Zolpidem Tartrate

Zolpidem Tartrate Capsules, a gamma-aminobutyric acid (GABA) A receptor positive modulator, is indicated for the short-term treatment of transient insomnia characterized by difficulties with sleep initiation in adults younger than age 65 years of age.

Zolpidem is a GABA A receptor positive modulator presumed to exert its therapeutic effects in the short-term treatment of transient insomnia through binding to the benzodiazepine site of α1 subunit containing GABA A receptors, increasing the frequency of chloride channel opening resulting in the inhibition of neuronal excitation. Zolpidem binds to GABA A receptors with greater affinity for α1 subunit relative to α2 and α3 subunit containing receptors. Zolpidem has no appreciable binding affinity for α5 subunit containing GABA A receptors. This binding profile may explain the relative absence of myorelaxant effects in animal studies. Zolpidem has no appreciable binding affinity for dopaminergic D2, serotonergic 5HT2, adrenergic, histaminergic or muscarinic receptors.

Zolpidem Tartrate Capsules are only available in 7.5 mg strength. Use another zolpidem tartrate immediate-release product for 5 mg or 10 mg dosage.

Avoid use of Zolpidem Tartrate Capsules in geriatric patients.

Recommended dosage of zolpidem tartrate (use the lowest effective zolpidem tartrate dosage):

• Females: The recommended starting dosage of zolpidem tartrate immediaterelease in females is 5 mg once nightly. Use another zolpidem tartrate immediate-release product for dosage initiation in females.
• Males: The recommended starting dosage of zolpidem tartrate immediaterelease in males is either zolpidem tartrate immediate-release 5 mg, Zolpidem Tartrate Capsules 7.5 mg, or zolpidem tartrate immediate-release 10 mg, once nightly. Use another zolpidem tartrate immediate-release product for 5 mg and 10 mg dosing.
• In both males and females: If a 5 mg nightly dose of another zolpidem tartrate immediate-release product is not effective, the zolpidem tartrate dosage may be increased to Zolpidem Tartrate Capsules 7.5 mg once nightly or 10 mg once nightly of another zolpidem tartrate immediate-release product. The maximum recommended dosage of zolpidem tartrate immediate-release is 10 mg once nightly.

Zolpidem Tartrate Capsules are for short-term use only.

Administer Zolpidem Tartrate Capsules orally once per night immediately before bedtime with at least 7 to 8 hours remaining before the planned time of awakening.

Zolpidem Tartrate Capsules should not be taken with or immediately after a meal. Swallow whole. Do not open, crush, or chew.

Lower doses of CNS depressants may be necessary when taken concomitantly with Zolpidem Tartrate Capsules.

The effect of Zolpidem may be slowed by ingestion with or immediately after a meal.

• CNS depressants, including alcohol: Possible adverse additive CNS-depressant effects. Dose adjustment may be necessary.
• Opioids: Concomitant use may increase risk of respiratory depression.
• Imipramine: Decreased alertness observed.
• Chlorpromazine: Impaired alertness and psychomotor performance observed.
• CYP3A4 inducers: Combination use may decrease effects.
• CYP3A4 inhibitors: Combination use may increase effects.

Zolpidem Tartrate Capsules are contraindicated in patients:

• who have experienced complex sleep behaviors after taking zolpidem
• with known hypersensitivity to zolpidem. Observed reactions include anaphylaxis and angioedema

Most commonly observed adverse reactions: headache, drowsiness, dizziness, and diarrhea.

The following serious adverse reactions are discussed in greater detail in other sections of the labeling:

• Complex Sleep Behaviors 
• CNS-Depressant Effects and Next-Day Impairment 
• Severe Anaphylactic and Anaphylactoid Reactions
• Abnormal Thinking and Behavior Changes 
• Withdrawal Effects

There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to psychiatric medications during pregnancy. Limited data from published literature report the presence of zolpidem tartrate in human milk. There are reports of excess sedation in infants exposed to zolpidem tartrate through breastmilk.

CNS-Depressant Effects: Impaired alertness and motor coordination including risk of morning impairment. Risk increases with dose and use with other CNS depressants and alcohol. Caution patients against driving and other activities requiring mental alertness the morning after use. Instruct patients on correct use.

Need to Evaluate for Comorbid Diagnoses: Reevaluate if insomnia persists after 7 to 10 days of use.

Severe Anaphylactic/Anaphylactoid Reactions: Angioedema and anaphylaxis have been reported. Do not rechallenge if such reactions occur.

Abnormal Thinking and Behavioral Changes: Changes including decreased inhibition, bizarre behavior, agitation, and depersonalization have been reported. Immediately evaluate any new onset behavioral changes.

Depression: Worsening of depression or suicidal thinking may occur. Prescribe the least amount of capsules feasible to avoid intentional overdose.

Respiratory Depression: Consider this risk before prescribing in patients with compromised respiratory function.

Precipitation of Hepatic Encephalopathy: Avoid zolpidem tartrate in patients with severe hepatic impairment.

Withdrawal Effects: Symptoms may occur with rapid dose reduction or discontinuation.

Pediatric use: Safety and effectiveness not established. Hallucinations (incidence rate 7%) and other psychiatric and/or nervous system adverse reactions were observed frequently in a study of pediatric patients with Attention-Deficit/Hyperactivity Disorder.

Geriatric Use: Zolpidem Tartrate Capsules are not indicated in geriatric patients. Avoid use of Zolpidem Tartrate Capsules 7.5 mg in geriatric patients because necessary dosage adjustment is not possible with the available dosage strength.

Miscellaneous sedatives & hypnotics

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.