Since heart disease is the leading cause of death in people with diabetes, these new treatment options including PCSK9 Inhibitors and ACL Inhibitors, offer hope of decreasing cardiovascular mortality and morbidity. In addition rates of Chronic Kidney Disease (CKD) rates are rising worldwide and people with diabetes account for the majority of people receiving treatment for end-stage renal disease.
The new nonsteroidal Selective Mineralcorticoid Antagonists reduce the risk of kidney function decline and failure, plus reduce risk of cardiovascular death. We asked our PharmD experts to update our Cheat Sheets with the latest info and provide a summary of these medication classes, action and considerations. Special thanks to our contributing experts Diana Isaacs, PharmD, BCPS, BCACP, BC-ADM, CDCES, FADCES, FCCP and Kristapor Thomassian, PharmD, BCPS.
Download Updated Cheat Sheets Here
PCSK9 Inhibitors (proprotein convertase subtillisin / kexin type 9)
This class of drugs are monoclonal antibodies designed to bind to the PCSK9 enzyme in the liver. PCSK9 enzyme is involved in inactivating LDL receptors, resulting in continued high levels of LDL circulating in the blood. The PCSK9 inhibitors (monoclonal antibodies) bind to the enzyme and increase the LDL receptors, helping reduce circulating LDL in the blood by appropriately metabolizing LDL in the liver.
There are specific FDA approved indications for this class of medications. Please refer to appropriate guidelines to determine if the individual meets criteria for agents in this class for treatment.
ACL Inhbitor (Adenosine Triphosphte-citrate Lyase)
This class of drug is designed to bind to the ATP-citrate Lyase enzyme. The ATP-citrate Lyase enzyme is the one of the initial enzymes involved in Cholesterol synthesis. Statins are the main class of agents we currently use to help block the HMG-CoA reductase enzyme, one of the primary enzymes involved in cholesterol production. The ACL inhibitor works upstream on the same cascade to help reduce cholesterol production, to achieve additional LDL lowering.
Nonsteroidal Selective Mineralocorticoid Receptor Antagonist
This class of drug is designed to bind to the Mineralocorticoid receptor. Mineralocorticoid receptors are found in regions most important for regulating electrolytes like sodium and potassium in key organs such as the kidney, heart and brain. Reducing the progression of chronic kidney disease (CKD) is one of our most important goals in keeping preventing end stage renal disease and CB events. Excess aldosterone production, the primary steroid based mineralocorticoid found in our bodies, has been implicated in nephrololgy and cardiovascular pathophysiology. The mineralocorticoid receptor antagonist blocks the effects of aldosterone and reduces the risk of kidney function decline as well as heart failure.
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