Rapidem®

Therapeutic Area:

Generic Name:

Zolpidem

Dosage Form:

5 & 10 mg film coated tablet

Drug Dose

Therapeutic Indications:

Short-term treatment of insomnia with difficulty of sleep onset.

Mechanism of Action:

Zolpidem, an imidazopyridine hypnotic that is structurally dissimilar to benzodiazepines, enhances the activity of the inhibitory neurotransmitter, γ-aminobutyric acid (GABA), via selective agonism at the benzodiazepine-1 (BZ) receptor; the result is increased chloride conductance, neuronal hyperpolarization, inhibition of the action potential, and a decrease in neuronal excitability leading to sedative and hypnotic effects

Method of Administration:

Sleep-onset insomnia:

5 mg (females) or 5 to 10 mg (males) immediately before bedtime with ≥7 to 8 hours of planned sleep before waking. Use lowest effective dose, not to exceed 10 mg.

Notes

Contraindications:

Hypersensitivity to zolpidem or any component of the formulation; patients who have experienced complex sleep behaviors after taking zolpidem.

Interactions:

Ciprofloxacin (Systemic): May increase the serum concentration of Zolpidem. Management: Consider avoiding the combination of ciprofloxacin and zolpidem if possible. If combined, monitor for signs of zolpidem toxicity (eg, somnolence, dizziness, lethargy). Risk D: Consider therapy modification

FluvoxaMINE: May enhance the CNS depressant effect of Zolpidem. FluvoxaMINE may increase the serum concentration of Zolpidem. Risk C: Monitor therapy

Melatonin: May enhance the sedative effect of Hypnotics (Nonbenzodiazepine). Risk C: Monitor therapy

Metoclopramide: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Pregnancy and Lactation:

Severe neonatal respiratory depression and sedation have been reported when zolpidem was used at the end of pregnancy

Zolpidem is present in breast milk, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Warning and Precaution:

  • Depression: Use with caution in patients with depression, particularly if suicidal risk may be present.
  • Drug abuse: Use with caution in patients with a history of drug dependence. Risk of abuse is

increased in patients with a history or family history of alcohol or drug abuse or mental illness.

  • Hepatic impairment: GABA agonists, including zolpidem, have been associated with precipitation of

hepatic encephalopathy in patients with hepatic impairment. Patients with hepatic impairment do not

clear zolpidem as rapidly as patients with normal hepatic function. Use with caution in patients with mild to moderate hepatic impairment; dose adjustment recommended. Avoid use of immediate and

extended-release tablets in patients with severe hepatic impairment; may result in encephalopathy.

  • Myasthenia gravis: Use with caution in patients with myasthenia gravis.
  • Respiratory disease: Use with caution in patients with respiratory compromise, COPD, or sleep

apnea.

Adverse Reactions:

Dizziness, drowsiness, headache, Chest discomfort, chest pain, edema, hypertension, increased blood pressure, orthostatic hypotension, palpitations, tachycardia

Storage:

Store below 30 and protect from light and moisture.