The originating document has been archived. We cannot confirm the completeness, accuracy and currency of the content.
Pronunciation: zole-PI-dem TAR-trate
- Tablets 5 mg
- Tablets 10 mg
- Tablets, ER 6.25 mg
- Tablets, ER 12.5 mg
- Tablets, sublingual 5 mg
- Tablets, sublingual 10 mg
- Spray, solution, lingual 5 mg/actuation
Mechanism is unknown, but may involve subunit modulation of the GABA A receptor chloride channel macromolecular complex.
Rapid absorption from the GI tract. T max is 1.6 h. C max (5 mg tablet) is about 29 to 113 ng/mL; C max (10 mg tablet) is about 58 to 272 ng/mL.ER tablet
Mean C max and AUC are 134 ng/mL and 740 ng•h/mL, respectively, while median T max is 1.5 h.Oral spray
Bioequivalent to oral tablets. Absorption is rapid from the oral mucosa and GI tract. C max following 5 and 10 mg spray is 114 and 210 ng/mL, respectively, with both occurring at a mean T max of 0.9 hours.Food
Reduces absorption of zolpidem. Administration with food decreased the mean AUC and C max 27% and 58%, respectively, while the mean T max was prolonged 225 h (from 0.8 to 2.6 h). For faster sleep onset, do not administer zolpidem products with or immediately after a meal.
Protein binding is about 92.5%.
Converted to inactive metabolites.
Primarily excreted in the urine.
The half-life is 2.6 h (5 mg tablet), 2.5 h (10 mg tablet), 2.8 h (ER tablet).Oral spray
Mean half-life for the 5 and 10 mg spray is 2.8 and 3 hours, respectively.
Special PopulationsRenal Function Impairment
No dosage adjustment is necessary.Hepatic Function Impairment
C max and AUC were found to be 2 and 5 times higher, respectively, in hepatically compromised patients. Modify dosing accordingly in patients with hepatic function impairment.Elderly
C max , half-life, and AUC were significantly increased when compared with results in younger adults.ER tablet
Mean C max and mean AUC are 70.6 ng/mL and 413 ng•h/mL, respectively, while the median T max is 2 h.
Indications and UsageER tablet
Treatment of insomnia characterized by difficulties with sleep onset and/or sleep maintenance.Immediate-release tablet, oral spray, and sublingual tablets
Short-term treatment of insomnia characterized by difficulties in sleep initiation.
Improvement in motor symptoms associated with Parkinson disease.
Dosage and AdministrationER tablets
PO 12.5 mg immediately before bedtime.Elderly, debilitated, or hepatic function impairment
An initial 6.25 mg dose is recommended.Immediate-release, oral spray, sublingual tablets
PO 10 mg immediately before bedtime. Max dose is no more than 10 mg.Elderly, debilitated, or hepatic function impairment
An initial 5 mg dose is recommended.
- Administer immediately before bedtime.
- Administer on an empty stomach for fast sleep onset. Administer with food if GI upset occurs. Do not administer with or immediately after a meal.
- Instruct patient receiving ER not to chew, crush, or split the tablet.
- Oral spray
- To prime, press down on pump 5 times.
- Press down fully on the pump to deliver a full dose (ie, 5 mg). To deliver a 10 mg dose, a second spray should be administered.
- Spray directly into the mouth over the tongue.
- If oral spray is not used for at least 14 days, it must be primed again with 1 spray.
- The effect of the oral spray may be slowed by ingestion with or immediately after a meal.
- Sublingual Tablets
- Place under the tongue; do not swallow.
- Do not take with water.
Store immediate-release tablets and sublingual tablets at 68° to 77°F. Store ER tablets at 59° to 77°F, with limited excursions up to 86°F permitted. Store oral spray upright at 59° to 86°F. Do not freeze. Avoid prolonged exposure to temperatures above 86°F.
Drug InteractionsAzole antifungal agents (eg, itraconazole, voriconazole), sertraline
Zolpidem plasma levels may be increased.CNS depressants (eg, alcohol)
Possible additive or potentiation of CNS depressant effects.Flumazenil
May reverse the sedative/hypnotic effects of zolpidem.Rifamycins (eg, rifampin)
Zolpidem plasma levels may be reduced, decreasing the pharmacologic effects.Ritonavir
Possible severe sedation and respiratory depression.
Laboratory Test Interactions
None well documented.
Palpitation (2%); BP increased (1%).
Headache (19%); somnolence (15%); dizziness (12%); drowsiness (8%); hallucinations (4%); anxiety, disorientation, drugged feeling, fatigue, lethargy, memory disorders (3%); balance disorder, depression, disturbance in attention, hypoesthesia, light-headedness, psychomotor retardation (2%); asthenia, ataxia, confusion, euphoria, insomnia (more than 1%); abnormal dreams, amnesia, binge eating, depersonalization, disinhibition, mood swings, nervousness, paresthesia, sleep disorder, stress symptoms (1%).
Rash (2%); skin wrinkling, urticaria (1%).
Visual disturbance (3%); eye redness, vision blurred (2%); abnormal vision, diplopia (more than 1%); altered depth perception, asthenopia, labyrinthitis, rhinitis, throat irritation, tinnitus (1%).
