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Desloratadine and Pseudoephedrine [keywords]
- Stability-indicating micelle-enhanced spectrofluorimetric method for determination of loratadine and desloratadine in dosage forms. [Journal Article]
- Luminescence 2011 Nov-Dec; 26(6):670-9.
A highly sensitive and simple spectrofluorimetric method was developed for the determination of loratadine (LRT) and desloratadine (DSL) in their pharmaceutical formulations. The proposed method is based on investigation of the fluorescence spectral behaviour of LRT and DSL in a sodium dodecyl sulphate (SDS) micellar system. In aqueous solution of acetate buffer of pH 4.5, the fluorescence intensities of both LRT and DSL were greatly enhanced (240%) in the presence of SDS. The fluorescence intensity was measured at 438 nm after excitation at 290 nm for both drugs. The fluorescence-concentration plots were rectilinear over the range 0.05-2.0 µg/mL for both LRT and DSL, with lower detection limits of 5.13 × 10(-3) and 6.35 × 10(-3) µg/mL for LRT and DSL, respectively. The method was successfully applied to the analysis of the two drugs in their commercial tablets, capsules and syrups, and the results were in good agreement with those obtained with the official or comparison methods. The proposed method is specific for the determination of LRT in the presence of other co-formulated drugs, such as pseudoephedrine. The application of the proposed method was extended to stability studies of LRT and DSL after exposure to different forced degradation conditions, such as acidic, alkaline and oxidative conditions, according to ICH guidelines.
- Loratadine and montelukast administered in combination produce decongestion in an experimental feline model of nasal congestion. [Journal Article]
- Am J Rhinol Allergy 2009 Nov-Dec; 23(6):e17-22.
Histamine and leukotrienes act to exert numerous local and systemic effects that contribute to the pathophysiology of allergic rhinitis. The aim of these experiments was to evaluate the nasal decongestant effects of loratadine and montelukast alone and in combination in a feline model of nasal congestion. We also studied the decongestant actions of the alpha-agonist adrenergic agonist D-pseudoephedrine with and without desloratadine.Acoustic rhinometry was used to determine nasal cavity dimensions after intranasal compound 48/80. Cats were given D-pseudoephedrine (0.3 mg/kg) alone or in combination with desloratadine (5 mg/kg) 1 hour before nasal provocation with compound 48/80 (1%, 75 microliters) to either the left or right nasal passageway. Using a similar design, the nasal decongestant effects of montelukast (1 mg/kg) and loratadine (10 mg/kg) were studied alone and in combination.The addition of desloratadine to D-pseudoephedrine did not improve decongestant efficacy compared with each drug given individually. In contrast, when montelukast (1 mg/kg) was given in combination with loratadine (10 mg/kg), the decongestant activity was greater than when these drugs were administered separately. Sixty minutes after compound 48/80 provocation the nasal cavity volume ratio (volume ratio of the compound 48/80 treated/untreated nasal passageway) for the control, montelukast alone, loratadine alone, and the montelukast plus loratadine-treated groups were 0.20 +/- 0.03, 0.24 +/- 0.01, 0.28 +/- 0.03, and 0.50 +/- 0.03.Concomitant montelukast plus loratadine produces a greater degree of nasal decongestion compared with montelukast or loratadine alone in an experimental model of nasal congestion.
- Efficacy and safety of desloratadine/pseudoephedrine combination vs its components in seasonal allergic rhinitis. [Comparative Study, Journal Article, Multicenter Study, Randomized Controlled Trial, Research Support, Non-U.S. Gov't]
- J Investig Allergol Clin Immunol 2009; 19(2):117-24.
