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Repaglinide (Prandin) and Nateglinide (Starlix), known as glinides, are oral insulin secretagogues that stimulate insulin release from pancreatic β cells by closing the ATP-sensitive potassium channels (KATP channel). Repaglinide controls insulin release from pancreatic β cells by managing potassium efflux. It shares two binding sites with sulfonylureas and also has a unique site, indicating overlapping mechanisms of action. With a rapid onset and a 4-7 hour duration, it effectively...
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Biguanides, particularly metformin (Glucophage), are insulin sensitizers that enhance glucose uptake, thereby reducing insulin resistance. Unlike sulfonylureas, metformin doesn't prompt insulin secretion, which helps to curb hypoglycemia risk. Metformin is beneficial in treating conditions like polycystic ovary syndrome due to its insulin-resistance reduction capability. The drug's primary action involves curtailing hepatic gluconeogenesis, a significant contributor to high blood...
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Dipeptidyl Peptidase 4 Inhibitors01:23

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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
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α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
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Oral Hypoglycemic Agents: Sulfonylureas01:17

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Updated: May 1, 2026

Glucose Uptake Measurement and Response to Insulin Stimulation in In Vitro Cultured Human Primary Myotubes
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Dapagliflozin: glucuretic action and beyond.

Pitchai Balakumar1, Karupiah Sundram2, Sokkalingam A Dhanaraj3

  • 1Pharmacology Unit, Faculty of Pharmacy, Asian Institute of Medicine, Science and Technology (AIMST) University, Semeling, 08100 Bedong, Kedah Darul Aman, Malaysia.

Pharmacological Research
|April 8, 2014
PubMed
Summary

Dapagliflozin, an SGLT2 inhibitor, helps manage type 2 diabetes by increasing glucose excretion. This drug may also lower blood pressure and promote weight loss in diabetic patients.

Keywords:
DapagliflozinDiabetes mellitusPerspectivesSGLT2 inhibition

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Area of Science:

  • Pharmacology
  • Endocrinology
  • Nephrology

Background:

  • Type 2 diabetes mellitus (T2DM) management remains challenging despite available treatments.
  • Sodium-glucose co-transporter type 2 (SGLT2) in the kidney is crucial for glucose reabsorption.
  • Targeting SGLT2 offers a novel approach to glycemic control.

Purpose of the Study:

  • To review the pharmacology of dapagliflozin, a selective SGLT2 inhibitor.
  • To explore the potential dual antidiabetic effects of dapagliflozin.
  • To discuss additional benefits in hypertensive, obese T2DM patients.

Main Methods:

  • Review of existing literature on SGLT2 inhibitors and dapagliflozin.
  • Analysis of dapagliflozin's mechanism of action (SGLT2 inhibition and glucosuria).
  • Discussion of potential secondary effects like diuresis and weight reduction.

Main Results:

  • Dapagliflozin selectively inhibits SGLT2, leading to urinary glucose excretion (glucosuria).
  • It improves glycemic control, reduces HbA1c, and promotes weight loss.
  • Potential for improved insulin sensitivity, blood pressure reduction, and calorie deficit.

Conclusions:

  • Dapagliflozin offers a unique mechanism for T2DM management via SGLT2 inhibition.
  • It presents potential benefits beyond glycemic control, including cardiovascular and weight management.
  • Further long-term studies are required to confirm these additional therapeutic advantages.