Flurazepam Hydrochloride

Trade Names:Flurazepam Hydrochloride- Capsules 15 mg- Capsules 30 mg

Pharmacology

Potentiates action of gamma-aminobutyric acid, an inhibitory neurotransmitter, resulting in increased neural inhibition and CNS depression, especially in limbic system and reticular formation.

Pharmacokinetics

Absorption

T _max is 0.5 to 1 h (parent) and 7.6 to 13.6 h (active metabolite). It is rapidly and completely absorbed.

Distribution

Protein binding is 97%. Flurazepam crosses the placenta and is secreted into breast milk. It has a high lipid:water distribution coefficient in the nonionized form.

Metabolism

The major metabolite is N-desalkylflurazepam (active).

Elimination

The t _{1/ 2} is 2 to 3 h and 47 to 100 h for the active metabolite. Less than 1% is excreted unchanged in the urine.

Indications and Usage

Treatment of insomnia.

Contraindications

Hypersensitivity to benzodiazepines; pregnancy.

Dosage and Administration

PO 15 to 30 mg at bedtime.

PO 15 mg until individual response is determined.

PO 15 mg until individual response is determined.

Storage/Stability

Store at room temperature in light-resistant container.

Drug Interactions

Additive CNS depressant effects; may continue several days after discontinuation.

Increased effects of flurazepam.

Serum digoxin concentrations may increase.

Serum concentrations may be increased.

Decreased effects of flurazepam.

May antagonize sedative effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations; chest pains; tachycardia; hypotension (rare).

CNS

Dizziness; drowsiness; lightheadedness; staggering; ataxia; falling; lethargy; confusion; impaired memory; headache; weakness; paradoxical excitement; talkativeness; euphoria; apprehension; irritability; hallucinations; slurred speech; depression.

Dermatologic

Pruritus; rash.

EENT

Difficulty focusing; blurred vision; burning of eyes; taste alterations.

GI

Heartburn; nausea and vomiting; diarrhea; constipation; anorexia; upset stomach; GI pain; dry mouth.

Genitourinary

Urinary incontinence; urinary retention, hesitancy, or urgency.

Hematologic

Leukopenia; granulocytopenia.

Hepatic

Elevated AST, ALT, bilirubin and alkaline phosphatase; hepatitis.

Respiratory

Shortness of breath.

Miscellaneous

Tolerance; physical and psychological dependence; body and joint pains; sweating; flushing.

Precautions

Pregnancy

Contraindicated.

Lactation

Excreted in breast milk.

Children

Not recommended in children younger than 15 yr of age.

Elderly

Increased adverse reactions; start with lowest dose.

Renal Function

Use with caution. Abnormal LFTs and blood dyscrasias have occurred.

Hepatic Function

Use with caution. Abnormal LFTs and blood dyscrasias have occurred.

Debilitated patients

Increased adverse reactions; start with lowest dose.

Anterograde amnesia

Has occurred with similar drugs. Alcohol may increase risk.

Depression

Administer with caution to severely depressed patients or those with suicidal tendencies. Signs and symptoms of depression may be intensified.

Withdrawal

Withdrawal symptoms may occur after discontinuation of higher doses taken over long periods.

Overdosage

Symptoms

Somnolence, confusion, respiratory depression, apnea, hypotension, impaired coordination, slurred speech, seizures, coma.

Patient Information

• Caution patient that this medication must not be taken during pregnancy or when pregnancy is possible. Advise patient to use reliable form of birth control while taking this drug.
• Tell patient to take drug with full glass of water at bedtime.
• Emphasize importance of not exceeding recommended dosage. If symptoms do not improve within 2 to 3 days of beginning drug therapy, or if tolerance develops, notify health care provider.
• Tell patient not to stop taking drug abruptly to avoid withdrawal symptoms. Explain that nighttime sleep may be disturbed for 1 to 2 nights after gradual discontinuation.
• Instruct patient to monitor weight and to report any excessive gain or loss.
• Advise patient to report the following symptoms to health care provider: palpitations or chest pain, signs of bleeding, abdominal pain, jaundice, shortness of breath, rash, confusion, dizziness, nausea, vomiting.
• Instruct patient to take sips of water frequently, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Advise patient to avoid intake of alcoholic beverages or other CNS depressants.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

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