piperidines and Conjunctivitis

The guidelines of German and European associations of allergology recommend the treatment of severe allergic rhinitis with a combination of oral antihistamines and nasal steroids. Many patients face this option rather skeptically, so that ENT specialists mostly use antihistamine monotherapy with a higher dosage. This increased dose may cause drowsiness, as has been demonstrated for cetirizine and loratadine. However, ebastine is a non-sedating antihistamine. Furthermore, it has been shown that improved clinical efficacy can be attained with an increased dosage of 20 mg daily in comparison to the usual dosage of 10 mg/day without increasing the rate of side effects.. In this prospective post-marketing survey, the treatment of 4,307 patients with allergic rhinitis was documented during the pollen season 2005. The severity of rhinitis symptoms and satisfaction with the treatment were recorded.. Treatment with 20 mg ebastine daily as monotherapy led to a significantly greater reduction in symptoms (P=0.002) than the combination therapy.. This outcome could be attributed to an assumed better compliance in patients with monotherapy.

Topics: Adrenal Cortex Hormones; Adult; Butyrophenones; Conjunctivitis; Drug Combinations; Female; Germany; Histamine H1 Antagonists; Humans; Male; Piperidines; Practice Patterns, Physicians'; Prevalence; Rhinitis, Allergic, Seasonal; Treatment Outcome

We have evaluated the efficacy of topical levocabastine in 42 patients (20 males and 22 females; mean age 37.5 yrs.) affected by perennial allergic rhinoconjunctivitis due to Dermatophagoides pteronyssinus. Diagnosis was performed on the basis of clinical history, Skin Prick test and RAST. The study lasted for 90 days and nasal spray levocabastine was administered at the dose of 2 puff in each nostril twice a day. Patients had to record the severity of the symptoms considered (sneezing, nasal pruritus, nasal obstruction and rhinorrhea) on a diary card according to an arbitrary score from 0 to 3. At the end of the treatment patients experienced a significant improvement of their symptoms and no side effects were recorded. On the basis of our results levocabastine can be considered a useful drug in the treatment of allergic rhinitis due to Dermatophagoides pteronyssinus.

Topics: Administration, Intranasal; Adult; Aerosols; Analysis of Variance; Conjunctivitis; Female; Histamine H1 Antagonists; Humans; Male; Piperidines; Rhinitis, Allergic, Perennial

H1-antihistamines are commonly used drugs, and probably the most frequently used for allergic diseases. They are pharmacologic inverse agonists of histamine at H1 receptor sites and try to shift the equilibrium of this receptor toward the inactive state, preventing H1 response. A wide variety of adverse effects have been attributed to antihistamines, and they can exceptionally induce skin reactions. We report the case of a patient with several episodes of urticaria induced by different families of antihistamines - piperazines and piperidines. We performed skin prick tests (SPT), patch tests and oral challenges to different antihistamines. We found positive SPT to some antihistamines, and positive oral challenge in others with negative SPT. The route of sensitization remained unclear, and our patient could not finally tolerate any antihistamine after the oral challenges we performed. We support the hypothesis that antihistamines may shift the H1 histamine receptor to the active conformation instead of the inactive conformation, prompting adverse reactions after dosing. This is the first report of urticaria induced by different antihistamines in the same patient with positive SPT to several others.

Topics: Adult; Conjunctivitis; Drug Hypersensitivity; Female; Histamine H1 Antagonists; Humans; Piperazines; Piperidines; Rhinitis; Urticaria

Recent decades have been marked by an increasing number of patients suffering from ocular allergic-like symptoms without being associated with an increase in IgE levels. These symptoms include heaviness of the lid, foreign body sensation, burning, stinging and photophobia. Both epidemiological studies and controlled human exposure clinical studies have shown cause-effect relationships between allergic-like symptoms and environmental factors such as outdoor air pollutants or poor indoor air quality. An ocular surface subclinical inflammation is thought to be responsible for pseudoallergic, pollution-related conjunctivitis. The complement system is considered as one of the major effector mechanisms involved in initiation of the subclinical inflammation that leads to IgE-independent eye irritation.. To study the capability of nine antiallergic eyedrops commonly used in the treatment of allergic conjunctivitis to inhibit complement activation induced in vitro by pollutants.. Normal human serum obtained from healthy individuals was used as a source of complement. Activation of complement was assessed using the complement hemolytic 50% (CH50) assay, in the absence or the presence of antiallergic eyedrops and in the absence or the presence of various stimuli, including sand, common house dust, eye mascara, and Dactylis glomerata pollen extract. Zymosan was used as a standardized complement activator. The following eyedrops were studied: Naabak (4.9% N-acetyl aspartic acid-glutamic acid, NAAGA, sodium salt), Almide (lodoxamide 0.1%), Levophta (0.05% levocabastine), Emadine (0.05% emedastine), Tilavist (2% nedocromil), Allergodil (0.05% azelastine), Patanol (olopatadine), and Zaditen (0.025% ketotifen). Effects of preservative-free lodoxamide and ketotifen were also assessed and compared to those of the preserved formulations. A solution of 0.01% benzalkonium chloride (BAC), the most widely used preservative in topical eyedrops, was also tested.. Zymosan-induced activation of complement (30+/-6%) was significantly lowered by preincubation of serum with unpreserved NAAGA (16.6+/-4%, p=0.0026) or benzalkonium-preserved nedocromil (20+/-2%, p=0.022). Preserved levocabastine, emedastine, olopatadine and ketotifen did not interfere with zymosan-induced complement activation, whereas preserved azelastine, lodoxamide and benzalkonium chloride significantly aggravated complement activation induced by zymosan. Similar results were obtained when complement activation was triggered by sand, common house dust, mascara, or by an allergenic extract of Dactylis glomerata pollen. In the absence of complement activator, none of the antiallergic eyedrops induced a significant change in CH50 titer, indicating that the deleterious pro-inflammatory effect of preserved azelastine and lodoxamide may occur only once complement activation has been initiated, i.e., on an inflamed ocular surface.. Among the antiallergic eyedrops tested in this study, only Naabak and Tilavist were found to significantly inhibit complement activation triggered by particulate matters or pollen allergenic extract. Such an anticomplement activity confers these two molecules a potential in the therapeutic management of pollution-related pseudoallergic conjunctivitis.

Topics: Air Pollutants; Anti-Allergic Agents; Benzalkonium Compounds; Benzimidazoles; Complement Activation; Conjunctivitis; Cosmetics; Dibenzoxepins; Dipeptides; Drug Evaluation; Dust; Humans; In Vitro Techniques; Ketotifen; Nedocromil; Olopatadine Hydrochloride; Ophthalmic Solutions; Oxamic Acid; Phthalazines; Piperidines; Pollen; Silicon Dioxide; Zymosan

Topics: Anti-Allergic Agents; Antifungal Agents; Asthma; Conjunctivitis; Histamine H1 Antagonists; Humans; Piperidines; Rhinitis, Allergic, Seasonal