Summary: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.

Top Publications

  1. Klockowski P, Levy G. Kinetics of drug action in disease states. XXV. Effect of experimental hypovolemia on the pharmacodynamics and pharmacokinetics of desmethyldiazepam. J Pharmacol Exp Ther. 1988;245:508-12 pubmed
    ..Thus, the pharmacodynamics as well as the pharmacokinetics of a benzodiazepine are altered by hypovolemia. ..
  2. Liu J, Zhang Y. [Determination of N-demethyldiazepam and its metabolite oxazepam in plasma by HPLC and their pharmacokinetics in rats]. Yao Xue Xue Bao. 1995;30:655-61 pubmed was investigated by this method. The concentration-time curve was fitted to a two-compartment open model. Its main pharmacokinetic parameters were: Tmax = 0.24 h, Cmax = 1211.78, T1/2 beta = 2.84 h, AUC = 1264 ..
  3. Fiers T, Maes V, Sevens C. Automation of toxicological screenings on a Hewlett Packard Chemstation GC-MS system. Clin Biochem. 1996;29:357-61 pubmed
    ..The incorporation of a rule-based decision support system enhances the quality of the GC-MS toxicological screenings and results in faster, easier, and more reliable processing. ..
  4. Fishbain D, Lewis J, Gao J, Cole B, Rosomoff R. Alleged breaches of "standards of medical care" in a patient overdose death possibly related to chronic opioid analgesic therapy, application of the controlled substances model guidelines: case report. Pain Med. 2009;10:565-72 pubmed publisher
  5. Greenblatt D, Harmatz J, Friedman H, Locniskar A, Shader R. A large-sample study of diazepam pharmacokinetics. Ther Drug Monit. 1989;11:652-7 pubmed
    ..Parametric statistical testing procedures and pharmacokinetic forecasting schemes may be improved by more precise delineation of the underlying distributions for pharmacokinetic variables. ..
  6. Inaba T, Tait A, Nakano M, Mahon W, Kalow W. Metabolism of diazepam in vitro by human liver. Independent variability of N-demethylation and C3-hydroxylation. Drug Metab Dispos. 1988;16:605-8 pubmed
    ..This variability is consistent with the presence of at least two different cytochrome P-450 species controlling formation of these metabolites. In the same livers, Vmax for NDZ and TMZ production varied 6-fold and 15-fold, respectively. ..
  7. Reubsaet K, Ragnar Norli H, Hemmersbach P, Rasmussen K. Determination of benzodiazepines in human urine and plasma with solvent modified solid phase micro extraction and gas chromatography; rationalisation of method development using experimental design strategies. J Pharm Biomed Anal. 1998;18:667-80 pubmed
    ..This method offers sufficient enrichment for bioanalysis after a single dose of high dose benzodiazepines as diazepam, but for low dose benzodiazepines as flunitrazepam, further sensitivity is needed. ..
  8. Oliveira Silva D, Oliveira C, Mendes G, Galvinas P, Barrientos Astigarraga R, De Nucci G. Quantification of chlordesmethyldiazepam by liquid chromatography-tandem mass spectrometry: application to a cloxazolam bioequivalence study. Biomed Chromatogr. 2009;23:1266-75 pubmed publisher
    ..The pharmacokinetic profiles indicated bioequivalence since all ratios were as proposed by FDA and ANVISA. ..
  9. Wasilewski D, Matsumoto H, Kur E, Dziklińska A, Woźny E, Stencka K, et al. Assessment of diazepam loading dose therapy of delirium tremens. Alcohol Alcohol. 1996;31:273-8 pubmed
    ..The results show a large efficacy of the loading dose method corresponding to substantial reduction of the psychosis duration (fivefold in comparison to the control group). The method proved to be safe, with no significant complications...

More Information

Publications108 found, 100 shown here

  1. Acikgöz A, Karim N, Giri S, Schmidt Heck W, Bader A. Two compartment model of diazepam biotransformation in an organotypical culture of primary human hepatocytes. Toxicol Appl Pharmacol. 2009;234:179-91 pubmed publisher
  2. Sohn D, Kusaka M, Ishizaki T, Shin S, Jang I, Shin J, et al. Incidence of S-mephenytoin hydroxylation deficiency in a Korean population and the interphenotypic differences in diazepam pharmacokinetics. Clin Pharmacol Ther. 1992;52:160-9 pubmed
  3. Yasar S, Bergman J, Munzar P, Redhi G, Tober C, Knebel N, et al. Evaluation of the novel antiepileptic drug, AWD 131-138, for benzodiazepine-like discriminative stimulus and reinforcing effects in squirrel monkeys. Eur J Pharmacol. 2003;465:257-65 pubmed
    ..The failure of AWD 131-138 to produce benzodiazepine-like discriminative effects and the absence of drug self-administration behavior when substituted for cocaine suggest that its abuse liability is low. ..
