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Medical research on claritin
Allergol Int. 2008 Jul 1; 57(3):
Izumi N, Mizuguchi H, Umehara H, Ogino S, Fukui H
Background: H(1) antihistamines are widely used as therapeutics for allergic diseases. Sedation is a well-known side effect of H(1) antihistamines and sometimes it is life-threatening for patients. Thus it is important to evaluate the sedative properties of H(1) antihistamines to avoid side effects. For this purpose, histamine H(1) receptor (H1R) occupancy and proportional impairment ratios (PIR) are now being used. However, it is not easy to obtain these parameters. Here, we sought to evaluate the sedative properties of H(1) antihistamines by means of a large-scale surveillance at health insurance pharmacies. Methods: The survey was conducted at 37 health insurance pharmacies. The therapeutic efficacy and the degree of sleepiness were quantified through a questionnaire using the visual analog scale (VAS) directly from 1742 patients who received H(1) antihistamines. Results: The degree of sleepiness caused by the first-generation antihistamines was significantly higher than that of the second-generation antihistamines. The high VAS score in case of efficacy was found in d-chlorpheniramine, olopatadine, and ebastine. Among the mean values of efficacy, all second-generation antihistamines except for loratadine, bepotastine, and mequitazine were significantly higher than that of clemastine. Regarding the degree of sleepiness, clemastine scored the highest VAS score, and significantly lower scores were obtained in all second-generation antihistamines. Conclusions: The sedative properties of the H(1) antihistamines obtained from VAS analysis were very similar to those of H1R occupancy from positron emission tomography (PET) studies and PIR from meta-analysis. Our results indicate that large-scale surveillance using VAS might be useful to evaluate the profiles of H(1) antihistamines.
Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine.
Acta Pharm. 2008 Jun 1; 58(2): 187-197
Mishra SK, Pathak K
A gastro retentive controlled release system of loratadine was formulated to increase the residence time in stomach and to modulate the release behaviour of the drug. Oil entrapped floating microbeads prepared by the emulsion gelation method were optimized by 23 factorial design and a polymer ratio of 2.5:1.5 (pectin/sodium alginate) by mass, 15% (m/V) of oil (mineral oil or castor oil) and 0.45 mol L-1 calcium chloride solution as the optimized processing conditions for the desired buoyancy and physical stability. In vitro drug release in the fed state conditions demonstrated sustained release of loratadine for 8 h, which best fitted the Peppas model with n < 0.45. The ethyl cellulose coating on microbeads optimized by 22 factorial design resulted in a controlled release formulation of loratadine that provided zero-order release for 8 h.
Ann Allergy Asthma Immunol. 2008 Mar; 100(3): 264-71
Anolik R,
BACKGROUND: Intranasal corticosteroids and nonsedating antihistamines are the drug classes most often prescribed to treat allergic rhinitis (AR). Treatment guidelines recommend a combination of these agents for moderate-to-severe AR. However, clinical studies have found that combining an antihistamine with an intranasal corticosteroid provides few or no advantages over monotherapy with an intranasal corticosteroid. OBJECTIVE: To compare the efficacy of mometasone furoate nasal spray (NS) plus loratadine with that of monotherapy with the individual agents in patients 12 years and older with at least a 2-year history of seasonal AR. METHODS: In a multicenter, randomized, double-blind, parallel-group, placebo-controlled clinical study, 702 patients were randomized to receive mometasone furoate NS, 200 microg, plus loratadine, 10 mg (n = 169); mometasone furoate NS, 200 microg (n = 176); loratadine, 10 mg (n = 181); or placebo (n = 176) once daily for 15 days. Primary efficacy variables were total nasal symptom score (TNSS) and total symptom score (TSS) as recorded on diary cards. RESULTS: No statistically significant differences were observed between mometasone furoate NS plus loratadine and mometasone furoate NS monotherapy for the primary efficacy variables. For TNSS and TSS, all 3 active drug therapies were more effective than placebo (P < or = .02). Both mometasone furoate NS treatment regimens were more effective than loratadine or placebo for TNSS (P < .01 for both) and TSS (P < or = .03 for both), whereas loratadine was more effective than placebo for TNSS only (P = .02). CONCLUSIONS: Combination therapy with mometasone furoate NS and loratadine provided benefits similar to monotherapy with mometasone furoate NS for the symptoms of seasonal AR. Therefore, mometasone furoate NS monotherapy was shown to be an effective treatment for seasonal AR.
Eosinophilic angiocentric fibrosis of the orbit.
Clin Experiment Ophthalmol. 2008 Apr; 36(3): 274-6
Kiratli H, Onder S, Yildiz S, Ozşeker H
A 30-year-old woman complained of right-sided epiphora for 2 years. She also reported diplopia on certain gaze positions and felt a hard mass behind the right medial inferior orbital rim. Magnetic resonance imaging studies demonstrated a relatively well-delineated mass in the right inferomedial orbit with minimal ethmoid sinus involvement. Histopathological evaluation following a large incisional biopsy showed massive eosinophilic infiltration and fibrosis with the final diagnosis of eosinophilic angiocentric fibrosis. She was then discovered to have significant peripheral eosinophilia and elevated serum IgE levels and clinical findings of allergic rhinitis and sinusitis. She was treated with systemic fluorocortolon and desloratadin for 4 months. She remained stable without recurrence for 32 months. The patient with this exceptionally rare tumour of the orbit benefited from debulking surgery followed by systemic corticosteroids and antihistaminics.
