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desloratadine + pseudoephedrine (Clarinex D / Aerinaze)

✓ Approved

Merck & Co. · HRH1 · 小分子

什么是 desloratadine + pseudoephedrine？

desloratadine + pseudoephedrine 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Clarinex D, Aerinaze
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

desloratadine + pseudoephedrine 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

desloratadine + pseudoephedrine 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Immune system disordersSeasonal allergy✓ Approved

相关研究文献

PubMedCureus2026-08-02

Mycoplasma pneumoniae-Associated Reactive Infectious Mucocutaneous Eruption Mimicking Atypical Stevens-Johnson Syndrome: A Case Report.

Burbea Alexandru C AC, Verlekar Pankaj P

Reactive infectious mucocutaneous eruption (RIME) is an infection-associated mucositis syndrome previously described under terms including incomplete Stevens-Johnson syndrome (SJS), Fuchs syndrome, and Mycoplasma pneumoniae-induced rash and mucositis (MIRM). It is characterised by an infectious prodrome, prominent mucosal involvement, and sparse or absent cutaneous disease. Severe ocular involvement may clinically mimic atypical Stevens-Johnson syndrome. We report the case of a previously healthy woman in her 20s who developed coryzal symptoms and self-treated with ibuprofen, paracetamol, and pseudoephedrine before presenting with worsening cough, pyrexia, odynophagia, and bilateral conjunctival discharge. She received doxycycline and topical chloramphenicol but re-presented overnight with rapidly progressive lip swelling, dysphagia, oral mucosal ulceration, and severe bilateral ocular inflammation without cutaneous lesions. Recent exposure to non-steroidal anti-inflammatory medication and doxycycline created initial diagnostic uncertainty, while the preceding respiratory prodrome and skin-sparing mucositis supported infection-associated RIME. Ophthalmological assessment demonstrated severe ocular surface inflammation with pseudomembrane formation, early symblepharon, and progressive corneal involvement, requiring tertiary transfer and amniotic membrane grafting. Initial chest radiography and respiratory multiplex polymerase chain reaction (PCR) testing were negative, including for Mycoplasma pneumoniae; however, subsequent serology returned positive for Mycoplasma pneumoniae IgM. Later drug challenge testing demonstrated tolerance to suspected medications, supporting an infection-associated rather than drug-induced aetiology. This case highlights that Mycoplasma pneumoniae-associated RIME may mimic atypical Stevens-Johnson syndrome, particularly when severe ocular and oral mucositis occurs after recent medication exposure. Early dermatology and ophthalmology involvement, combined molecular and serological testing, and prompt ocular treatment are essential to reduce long-term ocular morbidity.

PMID 42540076
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PubMedBirth defects research2026-07-30

Intentional Dexketoprofen Overdose During Pregnancy: Maternal and Fetal Outcomes in Three Cases.

Uysal Nusret N, Gungor Mesut M, Karadas Baris B, Yilmaz Ismail I et al.

Dexketoprofen trometamol is a widely used short-acting nonsteroidal anti-inflammatory drug. Despite its widespread clinical use, pregnancy-specific safety data for dexketoprofen as an individual agent are lacking, and no previous report has described maternal or fetal outcomes following overdose in pregnant women. We present three cases of intentional dexketoprofen overdose during pregnancy. Case 1 involved a 33-year-old woman at 8 weeks of gestation who ingested dexketoprofen with ibuprofen, pseudoephedrine, and cefuroxime; she delivered a healthy male infant at 37 weeks with no congenital anomalies on follow-up. Case 2 involved a 36-year-old woman at 17 weeks who ingested dexketoprofen with ergotamine tartrate, mecloxamine, caffeine, and paracetamol; she experienced a spontaneous abortion at 20 weeks, complicated by cyst rupture requiring hysterectomy. Case 3 involved a 29-year-old woman at 6 weeks who ingested dexketoprofen, paracetamol, and chlorpheniramine, and underwent elective termination at 10 weeks. The three cases demonstrated heterogeneous pregnancy outcomes. No congenital anomalies were identified in the single evaluable live-born infant. Multiple co-ingested agents substantially complicate causal attribution, most notably ergotamine tartrate in Case 2. The limited case number and outcome heterogeneity preclude identification of a consistent pattern of fetal adverse effects or definitive conclusions regarding fetal risk. All overdoses were intentional, underscoring the importance of integrating psychiatric assessment into toxicological management during pregnancy. These cases represent the first available observational data on maternal and fetal outcomes following intentional dexketoprofen overdose in pregnancy, highlighting the need for a multidisciplinary approach in this clinical setting.

