Lokelma
Lokelma Uses, Dosage, Side Effects, Food Interaction and all others data.
Lokelma is approved as the trade product Lokelma developed by AstraZeneca - an insoluble, non-absorbed sodium zirconium silicate, formulated as a powder for oral suspension that acts as a highly selective potassium removing agent. It is administered orally and is odorless, tasteless, and stable at room temperature. Approval of the medication is supported by data from three double-blind, placebo-controlled trials and two open-label trials which showed that the onset of action was approximately 1.0 hour and the median time to achieving normal potassium levels in the blood was 2.2 hours, with 92% of patients achieving normal potassium levels within 48 hours following administration. The treatment effect was maintained for up to 12 months.
Lokelma is capable of reducing serum potassium concentrations as quickly as one hour after ingestion and normokalaemia can be achieved typically within 24 to 48 hours. Lokelma does not affect serum calcium or magnesium concentrations, or urinary sodium excretion. A close correlation is observed between starting serum potassium levels and effect size; patients with higher starting serum potassium levels have greater reductions in serum potassium. As a consequence of the resultant reduction in serum potassium concentration, there is a reduction in urinary potassium excretion as well. In a study of healthy subjects given sodium zirconium cyclosilicate 5 or 10 grams daily for four days, a dose-dependent reduction in serum potassium concentration and total urinary potassium excretion were accompanied by mean increases in fecal potassium excretion. No statistically significant changes in urinary sodium excretion were observed.
Lokelma has also been observed to bind ammonium in vitro and in vivo, thereby removing ammonium and increasing serum bicarbonate levels. Patients treated with sodium zirconium cyclosilicate were documented as experiencing an increase of 1.1 mmol/L at 5 g once daily, 2.3 mmol/L at 10 g once daily, and 2.6 mmol/L at 15 g once daily in bicarbonate compared with a mean increase of 0.6 mmol/L for the patients receiving placebo. In an environment where other factors affecting renin and aldosterone were not controlled, sodium zirconium cyclosilicate demonstrated a dose-independent reduction in mean serum aldosterone levels (range of -30% to -31%) compared with the placebo group (+14%). No consistent effect on systolic and diastolic blood pressure has yet to be observed.
| Trade Name | Lokelma |
| Generic | Sodium zirconium cyclosilicate |
| Sodium zirconium cyclosilicate Other Names | Sodium zirconium cyclosilicate, Sodium zirconium silicate |
| Weight | 10g, 5g, |
| Type | Oral Suspension, Oral Powder For Reconstitution |
| Formula | Na2O9Si3Zr |
| Weight | Average: 365.452 Monoisotopic: 363.77144 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | AstraZeneca UK Limited |
| Available Country | United Kingdom, United States, |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lokelma is a potassium binder used to treat hyperkalemia.
Lokelma is a potassium binder indicated for the treatment of hyperkalemia in adult patients.
Lokelma is also used to associated treatment for these conditions: Hyperkalemia
How Lokelma works
Hyperkalemia is a condition defined by elevated potassium levels in the blood, often caused by cardiovascular, renal, and metabolic diseases. Hyperkalemia occurs in 23 to 47% of patients with chronic kidney disease and/or chronic heart failure, and may lead to cardiac arrest and death.
Lokelma is subsequently a non-absorbed, non-polymer inorganic powder with a uniform micropore structure that preferentially captures potassium in exchange for hydrogen and sodium cations. Lokelma is highly selective for potassium ions, even in the presence of other cations such as calcium and magnesium, in vitro. Lokelma captures potassium throughout the entire gastrointestinal (GI) tract and reduces the concentration of free potassium in the GI lumen, thereby lowering serum potassium levels and increasing fecal potassium excretion to resolve hyperkalemia.
Toxicity
Overdose with sodium zirconium cyclosilicate could lead to hypokalemia.
Food Interaction
No interactions found.Elimination Route
Lokelma is an inorganic, insoluble compound that is not susceptible to enzymatic metabolism. Additionally, studies have shown it not to be systemically absorbed either. An in vivo mass balance study in rats showed that sodium zirconium cyclosilicate was recovered in the feces with no evidence of systemic absorption.
Elimination Route
Lokelma is eliminated in the feces.
Innovators Monograph
You find simplified version here Lokelma
