Zolpidem (12.5mg) is an extended-release (ER) formulation of a non-benzodiazepine hypnotic agent, specifically a Z-drug, used for the short-term treatment of insomnia characterized by difficulties with sleep maintenance. The 12.5mg ER tablet is designed to release the drug in two phases: an initial dose for sleep onset and a delayed release for sleep maintenance. It is a Schedule H1 drug in India, indicating high potential for abuse and dependence, requiring special prescription monitoring.
Adult: 12.5 mg orally once daily immediately before bedtime. Must ensure a full 7-8 hours dedicated to sleep before being active.
Note: Take ONE tablet IMMEDIATELY BEFORE GOING TO BED. Do not take with or immediately after a meal. Swallow whole; do not crush, split, or chew the extended-release tablet. Must be taken only when the patient can dedicate a full 7-8 hours to uninterrupted sleep. Do not re-dose during the same night.
Zolpidem is a selective agonist at the benzodiazepine-1 (BZ1 or ω1) receptor subtype, which is a part of the GABA-A receptor-chloride ion channel macromolecular complex. This selective binding potentiates the inhibitory effects of GABA (gamma-aminobutyric acid), leading to neuronal hyperpolarization and reduced neuronal excitability.
Pregnancy: Category C: Animal studies have shown adverse effects. There are no adequate and well-controlled studies in pregnant women. Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Avoid, especially during the first trimester and near term (risk of neonatal flaccidity and withdrawal symptoms).
Driving: STRICTLY NOT ADVISED the morning after ingestion until the individual is sure they are not experiencing any residual sedation or impaired alertness. The drug can impair cognitive and motor functions for hours after waking. Label carries a specific warning against driving or operating machinery.
| Alcohol | Profoundly increases CNS depression, psychomotor impairment, risk of complex sleep behaviors, and respiratory depression. | Contraindicated |
| Other CNS Depressants (e.g., Opioids, Benzodiazepines, Barbiturates, Sedating Antihistamines) | Additive CNS depression, increased risk of sedation, respiratory depression, and death. | Major |
| CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir) | Increase Zolpidem plasma levels, leading to enhanced and prolonged sedative effects and toxicity. | Major |
| CYP3A4 Inducers (e.g., Rifampicin, Carbamazepine, Phenytoin, St. John's Wort) | Decrease Zolpidem plasma levels, potentially reducing efficacy. | Moderate |
| SSRIs (e.g., Sertraline, Fluoxetine) | Potential pharmacodynamic interaction increasing CNS effects; some SSRIs may inhibit metabolism. | Moderate |
| Sodium Oxybate | Profound CNS and respiratory depression. | Contraindicated |
Same composition (Zolpidem (12.5mg)), different brands: