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loratadine (Clarityn RediTabs / Claritin Reditabs / loratadine, Zydis)

✓ Approved

Merck & Co. · HRH1 · 小分子

什么是 loratadine？

loratadine 是一种小分子，由Merck & Co.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Clarityn RediTabs, Claritin Reditabs, loratadine, Zydis
公司Merck & Co.
药物类别小分子
分子靶点HRH1
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Merck & Co.

作用机制

分子靶点

loratadine 作用于 1 个分子靶点：

HRH1histamine receptor H1 (HH1R, H1R)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

loratadine 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Respiratory, thoracic and mediastinal disordersRhinitis allergic✓ Approved
Skin and subcutaneous tissue disordersUrticaria✓ Approved

相关研究文献

PubMedBMJ (Clinical research ed.)2026-07-30

Antihistamines for atopic dermatitis (eczema): systematic review and network meta-analysis of randomised trials.

Chu Alexandro W L AWL, Wen Aaron A, Guyatt Gordon H GH, Rao Muhammad M et al.

To systematically synthesise the benefits and harms of add-on oral antihistamines for managing atopic dermatitis (eczema). Systematic review and network meta-analysis of randomised trials. Medline, Embase, CENTRAL, the United States Food and Drug Administration, and the European Medicines Agency databases from database inception to 5 May 2025. Randomised trials assessing add-on oral H1 antihistamines, H2 blockers, mast cell stabilisers (nedocromil sodium and sodium cromoglycate), or their combinations. Paired reviewers independently screened records, extracted data, and assessed risk of bias using a modified Cochrane Risk of Bias tool version 2. Random effects bayesian meta-analyses synthesised atopic dermatitis severity (oSCORAD-objective scoring atopic dermatitis, 0-83; minimal important difference 8.2; lower better), itch severity (numerical rating scale, 0-10; minimal important difference 3; lower better), sleep disturbance, atopic dermatitis related quality of life, and harms. The network meta-analysis GRADE (Grading of Recommendations Assessment, Development and Evaluation) and Core GRADE approaches informed certainty of evidence ratings. 47 trials enrolled 6230 children and adults with primarily moderate to severe atopic dermatitis. With moderate certainty, compared with placebo, adding a first generation or second generation H1 antihistamine likely resulted in a small reduction in atopic dermatitis severity (mean difference -1.87, 95% credible interval -3.47 to -0.27) and itch severity (-0.89, -1.41 to -0.37). Although statistically detectable, these effects are well below established minimal important differences (smallest change in an outcome that a patient would identify as important). With low certainty, all studied interventions may not improve sleep disturbance or reduce atopic dermatitis exacerbations. First generation agents probably increase cognitive impairment and may increase treatment discontinuation because of adverse events (risk difference 66 more per 1000, 95% credible interval 0 to 231 more; moderate certainty). Second generation agents differ in their risk of cognitive impairment (range of mean effects 0 more per 1000 for loratadine, 16 more per 1000 for levocetirizine, and 17 more per 1000 for cetirizine). Among patients with atopic dermatitis, adding H1 antihistamines probably results in a clinically unimportant reduction in atopic dermatitis severity and itch severity, and may not reduce sleep disturbance or atopic dermatitis exacerbations. First generation agents increase cognitive impairment and may increase treatment discontinuation because of adverse events. Cognitive impairment risk differs among second generation agents. These findings provide evidence against routine antihistamine use in atopic dermatitis management and will inform updated clinical guidelines. PROSPERO CRD42022345643.

PMID 42526949
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PubMedEuropean journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences2026-07-29

COMBINED SECOND HARMONIC AND LINEAR LIGHT SCATTERING AS A TOOL FOR SOLUBILITY AND AGGREGATION SCREENING.