  4. St Pierre M, Pang K. Kinetics of sequential metabolism. I. Formation and metabolism of oxazepam from nordiazepam and temazepam in the perfused murine liver. J Pharmacol Exp Ther. 1993;265:1429-36 pubmed
    ..abstract truncated at 250 words) ..
  5. Lamson M, Sitki Green D, Wannarka G, Mesa M, Andrews P, PELLOCK J. Pharmacokinetics of diazepam administered intramuscularly by autoinjector versus rectal gel in healthy subjects: a phase I, randomized, open-label, single-dose, crossover, single-centre study. Clin Drug Investig. 2011;31:585-597 pubmed publisher
    ..Results of the present study indicated that diazepam can be safely and reliably administered IM using a diazepam autoinjector. ..
  6. Mozayani A, Carter J, Nix R. Distribution of topiramate in a medical examiner's case. J Anal Toxicol. 1999;23:556-8 pubmed
    ..The cause of death was seizure disorder with upper respiratory infection. The manner of death was determined as natural. To our knowledge, this is the first report of the presence of topiramate in postmortem specimens. ..
  7. Djeridane Y, Touitou Y. Effects of diazepam and its metabolites on nocturnal melatonin secretion in the rat pineal and Harderian glands. A comparative in vivo and in vitro study. Chronobiol Int. 2003;20:285-97 pubmed
    ..The results also show that the control of melatonin production in the Harderian glands differ from that observed in the pineal gland. ..
  8. Lamka J, Jindrova O. Lymphatic bioavailability of diazepam and desmethyldiazepam in the rat. Physiol Res. 1996;45:23-9 pubmed
  9. Baillif Couniou V, Bartoli C, Sastre C, Chèze M, Deveaux M, Léonetti G, et al. Repeated attempted homicide by administration of drugs documented by hair analysis. J Forensic Leg Med. 2018;54:82-86 pubmed publisher
    ..been part of the victim's treatment were detected, as well as some benzodiazepines (alprazolam, bromazepam, nordazepam); cyamemazine was also detected in all the segments (9960/1610/2367) though only a single dose administration ..
  10. Kudo K, Nagata T, Kimura K, Imamura T, Noda M. Sensitive determination of diazepam and N-desmethyldiazepam in human material using capillary gas chromatography-mass spectrometry. J Chromatogr. 1988;431:353-9 pubmed
    ..0 ng/g to 1.0 microgram/g for diazepam and N-desmethyldiazepam. Using this method, trace amounts of diazepam and N-desmethyldiazepam were detected in the tissues of an autopsied individual. ..
  11. Rocca P, Beoni A, Eva C, Ferrero P, Zanalda E, Ravizza L. Peripheral benzodiazepine receptor messenger RNA is decreased in lymphocytes of generalized anxiety disorder patients. Biol Psychiatry. 1998;43:767-73 pubmed
    ..These results suggest that the turnover rate of pBR is reduced in PBMC of generalized anxiety disorder patients, and that this change occurs at the transcriptional level. ..
  12. Amano K, Takamatsu J, Ogata A, Katsuragi S, Miyazaki C, Deshimaru M, et al. Effect of dipotassium clorazepate on amygdaloid-kindling and comparison between amygdaloid- and hippocampal-kindled seizures in rats. Eur J Pharmacol. 1999;385:111-7 pubmed
    ..Thus, differences in effective dosages in both amygdaloid- and hippocampal-kindled seizures may suggest a difference in the neuronal mechanisms involved in this kindling. ..
  13. Holloway C, Kenyon C, Dowie L, Corrie J, Gray C, Fraser R. Effect of the benzodiazepines diazepam, des-N-methyldiazepam and midazolam on corticosteroid biosynthesis in bovine adrenocortical cells in vitro; location of site of action. J Steroid Biochem. 1989;33:219-25 pubmed
    ..The plasma concentrations required for these effects are high in relation to therapeutic levels but may be achieved, for example, during acute infusions or when they are used in combination with imidazole drugs such as cimetidine. ..
  14. Okiyama M, Ueno K, Ohmori S, Igarashi T, Kitagawa H. Imipramine treatment alters the pharmacokinetics and pharmacodynamics of diazepam. J Pharm Sci. 1987;76:880-5 pubmed
    ..The concomitant use of imipramine hydrochloride led to an increased antipentylenetetrazole effect of diazepam. This result is in accordance with the findings on brain concentrations of diazepam and its metabolites. ..
  15. Andersson T, Miners J, Veronese M, Birkett D. Diazepam metabolism by human liver microsomes is mediated by both S-mephenytoin hydroxylase and CYP3A isoforms. Br J Clin Pharmacol. 1994;38:131-7 pubmed
  16. Glover S, Allen K. Measurement of benzodiazepines in urine by liquid chromatography-tandem mass spectrometry: confirmation of samples screened by immunoassay. Ann Clin Biochem. 2010;47:111-7 pubmed publisher
    ..The lower limit of detection and assay specificity offers a longer window of detection and more detailed clinical information compared with immunoassay screening. ..
