levocetirizine and montelukast

Allergic rhinitis is the most prevalent of the atopic disorders, affecting 25% to 35% of persons, depending on the population studied. Considered by non-sufferers to be a trivial disease, allergic rhinitis delivers a significant personal impact on quality of life. Antihistamines have been successfully used for years in the treatment of seasonal/persistent allergic rhinitis. The new generation antihistaminics are all safe, with negligible sedative effects, excellent tolerability and have no influence on cardiac parameters. Montelukast when used as monotherapy is efficacious and improves quality of life. Combination therapy (montelukast plus levocetirizine) is a more effective strategy than monotherapy in the treatment of persistent allergic rhinitis.

Topics: Acetates; Cetirizine; Cyclopropanes; Drug Therapy, Combination; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Quality of Life; Quinolines; Randomized Controlled Trials as Topic; Rhinitis, Allergic, Perennial; Sulfides

Asthma patients often have co-existing symptoms of allergic rhinitis and are often prescribed with both asthma and rhinitis treatments such as montelukast and levocetirizine. The objective of this study was to compare the pharmacokinetic profiles of a montelukast/levocetirizine fixed-dose combination chewable tablet with individual administration of montelukast and levocetirizine in healthy subjects.. A randomized, open-label, single-dose crossover study was conducted in healthy male subjects. One of the following treatments was administered in each period: co-administration of 1 chewable tablet of montelukast 5 mg and 1 tablet of levocetirizine 5 mg or administration of 1 chewable tablet of montelukast/levocetirizine 5/5 mg fixed-dose combination. Serial blood samples were collected up to 48 hours post dose. Plasma drug concentrations were measured by liquid chromatography/tandem mass spectrometry. Pharmacokinetic parameters, including maximum plasma concentration (C. A total of 22 subjects were included in pharmacokinetic analysis. The GLSM ratios and 90% CIs of C. The pharmacokinetic parameters of montelukast and levocetirizine when administered as separate tablets or as a fixed-dose combination were compared, and the parameters met the pharmacokinetic equivalence criteria. (ClinicalTrials.gov Identifier: NCT03371849).

Topics: Acetates; Administration, Oral; Area Under Curve; Cetirizine; Cross-Over Studies; Cyclopropanes; Drug Combinations; Healthy Volunteers; Humans; Male; Quinolines; Republic of Korea; Sulfides; Tablets; Therapeutic Equivalency

The aim of this study was to evaluate the efficacy and safety of a fixed-dose combination of montelukast and levocetirizine in patients with perennial allergic rhinitis with mild to moderate asthma compared with the efficacy and safety of montelukast alone.. The fixed-dose combination of montelukast and levocetirizine was effective and safe in treating perennial allergic rhinitis in patients with asthma compared with montelukast alone. ClinicalTrials.gov identifier: NCT02552667.

Topics: Acetates; Adult; Anti-Allergic Agents; Anti-Asthmatic Agents; Asthma; Cetirizine; Cyclopropanes; Double-Blind Method; Drug Therapy, Combination; Female; Humans; Male; Quinolines; Republic of Korea; Respiratory Function Tests; Rhinitis, Allergic, Perennial; Sulfides; Treatment Outcome

A novel fixed-dose combination (FDC) capsule of 10/5 mg of montelukast/levocetirizine may lead to better compliance than two separate tablets taken together. The aim of this study was to evaluate the pharmacokinetics (PK) and tolerability of an FDC of montelukast and levocetirizine compared to separate tablets.. A randomized, open-label, single-dose, two-sequence, two-period, crossover study was conducted with healthy male subjects. In each period, either an FDC or separate tablets were administered orally, and serial blood samples were collected for PK analysis for up to 34 hours after dosing. PK parameters were calculated using noncompartmental methods. The 90% confidence intervals (CIs) of the geometric mean ratios (GMRs) of the maximum plasma concentration (Cmax) and the area under the curve to the last measurable concentration (AUClast) for the two interventions were estimated. Tolerability assessments were performed for all the subjects who received the drug at least once.. The PK profiles of the two interventions were comparable. For montelukast, the GMRs and 90% CIs for the Cmax and AUClast were 0.9800 (0.8903 - 1.0787) and 1.0706 (0.9968 - 1.1498), respectively. The corresponding values for levocetirizine were 0.9195 (0.8660 - 0.9763) and 1.0375 (1.0123 - 1.0634), respectively. Both interventions were well tolerated.. The PK and tolerability profiles of montelukast and levocetirizine after a single oral administration were comparable between the FDC and separate tablets. For patients with allergic rhinitis who require a combination treatment, the FDC of montelukast and levocetirizine will be a convenient therapeutic option.
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Topics: Acetates; Administration, Oral; Adult; Area Under Curve; Biological Availability; Cetirizine; Cross-Over Studies; Cyclopropanes; Drug Compounding; Half-Life; Healthy Volunteers; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Male; Metabolic Clearance Rate; Middle Aged; Quinolines; Republic of Korea; Sulfides; Tablets; Young Adult

