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Levocetirizine 5

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Last Updated: 27 September 2020

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General | Latest Info

The daily recommended dose is 5 mg. Adjustment of dose is recommended in elderly patients with moderate to severe Renal impairment. Dosing intervals must be individualise according to Renal function. Refer to the following table and adjust dose as indicated. To use this dosing table, estimate of patient's creatinine clearance in ml / min is needed. CLcr may be estimated from serum creatinine determination using the following formula: in paediatric patients suffering from Renal impairment, dose will have to be adjusted on an individual basis taking into account Renal clearance of patient and his body weight. There is no specific data for children with Renal impairment. No dose adjustment is needed in patients with solely hepatic impairment. In patients with hepatic impairment and Renal impairment, adjustment of dose is recommend. The daily recommended dose is 5 mg. For children aged 2 to 6 years, no adjusted dosage is possible with film - coat tablet formulation. It is recommended to use paediatric formulation of Levocetirizine. Film - coated tablets must be taken orally, swallowed whole with liquid and may be taken with or without food. It is recommended to take daily dose in one single intake. Intermittent allergic rhinitis has to be treated according to the disease and its history; it can be stopped once symptoms have disappeared and can be restart again when symptoms reappear. In case of persistent allergic rhinitis, continuous therapy can be proposed to patients during period of exposure to allergens. There is clinical experience with use of Levocetirizine for treatment periods of at least 6 months. In chronic urticaria and chronic allergic rhinitis, there is clinical experience of use of cetirizine for up to one year. Precaution is recommended with concurrent intake of alcohol. Caution should be taken in patients with predisposing factors of urinary retention, as Levocetirizine may increase the risk of urinary retention. Caution should be taken in patients with epilepsy and patients at risk of convulsion as Levocetirizine may cause seizure aggravation. Response to allergy skin tests is inhibited by antihistamines and a wash - out period is required before performing them. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose - galactose malabsorption should not take this medicine. Pruritus may occur when Levocetirizine is stopped even if those symptoms were not present before treatment initiation. Symptoms may resolve spontaneously. In some cases, symptoms may be intense and may require treatment to be restart. Symptoms should resolve when treatment is restart. Use of film - coat tablet formulation is not recommended in children aged less than 6 years since this formulation does not allow for appropriate dose adaptation. It is recommended to use paediatric formulation of Levocetirizine. No interaction studies have been performed with Levocetirizine; studies with racemate compound cetirizine demonstrate that there were no clinically relevant adverse interactions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Interactions

Drug interactions may change how your medications work or increase your risk of serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use and share it with your doctor and pharmacist. Do not start, stop, or change dosage of any medicines without your doctor's approval. Tell your doctor or pharmacist if you are taking other products that cause drowsiness, such as opioid pain or cough relievers, alcohol, marijuana, drugs for sleep or anxiety, muscle relaxants, or other antihistamines. Check labels on all your medicines because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely. Do not use any other antihistamines applied to the skin because increased side effects may occur. Levocetirizine is very similar to hydroxyzine and cetirizine. Do not use these medications while using levocetirizine. This medication may interfere with certain laboratory tests, possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Drug Class: Antihistamines, 2nd Generation

H 1 antihistamines act as inverse agonists that combine with and stabilize inactive conformation of H 1 receptor, shifting equilibrium toward an inactive state. H 1 receptor polymorphisms have been describe, although it is not yet clear how they influence clinical response to H 1 antihistamines. Human H 1 receptors have approximately 45% homology with muscarinic receptors. H 1 antihistamines down - regulate allergic inflammation through H 1 receptor, either directly or indirectly through nuclear factor - B, ubiquitous transcription factor, through which they down - regulate antigen presentation, expression of proinflammatory cytokines and cell adhesion molecules, and chemotaxis. In addition, through their effects on calcium ion channel activity, H 1 antihistamines decrease mediator release; however, this effect is only seen at high H 1 - antihistamine concentrations. Traditionally, H 1 antihistamines have been classified into 6 chemical groups: alkylamines, ethanolamines, ethylenediamines, phenothiazines, piperazines, and piperidines. Currently, most commonly used classification system is the functional one, in which H 1 antihistamines are classified as either first - generation medications that readily cross the bloodbrain barrier and potentially sedate and impair cognitive and psychomotor function, or second - generation drugs that cross the blood - brain barrier to minimal extent and are relatively nonsedating and nonimpairing. H 1 antihistamines, formerly know as H 1 receptor antagonists or H 1 receptor blockers, are among the most commonly used medications in the world, not only for prevention and treatment of symptoms of allergic rhinitis, allergic conjunctivitis, and urticaria, in which there is good evidence for their efficacy, but also for variety of other allergic and nonallergic diseases, in which there is No satisfactory evidence for their efficacy. More than 40 H 1 antihistamines are available worldwide. Health care professionals and consumers generally assume that all H 1 antihistamines approved for use are proven to be efficacious and safe. This is an incorrect assumption with regard to first - generation medications in this class, most of which were introduced decades before clinical pharmacology studies and randomized controlled trials of medication efficacy and safety were required by regulatory agencies. In contrast, second - generation H 1 antihistamines, particularly cetirizine, desloratadine, fexofenadine, levocetirizine, and loratadine, have been systematically and thoroughly investigated in clinical pharmacology studies and in randomized placebo - control trials in allergic rhinoconjunctivitis and chronic urticaria. In this review, we compare clinical pharmacology, efficacy, and safety of first - generation H 1 antihistamines with those of second - generation H 1 antihistamines.


