Cetirizine interactions

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Cetirizine Interactions: A Comprehensive Overview

Introduction to Cetirizine

Cetirizine is a second-generation antihistamine commonly used to treat allergic conditions such as seasonal allergic rhinitis, perennial allergic rhinitis, and chronic idiopathic urticaria. It is known for its rapid onset, long duration of action, and low potential for causing sedation compared to first-generation antihistamines 25.

Pharmacokinetics and Drug Interactions

Renal Excretion and Drug Interactions

Cetirizine is primarily excreted unchanged through the kidneys, which reduces its potential for interactions involving hepatic enzyme systems . However, interactions can occur when cetirizine is co-administered with other drugs that are also excreted via renal pathways. For instance, a significant interaction was observed between cetirizine and pilsicainide in a patient with renal insufficiency, leading to severe arrhythmia. This interaction was attributed to competition for excretion via renal multidrug resistance protein 1 and organic cation transporter 2 .

Interaction with NSAIDs

Studies have shown that cetirizine can interact with non-steroidal anti-inflammatory drugs (NSAIDs) such as diclofenac, ibuprofen, and meloxicam. These interactions were characterized using high-performance liquid chromatography (HPLC) and spectroscopic techniques, indicating that co-administration can affect the availability of cetirizine . Therefore, it is recommended to have a suitable time lapse between the oral uses of cetirizine and NSAIDs to avoid potential interactions .

Interaction with Gabapentin

Cetirizine has also been shown to reduce the plasma concentrations and efficacy of gabapentin, a drug used to treat neuropathic pain. This interaction is believed to be mediated by renal drug transporters for organic cations, affecting the pharmacokinetics of gabapentin .

Interaction with H2 Receptor Antagonists

In vitro studies have investigated the interaction between cetirizine and H2 receptor antagonists like cimetidine, ranitidine, and famotidine. The results indicated that the availability of cetirizine was unaffected by the simultaneous administration of these H2 receptor antagonists, suggesting that they can be safely co-administered .

Safety and Efficacy

Lack of Cardiac Toxicity

Cetirizine has been found to have no cardiac toxicity, making it a safer option compared to some other antihistamines . It is also effective in treating various dermatologic disorders, including urticaria and atopic eczema, without significant impairment of cognitive function or driving performance 19.

Minimal Sedative Effects

While cetirizine is generally associated with a lower incidence of sedation compared to first-generation antihistamines, some studies have reported that it can be more sedating than placebo, loratadine, or terfenadine in certain clinical trials. However, this sedative effect is dose-dependent and usually mild 25.

Conclusion

Cetirizine is a well-tolerated and effective second-generation antihistamine with a favorable safety profile. While it has minimal interactions with hepatic enzyme systems, caution is advised when co-administering it with other drugs that are excreted via renal pathways, such as pilsicainide and gabapentin. Additionally, interactions with NSAIDs should be carefully managed to avoid potential adverse effects. Overall, cetirizine remains a valuable option for treating a wide range of allergic disorders.

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Most relevant research papers on this topic

Use 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 Review

1999·

28citations

·T. Zuberbier et al.

Cetirizine

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 Cited

1993·

169citations

·C. Spencer et al.

Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).

Cetirizine and levocetirizine show high affinity and stereoselectivity for human H(1) histamine receptors, with the carboxylic function of levocetirizine responsible for its long dissociation time.

In Vitro StudyHighly Cited

2002·

201citations

·M. Gillard et al.

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 Study

2014·

10citations

·H. Shamshad et al.

Cetirizine

Cetirizine is an effective and well-tolerated treatment for seasonal, perennial, and chronic allergic rhinitis in adults, adolescents, and children, with no adverse effects on cognitive function or behavior.

Highly Cited

2012·

81citations

·M. Curran et al.

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 Report

2006·

48citations

·S. Tsuruoka et al.

Cetirizine 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.

RCTRigorous Journal

2020·

7citations

·Ana Carolina Conchon Costa et al.

Drug-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.

2005·

45citations

·I. M. Kenawi et al.

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

2004·

34citations

·A. Patat et al.

In 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 Study

2010·

12citations

·N. Sultana et al.

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