This study demonstrated that treatment with montelukast in combination with levocetirizine may have a beneficial effect on clinical improvement of middle ear fluid in children with otitis media with effusion (OME).. To evaluate the effect of the combination of montelukast and levocetirizine on shortening the duration of effusion in successfully treated OME in children.. This was a randomized, prospective, double-blind, placebo-controlled trial. The study group consisted of 120 children (age range 2-6 years), who were diagnosed with OME of at least 2 months duration. The children were randomized into one of four groups. The treatment packs containing montelukast 4 mg (tablet) and/or levocetirizine 2.5 mg/5 ml as the active drug or placebo were prepared, numbered, and distributed by the second author.. The amelioration of bilateral otoscopic sign scores in the combination therapy group was statistically significantly greater than in all the other groups (p < 0.05). Improvement in bilateral tympanometric findings in the combination therapy group and montelukast group was greater than in the other groups. However, this difference was not statistically significant (p > 0.05). When we compared the difference between otoscopic sign scores before and after treatment we found that it was statistically significant in every group (p > 0.05). However, the significant improvement in tympanometric findings occurred in all groups except the levocetirizine group (p > 0.05).

Topics: Acetates; Administration, Oral; Cetirizine; Child; Child, Preschool; Cyclopropanes; Dose-Response Relationship, Drug; Double-Blind Method; Drug Therapy, Combination; Follow-Up Studies; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Male; Otitis Media with Effusion; Otoscopy; Prospective Studies; Quinolines; Sulfides; Treatment Outcome

To date, no adequate data are available on direct comparison of the efficacy of levocetirizine, a recently approved histamine1-antihistamine, with that of a leukotriene antagonist in the treatment of seasonal allergic rhinitis (SAR) symptoms.. To compare the efficacy of therapeutic doses of 5 mg of levocetirizine and 10 mg of montelukast in ragweed sensitized patients.. A randomized, double-blind, placebo-controlled, parallel-group study was conducted between July and October 2006. Symptomatic patients with SAR were exposed to ragweed pollen under controlled conditions in an environmental exposure chamber for 4 to 5 hours after treatment with 5 mg of levocetirizine, 10 mg of montelukast, or matched placebo on 2 consecutive days. The mean change from baseline in pollen-induced rhinitis symptoms, expressed as a major symptoms complex (MSC) score (sum of scores for rhinorrhea, itchy nose, sniffles, nose blows, sneezes, and watery eyes), in period 1 (first 5 hours after first drug intake) was the primary efficacy outcome.. A total of 611 patients were screened, of whom 403 were randomized to receive treatment (102 placebo, 152 levocetirizine, and 149 montelukast). The MSC score in period 1 was progressively decreased to a significantly greater extent in the levocetirizine group compared with the montelukast and placebo groups (adjusted mean differences, -2.18 [95% confidence interval, -3.35 to -1.01; P < .001] and -2.22 [95% confidence interval, -3.51 to -0.92; P < .001] for levocetirizine vs montelukast and vs placebo, respectively). The effect of 10 mg of montelukast was not significantly different compared with placebo. Levocetirizine also achieved a significantly faster onset of action within 2.5 hours of administration. Both products were well tolerated.. This study in an environmental exposure chamber confirms the therapeutic efficacy of 5 mg of levocetirizine in improving symptoms of SAR, which was superior to 10 mg of montelukast.

