Zolpidem (Oromucosal, Sublingual)

Generic name: Zolpidem

Drug class: Non-benzodiazepine hypnotic

Dosage form: Sublingual tablets, oral spray

Route of administration: Sublingual (under the tongue), oromucosal (oral spray)

Dose:

• Adults:
• Sublingual tablets: 5 mg for women; 5 mg or 10 mg for men, taken once at bedtime. Maximum dose: 10 mg per day.
• Oral spray: 10 mg (2 sprays) taken once at bedtime. For older adults, 5 mg (1 spray) is recommended.
• Older adults:
• Sublingual tablets: 5 mg for both men and women, taken once at bedtime.
• Oral spray: 5 mg (1 spray) taken once at bedtime.
• Children: Use and dose must be determined by a doctor; not recommended for children.

Mechanism of action: Zolpidem enhances the activity of gamma-aminobutyric acid (GABA) at GABA_A receptors in the brain, leading to sedative and hypnotic effects that facilitate sleep initiation and maintenance.

Drug usage cases:

• Short-term treatment of insomnia characterized by difficulties with sleep initiation.
• Management of sleep disturbances associated with middle-of-the-night awakenings (e.g., Intermezzo® formulation).

Drug contraindications:

• Hypersensitivity to zolpidem or any component of the formulation.
• Severe hepatic impairment (Child-Pugh class C).
• History of complex sleep behaviors (e.g., sleepwalking, sleep driving) after taking zolpidem.
• Obstructive sleep apnea syndrome.
• Myasthenia gravis.
• Acute or severe respiratory depression.

Side effects:

• Common: Drowsiness, dizziness, headache, nausea, diarrhea.
• Serious: Allergic reactions (e.g., rash, itching, swelling of face or throat), memory problems, hallucinations, complex sleep behaviors (e.g., sleepwalking, sleep driving), mood changes (e.g., depression, anxiety, irritability), impaired coordination, visual disturbances (e.g., blurred vision, double vision), next-day drowsiness or impaired alertness.

Warnings:

• Risk of next-day drowsiness or impaired alertness; avoid activities requiring full alertness until the effects are known.
• Potential for complex sleep behaviors; monitor for unusual sleep-related activities.
• Use caution in patients with a history of depression, psychiatric disorders, or substance abuse.
• Concomitant use with alcohol or other central nervous system depressants may increase the risk of serious side effects.
• Not recommended for use in children; safety and efficacy have not been established.
• Use during pregnancy may harm the fetus; avoid use during the first trimester and consult a healthcare provider if pregnant or planning to become pregnant.
• Use during breastfeeding is not recommended; consult a healthcare provider before use.
• Discontinue use and seek medical attention if experiencing signs of an allergic reaction.
• Gradual dose reduction is recommended to minimize withdrawal symptoms if discontinuing after prolonged use.

Use during pregnancy or breastfeeding:

Pregnancy: Zolpidem is classified as a Category C medication for pregnancy, indicating that risk to the fetus cannot be ruled out. It is recommended to avoid using zolpidem during the first trimester. If you are pregnant or planning to become pregnant, consult your healthcare provider before using this medication.

Breastfeeding: Zolpidem is excreted in human milk, and its effects on a nursing infant are unknown. Due to potential risks, it is not recommended for use during breastfeeding. If you are breastfeeding or planning to breastfeed, consult your healthcare provider before using this medication.