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Medication Safety Issues
Sound-alike/look-alike issues:
Sonata® may be confused with Soriatane®
Zaleplon may be confused with zolpidem
Pronunciation
(ZAL e plon)
U.S. Brand Names
Generic Available
Yes
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Short-term (7-10 days) treatment of insomnia (has been demonstrated to be effective for up to 5 weeks in controlled trial)
Use: Dental
Has not be established
Restrictions
C-IV
Pregnancy Risk Factor
C
Pregnancy Considerations
Not recommended for use during pregnancy
Lactation
Enters breast milk/not recommended
Contraindications
Hypersensitivity to zaleplon or any component of the formulation
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. These changes may occur unpredictably and may indicate previously unrecognized psychiatric disorders; evaluate appropriately.
• Amnesia: Can occur, do not take unless a full night's sleep and clearance of the drug from the body are possible.
• CNS depression: May cause CNS depression impairing physical and mental capabilities; patients must be cautioned about performing tasks which require mental alertness (operating machinery or driving).
• Hypersensitivity reactions: Postmarketing studies have indicated that the use of hypnotic/sedative agents for sleep has been associated with hypersensitivity reactions including anaphylaxis as well as angioedema.
• Sleep-related activities: An increased risk for hazardous sleep-related activities such as sleep-driving, cooking and eating food, and making phone calls while asleep have been noted.
Disease-related concerns:
• Depression: Use with caution in patients with depression; worsening of depression, including suicidal ideation, has been reported with the use of hypnotics. Intentional overdose may be an issue in this population; prescribe least amount of medication needed.
• Drug abuse: Use with caution in patients with a history of drug dependence.
• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment recommended in mild-to-moderate impairment and avoid use in severe impairment.
• Respiratory disease: Use with caution in patients with respiratory compromise, COPD, or sleep apnea.
Concurrent drug therapy issues:
• CNS depressants/psychoactive medications: Use with caution in patients receiving other CNS depressants or psychoactive medication; effects with other sedative drugs or ethanol may be potentiated.
Special populations:
• Elderly: Use with caution in the elderly; dosage adjustment recommended.
• Pediatrics: Safety and efficacy have not been established in children.
Dosage form specific issues:
• Tartrazine (FDC yellow #5): Capsules contain tartrazine; avoid in patients with sensitivity (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 7-10 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.
• Withdrawal: Abrupt discontinuance may lead to withdrawal symptoms.
Adverse Reactions
>10 %: Central nervous system: Headache (30% to 42%)
1% to 10%:
Cardiovascular: Chest pain (?1%), peripheral edema (?1%)
Central nervous system: Dizziness (7% to 9%), somnolence (5% to 6%), amnesia (2% to 4%), depersonalization (<1% to 2%), hypoesthesia (<1% to 2%), malaise (<1% to 2%), abnormal thinking (?1%), anxiety (?1%), depression (?1%), fever (?1%), migraine (?1%), nervousness (?1%), confusion (?1%), hallucination (?1%), vertigo (?1%)
Dermatologic: Pruritus (?1%), rash (?1%), photosensitivity reaction (?1%)
Endocrine & metabolic: Dysmenorrhea (3% to 4%)
Gastrointestinal: Nausea (6% to 8%), abdominal pain (6%), anorexia (<1% to 2%), constipation (?1%), dyspepsia (?1%), taste perversion (?1%), xerostomia (?1%), colitis (up to 1%)
Neuromuscular & skeletal: Weakness (5% to 7%), paresthesia (3%), tremor (2%), arthralgia (?1%), arthritis (?1%), back pain (?1%), myalgia (?1%), hypertonia (1%)
Ocular: Eye pain (3% to 4%), abnormal vision (<1% to 2%), conjunctivitis (?1%)
Otic: Hyperacusis (1% to 2%), ear pain (?1%)
Respiratory: Bronchitis (?1%), epistaxis (?1%)
Miscellaneous: Parosmia (<1% to 2%)
<1% (Limited to important or life-threatening): Alopecia, ALT increased, anemia, angina, AST increased, ataxia, bigeminy, bilirubinemia, bleeding gums, bundle branch block, cardiospasm, cerebral ischemia, cholelithiasis, circumoral paresthesia, CNS stimulation, cyanosis, delusions, diabetes mellitus, duodenal ulcer, dysarthria, dystonia, dysuria, ecchymosis, eosinophilia, facial paralysis, gastroenteritis, glaucoma, goiter, hematuria, hyper-/hypoglycemia, hyper-/hypotension, hyperuricemia, hypothyroidism, impotence, incontinence, intestinal obstruction, ketosis, lactose intolerance, leukocytosis, lymphocytosis, liver function tests (abnormal), lymphadenopathy, myasthenia, myositis, osteoporosis, palpitation, peptic ulcer, pericardial effusion, photophobia, ptosis, pulmonary embolus, purpura, rash, rectal bleeding, sinus bradycardia, substernal chest pain, syncope, thrombophlebitis, tongue edema, ulcerative stomatitis, urinary retention, ventricular tachycardia, vasodilation, ventricular extrasystoles
Postmarketing and/or case reports: Anaphylaxis, angioedema, complex sleep-related behavior (sleep-driving, cooking or eating food, making phone calls)
Metabolism/Transport Effects
Substrate of CYP3A4 (minor)
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Cimetidine: May decrease the metabolism of Zaleplon. Risk D: Consider therapy modification
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Flumazenil: May diminish 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 adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
Rifamycin Derivatives: May increase the metabolism of Zaleplon. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may increase CNS depression).