Topics: Abdominal Pain; Acetates; Adolescent; Adult; Aged; Ambrosia; Cetirizine; Cyclopropanes; Double-Blind Method; Exanthema; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Male; Middle Aged; Patient Satisfaction; Quinolines; Rhinitis, Allergic, Seasonal; Sulfides; Time Factors; Treatment Outcome

Persistent allergic rhinitis often impairs quality of life.. We assessed the extent to which treating persistent allergic rhinitis with montelukast, desloratadine, and levocetirizine alone or in combination improved quality of life.. A 32-week randomized, double-blind, placebo-controlled, crossover study was performed in 2 arms: 20 patients received montelukast 10 mg/d and/or desloratadine 5 mg/d or placebo; 20 patients received montelukast 10 mg/d and/or levocetirizine 5 mg/d or placebo. The treatment periods were separated by 2-week washout periods. Quality of life was assessed on the day before starting treatment and on the last day of each treatment period using the Rhinoconjunctivitis Quality of Life Questionnaire. Sleep problems were also assessed.. In the desloratadine plus montelukast arm, the mean (SEM) quality of life score before treatment was 3.1 (0.41). After placebo, this score was 2.16 (0.43), after desloratadine it was 1.79 (0.38), after montelukast it was 1.48 (0.37), and after montelukast plus desloratadine it was 1.59 (0.37). In the montelukast plus levocetirizine arm, the mean quality of life score before treatment was 2.58 (0.49). After placebo it was 1.78 (0.46), after levocetirizine it was 1.38 (0.42), after montelukast it was 1.36 (0.37), and after montelukast plus levocetirizine it was 1.26 (0.39).. Placebo, montelukast, desloratadine and levocetirizine significantly improved quality of life. Combining montelukast with either levocetirizine or desloratadine gave additional benefits in comparison to each agent alone and could be considered for patients whose quality of life is impaired by persistent allergic rhinitis.

Topics: Acetates; Adolescent; Adult; Aged; Cetirizine; Chronic Disease; Cross-Over Studies; Cyclopropanes; Double-Blind Method; Drug Interactions; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Loratadine; Male; Middle Aged; Quality of Life; Quinolines; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Sulfides; Treatment Outcome

Montelukast sodium is approved as a treatment for intermittent and persistent allergic rhinitis (AR), but it has not been evaluated as combined therapy with antihistamines for persistent AR.. To investigate the effects of 6 weeks of treatment of persistent AR with desloratadine, levocetirizine, or montelukast alone or in combination.. A randomized, double-blind, placebo-controlled crossover study was performed. Patients were assigned to 2 arms: 20 received montelukast, 10 mg/d, desloratadine, 5 mg/d, or both or placebo and 20 received montelukast, levocetirizine, or both, 5 mg/d, or placebo. The treatment periods were separated by 2-week washout periods. Symptom scoring, skin prick tests, spirometry, rhinometry, and nasal lavage were performed the day before and the last days of the treatment periods. Eosinophil cationic protein levels were evaluated by means of nasal lavage.. The mean +/- SD total baseline nasal symptom score was 7.7 +/- 0.49 before treatment, 3.74 +/- 0.54 after desloratadine use, 3.6 +/- 0.48 after montelukast use, and 3.04 +/- 0.4 after montelukast-desloratadine use. The mean +/- SD baseline nasal symptom score was 7.95 +/- 0.68 before treatment, 3.02 +/- 0.64 after levocetirizine use, 3.44 +/- 0.55 after montelukast use, and 2.14 +/- 0.39 after montelukast-levocetirizine use. The greatest improvement in nasal symptoms occurred after combination treatment. Decreases in the level of eosinophil cationic protein were greater after the combined use of montelukast and antihistamine than after each agent given alone.. For persistent AR, the combination of montelukast and either desloratadine or levocetirizine is more effective than monotherapy with these agents.

Topics: Acetates; Adolescent; Adult; Aged; Anti-Asthmatic Agents; Cetirizine; Cross-Over Studies; Cyclopropanes; Double-Blind Method; Drug Therapy, Combination; Eosinophil Cationic Protein; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Male; Middle Aged; Nasal Lavage Fluid; Piperazines; Quinolines; Rhinitis, Allergic, Perennial; Rhinometry, Acoustic; Sulfides; Treatment Outcome

