Zaleplon: Drug information

(For additional information see "Zaleplon: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)

ALERT: US Boxed Warning

Complex sleep behaviors:

Complex sleep behaviors, including sleep-walking, sleep-driving, and engaging in other activities while not fully awake, may occur following use of zaleplon. Some of these events may result in serious injuries, including death. Discontinue zaleplon immediately if a patient experiences a complex sleep behavior.

Pharmacologic Category

Hypnotic, Miscellaneous;
Nonbenzodiazepine Benzodiazepine Receptor Agonist

Dosing: Adult

Insomnia, sleep onset

Insomnia, sleep onset:

Note: Limit long-term use (>4 weeks) to cases for which nonpharmacologic treatments are not available or not effective and benefits are felt to outweigh risks (Ref).

Oral: Initial: 5 to 10 mg once daily immediately before bedtime, as needed; may increase to 20 mg based on response and tolerability (maximum dose: 20 mg/day).

Discontinuation of therapy: Reduce by ~25% of the original dose each week or every other week. For patients taking higher doses of zaleplon (eg, 20 mg/day) for an extended period, tapering zaleplon even more slowly in conjunction with cognitive behavioral therapy for insomnia is encouraged (Ref).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

Mild to moderate impairment: No dosage adjustment necessary.

Severe impairment: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

Dosing: Hepatic Impairment: Adult

Mild to moderate impairment: 5 mg immediately before bedtime

Severe impairment: Use is not recommended.

Dosing: Older Adult

Avoid use (Ref).

Insomnia, sleep onset: Oral: Initial: 5 mg once daily immediately before bedtime, as needed; may increase to 10 mg based on response and tolerability (maximum dose: 10 mg/day).

Discontinuation of therapy: Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Central nervous system: Headache (42%)

1% to 10%:

Cardiovascular: Chest pain (≥1%), peripheral edema (≤1%)

Central nervous system: Dizziness (9%), drowsiness (5% to 6%), amnesia (2% to 4%), paresthesia (3%), altered sense of smell (2%), depersonalization (2%), hypoesthesia (2%), malaise (2%), hyperacusis (1% to 2%), abnormality in thinking (≥1%), anxiety (≥1%), depression (≥1%), migraine (≥1%), nervousness (≥1%), hallucination (1%), hypertonia (1%), vertigo (1%)

Dermatologic: Pruritus (≥1%), skin rash (≥1%), skin photosensitivity (1%)

Gastrointestinal: Nausea (8%), abdominal pain (6%), anorexia (2%), constipation (≥1%), dysgeusia (≥1%), dyspepsia (≥1%), xerostomia (≥1%), colitis (1%)

Genitourinary: Dysmenorrhea (3% to 4%)

Neuromuscular & skeletal: Asthenia (7%), tremor (2%), arthralgia (≥1%), arthritis (≥1%), back pain (≥1%), myalgia (≥1%)

Ophthalmic: Eye pain (3% to 4%), visual disturbance (2%), conjunctivitis (≥1%)

Otic: Otalgia (≤1%)

Respiratory: Bronchitis (≥1%), epistaxis (1%)

Miscellaneous: Fever (≥1%)

