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doxepin (doxepin, GenDerm / Zonalon / Xepicort)

✓ Approved

Takeda · HRH1 · 小分子

什么是 doxepin？

doxepin 是一种小分子，由Takeda研发。该药已获批，用于治疗相关适应症，给药途径：Topical。

药物档案

商品名doxepin, GenDerm, Zonalon, Xepicort
公司Takeda
药物类别小分子
分子靶点HRH1, HRH2, SLC6A2
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Takeda

作用机制

分子靶点

doxepin 作用于 3 个分子靶点：

HRH1histamine receptor H1 (HH1R, H1R)
HRH2histamine receptor H2 (HH2R, H2R)
SLC6A2solute carrier family 6 member 2 (SLC6A5, NAT1)
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

doxepin 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
Skin and subcutaneous tissue disordersPruritus✓ Approved

相关研究文献

PubMedMolecules (Basel, Switzerland)2026-10-16

A Robust AQbD-Based RP-HPLC Method for Simultaneous Quantification of Acyclovir and Doxepin Hydrochloride in Bulk and Topical Cream Formulation.

Kumar Akshay A, Kumar Mohit M, Saini Abhishek A, Agrawal Mohit M et al.

The present study describes the development and validation of a simple, rapid, and reliable RP-HPLC method for the simultaneous estimation of acyclovir and doxepin hydrochloride in bulk and topical cream formulation using an Analytical Quality by Design (AQbD) approach. The combination of acyclovir, an antiviral agent, and doxepin, an antipruritic and anti-inflammatory drug, offers a combined topical approach for the management of herpes-associated skin conditions. The method development was guided by a predefined Analytical Target Profile (ATP), followed by systematic risk assessment to identify critical quality attributes (CQAs) and critical method parameters (CMPs). The central composite design (CCD) was employed to optimize key chromatographic variables, including mobile phase composition and flow rate. The chromatographic separation was achieved on a C18 column using an isocratic mobile phase of acetonitrile and water (40:60 v/v) at a flow rate of 1.0 mL/min, with UV detection at 240 nm. The retention times were found to be 2.58 min for acyclovir and 4.64 min for doxepin hydrochloride, indicating efficient separation with good peak symmetry. The method was validated according to ICH Q2(R2) guidelines and demonstrated excellent linearity over the concentration ranges of 2-10 µg/mL (acyclovir) and 12-28 µg/mL (doxepin hydrochloride), with correlation coefficients greater than 0.997. The method exhibited high precision (%RSD < 2%), accuracy (recovery within 99-101%), and good sensitivity with low LOD and LOQ values. The robustness studies confirmed the reliability of the method under small, deliberate variations in chromatographic conditions. The developed cream formulation showed uniform drug content and satisfactory in vitro drug release, with a sustained release profile reaching approximately 96% over 24 h. In conclusion, the proposed AQbD-based RP-HPLC method is suitable for routine quantitative analysis and quality control of acyclovir and doxepin hydrochloride in combined topical formulations.

PMID 42883330
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PubMedThe Journal of allergy and clinical immunology2026-10-16

Comparative efficacy and safety of antihistamines, increased antihistamine dosing, and antihistamine adjuncts for chronic urticaria: a systematic review, dose-response, and network meta-analysis of randomized trials.

Chu Alexandro W L AWL, Zhao Irene X IX, Rayner Daniel G DG, Guyatt Gordon H GH et al.