Levocetirizine, a third-generation antihistamine, and montelukast, a leukotriene receptor antagonist, exhibit remarkable synergistic anti-inflammatory activity across a spectrum of signaling proteins, cell adhesion molecules, and leukocytes. By targeting cellular protein activity, they are uniquely positioned to treat the symptoms of COVID-19. Clinical data to date with an associated six-month follow-up, suggests the combination therapy may prevent the progression of the disease from mild to moderate to severe, as well as prevent/treat many of the aspects of 'Long COVID,' thereby cost effectively reducing both morbidity and mortality. To investigate patient outcomes, 53 consecutive COVID-19 test (+) cases (ages 3-90) from a well-established, single-center practice in Boston, Massachusetts, between March - November 2020, were treated with levocetirizine and montelukast in addition to then existing protocols [2]. The data set was retrospectively reviewed. Thirty-four cases were considered mild (64%), 17 moderate (32%), and 2 (4%) severe. Several patients presented with significant comorbidities (obesity: n = 22, 41%; diabetes: n = 10, 19%; hypertension: n = 24, 45%). Among the cohort there were no exclusions, no intubations, and no deaths. The pilot study in Massachusetts encompassed the first COVID-19 wave which peaked on April 23, 2020 as well as the ascending portion of the second wave in the fall. During this period the average weekly COVID-19 case mortality rate (confirmed deaths/confirmed cases) varied considerably between 1 and 7.5% [37]. FDA has approved a multicenter, randomized, placebo-controlled, Phase 2 clinical trial design, replete with electronic diaries and laboratory metrics to explore scientific questions not addressed herein.

Topics: Acetates; Adolescent; Adult; Aged; Aged, 80 and over; Cetirizine; Child; Child, Preschool; COVID-19 Drug Treatment; Cyclopropanes; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Male; Middle Aged; Quinolines; Retrospective Studies; SARS-CoV-2; Sulfides; Treatment Outcome; Young Adult

Allergic rhinitis and asthma share a common inflammatory mechanism and are closely related, recognized as "one airway disease." Thus, the guidelines recommend allergic rhinitis and asthma be treated together, and leukotriene antagonists and antihistamines have been administered simultaneously; however, there are few reports of the use of combination drugs so far.. The aim of the study was to evaluate the treatment effects and adverse events of Monterizine® (a combination of montelukast and levocetirizine); a total of 2,254 patients with perennial allergic rhinitis and asthma were prospectively enrolled from 60 hospitals nationwide in Korea. They were followed up for 3 (Period 1) or 6 months (Period 2). Total nasal symptom score (TNSS), satisfaction, and safety data were collected and compared to baseline.. TNSS scores were analyzed for 2,254 subjects. At Period 1 (n = 2,024) and 2 (n = 1,861), the scores decreased significantly from baseline (-1.20 ± 2.49 and -1.63 ± 2.78, p < 0.001). The mean quality of life (QoL) was significantly improved at Period 1 and 2 relative to baseline (-3.75 ± 6.58, -4.83 ± 7.11, both p < 0.0001). There were no serious adverse drug reactions, but there were some minor reactions including nasopharyngitis (2.92%), rhinitis (0.37%), and somnolence (0.34%).. TNSS score and QoL were significantly improved by 3-6 months' treatment with Monterizine without significant adverse reactions. These results indicate that Monterizine, as a combination drug, is effective and safe for improving nasal symptoms and quality of life in patients with allergic rhinitis who also have asthma.

Topics: Acetates; Asthma; Cyclopropanes; Drug Combinations; Humans; Quality of Life; Quinolines; Rhinitis, Allergic; Treatment Outcome

It has been hypothesised that antiallergic medications (AAMs) like montelukast and levocetirizine both the two bitter chloro compounds could be repurposed either alone or combinedly as an antiviral against SARS-CoV-2, like chloroquine/hydroxychloroquine (CQ/HCQ), another two bitter chloro compounds. Both AAMs and CQ/HCQ are bitter tasted chloro compounds. Depending on their these two similar physical properties and the safety and efficacy of AAMs by controlling over post viral episodes as comparing with viral inhibitory activities including SARS-CoV-2 by CQ/HCQ, a reposition of AAMs either alone/combinedly could be rationalised as an antiviral approach to nCoV.

Topics: Acetates; Anti-Asthmatic Agents; Antiviral Agents; Cetirizine; Clinical Trials as Topic; COVID-19 Drug Treatment; Cyclopropanes; Drug Repositioning; Histamine H1 Antagonists, Non-Sedating; Humans; Hypersensitivity; Models, Theoretical; Patient Safety; Quinolines; Sulfides; Taste