PMID 42527370
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PubMedJournal of pharmaceutical sciences2026-07-25

Efficacy of ultraviolet irradiation of pharmaceutical excipients in mitigating N-nitrosamine generation.

Minamioka Saki S, Matsuzawa Shun S, Yoshihara Naoki N, Oikawa Michinori M et al.

The generation of N-nitrosamine compounds (NOCs) in drugs presents a critical regulatory challenge owing to their potential mutagenicity and exceptionally strict acceptable intake limits required for patient safety. These impurities arise primarily from the reaction between amine-containing active pharmaceutical ingredients and trace amounts of nitrosating agents (reactive NOx), which contribute to N-nitrosation. Reactive NOx species are frequently found in pharmaceutical excipients. Therefore, efficiently reducing reactive NOx is essential for robust management of the risk posed by NOCs. In this study, we employed ultraviolet (UV) irradiation of excipients as a novel preemptive strategy to reduce reactive NOx levels. Desloratadine was used as a secondary amine model to evaluate the generation of N-nitrosamine in physical mixtures with various excipients. The excipients were exposed to different UV wavelengths (248, 313, and 365 nm), and N-nitrosodesloratadine (NDLRT) generation was quantified after storage under stress conditions. We found that 365 nm UV irradiation was the most effective in reducing reactive NOx under all conditions. In a formulation study, 365 nm UV irradiation successfully reduced NDLRT generation in the tablet by 54-68% compared with the control. Overall, the novel strategy described herein should be useful for reducing NOCs without affecting the quality of drugs.

PMID 42497957
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PubMedEuropean journal of clinical pharmacology2026-07-22

The incidence of sleepiness in newer-generation antihistamine users: a systematic review and network meta-analysis.

Leelakanok Nattawut N, Pongpun Anchana A, Sapapsap Bannawich B, Jirathawonkul Nattanich N et al.

This systematic review and meta-analysis aimed to summarize the incidence of sleepiness in patients who used newer-generation antihistamines. CINAHL Complete, Medline, Scopus, ScienceDirect, and Google Scholar were systematically searched from inception to July 2025. The pairwise meta-analysis of the sleepiness incidence was conducted using a binary random-effects model. The network meta-analysis was performed using a random-effects model in a frequentist framework. Heterogeneity was evaluated using the I2 statistic. One hundred and sixty-three studies were included in the systematic review and meta-analysis. We found that 1.3% (95% CI: 1.0-1.6%, I2 = 40.45) of those taking a placebo reported sleepiness. The least-sedating antihistamine in adults was bilastine 20 mg (prevalence = 1.6%; 95% CI: 0.7-2.5%, I2 = 47.83). Data from network meta-analysis also supported that bilastine 20 mg has the least sedative effect (relative risk = 1.06; 95%CI: 0.67-1.69). At their usual therapeutic dose, bepotastine 20 mg, bilastine 20 mg, desloratadine 5 mg, and fexofenadine 120 mg-180 mg had a prevalence of sleepiness of less than 10% and not significantly different from placebos (p > 0.05). All nonsedating antihistamines administered at their usual doses have a higher prevalence of sleepiness compared to the placebo. However, most of the prevalence values are not statistically different from those of the placebo.

