Converting Lithium Carbonate to Extended-Release Formulation
When switching from immediate-release lithium carbonate 300 mg BID (total 600 mg/day) to extended-release, use the same total daily dose of 600 mg given as a single evening dose, then check serum lithium levels after 7-8 days to ensure therapeutic range is maintained. 1, 2
Conversion Strategy
Direct Dose Conversion
- Convert the total daily dose on a 1:1 basis from immediate-release to extended-release formulation 1, 2
- Your patient currently takes 600 mg/day total, so prescribe lithium carbonate extended-release 600 mg once daily 1, 3
- Administer as a single evening dose to optimize compliance and reduce side effects 2, 3
Expected Pharmacokinetic Changes
- Extended-release formulations produce 30-50% lower peak plasma concentrations compared to immediate-release, without significantly changing total drug exposure 2
- Peak concentration occurs at 4-5 hours (versus 1-2 hours for immediate-release) 2
- Because of the delayed peak, maintain serum concentrations in the upper therapeutic range (0.8-1.0 mmol/L) rather than 0.6-0.8 mmol/L used for standard formulations 2
Critical Monitoring Timeline
Initial Monitoring After Conversion
- Check serum lithium level 7-8 days after the switch, as this is when steady-state is achieved regardless of formulation 2
- Draw blood sample 12 hours after the evening dose (i.e., the next morning before any dose) 1
- For once-daily dosing, the 24-hour trough level serves as the control value 2
Ongoing Monitoring Schedule
- Every 3-6 months during stable maintenance therapy 4
- More frequently (1-2 weeks) if the patient has renal impairment (eGFR <60 mL/min/1.73 m²), takes interacting medications (NSAIDs, ACE inhibitors, ARBs, thiazide diuretics), or experiences intercurrent illness 4
Essential Pre-Conversion Assessment
Renal Function Evaluation
- Check current serum creatinine and eGFR before switching 4
- If eGFR <60 mL/min/1.73 m², the patient requires monthly monitoring rather than every 3-6 months 4
- If eGFR <30 mL/min/1.73 m², reassess the risk-benefit of continuing lithium and monitor at least monthly if continued 4
Medication Review
- Identify and document all interacting medications: NSAIDs, ACE inhibitors, ARBs, thiazide diuretics 4
- These medications significantly increase lithium toxicity risk and necessitate more frequent monitoring 4
- Avoid concomitant NSAIDs whenever possible due to nephrotoxicity risk 4
Advantages of Extended-Release Formulation
Clinical Benefits
- Significantly reduced urinary frequency compared to twice-daily dosing 3
- Improved patient compliance with once-daily administration 2, 3
- Lower peak-related side effects due to reduced peak plasma concentrations 2
- Similar efficacy to immediate-release formulations 3, 5
Practical Considerations
- The once-daily evening schedule is well-established and recommended by expert panels 2
- Extended-release formulations produce smooth, extended absorption comparable to commercial products like Eskalith CR 5
Common Pitfalls to Avoid
Dosing Errors
- Do not reduce the total daily dose when converting to extended-release unless there are specific clinical reasons (e.g., toxicity concerns, renal impairment) 1, 2
- Do not check lithium levels before 7-8 days after the switch, as steady-state will not yet be achieved 2
- Do not draw blood samples at random times—always obtain trough levels 12 hours post-dose for twice-daily or 24 hours for once-daily dosing 1, 2
Monitoring Failures
- Do not rely solely on serum levels—accurate evaluation requires both clinical assessment and laboratory analysis 1
- Do not forget to increase monitoring frequency if the patient develops intercurrent illness, especially if eGFR <60 mL/min/1.73 m² 4
- Do not overlook drug interactions—NSAIDs, ACE inhibitors, ARBs, and thiazides all increase lithium levels 4
Special Population Considerations
- Elderly patients often require reduced doses and may exhibit toxicity at levels tolerated by younger patients 1
- Patients with renal impairment require dose interval extension (not dose increases) to avoid excessive peak concentrations 4