Zolpidem: Uses, Interactions, Mechanism of Action | DrugBank Online

Step 2

Lemmer B: The sleep-wake cycle and sleeping pills. Physiol Behav. 2007 Feb 28;90(2-3):285-93. Epub 2006 Oct 16. [Article] Depoortere H, Zivkovic B, Lloyd KG, Sanger DJ, Perrault G, Langer SZ, Bartholini G: Zolpidem, a novel nonbenzodiazepine hypnotic. I. Neuropharmacological and behavioral effects. J Pharmacol Exp Ther. 1986 May;237(2):649-58. [Article] Clauss RP, Guldenpfennig WM, Nel HW, Sathekge MM, Venkannagari RR: Extraordinary arousal from semi-comatose state on zolpidem. A case report. S Afr Med J. 2000 Jan;90(1):68-72. [Article] Schlich D, L'Heritier C, Coquelin JP, Attali P, Kryrein HJ: Long-term treatment of insomnia with zolpidem: a multicentre general practitioner study of 107 patients. J Int Med Res. 1991 May-Jun;19(3):271-9. [Article] Maarek L, Cramer P, Attali P, Coquelin JP, Morselli PL: The safety and efficacy of zolpidem in insomniac patients: a long-term open study in general practice. J Int Med Res. 1992 Apr;20(2):162-70. [Article] Swainston Harrison T, Keating GM: Zolpidem: a review of its use in the management of insomnia. CNS Drugs. 2005;19(1):65-89. doi: 10.2165/00023210-200519010-00008. [Article] Salva P, Costa J: Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications. Clin Pharmacokinet. 1995 Sep;29(3):142-53. doi: 10.2165/00003088-199529030-00002. [Article] Fitzgerald AC, Wright BT, Heldt SA: The behavioral pharmacology of zolpidem: evidence for the functional significance of alpha1-containing GABA(A) receptors. Psychopharmacology (Berl). 2014 May;231(9):1865-96. doi: 10.1007/s00213-014-3457-x. Epub 2014 Feb 22. [Article] Du B, Shan A, Zhang Y, Zhong X, Chen D, Cai K: Zolpidem arouses patients in vegetative state after brain injury: quantitative evaluation and indications. Am J Med Sci. 2014 Mar;347(3):178-82. doi: 10.1097/MAJ.0b013e318287c79c. [Article] Guo T, Mao G, Zhao L, Xia D, Yang L: Comparative pharmacokinetics of zolpidem tartrate in five ethnic populations of China. Acta Pharm Sin B. 2014 Apr;4(2):146-50. doi: 10.1016/j.apsb.2014.02.001. Epub 2014 Mar 15. [Article] Tan KR, Rudolph U, Luscher C: Hooked on benzodiazepines: GABAA receptor subtypes and addiction. Trends Neurosci. 2011 Apr;34(4):188-97. doi: 10.1016/j.tins.2011.01.004. Epub 2011 Feb 25. [Article] Vlainic J, Pericic D: Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam. Neuropharmacology. 2009 Jun;56(8):1124-30. doi: 10.1016/j.neuropharm.2009.03.010. Epub 2009 Apr 1. [Article] Crestani F, Martin JR, Mohler H, Rudolph U: Mechanism of action of the hypnotic zolpidem in vivo. Br J Pharmacol. 2000 Dec;131(7):1251-4. doi: 10.1038/sj.bjp.0703717. [Article] FDA Drug Safety Communication: FDA approves new label changes and dosing for zolpidem products and a recommendation to avoid driving the day after using Ambien CR [Link] NIH Stat Pearls, Internet: Zolpidem [Link] Questions and Answers: 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) [Link] FDA Approved Drug Products: Ambien (zolpidem tartrate) oral tablets [Link] Ambien CR (extended release) label [File]