PMID 42481869
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PubMedJournal of chemical information and modeling2026-07-14

Discovery and Mechanism of Action of a Novel Desloratadine Derivative Inhibiting Mycobacterium tuberculosis 3-Dehydroquinate Synthase.

Belachew Aweke Mulu AM, Li Haizhou H, Tian Xirong X, Liu Zhiyong Z et al.

Mycobacterium tuberculosis, the etiological agent of tuberculosis (TB), remains a leading cause of mortality from infectious disease worldwide. The continued emergence of multidrug-resistant strains highlights the urgent need for new therapeutic agents with novel mechanisms of action. Here, we report the discovery and comprehensive characterization of DL25, a synthetic desloratadine-derived small molecule exhibiting potent antimycobacterial activity (minimum inhibitory concentration (MIC) 2-4 μg/mL against multiple mycobacterial species). Using a supra-inhibitory DL25 selection strategy, we isolated and characterized spontaneous resistant mutants. Whole-genome sequencing identified recurrent mutations in aroB, which encodes 3-dehydroquinate synthase (DHQS), an essential enzyme of the shikimate pathway. Consistent with target involvement, aroB overexpression reduced susceptibility to DL25, while DL25 decreased DHQS-associated biochemical activity in vitro with an apparent IC50 of approximately 5.0 μg/mL. In addition, DL25 exhibited concentration- and time-dependent bactericidal activity and showed partial synergy with several established antitubercular agents. Structural modeling, molecular docking, and 100 ns molecular dynamics simulations supported stable binding of DL25 within the DHQS active site and identified interactions with residues implicated in substrate recognition and catalysis. Collectively, the genetic, biochemical, and computational findings support DHQS as a biologically relevant target associated with DL25 activity and establish DL25 as a promising lead-like scaffold for the development of future shikimate pathway-directed antimycobacterial agents. More broadly, this study demonstrates the value of integrating genetic, biochemical, and computational approaches for mechanism-guided antituberculosis drug discovery.

PMID 42447414
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PubMedCells2026-07-13

Plant-Derived Diamine Oxidase Modulation of Histamine-Induced Ca2+ Release in Intestinal Caco-2 Cells: A Cellular System to Evaluate Its Histaminase Efficacy.

Neree Armelle Tchoumi AT, Jumarie Catherine C, Marcocci Lucia L, Pietrangeli Paola P et al.

Histamine accumulation is associated with allergic reactions and intestinal dysfunction through activation of H1R Receptors (H1Rs) and subsequent intracellular Ca2+ mobilization. Although antihistamines such as desloratadine block H1Rs to alleviate symptoms, they may induce adverse effects (dizziness, nausea, neurological disorders). Diamine oxidases (DAOs) catalyze the oxidative deamination of histamine to imidazole acetaldehyde with consumption of oxygen and concomitant production of hydrogen peroxide and ammonia. Instead of blocking H1R, we have proposed vegetal diamine oxidase (vDAO) as an enzymatic approach to decompose histamine. This study investigated whether vDAO, by degrading histamine, could modulate histamine-induced Ca2+ mobilization compared with desloratadine. Using intestinal Caco-2 cultured cells loaded with the fluorescent Ca2+ indicator Fluo-4 AM, intracellular calcium (Ca2+) dynamics were analyzed by confocal microscopy following histamine stimulation. vDAO significantly downregulated histamine-induced Ca2+ mobilization. Notably, at a fixed histamine concentration sufficient to trigger Ca2+ release, vDAO achieved the same level of calcium mobility inhibition at a concentration three-fold lower than that of desloratadine, suggesting a high efficiency of DAO. These findings indicate that histamine degradation with orally administrable DAO may reduce Ca2+ signaling in intestinal epithelial cells, providing a promising approach to reduce histamine-related damage or a reinforcement of current antihistamine anti-inflammatory medication based on histamine receptor blockade.

PMID 42439652
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