Zaleplon

Sample preparation Evaporate 100 [xL 1 p,g/mL IS in MeOH in the bottom of a tube using a stream of nitrogen, add 1 mL whole blood, add 1 mL buffer, vortex for 1 min, add 5 mL dichloromethane hexane ethyl acetate 50 40 10, shake horizontally at 200 cycles/min for 30 min, centrifuge at 2000 rpm for 30 min. Evaporate the organic layer to dryness under a stream of nitrogen, reconstitute the residue with 100 xL initial mobile phase, inject an aliquot. (Prepare the buffer by adjusting the pH of 1 L saturated ammonium chloride solution to 9.5 with 25% ammonium hydroxide.) 

Mobile phase Gradient. MeCN l mM pH 4.0 ammonium formate buffer 10 90 for 2 min, to 60 40 over 15 min, maintain at 60 40 for 3 min, return to initial conditions over 1 min, 

Detector MS, PE Sciex API 150EX, single quadrupole, turbo ionspray, atmospheric pressure ionization, positive mode, heater gas nitrogen, ionspray 5000 V, nebulizer gas nitrogen at 1.2 L/min, curtain gas nitrogen at 1.0 L/min, turbo probe 475°, orifice 35 V, ring 175 V, m/z 306.21 

Giroud, C. Augsburger, M. Menetrey, A. Mangin, P. Determination of zaleplon and zolpidem by liquid chromatography-turbo-ionspray mass spectrometry application to forensic cases, J.Chromatogr.B, 2003, 789, 131-138. 

Sample preparation Add IS to 200 ixL plasma, add 400 ixL MeCN, vortex, centrifuge, inject an aliquot of the supernatant. 

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A class of sedative/hypnotic type drug that exert their effects through the benzodiazepine binding site on GABAa receptors. The class consists both of molecules that contain the benzodiazepine moiety, for example diazepam, lorazepam and flunitrazepam, and the newer, non-benzodiazepine compounds such as zolpidem, zopiclone, indiplon and zaleplon. BzRAs are primarily used for the treatment of anxiety, insomnia and to elicit varying levels of sedation. The wide selection of compounds currently available affords the prescribing clinician extensive options in terms of relative efficacies and durations of action. 

Zaleplon, a miscellaneous sedative, is the first prescription sleep preparation that the patient can take, later in the night, if you have at least 4 hours in bed before you become active again. With zaleplon the patient will fall asleep quickly and wake up with little or no aftereffects of the drug. 

Zaleplon may be taken at bedtime or later in die night if the you have at least 4 hours of bedtime left. You will still wake up naturally without excessive drowsiness in the morning. 

Zaleplon should not be given with a high fat meal or snack because fat interferes with absorption of the drug. 

C2H5I 75-03-6) see Butibufen Cinoxacin Diethylstilbestrol Enoxacin Ethotoin Gallamine triethiodide Imiquimod Lomefloxacin Mosapride citrate Nalidixic acid Oxolinic acid Pefloxacin Pipemidic acid Tridihexethyl chloride Zaleplon... 

The two selective GABA j receptor agonists currently marketed in the United States, zaleplon and Zolpidem, are a pyrazolopyrimidine and a imidaz-opyridine, respectively. Both of these drugs are approved only for the shortterm treatment of insomnia. 

Limited results from clinical laboratory evaluations suggested that the GABAj l agonists zaleplon (Rush et al. 1999b) and Zolpidem (Rush et al. 1999a) produce effects that are consistent with abuse potential comparable to that of the benzodiazepine triazolam. The reported incidence of dependence on Zolpidem in the medical literature is low, compared with that for benzodiazepines, and is characterized by use of high doses, often in individuals with a history of substance abuse (Hajak et al. 2003 Vartzopoulos et al. 2000). 

Ator NA, Weerts EM, Kaminski BJ, et al Zaleplon and triazolam physical dependence assessed across increasing doses under a once-daily dosing regimen in baboons. Drug Alcohol Depend 61 69-84, 2000... 

Greenblatt DJ, Harmatz JS, von Moltke LL, et al Comparative kinetics and dynamics of zaleplon, zolpidem, and placebo. Clin Pharmacol Ther 64 553-561, 1998... 

Benzodiazepine receptor agonists, including traditional benzodiazepines, zolpidem, zaleplon, and eszopiclone, are approved... 

Zaleplon (Sonata ) 1 6 5-10 Oxidation — Short-acting, only for difficulty falling asleep... 

Zaleplon also binds to the GABAa receptor. It has a rapid onset, a half-life of about 1 hour, and no active metabolites. It does not reduce nighttime awakenings or increase the total sleep time. It may be best used for middle-of-the-night awakenings. It does not appear to cause significant rebound insomnia or next-day psychomotor impairment. The most common side effects are dizziness, headache, and somnolence. The recommended dose is 10 mg (5 mg in the elderly). 

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