<1%: Abnormal gait, abnormal hepatic function tests, abnormal uterine bleeding, accommodation disturbance, acne vulgaris, ageusia, agitation, albuminuria, alopecia, anaphylaxis, anemia, angina pectoris, apathy, aphthous stomatitis, apnea, arthropathy, asthma, ataxia, bigeminy, biliary colic, bladder pain, blepharitis, blepharoptosis, bruxism, bundle branch block, bursitis, cataract, central nervous system stimulation, cerebral ischemia, cheilitis, chills, cholelithiasis, confusion, conjunctival hyperemia (subconjunctival hemorrhage), contact dermatitis, corneal erosion, cyanosis, cystitis, deafness, decreased libido, delusions, diabetes mellitus, diaphoresis, diplopia, dry eye syndrome, duodenal ulcer, dysarthria, dysphagia, dyspnea, dystonia, dysuria, ecchymoses, eczema, edema, emotional lability, enteritis, eosinophilia, eructation, esophageal achalasia, esophagitis, euphoria, facial edema, facial paralysis, flatulence, gastritis, gastroenteritis, gingival hemorrhage, gingivitis, glaucoma, glossitis, goiter, gout, hangover effect, heavy menstrual bleeding, hematuria, hemorrhage (eye), hiccups, hostility, hyperbilirubinemia, hypercholesterolemia, hyperesthesia, hyperglycemia, hyperkinetic muscle activity, hyperreflexia, hypertension, hyperuricemia, hyperventilation, hypoglycemia, hypokinesia, hyporeflexia, hypotension, hypothyroidism, hypotonia, impaired consciousness, impotence, increased appetite, increased bronchial secretions, increased serum alanine aminotransferase, increased serum aspartate aminotransferase, increased thirst, insomnia, intestinal obstruction, irregular menses, ketosis, labyrinthitis, laryngitis, leukocytosis, leukorrhea, lymphadenopathy, lymphocytosis, maculopapular rash, mastalgia, melanosis, melena, menopause, menstrual disease, myasthenia, myoclonus, myositis, neck stiffness, nephrolithiasis, neuralgia, neuropathy, nightmares, nystagmus disorder, oral mucosa ulcer, oral paresthesia, orthostatic hypotension, osteoporosis, palpitations, paradoxical central nervous system stimulation, peptic ulcer, pericardial effusion, photophobia, pleural effusion, pneumonia, psoriasis, psychomotor retardation, pulmonary embolism, purpuric disease, pustular rash, rectal hemorrhage, renal pain, reduced urine flow, retinal detachment, sialorrhea, sinus bradycardia, skin discoloration, skin hypertrophy, slurred speech, snoring, stomatitis, stupor, substernal pain, syncope, tachycardia, tenosynovitis, thrombophlebitis, tinnitus, tongue discoloration, tongue edema, trismus, urethritis, urinary frequency, urinary incontinence, urinary retention, urinary urgency, urticaria, vaginal hemorrhage, vaginitis, vasodilatation, ventricular premature contractions, ventricular tachycardia, visual field defect, voice disorder, watery eyes, weight gain, weight loss, xeroderma

Frequency not defined:

Central nervous system: Central nervous system depression, complex sleep-related disorder

Hypersensitivity: Angioedema, hypersensitivity condition

Postmarketing: Anaphylaxis, nightmares, nonimmune anaphylaxis

Contraindications

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

Warnings/Precautions

Concerns related to adverse effects:

• Abnormal thinking/behavioral changes: Hypnotics/sedatives have been associated with abnormal thinking and behavior changes including decreased inhibition, aggression, bizarre behavior, agitation, hallucinations, and depersonalization. Amnesia and other neuropsychiatric symptoms may occur unpredictably and may indicate previously unrecognized psychiatric disorders; evaluate appropriately.

• CNS depression: May cause CNS depression impairing physical and mental capabilities; caution patients about performing tasks that require mental alertness (eg, operating machinery, driving). The risk of next-day psychomotor impairment is increased if patient is unable to stay in bed for a full night of sleep (7 to 8 hours), if a higher-than-recommended dose is taken, and/or if coadministered with other CNS depressants or other drugs that increase the blood levels of zaleplon. Dose adjustment may be necessary if taking concomitant CNS depressants; use with other sedative-hypnotics at bedtime or in the middle of the night is not recommended.

• Complex sleep behaviors: [US Boxed Warning]: Complex sleep behaviors, including sleep-walking, sleep-driving, and engaging in other activities while not fully awake, may occur following the use of zaleplon. Some of these events may result in serious injuries, including death. Other complex sleep behaviors (eg, preparing and eating food, making phone calls, having sex) while asleep have also been reported. Patients usually do not remember these events. May occur with first use and at recommended dosages with or without the use of alcohol or other CNS depressants. Discontinue immediately if a patient experiences a complex sleep behavior; use is contraindicated in patients who have experienced these events.

• Hypersensitivity reactions: Hypersensitivity reactions, including anaphylaxis, as well as angioedema, have been reported. Do not rechallenge patient if such reactions occur.

