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Zolpidem has a strong sedative effect due to increased activity of the inhibitory neurotransmitter GABA. It is indicated for the short-term treatment of occasional insomnia and temporary stress-induced insomnia.1. What is Zolpidem?
Zolpidem is a derivative of imidazopyridine with a strong sedative effect. Zolpidem enhances the activity of the inhibitory neurotransmitter, γ-aminobutyric acid (GABA), through selective agonism at the benzodiazepine-1 receptor, resulting in increased neuronal polarization, inhibition action potentials and decreased excitability of neurons leading to a sedative effect that induces sleep. Due to the drug's selectivity for the BZ1 receptor, Zolpidem has little anxiolytic, analgesia, and anti-gastrointestinal activity. Zolpidem is a quick and short acting drug. At doses normally inducing sleep in humans, Zolpidem has the ability to shorten the time to sleep onset and prolong sleep time, maintaining deep sleep.
2. Uses of Zolpidem
Zolpidem is indicated for the short-term treatment of occasional insomnia such as when traveling and for the temporary treatment of insomnia caused by stress.Zolpidem is contraindicated in the following cases:
Hypersensitivity to the drug or any of the ingredients listed in the formula. People with sleep apnea. Acute respiratory failure. Chronic obstructive pulmonary disease. Myasthenia gravis. Liver failure, severe renal failure. Deity. People who are pregnant or breastfeeding
3. Dosage of Zolpidem
Adult patients: The dose of Zolpidem varies from patient to patient. The smallest effective dose should be used, especially in the elderly, debilitated and people with liver disease, avoiding prolonged treatment. The usual dose in adult patients is as follows:
Regular Tablets: The recommended dose is 10mg at bedtime. Extended-release tablets: The recommended dose is 12.5mg. In all cases, Zolpidem should not be taken in excess of 10 mg per day. Children: The safety and efficacy of Zolpidem in children under 18 years of age have not been established, therefore, Zolpidem is not recommended for use in children.
Elderly or debilitated patients: The recommended starting dose is 5mg (regular tablet) or 6.25mg (extended release tablet) at bedtime; The dose can then be adjusted if necessary.
Patients with hepatic impairment: The starting dose of Zolpidem is 5 mg (regular tablet) or 6.25 mg (extended release tablet) at bedtime; The dose can then be adjusted if necessary.
Patients with renal impairment: The manufacturer recommends that no dose adjustment is required, but close monitoring is required during the dosing process. Some investigators have suggested that a dose reduction is necessary because the elimination rate of Zolpidem is slower than in subjects with renal impairment.
Other subjects: The dose should be reduced in patients receiving Zolpidem concomitantly with other CNS depressants due to increased potency.
How to use:
Patients need to take Zolpidem right before going to bed. For slow-release tablets, they must be swallowed whole, not chewed or divided. The duration of dosing should be as short as possible, usually from a few days to 4 weeks, including time to reduce the dose. It is necessary to guide the specific treatment time for each patient in each case. For example, patients with occasional insomnia due to travel often take the drug for 2 - 5 days; Temporary insomnia due to mental stress is usually treated for 2 to 3 weeks. In the case of patients taking the drug for a very short time, there is no need to gradually reduce the dose before stopping the drug.
4. What are the side effects of Zolpidem?
Patients using Zolpidem may experience unwanted effects as follows:
Common: Drowsiness, lethargy, headache, dizziness, confusion, weakness, anxiety, difficulty concentrating, sweating, diarrhea, nausea, vomiting, bloating, dyspepsia, constipation, abdominal pain, loss of appetite, muscle and joint pain. Uncommon: Psychosis, nervousness, anxiety, sleep disturbance, paresthesia, migraine, neuralgia, neuritis, decreased libido, tremor, difficulty speaking, dysphagia, confusion dysgeusia, dyspnea, cramps, flatulence, cough, bronchitis. Rare: Hallucinations, insomnia, suicidal tendencies, convulsions, sciatica, intestinal obstruction, rectal bleeding, epistaxis, anaphylaxis, skin allergy, photosensitivity, muscle weakness, tendinitis, osteoarthritis, bronchospasm, increased liver enzymes and low blood pressure.
5. What are the precautions when using Zolpidem?
Zolpidem should be used with caution in patients with depression, especially those at risk of suicide. Zolpidem should not be used for a long time. Avoid abrupt discontinuation or rapid dose reduction in patients on prolonged use as withdrawal symptoms may develop. When Zolpidem is used in combination with alcohol or other CNS depressants, anxiety, loss of concentration, and forgetfulness may occur. Zolpidem should be used with caution in patients with impaired respiratory function because hypnotic sedatives are capable of respiratory depression. Drug abuse: Zolpidem should be used with caution in patients with a history of drug dependence. The risk of drug abuse is increased in patients with a history or family history of alcohol, drug abuse, or mental illness. Hepatic impairment: GABA agonists, including Zolpidem, have been associated with hepatic encephalopathy in patients with hepatic impairment because patients with hepatic impairment do not clear Zolpidem as rapidly as patients with normal liver function. Use with caution in patients with mild to moderate hepatic impairment and dose adjustment is recommended. Avoid use in patients with severe hepatic impairment because of possible encephalopathy. Zolpidem should be used with caution in patients with myasthenia gravis, respiratory failure or sleep apnea. Zolpidem should be used with caution in debilitated patients because of the potential for overdose, impaired coordination, and confusion. Zolpidem should be used with caution in elderly patients. Dosage adjustment and monitoring of cognitive and/or motor abilities are recommended because of the risk of confusion and falls. Women: Dosage should be adjusted for women. Pharmacokinetic studies involving Zolpidem showed a significant increase in exposure in females compared with males at the same dose. Pregnancy: Zolpidem crosses the placenta. Respiratory depression and neonatal sedation have been reported following maternal use of the drug at the end of the third trimester. Therefore, Zolpidem should not be used by pregnant women. Lactation: Zolpidem is excreted in human milk in small amounts and its effect on the nursing infant is unknown. Therefore, in order to avoid adverse effects on the infant, the mother should not take Zolpidem or should discontinue breast-feeding when considering the benefit of treatment to the mother.
6. Zolpidem drug interactions
Drug interactions can cause many clinical consequences such as changing the therapeutic effect and increasing the side effects of the drug. To avoid drug interactions, patients should inform their doctor of all medications and supplements they are taking. Here are some drug interactions to watch out for when using Zolpidem:
Zolpidem is metabolized mainly by the enzyme CYP3A4 and to a small extent by CYP1A2 and CYP2D6. Therefore, drugs that affect liver enzymes have the potential to interact with Zolpidem. For example, antifungal drugs of the Azol group (Ketoconazole, Fluconazole...) inhibit the CYP3A4 enzyme and increase the concentration and increase the effect of Zolpidem. Rifampicin: Increases CYP3A4 enzyme activity, thereby reducing plasma concentrations and reducing the effect of Zolpidem. Ritonavir and other drugs in the same class: Inhibits hepatic metabolism of Zolpidem, increasing its concentration, leading to strong sedation and respiratory depression. Metabolism-inhibiting serotonin uptake inhibitors potentiate the effects of Zolpidem. Flumazepnil has the potential to reverse the sedating effects of Zolpidem. Above is information about the uses, dosage and precautions when using Zolpidem. If you need more information about the drug, you should contact your doctor for advice.
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