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H1-antihistamines

Dec 21
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An evaluation of remission rates with first and second line treatments and indicators of antihistamine refractoriness in chronic urticaria

By New, Selected articles

Sinem Ayse Ornek

Int Immunopharmacol . 2022 Sep 15;112:109198. doi: 10.1016/j.intimp.2022.109198. Online ahead of print.

Chronic urticaria is a common condition characterized by recurrent pruritic wheals and/or angioedema for more than 6 weeks. As a first-line treatment, guidelines recommend standard doses of antihistamines and as second-line an increase in antihistamines’ dose. There is a lack of studies on remission rates with first and second-line treatments as well as indicators of antihistamine response. The aim of this study was to assess response rates to chronic urticaria first and second-line treatments and to identify characteristics of the patients that can help estimate treatment outcomes.

Different types of urticaria outcomes were retrospectively analyzed: 556 chronic spontaneous urticaria and 101 chronic inducible urticaria cases on at least 3 months of follow-up data.

Results have shown that a standard dose of 2nd generation antihistamines was proving efficacy in 43% of the patients. An additional 28.8% of patients were in remission with 2nd line treatments. Increasing antihistamine dose, combining two different 2nd generation antihistamines, combining 1st and 2nd generation antihistamines or combining leukotriene receptor antagonist offered remission in 38.3 %, 35.8 %, 37.5% and 25 % of patients who were given these treatments, respectively.

In conclusion, it is important to have a stepwise approach to managing chronic urticaria because the number of patients who respond to treatment increases with each step.

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Sep 29
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The Role of Coagulation and Complement Factors for Mast Cell Activation in the Pathogenesis of Chronic Spontaneous Urticaria

By Artículos seleccionados, Selected articles

Yuhki Yanase, Shunsuke Takahagi, Koichiro Ozawa y Michihiro Hide

Cells. 2021 Jul 12;10(7):1759. doi: 10.3390/cells10071759.

Chronic spontaneous urticaria is a skin condition characterized by skin edema and itchy flares for more than six weeks. Inflammatory mediators, such as histamine, are released from skin mast cells and/or peripheral basophils at the cell level. It is known that the extrinsic coagulation cascade triggered by tissue (TF) and complement factors is based on the pathogenesis of chronic spontaneous urticaria (CSU).

This review aimed to give a detailed role of vascular endothelial cells, leukocytes, extrinsic coagulation factors, and complement components on TF-induced activation of skin mast cells and peripheral basophils to form edema.

The extrinsic coagulation system triggered by TF and activated coagulation factors has been suggested in urticaria’s pathogenesis. Some studies have reported its improvement with heparin or warfarin treatment.

The detailed role of vascular endothelial cells in plasma leakage, especially at local areas of the skin in CSU is unclear. In vitro studies revealed that vascular endothelial cells might have a role in the early stage of CSU pathogenesis, as human umbilical vein endothelial cells and human dermal microvascular endothelial cells express a large amount of TF on their surface in response to the combination of several molecules such as histamine. TF-expressing leucocytes can generate the extrinsic coagulation cascade and produce activated coagulation factors, followed by the induction of intercellular gap formation of human umbilical vein endothelial cells. TF expression on monocytes may be utilized as a marker for pathological conditions of CSU and a therapeutic target of severe and refractory CSU. Studies have also shown that complement factors, such as C5a are increased in people with CSU.

Medications that target the activated coagulation factors and/or complement components may constitute a new and effective treatment for severe and refractory urticaria, namely low-molecular-weight antagonists of C5a and targets of the TF-triggered extrinsic coagulation pathway – complement system – mast cell and/or basophil activation axis.

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Aug 10
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Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation

By Articles about Bilastine, Publicaciones sobre Bilastina

Dolores Ochoa, Manuel Roman, Carmen Belmonte, Samuel Martin-Vilchez, Gina Mejia-Abril, Francisco Abad-Santos, Gonzalo Hernandez, Paula Arranz, Lorena Elgezabal, Nieves Fernandez

Adv Ther . 2021 Jun 12. doi: 10.1007/s12325-021-01801-y. Online ahead of print.