  17. Shou M, Mei Q, Ettore M, Dai R, Baillie T, Rushmore T. Sigmoidal kinetic model for two co-operative substrate-binding sites in a cytochrome P450 3A4 active site: an example of the metabolism of diazepam and its derivatives. Biochem J. 1999;340 ( Pt 3):845-53 pubmed
    ..Thus our results provide some new insights into the co-operative binding of two substrates in the inner portions of an allosteric CYP3A4 active site. ..
  18. de Haro L, Valli M, Bourdon J, Iliadis A, Hayek Lanthois M, Arditti J. Diazepam poisoning with one-month monitoring of diazepam and nordiazepam blood levels. Vet Hum Toxicol. 2001;43:174-5 pubmed
    ..The half-lives in this benzodiazepine overdose were longer than those seen with therapeutic doses. Benzodiazepines should not be readministrated when patients awake after suicide attempts. ..
  19. Kirvela O, Katila A, Aantaa R, Kanto J, Himberg J. Metabolic and subjective responses to oral diazepam and midazolam. Eur J Anaesthesiol. 1994;11:365-9 pubmed
    ..These results indicate that both diazepam and midazolam, in addition to their CNS effects, significantly decrease the overall metabolic rate and oxygen consumption in healthy volunteers. ..
  20. Yang T, Shou M, Korzekwa K, Gonzalez F, Gelboin H, Yang S. Role of cDNA-expressed human cytochromes P450 in the metabolism of diazepam. Biochem Pharmacol. 1998;55:889-96 pubmed
    ..Human liver microsomes converted DZ to both TMZ and NDZ at a ratio of 2:1. Our results suggest that hepatic CYP3A, 2C, and 2B6 enzymes have an important role in the metabolism of DZ by human liver. ..
  21. Verster J, Roth T. Blood drug concentrations of benzodiazepines correlate poorly with actual driving impairment. Sleep Med Rev. 2013;17:153-9 pubmed publisher
    ..Future driving studies should assess blood drug levels as a standard procedure, to enable further research into the relationship between blood drug concentration and performance impairment. ..
  22. Wong P. Characterization by saturation studies of the in vivo binding of [3H]flunitrazepam in mouse brain. Can J Physiol Pharmacol. 1991;69:176-80 pubmed
    ..The reduced binding may be explained by receptor occupancy by residual oxazepam. However, the low concentration of the residual oxazepam is an unlikely cause of the phenomenon of "acute tolerance" observed in these mice. ..
  23. Locniskar A, Greenblatt D, Harmatz J, Shader R. Bioinequivalence of a generic brand of diazepam. Biopharm Drug Dispos. 1989;10:597-605 pubmed
    ..Findings for desmethyldiazepam were similar. Thus, diazepam absorption from the generic brand of diazepam is significantly slower than from Valium, which in turn could lead to therapeutic inequivalence. ..
  24. Jing X, Wala E, Sloan J. Flunitrazepam and nordiazepam slowly released from silastic capsules induce physical dependence in rat. Drug Alcohol Depend. 1995;39:63-70 pubmed
    ..These data indicate that, as for DZ, the capsule implantation is an effective method of producing physical dependence on FN and ND in the rat. ..
  25. Wala E, Martin W, Sloan J. Pharmacokinetics of nordiazepam in physical dependence and precipitated abstinence in dogs. Pharmacol Biochem Behav. 1993;44:857-64 pubmed
    ..Reduced plasma clearance of ND and altered plasma protein binding were observed in dogs physically dependent upon ND. The benzodiazepine antagonist, flumazenil, significantly reduces steady-state plasma levels of total and free ND. ..
  26. Okamura T, Sugiura W, Miyazawa M. Reduction of oxazepam to desmethyldiazepam by human intestinal bacteria. Biol Pharm Bull. 1996;19:647-48 pubmed
    ..The biotransformation of oxazepam by Bifidobacterium bifidum was studied. The major metabolite was purified by chromatographic methods and found to be desmethyldiazepam using NMR, IR and other physicochemical data. ..
  27. Caraco Y, Tateishi T, Wood A. Interethnic difference in omeprazole's inhibition of diazepam metabolism. Clin Pharmacol Ther. 1995;58:62-72 pubmed
    ..The extent of the inhibitory effect of omeprazole on diazepam metabolism is dependent on ethnicity. Further studies are needed to determine the mechanism responsible for this phenomenon. ..
  28. Manani G, Facco E, Favero L, Favero G, Favero G, Berengo M, et al. Comparison by means of bispectral index score, between anxiolysis induced by diazepam and sedation induced by midazolam. Minerva Stomatol. 2011;60:365-81 pubmed
  29. Qin X, Xie H, Wang W, He N, Huang S, Xu Z, et al. Effect of the gene dosage of CgammaP2C19 on diazepam metabolism in Chinese subjects. Clin Pharmacol Ther. 1999;66:642-6 pubmed
    ..2 +/- 2.6 mL/min). The presence of a single-nucleotide polymorphism (G681A) of the CYP2C19 gene cosegregates with the impaired metabolism of diazepam and desmethyldiazepam among Chinese subjects in a gene-dosage effect manner. ..
