Temazepam

Pronunciation

(te MAZ e pam)

U.S. Brand Names

Restoril®

Generic Available

Yes

Canadian Brand Names

Apo-Temazepam®; CO Temazepam; Gen-Temazepam; Novo-Temazepam; Nu-Temazepam; PMS-Temazepam; ratio-Temazepam; Restoril®

Use

Short-term treatment of insomnia

Use - Unlabeled/Investigational

Treatment of anxiety; adjunct in the treatment of depression; management of panic attacks

Restrictions

C-IV

Pregnancy Risk Factor

Lactation

Enters breast milk/not recommended (AAP rates "of concern")

Contraindications

Hypersensitivity to temazepam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist); narrow-angle glaucoma (not in product labeling, however, benzodiazepines are contraindicated); pregnancy

Warnings/Precautions

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.

Use with caution in elderly or debilitated patients, patients with hepatic disease (including alcoholics), or renal impairment. Use with caution in patients with respiratory disease, or impaired gag reflex. Avoid use inpatients with sleep apnea.

Causes CNS depression (dose-related) resulting in sedation, dizziness, confusion, or ataxia which may impair physical and mental capabilities. Patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). Use with caution in patients receiving other CNS depressants or psychoactive agents. Effects with other sedative drugs or ethanol may be potentiated. Benzodiazepines have been associated with falls and traumatic injury and should be used with extreme caution in patients who are at risk of these events (especially the elderly).

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 (may occur after as little as 10 days). Acute withdrawal, including seizures, may be precipitated after administration of flumazenil to patients receiving long-term benzodiazepine therapy.

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.

Adverse Reactions

1% to 10%:

Central nervous system: Confusion, dizziness, drowsiness, fatigue, anxiety, headache, lethargy, hangover, euphoria, vertigo

Dermatologic: Rash

Endocrine & metabolic: Decreased libido

Gastrointestinal: Diarrhea

Neuromuscular & skeletal: Dysarthria, weakness

Ocular: Blurred vision

Miscellaneous: Diaphoresis

<1%: Amnesia, anorexia, ataxia, back pain, blood dyscrasias, drug dependence, increased dreaming, menstrual irregularities, palpitation, paradoxical reactions, reflex slowing, tremor, vomiting

Overdosage/Toxicology

Symptoms of overdose include somnolence, confusion, coma, hypoactive reflexes, dyspnea, hypotension, slurred speech, and impaired coordination. Treatment for benzodiazepine overdose is supportive. Flumazenil has been shown to selectively block the binding of benzodiazepines to CNS receptors, resulting in a reversal of benzodiazepine-induced CNS depression but not always respiratory depression due to toxicity.

Drug Interactions

Substrate (minor) of CYP2B6, 2C8/9, 2C19, 3A4

CNS depressants: Sedative effects and/or respiratory depression may be additive with CNS depressants; includes ethanol, barbiturates, narcotic analgesics, and other sedative agents; monitor for increased effect

Theophylline: May partially antagonize some of the effects of benzodiazepines; monitor for decreased response; may require higher doses for sedation

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression).

Food: Serum levels may be increased by grapefruit juice.

Herb/Nutraceutical: St John's wort may decrease temazepam levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).

Mechanism of Action

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.

Pharmacodynamics/Kinetics

Distribution: Vd: 1.4 L/kg

Protein binding: 96%

Metabolism: Hepatic

Half-life elimination: 9.5-12.4 hours

Time to peak, serum: 2-3 hours

Excretion: Urine (80% to 90% as inactive metabolites)

Dosage

Oral:

Adults: 15-30 mg at bedtime

Elderly or debilitated patients: 15 mg

Monitoring Parameters

Respiratory and cardiovascular status

Reference Range

Therapeutic: 26 ng/mL after 24 hours

Patient Education

Use exactly as directed; do not increase dose or frequency or discontinue without consulting prescriber. Drug 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); or dry mouth or GI discomfort (small, frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report CNS changes (confusion, depression, increased sedation, excitation, headache, abnormal thinking, insomnia, or nightmares, memory impairment, impaired coordination); muscle pain or weakness; respiratory difficulty; persistent dizziness, chest pain, or palpitations; alterations in normal gait; vision changes; 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.

Nursing Implications

Provide safety measures (ie, side rails, night light, and call button); remove smoking materials from area; supervise ambulation

Additional Information

Abrupt discontinuation after sustained use (generally >10 days) may cause withdrawal symptoms.

Anesthesia and Critical Care Concerns/Other Considerations

Chronic use of this agent may increase perioperative benzodiazepine dose needed to achieve desired effect. Abrupt discontinuation after sustained use (generally >10 days) may cause withdrawal symptoms. Benzodiazepines, as a class, may depress respiration; may exacerbate sleep-disordered breathing.

Cardiovascular Considerations

Hypotension may result in orthostatic lightheadedness or syncope. Benzodiazepines, as a class, may depress respiration. These medications may often be prescribed for difficulty in sleeping but may exacerbate sleep-disordered breathing.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Significant xerostomia (normal salivary flow resumes upon discontinuation).

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Dosage Forms

Capsule: 15 mg, 30 mg

Restoril®: 7.5 mg, 15 mg, 30 mg

References

"American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk," Pediatrics , 2001, 108(3):776-89.

Divoll M, Greenblatt DJ, Harmatz JS, et al, "Effect of Age and Gender on Disposition of Temazepam," J Pharm Sci , 1981, 70(10):1104-7.

Grahame-Smith DG, "Misuse of Temazepam," Br Med J (Clin Res Ed) , 1991, 302(6786):1210.

Ho PC, Triggs EJ, Heazlewood V, et al, "Determination of Nitrazepam and Temazepam in Plasma by High Performance Liquid Chromatography," Ther Drug Monit , 1983, 5(3):303-7.

Klotz U and Kanto J, "Pharmacokinetics and Clinical Use of Flumazenil (Ro 15-1788)," Clin Pharmacokinet , 1988, 14(1):1-12.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings," Chest , 2003, 123(3):897-922.

Scharf MB, Berkowitz DV, and Brannen DE, "Effectiveness of Low-Dose Temazepam on Sleep Patterns in Geriatric Insomniac Subjects," Consult Pharm , 1993, 8(12):1367-73.

International Brand Names

Apo-Temazepam® (CA); CO Temazepam (CA); Euhypnos® (AU, BE, HK, IE, LU, NZ, TH); Euipnos® (IT); Gen-Temazepam (CA); Levanxol® (AT, BE, LU); Mabertin® (AR); Nocturne® (AU); Norkotral Tema® (DE); Normison® (AU, BE, CH, FI, FR, HK, IE, IT, LU, NL, NZ, ZA); Normitab® (NL); Nortem® (IE); Novo-Temazepam (CA); Nu-Temazepam (CA); Planum® (DE); PMS-Temazepam (CA); Pronervon T® (DE); ratio-Temazepam (CA); Remestan® (AT, DE); Restoril® (CA); Signopam® (HU, PL); Somapam® (NZ); Temador® (BE); Temaze® (AU); Temazepam® (GB); temazep von ct® (DE); Temtabs® (AU); Tenox® (FI, IE)

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