Antihistamines are first-line therapy for the treatment of seasonal allergic rhinitis (AR); however, an oral decongestant is often added to improve control of nasal congestion.To examine whether a tablet combining the nonsedating antihistamine desloratadine and the decongestant pseudoephedrine was more effective than either drug administered alone in reducing the symptoms of seasonal AR, including nasal congestion.In this multicenter, double-blind study, participants (N = 598) with symptomatic seasonal AR were administered either a combination tablet of desloratadine 2.5 mg/pseudoephedrine 120 mg (DL/PSE) bid, a desloratadine 5.0 mg qd and a placebo tablet, or pseudoephedrine 120 mg bid. Participants assessed their symptom severity twice daily over the 2-week treatment period.The primary variable to assess the effects of the antihistamine component--mean change from baseline in average AM/PM reflective total symptom score (TSS), excluding nasal congestion--was significantly greater (-6.54) for DL/PSE than for desloratadine (-5.09) or pseudoephedrine (-5.07) monotherapy (P < .001 for both). The primary variable to assess the effects of the decongestant component--mean change from baseline in average AM/PM reflective nasal congestion score--was also significantly greater (-0.93) for DL/PSE than for desloratadine (-0.66) or pseudoephedrine (-0.75) (P < .001 vs desloratadine; P = .006 vs pseudoephedrine).This study demonstrated that DL/PSE therapy was more effective in reducing symptoms of seasonal AR, including nasal congestion, than the individual components when administered alone, thus supporting use of this combination in participants with symptomatic seasonal AR and prominent nasal congestion.
- Desloratadine and pseudoephedrine combination therapy as a comprehensive treatment for allergic rhinitis and nasal congestion. [Journal Article, Research Support, Non-U.S. Gov't, Review]
- Expert Opin Drug Metab Toxicol 2009 Jun; 5(6):683-94.
Allergic rhinitis (AR) is rapidly increasing in global prevalence. Symptoms of AR, particularly nasal congestion, can cause quality of life (QoL) impairment. Second-generation antihistamines are a recommended first-line therapy for AR but are not viewed as very effective for the treatment of congestion. Therefore, an antihistamine plus a decongestant, such as the combination of desloratadine and pseudoephedrine, is a convenient and efficacious treatment.To review the clinical evidence on the efficacy and safety of combination desloratadine/pseudoephedrine for the treatment of AR symptoms, particularly nasal congestion.Four large studies found that improvement in nasal congestion is enhanced when patients are treated with combination desloratadine/pseudoephedrine. The combination drug significantly improved mean reflective nasal congestion scores in these studies compared with either component as monotherapy (p <or= .009 for all). These improvements in congestion were observed by day 2. Mean reductions in nasal congestion scores were comparable between the once- and twice-daily dosing regimens of the combination drug.Comprehensive treatment of AR that effectively relieves nasal congestion can also improve patient QoL. Administration of the second-generation antihistamine desloratadine in combination with the decongestant pseudoephedrine may be regarded as an efficacious and convenient option for patients with AR who are particularly troubled by nasal congestion.
- Ebastine in allergic rhinitis and chronic idiopathic urticaria. [Comparative Study, Journal Article, Review]
- Allergy 2008 Dec.:1-20.
Histamine is a key mediator in the development of allergy symptoms, and oral H(1)-antihistamines are among the most widely used treatments for symptomatic relief in conditions such as allergic rhinitis and chronic urticaria. Ebastine is a second-generation antihistamine which has been shown to be an effective treatment for both seasonal and perennial allergic rhinitis. In controlled clinical trials in adult and adolescent patients with allergic rhinitis, ebastine 10 mg once-daily improved symptoms to a significantly greater extent than placebo and to a similar extent as loratadine 10 mg and cetirizine 10 mg (both once-daily), while ebastine 20 mg proved to be more effective than these two comparator antihistamines. In addition, ebastine was significantly more effective than placebo at relieving the symptoms of chronic idiopathic urticaria. Ebastine provides efficacy throughout the 24-h dosing interval with once-daily administration and clinical benefit is seen from the first day of treatment. Small studies have found beneficial effects for ebastine in patients with other disorders, including cold urticaria, dermographic urticaria, atopic asthma, mosquito bites and (in combination with pseudoephedrine) the common cold. In addition to the regular ebastine tablet, a fast-dissolving tablet (FDT) formulation, which disintegrates in the mouth without the aid of a drink, is also available. It has been shown to be bioequivalent to the regular tablet, and to be significantly more effective than desloratadine at reducing histamine-induced cutaneous wheals. A number of patient surveys demonstrated that the majority of individuals who tried the fast-dissolving formulation reported it to be convenient for use, fast-acting and preferred it to their previous antihistamine medication. Perhaps most importantly, a large proportion of patients indicated that they would prefer to use this new formulation in the future. Ebastine has a rapid onset of action and it can be administered once-daily, with or without food. Dose modifications are not needed in elderly patients, or in those with renal or mild to moderate hepatic impairment. Ebastine is generally well-tolerated, and clinical studies showed that at usual therapeutic doses of 10 and 20 mg once-daily, it had no clinically relevant adverse effects on cognitive function and psychomotor performance or on cardiovascular function. In conclusion, ebastine is an effective and generally well-tolerated treatment for allergic rhinitis and chronic idiopathic urticaria. In addition to the regular tablet formulation, ebastine is available as a FDT, providing a treatment option that is particularly convenient for patients.