Table 2

* Acrivastine is related to tripolidine. Cetirizine is a metabolite of hydroxyzine, levocetirizine is an enantiomer of cetirizine, desloratadine is a metabolite of loratadine, and fexofenadine is a metabolite of terfenadine. * In United States, these H 1 antihistamines are not yet approve, have never been approve, or have had approval withdrawn. H 1 antihistamines azelastine, emedastine, epinastine, ketotifen, levocabastine, and olopatadine are available in ophthalmic formulations; and azelastine, dimethindene, levocabastine, and olopatadine are available in intranasal formulations. In some countries, azelastine, dimethindene, ketotifen, and olopatadine are also available in oral formulations. Doxepin has H 1 and H 2 antihistamine activities and is also classified as a tricyclic antidepressant.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Precautions

It is very important that your doctor check your or your child's progress to make sure this medicine is working properly. Urine tests may be needed to check for unwanted effects. If your symptoms do not improve within a few days or if they become worse, check with your doctor. This medicine may cause incomplete emptying of the bladder. Check with your doctor right away if you have a decrease in the frequency of urination or urine volume, difficulty in passing urine, or painful urination. This medicine may make you tired or drowsy. Do not drive or do anything else that could be dangerous until you know how this medicine affects you. Check with your doctor before using this medicine with alcohol or other medicines that affect the central nervous system. Use of alcohol or other medicines that affect CNS with levocetirizine may worsen side effects of this medicine, such as dizziness, poor concentration, drowsiness, unusual dreams, and trouble with sleeping. Some examples of medicines that affect CNS are antihistamines or medicine for allergies or colds, sedatives, tranquilizers, or sleeping medicines, medicine for depression, medicine for anxiety, prescription pain medicine or narcotics, medicine for attention deficit and hyperactivity disorder, medicine for seizures or barbiturates, muscle relaxants, or anesthetics, including some dental anesthetics. Do not take other medicines unless they have been discussed with your doctor. This includes prescription or non - prescription medicines and herbal or vitamin supplements. Copyright 2020 IBM Watson Health. All rights reserve. Information is for the end user's use only and may not be sell, redistributed or otherwise used for commercial purposes.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Side Effects

Get emergency medical help if you have signs of allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using levocetirizine and call your doctor at once if you have: worsening allergy or urticaria symptoms; painful or difficult urination; little or no urination; light - head feeling, like you might pass out; fever; or signs of ear infection - ear pain or full feeling, trouble hearing, drainage from your ear, fussiness in child. Drowsiness, tiredness; sinus pain; ear infection; cough; fever; nosebleed; vomiting, diarrhea, constipation; dry mouth; or weight gain. This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1 - 800 - FDA - 1088.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Anti-inflammatory effects - In vitro

