Influences of Urinary pH on the Pharmacokinetics of Three Amphetamine‐Type Stimulants Using a New High‐Performance Liquid Chromatographic Method

Wang, Ling; Fěng, Fang; Wang, Xue Quan; Zhu, Lan

doi:10.1002/jps.21438

Cited by 6 publications

(5 citation statements)

References 18 publications

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“…One important factor could be differences in urine pH. Elimination of sympathomimetic amines is pH-dependent (29,30). Beckett et al (30) showed that the mean urinary excretion rate of amphetamine in normal men was reduced 5-fold by maintaining a urine pH of about 8.0 and increased 3.8-fold when the pH was lowered to 5.0.…”

Section: Discussionmentioning

confidence: 99%

Urinary MDMA, MDA, HMMA, and HMA Excretion Following Controlled MDMA Administration to Humans

Abraham¹,

Barnes²,

Lowe³

et al. 2009

Journal of Analytical Toxicology

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3,4-Methylenedioxymethamphetamine (MDMA), or ecstasy, is excreted as unchanged drug, 3,4-methylenedioxyamphetamine (MDA), and free and glucuronidated/sulfated 4-hydroxy-3-methoxymethamphetamine (HMMA), and 4-hydroxy-3-methoxyamphetamine (HMA) metabolites. The aim of this paper is to describe the pattern and timeframe of excretion of MDMA and its metabolites in urine. Placebo, 1.0 mg/kg, and 1.6 mg/kg oral MDMA doses were administered double-blind to healthy adult MDMA users on a monitored research unit. All urine was collected, aliquots were hydrolyzed, and analytes quantified by gas chromatography–mass spectrometry. Median Cmax, Tmax, ratios, first and last detection times, and detection rates were determined. Sixteen participants provided 916 urine specimens. After 1.6 mg/kg, median Cmax were 21,470 (MDMA), 2229 (MDA), 20,793 (HMMA), and 876 ng/mL (HMA) at median Tmax of 13.9, 23.0, 9.2 and 23.3 h. In the first 24 h, 30.2–34.3% total urinary excretion occurred. HMMA last detection exceeded MDMA’s by more than 33 h after both doses. Identification of HMMA as well as MDMA increased the ability to identify positive specimens but required hydrolysis. These MDMA, MDA, HMMA, and HMA pharmacokinetic data may be useful for interpreting workplace, drug treatment, criminal justice, and military urine drug tests. Measurement of urinary HMMA provides the longest detection of MDMA exposure yet is not included in routine monitoring procedures.

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Section: Discussionmentioning

confidence: 99%

Urinary MDMA, MDA, HMMA, and HMA Excretion Following Controlled MDMA Administration to Humans

Abraham¹,

Barnes²,

Lowe³

et al. 2009

Journal of Analytical Toxicology

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“…PSE is mainly excreted unchanged in the urine (43–96%); only a small amount, approximately 1–6%, is metabolised in the liver by N-demethylation to the active metabolite norpseudoephedrine (cathine). The time the drug remains in the body depends on the pH of the urine; the value of the biological half-life ( t 0.5 ) decreases when the urine is acidic, and increases when the urine is alkaline [ 8 , 14 , 15 , 16 , 17 , 18 , 19 ]. Selected pharmacokinetic properties of pseudoephedrine are presented in Table 1 .…”

Section: Pharmacokineticsmentioning

confidence: 99%

“…The on after 30 min and after 1-4 h the drug reaches its maximum concentr When using the extended-release formulation, this time is twice as lo excreted unchanged in the urine (43-96%); only a small amount, appr metabolised in the liver by N-demethylation to the active metabolite no (cathine). The time the drug remains in the body depends on the pH of of the biological half-life (t0.5) decreases when the urine is acidic, and urine is alkaline [8,[14][15][16][17][18][19]. Selected pharmacokinetic properties of ps presented in Table 1.…”

Section: Pharmacokineticsmentioning

confidence: 99%

Pseudoephedrine—Benefits and Risks

Głowacka

Wiela−Hojeńska

2021

IJMS

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Pseudoephedrine (PSE) is a drug with a long history of medical use; it is helpful in treating symptoms of the common cold and flu, sinusitis, asthma, and bronchitis. Due to its central nervous system (CNS) stimulant properties and structural similarity to amphetamine, it is also used for non-medical purposes. The substance is taken as an appetite reducer, an agent which eliminates drowsiness and fatigue, to improve concentration and as a doping agent. Due to its easier availability, it is sometimes used as a substitute for amphetamine or methamphetamine. Pseudoephedrine is also a substrate (precursor) used in the production of these drugs. Time will tell whether legal restrictions on the sale of this drug will reduce the scale of the problem associated with its misuse.

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“…In general, all of these studies demonstrated a large inter‐individual difference in the urinary concentrations and the pharmacokinetics of excretion of PSE and CATH following the administration of PSE, which could be attributed to differences in urinary flow and pH. Thus, the elimination half‐time of PSE in urine increases with increasing urinary pH 6, 17. The previous urinary threshold for PSE, 25 µg/ml, and the existing threshold for CATH, 5 µg/ml, can be greatly exceeded in certain individuals following the therapeutic intake of PSE a few hours prior to urine collection.…”

Section: Introductionmentioning

confidence: 99%

“…Thus, the elimination half-time of PSE in urine increases with increasing urinary pH. [6,17] The previous urinary threshold for PSE, 25 µg/ml, and the existing threshold for CATH, 5 µg/ml, can be greatly exceeded in certain individuals following the therapeutic intake of PSE a few hours prior to urine collection. Conversely, such thresholds were not reached after the administration of supratherapeutic doses of PSE in other subjects.…”

Section: Introductionmentioning

confidence: 99%

Determination of urinary concentrations of pseudoephedrine and cathine after therapeutic administration of pseudoephedrine‐containing medications to healthy subjects: implications for doping control analysis of these stimulants banned in sport

Barroso

Goudreault

Carbó

et al. 2011

Drug Testing and Analysis

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Due to its stimulatory effects on the central nervous system, and its structural similarity to banned stimulants such as ephedrine and methamphetamine, pseudoephedrine (PSE) at high doses is considered as an ergogenic aid for boosting athletic performance. However, the status of PSE in the International Standard of the Prohibited List as established under the World Anti-Doping Code has changed over the years, being prohibited until 2003 at a urinary cut-off value of 25 µg/ml, and then subsequently removed from the Prohibited List during the period 2004-2009. The re-consideration of this position by the World Anti-Doping Agency (WADA) List Expert Group has led to the reintroduction of PSE in the Prohibited List in 2010. In this manuscript, we present the results of two WADA-sponsored clinical studies on the urinary excretion of PSE and its metabolite cathine (CATH) following the oral administration of different PSE formulations to healthy individuals at therapeutic regimes. On this basis, the current analytical urinary threshold for the detection of PSE as a doping agent in sport has been conservatively established at 150 µg/ml

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Influences of Urinary pH on the Pharmacokinetics of Three Amphetamine‐Type Stimulants Using a New High‐Performance Liquid Chromatographic Method

Cited by 6 publications

References 18 publications

Urinary MDMA, MDA, HMMA, and HMA Excretion Following Controlled MDMA Administration to Humans

Urinary MDMA, MDA, HMMA, and HMA Excretion Following Controlled MDMA Administration to Humans

Pseudoephedrine—Benefits and Risks

Determination of urinary concentrations of pseudoephedrine and cathine after therapeutic administration of pseudoephedrine‐containing medications to healthy subjects: implications for doping control analysis of these stimulants banned in sport

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