  30. Musteata F, Musteata M, Pawliszyn J. Fast in vivo microextraction: a new tool for clinical analysis. Clin Chem. 2006;52:708-15 pubmed
    ..The proposed technique has several advantages and is suitable for fast clinical analyses. This approach could be used not only for drugs, but for any other endogenous or exogenous compounds. ..
  31. Pacifici G, Cuoci L, Placidi G. Placental transfer and distribution of pinazepam and its metabolite N-desmethyldiazepam in the maternal and fetal rabbit: effect of the stage of gestation. Eur J Drug Metab Pharmacokinet. 1989;14:1-6 pubmed
    ..In this tissue the concentrations of pinazepam were 5-10 times higher on the 27th rather than the 20th day of pregnancy. The stage of pregnancy influences the distribution pattern of pinazepam in rabbit fetuses and their mothers. ..
  32. Meyer B, Muller F, Badian M, Hundt H, Joubert A, Luus H. Effects of HOE 760 (histamine H2-receptor antagonist) on diazepam pharmacokinetics. S Afr Med J. 1988;73:421-3 pubmed
    ..Blood was taken up to 1 week after the diazepam injections for assay of diazepam and desmethyldiazepam. The co-administration of HOE 760 did not affect the pharmacokinetics of diazepam and desmethyldiazepam. ..
  33. Valavani P, Atta Politou J, Panderi I. Development and validation of a liquid chromatographic/electrospray ionization mass spectrometric method for the quantitation of prazepam and its main metabolites in human plasma. J Mass Spectrom. 2005;40:516-26 pubmed
    ..0% and an overall accuracy (relative error) of < 4.6%. The method can be used to quantify prazepam and its metabolites in human plasma covering a variety of pharmacokinetic or bioequivalence studies. ..
  34. Aresta A, Monaci L, Zambonin C. Determination of delorazepam in urine by solid-phase microextraction coupled to high performance liquid chromatography. J Pharm Biomed Anal. 2002;28:965-72 pubmed
    ..The procedure required simple sample pre-treatment and was able to detect 5 ng/ml in spiked urine, regardless of the complexity of the matrix. ..
  35. St Pierre M, Pang K. Kinetics of sequential metabolism. II. Formation and metabolism of nordiazepam and oxazepam from diazepam in the perfused murine liver. J Pharmacol Exp Ther. 1993;265:1437-45 pubmed
    ..The atypical kinetic behavior of generated NZ may have also influenced the ensuing metabolic fate of its product, OZ, such that E[OZ,NZ] approximately E[OZ,DZ].(ABSTRACT TRUNCATED AT 250 WORDS) ..
  36. Ahlburg A, Lindhardt A, Taaning R, Modvig A, Skrydstrup T. An air-tolerant approach to the carbonylative Suzuki-Miyaura coupling: applications in isotope labeling. J Org Chem. 2013;78:10310-8 pubmed publisher
    ..Finally, the developed system was applied in the synthesis and isotope labeling of two pharmaceuticals, nordazepam and Tricor.
  37. Klima M, Altenburger M, Kempf J, Auwärter V, Neukamm M. Determination of medicinal and illicit drugs in post mortem dental hard tissues and comparison with analytical results for body fluids and hair samples. Forensic Sci Int. 2016;265:166-71 pubmed publisher
    ..11 drugs (amphetamine, MDMA, morphine, codeine, norcodeine, methadone, EDDP, fentanyl, tramadol, diazepam, nordazepam, and promethazine) could be detected and concentrations ranged from approximately 0.13pg/mg to 2,400pg/mg...
  38. Margalho C, Barroso M, Gallardo E, Monsanto P, Vieira D. Massive intoxication involving unusual high concentration of amitriptyline. Hum Exp Toxicol. 2007;26:667-70 pubmed
    ..Taking into account both the available circumstantial information and toxicological results, it is very likely that death was caused by self-poisoning. Human & Experimental Toxicology (2007) 26, 667-670. ..
  39. Forrester S, Brown S, Lees G, Hartsfield S. Disposition of clorazepate in dogs after single- and multiple-dose oral administration. Am J Vet Res. 1990;51:2001-5 pubmed
    ..001) than after a single dose (6.54 +/- 2.15 ml/min/kg). Absorption half-life after multiple doses (72 minutes) was longer (P less than 0.01) than after a single dose (33 minutes).(ABSTRACT TRUNCATED AT 250 WORDS) ..
  40. Dusci L, Good S, Hall R, Ilett K. Excretion of diazepam and its metabolites in human milk during withdrawal from combination high dose diazepam and oxazepam. Br J Clin Pharmacol. 1990;29:123-6 pubmed
    ..5 and 9.6 micrograms l-1) were present. The infant showed no overt physical or mental symptoms of benzodiazepine intoxication. ..