Disease-related concerns:

• Depression: Use with caution in patients with depression; worsening of depression, including suicide or suicidal ideation, has been reported with the use of hypnotics. Intentional overdose may be an issue in this population. The minimum dose that will effectively treat the individual patient should be used. Prescriptions should be written for the smallest quantity consistent with good patient care.

• Drug abuse: Use with caution in patients with a history of drug dependence, benzodiazepine abuse, or benzodiazepine-like hypnotic abuse.

• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment recommended in mild to moderate impairment. Use is not recommended in patients with severe impairment.

• Respiratory disease: Use with caution in patients with respiratory compromise, chronic obstructive pulmonary disease, or sleep apnea.

Special populations:

• Debilitated patients: Use with caution in debilitated patients; increased risk of impaired cognitive and/or motor performance. Dosage adjustment recommended; monitor closely.

• Older adult: Increased risk of impaired cognitive and/or motor performance and falls; monitor closely.

Dosage form specific issues:

• Tartrazine (FDC yellow #5): Capsules contain tartrazine; avoid in patients with sensitivity; reactions may be more frequently seen in patients with aspirin hypersensitivity; use caution in patients with asthma.

Other warnings/precautions:

• Appropriate use: Symptomatic treatment of insomnia should be initiated only after careful evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7 to 10 days may indicate psychiatric and/or medical illness.

• Rapid onset: Because of the rapid onset of action, administer immediately prior to bedtime or after the patient has gone to bed and is having difficulty falling asleep.

• Rebound insomnia: Following withdrawal of therapy, transient insomnia may recur accompanied by other reactions, including restlessness, anxiety, and mood changes (Bélanger 2009).

• Withdrawal: A longer sleep-onset latency and increased awakenings during sleep may occur for 1 to 2 days following the discontinuation of GABA-mediated (GABAergic) medications. A more severe withdrawal syndrome may rarely occur following abrupt discontinuation or large decreases in dose after sustained use, and is characterized by abdominal pain, anxiety, confusion, delirium, disorientation, euphoria, hypertension, insomnia, irritability, restlessness, speech difficulties, seizures, and tremor. This withdrawal syndrome is generally mild and infrequent and resolves within weeks or upon re-initiation of the GABAergic medication. Intermittent dosing may reduce the risk of withdrawal symptoms (BAP [Wilson 2019]; Schifano 2019).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Generic: 5 mg, 10 mg

Generic Equivalent Available: US

Yes

Pricing: US

Capsules (Zaleplon Oral)

5 mg (per each): $3.65 - $3.69

10 mg (per each): $3.75 - $3.79

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Controlled Substance

C-IV

Administration: Adult

Oral: Administer immediately before bedtime or when the patient is in bed and cannot fall asleep. Do not take with, or immediately following, a high-fat meal (may delay onset).

Medication Guide and/or Vaccine Information Statement (VIS)

An FDA-approved patient medication guide, which is available with the product information and at https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020859s016lbl.pdf#page=21, must be dispensed with this medication.

Use: Labeled Indications

Insomnia, sleep onset: Short-term treatment of insomnia (ie, up to 30 days).

Medication Safety Issues

Sound-alike/look-alike issues:

Sonata may be confused with Soriatane

Zaleplon may be confused with Zelapar, Zemplar, zolpidem, ZyPREXA Zydis

Older Adult: High-Risk Medication:

Beers Criteria: Zaleplon, a nonbenzodiazepine benzodiazepine-receptor agonist hypnotic, is identified in the Beers Criteria as a potentially inappropriate medication to be avoided in patients 65 years and older (independent of diagnosis or condition) due to adverse events similar to benzodiazepines in older adults (eg, delirium, falls, fractures) and an increase in emergency room visits, hospitalizations, and motor vehicle crashes. In addition, improvement in sleep latency and duration is minimal (Beers Criteria [AGS 2023]).

