Product Name: Ambien
Common Brand Names: Stilnoct; Stilnox; Zoldem
Pharmaceutical Category: Sleep Aid
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There is an additional general information about this medication active ingredient zolpidem:
Ambien is a sleeping drug from the group of imidazopyridine, specific agonist of omega1-receptors in CNS. It shortens the time to sleep, reduces the number of nighttime awakenings, increased sleep duration and improves its quality. This medication extends phase II of sleep, phases III and IV of deep sleep, does not affect the duration of REM sleep. Zolpidem characterized also by a central muscle relaxant and anticonvulsant effects.
After oral administration, Cmax plasma levels observed after 0.5-3 hours. Bioavailability is approximately 70%. Plasma protein binding is 92%. There is a linear relationship between the magnitude of the dose and concentration of the active substance in the plasma. Vd is 0.52-0.56 L / kg.
Zolpidem is metabolized in the liver and in the form of inactive metabolites are excreted in the urine (56%) and feces (37%). It does not induce liver enzymes.
T1/2 is from 0.7 hours to 3.5 hours (mean is 2.4 h).
In elderly patients may decreases plasma clearance of zolpidem, while T1/2 increased slightly (to an average of 3 hours), Cmax increased by 50%, Vd decreased to 0.29-0.39 L / kg.
In patients with severe renal impairment the clearance of zolpidem is reduced slightly, other pharmacokinetic parameters were not changed.
In patients with severe liver dysfunction increases the bioavailability of zolpidem, clearance is somewhat reduced, T1/2 increases to 10 hours.
Why is Ambien prescribed?
Episodic, transient and chronic insomnia.
Dosage and administration
For oral administration for adults aged under 65 years a single dose is 10 mg, if necessary, may increases to 15-20 mg. For patients older than 65 years or with concomitant hepatic insufficiency initial single dose is 5 mg. Zolpidem is taken just before bedtime. The course of treatment is from several days to 4 weeks. Maximum dose is 10 mg / day.
Ambien side effects
Digestive system: in some cases - abdominal pain, nausea, vomiting, diarrhea.
CNS and peripheral nervous system: depending on the dose and individual sensitivity (especially in elderly patients) - vertigo, imbalance, ataxia, headache, daytime sleepiness, distraction, muscle weakness, double vision, anterograde amnesia, paradoxical or mental disorders; also it is possible ricochet insomnia when used in high doses or long-term treatment.
Allergic reactions: skin rash, itching.
Other: rarely - violation of sexual desire; development of addiction, the formation of psychic and physical dependence (when applying for a few weeks).
Severe respiratory failure, nocturnal apnea, severe hepatic insufficiency, childhood and adolescence to 15 years, I trimester of pregnancy, lactation (breastfeeding), increased sensitivity to zolpidem.
Using during pregnancy and breastfeeding
Zolpidem is contraindicated in pregnancy and lactation (breastfeeding).
Ambien is not recommended for use with myasthenia gravis.
With careful use in patients with respiratory failure. In case of insufficiency of liver function may be necessary to decrease the dose.
If you cancel the therapy dose should be reduced gradually. The likelihood of habituation increases with prolonged use of zolpidem.
Avoid alcohol during the period of treatment.
During the period of treatment should refrain from potentially hazardous activities that require concentration and a high speed of psychomotor reactions.
Zolpidem drug interactions
When Ambien used with opioid analgesics, antitussives, barbiturates, antidepressants, sedatives, antihistamines, benzodiazepines, clonidine, neuroleptics, ethanol may develop symptoms of CNS depression and respiratory center.
When Ambien used with rifampicin, the concentration of zolpidem in the blood plasma, which is accompanied by a decrease in its hypnotic effect. Interaction is due to induction of isoenzyme CYP3A4.
Simultaneous administration with inducers of CYP3A4 isoenzyme (including with carbamazepine, phenytoin) may be possible reducing the concentration of zolpidem in the blood plasma.
Simultaneous administration with clozapine increases the risk of collapse, stop breathing and circulation.
Ambien in case of emergency / overdose
Symptoms: disturbance of consciousness (from lethargy to mild coma). There was recorded one case of cardiovascular and respiratory disorders; observed a full recovery after receiving doses of zolpidem tartrate up to 400 mg.
Treatment: immediate induction of vomiting or gastric lavage (depending on state), the appointment of activated carbon. Should abandon the use of any sedative drugs (even when expressed excitation). Hemodialysis is ineffective. Specific antidote is flumazenil (benzodiazepine receptor antagonist).