Lokelma (sodium zirconium cyclosilicate)
Potassium-Removing Resins Oral Powder In Packet (EA)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Sodium zirconium cyclosilicate, a nonabsorbed cation-exchange crystalline compound, is used for the removal of excess potassium.
Sodium zirconium cyclosilicate is a highly selective inorganic cation-exchange crystalline compound that preferentially captures potassium in exchange for hydrogen (i.e., protons) and sodium. Sodium zirconium cyclosilicate binds potassium throughout the intestinal tract (including potassium in food), reducing the concentration of free potassium in the GI lumen, increasing fecal potassium excretion, and consequently reducing serum potassium concentrations. The drug's high specificity for potassium has been attributed to the chemical composition and diameter of the micropores contained in the zirconium silicate crystal structure, which mimic the action of physiologic potassium channels.
The potassium-binding capacity of sodium zirconium cyclosilicate is 9.3 times that of sodium polystyrene sulfonate. In vitro, sodium zirconium cyclosilicate has a high affinity for potassium ions, even in the presence of other cations (e.g., calcium, magnesium). Sodium zirconium cyclosilicate is more than 25 times more selective for potassium than for calcium and magnesium.
Compared with nonselective organic exchange resins that exert their function in the colon, the stable crystal structure of sodium zirconium cyclosilicate allows for binding of potassium throughout the entire lumen of the GI tract, including the acidic conditions of the duodenum. Sodium zirconium cyclosilicate is insoluble and does not absorb water within the GI tract.
Pharmacodynamic studies of sodium zirconium cyclosilicate have demonstrated efficient uptake and removal of potassium ions. In simulations performed in intestinal fluid, initial rapid uptake of potassium occurred within 5 minutes of administration, followed by a slower re-equilibration phase over a period of 20-100 minutes depending on the pH of the intestinal fluid and potassium concentration. When administered at dosages of 5 or 10 g daily for 4 days in healthy individuals, sodium zirconium cyclosilicate produced dose-dependent increases in fecal potassium excretion and corresponding decreases in urinary potassium excretion and serum potassium concentrations.
The potassium-lowering effect of sodium zirconium cyclosilicate is rapid in patients with hyperkalemia; in patients receiving a dosage of 10 g 3 times daily for up to 48 hours, reductions in serum potassium concentration were observed within 1 hour after administration of the first dose and continued to decline over the 48-hour treatment period. The degree of reduction was greater in patients with higher potassium concentrations at baseline. Serum potassium concentrations increased in patients who did not continue maintenance treatment.
Sodium zirconium cyclosilicate causes mild, dose-dependent increases in serum bicarbonate concentrations. Mild increases in urinary pH and reductions in blood urea nitrogen (BUN) also have been observed, which have been attributed to the binding of ammonium to sodium zirconium cyclosilicate. The clinical importance of these physiologic effects is not known.
Sodium zirconium cyclosilicate is neither systemically absorbed nor metabolized; in vivo mass balance studies demonstrated 99% fecal recovery of the drug in rats.
USES: This medication is used to treat high levels of potassium in the blood. It works by binding to potassium in the gut. This medication does not work right away, and should not be used to treat life-threatening high levels of potassium.
High potassium levels can cause symptoms such as nausea, muscle weakness/tiredness, irregular heartbeats, or paralysis.
Generic name: sodium zirconium cyclosilicate
Pronunciation: (SOE-dee-um zir-KOE-nee-um SYE-kloe-SIL-i-kate)
Drug class: Potassium-Removing Resins
Therapeutic class: Electrolyte Balance-Nutritional Products
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Lokelma
Indications
The following indications are listed for Lokelma:
- Hyperkalemia
Also known as: Hyperpotassemia.
Dosing
The recommended adult dosage of sodium zirconium cyclosilicate for the initial treatment of hyperkalemia is 10 g 3 times daily for up to 48 hours.
For continued maintenance treatment of hyperkalemia, the recommended adult dosage of sodium zirconium cyclosilicate is 10 g once daily. Serum potassium concentrations should be monitored and dosage should be adjusted accordingly. Dosage may be increased (in 5-g increments at intervals of 1 week or longer) or decreased, or therapy may be discontinued based on the patient's serum potassium concentration and desired target range. The recommended maintenance dosage range of sodium zirconium cyclosilicate is 5 g every other day to 15 g once daily.
No dosing information is available for this tab.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Lokelma 5 Gram Powder Packet | Maintenance | Take 1 packet (5 gram) mix in 45 mL water and drink immediately by oral route once daily rinse glass with water and drink for full dose. |
| Lokelma 10 Gram Powder Packet | Maintenance | Take 1 packet (10 gram) mix in 45 mL water and drink immediately by oral route once daily rinse glass with water and drink for full dose. |
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Potassium Binders/Potassium Supplements
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Patiromer, sodium polystyrene sulfonate and sodium zirconium cyclosilicate bind to potassium.(1-3)
CLINICAL EFFECTS: Concurrent use of potassium supplements and patiromer, sodium polystyrene sulfonate or sodium zirconium cyclosilicate may decrease the effectiveness of both agents.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Patients should normally not receive potassium supplements and patiromer, sodium polystyrene sulfonate or sodium zirconium cyclosilicate concurrently.(1-3) Patiromer, sodium polystyrene sulfonate or sodium zirconium cyclosilicate are indicated for management of hyperkalemia. Consider discontinuing or holding potassium supplements in patients who develop hyperkalemia requiring treatment.
DISCUSSION: Patiromer, sodium polystyrene sulfonate and sodium zirconium cyclosilicate are indicated for hyperkalemia. Consider discontinuing or holding potassium supplements in patients receiving sodium polystyrene sulfonate or sodium zirconium cyclosilicate.
There are no moderate interactions for this drug.
Contraindications
The manufacturer states that there are no known contraindications to the use of sodium zirconium cyclosilicate.
- Gastrointestinal obstruction
- Gastrointestinal hypomotility
- Chronic heart failure
- Kidney disease with likely reduction in glomerular filtration rate (GFr)
Adverse reactions
Adverse effects reported in 4% or more of patients receiving sodium zirconium cyclosilicate in clinical studies include edema and hypokalemia.
Less Frequent
- Hypokalemia
More Frequent
- Constipation
- Edema
- Peripheral edema
Less Frequent
- Diarrhea
- Hypomagnesemia
- Muscle spasm
Rare or Very Rare
- Gastroenteritis
- Hypocalcemia
- Vomiting
Precautions
No enhanced messaging available.
Safety and efficacy of sodium zirconium cyclosilicate have not been established in pediatric patients.
Because sodium zirconium cyclosilicate is not absorbed systemically following oral administration, use of the drug during pregnancy is not expected to result in fetal exposure.
Breast-feeding is not expected to result in infant exposure to sodium zirconium cyclosilicate because the drug is not systemically absorbed following oral administration.
In clinical studies of sodium zirconium cyclosilicate, 58% of patients receiving the drug were 65 years of age or older and 25% were 75 years of age or older. No overall differences were observed between geriatric patients and younger adults.
ICD codes
| Code | Type | Description |
|---|---|---|
| Hyperkalemia | ||
| E87.5 | ICD10CM | Hyperkalemia |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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