levocetirizine and Pruritus

Levocetirizine is classified as a nonsedating second-generation antihistamine. This drug is used to treat allergic disorders such as urticaria and pruritus. Thus far, studies have demonstrated an increase in efficacy for refractory urticaria by increasing doses of antihistamines; however, more lines of supportive evidence for these guidelines are required to justify this management strategy. In this study, we found that a double dose of levocetirizine suppressed histamine-induced flare formation more rapidly and sustainably, and wheal and itch more extensively, compared with the conventional dose using both visual and laser Doppler imaging scales in a noninvasive manner. These results suggest that double-dosed levocetirizine treatment suppresses histamine-induced skin symptoms more rapidly, profoundly and sustainably than conventionally dosed levocetirizine treatment.

Topics: Adult; Cetirizine; Cross-Over Studies; Dose-Response Relationship, Drug; Double-Blind Method; Female; Histamine; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Pruritus; Urticaria

The antihistamine effects of olopatadine and levocetirizine, in standard-dose application described in their information (5 mg twice a day for olopatadine; 5 mg once daily for levocetirizine), were examined from 11.5 to 24 h after application. The test was designed in a double-blind, randomized, cross-over, placebo-controlled study of 12 healthy volunteers on histamine-induced flare and wheal response using an iontophoresis technique. The suppressive effect of olopatadine on the wheals induced by a 0.1-mA histamine iontophoresis lasted for 24 h after dosing. Both drugs inhibited flare induced by histamine iontophoresis almost completely until 24 h after the first administration. Suppression of the 0.2-mA-induced wheal response by levocetirizine, taken once daily, decreased with time, although 0.1-mA-induced flare was almost completely suppressed by the drug. Olopatadine completely suppressed even the wheal response induced by a 0.2-mA histamine iontophoresis. Compared with the placebo, the two drugs significantly suppressed the subjective itching assessed by visual analog scale at all intervals. There were no significant differences in subjective drowsiness and objective cognitive function between drug- and placebo-treated subjects. These results demonstrate that olopatadine seems to be more potent than levocetirizine when administrated in a standard dose. In conclusion, mild to moderate urticaria could be controlled by standard application as described in their information. On the other hand, severe urticaria could be managed by a standard application of olopatadine, but levocetirizine may need an additional dose to control severe urticaria.

Topics: Adult; Cetirizine; Cognition; Cross-Over Studies; Dibenzoxepins; Double-Blind Method; Female; Healthy Volunteers; Histamine; Histamine H1 Antagonists, Non-Sedating; Humans; Iontophoresis; Male; Middle Aged; Olopatadine Hydrochloride; Pruritus; Sleep Stages; Young Adult

This randomized, double-blind, placebo-controlled crossover study compared inhibition by one 5 mg dose of levocetirizine with two 60 mg doses of fexofenadine separated by 12 h of histamine-induced wheal and flare responses in 9 Caucasian and 9 Japanese healthy male volunteers. Levocetirizine was more inhibitory than fexofenadine on wheal, flare and pruritus (p < 0.005). Variability, evaluated from the standard deviation of inhibition, ranged from 14% to 23.2% for levocetirizine and 65.4% to 112.4% for fexofenadine. Levocetirizine had a faster onset of action (30-90 min versus 2 h), shorter time to maximum effect (3-4 versus 3-6 h) and longer duration of action (at least 24 h versus ~12 h) than fexofenadine. The plasma levels of levocetirizine rose more quickly, reached higher levels, were more consistent and decreased slower than those of fexofenadine. There were no clinically significant ethnic differences in responsiveness to the drugs.

