Study on the Pharmacokinetics of Diazepam and Its Metabolites in Blood of Chinese People

Wang, Lele; Ren, Xinxin; He, Yi; Cui, Guan-Feng; Wei, Zhiwen; Jia, Jingying; Cao, Jie; Liu, Yao; Cong, Bin; Niu, Yong; Kuang, Yun

doi:10.1007/s13318-020-00614-8

Cited by 8 publications

(6 citation statements)

References 22 publications

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“… 29 The half-life of diazepam ranges from 36.62–334.69 hours. 30 Diazepam exhibits high plasma protein binding, with a rate of up to 99%. It is highly lipophilic, allowing it to easily cross the blood‒brain barrier.…”

Section: Discussionmentioning

confidence: 99%

The Efficacy and Safety of Diazepam for Intraoperative Blood Pressure Stabilization in Hypertensive Patients Undergoing Vitrectomy Under Nerve Block Anesthesia: A Prospective, Single-Center, Double-Blind, Randomized, Controlled Trial

Qian,

Gong,

Shu

et al. 2024

TCRM

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Purpose To evaluate the effectiveness and safety of diazepam in maintaining stable intraoperative blood pressure (BP) in hypertensive patients undergoing vitrectomy under nerve block anesthesia. Methods A total of 180 hypertensive patients undergoing vitrectomy with nerve block anesthesia were randomized into two groups. The intervention group was given oral diazepam 60 min before operation, while the control group was given oral placebo 60 min before operation. The primary outcome is the effective rate of intraoperative BP control, defined as systolic blood pressure (SBP) during the operation maintained < 160 mmHg at all timepoints. The logistic regression model will be performed to analyze the compare risk factors for ineffective BP control. Results The effective rate of intraoperative SBP control in the diazepam group was significant higher than that in the placebo group from 15 min to 70 min of the surgery ( P < 0.05). The proportion of patients with SBP ≥180 mmHg at any timepoint from operation to 1 h postoperation was higher in the placebo group (12.22%) than in the diazepam group (2.22%) ( P = 0.0096). We observed that the change in SBP from baseline consistently remained higher in the placebo group than in the diazepam group. In the logistic regression analysis, age, years of diagnosed hypertension and SBP 1h before surgery were significant risk factors for ineffective BP control. Conclusion This study provides robust evidence supporting the effectiveness of oral diazepam as a pre-surgery intervention in maintaining stable blood pressure during vitrectomy in hypertensive patients. Trial Registration Chinese Clinical Trial Registry (ChiCTR), ChiCTR2100041772.

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Section: Discussionmentioning

confidence: 99%

The Efficacy and Safety of Diazepam for Intraoperative Blood Pressure Stabilization in Hypertensive Patients Undergoing Vitrectomy Under Nerve Block Anesthesia: A Prospective, Single-Center, Double-Blind, Randomized, Controlled Trial

Qian,

Gong,

Shu

et al. 2024

TCRM

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“…Diazepam and its main metabolites (nordiazepam, oxazepam, TG, and OG) in urine samples from each volunteer were extracted via SPE and analyzed by an LC–MS/MS method operated in a positive multiple response monitoring mode. The analysis was based on our published LC–MS/MS method for the measurement of diazepam and its metabolites in blood [ 17 ] and validated for the analysis of diazepam and its metabolites in urine.…”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics of Diazepam and Its Metabolites in Urine of Chinese Participants

Wang

Ren

et al. 2022

Drugs R D

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Background Urine is conventionally used as a specimen to document diazepam-related crimes; however, few reports have described the pharmacokinetics of diazepam and its metabolites in urine. Objective This study aimed to investigate the pharmacokinetics of diazepam and its metabolites, including glucuronide compounds, in the urine of Chinese participants. Methods A total of 28 volunteers were recruited and each participant ingested 5 mg of diazepam orally. Ten milliliters of urine were collected from each participant at post-consumption timepoints of prior (zero), 1, 2, 4, 8, 12, and 24 h and 2, 3, 6, 12, and 15 days. All samples were extracted by solid-phase extraction and analyzed using high-performance liquid chromatography-tandem mass spectrometry. Diazepam and its main metabolites, except for temazepam, were detected in the urine of volunteers. Pharmacokinetic parameters were analyzed using the pharmacokinetic software DAS according to the non-compartment model. Results Urinary diazepam peaked at 2.38 ng/mL (C max ) and 1.93 h (T max ). The urinary metabolite nordiazepam peaked at 1.17 ng/mL and 100.21 h; temazepam glucuronide (TG) peaked at 145.61 ng/mL and 41.14 h; and oxazepam glucuronide (OG) peaked at 101.57 ng/mL and 165.86 h. The elimination half-life (t ½z ) and clearance (CLz/F) for diazepam were 119.58 h and 65.77 L/h, respectively. The t ½z of the metabolites nordiazepam, TG, and OG was 310.58 h, 200.17 h, and 536.44 h, respectively. Finally, this study found that both diazepam and its main metabolites in urine were detectable for at least 15 days, although there were individual differences. ConclusionThe results regarding diazepam pharmacokinetics in urine would be of great help in forensic science and drug screening.

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“…For plasma preparation, a single blood sample (0.3 ml for each time point) was collected from the canthus of rat eyes at 0, 0.033, 0.083, 0.117, 0.167, 0.25, 0.5, 1, 2, 3, 4, 5 and 7 h aer administration, respectively, followed by an immediate centrifugation at 1920 Â g for 10 min. Aer centrifugation, these samples were mixed and stored at À80 C. The Drug and Statistics 3.0 soware program [31][32][33] (DAS 3.0, http:// www.drugchina.net) was used to calculate pharmacokinetic parameters of eupatorin in the non-compartmental model.…”

Section: Pharmacokinetics Analysismentioning

confidence: 99%

Assessment of a developed HPLC-MS/MS approach for determining plasma eupatorin in rats and its application in pharmacokinetics analysis

Feng

Zhang

et al. 2020

RSC Adv.

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Study on the Pharmacokinetics of Diazepam and Its Metabolites in Blood of Chinese People

Cited by 8 publications

References 22 publications

The Efficacy and Safety of Diazepam for Intraoperative Blood Pressure Stabilization in Hypertensive Patients Undergoing Vitrectomy Under Nerve Block Anesthesia: A Prospective, Single-Center, Double-Blind, Randomized, Controlled Trial

The Efficacy and Safety of Diazepam for Intraoperative Blood Pressure Stabilization in Hypertensive Patients Undergoing Vitrectomy Under Nerve Block Anesthesia: A Prospective, Single-Center, Double-Blind, Randomized, Controlled Trial

Pharmacokinetics of Diazepam and Its Metabolites in Urine of Chinese Participants

Assessment of a developed HPLC-MS/MS approach for determining plasma eupatorin in rats and its application in pharmacokinetics analysis

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