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Sodium zirconium cyclosilicate: Drug information

Sodium zirconium cyclosilicate: Drug information
(For additional information see "Sodium zirconium cyclosilicate: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Lokelma
Brand Names: Canada
  • Lokelma
Pharmacologic Category
  • Antidote;
  • Potassium Binder
Dosing: Adult
Hyperkalemia, chronic

Hyperkalemia, chronic:

Oral: Initial: 10 g 3 times daily for up to 48 hours, followed by 10 g once daily; adjust dose by 5 g daily at ≥1-week intervals as needed based on serum potassium levels. Usual dosage range: 5 g once every other day to 15 g once daily; maximum maintenance dose: 15 g/day.

Hyperkalemia, severe/emergent

Hyperkalemia, severe/emergent (adjunctive agent) (off-label use): Note: May be used for severe/emergent hyperkalemia (in combination with other acute therapies) to facilitate the elimination of potassium (Ref).

Oral: Initial: 10 g 3 times daily for up to 48 hours (Ref).

Dosing: Kidney Impairment: Adult

The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.

Hyperkalemia, chronic:

Altered kidney function: No dosage adjustment necessary for any degree of kidney dysfunction (minimal systemic absorption) (Ref).

Hemodialysis, intermittent (thrice weekly): Initial: 5 g once daily on nondialysis days (an initial dose of 10 g once daily on nondialysis days may be considered in patients with serum potassium level >6.5 mEq/L); adjust dose at 1-week intervals based on predialysis serum potassium measured after the long interdialytic interval and desired target range; maintenance: 5 to 15 g once daily on nondialysis days.

Peritoneal dialysis: No dosage adjustment necessary (minimal systemic absorption) (Ref).

Hyperkalemia, severe/emergent (off-label use): No dosage adjustment necessary for any degree of kidney dysfunction, including patients receiving kidney replacement therapies (minimal systemic absorption) (Ref).

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Adjustment for Toxicity: Adult

Serum potassium below desired target range or for clinically significant hypokalemia: Decrease dose or discontinue therapy.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Cardiovascular: Edema (4% to 16%)

1% to 10%: Endocrine & metabolic: Hypokalemia (3% to 4%)

Contraindications

There are no contraindications listed in the US manufacturer's labeling.

Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to sodium zirconium cyclosilicate or any component of the formulation.

Warnings/Precautions

Concerns related to adverse effects:

• Edema: Mild to moderate edema has been reported and was more common in patients not on dialysis or treated with higher doses. Monitor for signs of edema, especially in patients on sodium-restricted diet or who are prone to fluid overload (eg, heart failure, renal disease).

Disease-related concerns:

• GI motility disorders: Avoid use in patients with severe constipation, bowel obstruction or impaction, including abnormal postoperative bowel motility disorders (may be ineffective and may worsen GI conditions).

Special populations:

• Hemodialysis patients: May be at increased risk of hypokalemia due to associated conditions (eg, diarrhea, decreased oral intake); monitor serum potassium and adjust dose accordingly.

Dosage form specific issues:

• Sodium: Each 5 g dose contains ~400 mg sodium. Adjust dietary sodium intake as needed.

Other warnings or precautions:

• Abdominal x-rays: Sodium zirconium cyclosilicate has radio-opaque properties; may appear as an imaging agent on abdominal x-ray.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Packet, Oral:

Lokelma: 5 g (1 ea, 11 ea, 30 ea); 10 g (1 ea, 11 ea, 30 ea)

Generic Equivalent Available: US

No

Pricing: US

Pack (Lokelma Oral)

5 g (per each): $32.82

10 g (per each): $32.82

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Packet, Oral:

Lokelma: 5 g (3 ea, 30 ea); 10 g (3 ea, 30 ea)

Administration: Adult

Oral: Empty entire contents of the packet(s) into a glass with ≥3 tablespoons (45 mL) of water. Stir well and drink immediately; if powder remains in the glass, add water, stir and drink immediately; repeat until no powder remains. Administer other oral medications ≥2 hours before or 2 hours after dose.

Use: Labeled Indications

Hyperkalemia, chronic: Treatment of hyperkalemia in adults.

