ZOLPIDEM

(zol'-pi-dem)

Ambien, Ambien CR, Tovalt ODT
Classifications: anxiolytic; sedative-hypnotic, non-benzodiazepine;
Therapeutic: sedative-hypnotic; antianxiety
Pregnancy Category: C
Controlled Substance: Schedule IV

Availability

5 mg, 10 mg tablets; 6.25 mg, 12.5 mg extended release tablets; 5 mg, 10 mg orally disintegrating tablets

Action

An agonist that binds to the BZD1 subunit on the gamma-aminobutyric acid (GABA)-A receptor chloride channel, thus inhibiting the action potential.

Therapeutic Effect

Sedative, anticonvulsant, and antianxiety effects thought to be due to GABA-A agonism.

Uses

Short-term treatment of insomnia.

Contraindications

Suicidal ideation; labor or obstetric delivery; pregnancy (category C), children <18 y.

Cautious Use

Depressed patients, hepatic/renal impairment, older adults, alcohol or drug abuse; patients with compromised respiratory status, COPD, sleep apnea; chronic depression.

Route & Dosage

Short-Term Treatment of Insomnia
Adult: PO 10 mg (immediate release/ODT) OR 12.5 mg (extended release) at bedtime
Geriatric: PO 5 mg (immediate release) or 6.25 mg (extended release) at bedtime

Hepatic Impairment
5 mg (immediate release) or 6.25 mg (extended release) at bedtime

Administration

Oral

Give immediately before bedtime; for more rapid sleep onset, do NOT give with or immediately after a meal.
Extended release tablets should be swallowed whole. Ensure that they are not crushed or chewed.
Use reduced dosage of 5 mg in older adult or debilitated patients.
Store at room temperature, 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

CNS: Headache on awakening, drowsiness or fatigue, lethargy, drugged feeling, depression, anxiety, irritability, dizziness, double vision. Confusion and falls reported in elderly. Doses >10 mg may be associated with anterograde amnesia or memory impairment. GI: Dyspepsia, nausea, vomiting. Other: Myalgia.

Interactions

Drug: cns depressants, alcohol, phenothiazines by augmenting CNS depression. Food: Extent and rate of absorption of zolpidem are significantly decreased.

Pharmacokinetics

Absorption: Readily from GI tract. 70% reaches systemic circulation. Food decreases rate and extent of absorption. Onset: 7–27 min. Peak: 0.5–2.3 h. Duration: 6–8 h. Distribution: Highly protein bound. Lowest concentrations in CNS, highest concentrations in glandular tissue and fat. Crosses placenta, very small amounts (<0.02%) distributed into breast milk. Metabolism: In the liver to 3 inactive metabolites. Elimination: 79–96% of dose appears as metabolites in the bile, urine, and feces. Half-Life: 1.7–2.5 h.

Nursing Implications

Assessment & Drug Effects

Assess respiratory function in patients with compromised respiratory status. Report immediately to physician significantly depressed respiratory rate (<12/min).
Monitor patients for S&S of depression (see Appendix F); zolpidem may increase level of depression.
Monitor older adult or debilitated patients closely for impaired cognitive or motor function and unusual sensitivity to the drug's effects.

Patient & Family Education

Avoid taking alcohol or other CNS depressants while on zolpidem.
Do not drive or engage in other potentially hazardous activities until response to drug is known.
Report vision changes to physician.
Note: Onset of drug is more rapid when taken on an empty stomach.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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