- Simultaneous determination of desloratadine and pseudoephedrine in human plasma using micro solid-phase extraction tips and aqueous normal-phase liquid chromatography/tandem mass spectrometry. [Evaluation Studies, Journal Article, Validation Studies]
- Rapid Commun Mass Spectrom 2007; 21(18):3145-55.
Cation-exchange micro solid-phase extraction (SPE) tips and aqueous normal-phase (ANP) chromatography coupled with tandem mass spectrometry were explored for the rapid, selective and sensitive quantitation of desloratadine and pseudoephedrine in human plasma. A novel micro-SPE device was evaluated for analyte capacity, extraction efficiency and its ability to maximize recovery of an analyte of interest from bioanalytical matrices by successive replicates of linked extraction steps. Ion suppression using two different methods with micro-SPE tips was negligible when compared to protein precipitation. The use of ANP chromatography eliminated the need for sample reconstitution following extraction and was found to be highly selective. A reliable chromatography system was developed with a short duty cycle of 2 min/sample. The proposed bioanalytical method required 50 microL of plasma for the determination of desloratadine and pseudoephedrine at limits of quantitation of 0.1 and 1.25 ng/mL, respectively. The analytical method was validated in accordance with the FDA guidance on bioanalytical method validation; selectivity, linearity, reproducibility and accuracy were all acceptable.
- Simultaneous determination of loratadine and desloratadine in pharmaceutical preparations using liquid chromatography with a microemulsion as eluent. [Journal Article]
- J Pharm Biomed Anal 2007 Mar 12; 43(4):1236-42.
A rapid HPLC procedure for analytical quality control of pharmaceutical preparations containing the antihistaminic drug substance loratadine and/or its analog desloratadine (which is also an active metabolite of loratadine) was developed using a microemulsion as the eluent. The separation was performed on a column packed with cyanopropyl bonded stationary phase adopting UV detection at 247 nm using a flow rate of 1 ml/min. The optimized microemulsion mobile phase consisted of 0.1M sodium dodecyl sulphate, 1% octanol, 10% n-propanol and 0.3% triethylamine in 0.02 M phosphoric acid, pH 3.0. The developed method was validated in terms of specificity, linearity, lower limit of quantification, lower limit of detection, precision and accuracy. With the proposed method satisfactory resolution between loratadine and desloratadine (resolution factor=3.85). The method requires a minimum of sample handling and is rapid (10 min), and reproducible (R.S.D.<2.0%). The mean recoveries of the analytes in pharmaceutical preparations were in agreement with those obtained from a reference method, as revealed by statistical analysis of the obtained results using the Student's t-test and the variance ratio F-test. Pseudoephedrine, the co-formulated drug substance, did not interference with the assay and was successfully separated using the developed HPLC method.
- Combining desloratadine and pseudoephedrine in the treatment of seasonal allergic rhinitis. [Journal Article]
- Expert Rev Clin Immunol 2006 Jul; 2(4):519-31.
Nonsedating antihistamines are a first-line therapy in the management of allergic rhinitis. They relieve the majority of the histamine-mediated symptoms of the condition, including rhinorrhea, sneezing, and pruritus. The nonsedating antihistamine desloratadine is effective in alleviating the symptoms of both seasonal and perennial allergic rhinitis. It may also have some decongestant properties, and thus help to alleviate nasal congestion. Administering desloratadine in combination with the decongestant pseudoephedrine may offer allergic rhinitis patients with moderate-to-severe nasal congestion the benefits of desloratadine's effectiveness for alleviating histamine-mediated symptoms plus pseudoephedrine's relief from nasal congestion. This drug profile reviews a combination therapy containing desloratadine and pseudoephedrine, approved in the USA for the relief of the symptoms of seasonal allergic rhinitis, including nasal congestion.