Rupatadine in allergic rhinitis and chronic urticaria.
Allergy. 2008 Apr; 63 Suppl 87: 5-28
Mullol J, Bousquet J, Bachert C, Canonica WG, Gimenez-Arnau A, Kowalski ML, Martí-Guadaño E, Maurer M, Picado C, Scadding G, Van Cauwenberge P
Histamine is the primary mediator involved the pathophysiology of allergic rhinitis and chronic urticaria, and this explains the prominent role that histamine H(1)-receptor antagonists have in the treatment of these disorders. However, histamine is clearly not the only mediator involved in the inflammatory cascade. There is an emerging view that drugs which can inhibit a broader range of inflammatory processes may prove to be more effective in providing symptomatic relief in both allergic rhinitis and chronic urticaria. This is an important consideration of the Allergic Rhinitis and its Impact on Asthma (ARIA) initiative which provides a scientific basis for defining what are the desirable properties of an 'ideal' antihistamine. In this review of rupatadine, a newer dual inhibitor of histamine H(1)- and PAF-receptors, we evaluate the evidence for a mechanism of action which includes anti-inflammatory effects in addition to a powerful inhibition of H(1)- and PAF-receptors. We assess this in relation to the clinical efficacy (particularly the speed of onset of action) and safety of rupatadine, and importantly its longer term utility in everyday life. In clinical trials, rupatadine has been shown to be an effective and well-tolerated treatment for allergic rhinitis and chronic idiopathic urticaria (CIU). It has a fast onset of action, producing rapid symptomatic relief, and it also has an extended duration of clinical activity which allows once-daily administration. In comparative clinical trials rupatadine was shown to be at least as effective as drugs such as loratadine, cetirizine, desloratadine and ebastine in reducing allergic symptoms in adult/adolescent patients with seasonal, perennial or persistent allergic rhinitis. Importantly, rupatadine demonstrated no adverse cardiovascular effects in preclinical or extensive clinical testing, nor negative significant effects on cognition or psychomotor performance (including a practical driving study). It improved the overall well-being of patients with allergic rhinitis or CIU based on findings from quality of life questionnaires and patient global rating scores in clinical trials. Thus, rupatadine is a recently introduced dual inhibitor of histamine H(1)- and PAF-receptors, which has been shown to be an effective and generally well-tolerated treatment for allergic rhinitis and chronic urticaria. It possesses a broader profile of anti-inflammatory properties inhibiting both inflammatory cells and a range of mediators involved in the early- and late-phase inflammatory response, but the clinical relevance of these effects remain to be clarified.
Anal Chim Acta. 2008 Apr 21; 613(2): 169-76
Suchara EA, Budziak D, Martendal E, Costa LL, Carasek E
In this study, a new solid-phase microextraction (SPME) method for simultaneous extraction of pharmaceutical compounds with acidic and basic characteristics (ibuprofen, fenoprofen, diclofenac, diazepam and loratadine) from residual water samples is proposed. In this procedure, the extraction is processed using two distinct sample pH values. The extraction is begun at pH 2.5 to promote the sorption of acidic pharmaceuticals and after 35 min the sample pH is changed to 7.0 by adding 0.4 mol L(-1) disodium hydrogenphosphate, so that the basic compounds can be sorbed by the fiber (20 min). The pH change is performed without interruption of the extraction process. A comparison between the proposed method and the SPME method applied to each group of the target compounds was performed. Gas chromatography coupled to mass spectrometry was used for separation and detection of analytes. The extraction conditions for the three methods were optimized using full factorial experimental design, response surface through a Doehlert matrix and central composite design. Limits of detection (0.02-0.43 microg L(-1)) and correlation coefficients (0.9970-0.9998) were determined for the three methods. The proposed extraction procedure was applied to samples of sewage treatment plant effluent and untreated wastewater. Recovery and relative standard deviation values ranged from 67 to 116% and 4.6 to 14.5%, respectively, for all compounds studied. Modification of sample pH during the extraction procedure was shown to be an excellent option for all of the compounds and may be extended to the simultaneous extraction of other compounds with different acid-base characteristics.