There is considerable interest in the effect of anti - inflammatory drugs on the pro - inflammatory process responsible for manifestations of allergic disease. Anti - inflammatory effects independent of H1 - receptor blockade have been described for the majority of anti - histamines while the parent compound of Levocetirizine, cetirizine has extensive well documented anti - inflammatory properties both in vivo and in vitro. A number of recent in vitro studies have been conducted to assess whether Levocetirizine has similar properties. Levocetirizine inhibits eotaxin - induced eosinophil transendothelial migration through monolayers of human dermal or lung microvascular endothelial cells in vitro at concentrations equal to or lower than those achieved in clinical setting. Physiologically - Relevant concentrations of Levocetirizine also inhibit both resting and GM - CSF - stimulate eosinophil adhesion to vascular cell adhesion molecule - 1 under flow conditions in an in vitro model of post - capillary venules. Real time imaging reveal that the effect of Levocetirizine on post - adhesion behaviour contribute to its inhibitory action on eosinophil adhesion to rhVCAM - 1. Other studies have also demonstrated in vitro anti - inflammatory effects of Levocetirizine at therapeutically meaningful drug concentrations, including inhibition of eotaxin production by endothelial cells or inhibition of ICAM - 1 and major histocompatability complex class I expression by IFN - stimulate keratinocytes together with modulation of histamine - dependent release of GM - CSF and chemokines by these cells. Furthermore, histamine - induced, but not IL - 4 / TNF - induce, VCAM - 1 expression by nasal polyp - derive human fibroblasts was also inhibited by low concentrations of Levocetirizine. Levocetirizine does not appear to accelerate the rate of apoptosis - induction in eosinophils either in the presence or absence of viability - enhancing cytokines. However, Levocetirizine increases release of metalloproteinase MMP - 9, which is important in airway remodelling in asthma and metalloproteinase inhibitors TIMP - 4, and TIMP - 1 together with reduction in release of IL - 7 and stem cell factor by lipopoylsaccharide - stimulate eosinophils. Former is important in T cell function and to some extent eosinophil function while stem cell factor is a key factor in mast cell proliferation. Another recent study demonstrates that both Levocetirizine and cetirizine inhibit IL - 8 and GM - CSF production by IL - 1stimulated A549 epithelial cells. The latter is cell line derived from type II malignant pneumocytes and positive inhibitory effects were only seen at rather high non - physiological concentrations of cetirizine or Levocetirizine. Physiologically - Relevant concentrations of Levocetirizine inhibit ICAM - 1 expression and secretion of IL - 6 and IL - 8 in primary human nasal epithelial cells infected with human rhinovirus. Nasal epithelial cells treated with Levocetirizine also exhibit significantly reduced rhinovirus titres and reduced NF - B activation. These studies demonstrate in vitro anti - inflammatory effects of Levocetirizine at low, physiologically - relevant concentrations on diverse cell types comparable to those reported for cetirizine. However, obvious question is the extent to which these anti - inflammatory properties for give antihistamine have any clinical impact in addition to that given by H1 - receptor blockade. This question can only be answered by well conducted in vivo studies.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Conclusions

Pharmacokinetics of levocetirizine present linear correlation with administered dose, are not time dependent, and exhibit little variability among different subjects. Administer orally, levocetirizine is absorbed quickly and broadly; its bonding to plasma proteins is 95% and its distribution volume is low, which, for H - 1 receptor antagonist, represents a real advantage. 17 Because its metabolism is limited, its pharmacokinetics are poorly modified by concomitant intake of other drugs. It is mainly excreted through urine by glomerular filtration and active tubular secretion; therefore, it is recommended to prolong the time between doses in patients with chronic renal failure. In regards to its safety profile, no negative effects on alertness, reaction abilities, or ability to drive vehicles have emerged from clinical studies reported in literature after one or more doses of levocetirizine at a recommended dosage of 5 mg / day. 18 - 22 Verster and colleagues 18 have evaluated the effects of treatment with various antihistamines on memory, psychomotor abilities and mood state. Two antihistamines were examine: levocetirizine and diphenhydramine vs placebo, administered three different times once daily on four consecutive days. A study group consisting of 48 healthy volunteers underwent a series of laboratory tests three hours after the first dose and at the end of study, ie, on the fourth day. Results demonstrate that single dose or repeated doses of levocetirizine had no modification on memory, attention and motor skills, whereas diphenhydramine induced significant reduction in attention and motor skills as early as the first dose. 18 in the same group, assessment of effects on driving skills showed no statistically significant changes in the group treated with levocetirizine compared with placebo, unlike results observed with diphenhydramine. 19 absence of sedative effects has been confirmed by two other double - blind, placebo control clinical studies conducted to evaluate effects on cognitive and psychomotor functions, in groups of 20 and 19 subjects respectively, of treatment with levocetirizine 20 21 or first - generation antihistamines like promethazine 20 and diphenhydramine 21 and second - generation antihistamines. 20 study by Potter 22 reports absence of significant adverse reactions during six - week treatment with levocetirizine at 5 mg / day. In both, two examine groups reported at least one adverse reaction in similar percentages: 60. 0% and 68. 1%, respectively. 22 most frequent adverse reaction was headache, influenza - like symptoms, high respiratory tract infections and drowsiness. 22 Apart from cases of drowsiness, no reduction of memory and psychomotor functions has been demonstrate. 20 in one subject, there was an increase in alanine aminotransferase, related with drug, which regress spontaneously after nine days. 22 During this study there were no cases of increased electrocardiogram QT interval. 22 absence of cardiotoxic effects of levocetirizine has been recently confirmed by study conducted on 52 healthy subjects treated with 5 mg and 30 mg under dynamic monitoring according to Holter method in 24 hours following dose.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

What is levocetirizine?

Some medicines are not suitable for people with certain conditions, and sometimes medicine can only be used if extra care is take. For these reasons, before you start taking levocetirizine it is important that your doctor knows: if you are pregnant or breastfeeding. If you have any problems with the way your kidneys work. If you have epilepsy. If you have a rare inherited blood disorder, called porphyria. If you are taking or using any other medicines. This includes any medicines you are taking which are available to buy without prescription, as well as herbal and complementary medicines. If you have ever had an allergic reaction to another antihistamine, or to any other medicine.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

Sources

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions.

* Please keep in mind that all text is machine-generated, we do not bear any responsibility, and you should always get advice from professionals before taking any actions

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