-Description:
ZOLPIM (zolpidem tartrate), is a non-benzodiazepine hypnotic of the imidazopyridine class and is available in 5-mg and 10-mg strength tablets for oral administration.
-Pharmacodynamics & Pharmacokinetics:
Zolpidem is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with a gamma amino butaric acid-benzodiazepines (GABA-BZ) receptor complex and shares some of the pharmacological properties of the benzodiazepines.
In contrast to benzodiazepines, which non-selectively bind to and activate all omega receptor subtypes, zolpidem in vitro binds the Omega-1 receptor preferentially with a high affinity ratio of alpha1 / alpha5 subunits.
The Omega-1 receptor is found primarily on the lamina IV of the sensorimotor cortical regions, substantia nigra (parsreticulata), cerebellum molecular layer, olfactory bulb, ventral thalamic complex, pons, inferior colliculus, and globus pallidus. This selective binding of zolpidem on the Omega-1 receptor is not absolute, but it may explain the relative absence of myorelaxant and anti-convulsant effects in animal studies as well as the preservation of deep sleep (stage 3 and 4 ) in human studies of zolpidem at hypnotic doses.
Zolpidem is characterized by rapid absorption from the gasterointestinal tract and short elimination half-life in healthy subjects, and for faster sleep onset, ZOLPIM should not be administered with or immediately after a meal.
-Indications:
ZOLPIM (zolpidem tartrate) is indicated for short-term treatment of insomnia.
ZOLPIM has been shown to decrease sleep latency and increase the duration of sleep.
Hypnotics should generally be limited to 7 to 10 days of use and reevaluation of the patient is recommended if they are to be taken for more than 2 to 3 weeks.
ZOLPIM should not be prescribed in quantities exceeding a 1-month supply.
-Contraindications:
None known.
-Adverse Reactions:
The most commonly adverse events were daytime drowsiness, dizziness, and diarrhea, also headache, nausea, vomiting, myalgia, amnesia, were observed.
-Warning & Precautions:
The failure of insomnia to remit after 7 to 10 days of treatment may indicate the presence of a primary psychiatric and / or medical illness which should be evaluated.
Because some of the important adverse effects of zolpidem appear to be dose related, it is important to use the smallest possible effective dose, especially in the elderly.
Due to the rapid onset of action, ZOLPIM should only be ingested immediately prior to going to bed.
Patients should be cautioned against engaging in hazardous occupations requiring complete mental alertness or motor coordination such as operating machinery or driving a motor vehicle after ingesting the drug, including potential impairment of the performance of such activities that may occur the day following ingestion of zolpidem.
ZOLPIM showed additive effects when combined with alcohol and should not be taken with alcohol.
Patient should also be cautioned about possible combined effects with other CNS-depressant drugs dosage adjustments may be necessary when ZOLPIM is administered with such agents because of the potentially additive effects.
-Use in The Elderly and / or Debilitated Patients:
The recommended ZOLPIM dosage is 5mg in such patients to decrease the possibility of side effects. Those patients should be closely monitored.
-Use in Patients With Concomitant Illness:
-Caution is advisable in using ZOLPIM in patients with diseases or conditions that could affect metabolism or hemodynamic responses.
-Precautions should be observed if ZOLPIM prescribed to patients with compromised respiratory function, since sedative / hypnotics have the capacity to depress respiratory drive.
-In end-stage renal failure patients treated with zolpidem did not demonstrate drug accumulation or alterations in pharmacokinetic parameters, and no dosage adjustment in renally impaired patients is required, however, those patients should be closely monitored.
-Patients with hepatic impairment did reveal prolonged elimination time of zolpidem, therefore, treatment should be initiated with 5mg in patients with hepatic compromise, and they should be closely monitored.
-Use in depression: ZOLPIM should be administered with caution to patients exhibiting signs or symptoms of depression, intentional over-dosage is more common in this group of patients; therefore, the least amount of drug that feasible should be prescribed.
-Laboratory Tests:
There are no specific laboratory test recommended.
-Drug Interactions:
-Haloperidol and zolpidem revealed no effect of haloperidol on the pharmacokinetics or pharmacodynamics of zolpidem.
-Imipramine in combination with zolpidem produced no pharmacokinetic interaction, but there was an additive effect of decreased alertness.
-Chlorpromazine in combination with zolpidem produced no pharmacokinetic interaction, but there was an additive effect of decreased alertness and psychomotor performance.
-Zolpidem and alcohol produce an additive effect on psychomotor performance.
-Fluoxetine in combination with zolpidem there was no evidence of an additive effect in psychomotor performance.
-Zolpidem 10mg in the presence of sertraline 50mg, zolpidem (Cmax) was significantly higher and (Tmax) was significantly decreased (53%) , pharmacokinetics of sertraline were unaffected by zolpidem.
-In combination with other CNS-active drugs, careful consideration should be given to the pharmacology of any CNS-active drug to be used with zolpidem.
Any drug with CNS-depressant effects could be potentially enhance the CNS-depressant effects of zolpidem.
-Zolpidem in combination with itraconazole (drug that affect drug metabolism via cytochrome P450) and zolpidem, there were no significant pharmacodynamic effects of zolpidem on subjective drowsiness, postural sway, or psychomotor performance.
-Zolpidem in combination with rifampin showed significant reductions of pharmacokinetics and pharmacodynamic effects of zolpidem.
-Zolpidem in combination with cimetidine or ranitidine revealed no drug interactions.
-Zolpidem had no effect on digoxin kinetic.
-Zolpidem with warfarin did not affect prothrombin time in normal subject.
-Zolpidem`s sedative / hypnotic effect was reversed by flumazenil, no significant alterations in zolpidem pharmacokinetics were found.
- Drug / laboratory Test Interactions:
- Zolpidem is not known to interfere with commonly employed clinical laboratory tests, also zolpidem dose not cross-react with benzodiazepines, opiates, barbiturates, cocaine, cannabinoids, or amphetamines.
- Use In Pregnancy : Pregnancy Category B
ZOLPEM (zolpidem tartrate) should be used during pregnancy only if clearly needed.
- Use In Nursing Mothers:
The use of ZOLPIM (zolpidem tartrate) is not recommended.
- Pediatric Use:
Safety and effectiveness in pediatric patients below the age of 18 have no been established.
- Drug Abuse And Dependence:
Rare reports of abuse, dependence and withdrawal have been received, since persons with history of addiction to , or abuse of , drug or alcohol are at increased risk of habituation and dependence, they should be under careful surveillance when receiving zolpidem or any other hypnotic.
- Dosage & Administration:
The dose of ZOLPIM should be individualized. The recommended dose for adults is 10mg immediately before bedtime.
Downward dosage adjustment may be necessary when ZOLPIM is administered with agents having known CNS-depressant effects.
Elderly and debilitated patients may be especially sensitive to the effects of (zolpidem tartrate). Patients with hepatic insufficiency do not clear the drug as rapidly as normals. So an initial 5-mg dose is recommended in these patients the total ZOLPIM dose should not exceed 10-mg.
- How Supplied:
ZOLPIM-5mg : Box of 30 film-coated tablets in blisters.
ZOLPIM-10mg : Box of 30 film-coated tablets in blisters.
Store at controlled room temperature 20 º C to 25 º C away of light and keep out of children
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