We report the history of a 15-year old patient with a hypermobile Ehlers-Danlos syndrome (hEDS) (his mother, his two brothers and his sister have the same phenotype as him). He suffers mainly from a severe mast cell activation syndrome (MCAS) with an overreaction of the skin to any kind of contact (water of the shower, clothes, bed sheets) but he has also fatigue, headaches, and rash. This impressive rash is exacerbated after the shower and he has the urge to rest («shower's sign»). We describe the MCAS and its easy, fast and very effective medication management, without any significant side effects as well as its frequent association with the hEDS. We finally introduce the original term of «MASED» to this MCAS, associated, linked or entangled to hEDS.. Nous présentons le cas d’un jeune patient âgé de 15 ans atteint d’un syndrome d’Ehlers-Danlos (SED) de type hypermobile (sa mère, ses deux frères et sa soeur présentent le même phénotype que lui). Il présente principalement un syndrome d’activation mastocytaire (SAMA) sévère avec une atteinte démesurée au niveau de la peau exposée au simple contact (avec l’eau, les draps, les vêtements), mais également de la fatigue, des céphalées ainsi que des éruptions qui sont exacerbées après la douche avec l’envie impérieuse de se reposer (le «signe de la douche»). Nous décrivons le SAMA, sa prise en charge médicamenteuse simple, rapide et efficace et dépourvue d’effets secondaires notables ainsi que son association fréquente au SED. Nous introduisons finalement le terme original de «SAMED» à ce SAMA associé, lié ou intriqué au SED.

Topics: Acetates; Adolescent; Antioxidants; Ascorbic Acid; Cetirizine; Cyclopropanes; Ehlers-Danlos Syndrome; Histamine H1 Antagonists, Non-Sedating; Histamine H2 Antagonists; Humans; Male; Mastocytosis; Quinolines; Ranitidine; Sulfides

Allergic rhinitis (AR) affects a large percentage of paediatric patients. With the wide array of available agents, it has become a challenge to choose the most appropriate treatment for patients. Second-generation antihistamines have become increasingly popular because of their comparable efficacy and lower incidence of adverse effects relative to their first-generation counterparts, and the safety and efficacy of this drug class are established in the adult population. Data on the use of the second-generation antihistamines oral cetirizine, levocetirizine, loratadine, desloratadine and fexofenadine, and the leukotriene receptor antagonist montelukast as well as azelastine nasal spray in infants and children are evaluated in this review. These agents have been found to be relatively safe and effective in reducing symptoms associated with AR in children. Alternative dosage forms such as liquids or oral disintegrating tablets are available for most agents, allowing ease of administration to most young children and infants; however, limited data are available regarding use in infants for most agents, except desloratadine, cetirizine and montelukast. Unlike their predecessors, such as astemizole and terfenadine, the newer second-generation antihistamines and montelukast appear to be well tolerated, with absence of cardiotoxicities. Comparative studies are limited to cetirizine versus ketotifen, oxatomide and/or montelukast. Although second-generation antihistamines and montelukast are deemed relatively safe for use in paediatric patients, there are some noteworthy drug interactions to consider when selecting an agent. Given the wide variety of available agents for treatment of AR in paediatric patients, the safety and efficacy data available for specific age groups, type of AR, dosage form availability and cost should be considered when selecting treatment for AR in infants and children.

Topics: Acetates; Administration, Oral; Adult; Anti-Allergic Agents; Anti-Asthmatic Agents; Astemizole; Cetirizine; Child; Cyclopropanes; Drug Administration Schedule; Drug Interactions; Histamine H1 Antagonists, Non-Sedating; Humans; Ketotifen; Leukotriene Antagonists; Loratadine; Piperazines; Quinolines; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Safety; Sulfides; Tablets; Terfenadine; Treatment Outcome

Allergic rhinitis is the most common allergic disease worldwide and affects about 18% to 40% of the general population. Anti-allergic medicines (eg, some antihistamines) can cause adverse events such as somnolence and can have an additional negative impact on quality of life. Combining montelukast with levocetirizine gives additional benefits in comparison with either drug alone and could be considered for patients whose quality of life is impaired by persistent allergic rhinitis. Montelukast sodium is alkaline, stable and levocetirizine dihydrochloride is acid stable, when we prepare a matrix tablet, both the drugs would be in contact and make it unstable during the shelf life of the formulation. Hence it is recommended to prepare bilayer tablet, as it improves and increases the stability of both the drugs in combination. Bilayer tablet of montelukast with levocetirizine is more stable with respect to stability studies, in comparison to matrix tablet.

Topics: Acetates; Cetirizine; Cyclopropanes; Drug Combinations; Histamine H1 Antagonists, Non-Sedating; Humans; Leukotriene Antagonists; Quality of Life; Quinolines; Rhinitis, Allergic, Perennial; Sulfides; Tablets; Treatment Outcome