Drug interactions of cetirizine
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Drug Interactions of Cetirizine
Cetirizine and NSAIDs: Potential Pharmacokinetic Interactions
Cetirizine, a commonly used antihistamine, is often co-administered with non-steroidal anti-inflammatory drugs (NSAIDs) such as diclofenac, ibuprofen, and meloxicam. Studies have shown that cetirizine, a P-glycoprotein substrate, may interact with these NSAIDs, potentially affecting its pharmacokinetic profile. Research using high-performance liquid chromatography (HPLC) has demonstrated that the availability of cetirizine can vary significantly when taken with NSAIDs at different pH levels, indicating a potential interaction that could alter the drug's effectiveness and safety profile1.
Cetirizine and Diclofenac: Formation of Ionic Salts
Specific interactions between cetirizine and diclofenac have been observed, where the two drugs form a high molecular weight, water-insoluble ionic salt in aqueous solutions. This interaction is characterized by a charge transfer between the piperazine moiety of cetirizine and the aromatic groups of diclofenac, which could potentially impact the bioavailability and therapeutic efficacy of both drugs2.
Cetirizine and Pilsicainide: Risk of Severe Arrhythmia
A significant pharmacokinetic interaction has been reported between cetirizine and pilsicainide, particularly in patients with renal insufficiency. Co-administration of these drugs can lead to elevated plasma concentrations due to competition for renal excretion pathways, specifically via the human multidrug resistance protein 1 and organic cation transporter 2. This interaction has been associated with severe arrhythmias, highlighting the need for careful monitoring and potential dose adjustments in patients with compromised renal function3.
Cetirizine and H2 Receptor Antagonists: No Significant Interaction
In contrast to the interactions with NSAIDs and pilsicainide, studies have shown that cetirizine does not significantly interact with H2 receptor antagonists such as cimetidine, ranitidine, and famotidine. In vitro studies using reversed-phase high-performance liquid chromatography (RP-HPLC) and ultraviolet (UV) spectrophotometry have indicated that the pharmacokinetics of cetirizine remain unaffected when co-administered with these H2 receptor antagonists, suggesting that they can be safely used together4.
Cetirizine and Gabapentin: Reduced Plasma Concentrations
Cetirizine has been found to reduce the plasma concentrations and therapeutic effects of gabapentin, a drug used for neuropathic pain. This interaction is thought to be mediated by the inhibition of renal drug transporters for organic cations, which are involved in the excretion of gabapentin. As a result, patients may experience reduced pain relief when these drugs are taken together, necessitating careful consideration of dosing and monitoring6.
Conclusion
Cetirizine, while generally safe and effective, can interact with various other medications, leading to altered pharmacokinetics and potential adverse effects. Notable interactions include those with NSAIDs, diclofenac, pilsicainide, and gabapentin, which can affect drug availability and efficacy. However, cetirizine does not significantly interact with H2 receptor antagonists, making it a safer option in combination with these drugs. Clinicians should be aware of these interactions and manage co-administration carefully to ensure patient safety and therapeutic effectiveness.
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Most relevant research papers on this topic
Spectroscopic characterization of in vitro interactions of cetirizine and NSAIDS
Cetirizine and NSAIDs interact at various pH levels, suggesting further studies on their co-administration for better understanding of their pharmacokinetic and pharmacodynamic profiles.
In Vitro StudyDrug-drug interaction between diclofenac, cetirizine and ranitidine.
Diclofenac, cetirizine, and ranitidine exhibit weak charge transfer interactions, leading to a high molecular weight (1:1), water insoluble ionic salt in aqueous solution.
Severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency: First case presentation showing competition for excretion via renal multidrug resistance protein 1 and organic cation transporter 2
The interaction of cetirizine and pilsicainide may cause severe arrhythmias in patients with renal insufficiency, especially when both drugs are administered together.
Case ReportIn vitro studies of the interaction between cetirizine and H2 receptor antagonists using spectrophotometry and reversed-phase high-performance liquid chromatography
Cetirizine availability is unaffected by simultaneous administration of H1 and H2 receptor antagonists, indicating that the two drugs can be safely administered together.
In Vitro StudyUse of cetirizine in dermatologic disorders.
Cetirizine is a safe second-generation antihistamine that effectively treats urticaria and reduces pruritus in atopic eczema, with individual dosages based on symptom severity.
Systematic ReviewCetirizine Reduces Gabapentin Plasma Concentrations and Effect: Role of Renal Drug Transporters for Organic Cations
Cetirizine reduces gabapentin plasma concentrations and its effect on neuropathic pain attenuation, but this interaction is not mediated by renal transporters.
RCT
Rigorous JournalCetirizine
Cetirizine is an effective and well-tolerated treatment for seasonal/perennial allergic rhinitis, chronic idiopathic urticaria, and allergic asthma in adults and children, with a lower incidence of sedation compared to other antihistamines.
Highly CitedComparison of the bronchodilatory effects of cetirizine, albuterol, and both together versus placebo in patients with mild-to-moderate asthma.
Cetirizine has a significant bronchodilatory effect in patients with mild-to-moderate asthma and can be used alongside albuterol without causing asthma worsening or interference with the drug's effect.
RCTHighly CitedPhysicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine.
Cetirizine and levocetirizine show distinct advantages over hydroxyzine in slow receptor dissociation rate, high selectivity, negligible liver enzyme interaction, and low CNS penetration.
Lack of interaction between two antihistamines, mizolastine and cetirizine, and ethanol in psychomotor and driving performance in healthy subjects
A therapeutic dose of mizolastine or cetirizine does not impair driving task performance and does not interact with ethanol at concentrations of 0.7 g/l.
RCT