Comparison of pharmacokinetic profiles of zolpidem buffered sublingual tablet and zolpidem oral immediate-release tablet: Results from a single-center, single-dose, randomized, open-label crossover study in healthy adults

Clinical Therapeutics

Volumn 35, Issue 5, 2013, Pages 604-611

  Greenblatt, David J ^a   Harmatz, Jerold S ^a   Roth, Thomas ^b   Singh, Nikhilesh N ^c   Moline, Margaret L ^d   Harris, Stephen C ^d   Kapil, Ram P ^d  

^a TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b HENRY FORD HOSPITAL   (United States)

^c Transcept Pharmaceuticals Inc   (United States)

^d PURDUE PHARMA L P   (United States)

Author keywords

Gender; Insomnia; Middle of the night awakening; Pharmacokinetics; Sublingual zolpidem tartrate

Indexed keywords

ZOLPIDEM;

ADULT; AREA UNDER THE CURVE; ARTICLE; BODY WEIGHT; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG ABSORPTION; DRUG CLEARANCE; DRUG DOSAGE FORM COMPARISON; DRUG FORMULATION; DRUG RELEASE; FEMALE; HUMAN; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; OPEN STUDY; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE;

ADMINISTRATION, ORAL; ADMINISTRATION, SUBLINGUAL; ADOLESCENT; ADULT; AREA UNDER CURVE; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HUMANS; HYPNOTICS AND SEDATIVES; MALE; MIDDLE AGED; PYRIDINES; SEX FACTORS; TABLETS; TIME FACTORS; YOUNG ADULT;

EID: 84877920042     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2013.03.007     Document Type: Article

References (21)

1. Greenblatt D.J., Roth T. Zolpidem for insomnia. Expert Opin Pharmacother 2012, 13:879-893.
2. Moen M.D., Plosker G.L. Zolpidem extended-release. CNS Drugs 2006, 20:419-426.
3. Barkin R.L. Zolpidem extended-release: a single insomnia treatment option for sleep induction and sleep maintenance symptoms. Am J Ther 2007, 14:299-305.
4. Owen R.T. Novel zolpidem formulations. Drugs Today (Barc) 2009, 45:395-400.
5. Intermezzo (zolpidem tartrate sublingual tablet) [full prescribing information], Accessed January 15, 2013. http://app.purduepharma.com/xmlpublishing/pi.aspx?id=i.
6. Lankford A. Sublingual zolpidem tartrate lozenge for the treatment of insomnia. Expert Rev Clin Pharmacol 2009, 2:333-337.
7. Langtry H.D., Benfield P. Zolpidem. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential. Drugs 1990, 40:291-313.
8. Salvà P., Costa J. Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications. Clin Pharmacokinet 1995, 29:142-153.
9. von Moltke L.L., Greenblatt D.J., Granda B.W., et al. Zolpidem metabolism in vitro: responsible cytochromes, chemical inhibitors, and in vivo correlations. Br J Clin Pharmacol 1999, 48:89-97.
10. Greenblatt D.J., Harmatz J.S., von Moltke L.L., et al. Comparative kinetics and response to the benzodiazepine agonists triazolam and zolpidem: evaluation of sex-dependent differences. J Pharmacol Exp Ther 2000, 293:435-443.
11. Olubodun J.O., Ochs H.R., von Moltke L.L., et al. Pharmacokinetic properties of zolpidem in elderly and young adults: possible modulation by testosterone in men. Br J Clin Pharmacol 2003, 56:297-304.
12. Roth T., Mayleben D., Corser B.C., Singh N.N. Daytime pharmacodynamic and pharmacokinetic evaluation of low-dose sublingual transmucosal zolpidem hemitartrate. Hum Psychopharmacol 2008, 23:13-20.
13. Greenblatt D.J., Roth T. Zolpidem tartrate sublingual tablet c-IV: PK/PD profile supports middle-of-the-night dosing of 1.75 mg in women and 3.5 mg in men. Presented at: 165th Annual Meeting of the American Psychiatric Association; May 5-9 2012, Philadelphia, Pa. Abstract.
14. Roth T., Hull S.G., Lankford D.A., et al. Low-dose sublingual zolpidem tartrate is associated with dose-related improvement in sleep onset and duration in insomnia characterized by middle-of-the-night (MOTN) awakenings. Sleep 2008, 31:1277-1284. Intermezzo Study Group.
15. Greenblatt D.J., Legangneux E., Harmatz J.S., et al. Dynamics and kinetics of a modified-release formulation of zolpidem: comparison with immediate-release standard zolpidem and placebo. J Clin Pharmacol 2006, 46:1469-1480.
16. Greenblatt D.J., Harmatz J.S., von Moltke L.L., et al. Comparative kinetics and dynamics of zaleplon, zolpidem, and placebo. Clin Pharmacol Ther 1998, 64:553-561.
17. Cotreau M.M., von Moltke L.L., Greenblatt D.J. The influence of age and sex on the clearance of cytochrome P450 3A substrates. Clin Pharmacokinet 2005, 44:33-60.
18. Greenblatt D.J., von Moltke L.L. Gender has a small but statistically significant effect on clearance of CYP3A substrate drugs. J Clin Pharmacol 2008, 48:1350-1355.
19. Chetty M., Mattison D., Rostami-Hodjegan A. Sex differences in the clearance of CYP3A4 substrates: exploring possible reasons for the substrate dependency and lack of consensus. Curr Drug Metab 2012, 13:778-786.
20. de Haas S.L., Schoemaker R.C., van Gerven J.M., et al. Pharmacokinetics, pharmacodynamics and the pharmacokinetic/pharmacodynamic relationship of zolpidem in healthy subjects. J Psychopharmacol 2010, 24:1619-1629.
21. FDA Drug Safety Communication: Risk of Next-Morning Impairment After Use of Insomnia Drugs; FDA Requires Lower Recommended Doses for Certain Drugs Containing Zolpidem (Ambien, Ambien CR, Edluar, and Zolpimist) Food and Drug Administration, US Dept Health and Human Services, Accessed January 15, 2013. http://www.fda.gov/drugs/drugsafety/UCM334033.htm.