Chronic urticaria is a common immune-mediated condition characterized by wheals (itch and hives), angioedema, or both, lasting for greater than six weeks. It is managed with H1 antihistamines as the first-line therapy. Fundamental unresolved questions remain regarding the comparative benefits and harms of antihistamines and their adjuncts, and of H1 antihistamine dose-escalation. To analyze the comparative benefits and harms of antihistamines and their adjuncts (H2 blockers or montelukast), and of H1 antihistamine dose-escalation. As part of updating the American Academy of Allergy, Asthma & Immunology and American College of Allergy, Asthma and Immunology Joint Task Force on Practice Parameters Chronic Urticaria guidelines, we searched MEDLINE, EMBASE, CENTRAL, and regulatory databases from inception to March 17, 2025, for randomized trials addressing antihistamines or their adjuncts for chronic urticaria. Paired reviewers independently screened records, extracted data, and assessed risk of bias. Random effects network and dose-response meta-analyses addressed urticaria activity (composed of itch and wheal scores), angioedema activity, urticaria-related quality of life, and harms including sedation. The GRADE approach informed certainty of evidence ratings. CRD42022367280. 211 trials (22,187 participants) evaluated 55 unique treatments. Bilastine, desloratadine, fexofenadine, and levocetirizine are among the most effective in improving overall urticaria activity, urticaria-related quality of life, and sleep disturbance. Cetirizine and loratadine are among the most effective in reducing overall urticaria activity and its subcomponents, with cetirizine also among the most effective in improving urticaria-related quality of life. Escalating from a single to quadruple daily dose may yield diminishing additional benefit. Second-generation agents as a class may be more effective than first-generation agents in improving urticaria activity and sleep disturbance. Sedation risk likely increases with higher doses, with first-generation agents (e.g., diphenhydramine, hydroxyzine) and doxepin among the most sedating; cetirizine, ketotifen, levocetirizine, and rupatadine among the intermediate sedating; and bepotastine, bilastine, desloratadine, ebastine, fexofenadine, and loratadine among the least sedating. Adding montelukast (moderate certainty) or an H2 blocker (very low certainty) to a second-generation agent may further reduce urticaria activity. For chronic urticaria, second-generation agents differ in their efficacy and safety. First-generation agents are less beneficial and more harmful. Escalating to higher daily doses may provide additional benefits but likely increases sedation.

PMID 42887704
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PubMedCurrent neuropharmacology2026-10-14

Doxepin Attenuates Cognitive and Anxiety-like Behavioral Deficits Induced by Acute Kidney Injury in Rats.

Jaber Sanaa S, Alsmadi Mo'tasem M, Alzoubi Karem K, Khabour Omar O et al.

Acute kidney injury (AKI) is a systemic disorder with consequences extending beyond the kidney, including central nervous system dysfunction. Clinical and experimental evidence indicates that AKI is associated with cognitive impairment and neuropsychiatric disturbances. However, effective strategies to prevent or attenuate AKI-associated brain dysfunction are lacking. Doxepin, a tricyclic antidepressant, exhibits neuroprotective properties that may counteract key mechanisms implicated in AKI-induced neural injury. In this study, acute renal failure (ARF) was used as an experimental model of AKI. ARF was induced in male Wistar rats through glycerol injection. Animals were allocated into four experimental groups: Control, doxepin (DOX), ARF, or ARF-DOX. Doxepin was given orally at a dose of 5 mg/kg once daily over a 12-day period. Renal function was assessed using serum and urinary urea measurements. Anxiety-related behavior was assessed using the open field test and the elevated plus maze, whereas spatial learning and memory were evaluated with the radial arm water maze. Glycerol-induced ARF resulted in significant alterations in urinary parameters, including reduced urinary urea concentration and increased urine output and flow rate, while serum urea levels did not differ significantly among groups. ARF did not impair spatial learning acquisition but significantly disrupted short- and long-term memory retention. In addition, ARF induced specific anxiety-like behavioral alterations, including increased freezing behavior, reduced rearing activity, and decreased open-arm entries in anxiogenic environments. Doxepin treatment significantly attenuated memory impairments and partially normalized anxiety-related behaviors, without improving biochemical markers of renal dysfunction. These findings demonstrate that AKI induces selective cognitive and anxiety-like behavioral deficits and support the existence of a kidney-brain axis. Doxepin attenuated AKI-associated neurobehavioral impairments. This study supports the potential repurposing of doxepin, an established clinically used and brain-penetrant drug, as a therapeutic strategy for attenuating AKI-associated neurobehavioral dysfunction.