Step 3

Vlainic J, Pericic D: Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam. Neuropharmacology. 2009 Jun;56(8):1124-30. doi: 10.1016/j.neuropharm.2009.03.010. Epub 2009 Apr 1. [Article] Smith AJ, Alder L, Silk J, Adkins C, Fletcher AE, Scales T, Kerby J, Marshall G, Wafford KA, McKernan RM, Atack JR: Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux. Mol Pharmacol. 2001 May;59(5):1108-18. [Article] Pritchett DB, Seeburg PH: Gamma-aminobutyric acidA receptor alpha 5-subunit creates novel type II benzodiazepine receptor pharmacology. J Neurochem. 1990 May;54(5):1802-4. [Article] Sramka M, Nadvornik P: Surgical complication of posterior hypothalamotomy. Confin Neurol. 1975;37(1-3):193-4. [Article] Tan KR, Rudolph U, Luscher C: Hooked on benzodiazepines: GABAA receptor subtypes and addiction. Trends Neurosci. 2011 Apr;34(4):188-97. doi: 10.1016/j.tins.2011.01.004. Epub 2011 Feb 25. [Article]

Step 4

Pritchett DB, Seeburg PH: Gamma-aminobutyric acidA receptor alpha 5-subunit creates novel type II benzodiazepine receptor pharmacology. J Neurochem. 1990 May;54(5):1802-4. [Article] Smith AJ, Alder L, Silk J, Adkins C, Fletcher AE, Scales T, Kerby J, Marshall G, Wafford KA, McKernan RM, Atack JR: Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux. Mol Pharmacol. 2001 May;59(5):1108-18. [Article] Vlainic J, Pericic D: Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam. Neuropharmacology. 2009 Jun;56(8):1124-30. doi: 10.1016/j.neuropharm.2009.03.010. Epub 2009 Apr 1. [Article] Crestani F, Martin JR, Mohler H, Rudolph U: Mechanism of action of the hypnotic zolpidem in vivo. Br J Pharmacol. 2000 Dec;131(7):1251-4. doi: 10.1038/sj.bjp.0703717. [Article] Tan KR, Rudolph U, Luscher C: Hooked on benzodiazepines: GABAA receptor subtypes and addiction. Trends Neurosci. 2011 Apr;34(4):188-97. doi: 10.1016/j.tins.2011.01.004. Epub 2011 Feb 25. [Article]

Step 5

Pritchett DB, Seeburg PH: Gamma-aminobutyric acidA receptor alpha 5-subunit creates novel type II benzodiazepine receptor pharmacology. J Neurochem. 1990 May;54(5):1802-4. [Article] Smith AJ, Alder L, Silk J, Adkins C, Fletcher AE, Scales T, Kerby J, Marshall G, Wafford KA, McKernan RM, Atack JR: Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux. Mol Pharmacol. 2001 May;59(5):1108-18. [Article] Vlainic J, Pericic D: Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam. Neuropharmacology. 2009 Jun;56(8):1124-30. doi: 10.1016/j.neuropharm.2009.03.010. Epub 2009 Apr 1. [Article] Crestani F, Martin JR, Mohler H, Rudolph U: Mechanism of action of the hypnotic zolpidem in vivo. Br J Pharmacol. 2000 Dec;131(7):1251-4. doi: 10.1038/sj.bjp.0703717. [Article] Tan KR, Rudolph U, Luscher C: Hooked on benzodiazepines: GABAA receptor subtypes and addiction. Trends Neurosci. 2011 Apr;34(4):188-97. doi: 10.1016/j.tins.2011.01.004. Epub 2011 Feb 25. [Article]

Step 6

Hadingham KL, Garrett EM, Wafford KA, Bain C, Heavens RP, Sirinathsinghji DJ, Whiting PJ: Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors. Mol Pharmacol. 1996 Feb;49(2):253-9. [Article] Vlainic J, Pericic D: Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam. Neuropharmacology. 2009 Jun;56(8):1124-30. doi: 10.1016/j.neuropharm.2009.03.010. Epub 2009 Apr 1. [Article] Criswell HE, Simson PE, Knapp DJ, Devaud LL, McCown TJ, Duncan GE, Morrow AL, Breese GR: Effect of zolpidem on gamma-aminobutyric acid (GABA)-induced inhibition predicts the interaction of ethanol with GABA on individual neurons in several rat brain regions. J Pharmacol Exp Ther. 1995 Apr;273(1):526-36. [Article]

