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Pesquisa : D03.383.679.875.500 [Categoria DeCS]
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  1 / 6 MEDLINE  
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PMID:27390052
Autor:Chen X; Zhao Q; Zhang J; Liu T; Jiang J; Hu P
Título:An open-label, multiple-dose study to assess the pharmacokinetics and tolerability of sitagliptin/metformin fixed-dose combination (FDC) tablet in healthy Chinese adult subjects.
Fonte:Int J Clin Pharmacol Ther; 54(9):705-11, 2016 Sep.
ISSN:0946-1965
País de publicação:Germany
Idioma:eng
Resumo:AIM: This study investigated the pharmacokinetics of sitagliptin and metformin after multiple oral doses of the sitagliptin/metformin fixed-dose combination (MK0431A) tablet in healthy Chinese volunteers. METHODS: This was a singlecenter, randomized study in 24 healthy adults. Subjects received twice-daily doses of MK0431A 50-mg/500-mg tablet and 50-mg/850-mg tablet for 7 days. Serial blood and urine samples were collected at predefined time points for bioassay of sitagliptin and metformin. Safety was assessed throughout the study. RESULTS: Based on consecutive trough concentrations, the steady states of sitagliptin and metformin were reached after twice-daily administration of MK0431A tablets for 5 days. After the last dose, the mean ± SD (standard deviation) peak sitagliptin concentration of 167.3 - 22.52 and 174.1 ± 22.16 ng/mL was reached in a median tmax of 2.25 - 3 hours. The mean ± SD Cmax of metformin appeared in a median tmax of 1.75 - 2.25 hours at 888.3 ± 195.19 and 1,337 ± 269.19 ng/mL with MK0431A 50 mg/500 mg and 50 mg/850 mg, respectively Mean ± SD AUC012h of sitagliptin was between 1,404 ± 147.48 and 1,374 ± 179.12 h×ng/mL, while mean ± SD AUC0-12h of metformin were 6,015 ± 854.98 and 8,587 ± 1,715.93 h×ng/mL with MK0431A 50 mg/500 mg and 50 mg/850 mg, respectively. Approximately 75% sitagliptin and 40% metformin were excreted unchanged in the urine, corresponding to a renal clearance of 17.84 - 18.27 L/h for sitagliptin and 27.11 - 27.94 L/h for metformin. CONCLUSION: No clinically-significant pharmacokinetic difference was identified between Chinese and foreign healthy volunteers regarding sitagliptin and metformin with multiple doses of MK0431A tablets. The treatments were well tolerated.
Tipo de publicação: JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
Nome de substância:0 (Hypoglycemic Agents); 0 (Sitagliptin Phosphate, Metformin Hydrochloride Drug Combination); 0 (Tablets)


  2 / 6 MEDLINE  
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PMID:24298724
Autor:Scheen AJ; Van Gaal LF
Endereço:Université de Liège, Belgique.
Título:[Sitagliptin in the treatment of type 2 diabetes: insights five years after commercialisation].
Título:La sitagliptine dans le traitement du diabète de type 2: le point, cinq ans après sa commercialisation..
Fonte:Rev Med Liege; 68(10):504-10, 2013 Oct.
ISSN:0370-629X
País de publicação:Belgium
Idioma:fre
Resumo:Sitagliptin (Januvia) was the first selective inhibitor of dipeptidyl peptidase-4 commercialized for the management of type 2 diabetes. It is also available as a fixed-dose combination with meformin (Janumet). Almost 5 years after its launch in Belgium, the present review summarizes the most recent data regarding the clinical efficacy of this antidiabetic agent, the controversy about its safety profile, its use at lower dosage in case of moderate to severe renal insufficiency, the various indications that have been successively accepted and reimbursed, and, finally, the perspectives offered by a large ongoing cardiovascular outcome trial (TECOS).
Tipo de publicação: ENGLISH ABSTRACT; JOURNAL ARTICLE
Nome de substância:0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Drug Combinations); 0 (Hypoglycemic Agents); 0 (Pyrazines); 0 (Sitagliptin Phosphate, Metformin Hydrochloride Drug Combination); 0 (Triazoles); 9100L32L2N (Metformin); TS63EW8X6F (Sitagliptin Phosphate)


