness, dizziness, falling, apprehension, irritability, euphoria, slurred speech, restlessness, hallucinations, paradoxical reactions, talkativeness

Dermatologic: Rash, pruritus

Gastrointestinal: Xerostomia, constipation, excessive salivation, heartburn, upset stomach, nausea, vomiting, diarrhea, increased or decreased appetite, bitter taste, weight gain or loss, increased salivation

Hematologic: Euphoria, granulocytopenia

Hepatic: Elevated SGOT/SGPT, total bilirubin, alkaline phosphatase, cholestatic jaundice

Neuromuscular & skeletal: Dysarthria, body/joint pain, reflex slowing, weakness

Ocular: Blurred vision, burning eyes, difficulty focusing

Otic: Tinnitus

Respiratory: Apnea, shortness of breath

Miscellaneous: Diaphoresis, drug dependence

Symptoms of overdose include respiratory depression, hypoactive reflexes, unsteady gait, hypotension

Treatment for benzodiazepine overdose is supportive. Rarely is mechanical ventilation required. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced CNS depression.

Carbamazepine, rifampin, rifabutin may enhance the metabolism of flurazepam and decrease its therapeutic effect; consider using an alternative sedative/hypnotic agent

Cimetidine, ciprofloxacin, clarithromycin, clozapine, CNS depressants, diltiazem, disulfiram, digoxin, erythromycin, ethanol, fluconazole, fluoxetine, fluvoxamine, grapefruit juice, isoniazid, itraconazole, ketoconazole, labetalol, levodopa, loxapine, metoprolol, metronidazole, miconazole, nefazodone, omeprazole, phenytoin, protease inhibitors like amprenavir and ritonavir, rifabutin, rifampin, troleandomycin, valproic acid, verapamil may increase the serum level and/or toxicity of flurazepam; monitor for altered benzodiazepine response

Store in light-resistant containers

Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. 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.

Onset of hypnotic effect: 15-20 minutes

Peak: 3-6 hours

Duration of action: 7-8 hours

Metabolism: In the liver to N-desalkylflurazepam (active)

Half-life: Adults: 40-114 hours

Oral:

<15 years: Dose not established

>15 years: 15 mg at bedtime

Adults: 15-30 mg at bedtime

Alcohol: Additive CNS effect, avoid use

Respiratory and cardiovascular status

Therapeutic: 0-4 ng/mL (SI: 0-9 nmol/L); Metabolite N-desalkylflurazepam: 20-110 ng/mL (SI: 43-240 nmol/L); Toxic: >0.12 mg/mL

No information available to require special precautions

>10% of patients experience dry mouth

Use exactly as directed (do not increase dose or frequency or discontinue without consulting prescriber); may cause physical and/or psychological dependence. May take with food to decrease GI upset. While using this medication, do not use alcohol or other prescription or OTC medications (especially, pain medications, sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness, dizziness, lightheadedness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); dry mouth, nausea or vomiting (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); difficulty urinating (void before taking medication); or altered libido (resolves when medication is discontinued). Report CNS changes (confusion, depression, increased sedation, excitation, headache, abnormal thinking, insomnia, or nightmares, memory impairment, impaired coordination); muscle pain or weakness; difficulty breathing; persistent dizziness, chest pain, or palpitations; alterations in normal gait; vision changes; ringing in ears; or ineffectiveness of medication. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not get pregnant during or for 1 month following therapy. Consult prescriber for instruction on appropriate barrier contraceptive measures. This drug may cause severe fetal defects. Breast-feeding is not recommended.

Provide safety measures (ie, side rails, night light, and call button); remove smoking materials from area; supervise ambulation; avoid abrupt discontinuance in patients with prolonged therapy or seizure disorders

Capsule, as hydrochloride: 15 mg, 30 mg

Maletta G, Mattox KM, and Dysken M, "Guidelines for Prescribing Psychoactive Drugs in the Elderly: Part 1," Geriatrics, 1991, 46(9):40-7.

Reidenberg MM, Levy M, Warner H, et al, "Relationship Between Diazepam Dose, Plasma Level, Age, and Central Nervous System Depression," Clin Pharmacol Ther, 1978, 23(4):371-4.

Ruff RL, Kutt H, and Hafler D, "Prolonged Benzodiazepine Coma," N Y State J Med, 1981, 81(5):776-7.

Stringer MD, "Adult Respiratory Distress Syndrome Associated With Flurazepam Overdose," J R Soc Med, 1985, 78(1)1:74-5.