Metabolism/Transport Effects

Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy

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

Azelastine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider therapy modification

Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

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

Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider therapy modification

Cannabinoid-Containing Products: CNS Depressants may enhance the CNS depressant effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider therapy modification

Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Risk C: Monitor therapy

Cimetidine: May increase the serum concentration of Zaleplon. Management: The initial dose of zaleplon should be limited to 5 mg in patients taking cimetidine. Monitor patients for increased zaleplon effects/toxicities (ie, sedation, CNS depression) when these agents are combined. Risk D: Consider therapy modification

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Zaleplon. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Zaleplon. Management: Consider the use of an alternative hypnotic that is not metabolized by CYP3A4 in patients receiving strong CYP3A4 inducers. If zaleplon is combined with a strong CYP3A4 inducer, monitor for decreased effectiveness of zaleplon. Risk D: Consider therapy modification

Daridorexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

DexmedeTOMIDine: CNS Depressants may enhance the CNS depressant effect of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider therapy modification

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

Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Doxylamine: CNS Depressants may enhance the CNS depressant effect of Doxylamine. Risk C: Monitor therapy

DroPERidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification

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

Flunarizine: CNS Depressants may enhance the CNS depressant effect of Flunarizine. Risk X: Avoid combination

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider therapy modification

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

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

Kratom: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider therapy modification

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

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

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

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

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider therapy modification

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

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Risk C: Monitor therapy

Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Olopatadine (Nasal): May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Risk X: Avoid combination

Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Risk X: Avoid combination

Oxybate Salt Products: Hypnotics (Nonbenzodiazepine) may enhance the CNS depressant effect of Oxybate Salt Products. Risk X: Avoid combination

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Risk X: Avoid combination

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

Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Risk C: Monitor therapy

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Risk C: Monitor therapy

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

Ropeginterferon Alfa-2b: CNS Depressants may enhance the adverse/toxic effect of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider therapy modification

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Risk C: Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Risk C: Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Risk C: Monitor therapy

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider therapy modification

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Risk X: Avoid combination

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

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

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider therapy modification

Zuranolone: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider therapy modification

Food Interactions

High-fat meals prolong absorption; delay T_max by 2 hours, and reduce C_max by 35%. Management: Avoid taking after a high-fat meal.

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies. A small study of pregnant women did not show an increased risk of teratogenic effects when used early in pregnancy (Wikner 2011). Use during pregnancy is not recommended by the manufacturer.

Breastfeeding Considerations

Zaleplon is excreted in human milk with the highest concentration ~1 hour after administration; therefore, the manufacturer does not recommend use while breast-feeding.

Dietary Considerations

Avoid taking with or after a heavy, high-fat meal; reduces absorption.

Monitoring Parameters

Daytime alertness; fall risk; respiratory rate (patients with compromised respiration); behavior changes; tolerance, abuse, and dependence; reevaluate if insomnia persists after 30 days of use.

Mechanism of Action

Zaleplon is unrelated to benzodiazepines, barbiturates, or other hypnotics. However, it interacts with the benzodiazepine GABA receptor complex. Nonclinical studies have shown that it binds selectively to the brain omega-1 receptor situated on the alpha subunit of the GABA-A receptor complex.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Rapid

Absorption: Rapid and almost complete; high-fat meal delays absorption

Distribution: V_d: ~1.4 L/kg

Protein binding: ~45% to 75%

Metabolism: Extensive, primarily via aldehyde oxidase to form 5-oxo-zaleplon and, to a lesser extent, by CYP3A4 to desethylzaleplon; all metabolites are pharmacologically inactive

Bioavailability: ~30%

Half-life elimination: ~1 hour

Time to peak, serum: ~1 hour

Excretion: Urine (~70% primarily metabolites, <1% as unchanged drug); feces (~17%)

Clearance: Plasma: Oral: 3 L/hour/kg

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Hepatic function impairment: Oral Cl was reduced 70% and 87% in compensated and decompensated cirrhotic patients, respectively.

Race/ethnicity: C_max and AUC were increased 37% and 64%, respectively in Asian populations.

