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Prescribing Information LOKELMA® (sodium zirconium cyclosilicate)
Adverse Event Reporting

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LOKELMA® (sodium zirconium cyclosilicate) is indicated for the treatment of hyperkalaemia in adult patients.

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  • Mechanism of action | LOKELMA (sodium zirconium cyclosilicate) | AstraZeneca UK
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Mechanism of action | LOKELMA (sodium zirconium cyclosilicate) | AstraZeneca UK

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LOKELMA®

(sodium zirconium cyclosilicate): Mode of action

LOKELMA® (sodium zirconium cyclosilicate) mechanism of action

In vitro, LOKELMA is a highly selective potassium (K+) binder for the treatment of hyperkalaemia.1,2

The mechanism of action of LOKELMA as a potassium binder

LOKELMA’s mechanism of action reduces potassium levels by facilitating its elimination through faeces, although LOKELMA works throughout the gastrointestinal (GI) tract. The distinctive crystal lattice configuration of sodium zirconium cyclosilicate selectively binds potassium ions, even in the presence of other cations, exchanging them for sodium and hydrogen ions.3

 

In vitro, LOKELMA works by effectively by capturing potassium throughout the GI tract. This process reduces the concentration of free potassium in the GI lumen.1-3

 

Consequently, this leads to decreased serum potassium levels and increased faecal potassium excretion, preventing its absorption into the bloodstream and ultimately resolving hyperkalaemia.

 

Due to LOKELMA’s mechanism of action, normokalaemia can be maintained if treatment is sustained. LOKELMA is generally well tolerated with limited drug-drug interactions and it can be used alongside oral medications that do not exhibit pH-dependent bioavailability.

More information on the safety of LOKELMA

Discover more about LOKELMA as a potassium binder

Watch this video to learn about the mechanism of action of LOKELMA.

Other video resources

LOKELMA’s onset of action

LOKELMA starts reducing serum potassium concentration as early as one hour after ingestion, and normokalaemia can typically be achieved within 24 to 48 hours.

More information about the efficacy of LOKELMA

Key molecular characteristics of LOKELMA

LOKELMA’s efficacy is underpinned by its key molecular features, contributing to its selective potassium binding and GI excretion.1-3

  • Inorganic crystalline compound
  • Non-polymer
  • Uniform micropore structure
  • Insoluble
  • Not systemically absorbed
  • Powder form

Importantly, LOKELMA has no effect on urinary sodium excretion, or serum calcium or magnesium concentrations.1,2

LOKELMA (sodium zirconium cyclosilicate) crystal structure

The sodium zirconium cyclosilicate structure consists of zirconium and silicon atoms which are respectively octahedrally and tetrahedrally coordinated with oxygen. Oxygen atoms act as bridges between these complexes to form a well-ordered cubic structure with microporous that effectively mimics the highly selective nature of physiologic K+ channels in the body. The pore opening, illustrated on the right-hand side, is composed of an asymmetrical seven-member ring. On average, the size of the sodium zirconium cyclosilicate pore opening was estimated to be ∼3 Å.3

crystal crystal

Adapted from Stavros et al. 2014.3

Images are illustrative only. Å is a metric unit of length equal to 10-10 m (0.1 nanometre).

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All Resources

Explore informative videos and guides to help you understand more about LOKELMA and support your patients

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LOKELMA dosing and administration card

This resource clarifies the dosing and administration information for LOKELMA

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Å, angstrom; GI, gastrointestinal; K+, potassium.

 
  1. Lokelma(R) Summary of Product Characteristics, Great Britain.
  2. Lokelma(R) Summary of Product Characteristics, Northern Ireland.
  3. Stavros F. et al. PLoS One. 2014;9(12):e114686.

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