Are levociz (levocetirizine) and deriphyllin (theophylline) safe during lactation?

Safety of Levociz (Levocetirizine) and Deriphyllin (Theophylline) During Lactation

Both levocetirizine and theophylline can be used during lactation, but with important caveats: levocetirizine transfers minimally into breast milk and is compatible with breastfeeding, while theophylline requires careful monitoring due to potential infant exposure and drug interactions.

Levocetirizine (Levociz) Safety Profile

Evidence for Compatibility with Breastfeeding

• Recent human lactation studies demonstrate that levocetirizine transfers into breast milk at very low levels, with a relative infant dose (RID) of only 1.9%, well below the 10% safety threshold. 1

• The absolute infant dose for levocetirizine is approximately 1.1 μg/kg per day, which represents minimal drug exposure to the nursing infant. 1

• Maximum milk concentrations occur approximately 2-4 hours after maternal intake, with a mean half-life in milk of 7.0 hours. 1

Clinical Recommendations for Levocetirizine

• Levocetirizine is compatible with breastfeeding based on low milk transfer and established safety data. 1

• British guidelines recommend caution with antihistamines during lactation, though they acknowledge that cetirizine (the racemic mixture containing levocetirizine) has a reasonable safety profile. 2

• No severe adverse events have been reported in breastfed infants whose mothers used levocetirizine. 1

Dosing Considerations

• In renal impairment, the dose of levocetirizine should be halved, and it should be avoided in severe renal impairment (creatinine clearance <10 mL/min). 2

• Standard dosing can be maintained in lactating women with normal renal function. 1

Theophylline (Deriphyllin) Safety Profile

Drug Interaction Concerns

• Theophylline has significant drug interactions with multiple medications, including macrolide antibiotics (erythromycin, clarithromycin), which can increase theophylline levels and toxicity. 2

• Cetirizine (and by extension levocetirizine) is listed among medications that interact with theophylline, requiring careful monitoring when used concurrently. 2

Lactation Safety

• While specific data on theophylline transfer into breast milk is limited in the provided evidence, general principles suggest that all drugs are excreted into breast milk to some degree. 3

• The combination of levocetirizine and theophylline requires particular attention due to their documented drug interaction profile. 2

Clinical Algorithm for Use During Lactation

Step 1: Assess Maternal Indication

• Determine if both medications are truly necessary or if alternatives exist
• Consider that levocetirizine alone may be sufficient for allergic conditions 2

Step 2: Evaluate Maternal Renal Function

• Check creatinine clearance before initiating levocetirizine 2
• Adjust levocetirizine dose if creatinine clearance is 10-50 mL/min 2

Step 3: Monitor for Drug Interactions

• If both medications must be used together, monitor for signs of theophylline toxicity (tachycardia, tremor, nausea, seizures) 2
• Consider checking theophylline levels if clinical symptoms suggest toxicity 2

Step 4: Timing of Breastfeeding

• For levocetirizine, breastfeeding can occur at any time, though peak milk levels occur 2-4 hours post-dose 1
• If concerned about infant exposure, consider breastfeeding just before the next maternal dose when milk levels are lowest 1

Step 5: Infant Monitoring

• Observe infant for sedation, irritability, or feeding difficulties 3, 4
• Monitor infant growth and development at routine pediatric visits 3

Common Pitfalls to Avoid

• Do not assume that because levocetirizine is safe, all antihistamines are equally safe during lactation. Hydroxyzine, for example, is specifically contraindicated in early pregnancy and requires caution during lactation. 2

• Do not overlook the drug interaction between levocetirizine and theophylline, which could lead to altered theophylline levels and potential toxicity. 2

• Do not use levocetirizine in women with severe renal impairment (creatinine clearance <10 mL/min) without dose adjustment or alternative therapy. 2

• Avoid prescribing sedating antihistamines as alternatives, as their anticholinergic and sedating effects may be more problematic than levocetirizine's minimal milk transfer. 2

Alternative Considerations

• If theophylline can be discontinued, levocetirizine monotherapy is preferable and has well-established lactation safety. 1

• Other antihistamines with documented lactation safety include chlorphenamine, though it has more sedating effects. 2

• For respiratory conditions requiring bronchodilation, consider whether inhaled medications might reduce systemic exposure and milk transfer compared to oral theophylline. 3