Related Experiment Video
Updated: Sep 27, 2025
06:34
Validation of Therapeutic Agent Conjugation to Polyvinyl Alcohol-Coated Medical Devices
Published on: November 29, 2024
370
SGLT2 Inhibitors: Physiology and Pharmacology
1Department of Physiology, David Geffen School of Medicine at UCLA, Los Angeles, California.
Kidney360
|April 14, 2022
Summary
Sodium-glucose cotransporter 2 (SGLT2) inhibitors reduce glucose reabsorption in the kidneys. These drugs effectively lower blood glucose and glycosylated hemoglobin levels in type 2 diabetes patients.
Area of Science:
- Nephrology
- Endocrinology
- Pharmacology
Background:
- Sodium-glucose cotransporters (SGLTs) are proteins in the kidney's proximal tubule responsible for reabsorbing glucose.
- SGLT2, specifically, reabsorbs 50-60% of filtered glucose daily.
- Phlorizin, a natural compound, is known to inhibit glucose reabsorption.
Purpose of the Study:
- To review the physiology of renal SGLTs.
- To summarize the pharmacology of SGLT inhibitors.
Main Methods:
- Review of existing literature on SGLT physiology and SGLT inhibitor pharmacology.
- Analysis of the mechanism of action of SGLT2 inhibitors.
Main Results:
- Oral SGLT2 inhibitors are absorbed into the bloodstream and circulate for hours.
- These inhibitors bind to SGLT2 in the proximal tubule, reducing glucose reabsorption.
- Glucose excretion leads to lower plasma glucose and HbA1c levels in type 2 diabetes.
Conclusions:
- SGLT2 inhibitors are effective in managing hyperglycemia in type 2 diabetes mellitus.
- These drugs offer protective benefits for the heart and kidneys.
- Understanding SGLT physiology is crucial for developing targeted diabetes therapies.
Related Concept Videos
01:27Glucose Transporters
25.2K
Glucose transporters facilitate the transport of glucose across the cell membrane. In addition to glucose, some glucose transporters can also aid the movement of other hexoses such as fructose, mannose, and galactose.
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:
25.2K
01:32Secondary Active Transport
7.9K
One example of how cells use the energy contained in electrochemical gradients is demonstrated by glucose transport into cells. The ion vital to this process is sodium (Na+), which is typically present in higher concentrations extracellularly than in the cytosol. Such a concentration difference is due, in part, to the action of an enzyme "pump" embedded in the cellular membrane that actively expels Na+ from a cell. Importantly, as this pump contributes to the high concentration of...
7.9K
01:19Oral Hypoglycemic Agents: α-Glucosidase Inhibitors
293
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.
Acarbose and miglitol are...
Acarbose and miglitol are...
293
01:23Dipeptidyl Peptidase 4 Inhibitors
274
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...
274
01:26Glucose Absorption Into the Small Intestine
32.6K
Complex carbohydrates consumed cannot be absorbed into the small intestine in their original form. First, they must be hydrolyzed to a monosaccharide form such as glucose or galactose. These monosaccharides are then transported across the intestinal membrane and into the blood via transcellular transport. The intestinal epithelial cells allow the movement of these monosaccharides with a defined 'entry' through membrane transporter proteins present on their apical membrane and...
32.6K
01:23Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists
443
Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
443