Topics: Adult; Asian People; Cetirizine; Cross-Over Studies; Dose-Response Relationship, Drug; Double-Blind Method; Germany; Histamine; Histamine H1 Antagonists, Non-Sedating; Humans; Japan; Male; Pruritus; Skin; Terfenadine; Time Factors; Treatment Outcome; Urticaria; White People; Young Adult

Nonsedating H(1)-antihistamines are recommended for the treatment of urticaria by the recent EAACI/GA(2)LEN/EDF guidelines. The aim of this study was to compare the efficacy, after 4 weeks of treatment, with levocetirizine 5 mg and desloratadine 5 mg, both once daily in the morning, in symptomatic chronic idiopathic urticaria (CIU) patients.. This multi-center, randomized, double-blind study involved 886 patients (438 on levocetirizine and 448 on desloratadine). The primary objective was to compare their efficacy on the mean pruritus severity score after 1 week of treatment. Mean pruritus severity score over 4 weeks and pruritus duration score, number and size of wheals, mean CIU composite score (sum of the scores for pruritus severity and numbers of wheals), quality of life, and the patient's and investigator's global satisfaction with treatment, were secondary efficacy measures.. Levocetirizine led to a significantly greater decrease in pruritus severity than desloratadine over the first treatment week; mean pruritus severity scores of 1.02 and 1.18 for levocetirizine and desloratadine, respectively (P < 0.001). The result was similar for the entire 4-week treatment period (P = 0.004). In addition, levocetirizine decreased pruritus duration and the mean CIU composite scores to a significantly greater extent than desloratadine during the first week (P = 0.002 and 0.005, respectively) and over the entire study (P = 0.009 and P < 0.05, respectively). Similarly, levocetirizine increased the patients' global satisfaction after one and 4 weeks (P = 0.012 and 0.021, respectively), compared with desloratadine. Safety and tolerability were similar in both groups.. Levocetirizine 5 mg was significantly more efficacious than desloratadine 5 mg in the treatment of CIU symptoms.

Topics: Cetirizine; Chronic Disease; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Loratadine; Male; Pruritus; Quality of Life; Severity of Illness Index; Urticaria

Levocetirizine, a second generation non-sedating antihistamine that blocks the H(1) histamine receptor, may exhibit immunoregulatory properties that augment its primary pharmacological mechanism. To investigate this possibility, 13 Kuwaiti seasonal allergic rhinitis (SAR) patients were treated with levocetirizine for four weeks in comparison with a 7-member placebo-treated control group, followed by clinical evaluation and flow cytometric analysis of peripheral venous blood for inflammatory cell and lymphocyte subpopulation profiles. Relative to the controls, levocetirizine-treated patients exhibited an expected reduction in early phase allergic symptoms, including sneezing (P<0.001), nasal itching (P<0.01), nasal congestion, and running nose (P<0.001); reduced percentages of eosinophils (P<0.05); and three subpopulations of activated T lymphocytes: CD4+CD29+, CD4+CD212+, and CD4+CD54+ (P<0.05). Levocetirizine treatment also correlated with a significant increase in the percentage of CD4+CD25+ T cells (P<0.001). The ability of levocetirizine to reduce percentage representation of cell phenotypes known to contribute to inflammatory tissue damage (eosinophils, CD4+CD29+, CD4+CD212+, and CD4+CD54+) and expand percentages of CD4+CD25+, which may include protective immunoregulatory (Treg) cells, indicates that the drug has pharmacological potential beyond the immediate effects of H(1) histamine-receptor inhibition. Although the present data does not define a therapeutic mechanism, the results reported here establish important trends that may be used to guide future mechanistic examination of immunoregulatory capacity of H(1) inhibitors.

Topics: Adult; Anti-Inflammatory Agents; Cetirizine; Eosinophils; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Immunophenotyping; Lymphocyte Activation; Male; Pruritus; Rhinitis, Allergic, Seasonal; Sneezing; T-Lymphocyte Subsets; Treatment Outcome