PMID 42872662
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PubMedExpert opinion on pharmacotherapy2026-10-14

Current perspectives on the pharmacotherapeutic management of insomnia in Veterans.

Saliba Ranime R, Cercone Julia J, El-Solh Ali A AA

Insomnia is a highly prevalent sleep disorder among Veterans and frequently co-occurs with post-traumatic stress disorder (PTSD), depression, chronic pain, and substance use disorders. This review synthesizes the current evidence on pharmacological management of insomnia in Veterans with attention to guideline recommendations, veteran-specific safety considerations, and comorbidity-driven prescribing. We discuss the rationale for reducing long-term reliance on benzodiazepines and benzodiazepine receptor agonists (BZRAs) in favor of agents with more favorable long-term risk profiles. Concurrent prescribing of GABAergic hypnotics with opioids is addressed in the context of existing VA Opioid Safety Initiative policy, FDA labeling, and observational overdose data. Off-label agents such as trazodone and quetiapine continue to be widely used despite limited efficacy evidence for insomnia; their use is best reserved for cases in which better-supported options have failed. Contemporary guidance places cognitive behavioral therapy for insomnia as first-line treatment, while pharmacotherapy is reserved for patients who do not respond to, cannot access, or decline behavioral treatment. The 2025 VA/DoD guideline suggests several medications when pharmacotherapy is used, including daridorexant, doxepin, eszopiclone, lemborexant, suvorexant, zaleplon, and zolpidem, and recommends against antipsychotics, benzodiazepines, and trazodone for chronic insomnia disorder.

PMID 42873187
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PubMedFrontiers in psychiatry2026-09-23

Pharmacological modulation of hyperarousal in insomnia associated with major depressive disorder: a narrative review of sedating antidepressants and orexin receptor antagonists.

Zhang Yiwei Y, Zhang Hua H, Tang Jingkai J, Wang Yibing Y et al.

Insomnia symptoms in major depressive disorder (MDD) are clinically heterogeneous, ranging from presleep rumination and prolonged sleep latency to repeated nocturnal awakenings and early-morning awakening. Their clinical significance and treatment implications may also differ between active MDD and residual insomnia symptoms during partial remission. This narrative review examines how these presentations may inform the use of sedating antidepressants and dual orexin receptor antagonists (DORAs). Sedating antidepressants, including mirtazapine, trazodone, doxepin, and other tricyclic antidepressants, differ in dose-dependent antidepressant activity, receptor profile, and adverse-effect burden. DORAs directly target orexin-mediated wake drive and have the strongest evidence for insomnia disorder, particularly sleep-maintenance outcomes, although evidence in active MDD remains limited. Because clinical presentations neither establish an underlying mechanism nor reliably predict treatment response, the proposed framework should be used as a hypothesis-generating aid rather than a validated treatment algorithm. Pharmacological selection should also consider suicide risk, substance-use history, comorbid sleep disorders, concomitant central nervous system depressants, and next-day functioning.

PMID 42774912
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PubMedFrontiers in medicine2026-09-18

Case Report: A case of cutaneous collagenous vasculopathy.

Tang Chenjian C, Chen Liping L, Yu Jiangxiu J, Zhu Mei M

We report a case of a 62-year-old woman presenting with a 6-year history of purpuric patches and macules on the lower extremities, initially misdiagnosed as allergic purpura and treated with prednisone. Skin biopsy revealed dilated dermal vessels with perivascular collagen deposition, positive for collagen IV and diastase-periodic acid-Schiff (D-PAS) staining, consistent with cutaneous collagenous vasculopathy (CCV). Treatment included hydroxychloroquine, vitamin C, doxepin, and topical mucopolysaccharide polysulfate cream. Prednisone was tapered by one tablet every 3 days. After 4 weeks, the rash improved significantly with no new lesions. We would like to present a case of CCV.

PMID 42755575
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