Glucosamine oral bioavailability and plasma pharmacokinetics after increasing doses of crystalline glucosamine sulfate in man

Persiani, Stefano; Roda, Enrico; Rovati, Lucio C.; Locatelli, Marcello; Giacovelli, Giampaolo; Roda, Aldo

doi:10.1016/j.joca.2005.07.009

Cited by 156 publications

(156 citation statements)

References 33 publications

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“…Upon oral ingestion, glucosamine hydrochloride is rapidly absorbed as free glucosamine in the intestine. A significant fraction of this is catabolized by first-pass metabolism in the liver resulting in a bioavailability of ϳ25% (28). Of note, when our subjects were given a single dose of glucosamine orally (500 mg), we detected significant increases in plasma glucosamine levels (peak concentrations at ϳ60 min) that were 10-to 20-fold higher than basal levels in healthy humans reported in other studies (28,41).…”

Section: Discussioncontrasting

confidence: 41%

“…The present study is the first clinical intervention study with oral glucosamine to evaluate glucosamine pharmacokinetics. Baseline plasma glucosamine levels in healthy humans (ϳ0.15 mol/l) are slightly below the lower limit of detection of our HPLC assay (Ͻ0.3 mol/l) (28). Thus, it is not surprising that we were unable to detect significant amounts of plasma glucosamine in any of our study subjects at baseline (before glucosamine administration) or in any of the placebo-treated subjects.…”

Section: Discussionmentioning

confidence: 59%

“…A significant fraction of this is catabolized by first-pass metabolism in the liver resulting in a bioavailability of ϳ25% (28). Of note, when our subjects were given a single dose of glucosamine orally (500 mg), we detected significant increases in plasma glucosamine levels (peak concentrations at ϳ60 min) that were 10-to 20-fold higher than basal levels in healthy humans reported in other studies (28,41). Although we did not observe statistically significant differences in C max , T max , or AUC between lean and obese groups, C max and AUC tended to be slightly lower in obese than in lean subjects.…”

Section: Discussionmentioning

confidence: 99%

“…Pharmacokinetic parameters for glucosamine were derived from analysis of plasma glucosamine concentrations after oral dosing, assuming first-order kinetics (28). The elimination constant, K e , was estimated from the slope of the linear regression of log-transformed concentration values plotted versus time in the terminal phase, assuming first-order kinetics and instantaneous mixing.…”

Section: Methodsmentioning

confidence: 99%

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Oral Glucosamine for 6 Weeks at Standard Doses Does Not Cause or Worsen Insulin Resistance or Endothelial Dysfunction in Lean or Obese Subjects

et al. 2006

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Glucosamine is a popular nutritional supplement used to treat osteoarthritis. Intravenous administration of glucosamine causes insulin resistance and endothelial dysfunction. However, rigorous clinical studies evaluating the safety of oral glucosamine with respect to metabolic and cardiovascular pathophysiology are lacking. Therefore, we conducted a randomized, placebo-controlled, double-blind, crossover trial of oral glucosamine at standard doses (500 mg p.o. t.i.d.) in lean (n ‫؍‬ 20) and obese (n ‫؍‬ 20) subjects. Glucosamine or placebo treatment for 6 weeks was followed by a 1-week washout and crossover to the other arm. At baseline, and after each treatment period, insulin sensitivity was assessed by hyperinsulinemic-isoglycemic glucose clamp (SI Clamp ) and endothelial function evaluated by brachial artery blood flow (BAF; Doppler ultrasound) and forearm skeletal muscle microvascular recruitment (ultrasound with microbubble contrast) before and during steady-state hyperinsulinemia. Plasma glucosamine pharmacokinetics after oral dosing were determined in each subject using a high-performance liquid chromatography method. As expected, at baseline, obese subjects had insulin resistance and endothelial dysfunction when compared with lean subjects (SI Clamp

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Section: Discussioncontrasting

confidence: 41%

Section: Discussionmentioning

confidence: 59%

Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Oral Glucosamine for 6 Weeks at Standard Doses Does Not Cause or Worsen Insulin Resistance or Endothelial Dysfunction in Lean or Obese Subjects

et al. 2006

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“…No caso da glucosamina sintética, essa dose leva a uma concentração de 10µMol no sangue e lí-quido sinovial (mínima dose terapêutica da glucosamina). A glucosamina hidroclorídrica, dada na dose de 500mg três vezes ao dia, chega em concentração de 3µMol no líquido sinovial (menor do que a da dose terapêutica) (39,40) .…”

Section: Glucosaminaunclassified

Tratamento medicamentoso da osteoartrose do joelho

Rezende¹,

Gobbi²

2009

Rev. bras. ortop.

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RESUMOO tratamento clínico da osteoartrite/artrose (OA) está sempre indicado e baseia-se no autocuidado feito pelo paciente e orientado pelo médico. O uso de medicamentos é complementar às medidas de emagrecimento, ganho de força, de propriocepção, de flexibilidade e de amplitude de movimento. Entre os medicamentos disponíveis para o tratamento da OA há os que são essencialmente analgésicos e que não interferem no curso da doença; bem como os anti-inflamatórios, controversos por seus efeitos colaterais e pelo seu papel na OA, porém, com propriedades analgésicas e anti-inflamatórias indiscutíveis; e, por fim, as drogas modificadoras de estrutura, que retardam a evolução da OA. As medicações ainda podem ser de uso tópico, intra-articular, oral e injetável (sistêmico). As várias apresentações de ácido hialurônico (AH) mostram o poder analgésico da droga e há indícios de poder modificador de estrutura da cartilagem pela medicação. Há nível de evidência IA, para diacereína e para a glucosamina, de que retardam a evolução da OA. Mais tecnologia para diagnóstico e controle de tratamento da OA, bem como mais estudos multicêntricos são necessários para consolidar o poder do tratamento medicamentoso de outras drogas. Declaramos existência de conflitos de interesse com Aché, Genzyme, Merck do Brasil, Solvay, TRB Pharma, Zambon, Zodiac. Neste artigo, não favorecemos nenhum produto comercial. Todas as informações são baseadas em literatura médica e não houve nenhuma forma de patrocínio para realização deste artigo pelas empresas responsáveis pelas medicações citadas. Descritores -

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Effect of Glucosamine on Pain-Related Disability in Patients With Chronic Low Back Pain and Degenerative Lumbar Osteoarthritis

Wilkens

Scheel²,

Grundnes³

et al. 2010

JAMA

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Glucosamine oral bioavailability and plasma pharmacokinetics after increasing doses of crystalline glucosamine sulfate in man

Cited by 156 publications

References 33 publications

Oral Glucosamine for 6 Weeks at Standard Doses Does Not Cause or Worsen Insulin Resistance or Endothelial Dysfunction in Lean or Obese Subjects

Oral Glucosamine for 6 Weeks at Standard Doses Does Not Cause or Worsen Insulin Resistance or Endothelial Dysfunction in Lean or Obese Subjects

Tratamento medicamentoso da osteoartrose do joelho

Effect of Glucosamine on Pain-Related Disability in Patients With Chronic Low Back Pain and Degenerative Lumbar Osteoarthritis

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