  3 / 6 MEDLINE  
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PMID:21189532
Autor:Scheen AJ
Endereço:Université de Liège, Service de Diabétologie, Nutrition et Maladies métaboliques et Unité de Pharmacologie clinique, CHU de Liège, Belgique.
Título:[Medication of the month. Sitagliptin-metformin fixed combination (Janumet)].
Título:Le médicament du mois. Combinaison fixe sitagliptine-metformine (Janumet)..
Fonte:Rev Med Liege; 65(11):648-54, 2010 Nov.
ISSN:0370-629X
País de publicação:Belgium
Idioma:fre
Resumo:Type 2 diabetes is a complex disease with the coexistence of several pathophysiological abnormalities such as a defect of insulin secretion, a relative hyperglucagonaemia, an increased hepatic glucose production and a muscular insulin resistance. In order to tackle all these abnormalities, the coadministration of several drugs with complementary actions is frequently required. Janumet is a fixed-dose combination of sitagliptin, a specific inhibitor of dipeptidylpeptidase-4 that blocks the rapid degradation of so-called incretin hormones (resulting in a potentiation of insulin secretion and reduction of glucagon secretion in a glucose-dependent manner), and of metformin, a biguanide compound that reduces glucose hepatic production and slightly improves insulin sensitivity. This pharmacological combination improves glucose control without inducing hypoglycaemia or weight gain. The tolerance profile is rather good, with (digestive) side effects and contraindications (risk of lactic acidosis in case of renal insufficiency) attributable to metformin. Janumet (50/850 mg or 50/1.000 mg), twice daily, is indicated in the treatment of type 2 diabetes and is currently reimbursed in Belgium after failure of metformin monotherapy or the prior demonstration of the efficacy of adding sitaglitptin (Januvia) to metformin.
Tipo de publicação: ENGLISH ABSTRACT; JOURNAL ARTICLE
Nome de substância:0 (Drug Combinations); 0 (Hypoglycemic Agents); 0 (Pyrazines); 0 (Sitagliptin Phosphate, Metformin Hydrochloride Drug Combination); 9100L32L2N (Metformin)


  4 / 6 MEDLINE  
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PMID:20923244
Autor:Migoya EM; Miller JL; Gutierrez M; Zheng W; Johnson-Levonas AO; Liu Q; Matthews CZ; Wagner JA; Gottesdiener KM
Endereço:Merck & Co., Inc., Rahway, New Jersey 07065-0900, USA. elizabeth_migoya@merck.com
Título:Bioequivalence of sitagliptin/metformin fixed-dose combination tablets and concomitant administration of sitagliptin and metformin in healthy adult subjects: a randomized, open-label, crossover study.
Fonte:Clin Drug Investig; 30(12):855-66, 2010.
ISSN:1173-2563
País de publicação:New Zealand
Idioma:eng
Resumo:BACKGROUND: Treatment with an oral antihyperglycaemic agent administered as monotherapy is often unsuccessful at achieving or maintaining glycaemic control in patients with type 2 diabetes mellitus. The combined use of sitagliptin and metformin is an effective treatment for type 2 diabetes mellitus, consistent with the complementary mechanisms of action by which these two agents improve glucose control. OBJECTIVES: To establish bioequivalence between sitagliptin/metformin fixed-dose combination (FDC) tablets (Janumet®) and co-administration of corresponding doses of sitagliptin and metformin as individual tablets. METHODS: This was an randomized, open-label, two-part, two-period crossover study, which included a total of 48 healthy subjects, 24 subjects per part (parts I and II). Within each part, subjects were assigned to receive treatments in random order; treatment periods were separated by a washout interval of at least 7 days. Eligible study participants included healthy, non-smoking (within previous 6 months), male and female subjects aged between 18 and 45 years with a body mass index ≤32 kg/m². Part I consisted of treatments A (co-administration of sitagliptin 50 mg and metformin 500 mg) and B (sitagliptin/metformin 50 mg/500 mg FDC tablet); part II consisted of treatments C (co-administration of sitagliptin 50 mg and metformin 1000 mg) and D (sitagliptin 50 mg/metformin 1000 mg FDC tablet). Blood samples were collected pre-dose and up to 72 hours post-dose in each treatment period for determination of plasma sitagliptin and metformin concentrations and calculation of the respective pharmacokinetic parameters. The area under the plasma concentration-time curve from time zero to infinity (AUC(∞)) and the maximum plasma concentration (C(max)) for both sitagliptin and metformin were designated as the primary and secondary study endpoints, respectively, and analysed using an ANOVA model after logarithmic transformation of the data. Bioequivalence was established if the 90% confidence intervals (CIs) for the geometric mean ratios (GMRs; FDC tablet/co-administration) of the AUC(∞) and C(max) for both sitagliptin and metformin fell within pre-specified bounds of (0.80, 1.25). RESULTS: The GMRs (90% CI) for the AUC(∞) of sitagliptin 50 mg and metformin 500 mg were 0.98 (0.96, 1.00) and 1.0 (0.95, 1.04), respectively, and for C(max) of sitagliptin and metformin were 1.00 (0.94, 1.06) and 1.00 (0.94, 1.06), respectively. The GMRs (90% CI) for the AUC(∞) of sitagliptin 50 mg and metformin 1000 mg (part II) were 0.97 (0.95, 0.99) and 1.00 (0.94, 1.07), respectively, and for the C(max) of sitagliptin and metformin were 0.94 (0.88, 1.01) and 1.01 (0.93, 1.10), respectively. In both part I and part II, the 90% CIs of the GMRs of the AUC(∞) and C(max) for both sitagliptin and metformin all fell within the pre-specified bioequivalence bounds of (0.80, 1.25). Administration of single doses of sitagliptin/metformin 50 mg/500 mg (part I) and 50 mg/1000 mg FDC tablets (part II) and co-administration of corresponding doses of sitagliptin and metformin as individual tablets were generally well tolerated. CONCLUSION: The sitagliptin/metformin 50 mg/500 mg and 50 mg/1000 mg FDC tablets are bioequivalent to co-administration of corresponding doses of sitagliptin and metformin as individual tablets and support bioequivalence to the sitagliptin/metformin 50 mg/850 mg tablet strength. These results indicate that the safety and efficacy profile of co-administration of sitagliptin and metformin can be extended to the sitagliptin/metformin FDC tablets.
Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
Nome de substância:0 (Blood Glucose); 0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Drug Combinations); 0 (Hypoglycemic Agents); 0 (Pyrazines); 0 (Sitagliptin Phosphate, Metformin Hydrochloride Drug Combination); 0 (Tablets); 0 (Triazoles); 9100L32L2N (Metformin); TS63EW8X6F (Sitagliptin Phosphate)


