Zolpidem

Ambien, Edluar and archived Zolpimist labeling address short-term sleep-initiation insomnia in adults. Ambien CR addresses sleep onset and/or maintenance. The 1.75/3.5 mg sublingual product treats difficulty returning to sleep after middle-of-night awakening, only when at least 4 hours of bedtime remain.

Ambien CR must be swallowed whole, without dividing, crushing or chewing. Place low-dose SL under the tongue until fully dissolved, then swallow; remove from pouch immediately before use. Edluar goes under the tongue, without water or swallowing the tablet whole. Food can delay effect. Archived Zolpimist: first-use priming is 5 sprays away from people; hold upright and spray over the tongue into the mouth. The archived full PI says 1 re-priming spray after ≥14 days without use, but its appended patient instructions imply 5 sprays. This conflict requires pharmacist review of the exact package instructions; do not use this profile to choose a re-priming count.

Ambien/CR: elderly or debilitated patients and mild/moderate hepatic impairment use 5 mg IR or 6.25 mg CR; avoid severe hepatic impairment because of encephalopathy. Renal impairment does not require adjustment in the reviewed pharmacokinetic data, but assess clinical vulnerability. Ambien long-term use is not recommended; Ambien/CR treatment should be as short as possible, with re-evaluation before extension. Older SL/Edluar/spray hepatic wording is product-specific and does not establish safety in severe liver disease.

Prior complex sleep behaviors following zolpidem and known zolpidem hypersensitivity, including anaphylaxis/angioedema. Do not rechallenge after zolpidem-associated angioedema.

Sleepwalking, sleep-driving and other activities without full wakefulness may occur with the first or later dose, at recommended doses, with or without alcohol/other sedatives. Serious injuries and deaths are reported. Discontinue immediately if a complex sleep behavior occurs.

Drowsiness, dizziness, diarrhea and drugged feelings occur with IR; headache, dizziness and next-day somnolence are prominent with CR. Low-dose SL trials report headache, nausea and fatigue. Overdose may cause coma, respiratory/cardiovascular compromise and death; obtain emergency/poison-center care. Supportive monitoring is required; flumazenil may provoke seizures and is a specialist decision.

• Alcohol, benzodiazepines, sedating antidepressants and other CNS depressants increase impairment. Avoid alcohol; review need for lower doses. Other zolpidem/sedative-hypnotic products are not recommended together.
• Opioids raise respiratory-depression risk: limit concomitant dosage and duration.
• Ambien labeling does not recommend rifampin or St. John’s wort because efficacy may decrease.
• Potent CYP3A4 inhibitors such as ketoconazole increase exposure/effect; consider a lower zolpidem dose. Sertraline increases exposure; review clinical effects.

Late-pregnancy exposure can cause neonatal sedation, hypotonia and respiratory depression; monitor exposed neonates. Human data have not shown a clear major-malformation association, but do not establish absence of risk. Zolpidem enters milk; monitor breastfed infants for sedation, poor tone and breathing problems. Ambien/CR labels permit considering interruption with pumping/discarding during treatment and for 23 hours after a dose; plan feeding with the clinician. Older SL/spray labels contain legacy pregnancy wording.

Under 18: use is not recommended; effectiveness was not established in the pediatric insomnia trial. Older/debilitated adults need reduced product-specific doses and fall monitoring. Women clear zolpidem more slowly, supporting lower initial doses. Review renal illness and drug burden despite no label renal adjustment; severe hepatic impairment should be avoided with Ambien/CR.

Zolpidem enhances GABA-A receptor activity, predominantly at α1-containing receptors, inhibiting neuronal excitation. Ambien IR mean peak time is about 1.6 hours and half-life 2.5–2.6 hours in healthy subjects. It forms inactive metabolites excreted mainly in urine. Women, older adults and hepatic impairment can have greater exposure. CR prolongs absorption; low-dose SL and Edluar have their own exposure profiles.

IR protein binding

About 92.5%.

Hepatic impairment

Markedly prolonged elimination; do not infer safety from healthy half-life.

Renal dialysis

Zolpidem was not hemodialyzable in reviewed studies.

• Assess cause and pattern of insomnia, response, daytime function, falls, breathing risk and depression/suicidality.
• Review sedatives/alcohol, dose escalation, refill patterns and dependence; reassess before extending therapy.
• Ask specifically about unremembered nighttime activities and stop immediately if they occur.

Take only the prescribed formulation and dose. Do not add another sleep medicine or alcohol. Bedtime products require 7–8 hours before waking; the low-dose middle-of-night product requires ≥4 hours and is not an extra bedtime dose. Do not drive while impaired; CR has a specific next-day driving caution. Secure the Schedule IV medicine and never share it. Discuss a supervised plan before stopping regular use.

Appearance / imprint

Pink, capsule-shaped film-coated tablet; AMB 5 / 5401.

Manufacturer

Sanofi.

Example NDC

0024-5401-31 · bottle of 100.

U.S. status

Prescription · Schedule IV.

Ambien / Ambien CR

IR 5/10 mg oral tablets; CR 6.25/12.5 mg oral tablets.

Sublingual products

Low-dose 1.75/3.5 mg for middle-of-night use; Edluar 5/10 mg for bedtime.

Archived Zolpimist

5 mg per 100 microliter oral spray; official label lists marketing end May 31, 2023.

Ambien: 20–25°C. CR: 15–25°C with limited excursions to 30°C. Low-dose SL: 20–25°C, excursions 15–30°C; protect from moisture and retain pouch until use. Edluar: 20–25°C, light/moisture protection. Archived spray: upright at 25°C, excursions 15–30°C, do not freeze; discard after labeled 30 or 60 sprays according to bottle.