- Efficacy and safety of desloratadine/pseudoephedrine tablet, 2.5/120 mg two times a day, versus individual components in the treatment of patients with seasonal allergic rhinitis. [Clinical Trial, Phase III, Journal Article, Multicenter Study, Randomized Controlled Trial]
- Allergy Asthma Proc 2005 Sep-Oct; 26(5):391-6.
Although antihistamines are highly effective in alleviating many symptoms associated with seasonal allergic rhinitis (SAR), relief from nasal congestion is variable. The efficacy of desloratadine, an effective antihistamine, in combination with pseudoephedrine, a potent nasal decongestant, was evaluated to determine whether combination therapy was more effective than individual component therapy in reducing nasal congestion, as well as other SAR symptoms. This multicenter, randomized, double-blind, three-arm study included 650 patients with SAR. For 2 weeks, patients were administered a combination tablet of desloratadine plus pseudoephedrine (desloratadine/pseudoephedrine, 2.5/120 mg) twice per day (b.i.d.), desloratadine (5 mg) once per day, or pseudoephedrine (120 mg) b.i.d. Patients assessed the severity of their SAR symptoms twice daily on symptom diary cards. The primary variable-change from baseline in the reflective A.M./P.M. total symptom score, excluding nasal congestion-was significantly superior (-6.7) compared with desloratadine (-5.4) or pseudoephedrine (-5.3) alone (p < or = 0.001 versus either group). Secondary efficacy variables including total symptom scores (plus congestion), total nasal symptom scores, and total nonnasal symptom scores were significantly reduced after desloratadine/pseudoephedrine therapy compared with the individual components. The most frequently reported adverse events were insomnia, headache, and dry mouth. Desloratadine/pseudoephedrine, 2.5/120 mg b.i.d., therapy was more effective in reducing total symptom scores of SAR, including nasal congestion, than were the individual components. These results support the use of this combination therapy over desloratadine or pseudoephedrine alone.
- Efficacy and safety of an extended-release formulation of desloratadine and pseudoephedrine vs the individual components in the treatment of seasonal allergic rhinitis. [Clinical Trial, Comparative Study, Journal Article, Multicenter Study, Randomized Controlled Trial, Research Support, Non-U.S. Gov't]
- Ann Allergy Asthma Immunol 2005 Mar; 94(3):348-54.
Antihistamine-decongestant combination products generally provide more benefit than individual components for adequately treating patients who have seasonal allergic rhinitis (SAR) with moderate-to-severe nasal congestion.To compare the effectiveness and safety of a 24-hour, extended-release formulation of desloratadine and pseudoephedrine with the individual components in patients who have SAR with moderate-to-severe nasal congestion.Patients with SAR and significant nasal congestion were enrolled in a multicenter, randomized, double-blind, double-dummy study. Patients were randomly assigned for 2 weeks to once-daily treatment with desloratadine-pseudoephedrine, 5/240-mg tablets; desloratadine, 5 mg; or pseudoephedrine, 240 mg. Primary efficacy variables for the antihistamine and decongestant components of desloratadine-pseudoephedrine were morning and evening reflective total symptom score (TSS), excluding nasal congestion, and morning and evening reflective nasal congestion score during the 2-week treatment period, respectively. Secondary variables included morning instantaneous (end-of-interval) TSS (excluding congestion), nasal congestion score, reflective morning and evening individual symptom scores, overall condition of SAR, and therapeutic response.A total of 1121 patients were enrolled in the study, and 1047 patients completed the 2-week study. Desloratadine-pseudoephedrine was significantly more effective than desloratadine or pseudoephedrine monotherapy in reducing morning and evening reflective TSS (excluding nasal congestion) during the entire treatment period. Desloratadine-pseudoephedrine also was significantly more effective in reducing the morning and evening reflective nasal congestion score compared with desloratadine or pseudoephedrine monotherapy. Significant differences were seen between the desloratadine-pseudoephedrine and monotherapy groups for changes in morning instantaneous TSS (excluding nasal congestion) and nasal congestion scores. No unusual or unexpected adverse events were reported.Desloratadine-pseudoephedrine, 5/240-mg once-daily tablets, provided additional benefit over desloratadine, 5 mg, or sustained-release pseudoephedrine, 240 mg, monotherapy in the treatment of patients with SAR and moderate-to-severe nasal congestion.