Chronic urticaria is a common skin condition. It is frequently a disabling disease because of the persistence of clinical symptoms, the unpredictable course and its negative influence on the quality of life.. To determine whether levocetirizine is efficacious in the treatment of chronic idiopathic urticaria.. A randomized, double-blind, placebo-controlled study was conducted in 106 patients with a diagnosis of chronic idiopathic urticaria. A 1-week single blind placebo run-in period (baseline) was followed by a 6-week double blind active treatment period. The patients were randomized to receive one of the following treatments once daily: (a) oral levocetirizine 5 mg, or (b) oral placebo. The study ended after another 1-week single blind placebo washout period.. The evaluable population consisted of 100 patients. Levocetirizine administered once daily is effective and well tolerated in the treatment of the symptoms of chronic idiopathic urticaria and in improving the patient's quality of life. Levocetirizine was superior to placebo in reducing the mean total symptoms score as well as individual symptoms, the number of daily episodes and the number of weals, the overall severity of symptoms and the quality of life. The significant beneficial effects of levocetirizine lasted only during the active trial, while at follow-up there was a significant worsening of all the variables evaluated in this study, after the end of the active trial (week 7).. A global assessment indicates that levocetirizine 5 mg once daily is an effective agent in patients with chronic idiopathic urticaria, as its action provides a rapid and satisfactory control of the symptoms and measures of subjective disease, although this is limited to the duration of treatment.

Topics: Adult; Aged; Cetirizine; Chronic Disease; Double-Blind Method; Drug Administration Schedule; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Piperazines; Pruritus; Quality of Life; Severity of Illness Index; Treatment Outcome; Urticaria

People frequently experience whealing and delayed papules from mosquito bites. Various antihistamines have previously been tried for the treatment of this condition. We performed a double-blind, placebo-controlled, cross-over study with levocetirizine 5 mg and matched placebo in 30 adults who were sensitive to mosquito bites. On the third treatment day the subjects received two Aedes aegypti bites on the forearm. The size of the bite lesions and the intensity of pruritus (visual analogue scale) were measured. Bite symptoms could be analysed in 28 subjects at 15 min and in 8 subjects at 24 h. Levocetirizine decreased the size of wheals by 60% (p < 0.001) and accompanying pruritus by 62% (p < 0.001) compared with placebo. The effect of levocetirizine increased in a linear fashion with the size of wheals and was most significant in the subjects with largest bite lesions. Levocetirizine also decreased the size of 24-h bite lesions by 71% (p=0.008) and accompanying pruritus by 56% (p=0.016). These results show that prophylactic levocetirizine 5 mg is an effective treatment for both immediate and delayed mosquito bite symptoms and is especially effective in subjects with large wheals.

Topics: Adult; Aedes; Animals; Cetirizine; Cross-Over Studies; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Hypersensitivity, Delayed; Hypersensitivity, Immediate; Insect Bites and Stings; Male; Middle Aged; Piperazines; Pruritus

Nasal obstruction is the main symptom in patients with persistent allergic rhinitis. Some antihistamines have been demonstrated to be capable of improving this symptom. The aim of this pilot study was to evaluate nasal symptoms, nasal airflow, and decongestent activity in patients with persistent allergic rhinitis, before and after treatment with levocetirizine or placebo.. Forty patients with persistent allergic rhinitis were evaluated, 35 males and 5 females (mean age 23.3 +/- 5.9 years). All of them received levocetirizine (5 mg/daily) or placebo for 4 weeks. The study was double-blind, parallel-group, placebo-controlled, and randomized. Total symptom score (including: nasal itching, sneezing, rhinorrhea, and nasal obstruction) was assessed before and after treatment. Rhinomanometry and decongestion test were performed in all subjects before and after treatment.. Levocetirizine treatment induced: significant symptom relief (p<0.001), improved nasal airflow (p<0.001), reduction of reversibility percentage (p<0.05), and increase of total airflow after decongestion test (p<0.03). Placebo did not improve nasal symptoms and airflow.. This pilot study demonstrates the effectiveness of levocetirizine in: i) relieving nasal symptoms, including obstruction, ii) improving nasal airflow, and iii) exerting decongestant activity. Thus, these findings are the first evidence of the impact on airflow and the decongestant activity exerted by levocetirizine in persistent allergic rhinitis.