Kalasová Jitka J, Tarun Orly O, Kuentz Martin M

Poor aqueous solubility and complex supersaturation behaviour of small-molecule drugs require rapid, material-sparing analytical tools that capture incipient aggregation and phase separation events under non-equilibrium conditions. This work evaluated a miniaturised optical platform that combined second harmonic scattering (SHS) with linear light scattering (LLS) driven by an ultrafast 1030 nm laser to monitor supersaturated solutions of 12 poorly water-soluble drugs prepared by DMSO solvent shift in 384-well plates. LLS and SHS signals were recorded after 1 h and 24 h and compared with apparent solubilities from a parallel solvent-shift HPLC assay. LLS, which reports on particle size/number, detected precipitation onsets typically close to or below HPLC values and could resolve particle formation down to ∼0.1 µM for pimozide, substantially exceeding the sensitivity of standard nephelometric methods. SHS, which is sensitive to interfacial asymmetry and nonlinear susceptibility, often showed onsets and complex peak-drop-rise patterns that deviated from LLS, particularly for lopinavir, loratadine, and ritonavir, indicating structurally distinct, largely centrosymmetric drug-rich assemblies above the solubility limit. Orthogonal characterization by scanning electron microscopy, Capflex (capillary flow with a hydrophobic fluorescent tracer), and confocal fluorescence microscopy provided independent evidence for droplet-like or amorphous drug-rich domains that preceded bulk precipitation. Together, the results showed that combined SHS-LLS enabled highly sensitive detection of precipitation, while revealing multistep, nonclassical aggregation pathways in pharmaceutical supersaturated systems.

PMID 42521104
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PubMedPathogens (Basel, Switzerland)2026-07-28

Investigation of the Anti-Toxoplasma gondii Potential of Loratadine.

Alves Stephanie Ortega SO, Dias Ingrid de Oliveira IO, Moura Gabriel Candido GC, Teixeira Samuel Cota SC et al.

Toxoplasmosis remains a major global health concern, particularly in immunocompromised individuals and pregnant women, while currently available therapies are associated with significant toxicity and limited efficacy against chronic infection. Drug repurposing represents an attractive strategy for the identification of safer and more effective anti-Toxoplasma gondii agents. This study investigated the antiparasitic potential of loratadine, a second-generation antihistamine, using an integrated in silico, in vitro, and in vivo approach. The anti-T. gondii activity of loratadine was evaluated through β-galactosidase-based proliferation assays, reversibility assays, and experiments using pretreated tachyzoites. In vivo efficacy was assessed in murine models of acute and chronic toxoplasmosis. Disease progression, survival, parasite burden, and cerebral cyst formation were analyzed following treatment. Loratadine inhibited the intracellular proliferation of T. gondii tachyzoites in a concentration-dependent manner and induced partially irreversible effects on parasite viability after drug withdrawal. Pretreatment of extracellular tachyzoites produced limited effects, suggesting that loratadine predominantly acts during the intracellular stage of infection. In the acute toxoplasmosis model, loratadine treatment delayed disease progression, prolonged animal survival, and significantly reduced the number of tachyzoites recovered from the peritoneal cavity. In the chronic infection model, treatment significantly decreased both the number and size of cerebral cysts, although these findings do not demonstrate cyst eradication or direct bradyzoite killing. Despite its measurable biological activity, loratadine exhibited a relatively low in vitro selectivity index, highlighting the need for further optimization. These exploratory findings identify loratadine as a promising lead compound (hit) for further optimization rather than an immediately translatable therapeutic candidate. Additional medicinal chemistry, pharmacokinetic, mechanistic, and confirmatory preclinical studies will be required to determine its potential for anti-T. gondii drug development.

PMID 42515100
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PubMedDrug metabolism and personalized therapy2026-07-16

The impact of antihistamine use on allergic reactions in pregnancy.

Lisiecka Maria Zofia MZ, Luczak Joanna J

Allergic diseases are common among women of reproductive age, which necessitates the use of antihistamine therapy during pregnancy while ensuring safety for both the mother and the foetus. The study aimed to determine the safety profile, pharmacological characteristics, and clinical consequences of antihistamine use during pregnancy for the maternal-foetal system. A systematic review of scientific publications for the period 2020-2025 was carried out using the PRISMA methodology with a search in five international databases, which allowed us to select 45 relevant sources analyzing pathophysiology, pharmacology, and clinical consequences. It has been established that maternal immunoglobulins of class E are transported across the placental barrier, where they may sensitise foetal mast cells in utero. Hormonal changes during pregnancy induce polarisation of the immune response towards Th2 with progressive suppression of eosinophils by 17-22 % in the second trimester and by 20-42 % in the third trimester. Population cohort studies covering more than 1.2 million pregnancies have found no statistically significant associations between the use of second-generation antihistamines and major congenital malformations, spontaneous abortions or premature births. Physiological changes during pregnancy modify the pharmacokinetic parameters of drugs, reducing plasma protein concentrations by 20-40 %, However, cetirizine and loratadine demonstrate a favourable safety profile based on data from more than 186,000 exposures in Scandinavian registries, and the relative infant dose remains below the 5 % safety threshold. The findings support the use of second-generation antihistamines as first-line therapy for allergic diseases in pregnancy and provide an evidence base for selecting safe pharmacological agents at different gestational stages.

