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Rupatadine: efficacy and safety of a non-sedating antihistamine with PAF-antagonist effects

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Summary

Rupatadine is a modern non-sedating H1-antihistamine that also haswith additional antagonist effects on platelet-activating factor (PAF). Under the tradenames Rupafin® and Urtimed®, Rrupatadine is approvedregistered in Germany for the treatment of allergic rhinitis and urticaria infor adults and children aged over 12 years. In this review, the available literature available to date onregarding the pharmacological profile and clinical application of Rrupatadine is reviewed and compared to other conventional histamines. In conclusionFinally, the side effects, safety and interaction profileincompatibility of Rrupatadine are discussed. Due to CYP p450 metabolism, Rrupatadine should not be given together with Eerythromycin, Kketoconazole or grapefruit juice. Rupatadine has been found to be effective and safe Iin a variety of randomized clinical trials both in both seasonal and perennial allergic rhinitis, as well as inbut also chronic urticaria Rupatadine has been found as effective and safe.

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Abbreviations

ARIA:

Allergic rhinitis and its impact on asthma

AUC:

Area under the curve

Cmax :

Maximum plasma concentration

CTZ:

Cetirizine

CYP:

Cytochrome P450

DLQI:

Dermatology life quality index

EEG:

Electroencephalogram

EKG:

Electrocardiogram

EMEA:

European Medicines Agency

GM-CSF:

Granulocyte macrophage colony-stimulating factor

HERG:

Human ether-a-go-go related gene

HUVEC:

Humane umbilical venous endothelial cells

IC50:

Mean inhibitory concentration

ICH:

International Conference on Harmonisation

IL:

Interleukin

Ki:

Dissociation constant

LCT:

Levocetirizine

LOR:

Loratadine

mDTSS:

Mean daily total symptom score

MNW:

Mean number of wheals score

MPS:

Mean pruritus severity score

NF-κ B:

Nuclear factor κ-light-chain-enhancer of activated B cells

nM:

Nanomolar

OLP:

Olopatadine

PAF:

Platelet activating factor

PAR:

Perennial allergic rhinitis

PL:

Placebo

RQLQ:

Rhinoconjunctivitis quality of life questionnaire

RU:

Rupatadine

SAR:

Seasonal allergic rhinitis

t1/2:

Plasma half-life

tmax :

Time to maximum effect

Tmax :

Time of maximum plasma concentration

TNF-α:

Tumor necrosis factor-α

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Authors and Affiliations

  1. Department of Dermatology and Allergy Biederstein, Technische Universität, Munich, Germany

    Soja Shamizadeh, Knut Brockow &  Johannes Ring

  2. Klinik und Poliklinik für Dermatologie und Allergologie am Biederstein, Biedersteiner Straße 29, 80802, München, Germany

    Johannes Ring

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  1. Soja Shamizadeh
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  2. Knut Brockow
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  3. Johannes Ring
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Correspondence to Johannes Ring.

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Cite this as: Shamizadeh S, Brockow K, Ring J. Rupatadine: efficacy and safety of a non-sedating antihistamine with PAF-antagonist effects. Allergo J Int 2014; 23: 87–95 DOI: 10.1007/s40629-014-0011-7

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Shamizadeh, S., Brockow, K. & Ring, J. Rupatadine: efficacy and safety of a non-sedating antihistamine with PAF-antagonist effects. Allergo J Int 23, 87–95 (2014). https://doi.org/10.1007/s40629-014-0011-7

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