Ambien for Insomnia Accompanied by Fatigue and IrritabilityAmbien exhibits a pronounced sedative action with minor anticonvulsant, anxiolytic, and central muscle relaxant effects. Learn about its administration and interaction features from this article.

Ambien – Effective Treatment for Sleep Disorders

Ambien (zolpidem) is a medicine for the short-term treatment of insomnia in adults. It is available by prescription and belongs to the benzodiazepine group of hypnotics and sedatives. Experimental studies have shown that Ambien produces a sedative effect at doses lower than those required for anxiolytic, anticonvulsant, or muscle relaxant effects. These effects are due to a specific impact on central receptors belonging to the macromolecular GABA-omega receptor complex (BZ1 and BZ2), which functions by opening chloride ion channels. The drug acts primarily on omega (BZ1) receptor subtypes. Ambien shortens the time it takes to fall asleep, reduces the number of nighttime awakenings, increases total sleep duration, and improves sleep quality. It extends stage II sleep and stages of deep sleep (III and IV). Does not cause drowsiness during the day.

Pharmacokinetics

Ambien demonstrates rapid absorption and the onset of a hypnotic effect. Bioavailability after oral administration is 70%. Within the therapeutic range, the drug exhibits linear kinetics. The therapeutic level in blood plasma is from 80 to 200 ng/ml. The maximum concentration in blood plasma is reached 0.5-3 hours after taking. The volume of distribution in adults is 0.54 l/kg (in elderly people this figure is usually 0.34 l/kg). Plasma protein binding reaches 92%. Metabolism during the first passage through the liver is about 35%. The half-life is 2.4 hours, while the duration of action is up to 6 hours. All metabolites of the drug are pharmacologically inactive and excreted in urine (56%) and feces (37%).

Administration Method

Ambien is for oral use. The pills should be swallowed whole, regardless of meals, with plenty of liquid. A single dose is usually 10 mg. Elderly people and those suffering from liver failure should reduce the dose to 5 mg.

Contraindications

The main contraindications to taking Ambien are as follows: • Hypersensitivity to the main or any of the auxiliary components of the drug; • Myasthenia gravis; • Sleep apnea syndrome; • Acute or severe respiratory failure; • Severe liver failure.

Interaction

There are several important interactions that you should be aware of before taking the drug: • Concomitant use of Ambien and CNS depressants such as opioid analgesics, cough suppressants, barbiturates, antipsychotics, antidepressants, tranquilizers, and antihistamines may increase their CNS depressant effects; • Flumazenil reverses the hypnotic effects of Ambien; • Ketoconazole and ritonavir may increase the sedative effects of the drug because they reduce the metabolism and zolpidem clearance; • Rifampicin decreases the plasma concentration of zolpidem and, therefore, its effect (this is due to increased metabolism); • Anxiolytics (tranquilizers) benzodiazepine derivatives used in conjunction with Ambien increase the risk of developing drug addiction; • Alcohol enhances the inhibitory effect of the drug on the central nervous system.

Special Notes

Due to its CNS depressant effect and rapid onset of effects, Ambien must be taken immediately before bedtime. Although clinical studies have not shown a suppressive effect of zolpidem on breathing, patients with respiratory impairment should use the medication with caution. Ambien may further reduce muscle tone in patients with myasthenia gravis. Therefore, they should be under close medical supervision during treatment. Long-term Ambien use increases the risk of addiction. So, you should limit the duration of taking sleeping pills to 2-3 weeks. If your sleep does not improve during this time, it is recommended to consult a doctor again. When used in therapeutic doses for more than 4 weeks, treatment should be discontinued gradually. During the treatment period, try to refrain from engaging in potentially hazardous activities that require enhanced concentration and speed of psychomotor reactions.

Side Effects

Ambien is usually well tolerated by patients. But side effects from treatment are still possible: • Daytime sleepiness; • Decreased vigilance; • Fatigue; • Dizziness; • Headache; • Depression; • Muscle weakness; • Back pain; • Nausea; • Vomiting; • Diarrhea; • Stomach ache; • Skin reactions, etc. Using the drug in strict accordance with the doctor’s recommendations minimizes the risk of side effects. In addition, side reactions practically do not appear when taking the drug immediately before bedtime.