ZOLE-pi-dem

Therapeutic Classification: sedative/hypnotics

• Insomnia with difficulties in sleep initiation (generic sublingual tablets are indicated for insomnia when a middle-of-the-night awakening is followed by difficulty returning to sleep).

• Produces CNS depression by binding to GABA receptors.
• Has no analgesic properties.

• Sedation and induction of sleep.

Absorption: Rapidly absorbed following oral administration. Controlled-release formulation releases 10 mg immediately, then another 2.5 mg later.

Distribution: Unknown.

Metabolism/Excretion: Converted to inactive metabolites, which are excreted by the kidneys; clearance of sublingual tablet lower in women than in men.

Half-life: 2.5–3 hr (↑ in older adults and patients with hepatic impairment).

(sedation)

*Food delays peak levels and effects.

Contraindicated in:

• Hypersensitivity
• History of experiencing complex sleep behaviors with zolpidem
• Severe hepatic impairment (↑ risk of hepatic encephalopathy).

Use Cautiously in:

• History of previous psychiatric illness, suicide attempt, drug or alcohol abuse
• Mild or moderate hepatic impairment (↑ risk of hepatic encephalopathy; initial dose ↓ recommended)
• Pulmonary disease
• Sleep apnea
• Myasthenia gravis
• OB: May ↑ risk of respiratory depression in neonates after birth
• Lactation: May cause excess sedation in breastfed infants; use while breastfeeding only if potential maternal benefit justifies potential risk in infants
• Pedi: Safety and effectiveness not established in children
• Geri: Appears on Beers list. ↑ risk of cognitive impairment, delirium, falls, fractures, and motor vehicle accidents in older adults. Avoid use in older adults.

EENT: blurred vision, double vision.

GI: diarrhea, nausea, vomiting.

Neuro: daytime drowsiness, dizziness, abnormal thinking, agitation, amnesia, behavior changes, COMPLEX SLEEP BEHAVIORS (INCLUDING SLEEP DRIVING, SLEEP WALKING, OR ENGAGING IN OTHER ACTIVITIES WHILE SLEEPING), delirium, hallucinations, prolonged reaction time.

Resp: respiratory depression.
Misc: (INCLUDING ANAPHYLAXIS)HYPERSENSITIVITY REACTIONS , physical dependence, psychological dependence, tolerance.

Drug-Drug:

• CNS and respiratory depression may ↑ with sedatives/hypnotics, alcohol, phenothiazines, tricyclic antidepressants, opioids, or antihistamines.
• CYP3A4 inducers, including rifampin, may ↓ levels and effectiveness.
• CYP3A4 inhibitors, including ketoconazole, may ↑ levels and the risk of toxicity; consider ↓ zolpidem dose.

Drug-Natural Products:

• Concomitant use of kava-kava, valerian, or chamomile can ↑ CNS depression.
• St. John's wort may ↓ levels; avoid concurrent use

Drug-Food:

• Food↓ and delays absorption.

• PO, SL (Adults): Tablets or SL tablets (Edluar): 5 mg (for women) and 5–10 mg (for men) at bedtime; may ↑ to 10 mg at bedtime if 5-mg dose not effective; SL tablets (generic): 1.75 mg (for women) or 3.5 mg (for men) once upon awakening in the middle of the night; Extended-release tablets: 6.25 mg (for women) and 6.25–12.5 mg (for men) at bedtime; may ↑ to 12.5 mg at bedtime if 6.25-mg dose not effective.
• PO, SL (Geriatric Patients , Debilitated Patients, or Patients with Mild/Moderate Hepatic Impairment): Tablets or SL tablets (Edluar): Do not exceed dose of 5 mg at bedtime; Extended-release tablets: Do not exceed dose of 6.25 mg at bedtime.
• SL (Geriatric Patients , Patients Taking Concomitant CNS Depressants, or Patients with Mild/Moderate Hepatic Impairment): SL tablets (generic): Do not exceed dose of 1.75 mg at bedtime (in either men or women).

(Generic available)

• Immediate-release tablets: 5 mg; 10 mg;
• Immediate-release capsules: 7.5 mg;
• Extended-release tablets: 6.25 mg; 12.5 mg;
• Sublingual tablets (Edluar): 5 mg; 10 mg;
• Sublingual tablets: 1.75 mg; 3.5 mg;

• Assess mental status, sleep patterns, and potential for abuse prior to administration. Prolonged use of >7–10 days may lead to physical and psychological dependence. Limit amount of drug available to the patient.
• Assess alertness at time of peak effect. Notify health care professional if desired sedation does not occur.
• Assess patient for pain. Medicate as needed. Untreated pain decreases sedative effects.
• Monitor respiratory drive; increased risk of respiratory depression should be considered before prescribing zolpidem in patients with respiratory impairment, including sleep apnea and myasthenia gravis, or with concomitant opioid use.

• High Alert:Do not confuse zolpidem with Zyloprim.
• Before administering, reduce external stimuli and provide comfort measures to increase effectiveness of medication.
  • Protect patient from injury. Raise bed side rails. Assist with ambulation. Remove patient’s cigarettes.
  • Use lowest effective dose.
• PO: Swallow tablets whole with full glass of water. For faster onset of sleep, do not administer with or immediately after a meal.
  • DNC: Swallow extended-release tablets whole; do not crush, break, or chew.
• SL: To open the blister pack, separate the individual blisters at the perforations. Peel off top layer of paper and push tablet through foil. Place the tablet under the tongue, allow to disintegrate; do not swallow or take with water.
  • Only take if at least 4 hr left prior to time to awakening.

• Instruct patient to take zolpidem as directed. Take as a single dose and do not readminister during the same night. Advise patient not to take zolpidem unless able to stay in bed a full night (7–8 hr) before being active again. Do not take more than the amount prescribed because of the habit-forming potential. Not recommended for use longer than 7–10 days. If used for 2 wk or longer, abrupt withdrawal may result in fatigue, nausea, flushing, light-headedness, uncontrolled crying, vomiting, GI upset, panic attack, or nervousness. Instruct patient to read Patient Information for correct product before taking and with each Rx refill in case of changes.
• Because of rapid onset, advise patient to go to bed immediately after taking zolpidem.
• May cause daytime drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to this medication is known.
• Caution patient that complex sleep-related behaviors (sleep-driving) may occur while asleep.
• Advise patient to notify health care professional immediately if signs of anaphylaxis (swelling of the tongue or throat, trouble breathing, and nausea and vomiting) occur.
• Caution patient to avoid concurrent use of alcohol or other CNS depressants, including opioids.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Monitor neonates exposed to zolpidem during pregnancy and breastfeeding for signs of excess sedation, hypotonia, and respiratory depression.

• Relief of insomnia.
  • Re-evaluate insomnia after 7–10 days of therapy.

Ambien, Ambien CR, Edluar

Sublinox

Schedule IV (C-IV)