Use: Off-Label: Adult

Hyperkalemia, severe/emergent

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Clopidogrel: Sodium Zirconium Cyclosilicate may decrease serum concentrations of the active metabolite(s) of Clopidogrel. Management: Separate the administration of sodium zirconium cyclosilicate and clopidogrel by at least 2 hours. Risk D: Consider therapy modification

Dabigatran Etexilate: Sodium Zirconium Cyclosilicate may decrease the serum concentration of Dabigatran Etexilate. Management: Separate the administration of sodium zirconium cyclosilicate and dabigatran by at least 2 hours. Risk D: Consider therapy modification

Tacrolimus (Systemic): Sodium Zirconium Cyclosilicate may decrease the serum concentration of Tacrolimus (Systemic). Management: Separate the administration of sodium zirconium cyclosilicate and tacrolimus by at least 2 hours. Risk D: Consider therapy modification

Warfarin: Sodium Zirconium Cyclosilicate may increase the serum concentration of Warfarin. Management: Separate the administration of sodium zirconium cyclosilicate and warfarin by at least 2 hours. If simultaneous administration is required, monitor for signs and symptoms of warfarin toxicity (eg, elevated INR, bleeding). Risk D: Consider therapy modification

Pregnancy Considerations

Sodium zirconium cyclosilicate is not systemically absorbed, therefore, exposure to the fetus would not be expected.

Breastfeeding Considerations

Sodium zirconium cyclosilicate is not systemically absorbed, therefore, distribution into breast milk would not be expected.

Monitoring Parameters

Serum potassium; signs/symptoms of edema

Reference Range

Note: Reference ranges may vary depending on the laboratory.

Serum potassium: Adults: 3.5 to 5 mEq/L.

Mechanism of Action

Sodium zirconium cyclosilicate is a potassium binder that preferentially exchanges potassium for hydrogen and sodium. Binding of potassium reduces the concentration of free potassium in the gastrointestinal lumen, lowering serum potassium levels.

Pharmacokinetics (Adult Data Unless Noted)

Onset: 1 hour

Absorption: Not systemically absorbed

Metabolism: None

Excretion: Feces

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Lokelma;
  • (AR) Argentina: Lokelma;
  • (AT) Austria: Lokelma;
  • (BE) Belgium: Lokelma;
  • (BG) Bulgaria: Lokelma;
  • (CN) China: Lokelma;
  • (CO) Colombia: Lokelma;
  • (DE) Germany: Lokelma;
  • (ES) Spain: Lokelma;
  • (FI) Finland: Lokelma;
  • (GB) United Kingdom: Lokelma;
  • (GR) Greece: Lokelma;
  • (IE) Ireland: Lokelma;
  • (IT) Italy: Lokelma;
  • (LU) Luxembourg: Lokelma;
  • (LV) Latvia: Lokelma;
  • (NL) Netherlands: Lokelma;
  • (NO) Norway: Lokelma;
  • (PR) Puerto Rico: Lokelma;
  • (QA) Qatar: Lokelma;
  • (SA) Saudi Arabia: Lokelma;
  • (SE) Sweden: Lokelma;
  • (SI) Slovenia: Lokelma
  1. Clase CM, Carrero JJ, Ellison DH, et al; Conference Participants. Potassium homeostasis and management of dyskalemia in kidney diseases: conclusions from a Kidney Disease: Improving Global Outcomes (KDIGO) Controversies Conference. Kidney Int. 2020;97(1):42-61. doi:10.1016/j.kint.2019.09.018 [PubMed 31706619]
  2. Expert opinion. Senior Renal Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
  3. Kosiborod M, Peacock WF, Packham DK. Sodium zirconium cyclosilicate for urgent therapy of severe hyperkalemia. N Engl J Med. 2015;372(16):1577-1578. doi:10.1056/NEJMc1500353 [PubMed 25875277]
  4. Lokelma (sodium zirconium cyclosilicate) [prescribing information]. Wilmington, DE: AstraZeneca Pharmaceuticals LP; September 2022.
  5. Lokelma (sodium zirconium cyclosilicate) [product monograph]. Mississauga, Ontario, Canada: AstraZeneca Canada Inc; September 2022.
  6. Mount DB. Treatment and prevention of hyperkalemia in adults. Post TW, ed. UpToDate. Waltham, MA: UpToDate Inc. http://www.uptodate.com. Accessed November 9, 2021.
  7. Packham DK, Rasmussen HS, Lavin PT, et al. Sodium zirconium cyclosilicate in hyperkalemia. N Engl J Med. 2015;372(3):222-231 [PubMed 25415807]
  8. Palmer BF, Carrero JJ, Clegg DJ, et al. Clinical management of hyperkalemia. Mayo Clin Proc. 2021;96(3):744-762. doi:10.1016/j.mayocp.2020.06.014 [PubMed 33160639]
  9. Peacock WF, Rafique Z, Vishnevskiy K, et al. Emergency potassium normalization treatment including sodium zirconium cyclosilicate: a phase II, randomized, double-blind, placebo-controlled study (ENERGIZE). Acad Emerg Med. 2020;27(6):475-486. doi:10.1111/acem.13954 [PubMed 32149451]
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