Food: High fat meal prolonged absorption; delayed tmax by 2 hours, and reduced Cmax by 35%.
Herb/Nutraceutical: St John's wort may decrease zaleplon levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
Storage
Store at controlled room temperature of 20°C to 25°C (68°F to 77°F). Protect from light.
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.
Pharmacodynamics/Kinetics
Onset of action: Rapid
Duration: 6-8 hours
Absorption: Rapid and almost complete; high-fat meal delays absorption
Distribution: Vd: ~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
Dosage
Oral:
Adults: 10 mg at bedtime (range: 5-20 mg); has been used for up to 5 weeks of treatment in controlled trial setting
Elderly: 5 mg at bedtime; recommended maximum: 10 mg/day
Dosage adjustment in renal impairment: No adjustment for mild-to-moderate renal impairment; use in severe renal impairment has not been adequately studied
Dosage adjustment in hepatic impairment: Mild-to-moderate impairment: 5 mg; not recommended for use in patients with severe hepatic impairment
Administration: Oral
Administer immediately before bedtime or when the patient is in bed and cannot fall asleep.
Dietary Considerations
Avoid taking with or after a heavy, high-fat meal; reduces absorption.
Patient Education
Take exactly as directed; immediately before bedtime, or when you cannot fall asleep. Do not alter dosage or frequency, may be habit forming. Avoid alcohol and other prescription or OTC medications (especially medications to relieve pain, induce sleep, reduce anxiety, treat or prevent cold, coughs, or allergies) unless approved by prescriber. You may experience drowsiness, dizziness, somnolence, vertigo, lightheadedness, blurred vision (avoid driving or engaging in activities that require alertness until response to drug is known); photosensitivity (avoid exposure to direct sunlight, wear protective clothing, and sunscreen); nausea or GI discomfort (small frequent meals, good mouth care, chewing gum, or sucking hard candy may help); constipation (increase exercise, fluids, fruit, or fiber may help); or menstrual disturbances (reversible when drug is discontinued). Discontinue drug and report any severe CNS disturbances (hallucinations, acute nervousness or anxiety, persistent sleepiness or lethargy, impaired coordination, amnesia, or impaired thought processes); skin rash or irritation; eye pain or major vision changes; respiratory difficulty; unusual swelling, especially on face or neck; chest pain; ear pain; or muscle weakness or pain. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.
Geriatric Considerations
In clinical trials, elderly responded to the 5 mg dose with decreased sleep latency. As with all hypnotics, assess underlying cause of insomnia.
Additional Information
Prescription quantities should not exceed a 1-month supply.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Comment
In 2007, the FDA requested that all manufacturers of sedative-hypnotic drug products revise labeling to include a greater emphasis on the risks of adverse effects. These risks include severe allergic reactions (anaphylaxis, angioedema) and complex sleep-related behaviors, which may include sleep-driving (driving while not fully awake and with no memory of the event), making phone calls, and preparing and eating food while asleep. Zaleplon may be associated with a lower potential for abuse compared to benzodiazepines.
Nursing: Physical Assessment/Monitoring
Evaluate etiology of insomnia; failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric and/or medical illness. Assess effectiveness and interactions of other medications. Evaluate risk for suicide and assess for history of addiction (long-term use may result in dependence, abuse, or tolerance). Prescription quantities should not exceed a 1 month supply; periodically evaluate need for continued use. Be alert to possibility of anaphylaxis any time during therapy. For inpatient use, institute safety measures and monitor effectiveness and adverse reactions. For outpatients, monitor therapeutic effectiveness and adverse reactions at beginning of therapy and periodically with long-term use. Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse reactions to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule: 5 mg, 10 mg
Sonata®: 5 mg, 10 mg [contains tartrazine]
Pricing: U.S. (www.drugstore.com)
Capsules (Sonata)
5 mg (30): $130.62
10 mg (30): $141.10
Capsules (Zaleplon)
5 mg (100): $39.99
10 mg (100): $39.99
International Brand Names
Lexi-Comp.com
Last full review/revision September 2009
Content last modified September 2009
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