Second‐ and third‐generation antihistamines in the treatment of urticaria

Ellis, Anne K.; Day, James H.

doi:10.1046/j.1529-8019.2000.00034.x

Cited by 12 publications

(6 citation statements)

References 77 publications

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“…Allylamines are an important class of compounds that have seen use as antifungals, 1 antihistimines, 2 antidepressants, 3 and even as a treatment for male sexual dysfunction. 4 They have also served as useful building blocks in complex molecule synthesis.…”

mentioning

confidence: 99%

Palladium-Catalyzed Regioselective Arylation of Unprotected Allylamines

Landge

Maxwell

Chand-Thakuri

et al. 2020

JACS Au

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Palladium-catalyzed organometallic transformations of free amines are often unsuccessful due to side reactions, such as oxidation, that can occur. However, the ability to furnish the free amine products from these reactions is important for improving the utility and sustainability of these processes, especially for accessing their potential as medicinal and agrochemical agents. Notably, the 3,3-diarylallylamine motif is prevalent in a variety of biologically relevant structures, yet there are few catalytic approaches to their synthesis, and none involving the free amine. Herein, we describe a simple protocol for the arylation of cinnamylamines and the diarylation of terminal allylamines to generate a diverse group of 3,3-diarylallylamine products using a Pd II precatalyst. Key features of the method are the ability to access relatively mild conditions that facilitate a broad substrate scope as well as direct diarylation of terminal allylamine substrates. In addition, several complex and therapeutically relevant molecules are included to demonstrate the utility of the transformation.

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mentioning

confidence: 99%

Palladium-Catalyzed Regioselective Arylation of Unprotected Allylamines

Landge

Maxwell

Chand-Thakuri

et al. 2020

JACS Au

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“…On the other hand, patients with autoimmune COU may respond poorly to antihistamines. Patients with DPU usually fail to respond to antihistamine treatment but high doses (30 mg daily) of cetirizine have been reported to be effective [33].…”

Section: Choice Of Antihistamines In Clinical Practicementioning

confidence: 99%

Urticaria: current and future treatments

Borzova

Grattan

2007

Expert Review of Dermatology

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Urticaria is a common disorder with diverse clinical presentations. Correct recognition of the different clinical patterns promotes more effective treatment. Management involves treatment of any identifiable external causes, including infection, avoidance of drug, food and physical triggers and the appropriate use of pharmacological therapies. These can be divided into first-, second-and third-line approaches. The choice of treatment will be influenced by many factors, including drug licensing, safety, pattern of disease, disease severity, pharmacoeconomic considerations and patient preference. H1 antihistamines are the mainstay of treatment of most patterns of urticaria and are effective in the majority of patients with mast cell-mediated disease. Second-generation antihistamines have a better therapeutic index and improved pharmacodynamic properties compared with older 'classic' antihistamines and should be prescribed preferentially for chronic urticaria. Patients who are unresponsive to H1 antihistamines at full dose may require short-term treatment with oral corticosteroids but their long-term use for urticaria should be avoided whenever possible on account of the risk of serious adverse effects. Antileukotrienes and alternative second-line agents, prescribed off licence, can be helpful for patients who respond poorly to antihistamines when taken in conjunction but a better evidence base is needed to guide prescribing. Third-line immunosuppressive therapies can be considered for debilitating urticaria, especially for patients with corticosteroid-dependent chronic disease, and may have some potential to modify the natural course of the illness. Possible new therapeutic approaches on the horizon include new H1 antihistamines, H4 receptor antagonists, a histidine decarboxylase inhibitor under development and biological agents that target histamine-releasing autoantibody production and function.

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“…Cetirizine lacks activity at α‐adrenergic, dopamine, serotonin, and muscarinic receptors. Although it does not readily cross the blood–brain barrier, it does cause a higher incidence of sedation than placebo (12,13). There are no reports of associated cardiac toxicity with cetirizine.…”

Section: The Pharmacology Of Antihistaminesmentioning

confidence: 99%

“…Animal studies suggest that desloratadine is approximately 2.5–4.0 times more potent as an H1 antihistamine than loratadine. Neither loratadine nor desloratadine have known cardiac toxicity (2,13,15).…”

Section: The Pharmacology Of Antihistaminesmentioning

confidence: 99%

Antihistamines and their role as antipruritics

O’Donoghue

Tharp

2005

Dermatologic Therapy

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Antihistamines that bind to the histamine 1 receptor (H1) serve as important therapeutic agents to counter the effects of histamine in the skin. Two generations of antihistamines exist; however, second-generation agents are more advantageous because they cause less sedation, have a longer half life and are more selective for the H1 receptor. While H1 antihistamines have proven to be effective at reversing the pruritus and cutaneous lesions of chronic urticaria, their ability to treat pruritus associated with other cutaneous and systemic diseases is unproven.

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Second‐ and third‐generation antihistamines in the treatment of urticaria

Cited by 12 publications

References 77 publications

Palladium-Catalyzed Regioselective Arylation of Unprotected Allylamines

Palladium-Catalyzed Regioselective Arylation of Unprotected Allylamines

Urticaria: current and future treatments

Antihistamines and their role as antipruritics

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