PMID 42461140
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PubMedZhongguo zhen jiu = Chinese acupuncture & moxibustion2026-07-14

[Acupoint catgut embedding for allergic rhinitis: a randomized controlled trial].

Tang Mi M, Zhang Qinxiu Q

To observe the clinical efficacy of acupoint catgut embedding for allergic rhinitis (AR), and to explore its mechanism of action. Eighty patients with AR were randomly divided into an observation group and a control group, with 40 patients in each group. The observation group received acupoint catgut embedding therapy, with bilateral Yingxiang (LI20) as the main acupoints and additional acupoints according to syndrome differentiation. Catgut embedding was performed once every 2 weeks, for a total of 2 treatments. The control group received oral loratadine tablets. Both groups were treated for 4 weeks. Total nasal symptom scores (TNSS) and rhinoconjunctivitis quality of life questionnaire (RQLQ) scores were observed before treatment, after 2 weeks of treatment, after 4 weeks of treatment, and at 1-month follow-up after treatment in both groups. The levels of immunoglobulin E (IgE), interleukin (IL)-4, interferon-γ (IFN-γ), IL-12, and IL-13 in nasal lavage fluid were detected before and after treatment in both groups. Clinical efficacy was evaluated after treatment. After 2 weeks of treatment, after 4 weeks of treatment, and at follow-up, TNSS and RQLQ scores in both groups were lower than those before treatment (P<0.05). After 4 weeks of treatment and at follow-up, TNSS and RQLQ scores in the observation group were lower than those in the control group (P<0.001). After treatment, the levels of IgE, IL-4, and IL-13 in nasal lavage fluid were decreased compared with those before treatment in both groups (P<0.001, P<0.05, P<0.01), and the levels of IFN-γ and IL-12 were increased compared with those before treatment in both groups (P<0.001, P<0.01, P<0.05); the levels of IgE, IL-4, and IL-13 in nasal lavage fluid in the observation group were lower than those in the control group (P<0.05, P<0.001), and the levels of IFN-γ and IL-12 were higher than those in the control group (P<0.05). The total effective rate in the observation group was 95.0% (38/40), higher than 82.5% (33/40) in the control group (P<0.05). Acupoint catgut embedding could improve clinical symptoms in patients with AR, and may exert its therapeutic effect by modulating immune balance.

PMID 42443072
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PubMedIranian journal of allergy, asthma, and immunology2026-07-12

Comparison of the Efficacy of Different Doses of Glucocorticoid Nasal Spray Combined with Loratadine in the Treatment of Rhinitis in Children: A Randomized Clinical Trial.

Wang Huiying H, Ren Zhen Z

Pediatric rhinitis is a common recurrent disorder that may progress to asthma or sinusitis in severe cases. This study aimed to compare the efficacy of different doses of glucocorticoid nasal spray combined with loratadine for rhinitis in children, and provide evidence for optimizing clinical treatment. A total of 150 children with rhinitis admitted from June 2022 to June 2024 were divided into three groups: group I (low-dose group, n=50), group II (medium-dose group, n=50), and group III (high-dose group, n=50). Patients in all three groups were treated with a glucocorticoid nasal spray with loratadine combined with antihistamines. The immune function, serum inflammatory factor level, quantitative Lund-Kennedy score by nasal endoscopy, nasal symptom score, Quality of Life Questionnaire (RQLQ) scores, clinical efficacy, incidence of adverse events, and treatment compliance were assessed. Post-treatment, all indices improved in the three groups. The percentages of CD4+ and CD8+ T cells, IL-10 content, and clinical efficacy in groups II and III were significantly higher than those in group I, while the immunoglobulin E (IgE), IL-6 and IL-17 content, the quantitative Lund-Kennedy score of nasal endoscopy, the children's nasal symptom scores, the RQLQ scores, and the incidence rate of adverse events were below in group I. No significant differences were found between groups II and III in all indices, nor in treatment compliance across the three groups. Loratadine combined with a glucocorticoid nasal spray therapy effectively improves clinical outcomes, inflammation, immune function, symptoms, and quality of life in rhinitis in children, with high clinical application value.

PMID 42437310
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