Product Information
Registration Status: ActiveLOKELMA POWDER FOR ORAL SUSPENSION 10G is approved to be sold in Singapore with effective from 2020-06-22. It is marketed by ASTRAZENECA SINGAPORE PTE LTD, with the registration number of SIN15962P.
This product contains Sodium Zirconium Cyclosilicate 10g/sachet in the form of POWDER, FOR SUSPENSION. It is approved for ORAL use.
This product is manufactured by Sharp Corporation (Primary and Secondary packager) in UNITED STATES,Sharp Corporation (Primary and Secondary packager) in UNITED STATES,Sharp Corporation (Primary and Secondary packager) in UNITED STATES,.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Sodium zirconium cyclosilicate 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 [L2933]. It is administered orally, is odorless, tasteless, and stable at room temperature [L2933]. It is a new medication that offers rapid and sustained treatment for adults with hyperkalaemia [L2933]. Approvals of the medication is supported by data from three double-blind, placebo controlled trials and two open-label trials which show that for patients receiving Lokelma the onset of action was at 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 from baseline [L2933]. The treatment effect was maintained for up to 12 months [L2933].
Indication
Sodium zirconium cyclosilicate is a potassium binder indicated for the treatment of hyperkalemia in adult patients [FDA Label, F130].
Mechanism of Action
Hyperkalemia is a condition defined by elevated potassium levels in the blood, often caused by cardiovascular, renal, and metabolic diseases [L2930]. 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 [L2930]. Sodium zirconium cyclosilicate 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 [FDA Label, F130]. Sodium zirconium cyclosilicate is highly selective for potassium ions, even in the presence of other cations such as calcium and magnesium, in vitro [FDA Label, F130]. Sodium zirconium cyclosilicate 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 [FDA Label, F130].
Pharmacokinetics
- Absorption
- Sodium zirconium cyclosilicate is an inorganic, insoluble compound that is not susceptible to enzymatic metabolism [F130]. Additionally, studies have shown it not to be systemically absorbed either [F130]. An in vivo mass balance study in rats showed that sodium zirconium cyclosilicate was recovered in the feces with no evidence of systemic absorption [F130]. Due to these factors and its insolubility, no in vivo or in vitro studies have thus far been performed to examine its effect on cytochrome P450 (CYP450) enzymes or transporter activity [F130].
- Distribution
- Sodium zirconium cyclosilicate is an inorganic, insoluble compound that is not susceptible to enzymatic metabolism [F130]. Additionally, studies have shown it not to be systemically absorbed either [F130]. An in vivo mass balance study in rats showed that sodium zirconium cyclosilicate was recovered in the feces with no evidence of systemic absorption [F130]. Due to these factors and its insolubility, no in vivo or in vitro studies have thus far been performed to examine its effect on cytochrome P450 (CYP450) enzymes or transporter activity [F130].
- Metabolism
- Sodium zirconium cyclosilicate is an inorganic, insoluble compound that is not susceptible to enzymatic metabolism [F130]. Additionally, studies have shown it not to be systemically absorbed either [F130]. An in vivo mass balance study in rats showed that sodium zirconium cyclosilicate was recovered in the feces with no evidence of systemic absorption [F130]. Due to these factors and its insolubility, no in vivo or in vitro studies have thus far been performed to examine its effect on cytochrome P450 (CYP450) enzymes or transporter activity [F130].
- Elimination
Clearance
Sodium zirconium cyclosilicate is an inorganic, insoluble compound that is not susceptible to enzymatic metabolism [F130]. Additionally, studies have shown it not to be systemically absorbed either [F130]. An in vivo mass balance study in rats showed that sodium zirconium cyclosilicate was recovered in the feces with no evidence of systemic absorption [F130]. Due to these factors and its insolubility, no in vivo or in vitro studies have thus far been performed to examine its effect on cytochrome P450 (CYP450) enzymes or transporter activity [F130].
Toxicity
Overdose with sodium zirconium cyclosilicate could lead to hypokalaemia [FDA Label, F130].
Active Ingredient/Synonyms
Sodium zirconium silicate | Sodium zirconium cyclosilicate |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.