  41. Unseld E, Klotz U. Benzodiazepines: are they of natural origin?. Pharm Res. 1989;6:1-3 pubmed
    ..Whether the measured low concentrations (ranging from 0.01 up to 600 ng/g wet weight) have any biological role or clinical significance remains to be determined. ..
  42. Franke M, Winek C, Kingston H. Extraction of selected drugs from serum using microwave irradiation. Forensic Sci Int. 1996;81:51-9 pubmed
    ..The quantitation was performed by GC/NPD. The procedure has been applied successfully to a number of forensic cases. The use of microwaves decreases the time of extraction and the solvent consumption. ..
  43. Rocca P, Fonzo V, Scotta M, Zanalda E, Ravizza L. Paroxetine efficacy in the treatment of generalized anxiety disorder. Acta Psychiatr Scand. 1997;95:444-50 pubmed
    ..Paroxetine and imipramine affect predominantly psychic symptoms, whereas 2'-chlordesmethyldiazepam affects predominantly somatic symptoms. Our results suggest that paroxetine is effective for the treatment of GAD. ..
  44. Marland A, Sarkar P, Leavitt R. The urinary elimination profiles of diazepam and its metabolites, nordiazepam, temazepam, and oxazepam, in the equine after a 10-mg intramuscular dose. J Anal Toxicol. 1999;23:29-34 pubmed
    ..Diazepam and nordiazepam were measured in equine postadministration serum out to collection times of 6 and 54 h, respectively. Oxazepam and temazepam were not detected in postadministration serum. ..
  45. Basile A, Hughes R, Harrison P, Murata Y, Pannell L, Jones E, et al. Elevated brain concentrations of 1,4-benzodiazepines in fulminant hepatic failure. N Engl J Med. 1991;325:473-8 pubmed
    ..The origin of these substances is unknown, but these findings provide a rational basis for trials of benzodiazepine-receptor antagonists in the management of this disorder. ..
  46. Bertin I, Colombo G, Furlanut M, Benetello P. Double-blind placebo cross-over study of long-acting (chlordesmethyldiazepam) versus short-acting (lorazepam) benzodiazepines in generalized anxiety disorders. Int J Clin Pharmacol Res. 1989;9:203-8 pubmed
    ..These results further support the use of a long-acting benzodiazepine rather than a short-acting one as an anti-anxiety agent. ..
  47. McNicholas L, Martin W, Sloan J, Wala E. Precipitation of abstinence in nordiazepam- and diazepam-dependent dogs. J Pharmacol Exp Ther. 1988;245:221-4 pubmed
  48. Bolognesi R, Tsialtas D, Vasini P, Conti M, Manca C. Abnormal ventricular repolarization mimicking myocardial infarction after heterocyclic antidepressant overdose. Am J Cardiol. 1997;79:242-5 pubmed
    ..Because serum electrolyte imbalance and acute myocardial ischemic events were excluded, the mechanism by which antidepressant overdose may produce such elevation of the ST tract remains unclear. ..
  49. Duthel J, Constant H, Vallon J, Rochet T, Miachon S. Quantitation by gas chromatography with selected-ion monitoring mass spectrometry of "natural" diazepam, N-desmethyldiazepam and oxazepam in normal human serum. J Chromatogr. 1992;579:85-91 pubmed
    ..The other two were present in only some individuals (1.0-7.6 pg/ml for N-desmethyldiazepam and 2.0-13.0 pg/ml for oxazepam). The origin (endogenous, dietary or microbial) of these substances is still to be elucidated. ..
  50. Andersson T, Cederberg C, Edvardsson G, Heggelund A, Lundborg P. Effect of omeprazole treatment on diazepam plasma levels in slow versus normal rapid metabolizers of omeprazole. Clin Pharmacol Ther. 1990;47:79-85 pubmed
    ..The mean plasma concentrations of desmethyldiazepam showed a more rapid formation in the rapid compared with the slow metabolizers, which is a logical consequence of the rate of diazepam metabolism. ..
  51. Seddon T, Lockwood G, Chenery R. In vitro drug metabolism and pharmacokinetics of diazepam in cynomolgus monkey hepatocytes during culture for six days. Biochem Pharmacol. 1989;38:2621-30 pubmed
  52. Frey H, Scherkl R. Clorazepate, correlation between metabolism and anticonvulsant activity. Eur J Pharmacol. 1988;158:213-6 pubmed
    ..This may be explained by a time lag needed to reach and bind to the benzodiazepine receptor. ..
  53. Berrueta L, Gallo B, Vicente F. Analysis of oxazepam in urine using solid-phase extraction and high-performance liquid chromatography with fluorescence detection by post-column derivatization. J Chromatogr. 1993;616:344-8 pubmed
    ..Within-day recoveries and reproducibilities from urine samples spiked with 0.2 and 0.02 microgram/ml oxazepam were 97.9 and 95.0 and 2.1 and 9.4%, respectively. ..
