No

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); concurrent therapy with CYP3A4 inhibitors (such as ketoconazole, itraconazole, protease inhibitors and nefazodone); pregnancy

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.

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 (ie, 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. Acute withdrawal, including seizures, may be precipitated after administration of flumazenil to patients receiving long-term benzodiazepine therapy.

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.

>10%: Central nervous system: Drowsiness

1% to 10%:

Central nervous system: Headache, dizziness, nervousness, lightheadedness, ataxia

Gastrointestinal: Nausea, vomiting

<1%: Tachycardia, euphoria, fatigue, confusion, depression, memory impairment, visual disturbance, pain, cramps

Symptoms of overdose include somnolence, confusion, coma, diminished reflexes, dyspnea, and 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 but not always respiratory depression.

CYP3A3/4 and 3A5-7 enzyme substrate

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, rifabutin, rifampin, troleandomycin, valproic acid, protease inhibitors like amprenavir and ritonavir, verapamil may increase the serum level and/or toxicity of triazolam; monitor for altered benzodiazepine response

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: Within 15-30 minutes

Duration: 6-7 hours

Distribution: V_d: 0.8-1.8 L/kg

Protein binding: 89%

Metabolism: Extensively in the liver

Half-life: 1.7-5 hours

Elimination: In urine as unchanged drug and metabolites

Onset of action is rapid, patient should be in bed when taking medication

Children <18 years: Dosage not established

Adults: 0.125-0.25 mg at bedtime

Dosing adjustment/comments in hepatic impairment: Reduce dose or avoid use in cirrhosis

Alcohol: Additive CNS effect, avoid use

Respiratory and cardiovascular status

No information available to require special precautions

No effects or complications reported

Take exactly as directed (do not increase dose or frequency); may take 2-3 weeks to achieve desired results; may cause physical and/or psychological dependence. Do not use excessive 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, lightheadedness, impaired coordination, dizziness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); nausea, vomiting, or dry mouth (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); constipation (increased exercise, fluids, or dietary fruit and fiber may help); altered sexual drive or ability (reversible); or photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). Report persistent CNS effects (eg, memory impairment, confusion, depression, increased sedation, excitation, headache, agitation, insomnia or nightmares, dizziness, fatigue, impaired coordination, changes in personality, or changes in cognition); changes in urinary pattern; muscle cramping, weakness, tremors, or rigidity; ringing in ears or visual disturbances; chest pain, palpitations, or rapid heartbeat; excessive perspiration; excessive GI symptoms (cramping, constipation, vomiting, anorexia); or worsening of condition. 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 contraceptive measures. This drug may cause severe fetal defects. Breast-feeding is not recommended.

Patients may require assistance with ambulation; lower doses in the elderly are usually effective; institute safety measures

Tablet: 0.125 mg, 0.25 mg

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