EDLUAR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EDLUAR (EDLUAR).

How it works

Zolpidem is a non-benzodiazepine hypnotic that acts as a positive allosteric modulator of GABA-A receptors, specifically binding to the alpha1 subunit, enhancing chloride ion conductance and producing sedative effects.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2C9 to inactive metabolites; minor metabolism by CYP1A2, CYP2D6, and CYP2C19.
Excretion	Primarily renal, with approximately 80% of the dose excreted in urine as metabolites (mostly glucuronide conjugates) and less than 1% as unchanged drug. Fecal excretion accounts for <15%.
Half-life	Terminal elimination half-life is approximately 2 hours (range 1.5–3 hours). This short half-life supports its use for sleep induction with minimal next-day residual effects.
Protein binding	Approximately 88–93% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Approximately 2.7 L/kg (range 2.1–3.4 L/kg), indicating extensive tissue distribution.
Bioavailability	Sublingual: approximately 70–80% (avoiding first-pass metabolism); oral: approximately 30–40% due to extensive hepatic first-pass effect.
Onset of Action	Sublingual: 10–20 minutes; oral: 30–45 minutes.
Duration of Action	Approximately 4–6 hours. Clinical effects for sleep induction last about 6–8 hours, with low risk of hangover due to rapid clearance.

Classification & Brands

Dosing & administration

10 mg sublingually once daily at bedtime for insomnia; maximum 10 mg per night.

Dosage form	TABLET
Renal impairment	No specific dose adjustment recommended; use with caution in severe renal impairment (CrCl <30 mL/min) due to increased risk of accumulation.
Liver impairment	Mild to moderate hepatic impairment (Child-Pugh A or B): initial dose 5 mg sublingually. Severe hepatic impairment (Child-Pugh C): contraindicated.
Pediatric use	Not approved for use in pediatric patients (safety and efficacy in children <18 years not established).
Geriatric use	Initial dose 5 mg sublingually once daily at bedtime; maximum 10 mg due to increased sensitivity and risk of falls.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EDLUAR (EDLUAR).

Breastfeeding	Zolpidem is excreted into breast milk; M/P ratio is approximately 0.13 (low). Relative infant dose is about 2% of maternal weight-adjusted dose. Limited data suggest no adverse effects in breastfed infants with occasional use. Caution with repeated doses due to potential sedation and withdrawal in infant.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: increased risk of congenital malformations (e.g., cleft palate) based on animal studies; limited human data. Second and third trimesters: risks include fetal CNS depression, hypotonia, and withdrawal symptoms. Use only if benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Complex sleep behaviors including sleep-driving, making phone calls, preparing and eating food, and other activities while not fully awake have been reported; discontinue immediately if such behaviors occur.

Side Effect Profile

Serious Effects

Absolute Contraindications

History of complex sleep behaviors after taking zolpidem, known hypersensitivity to zolpidem, severe hepatic impairment, and concomitant use with alcohol or other CNS depressants.

Clinical Precautions

Precautions

CNS depressant effects (risk of impaired alertness, next-day impairment), risk of abuse and dependence, worsening of depression or suicidal ideation, anaphylaxis and angioedema, respiratory depression (especially in patients with compromised respiratory function), sleep-related behaviors, and use with alcohol or other CNS depressants.

Clinical Tips & Counseling

Drug interactions

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EDLUAR

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EDLUAR (EDLUAR).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and CYP2C9 to inactive metabolites; minor metabolism by CYP1A2, CYP2D6, and CYP2C19.
Excretion	Primarily renal, with approximately 80% of the dose excreted in urine as metabolites (mostly glucuronide conjugates) and less than 1% as unchanged drug. Fecal excretion accounts for <15%.
Half-life	Terminal elimination half-life is approximately 2 hours (range 1.5–3 hours). This short half-life supports its use for sleep induction with minimal next-day residual effects.
Protein binding	Approximately 88–93% bound to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Approximately 2.7 L/kg (range 2.1–3.4 L/kg), indicating extensive tissue distribution.
Bioavailability	Sublingual: approximately 70–80% (avoiding first-pass metabolism); oral: approximately 30–40% due to extensive hepatic first-pass effect.
Onset of Action	Sublingual: 10–20 minutes; oral: 30–45 minutes.
Duration of Action	Approximately 4–6 hours. Clinical effects for sleep induction last about 6–8 hours, with low risk of hangover due to rapid clearance.

Classification & Brands

Dosing & administration

10 mg sublingually once daily at bedtime for insomnia; maximum 10 mg per night.

Dosage form	TABLET
Renal impairment	No specific dose adjustment recommended; use with caution in severe renal impairment (CrCl <30 mL/min) due to increased risk of accumulation.
Liver impairment	Mild to moderate hepatic impairment (Child-Pugh A or B): initial dose 5 mg sublingually. Severe hepatic impairment (Child-Pugh C): contraindicated.
Pediatric use	Not approved for use in pediatric patients (safety and efficacy in children <18 years not established).
Geriatric use	Initial dose 5 mg sublingually once daily at bedtime; maximum 10 mg due to increased sensitivity and risk of falls.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EDLUAR (EDLUAR).

Breastfeeding	Zolpidem is excreted into breast milk; M/P ratio is approximately 0.13 (low). Relative infant dose is about 2% of maternal weight-adjusted dose. Limited data suggest no adverse effects in breastfed infants with occasional use. Caution with repeated doses due to potential sedation and withdrawal in infant.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: increased risk of congenital malformations (e.g., cleft palate) based on animal studies; limited human data. Second and third trimesters: risks include fetal CNS depression, hypotonia, and withdrawal symptoms. Use only if benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

History of complex sleep behaviors after taking zolpidem, known hypersensitivity to zolpidem, severe hepatic impairment, and concomitant use with alcohol or other CNS depressants.