  5 / 6 MEDLINE  
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PMID:19637427
Título:Sitagliptin + metformin: new combination. Do not use this combination. Sitagliptin provides a slight increase of glucose-lowering effects, but there is a disturbing potential for long-term adverse effects: infections, depression, and cancer.
Fonte:Prescrire Int; 18(101):115, 2009 Jun.
ISSN:1167-7422
País de publicação:France
Idioma:eng
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Biguanides); 0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Drug Combinations); 0 (Hypoglycemic Agents); 0 (Pyrazines); 0 (Sitagliptin Phosphate, Metformin Hydrochloride Drug Combination); 0 (Sulfonylurea Compounds); 0 (Triazoles); 9100L32L2N (Metformin); TS63EW8X6F (Sitagliptin Phosphate)


  6 / 6 MEDLINE  
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PMID:18808315
Autor:Reynolds JK; Neumiller JJ; Campbell RK
Endereço:Washington State University, College of Pharmacy, Department of Pharmacotherapy, Pullman, WA, USA. jreynolds@wsu.edu
Título:Janumet: a combination product suitable for use in patients with Type 2 diabetes.
Fonte:Expert Opin Investig Drugs; 17(10):1559-65, 2008 Oct.
ISSN:1744-7658
País de publicação:England
Idioma:eng
Resumo:Inhibition of the enzyme dipeptidyl peptidase-4 represents the latest pharmacologic intervention to become available to assist patients with Type 2 diabetes to achieve glycemic control. A combination tablet of sitagliptin (Januvia) and metformin HCl (Glucophage) is now available from Merck (Janumet). The FDA has approved this drug for use in patients who are not adequately controlled by taking either sitagliptin or metformin HCl alone or for patients who are at present taking both simultaneously. Sitagliptin has been shown to be safe and effective at 100 mg daily doses. When given in combination with metformin the effect on glycemic control is thought to be complementary and possibly additive.
Tipo de publicação: JOURNAL ARTICLE; REVIEW
Nome de substância:0 (Dipeptidyl-Peptidase IV Inhibitors); 0 (Drug Combinations); 0 (Hypoglycemic Agents); 0 (Pyrazines); 0 (Sitagliptin Phosphate, Metformin Hydrochloride Drug Combination); 0 (Triazoles); 89750-14-1 (Glucagon-Like Peptide 1); 9100L32L2N (Metformin); TS63EW8X6F (Sitagliptin Phosphate)



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