Metformin containing drugs
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Metformin Containing Drugs: Mechanisms and Benefits
Introduction to Metformin
Metformin is a widely prescribed biguanide drug primarily used to manage type 2 diabetes due to its efficacy in lowering plasma glucose levels and its safety profile2 4. Over the past 60 years, its applications have expanded beyond diabetes management to include potential benefits for various other diseases, including cancer, cardiovascular diseases, and even aging2 4.
Mechanisms of Action
Glucose Metabolism and Diabetes
Metformin's primary mechanism in diabetes management involves reducing hepatic glucose production. This is achieved through both AMP-activated protein kinase (AMPK)-dependent and AMPK-independent pathways3. Additionally, metformin inhibits mitochondrial respiration and possibly mitochondrial glycerophosphate dehydrogenase, contributing to its glucose-lowering effects3. Recent studies also suggest a significant role for the gut in mediating metformin's effects3.
Anti-Cancer Properties
Metformin has shown promising anti-cancer properties, although its single administration has not demonstrated convincing efficiency in clinical trials1. When combined with chemotherapeutic drugs, metformin can decrease toxicity and reduce tumor resistance, leading to better clinical outcomes1. The molecular mechanisms vary depending on the combination:
- Hormone Modulating Drugs: Activation of the AMPK/mTOR signaling pathway1.
- Anti-Metabolites: Suppression of HIF-1, p-gp, and MRP1 protein expression1.
- Antibiotics: Inhibition of oxidative stress and inflammatory signaling pathways, providing cardio-protective effects1.
- Cisplatin: Induction of apoptotic mitochondria and nucleus1.
- Taxane: Down-regulation of lipoprotein or cholesterol synthesis1.
Broader Health Benefits
Cardiovascular and Renal Diseases
Metformin has demonstrated cardiovascular protective effects, which are partly attributed to its ability to inhibit oxidative stress and inflammatory pathways1 4. Additionally, it has shown benefits in managing renal diseases, although the exact mechanisms remain to be fully elucidated2.
Anti-Aging and Neuroprotection
Emerging evidence suggests that metformin may have anti-aging properties and neuroprotective effects. These benefits are thought to be mediated through various signaling pathways, although more research is needed to fully understand these mechanisms2 4.
Other Potential Indications
Metformin is also being explored as a treatment option for polycystic ovary syndrome (PCOS) due to its ability to improve insulin sensitivity and lower androgen levels4. Its potential role in treating obesity and liver diseases further highlights its versatility as a therapeutic agent2 4.
Conclusion
Metformin is a multifaceted drug with a wide range of applications beyond its primary use in managing type 2 diabetes. Its combination with other chemotherapeutic drugs shows promise in cancer treatment, while its benefits extend to cardiovascular protection, anti-aging, and neuroprotection. Understanding the diverse molecular mechanisms of metformin is crucial for optimizing its use in personalized medicine and achieving better clinical outcomes.
Sources and full results
Most relevant research papers on this topic
Combination of metformin with chemotherapeutic drugs via different molecular mechanisms.
Combining metformin with chemotherapeutic drugs can decrease toxicity and attenuate tumor resistance, with diverse molecular mechanisms playing a role in their synergistic effects.
Highly CitedMetformin and Its Benefits for Various Diseases
Metformin offers benefits for various diseases and aging, with potential underlying mechanisms still unclear.
Highly CitedThe mechanisms of action of metformin
Metformin improves glucose metabolism and diabetes-related complications through multiple mechanisms, including reducing hepatic glucose production and a key role for the gut.
Rigorous JournalHighly CitedMetformin: a review of its potential indications
Metformin may have potential roles beyond glucose lowering in type 2 diabetes, including antitumor effects, antiaging, cardiovascular protection, neuroprotective effects, and polycystic ovary syndrome treatment.
Literature ReviewRigorous JournalHighly CitedMetformin: An Old Drug with New Applications
Metformin may treat nonalcoholic fatty liver disease, cancer, obesity, and metabolic syndrome, but more clinical evidence is needed to confirm its benefits and prevent liver tumorigenesis.
Highly CitedMetformin and Aging: A Review
Metformin may be an "anti-aging" drug, but concerns exist about vitamin B12 and B6 deficiencies and potential adverse effects on cardiovascular fitness from exercise.
Literature ReviewHighly CitedMetformin: clinical use in type 2 diabetes
Metformin is a popular oral glucose-lowering medication for type 2 diabetes, with benefits including improved lipids, reduced cardiovascular events, and a lenient regulatory approach for patients with mild renal dysfunction.
Rigorous JournalHighly CitedRole of AMP-activated protein kinase in mechanism of metformin action.
Metformin's beneficial effects on lipids and glucose metabolism are due to activation of AMP-activated protein kinase, which reduces lipogenic enzyme expression and inhibits glucose production in hepatocytes.
Non-RCT
Animal StudyHighly CitedClinical Pharmacokinetics of Metformin
Metformin's pharmacokinetics and clinical response are largely mediated by organic cation transporters, with minimal impact on lactic acidosis risk.
Rigorous JournalHighly CitedMetformin: from mechanisms of action to therapies.
Metformin's mechanism of action centers on energy metabolism, with potential relevance to cardiovascular diseases and cancer, and its AMPK-dependent and -independent mechanisms influence its effectiveness.
Very Rigorous JournalHighly Cited