Distinguished by the structure from benzodiazepines, zolpidem has a sedative effect, and the anxiolytic, anticonvulsant and central muscle relaxant action is expressed only slightly.
According to the classification allosteric sites of the complex gamma-aminobutyric acid testosterone enanthate injection, which bind benzodiazepines are called ω-modulating sites or receptors. To date, three subtypes have been identified: 1, 2 and 3. In contrast to the benzodiazepines, which non-selectively bind and activate all three subtypes of ω-receptor zolpidem binds selectively to ω1-receptor, therefore sedative effect of the drug observed at lower doses than necessary for the development miorelaksiruyuschego, anticonvulsant and anxiolytic effect.
ω1-receptors are mainly in the fourth layer of the sensory cortex, the cerebellum, pons and lower tubercles quadrigemina.
Zolpidem showed low affinity for the ω 2 receptor (lumbar spine, the hippocampus) and ω3-receptor (certain peripheral regions). Modern experience shows that the pharmacological effect of zolpidem is different from the action of benzodiazepines.
Interaction with ω-receptors leads to neuronal ionoformnyh opening channels for chlorine ions.
The effect comes quickly. It shortens time to fall asleep, reduce the number of night awakenings, increases total sleep duration and improves its quality. Extend stage II sleep and deep-sleep stage.
The pharmacokinetics of zolpidem is rapidly absorbed from the gastrointestinal tract . After taking a dose of 5 mg and 10 mg of the maximum concentration in blood is respectively 59 ng / ml and 121 ng / ml, the time to reach maximum concentration of 0.5 to 3 hours . in the presence of food in the stomach zolpidem absorption slightly slowed down. in order to accelerate sleep onset, zolpidem should not be taken with food or shortly after ingestion. The pharmacokinetics of zolpidem remains unchanged for several weeks of use. Bioavailability zolpidem is 70% protein binding plasma – 92%. There is a linear relationship between dose size and the drug concentration in blood plasma zolpidem. Metabolized in the liver to form the three inactive metabolites that are excreted by the kidneys (approximately 60%) and in the intestine testosterone enanthate injectionis zolpidem from 0.7 to 3.5 hours (in average about 2.4 hours). The total clearance zolpidem is 0.26 l / h / kg, a volume of distribution of 0.54 l / kg. Do not induce liver enzymes. Koumouliruet not. In the elderly in plasma clearance may be reduced without a substantial increase in is increased by 50%. In patients with severe renal clearance increases slightly. In patients with liver dysfunction increases the bioavailability, increases to 10 hours.
Sleep disorders: difficulty falling asleep, waking up early and the night.
• hypersensitivity to zolpidem or any other components of the drug;
• severe, acute or chronic liver failure;
• sleep apnea syndrome;
• acute and / or severe respiratory insufficiency;
• pregnancy (I trimester) and breastfeeding;
• the age of 18 years ( efficacy and safety have not been established);
• lactase deficiency, lactose intolerance, glucose-galactose syndrome malabsorption;
• myasthenia gravis.
Hepatic insufficiency of mild to moderate severity, depression, alcoholism, drug addiction and other addictions, pregnancy II and III trimester, respiratory failure and mild to moderate severity, patients with mental illness.
Application of pregnancy and during breastfeeding
The drug testosterone enanthate injection is contraindicated for use in the I trimester of pregnancy.
If necessary, the appointment trimester of pregnancy should carefully evaluate the potential benefits of therapy for the mother and the potential risk to the fetus and newborn.Studies in animals have not revealed teratogenic and embryotoxic action of the drug.
Women of childbearing age receiving the drug, should be warned about the need to seek medical attention in the event of planned or ensuing pregnancy, and during treatment with patients should use reliable methods of contraception. In the case of admission zolpidem at the end of pregnancy or during childbirth (even at low doses) may develop in the newborn hypothermia, transient respiratory depression or apnea, axial hypotonia, hypotension, as well as violations of sucking. in addition, children born to mothers who long took sedatives / hypnotic drugs in late pregnancy, may form a physical dependence, and there is a risk of “cancellation” syndrome in the postnatal period. Zolpidem is released in breast milk, so is contraindicated during breast-feeding, if you must use Sanval drug ® during lactation, breast feeding should be discontinued.
Dosing and Administration
The drug is intended for oral administration, 1 time per day just before bedtime, with some liquid, after a short period of time after eating. The recommended adult dose should not exceed 10 mg per day. Each patient must be the appointment of the most effective minimum dose.
Patients in the application should assume that they can afford uninterrupted sleep for 7-8 hours.
Dosage and duration of treatment are determined by the attending physician. You must strictly adhere to the doctor’s instructions and do not exceed the prescribed doctor dosetestosterone enanthate injection.
The maximum daily dose for adults is 10 mg.
For patients of advanced age (over 65 years), debilitated patients, and patients with hepatic insufficiency, the starting dose is 5 mg; if necessary (insufficient clinical effect) and good tolerability of the drug dose may be increased to 10 mg.
The treatment should not exceed 4 weeks. When transient insomnia, the recommended course of treatment – 2-5 days, situational -. 2-3 weeks
Short periods of treatment does not require the gradual withdrawal of the drug.
In the case of long-term use of the drug to reduce the possibility of “rebound” insomnia cancellation of zolpidem should be done gradually (first reduction daily dose and then removal of the drug).