Bilastine is a second-generation H1 antihistamine for allergic conditions. A new ophthalmic formulation was developed based on the efficacy and safety profiles of the oral formulation. The aim of this study was to assess the safety and pharmacokinetics of ophthalmic bilastine (6 mg/ml) in adults after one and various doses.

This was an open-label, single-centre, phase 1, bioavailability study that included 12 healthy participants (aged 18-55 years old). Participants were administered one drop of the bilastine eye formulation in each eye for five days. Serum levels of bilastine were assessed by HPLC-MS/MS and adverse drug reactions registered during administration and follow-up.

After various admininistrations, bilastine blood levels were 2682,26 ± 1615,88 pg/mL at 2,5 hours. The half-life of bilastine was 7,88 ± 6,72 h. Area under the curve was 19512,51 ± 9248,76 h/pg/mL. Dysgeusia was the main adverse event, which was mild and transient.

The ophthalmic formulation has proved to be absorbed in low amounts to the bloodstream, showing a good safety profile after administration of various doses.

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Jul 09
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Could Histamine H1 Receptor Antagonists Be Used for Treating COVID-19?

By Selected articles

Changbo Qu, Gwenny M. Fuhler, Yihang Pan

Int J Mol Sci . 2021 May 26;22(11):5672. doi: 10.3390/ijms22115672.

The pandemic of COVID-19, caused by SARS-CoV-2, has led to extensive and long-term health issues in those affected by the disease. It is essential to identify new treatments for COVID-19 infection with a better outcome too. The objective of this review is to summarize the use of H1 receptor antagonists in SARS-CoV-2 infection.

One of the common characteristics of severe COVID-19 is unbalanced lung inflammation. Reducing lung inflammation can help improve COVID-19 clinical manifestations. H1 receptor antagonists may inhibit SARS-CoV-2 either via the H1 receptor or via the ACE2 receptor. The virus spike proteins interact with both cellular heparan sulfate and ACE2 through its receptor-binding domain, and H1-antihistamines may disrupt the interaction between heparan sulfate and spike protein, inhibiting the virus entry in the cell.

New-generation H1 receptor antagonists, such as loratadine and desloratadine, may help inhibit SARS-CoV-2 infection by reducing lung inflammation induced by histamine, as well as other inflammatory activities. These antihistamines have also been shown to exert antiviral effects when blocking H1 receptors and, therefore, to affect SARS-CoV-2 replication via the mediation of metabolism and immune responses.

In conclusion, H1 receptor antagonists are relatively inexpensive drugs, ready to use and with the capacity to improve patient outcomes due to their role in reducing inflammation and antiviral effects. They may also be attractive prophylactic candidates for lowering the risk of SARS-CoV-2 infection in the general population.

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May 14
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Use of H-1 Antihistamine in Dermatology: More than Itch and Urticaria Control: A Systematic Review

By Selected articles

Chang-Yu Hsieh, Tsen-Fang Tsai

Dermatol Ther (Heidelb). 2021 Apr 12. doi: 10.1007/s13555-021-00524-w. Epub ahead of print.

H1-antihistamines are known for their effects in suppression of pruritus, especially in urticaria. However, there are many other dermatological uses of H1-antihistamines, such as scarring and nonscarring alopecia, acne, Darier disease, eosinophilic dermatoses, paraneoplastic dermatoses, psoriasis, lichen nitidus, radiation dermatitis, skin dysesthesia, and cutaneous malignancies.

This review includes a literature search on articles that report the use of H1-antihistamines.

It is the modulation of the immune system, inflammatory cytokines, and mast cells that explain why H1-antihistamines are effective in some autoimmune conditions, such as Kaposi sarcoma, melanoma, and alopecia areata. Some eosinophilic dermatosis may be relieved with the use of cetirizine and bilastine due to their effects on the chemotaxis of eosinophils. Hydroxyzine, together with GABA receptor agonists, may have an effect on cutaneous dysesthesia. A combination of antihistamines with isotretinoin helps control acne better, probably due to the inhibition of the production of sebum. The reversing vascular effect of histamine seems to be of interest for erythema, edema, and pain control in radiation dermatitis and erythromelalgia.

