LOKELMA
Clinical safety rating
cautionComprehensive clinical and safety monograph for LOKELMA (LOKELMA).
Comprehensive clinical and safety monograph for LOKELMA (LOKELMA).
Treatment of hyperkalemiaOff-label: Management of hyperkalemia in patients with chronic kidney disease on renin-angiotensin-aldosterone system inhibitors
Patiromer, a non-absorbed potassium-binding polymer, exchanges calcium for potassium ions in the gastrointestinal tract, thereby increasing fecal potassium excretion and lowering serum potassium levels.
| Metabolism | Patiromer is not absorbed systemically and not metabolized; it is excreted unchanged in feces. |
| Excretion | Primarily eliminated unchanged in feces (approximately 90%) via gastrointestinal transit; <1% excreted in urine as absorbed sodium zirconium cyclosilicate is negligible. |
| Half-life | Not applicable as LOKELMA is not systemically absorbed; terminal half-life is not measurable in traditional sense. Clinical effect duration correlates with gastrointestinal transit time (~6-8 hours for peak potassium lowering). |
| Protein binding | Not bound to plasma proteins as it is non-absorbed and acts locally in the gastrointestinal tract. |
| Volume of Distribution | Not applicable (locally acting, non-absorbed); apparent Vd is negligible due to lack of systemic absorption. |
| Bioavailability | Oral bioavailability is <1% as the drug is not absorbed from the gastrointestinal tract. |
| Onset of Action | Onset of serum potassium reduction occurs within 1 hour following oral administration (suspension), reaching peak effect at approximately 4 hours. |
| Duration of Action | Duration of effect persists for up to 24 hours after a single dose; repeated dosing maintains effect throughout treatment period. |
| Molecular Weight | 1442 |
5 g (one packet) orally three times daily; titrate to maintain serum potassium 4.0-5.0 mEq/L; maximum 15 g three times daily (45 g/day).
| Dosage form | FOR SUSPENSION |
| Renal impairment | No dose adjustment required based on GFR; monitor serum potassium more frequently in patients with eGFR <30 mL/min/1.73m² due to increased risk of hypokalemia. |
| Liver impairment | No dose adjustment required for Child-Pugh Class A, B, or C; use with caution in severe hepatic impairment due to limited data. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no approved dosing recommendations. |
| Geriatric use | No specific dose adjustment; monitor serum potassium and renal function due to age-related decline in renal function and increased risk of hypokalemia. |
| 1st trimester | Lokelma (sodium zirconium cyclosilicate) is not absorbed systemically; limited data in pregnant women. No known risk of fetal harm based on mechanism. Use only if clearly needed. |
| 2nd trimester | Not absorbed; systemic exposure negligible. No teratogenic effects expected. Consider maternal benefit vs potential risks. |
| 3rd trimester | No absorption; no known risk to fetus. May be used for hyperkalemia if benefit outweighs risk. |
Clinical note
Comprehensive clinical and safety monograph for LOKELMA (LOKELMA).
| Placental transfer | Negligible due to non-absorbed, non-systemic mechanism; molecular weight >1000 Da. |
| Breastfeeding | Lokelma is not absorbed orally, so excretion into breast milk is negligible. Likely compatible with breastfeeding, but use caution due to lack of data. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | No human studies. Animal reproduction studies not conducted. Insufficient data in pregnant women. Risk cannot be excluded. Due to mechanism (potassium binder, non-absorbed polymer), systemic absorption is minimal; fetal exposure unlikely. However, no controlled data. Use only if clearly needed and potential benefit justifies potential risk to fetus. |
| Fetal Monitoring | Monitor serum potassium levels regularly. Assess for electrolyte disturbances (magnesium, calcium). Monitor for gastrointestinal adverse effects. No specific fetal monitoring indicated, but standard prenatal care applies. |
| Fertility Effects | No human data on effect on fertility. Animal studies not conducted. No known effect expected due to non-systemic mechanism of action. |
■ FDA Black Box Warning
None
| Serious Effects |
Known hypersensitivity to sodium zirconium cyclosilicate or any component
| Precautions | WARNING: Risk of hypomagnesemia; monitor serum magnesium. WARNING: Potential for gastrointestinal obstruction or perforation; use with caution in patients with severe gastrointestinal disorders. WARNING: May bind to other oral medications; separate dosing by at least 3 hours (or 6 hours for certain drugs). |
| Food/Dietary | LOKELMA should be taken with food to reduce gastrointestinal side effects. No specific food restrictions, but high-potassium foods should be avoided as per dietary guidelines for hyperkalemia. |
| Clinical Pearls | LOKELMA (patiromer) is a non-absorbed potassium-binding polymer indicated for hyperkalemia. Administer at least 6 hours apart from other oral medications due to potential binding. Monitor serum potassium weekly until stable. May cause hypomagnesemia; check magnesium levels periodically. Use with caution in patients with gastrointestinal motility disorders. |
| Patient Advice | Take LOKELMA exactly as prescribed, usually once daily with food. · Separate LOKELMA from other oral medications by at least 6 hours. · Do not crush, chew, or open capsules; swallow whole. · Notify your doctor if you experience constipation, nausea, or stomach pain. · Do not stop taking LOKELMA without consulting your doctor. |
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