Trade Names:Ambien- Tablets 5 mg- Tablets 10 mg
Trade Names:Ambien CR- Tablets, ER 6.25 mg- Tablets, ER 12.5 mg
Trade Names:Edluar- Tablets, sublingual 5 mg- Tablets, sublingual 10 mg
Trade Names:Zolpimist- 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.
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.ElderlyImmediate-release tablet
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.
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.
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 tabletsAdults
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.
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.
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.
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.
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.
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