New properties of antihistamines have also been studied in vitro: antibacterial activity, antiangiogenesis, and antifibrosis.

H1-antihistamines may improve symptoms of some conditions when used alone or in combination with other treatments; however, this evidence is still limited. More studies are needed to assess the efficacy and dosage of H1-antihistamines in other dermatological conditions.

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Nov 20
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Bilastina

Multidisciplinary Real-World Experience With Bilastine, a Second Generation Antihistamine

By Eprint, News

Lynde CW, Sussman G, Dion PL, Guenther L, Hébert J, Rao J, Leek TV, Waserman S.

J Drugs Dermatol. 2020 Feb 1;19(2):145-154. doi: 10.36849/JDD.2020.4835.

Allergic conditions, such as seasonal allergic rhinitis, perennial allergic rhinitis (PAR), and urticaria (both acute and chronic) are frequently treated with H1-antihistamines. However, first-generation H1-antihistamines cause impairment and potentially interfere with restful sleep, cause hangovers or “morning after” effects, impair learning and memory, and reduce work efficiency. Second generation antihistamines, such as bilastine have shown to decrease allergy symptoms effectively without causing night-time sleep disturbances and related adverse events.

Bilastine is a prescription medicine. It is not derived from nor is it a metabolite of another antihistamine, has a rapid one-hour onset of action and provides sustained efficacy. Bilastine does not penetrate the brain, is scarcely metabolized and does not interact with cytochrome P450. For the treatment of allergic conditions in adults and children over 12 years of age, a daily oral dose of bilastine 20 mg is recommended.

This real world case project was developed to help optimize patient care and supported with evidence from the literature. It included patients between 9 and 76 years old with seasonal allergic rhinitis, perennial allergic rhinitis and chronic and acute urticaria as well as urticarial vasculitis and pruritus associated with inflammatory skin conditions.

The presented cases using bilastine showed positive outcomes for the patients, relieving symptoms with safety and good tolerance.

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Nov 20
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urticaria y antihistaminicos H1

Current and emerging pharmacotherapy for chronic spontaneous urticaria: a focus on nonbiological therapeutics

By Artículos seleccionados, Selected articles

Kam Lun Hon, Joyce T. S. Li, Alexander K.C. Leung, Vivian Lee

Expert Opin Pharmacother. 2020 Sep 29. doi: 10.1080/14656566.2020.1829593. Online ahead of print.

Urticaria is characterized by pruritic wheals of the skin’s superficial layers, which occurs for six weeks or longer, with no apparent cause. It is a condition that reduces the quality of life of the patient and may have a significant economic and social burden. The objective of this revision was to review the guidelines for urticaria management.

According to the joint initiative of the EU-founded network of excellence, the Global Allergy and Asthma European Network, the European Academy of Allergology and Clinical Immunology, the World Allergy Organization, and the European Dermatology Forum, management of urticaria should be done in a stepwise manner. Second-generation H1-antihistamines are considered first-line treatment. Whenever symptoms are not adequately controlled, treatment should follow the algorithm. This algorithm includes an increase of the dose of second-generation H1-antihistamines, alongside first-generation H1-antihistamines, H2 antagonists, omalizumab, ciclosporin A, or short-term corticosteroids if needed. New treatments on development include spleen tyrosine kinase inhibitor, Bruton tyrosine kinase inhibitor, prostaglandin D2 receptor inhibitor, H4-antihistamines, and biologics. Alternative agents include leukotriene receptor antagonists, anticoagulant and antifibrinolytic agents, antidepressants, vitamin D, and other anti-inflammatory or immune-suppressing agents.

