Zolpidem
Zolpidem is a sedative, also called a hypnotic. It affects chemicals in the brain that may be unbalanced in people with sleep problems (insomnia). Zolpidem is used to treat insomnia.
Mechanism of effect
Zolpidem modulates the alpha-subunit, known as the benzodiazepine receptor, within the GABAA receptor chloride channel macromolecular complex.
Zolpidem preferentially binds to the alpha-1 receptor.
Pharmacodynamic
Zolpidem is a sedative or hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties
Pharmacokinetics
Zolpidem is rapidly absorbed from the GI tract. Protein binding: 92.5 ± 0.1%. Zolpidem is converted to inactive metabolites in the liver.
eliminated primarily by renal excretion.
Half life: 2.6 hours
Drug indications
InsomniaDosage
Usual Adult Dose for Insomnia For the short-term treatment of insomnia characterized by difficulties with sleep initiation:
5 mg (women) or 5 to 10 mg (men) orally once daily immediately before bedtime Maximum dose:
10 mg orally daily For insomnia characterized by difficulties with sleep onset and/or sleep maintenance (as measured by wake time after sleep onset):
-EXTENDED-RELEASE TABLETS: Initial dose: 6.25 mg (women) or 6.25 to
12.5 mg (men) orally once daily immediately before bedtime
Maximum dose: 12.5 mg orally once daily immediately before bedtime Usual Geriatric Dose for Insomnia For the short-term treatment of insomnia characterized by difficulties with sleep initiation:
Recommended dose: 5 mg orally once daily immediately before bedtime For insomnia characterized by difficulties with sleep onset and/or sleep maintenance (as measured by wake time after sleep onset): -EXTENDED-RELEASE TABLETS: Recommended dose: 6.25 mg orally once daily immediately before bedtime
Drug contraindications
hypersensitivity to drug or its components.Side effects
nausea , Headache , dry mouth , constipation , abdominal pain , dizziness , vomiting , allergic reaction , rash , vertigo , Depression , Dyspnea , Rhinitis , sinusitis , back pain , Upper respiratory tract infection , lethargyInteractions
Amitriptyline , Pregabalin , Aripiprazole , Alprazolam , Aprepitant , Ethosuximide , Oxazepam , Olanzapine , Pethidine , Voriconazole , Ketoconazole , Clobazam , Clozapine , Clomipramine , Clonazepam , Loratadin , Lorazepam , Maprotiline , Minocycline , Magnesium sulfate , Nitrazepam , Fluconazole , Phenobarbital , Phenytoin , Gabapentin , Lamotrigine , Levetiracetam , Zonisamide , Sertraline , Cetirizine , Flurazepam , Fluvoxamine , Fluoxetine , Trimipramine , Topiramate , Desipramine , Doxepin , Diazepam , Diphenhydramin , Itraconazole , Imipramine , Buspirone , Bosentan , Paroxetine , Posaconazole , Fluticasone propinate , Methocarbamol , Methimazole , Hydroxyzine , Chlordiaze poxide , Chlorpheniramine , fentanyl , Sodium Oxybate , Tapentadol , codeine , Pindolol , Hydrocodone , Armodafinil , Butalbital and Acetaminophen , Acetaminophen and benzhydrocodone , Difenoxin , Ramelteon , Secobarbital , Tolcapone , Clorazepate , Quazepam , Cariprazine , Oxymorphone , Methscopolamine , Lorlatinib , Opium , Ethchlorvynol , Blonanserin , lasmiditan , ethotoinAlerts
1- Patients should be cautioned against driving and other activities requiring complete mental alertness ifZolpidemtartrate is taken in these circumstances
2- Abnormal thinking and behavior changes have been reported in patients treated with sedative/hypnotics, including Zolpidem tartrate.
3- In primarily depressed patients treated with sedative-hypnotics, worsening of depression, and suicidal thoughts and actions
4- The risk of respiratory depression should be considered prior to prescribing Zolpidem tartrate in patients with respiratory impairment including sleep apnea and myasthenia gravis.
5- There have been reports of withdrawal signs and symptoms following the rapid dose decrease or abrupt discontinuation of Zolpidem.
6- The dose of Zolpidem tartrate in elderly patients is 5 mg to minimize adverse effects related to impaired motor and/or cognitive performance and unusual sensitivity to sedative/hypnotic drugs
Points of recommendation
1-Zolpidem tablets should not be taken with or immediately after a meal.
2-Women clear zolpidem from the body at a lower rate than men; therefore, men can tolerate higher doses.
3- If zolpidem is used daily for more than a few weeks, abrupt discontinuation is not recommended. Such cessation may precipitate symptoms of withdrawal.
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