Zolpidem: uses, side effects and safety
Zolpidem (Ambien) is a nonbenzodiazepine sedative-hypnotic (imidazopyridine). It is a US Schedule IV controlled substance. It is prescription only (rx) and remains on the US market.
What is Zolpidem?
Zolpidem is the generic name for Ambien, and belongs to the Nonbenzodiazepine sedative-hypnotic (imidazopyridine) class.
| Generic name | zolpidem tartrate |
|---|---|
| Brand name(s) | Ambien |
| Drug class | Nonbenzodiazepine sedative-hypnotic (imidazopyridine) |
| US legal status | US Schedule IV · Prescription only (Rx) |
| Route | Oral |
| Prescription required | Yes |
| Elimination half-life | Mean elimination half-life 2.6 hours (range 1.4-4.5) for the 5 mg tablet and 2.5 hours (range 1.4-3.8) for the 10 mg tablet; about 2.2 hours (range 1.6-2.4) in normal subjects |
| Time to peak concentration | 1.6 (mean time to peak concentration for both 5 mg and 10 mg tablets; food delays Tmax from 1.4 to 2.2 hours) |
| Metabolism | Converted to inactive metabolites that are eliminated primarily by renal excretion; rifampin (a CYP3A4 inducer) significantly reduces exposure, and CYP3A inhibitors such as ketoconazole increase exposure |
What is Zolpidem used for?
Zolpidem is approved by the FDA for the following uses. Approval is granted per indication, and a specific product may not be approved for all of them.
- Short-term treatment of insomnia characterized by difficulties with sleep initiation
How does Zolpidem work?
Zolpidem is a GABA-A receptor positive modulator presumed to exert its therapeutic effects through binding to the benzodiazepine site of alpha-1 subunit containing GABA-A receptors, increasing the frequency of chloride channel opening.
It is metabolised primarily by Converted to inactive metabolites that are eliminated primarily by renal excretion; rifampin (a CYP3A4 inducer) significantly reduces exposure, and CYP3A inhibitors such as ketoconazole increase exposure.
The elimination half-life is roughly Mean elimination half-life 2.6 hours (range 1.4-4.5) for the 5 mg tablet and 2.5 hours (range 1.4-3.8) for the 10 mg tablet; about 2.2 hours (range 1.6-2.4) in normal subjects. Longer half-lives mean the drug and its active metabolites persist in the body for longer after the last dose.
Common side effects of Zolpidem
These are the side effects people report most often. Many diminish after the body adjusts, usually within one to two weeks.
- Short-term (up to 10 nights) most commonly observed: drowsiness, dizziness, and diarrhea
- Long-term (28 to 35 nights) most commonly observed: dizziness and drugged feelings
- Placebo-controlled trials: drowsiness 2%, dizziness 1%, diarrhea 1%, headache 7%
- Long-term trials: drowsiness 8%, dizziness 5%, lethargy 3%, drugged feeling 3%, lightheadedness 2%, depression 2%, abnormal dreams 1%, amnesia 1%, diarrhea 3%
- Next-day drowsiness, prolonged reaction time, dizziness, sleepiness, blurred/double vision, reduced alertness, and impaired driving the morning after therapy
What does Zolpidem interact with?
Interactions matter because two safe medicines can become dangerous together. The entries below are the ones most likely to cause harm.
- Alcohol and other CNS depressants: additive adverse effects on psychomotor performance
- Concomitant opioid use: risk of additive CNS and respiratory depression (Warning, not a boxed warning)
- CYP3A inhibitors such as ketoconazole increase zolpidem exposure
- CYP3A4 inducers such as rifampin, carbamazepine, and phenytoin reduce zolpidem exposure and pharmacodynamic effects
- Fluoxetine, fluvoxamine, ciprofloxacin, and other CYP inhibitors prolong elimination half-life and increase exposure
Use our drug interaction checker before combining any two prescriptions.
Serious side effects and warning signs
Seek emergency care for any of these
- Boxed warning: complex sleep behaviors including sleepwalking, sleep-driving and other complex sleep behaviors, with amnesia of the events and rarely severe injury or death
- Severe anaphylactic and anaphylactoid reactions
- Respiratory depression; impairment of consciousness ranging from somnolence to coma with fatal outcomes reported with zolpidem alone or combined with CNS depressants
- Delirium and hallucinations
- Increases the risk of falls, particularly in the elderly
- Precipitation of hepatic encephalopathy in patients with hepatic insufficiency
Suspected overdose or a bad reaction should be reported to Poison Control on 1-800-222-1222. That is staffed around the clock and is free.
Legal status of Zolpidem
Zolpidem is a Schedule IV controlled substance in the United States. That placement is set out in Title 21 of the Code of Federal Regulations, Part 1308, and enforced by the Drug Enforcement Administration. It carries restrictions on prescribing, storage, record-keeping and transfer.
Statutory reference: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d34336b1-7041-4078-beda-94bc9d9f771e.
Can you get Zolpidem without a prescription?
Short answer: no. Zolpidem is a prescription medication. Sites advertising it without one are either operating illegally or selling something other than what they claim. We explain the legal routes, the counterfeit problem and how to check a source in detail.
Read the full answer: Zolpidem without a prescription →
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What is Zolpidem used for?
Short-term treatment of insomnia characterized by difficulties with sleep initiation
What schedule is Zolpidem in the United States?
Zolpidem is a Schedule IV controlled substance in the US, listed at 21 CFR Part 1308. Schedule IV means the drug has a defined potential for abuse and is subject to federal record-keeping, storage and prescribing restrictions.
What are the common side effects of Zolpidem?
The most frequently reported side effects are short-term (up to 10 nights) most commonly observed: drowsiness, dizziness, and diarrhea, long-term (28 to 35 nights) most commonly observed: dizziness and drugged feelings, placebo-controlled trials: drowsiness 2%, dizziness 1%, diarrhea 1%, headache 7%, long-term trials: drowsiness 8%, dizziness 5%, lethargy 3%, drugged feeling 3%, lightheadedness 2%, depression 2%, abnormal dreams 1%, amnesia 1%, diarrhea 3%, next-day drowsiness, prolonged reaction time, dizziness, sleepiness, blurred/double vision, reduced alertness, and impaired driving the morning after therapy. Many lessen over the first week or two of treatment.
What should not be combined with Zolpidem?
The most clinically important interactions are with alcohol and other cns depressants: additive adverse effects on psychomotor performance, concomitant opioid use: risk of additive cns and respiratory depression (warning, not a boxed warning), cyp3a inhibitors such as ketoconazole increase zolpidem exposure, cyp3a4 inducers such as rifampin, carbamazepine, and phenytoin reduce zolpidem exposure and pharmacodynamic effects. Always give a pharmacist or prescriber a complete list of everything you take, including over-the-counter drugs and supplements.
Sources & references
Important
This site provides educational information only and does not sell, prescribe or dispense medications. Always consult a licensed healthcare provider. This page is not medical advice.