According to the authors, second-generation H1-antihistamines should always be considered the first-line therapeutic option for urticaria management. For those who do not respond to a higher dose of H1-antihistamines, guidelines recommend adding omalizumab. Well-designed trials are required to draw clear conclusions.

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Aug 24
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Clinical Control of CSU with Antihistamines Allows for Tolerance of NSAID-Exacerbated Cutaneous Disease

By Selected articles

Jorge Sánchez

J Allergy Clin Immunol Pract . 2020 Jul 14;S2213-2198(20)30700-5. doi: 10.1016/j.jaip.2020.06.057. Online ahead of print.

A great number of patients with chronic spontaneous urticaria experience exacerbations after treatment with non-steroidal anti-inflammatory drug (NSAID). Although international guidelines suggest that people with urticaria avoid NSAIDs, this is sometimes difficult. Some case reports recommend that H1-antihistamines can help prevent these exacerbations.

The objective of this study was to evaluate if H1-antihistamines can help prevent NSAID-exacerbated reactions in people with chronic spontaneous urticaria.

This was a cross-over, multi-center, and ambispective study in 3 centers in Medellín, Colombia that included 121 participants with chronic spontaneous urticaria and a history of NSAIDs exacerbations. A diagnostic challenge test without the use of antihistamines and a challenge test using antihistamines were performed using the NSAID reported in the medical record. The order in which test were performed in each participant was determined by the investigator: participants with a positive first diagnostic challenge, were subject to a second challenge using H1-antihistamines, those with a negative first challenge using H1-antihistamines, were subject to a second one without the use of H1-antihistamines, and those with a negative first diagnostic challenge or a positive first challenge using H1-antihistamines, did not undergo a second challenge. Some patients were subject to an alternative NSAID before the diagnostic challenge test or the challenge test using H1-antihistamines.

The diagnostic challenge test retrieved 96 participants testing positive, with 75 % (72 participants) tolerating the NSAID involved in the reaction when they added H1-antihistamines.

In conclusion, although NSAID may represent some restrictions for people with chronic spontaneous urticaria, the use of H1-antihistamines can help control further urticaria exacerbations due to NSAID treatment.

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May 27
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skin microdyalisis

Chronic urticaria in the real-life clinical practice setting in the UK: results from the non-interventional multicentre AWARE study.

By Selected articles

Savic S, Leeman L, El-Shanawany T, Ellis R, Gach JE, Marinho S, Wahie S, Sargur R, Bewley AP, Nakonechna A, Randall R, Fragkas N, Somenzi O, Marsland A.

Clin Exp Dermatol. 2020 Apr 4. doi: 10.1111/ced.14230. [Epub ahead of print]

Chronic urticaria is a group of skin conditions that include chronic spontaneous urticaria and chronic inducible urticaria. Symptoms include itchy wheals and/or angioedema for a period longer than 6 weeks. The objective of this study was to provide information demonstrating the real-life burden of chronic urticaria in the UK.

The non-interventional AWARE study (A World-wide Antihistamine-Refractory chronic urticaria patient Evaluation) collected data from a representative sample of chronic urticaria patients worldwide. A subset of UK patients aged 18-75 diagnosed with H1-antihistamine-refractory chronic spontaneous urticaria was analysed.

Baseline analysis included 252 UK patients, mostly female (77,8%) with moderate-to-severe disease activity and a spontaneous component to their chronic urticaria. Comorbidities included depression/anxiety (24,6%), asthma (23,8%) and allergic rhinitis (12,7%). 57,9% of the patients had undergone a treatment. Their mean Dermatology Life Quality Index score was 9,5 with report of reduction in work productivity and activity. These patients referred a high need to use healthcare resources. Chronic spontaneous urticaria severity was linked to gender, obesity, anxiety and diagnosis.

Only 28,5% of UK patients completed all nine study visits, which limits analysis of long-term treatment patterns and disease impact. Chronic urticaria patients reported high rates of healthcare resource use and impairment in quality of life, work productivity and activity at baseline, which highlights the need to ensure appropriate management to optimise patient quality of life and reduce the socioeconomic burden of chronic urticaria in the UK.

