From the Guidelines
Lokelma (sodium zirconium cyclosilicate) works by selectively capturing potassium ions in the gastrointestinal tract, exchanging them for hydrogen and sodium ions, and eliminating them through feces, as stated in the study published in Mayo Clinic Proceedings 1. The mechanism of action of Lokelma involves:
- Selectively binding to potassium ions in the gastrointestinal tract
- Exchanging potassium ions for hydrogen and sodium ions
- Eliminating the bound potassium ions through feces This process helps to lower potassium levels in the blood, making Lokelma an effective treatment for hyperkalemia.
Key characteristics of Lokelma include:
- High selectivity for potassium ions
- Rapid onset of action, with significant reductions in serum potassium levels within 1 hour of administration 1
- Ability to maintain normokalemia over an extended period, as demonstrated in the DIALIZE study 1
- Low risk of serious adverse events, with the most common adverse events being hypokalemia and edema 1
The recommended dosing for Lokelma varies depending on the severity of hyperkalemia and the patient's response to treatment. For acute hyperkalemia, the recommended starting dose is 10g three times daily for up to 48 hours, followed by a maintenance dose of 5-10g once daily. For chronic hyperkalemia management, treatment typically begins with 10g once daily for 2-3 days, then adjusting to 5-15g once daily based on serum potassium levels 1.
It is essential to note that Lokelma should be taken as an oral suspension, mixed with water, and administered separately from other oral medications to prevent potential interactions. Overall, Lokelma is a valuable treatment option for patients with hyperkalemia, offering a rapid and effective way to lower potassium levels and reduce the risk of complications.
From the FDA Drug Label
LOKELMA (sodium zirconium cyclosilicate) is a non-absorbed zirconium silicate that preferentially captures potassium in exchange for hydrogen and sodium. In vitro, LOKELMA has a high affinity for potassium ions, even in the presence of other cations such as calcium and magnesium LOKELMA increases fecal potassium excretion through binding of potassium in the lumen of the gastrointestinal tract. Binding of potassium reduces the concentration of free potassium in the gastrointestinal lumen, thereby lowering serum potassium levels.
The mechanism of action (MoA) of Lokelma (sodium zirconium cyclosilicate) is as a potassium binder that preferentially exchanges potassium for hydrogen and sodium. It works by increasing fecal potassium excretion through binding of potassium in the gastrointestinal tract, which reduces the concentration of free potassium and thereby lowers serum potassium levels 2.
From the Research
Mechanism of Action of Lokelma (Sodium Zirconium Cyclosilicate)
- Lokelma (sodium zirconium cyclosilicate) is a non-absorbed, non-polymer zirconium silicate compound that preferentially exchanges hydrogen and sodium for potassium and ammonium ions in the gastrointestinal tract (GIT) 3.
- This exchange increases faecal potassium excretion and lowers serum potassium levels 3.
- The potassium lowering action of sodium zirconium cyclosilicate is predictable and rapid, leading to significant reduction of serum potassium within 1 hour of administration by irreversibly eliminating excess potassium rather than acting via intracellular translocation 4.
- Sodium zirconium cyclosilicate has a unique mechanism of action consisting of thermodynamically favorable sequestration of potassium ions, enabling rapid trapping and removal of excess potassium 4.
Key Features of Sodium Zirconium Cyclosilicate
- It is available as a powder for oral suspension (in water) and is approved in the EU and the USA for the treatment of hyperkalaemia in adults 3.
- Sodium zirconium cyclosilicate was generally well tolerated in adults with hyperkalaemia, with a tolerability profile similar to that of placebo over ≤ 28 days, and its safety profile appeared to remain consistent over the longer term (≤ 12 months) 3.
- The incidence of hypokalemia was low in patients treated with sodium zirconium cyclosilicate 3.