Drug Metab Dispos. 2008 Jul; 36(7): 1255-60
Lu C, Hatsis P, Berg C, Lee FW, Balani SK
Traditional cytochrome P450 (P450) based drug-drug interaction (DDI) predictions are based on the ratio of an inhibitor's physiological concentration [I] and its inhibition constant K(i). Determining [I] at the enzymatic site, although critical for predicting clinical DDIs, remains a technical challenge. In our previous study, a novel approach using cryopreserved human hepatocytes suspended in human plasma was investigated to mimic the in vivo concentration of ketoconazole at the enzymatic site (Lu et al., 2007), effectively eliminating the estimation of the elusive [I] value. P450 inhibition in this system appears to model that in vivo. Using the ketoconazole inhibition information in a human hepatocyte-plasma suspension together with quantitative P450 phenotypic information, we successfully predicted the pharmacokinetic DDIs for a small set of drugs, such as theophylline, tolbutamide, omeprazole, desipramine, midazolam, loratadine, cyclosporine, and alprazolam, as well as an investigational compound. For the applicability of this model on a wider scale the in vitro-in vivo correlation data set needed to be expanded. However, for most drugs in the literature there is not enough quantitative information on the involvement of individual P450s to predict DDIs retrospectively. To facilitate that, in this study we determined quantitative P450 phenotyping for seven marketed drugs: budesonide, buprenorphine, loratadine, sirolimus, tacrolimus, docetaxel, and methylprednisolone. Augmentation of the new data set with the one generated previously produced broader a database that provided further support for the wider applicability of this approach using ketoconazole as a potent CYP3A inhibitor. This application is predicted to be equally effective with other P450 inhibitors that are not substrates of efflux pumps.
Drug treatments for skin disease introduced in 2007.
Skin Therapy Lett. 2008 Mar; 13(2): 7-9
A comprehensive list of drug treatments for skin disease including: Adapalene Gel 0.3% (Differin(R)), Drospirenone/ Ethinyl Estradiol (Yaz(R)), Tretinoin 0.05% Gel (Anthralin(R)), Daptomycin for Injection (CUBICIN(R)), Retapamulin Ointment 1% (Altabax(R)), Tinidazole Tablets (Tindamax(R)), Ciclopirox Topical Solution 8%, Ketoconazole 2% Foam (Extina(R)), Terbinafine Hydrochloride (Lamisil(R)), Desloratadine (Aerius(R)/ Azomyr(R)/ Neoclarityn(R)), Levocetirizine Dihydrochloride (Xyzal(R)), Loratadine Dry Syrup 1% (Claritin(R)) and many other treatments introduced in 2007.
Clin Drug Investig. 1998 Dec; 16(6): 413-420
Davies RJ,
OBJECTIVE: To compare the dose-related efficacy and tolerability of the oral H(1) antihistamine ebastine (10 or 20mg) with a reference drug, loratadine (10mg), in the once-daily treatment of perennial allergic rhinitis (PAR). PATIENTS AND METHODS: The trial was conducted in 317 patients (aged 12 to 68 years) with ongoing symptoms of PAR. Mean 24-hour diary card symptom severity scores (0-3) were compared as changes from baseline between the randomised, double-blind treatment groups over a 4-week period. RESULTS: Symptom scores, including both 'perennial index' (PIN = sneezing + nasal itching + discharge) and total 'nasal index' (TNI = PIN + nasal stuffiness) showed statistically significantly greater improvements with ebastine 10 or 20mg than with loratadine 10mg for all parameters except sneezing, itching and ocular symptoms. The mean TNI scores were reduced by 44, 47 and 32%, respectively, over 4 weeks, and treatment differences were apparent from week 1 onwards. Patient and physician final opinions (percentage of patients improved) were also significantly in favour of ebastine (79 to 85%) vs loratadine (65 to 66%). The treatments were equally well tolerated and no serious adverse events occurred. CONCLUSION: This study found ebastine 10 or 20mg to be more effective than loratadine 10mg for the treatment of PAR.
Nasal challenge with allergen leads to maxillary sinus inflammation.
J Allergy Clin Immunol. 2008 May; 121(5): 1126-1132.e7
Baroody FM, Mucha SM, Detineo M, Naclerio RM
BACKGROUND: Allergic rhinitis and chronic rhinosinusitis are both characterized by chronic inflammation. OBJECTIVE: We sought to investigate the effect of nasal allergen challenge on the maxillary sinus and study the effect of premedication with loratadine. METHODS: We performed a double blind, crossover, randomized, placebo-controlled study in 20 allergic subjects out of season. After treatment with either placebo or loratadine (10 mg PO daily) for 1 week, a catheter was inserted into one maxillary sinus and used to lavage the cavity. The subjects then underwent nasal challenge with diluent for the allergen extract, followed by 3 concentrations of grass or ragweed. Nasal and ipsilateral sinus lavages were performed after each challenge and then hourly for 8 hours. Sneezes and symptoms were recorded, and the lavage specimens were evaluated for eosinophils and levels of eosinophil cationic protein, albumin, and histamine. Eleven of the subjects underwent a similar challenge with lactated Ringer's solution. RESULTS: Compared with the lactated Ringer's solution challenge, allergen challenge resulted in significant increases in most early- and late-phase nasal parameters. Allergen challenge of the nose also led to a significant increase compared with control values in maxillary sinus eosinophils and the levels of albumin, eosinophil cationic protein, and histamine during the late response. Loratadine resulted in significant inhibition of the nasal early response compared with that seen with placebo (P < .05). CONCLUSION: These findings suggest that a neural reflex or systemic allergic inflammation is responsible for the sinus inflammatory response and that this inflammatory response might play a role in the development of rhinosinusitis in allergic subjects.