Oral Antihyperglycemic Treatment Options for Type 2 Diabetes Mellitus

Brietzke, Stephen

doi:10.1016/j.mcna.2014.08.012

Cited by 32 publications

(24 citation statements)

References 113 publications

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“…However, secondary and tertiary add-on drug therapy should be individualized based not only on efficacy but also on tolerance and personal preferences, taking into account the wishes and priorities of the patient [2,3,57]. DPP-4i have a better tolerance profile than SGLT2i and have proven to be well tolerated in elderly patients [7] while SGLT2i should be used with caution in this more fragile population [9].…”

Section: Expert Opinionmentioning

confidence: 99%

DPP-4 inhibitor plus SGLT-2 inhibitor as combination therapy for type 2 diabetes: from rationale to clinical aspects

Scheen

2016

Expert Opinion on Drug Metabolism & Toxicology

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SUMMARYIntroduction : Type 2 diabetes (T2D) is a complex disease with multiple defects, which generally require a combination of several pharmacological approaches to control hyperglycemia. Combining a dipeptidyl peptidase-4 inhibitor (DPP-4i) and a sodium-glucose cotransporter type 2 inhibitor (SGT2i) appears to be an attractive approach.Area covered: An extensive literature search was performed to analyze the pharmacokinetics, pharmacodynamics and clinical experience of different gliptin-gliflozin combinations.Expert opinion: There is a strong rationale for combining a DPP-4i and a SGLT2i in patients with T2D because the two drugs exert different and complementary glucose-lowering effects.Dual therapy (initial combination or stepwise approach) is more potent than either monotherapy in patients treated with diet and exercise or already treated with metformin.Combining the two pharmacological options is safe and does not induce hypoglycemia. The additional glucose-lowering effect is more marked when a gliflozin is added to a gliptin than when a gliptin is added to a gliflozin. Two fixed-dose combinations (FDCs) are already available (saxagliptin-dapagliflozin and linagliptin-empagliflozin) and others are in current development. Bioequivalence of the two compounds given as FDC tablets was demonstrated when compared with coadministration of the individual tablets. FDCs could simplify the antihyperglycaemic therapy and improve drug compliance. Article highlights box -Type 2 diabetes (T2D) often requires the combination of several medications with complementary actions to reach glucose control targets while limiting side effects -The combination of a dipeptidyl peptidase-4 inhibitor (DPP-4i) and a sodium-glucose cotransporter type 2 inhibitor (SGLT2i) is an attractive approach for the management of T2D. Keywords-Both saxagliptin plus dapagliflozin and linagliptin plus empagliflozin combined therapies have been tested as separate tablets (no clinically relevant pharmacokinetic drug-drug interactions) and as fixed-dose combination (FDC : bioequivalence studies).-DPP-4i -SGLT2i combined therapies are more efficacious than either monotherapy to control blood glucose, without worsening of the safety profile.-Initial DPP-4i -SGLT2i combination may be considered or one compound may the added to the other. However, which one should be used in first place remains an open question.

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Section: Expert Opinionmentioning

confidence: 99%

DPP-4 inhibitor plus SGLT-2 inhibitor as combination therapy for type 2 diabetes: from rationale to clinical aspects

Scheen

2016

Expert Opinion on Drug Metabolism & Toxicology

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“…The most common adverse effects are gastrointestinal (diarrhea, nausea, abdominal pain and flatulence), reported by more than 30% of patients during the first 2 weeks, but resolve spontaneously in the majority and only 5% keeps intolerance [24]. Despite not having been validated in clinical trials, it is recommended to start metformin with low doses and gradually increase.…”

Section: Side-effects and Contraindicationsmentioning

confidence: 99%

“…Despite not having been validated in clinical trials, it is recommended to start metformin with low doses and gradually increase. Metformin alters the absorption of vitamin B12 and deficiency may occur (< 150 pmol/L) in 9.9% of patients [24].…”

Section: Side-effects and Contraindicationsmentioning

confidence: 99%

Diabetes-Old Therapies Revisited

Guimarães¹

2016

EMIJ

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Today, there are many therapeutic options for the treatment of type 2 Diabetes, which means that therapeutic decision making has become increasingly challenging and complex. With the recent introduction in clinical practice of new classes, with different mechanisms of action, what is the role of the older drugs? This article reviews these drugs, with recently published data update. Today, recommendations are not based on a simple algoritm, but in a patient centered approach. Besides the phenotypic heterogeneity of patients with type 2 diabetes, there is also a great diversity in response to treatment. This concept of personalized medicine has changed in recent years. The new era of personalized medicine evolves in order to identify molecular and clinical signs that can predict therapeutic response, reducing uncertainty in decision making. The "old" drugs may resurface, with more precise indications, in selected groups of patients.

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“…High expression of PPARγ has been associated with metabolic syndrome, obesity 4 , diabetes mellitus 5 8 , hypertension, arteriosclero-cy 10 . Binding of agonist to PPARγ improves carbohydrate and lipid metabolism 11 , in part reflecting the induction of mitochondrial uncoupling proteins UCP such as UCP-1 4 .…”

Section: Introductionmentioning

confidence: 99%

“…Although thiazolidine ingredients has demonstrated efficacy in the treatment of diabetes, it causes weight gain, fluid retention, and cardiovascular dysfunction 6,11 , warranting the development of dietary PPARγ agonists with fewer side effects. Thus, in the present study, the novel ingredient, 5-hydroxy-4-phenyl-butenolide fraglide-1 , was identified in 8-year-old Kozu hengshun fragrant vinegar by serially isolating active chromatographic fractions using PPARγ activation assays.…”

Section: Introductionmentioning

confidence: 99%

A New Agonist for Peroxisome Proliferation-activated Receptor γ (PPARγ), Fraglide-1 from Zhenjiang Fragrant Vinegar: Screening and Characterization Based on Cell Culture Experiments

Tsujino

2017

J. Oleo Sci.

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Oral Antihyperglycemic Treatment Options for Type 2 Diabetes Mellitus

Cited by 32 publications

References 113 publications

DPP-4 inhibitor plus SGLT-2 inhibitor as combination therapy for type 2 diabetes: from rationale to clinical aspects

DPP-4 inhibitor plus SGLT-2 inhibitor as combination therapy for type 2 diabetes: from rationale to clinical aspects

Diabetes-Old Therapies Revisited

A New Agonist for Peroxisome Proliferation-activated Receptor γ (PPARγ), Fraglide-1 from Zhenjiang Fragrant Vinegar: Screening and Characterization Based on Cell Culture Experiments

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