Nausea (7%); diarrhea, dry mouth (3%); abdominal pain, constipation (2%); dyspepsia, hiccup (more than 1%); abdominal discomfort/tenderness, anorexia, appetite disorder, frequent bowel movements, gastroenteritis, gastroesophageal reflux disease, vomiting (1%).
UTI (2%); menorrhagia (1%).
Myalgia (7%); arthralgia, back pain (4%).
Upper respiratory tract infection (5%); sinusitis (4%); pharyngitis (3%).
Allergy (4%); influenza (3%); influenza-like symptoms (2%); body temperature increase, chest discomfort, chest pain, contusion, infection, neck pain (1%).
Category C .
Excreted in breast milk.
Safety and efficacy not established.
Recommended immediate-release or oral spray dose is 5 mg, and recommended ER dose is 6.25 mg to decrease possibility of adverse reactions; closely monitor elderly or debilitated patients.
Monitor patient closely.
Initiate treatment with 5 mg immediate-release or oral spray, or 6.25 mg ER tablets, and closely monitor patient.
May impair judgment, thinking, or motor skills.
Abrupt discontinuation associated with withdrawal symptoms similar to those associated with other CNS depressant drugs.
Use with caution in patients with history of drug or alcohol abuse, depression, or suicidal tendencies.
Rare cases of angioedema involving the larynx, glottis, or tongue have been reported with the first or subsequent doses. Additional symptoms suggesting anaphylaxis have included dyspnea, nausea, throat closing, and vomiting.
A variety of abnormal thinking and behavior changes (eg, decreased inhibition, visual and auditory hallucinations) have been reported to occur in association with use of sedative/hypnotics. Worsening of insomnia or emergence of new thinking or behavior abnormalities may be the consequence of an unrecognized psychiatric or physical disorder, an adverse reaction of therapy, or spontaneous origin. Emergence of any new behavioral sign or symptom of concern requires careful and immediate evaluation.
Failure of insomnia to remit after 7 to 10 days may indicate the presence of a primary psychiatric and/or medical illness that should be evaluated.
Patients driving their car while not fully awake and with no memory of the event has been reported in patients taking sedative/hypnotics.
Use with caution in patients with conditions or diseases that could affect metabolism or hemodynamic responses.
Use with caution in patients exhibiting signs or symptoms of depression; may worsen depression.
Duration of therapy
Generally limit to 7 to 10 days; reevaluate patient if to be taken for more than 2 to 3 wk.
Before initiating symptomatic treatment, carefully evaluate patient for psychiatric and/or physical disorders that could cause sleep disturbance.
Use with caution in patients with compromised respiratory function.
Suicidal tendencies may be present; take protective measures. Prescribe the smallest quantity feasible in order to reduce the risk of overdose.
CV compromise, light coma, respiratory compromise, somnolence.
- Advise patient to read patient information leaflet carefully before starting therapy and to reread and check for new information each time the medication is refilled.
- Review lifestyle changes that may improve sleep (eg, avoidance of caffeine and nicotine, quiet and dark environment, relaxation techniques, warm water bath).
- Advise patient to take prescribed dose immediately before going to bed.
- Advise patient taking ER or orally disintegrating zolpidem not to crush, chew, or break the tablet.
- Advise patient to take on an empty stomach but to take with food if stomach upset occurs.
- Instruct patient receiving orally disintegrating tablet to place tablet in the mouth, where it will dissolve in seconds and then be swallowed with saliva.
- Inform patient that the orally disintegrating tablet may be taken with or without water.
- Caution patient not to take zolpidem unless planning to get 7 to 8 h of sleep before being active again. Advise patient that taking zolpidem with less than 7 to 8 h of sleep may result in daytime drowsiness, amnesia, or memory problems.
- Review safety precautions with regard to falls, especially for elderly and debilitated patients.
- Caution patient that medication may be habit forming and to take as prescribed. Caution patient not to change the dose unless advised by health care provider.
- Advise patient that sleep may be disturbed for 1 or 2 nights following discontinuation of zolpidem therapy.
- Advise patient that if medication needs to be discontinued after 2 or more weeks of nightly use, it will be slowly withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
- Instruct patient to avoid alcoholic beverages and other depressants while taking this medication.
- Instruct patient to contact health care provider if sleep problems do not appear to be getting better, are getting worse, or if bothersome adverse reactions (eg, changes in thinking or behavior, daytime drowsiness, dizziness, incoordination, memory problems) occur. Caution patient not to increase the dose if sleep problems do not appear to be improving.
- Advise patient that drug may have a carryover effect the next day and to use extreme care while driving or performing other tasks requiring mental alertness and coordination until tolerance is determined.
- Oral spray
- Instruct patients to prime by pressing down on pump 5 times.
- Instruct patients to press down fully on the pump to deliver a full dose (ie, 5 mg). To deliver a 10 mg dose, instruct patient to administer a second spray.
- Instruct patients to spray directly into the mouth over the tongue.
- Instruct patients that if the oral spray is not used for at least 14 days, it must be primed again with 1 spray.
- Inform patients that the effect of the oral spray may be slowed by ingestion with or immediately after a meal.
Copyright © 2009 Wolters Kluwer Health.