Topics: Adolescent; Adult; Cetirizine; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Naphazoline; Nasal Obstruction; Pilot Projects; Piperazines; Pruritus; Rhinitis, Allergic, Perennial; Rhinomanometry; Skin Tests

Itch is the most bothersome symptom in psoriasis, often leading to impaired quality of life. Treatment of psoriasis-induced itch is frequently unsatisfactory as the various therapies employed have a delayed onset of effect. Histamine-1 receptor (H1) antihistamines are not recommended in treatment guidelines as histamine is not considered a key mediator in psoriasis. However, patients using H1 antihistamines frequently report benefits in questionnaire-based studies. To address these contradictions, we examined the short-term effects of levocetirizine, a nonsedating H1 antihistamine, on psoriasis-related itch and itch-related quality of life. In this pilot study, patients with psoriasis-related itch received levocetirizine 5-10 mg daily as a concomitant treatment for 5 days. Change of itch intensity as measured by hourly itch ratings and the change of itch-related quality of life were measured at different time points. A total of 29 of 30 patients (96%) reported a decline in itch within 5 days. Mean itch reduction was 23% after Day 1 (p = .005), 40% after Day 3 (p < .001), and 41% after Day 5 (p < .001). Furthermore, itch-related quality of life also significantly improved after 5 days (p < .001). Only 2 of 30 patients (6.7%) reported mild sleepiness. Levocetirizine 5-10 mg daily as an add-on therapy seems to be an effective treatment to improve itch and itch-related quality of life within only a few days.

Topics: Adult; Cetirizine; Dose-Response Relationship, Drug; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Pilot Projects; Pruritus; Psoriasis; Quality of Life; Time Factors; Treatment Outcome

Topics: Adult; Cetirizine; Depression; Histamine H1 Antagonists, Non-Sedating; Humans; Middle Aged; Pruritus; Psoriasis; Quality of Life; Stress, Psychological; Surveys and Questionnaires

Levocetirizine is a second-generation nonsedative antihistaminic agent that has been demonstrated to be safe and effective for treating allergic disease. There was only one case report of levocetirizine-induced liver toxicity, but a liver biopsy was not performed. In this article, we present the first case of levocetirizine-induced liver injury with histologic findings. A 48-year-old man was hospitalized with jaundice and generalized pruritus that had developed after 2 months of therapy with levocetirizine for prurigo nodularis. Laboratory findings revealed acute hepatitis with cholestasis. A liver biopsy demonstrated portal inflammation and hepatitis with apoptotic hepatocytes. The patient fully recovered 3 weeks after withdrawing levocetirizine. Although levocetirizine is safe and effective, physicians should be aware of its potential hepatotoxicity.

Topics: Cetirizine; Chemical and Drug Induced Liver Injury; Histamine H1 Antagonists, Non-Sedating; Humans; Hypersensitivity; Jaundice; Liver; Male; Middle Aged; Pruritus

Anakinra is a recombinant form of interleukin-1 receptor antagonist. It is the drug of choice for Schnitzler syndrome and cryopyrin-associated periodic syndromes. It has also recently been demonstrated to have activity in the treatment of the non-Langerhans cell histiocytosis known as Erdheim-Chester disease.. To describe the activity of anakinra in a patient with co-existing lichen planus and Erdheim-Chester disease.. A 43-year-old woman with progressive Erdheim-Chester disease presented for management of her night sweats and chills, systemic skeletal bone pain, and neurologic (diabetes insipidus) manifestations. She also had widespread cutaneous lichen planus. Anakinra, 100 mg subcutaneously daily, was initiated for the treatment of her Erdheim-Chester disease.. Within 2 days of starting anakinra, there was prompt resolution of her Erdheim-Chester disease-related symptoms. Subsequently, her bone pain resolved and her diabetes insipidus improved. Also, the lichen planus-associated pruritus rapidly ceased and most of the skin lesions improved.. Our experience confirms the efficacy of anakinra for the treatment of Erdheim-Chester disease. The concomitant improvement of her lichen planus on anakinra suggests that this agent warrants additional study in this disorder.

Topics: Adult; Cetirizine; Deamino Arginine Vasopressin; Diabetes Insipidus; Drug Eruptions; Erdheim-Chester Disease; Female; Human Growth Hormone; Humans; Interleukin 1 Receptor Antagonist Protein; Lichen Planus; Progesterone; Pruritus; Radionuclide Imaging; Thyroiditis, Autoimmune; Thyroxine; Vitamin D; Vitamin D Deficiency