ZALEPLON

brands

Class

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

ZALEPLON commonly prescribed for

(Bold for FDA approved)

How ZALEPLON 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

How long until ZALEPLON works

• Generally takes effect in less than an hour

Notable Side Effects

• Sedation

• Dizziness, ataxia

• Dose-dependent amnesia

• Hyperexcitability, nervousness

• Rare hallucinations

• Headache

• Decreased appetite

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 ZALEPLON side effects

• Wait

• To avoid problems with memory, do not take zaleplon if planning to sleep for less than 4 hours

• Lower the dose

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

usual dosage range

• 10 mg/day at bedtime for 7–10 days

Dosage Forms

• Capsule 5 mg, 10 mg

long term use

• Not generally intended for long-term use

• Increased wakefulness during the latter part of the night (wearing off) or an increase in daytime anxiety (rebound) may occur because of short half-life

habit forming

• Zaleplon 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

• Use with caution in patients with severe impairment

Hepatic Impairment

• Mild to moderate impairment: recommended dose 5 mg

• Not recommended for use in patients with severe impairment

Cardiac Impairment

• Zaleplon has not been studied in patients with cardiac impairment, but dose adjustment may not be necessary

Elderly

• Recommended dose: 5 mg

Children and Adolescents

• Safety and efficacy have not been established

• Long-term effects of zaleplon in children/ adolescents are unknown

• Should generally receive lower doses and be more closely monitored

Pregnancy

• Effective June 30, 2015, the FDA requires changes to the content and format of pregnancy and lactation information in prescription drug labels, including the elimination of the pregnancy letter categories; the Pregnancy and Lactation Labeling Rule (PLLR or final rule) applies only to prescription drugs and will be phased in gradually for drugs approved on or after June 30, 2001

• Controlled studies have not been conducted in pregnant women

• In animal studies, administration during organogenesis was not teratogenic at doses up to 49 (rats) and 48 (rabbits) times the maximum recommended human dose (MRHD); in rats, pre- and postnatal growth was reduced and maternal toxicity occurred

• In a pre- and postnatal development study in rats, increased stillbirth and postnatal mortality, and decreased growth and physical development, were observed when zaleplon was administered at doses of 7 mg/kg/day during the latter part of gestation and during lactation; the no-effect dose for offspring development was 1 mg/ kg/day (0.5 times the MRHD of 20 mg on a mg/m2 basis)

• 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 bottle feed