Step 7

Cubala WJ, Wiglusz M, Burkiewicz A, Galuszko-Wegielnik M: Zolpidem pharmacokinetics and pharmacodynamics in metabolic interactions involving CYP3A: sex as a differentiating factor. Eur J Clin Pharmacol. 2010 Sep;66(9):955; author reply 957-8. doi: 10.1007/s00228-010-0854-x. Epub 2010 Jun 16. [Article] Galitz LA, Jayawardena S, Furey SA: Pharmacokinetic effects of simultaneous administration of single-dose gabapentin 500 mg and zolpidem tartrate 10 mg in healthy volunteers: a randomized, open-label, crossover trial. Drugs R D. 2015 Mar;15(1):71-7. doi: 10.1007/s40268-014-0079-z. [Article] Ambien FDA label [File]

Step 8

Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [Article] Von Moltke LL, Greenblatt DJ, Granda BW, Duan SX, Grassi JM, Venkatakrishnan K, Harmatz JS, Shader RI: Zolpidem metabolism in vitro: responsible cytochromes, chemical inhibitors, and in vivo correlations. Br J Clin Pharmacol. 1999 Jul;48(1):89-97. [Article] Inagaki T, Miyaoka T, Tsuji S, Inami Y, Nishida A, Horiguchi J: Adverse reactions to zolpidem: case reports and a review of the literature. Prim Care Companion J Clin Psychiatry. 2010;12(6). doi: 10.4088/PCC.09r00849bro. [Article]

Step 9

Byeon JY, Kim YH, Kim SH, Lee CM, Jung EH, Chae WK, Jang CG, Lee SY, Lee YJ: The influences of CYP2C9*1/*3 genotype on the pharmacokinetics of zolpidem. Arch Pharm Res. 2018 Sep;41(9):931-936. doi: 10.1007/s12272-018-1070-y. Epub 2018 Sep 3. [Article] Von Moltke LL, Greenblatt DJ, Granda BW, Duan SX, Grassi JM, Venkatakrishnan K, Harmatz JS, Shader RI: Zolpidem metabolism in vitro: responsible cytochromes, chemical inhibitors, and in vivo correlations. Br J Clin Pharmacol. 1999 Jul;48(1):89-97. [Article]

Step 10

Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article] Barkin RL: Zolpidem extended-release: a single insomnia treatment option for sleep induction and sleep maintenance symptoms. Am J Ther. 2007 May-Jun;14(3):299-305. doi: 10.1097/MJT.0b013e31804c7292. [Article] Von Moltke LL, Greenblatt DJ, Granda BW, Duan SX, Grassi JM, Venkatakrishnan K, Harmatz JS, Shader RI: Zolpidem metabolism in vitro: responsible cytochromes, chemical inhibitors, and in vivo correlations. Br J Clin Pharmacol. 1999 Jul;48(1):89-97. [Article] Byeon JY, Kim YH, Kim SH, Lee CM, Jung EH, Chae WK, Jang CG, Lee SY, Lee YJ: The influences of CYP2C9*1/*3 genotype on the pharmacokinetics of zolpidem. Arch Pharm Res. 2018 Sep;41(9):931-936. doi: 10.1007/s12272-018-1070-y. Epub 2018 Sep 3. [Article]

Step 11

Byeon JY, Kim YH, Kim SH, Lee CM, Jung EH, Chae WK, Jang CG, Lee SY, Lee YJ: The influences of CYP2C9*1/*3 genotype on the pharmacokinetics of zolpidem. Arch Pharm Res. 2018 Sep;41(9):931-936. doi: 10.1007/s12272-018-1070-y. Epub 2018 Sep 3. [Article] Pichard L, Gillet G, Bonfils C, Domergue J, Thenot JP, Maurel P: Oxidative metabolism of zolpidem by human liver cytochrome P450S. Drug Metab Dispos. 1995 Nov;23(11):1253-62. [Article]