brands

Class

• Neuroscience-based Nomenclature: GABA positive allosteric modulator (GABA-PAM)
• Non-benzodiazepine hypnotic; alpha 1 isoform selective agonist of GABA-A/ benzodiazepine receptors

Ambien CR commonly prescribed for

(Bold for FDA approved)

How Ambien CR works

• Binds selectively to a subtype of the benzodiazepine receptor, the alpha 1 isoform

• May enhance GABA inhibitory actions that provide sedative hypnotic effects more selectively than other actions of GABA

• Boosts chloride conductance through GABA-regulated channels

• Inhibitory actions in sleep centers may provide sedative hypnotic effects

• The controlled-release formulation may allow sufficient drug to persist at receptors to improve total sleep time and to prevent early morning awakenings that can be associated with the immediate-release formulation of zolpidem

How long until Ambien CR works

• Generally takes effect in less than an hour

Notable Side Effects

• Sedation

• Dizziness, ataxia

• Dose-dependent amnesia

• Hyperexcitability, nervousness

• Diarrhea, nausea

• Headache

• Rare hallucinations

Life Threatening Side Effects

• Respiratory depression, especially when taken with other CNS depressants in overdose

• Rare angioedema

weight gain

unusual

sedation

common

What to do about Ambien CR side effects

• Wait

• To avoid problems with memory, only take zolpidem or zolpidem CR if planning to have a full night’s sleep

• Lower the dose

• Switch to a shorter-acting sedative hypnotic

• Administer flumazenil if side effects are severe or life-threatening

usual dosage range

• 10 mg/day at bedtime for 7–10 days (immediate-release)

• 12.5 mg/day at bedtime (controlled-release)

Dosage Forms

• Immediate-release tablet 5 mg, 10 mg

• Immediate-release capsule 7.5 mg

• Extended-release tablet 6.25 mg, 12.5 mg

• Sublingual tablet 1.75 mg, 3.5 mg, 5 mg, 10 mg

long term use

• Original studies with zolpidem immediaterelease did not assess long-term use

• Increased wakefulness during the latter part of the night (wearing off) or an increase in daytime anxiety (rebound) may occur with immediate-release and be less common with controlled-release

habit forming

• Zolpidem is a Schedule IV drug

• Some patients may develop dependence and/or tolerance; risk may be greater with higher doses

• History of drug addiction may increase risk of dependence

Renal Impairment

• No dose adjustment necessary

• Patients should be monitored

Hepatic Impairment

• Recommended dose 5 mg (immediaterelease), 6.25 mg (controlled-release), 1.75 mg (Intermezzo)

• Patients should be monitored

Cardiac Impairment

• No available data

Elderly

• Recommended initial dose: 5 mg (immediate-release), 6.25 mg (controlledrelease), 1.75 mg (Intermezzo)

• Elderly may have increased risk for falls, confusion

Children and Adolescents

• Safety and efficacy have not been established

• Long-term effects of zolpidem or zolpidem CR in children/adolescents are unknown

• Should generally receive lower doses and be more closely monitored

• Hallucinations in children ages 6–17 have been reported

Pregnancy

• Controlled studies have not been conducted in pregnant women

• In animal studies, oral administration of zolpidem did not indicate a risk for adverse effects on fetal development at clinically relevant doses

• Infants whose mothers took sedative hypnotics during pregnancy may experience some withdrawal symptoms

• Neonatal flaccidity has been reported in infants whose mothers took sedative hypnotics during pregnancy

Breast Feeding

• Some drug is found in mother’s breast milk

• Recommended either to discontinue drug or formula feed