  54. Azzam R, Notarianni L, Ali H. Rapid and simple chromatographic method for the determination of diazepam and its major metabolites in human plasma and urine. J Chromatogr B Biomed Sci Appl. 1998;708:304-9 pubmed
    ..6+/-2.26%, 90+/-4.24%, 87.45+/-0.64% and 94.50+/-0.71% for DZP, DMDZP, TZP and OZP, respectively (from urine). The method has also proved to be selective and reproducible. ..
  55. Senczuk Przybylowska M, Florek E, Piekoszewski W, Merritt T, Lechowicz E, Mazela J, et al. Diazepam and its metabolites in the mothers' and newborns' hair as a biomarker of prenatal exposure. J Physiol Pharmacol. 2013;64:499-504 pubmed
    ..determination of diazepam (the main benzodiazepine used by pregnant women was diazepam) and its metabolites (nordazepam, oxazepam) in hair of mothers and newborns. LOQ 10 pg/mg of hair was used in the study...
  56. Unseld E, Krishna D, Fischer C, Klotz U. Detection of desmethyldiazepam and diazepam in brain of different species and plants. Biochem Pharmacol. 1989;38:2473-8 pubmed
    ..This would suggest that DD and D might be of natural origin and incorporated via the foodchain into the animal and human body. The biological role or clinical relevance of these intriguing findings need still to be elucidated. ..
  57. Ihara N, Kokufu T, Sugioka N, Ohta T, Nosaka K. Inhibitory effect of diltiazem on diazepam metabolism in the mouse hepatic microsomes. Biol Pharm Bull. 1993;16:331-3 pubmed
    ..8 microM, indicating that diltiazem exhibits an inhibitory effect on the hepatic oxidative metabolism of diazepam. It was therefore suggested that diltiazem may impair the metabolism of diazepam in vivo. ..
  58. Fernandes C, File S, Berry D. Evidence against oppositional and pharmacokinetic mechanisms of tolerance to diazepam's sedative effects. Brain Res. 1996;734:236-42 pubmed
    ..Thus, the mechanism underlying this behavioural tolerance was not oppositional in nature. It is suggested that a situation-independent learned behavioural strategy is the most likely mechanism for the observed tolerance. ..
  59. Rasmussen L, Steentoft A, Rasmussen H, Kristensen P, Moller J. Benzodiazepines and postoperative cognitive dysfunction in the elderly. ISPOCD Group. International Study of Postoperative Cognitive Dysfunction. Br J Anaesth. 1999;83:585-9 pubmed
    ..01). The postoperative cognitive dysfunction we found in elderly patients after operation could not be explained by benzodiazepine concentrations detected in blood. ..
  60. Pien K, Laloup M, Pipeleers Marichal M, Grootaert P, de Boeck G, Samyn N, et al. Toxicological data and growth characteristics of single post-feeding larvae and puparia of Calliphora vicina (Diptera: Calliphoridae) obtained from a controlled nordiazepam study. Int J Legal Med. 2004;118:190-3 pubmed
    ..To our knowledge, this is the first report describing the presence of nordiazepam and its metabolite, oxazepam, in single Calliphora vicina larvae and puparia. ..
  61. Goldberger B, Chronister C, Merves M. Quantitation of benzodiazepines in blood and urine using gas chromatography-mass spectrometry (GC-MS). Methods Mol Biol. 2010;603:75-87 pubmed publisher
    ..The final extracts are then analyzed using selected ion monitoring GC-MS. ..
  62. Musulin S, Mariani C, Papich M. Diazepam pharmacokinetics after nasal drop and atomized nasal administration in dogs. J Vet Pharmacol Ther. 2011;34:17-24 pubmed publisher
    ..This study confirms that i.n. administration of diazepam yields rapid anticonvulsant concentrations of diazepam in the dog before a hepatic first-pass effect. ..
  63. Nishikawa T, Nishida A, Ohtani H, Sunaoshi W, Miura H, Sudo Y, et al. Radioreceptor assay of clonazepam and diazepam in blood for therapeutic drug monitoring. Ther Drug Monit. 1989;11:483-6 pubmed
    ..This receptor assay method is accurate, simple, requires less than 0.5 ml of plasma, and is therefore suitable for analyzing numerous samples in a short time. ..
  64. D Eramo C, Follini L, Stocchetti N, Taverna A, Zennaro F. [Chlordesmethyldiazepam as an anesthesia-inducing agent: time of loss of consciousness. Statistical analysis in man]. Acta Biomed Ateneo Parmense. 1987;58:19-23 pubmed
    ..30 patients) and in 60 sec (Group 2.30 patients) to assess the times to spontaneous closing of the eyes and to disappearance of the palpebral reflex. It is concluded that the reflex times are not significantly different in both groups. ..
  65. Bareggi S, Pirola R, Potvin P, Devis G. Effects of liver disease on the pharmacokinetics of intravenous and oral chlordesmethyldiazepam. Eur J Clin Pharmacol. 1995;48:265-8 pubmed
    ..These results indicate a need for caution in the administration of chlordesmethyldiazepam to patients with liver disease. ..