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Apr 21
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eprint

Bilastine: a lifetime companion for the treatment of allergies

By Eprint

Martin K Church, Marysia Tiongco-Recto, Erminia Ridolo & Zoltán Novàk.

(2019) Current Medical Research and Opinion, DOI: 10.1080/03007995.2019.1681134

Bilastine is a potent and highly selective H1-antihistamine for the treatment of urticaria and allergic rhinoconjunctivitis.

This is a review article that gathers information available up to 25 February 2019 on the use of the H1-antihistamine bilastine in the treatment of allergic disorders in different age groups, from children to adults.

Teenagers and adults bilastine dose is usually 20 mg daily and children up to 12 years old is 10 mg of bilastine once daily. Bilastine has demonstrated efficacy at improving allergic rhinitis symptoms, such as nasal and ocular symptoms and at improving wheals and itching in urticaria. It has a rapid onset of action and a long duration of action.

Bilastine does not interact with the CYP450 system, making it a H1-antihistamine free from drug-drug interactions. Patients with renal or hepatic impairment or elderly ones don’t need dosage adjustment. Bilastine is well tolerated, even at above standard doses and doesn’t exhibit anticholinergic or cardiotoxic effects. It has minimal sedative properties due to its inexistence central nervous system penetration. Patients on bilastine show an overall improvement of health-related quality of life.

In conclusion, bilastine is a suitable option of H1-antihistamins for the treatment of allergic rhinoconjunctivitis or urticaria in all patients.

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Nov 27
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posición declaración c

CSACI position statement: Newer generation H1-antihistamines are safer than first-generation H1-antihistamines and should be the first-line antihistamines for the treatment of allergic rhinitis and urticaria

By Selected articles

Fein MN, Fischer DA, O’Keefe AW, Sussman GL.

Allergy Asthma Clin Immunol. 2019 Oct 1;15:61. doi: 10.1186/s13223-019-0375-9. eCollection 2019. Review.

H1-antihistamines are the most used class of medications for the treatment of allergic rhinitis and urticaria. The first generation of antihistamines has been available since 1946, however its common side effects, such as sedation, impairment with decreased cognitive function, poor sleep quality, dry mouth, dizziness and orthostatic hypotension led to the development of newer, less-sedating second and third generation antihistamines, which became available in the 1980s. These newer generations of H1-antihistamines have a better safety profile and improved potency and efficacy. They are the recommended first-line treatment for mild allergic rhinitis and acute and chronic urticaria.

The Canadian Society of Allergy Clinical Immunology (CSACI) recommends that second and third generations of H1-antihistamines are preferred over first generation antihistamines for the treatment of allergic rhinitis and urticaria. CSACI also recommends that first generation antihistamines should only be sold behind the counter in pharmacies and as a last resort due to the risks of their use.

To help change practice and improve patient health and safety, the CSACI recommends that efforts are needed to disseminate this information to healthcare providers and patients.

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Nov 27
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seguridad tolerabilidad bilastina

The safety and tolerability profile of bilastine for chronic urticaria in children

By Articles about Bilastine

Papadopoulos NG, Zuberbier T.

Clin Transl Allergy. 2019 Oct 23;9:55. doi: 10.1186/s13601-019-0294-3. eCollection 2019. Review.

Urticaria is characterized by the development of pruritic wheals, angioedema or both. Guidelines from early 2018 recommend that urticaria is classified based on its duration as acute (< 6 weeks) or chronic (> 6 weeks). In addition, they also classify chronic urticaria as spontaneous or inducible. Chronic urticaria is less frequent than acute in children, but is a condition that requires treatment, as it affects children’s daily activities, disturbs sleep, causes emotional distress and influences negatively learning and cognition.

Bilastine is a H1-antihistamine that has been studied in children at the dose of 10mg/daily and is licensed for the symptomatic relief of urticaria symptoms in children > 6 to 11 years.