Brand Names: International

International Brand Names by Country

For country code abbreviations (show table)

(AE) United Arab Emirates: Sonata;
(AR) Argentina: Hegon | Hipnodem;
(BD) Bangladesh: Eplon | Somna;
(BE) Belgium: Sonata;
(BR) Brazil: Sonata;
(CH) Switzerland: Sonata;
(CL) Chile: Noctiplon | Plenidon | Rhem | Sedartryl;
(CN) China: An ji xin | An lan | An wei de | Bai jie min | He bang li an | Qu ning | Sai mei | Shu meng | Si wei tan | Tong an qi;
(CO) Colombia: Sonata;
(CZ) Czech Republic: Sonata;
(DE) Germany: Sonata;
(EC) Ecuador: Rhem;
(EG) Egypt: Siesta | Zalosed;
(ES) Spain: Sonata;
(FI) Finland: Sonata;
(GB) United Kingdom: Sonata;
(GR) Greece: Sonata;
(HR) Croatia: Zan;
(HU) Hungary: Andante;
(IE) Ireland: Sonata;
(IN) India: Hyplon | Stilnite | Zalep | Zalpilo | Zanlop | Zaplon | Zaso | Zonesta;
(IT) Italy: Sonata | Zerene;
(LU) Luxembourg: Sonata;
(PE) Peru: Plenidon;
(PR) Puerto Rico: Sonata;
(PY) Paraguay: Ansiomida;
(RU) Russian Federation: Andante | Sonata adamed;
(SE) Sweden: Sonata;
(SK) Slovakia: Sonata;
(TW) Taiwan: Demare | Jalumen | Onsleep | Soandine | Solmin | Sonaplon | Sonimax;
(UA) Ukraine: Andante | Selofen;
(UY) Uruguay: Prox | Zaplonic

2023 American Geriatrics Society Beers Criteria Update Expert Panel. American Geriatrics Society 2023 updated AGS Beers Criteria for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2023;71(7):2052-2081. doi:10.1111/jgs.18372 [PubMed 37139824]
Bélanger L, Belleville G, Morin C. Management of hypnotic discontinuation in chronic insomnia. Sleep Med Clin. 2009;4(4):583-592. doi:10.1016/j.jsmc.2009.07.011 [PubMed 20607118]
Ganzberg S, Dietrich T, Valerin M, Beck FM. Zaleplon (sonata) oral sedation for outpatient third molar extraction surgery. Anesth Prog. 2005;52:128-131. [PubMed 16596911]
Qaseem A, Kansagara D, Forciea MA, Cooke M, Denberg TD; Clinical Guidelines Committee of the American College of Physicians. Management of chronic insomnia disorder in adults: a clinical practice guideline from the American College of Physicians. Ann Intern Med. 2016;165(2):125-133. doi:10.7326/M15-2175 [PubMed 27136449]
Riemann D, Baglioni C, Bassetti C, et al. European guideline for the diagnosis and treatment of insomnia. J Sleep Res. 2017;26(6):675-700. doi:10.1111/jsr.12594 [PubMed 28875581]
Schifano F, Chiappini S, Corkery JM, Guirguis A. An insight into Z-drug abuse and dependence: an examination of reports to the European Medicines Agency database of suspected adverse drug reactions. Int J Neuropsychopharmacol. 2019;22(4):270-277. doi:10.1093/ijnp/pyz007 [PubMed 30722037]
Sonata (zaleplon) [prescribing information]. New York, NY: Pfizer Inc; August 2019.
Wikner BN, Källen B. Are hypnotic benzodiazepine receptor agonists teratogenic in humans? J Clin Psychopharmacol. 2011;31(3):356-359. doi:10.1097/JCP.0b013e3182197055 [PubMed 21508851]
Wilson S, Anderson K, Baldwin D, et al. British Association for Psychopharmacology consensus statement on evidence-based treatment of insomnia, parasomnias and circadian rhythm disorders: an update. J Psychopharmacol. 2019;33(8):923-947. doi:10.1177/0269881119855343 [PubMed 31271339]
Zaleplon capsules [prescribing information]. East Windsor, NJ: Aurobindo Pharma USA Inc; October 2021.

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Zaleplon: Drug information