  66. Forrester S, Wilcke J, Jacobson J, Dyer K. Effects of a 44-day administration of phenobarbital on disposition of clorazepate in dogs. Am J Vet Res. 1993;54:1136-8 pubmed
    ..Adequate control of seizures in epileptic dogs, therefore, may require higher dosages of clorazepate when it is coadministered with phenobarbital. ..
  67. Jing X, Wala E, Sloan J. The effect of chronic benzodiazepines exposure on body weight in rats. Pharmacol Res. 1998;37:179-89 pubmed
    ..p.) did not affect the BW gain in DZ- and ND-treated female rats. The present data indicate that different BZs have different effects on BW gain in the rat suggesting that different subtypes of BZ receptors are involved. ..
  68. Ugland H, Krogh M, Rasmussen K. Liquid-phase microextraction as a sample preparation technique prior to capillary gas chromatographic-determination of benzodiazepines in biological matrices. J Chromatogr B Biomed Sci Appl. 2000;749:85-92 pubmed
    ..The limits of detection were from 0.020 to 0.115 nmol/ml for diazepam and N-desmethyldiazepam in plasma and urine using a nitrogen-phosphorus detector (NPD). ..
  69. Lehmann C, Wannarka G. Bioavailability and dose proportionality of intramuscular diazepam administered by autoinjector. J Clin Pharmacol. 2008;48:436-44 pubmed publisher
    ..A single (10-mg) autoinjector and 2 (20-mg) diazepam autoinjectors administered simultaneously produced plasma diazepam concentrations that were essentially dose proportional. ..
  70. de Wit H, Dudish S, Ambre J. Subjective and behavioral effects of diazepam depend on its rate of onset. Psychopharmacology (Berl). 1993;112:324-30 pubmed
    ..g., ratings of strength of drug effect). These data provide limited support for the notion that a faster rate of onset of drug effects is associated with greater euphoria. ..
  71. Swift R, Davidson D, Rosen S, Fitz E, Camara P. Naltrexone effects on diazepam intoxication and pharmacokinetics in humans. Psychopharmacology (Berl). 1998;135:256-62 pubmed
    ..A sub-analysis was conducted with 14 subjects who were FHP for alcoholism, but no differences were found on these outcome measures. ..
  72. Pirnay S, Hervé F, Bouchonnet S, Perrin B, Baud F, Ricordel I. Liquid chromatographic-electrospray ionization mass spectrometric quantitative analysis of buprenorphine, norbuprenorphine, nordiazepam and oxazepam in rat plasma. J Pharm Biomed Anal. 2006;41:1135-45 pubmed
    ..The validated method was applied to the determination of buprenorphine, norbuprenorphine, nordiazepam and oxazepam in plasma samples collected from rats at various times after intravenous administration of buprenorphine and nordiazepam. ..
  73. Saari T, Laine K, Bertilsson L, Neuvonen P, Olkkola K. Voriconazole and fluconazole increase the exposure to oral diazepam. Eur J Clin Pharmacol. 2007;63:941-9 pubmed
    ..Recurrent administration of diazepam increases the risk of clinically significant interactions during voriconazole or fluconazole treatment, because the elimination of diazepam is impaired significantly. ..
  74. Mercolini L, Mandrioli R, Iannello C, Matrisciano F, Nicoletti F, Raggi M. Simultaneous analysis of diazepam and its metabolites in rat plasma and brain tissue by HPLC-UV and SPE. Talanta. 2009;80:279-85 pubmed publisher
    ..The obtained data will hopefully contribute to the clarification of possible differences between depressed and non-depressed subjects with respect to benzodiazepine biotransformation. ..
  75. Dios Vieitez M, Renedo M, Fos D. Pharmacokinetic profiles of prazepam and 14C-prazepam in rat. Eur J Drug Metab Pharmacokinet. 1991;Spec No 3:3-8 pubmed
    ..Total radioactivity was measured in plasma by scintillation spectrometry. Pharmacokinetic analysis were carried out by two ways; according to compartmental pharmacokinetic models and by statistic moments. ..
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    ..The authors suggest a probable synergic or an enhanced effect between intramuscular chlordesmethyldiazepam and opiates in spinal anesthesia. ..
  77. van der Laan J, de Groot G, Wortelboer H, Noordhoek J. Pharmacokinetic differences of desmethyldiazepam in three outbred Wistar strains related to differences in liver enzyme activities. Pharmacol Toxicol. 1993;73:229-32 pubmed
    ..This strain difference in elimination of desmethyldiazepam may be related to differences in liver enzyme activities. ..
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    ..Death was considered to be due to acute poisoning by moclobemide. This case report is the first, to our knowledge, where death has been attributed to the toxic effects of moclobemide alone...
  79. Nishiya Y, Nakamura K, Okudaira N, Abe K, Kobayashi N, Okazaki O. Effects of organic solvents on the time-dependent inhibition of CYP3A4 by diazepam. Xenobiotica. 2010;40:1-8 pubmed publisher
    ..The effect of organic solvents should be taken into consideration when evaluating the in vitro time-dependent inhibition of new chemical entities. ..
