Embedded Files
Insulin Sensitizers:
An insulin sensitizer is a medication that helps the body use insulin more effectively, typically used to treat type 2 diabetes. They work by increasing the sensitivity of cells to insulin, allowing glucose to enter cells more easily and lowering blood sugar levels. Common examples include metformin and thiazolidinediones (TZDs).
History:
One of the earliest insulin sensitizers was metformin, which has been in use since the 1950s. It works by decreasing glucose production in the liver and increasing insulin sensitivity in muscle tissue.
Another class of insulin sensitizers is thiazolidinediones (TZDs), which include drugs like rosiglitazone and pioglitazone. These became available in the late 1990s and early 2000s. TZDs work by increasing insulin sensitivity in fat, muscle, and liver tissues.
How Insulin Sensitizers Work
*Enhance Glucose Uptake
Insulin sensitizers increase the ability of cells to utilize glucose, improving overall glucose homeostasis.
*Reduce Hepatic Glucose Production
These medications also decrease the liver's output of glucose, further lowering blood sugar levels.
*Improve Insulin Signaling
Insulin sensitizers optimize the body's response to insulin, enhancing its effects on target tissues
Common Insulin Sensitizers:
*Metformin:The first-line medication for type 2 diabetes, metformin primarily reduces hepatic glucose production
*Thiazolidinediones:These drugs, like pioglitazone, target nuclear receptors to enhance insulin sensitivity in peripheral tissues
*Biguanides:In addition to metformin, other biguanides like phenformin can also improve insulin sensitivity.
Mechanism of action:
Mechanism of Action: Thiazolidinediones
Thiazolidinediones (TZDs), another class of insulin sensitizers, primarily work by activating the peroxisome proliferator-activated receptor-gamma (PPAR-γ) nuclear receptor. This activation leads to a cascade of effects that ultimately improve insulin sensitivity and glucose homeostasis.
Mechanism of Action: Metformin
Metformin, a widely used insulin sensitizer, primarily works by activating the AMP-activated protein kinase (AMPK) pathway. This pathway plays a crucial role in cellular energy homeostasis, and its activation by metformin leads to a cascade of events that ultimately improve insulin sensitivity and glucose metabolism
pharmacokinetics:
Metformin is rapidly distributed following absorption and does not bind to plasma proteins. No metabolites or conjugates of metformin have been identified. The absence of liver metabolism clearly differentiates the pharmacokinetics of metformin from that of other biguanides, such as phenformin
Thiazolidinediones are taken orally, once a day, with or without food. The maximal effect is not seen for 6 to 12 weeks. They are metabolized by the cytochrome P450 oxidative enzyme system
Considerations with Insulin Sensitizers
*Tolerability:
Gastrointestinal side effects, like nausea and diarrhea, are common with some insulin sensitizers.
*Contraindications:
Certain conditions, like renal impairment, may limit the use of specific insulin sensitizing agents.
*Monitoring:
Regular monitoring of liver and kidney function is recommended when prescribing insulin sensitizers.
*Combination Therapy:
Insulin sensitizers are often used in combination with other diabetes medications for optimal glycemic control
Drug interaction:
Metformin can interact with some diabetes medications that decrease blood glucose, including insulin, glipizide (Glucotrol XL), and repaglinide. It may also interact with medications that can raise blood glucose. Examples of these medications include prednisone and hydrochlorothiazide (Microzide).
The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Chlorthalidone. Choline salicylate may increase the hypoglycemic activities of 2,4-thiazolidinedione. The risk or severity of hyperglycemia can be increased when Ciclesonide is combined with 2,4-thiazolidinedione
Side effect
whatch it!
Monograph
pharma activity٠٠.docxmenna.docxPage updated
Report abuse