Investigation in paediatric population included bilastine and rupatadine among the second-generation antihistamines. A phase III, doubleblind, randomized, placebo-controlled, parallel-group clinical trial was carried out to assess the safety and tolerability of bilastine 10 mg once daily for 12 weeks in 509 children aged 2–11 years with allergic rhinitis or chronic urticaria. The primary endpoint was the proportion of children in each treatment group without treatment-emergent adverse events (TEAEs). Secondary endpoints included the assessment of somnolence/sedation with the Pediatric Sleep Questionnaire (PSQ). No statistically significant differences were found between treatment groups for incidences of TEAEs or related TEAEs in the population overall or by age subgroup. The majority of related TEAEs were mild to moderate in intensity. PSQ scores for somnolence/sedation decreased slightly from baseline to week 12 in both the bilastine 10 mg and placebo groups.

In conclusion, bilastine is a suitable for treatment of urticaria in children, due to its efficacy and good tolerability profile that were proven in well-controlled studies. Specifically, lack of potential to induce sedation allows prolonged administration without impairment of performance and learning abilities.

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Jul 26
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The Role of Mobile Health Technologies in Allergy Care: an EAACI Position Paper.

The Role of Mobile Health Technologies in Allergy Care: an EAACI Position Paper

By Selected articles

Matricardi PM, (…)

Mobile Health (mHealth) uses mobile communication devices such as smartphones and tablet computers to support and improve health-related services, data flow and information, patient self-management, surveillance, and disease management from the moment of first diagnosis to an optimized treatment. The European Academy of Allergy and Clinical Immunology created a task force to assess the state of the art and future potential of mHealth in allergology.

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Jul 26
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Diagnosis and treatment of urticaria in primary care

Diagnosis and treatment of urticaria in primary care

By Selected articles

Kayiran MA, Akdeniz N.

Urticaria, also known as hives among people, is a very common disease characterized by erythematous, edematous, itchy, and transient plaques that involve skin and mucous membranes. It is classified as acute spontaneous urticaria, chronic spontaneous urticaria, chronic inducible urticaria, and episodic chronic urticaria. Many factors such as infections, medicines, food, psychogenic factors, and respiratory allergens are accused of etiology, but sometimes, it is idiopathic. Clinical presentation involves red, swelling, and itchy plaques. The lesions usually resolve spontaneously within 2-3 h without a trace.

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Jul 26
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Second generation antihistamines: an update

Second generation antihistamines: an update

By Selected articles

Allergic rhinoconjuntivitis, rhinitis and urticaria are major health problems that affect a sizable portion of the population of all ages, interfering with quality of life and resulting in an important burden for the health system.

First generation antihistamines have major unwanted effects, including sedation, weight gain and anticholinergic effects. Second generation H1-antihistamines (SGAHs) are free from the unacceptable side effects of the first-generation ones and are now preferred by physicians and patients as first line therapies.

SGAHs have a good absorption profile, whenever administered orally, with effective plasma concentrations being reached in most of them within 3 hours after dosing. Their liposolubility permits the crossing of cell membranes, helping their bioavailability.

Regarding their metabolism and elimination, H1-antihistamines bind to transporter plasmatic proteins, with plasma protein binding varying from 60 to 95%. The higher plasma protein binding, the less persistent antihistamine effects. Benzodiazepines may decrease H1-antihistamines plasma concentrations. Macrolides, antifungals and calcium antagonists may increase plasmatic concentrations.

H1-antihistamines are well tolerated for allergic rhinoconjunctivitis at the usual dosage. In respect to urticaria, their efficacy is attributed to their H1-antihistaminic activity on small unmyelinated afferent C-fibers to reduce itching, on axonic reflexes to reduce erythema and on the endothelial cells of the post-capillary venules to reduce extravasion and wheal formation. Most H1-antihistamines appear to have anti-inflammatory effects including the reduction of production of preformed and neoformed mediators, cytokines, chemokines and adherence molecules, inflammatory cell recruitment and inflammation in general.

This article summarizes an update on the clinical pharmacology, mechanisms of action and safety of the second-generation antihistamines.

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