  80. Sloan J, Martin W, Wala E, Dickey K. Chronic administration of and dependence on halazepam, diazepam, and nordiazepam in the dog. Drug Alcohol Depend. 1991;28:249-64 pubmed
    ..These data argue that the different dependencies produced by halazepam, diazepam and nordiazepam are not due solely to either the parent compound or to a single metabolite but most likely to their combined effects. ..
  81. Anthenelli R, Monteiro M, Blunt B, Schuckit M. Amnestic effects of intravenous diazepam in healthy young men. Am J Drug Alcohol Abuse. 1991;17:129-36 pubmed
    ..The data expand our current understanding of the amnestic effects of benzodiazepines and suggest that patients abusing these drugs in large doses may develop profound degrees of memory impairment. ..
  82. Garretty D, Wolff K, Hay A, Raistrick D. Benzodiazepine misuse by drug addicts. Ann Clin Biochem. 1997;34 ( Pt 1):68-73 pubmed
    ..However, temazepam was detected in only 14 of these samples. Multiple benzodiazepine abuse was evident from the high rate of detection of unrelated benzodiazepines. ..
  83. Smith Kielland A, Skuterud B, Olsen K, Mørland J. Urinary excretion of diazepam metabolites in healthy volunteers and drug users. Scand J Clin Lab Invest. 2001;61:237-46 pubmed
    ..Relating the metabolite concentration to creatinine concentration in the specimens decreased sample-to-sample variations. In some cases such correction could protect a subject from erroneous accusations of a new intake. ..
  84. Pavlic M, Libiseller K, Grubwieser P, Schubert H, Rabl W. Medicolegal aspects of tetrazepam metabolism. Int J Legal Med. 2007;121:169-74 pubmed
    ..Toxicological analyses revealed that tetrazepam is also metabolized to diazepam and further to nordazepam, which has not yet been reported...
  85. Meyer B, Muller F, Hundt H, Luus H, de la Rey N, Röthig H. The effects of felodipine on the pharmacokinetics of diazepam. Int J Clin Pharmacol Ther Toxicol. 1992;30:117-21 pubmed
    ..h/ml and mean peak concentrations of 40 vs 47 ng/ml. Felodipine might cause a retarded elimination of desmethyldiazepam, possibly by obtruding the formation of oxazepam. The clinical relevance of these findings remains to be elucidated. ..
  86. Lukey B, Corcoran K, Solana R. Pharmacokinetics of diazepam intramuscularly administered to rhesus monkeys. J Pharm Sci. 1991;80:918-21 pubmed
    ..3 ng/mL. These results, when compared with human pharmacokinetic studies, allow a means of extrapolating effective monkey anticonvulsant doses to humans on a pharmacokinetic basis. ..
  87. D Eramo C, Tirelli F, Maestri D. [Effects of chlordemethyldiazepam on blood cortisol during surgical stress]. Acta Biomed Ateneo Parmense. 1988;59:199-204 pubmed
    ..Blood samples were collected from each patient at the following times: 24 h before surgery (t0); 30 min after skin incision (t1); 30 min after extubation (t2). Significant variations of blood cortisol levels have not been shown. ..
  88. Wala E, Sloan J. Flumazenil, diazepam, nordiazepam and oxazepam interactions on plasma protein binding. Pharmacol Res. 1995;32:299-304 pubmed
    ..The results revealed that as the concentration of FLU added to plasma alone was increased its binding with plasma proteins decreased and that there were no significant binding interactions between FLU and OX, ND and DZ. ..
  89. Zeneroli M, Venturini I, Corsi L, Avallone R, Farina F, Ardizzone G, et al. Benzodiazepine-like compounds in the plasma of patients with fulminant hepatic failure. Scand J Gastroenterol. 1998;33:310-3 pubmed
  90. Jones A, Larsson H. Distribution of diazepam and nordiazepam between plasma and whole blood and the influence of hematocrit. Ther Drug Monit. 2004;26:380-5 pubmed
  91. Marin S, Roberts M, Wood M, McMillin G. Sensitive UPLC-MS-MS assay for 21 benzodiazepine drugs and metabolites, zolpidem and zopiclone in serum or plasma. J Anal Toxicol. 2012;36:472-6 pubmed publisher
    ..0708x + 1.6521, r(2) = 0.9822. This UPLC-MS-MS method is suitable for the quantification of benzodiazepines and hypnotics in serum and plasma, and offers fast, reliable and sensitive results. ..
  92. Iwaya N, Morita Y, Miyoshi K. Determination of pharmacodynamics of diazepam by quantitative pharmaco-EEG. Jpn J Psychiatry Neurol. 1989;43:675-84 pubmed
    ..In addition, the reduction in the pharmacological effect after continuous treatment with DZ depends not on autoinduction or interference, but on acute tolerance or adaptation. ..