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Levocetirizine

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Last Updated: 21 January 2021

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General | Latest Info

Levocetirizine

Chemical and physical data
3D model ( JSmol )Interactive image
FormulaC 21 H 25 Cl N 2 O 3
Molar mass388.89 gmol 1
Clinical data
AHFS / Drugs.comMonograph
ATC codeR06AE09 ( WHO )
License dataUS DailyMed : Levocetirizine
MedlinePlusa607056
Other namesLevocetirizine dihydrochloride
Routes of administrationBy mouth
Trade namesXyzal, Levazyr, others
Identifiers
CAS Number130018-77-8 N
ChEBICHEBI:94559
ChEMBLChEMBL1201191 N
ChemSpider1266001 Y
CompTox Dashboard ( EPA )DTXSID60156294
DrugBankDB06282 Y
IUPHAR/BPS1214
KEGGD07402 Y, as salt: D08118 Y
PDB ligandLCR ( PDBe , RCSB PDB )
PubChem CID1549000
UNII6U5EA9RT2O
Legal status
Legal statusUK : POM (Prescription only), US : OTC / Rx-only
Pharmacokinetic data
BioavailabilityHigh
Elimination half-life6 to 10 hours
ExcretionKidney and fecal
MetabolismLiver 14% CYP3A4
Protein binding90%

Levocetirizine is used to relieve runny nose; sneezing; and redness, itching, and tearing of eyes caused by hay fever, seasonal allergies, and allergies to other substances such as dust mites, animal dander, and mold. It is also used to treat symptoms of hives, including itching and rash. Levocetirizine is in a class of medications called antihistamines. It works by blocking action of histamine, substance in the body that causes allergic symptoms. Levocetirizine comes as a tablet to take by mouth. It is usually take once a day in the evening with or without food. Take levocetirizine at same time every day. Follow directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take levocetirizine exactly as direct. Do not take more or less of it or take it more often than prescribed by your doctor.

* 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 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

Society and culture

Levocetirizine, sold under the brand name Xyzal among others, is an antihistamine used for treatment of allergic rhinitis and long term hives of unclear cause. It is less sedating than older antihistamines. It is taken by mouth. Common side effects include sleepiness, dry mouth, cough, vomiting, and diarrhea. Use in pregnancy appears safe but has not been well studied and use when breastfeeding is of unclear safety. It is classified as a second-generation antihistamine and works by blocking histamine H 1-receptors. Levocetirizine was approved for medical use in the United States in 2007. It is available as a generic medication. In 2017, it was 175 most commonly prescribed medication in the United States, with more than three million prescriptions.

* 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

Contraindications

Available data on levocetirizine use during human pregnancy are insufficient to determine any drug-associated risks of miscarriage, birth defects, or adverse maternal or fetal outcomes. In animal reproduction studies, there was no evidence of fetal harm with administration of levocetirizine during organogenesis at doses greatly exceeding maximum recommended human dose in adults; animal studies are not always indicative of human response. Self-medication with cetirizine during pregnancy is not recommend. Pregnant patients should see their health care professional for proper diagnosis and treatment recommendations. The American College of Obstetricians and Gynecologists and American College of Allergy, Asthma, and Immunology consider cetirizine and loratadine as acceptable alternatives in pregnancy, preferably after the first trimester, when first-generation antihistamines are not tolerate. There is no data available on the presence of levocetirizine in human milk, effects on breastfed infant, or effects on milk production. Levocetirizine is R-enantiomer of cetirizine. Cetirizine is excrete in human breast milk, but quantitative amounts are not know. Because of its lack of sedation and low milk concentrations, loratadine is not expected to cause adverse effects in breastfed babies and loratadine is usually considered compatible with breast-feeding. The British Society for Allergy and Clinical Immunology also recommends loratadine at lowest dose as the preferred antihistamine in breast-feeding women.


Levocetirizine Drug Interactions

Acetaminophen; Butalbital: concurrent use of cetirizine / levocetirizine with barbiturates should generally be avoid. Coadministration may increase the risk of CNS depressant-related side effects. If concurrent use is necessary, monitor for excessive sedation and somnolence. Acetaminophen; Butalbital; Caffeine: concurrent use of cetirizine / levocetirizine with barbiturates should generally be avoid. Coadministration may increase the risk of CNS depressant-related side effects. If concurrent use is necessary, monitor for excessive sedation and somnolence. Acetaminophen; Butalbital; Caffeine; Codeine: concomitant use of opioid agonists with cetirizine may cause excessive sedation and somnolence. Limit use of opioid pain medication with cetirizine to only patients for whom alternative treatment options are inadequate. If concurrent use is necessary, use the lowest effective doses and minimum treatment durations needed to achieve desired clinical effect. Concurrent use of cetirizine / levocetirizine with barbiturates should generally be avoid. Coadministration may increase the risk of CNS depressant-related side effects. If concurrent use is necessary, monitor for excessive sedation and somnolence. Acetaminophen; Caffeine; Dihydrocodeine: concomitant use of opioid agonists with cetirizine may cause excessive sedation and somnolence. Limit use of opioid pain medication with cetirizine to only patients for whom alternative treatment options are inadequate. If concurrent use is necessary, use the lowest effective doses and minimum treatment durations needed to achieve desired clinical effect. Acetaminophen; Codeine: concomitant use of opioid agonists with cetirizine may cause excessive sedation and somnolence. Limit use of opioid pain medication with cetirizine to only patients for whom alternative treatment options are inadequate. If concurrent use is necessary, use the lowest effective doses and minimum treatment durations needed to achieve desired clinical effect. Acetaminophen; Hydrocodone: concomitant use of opioid agonists with cetirizine may cause excessive sedation and somnolence. Limit use of opioid pain medication with cetirizine to only patients for whom alternative treatment options are inadequate. If concurrent use is necessary, use the lowest effective doses and minimum treatment durations needed to achieve desired clinical effect. Acetaminophen; Oxycodone: concomitant use of opioid agonists with cetirizine may cause excessive sedation and somnolence. Limit use of opioid pain medication with cetirizine to only patients for whom alternative treatment options are inadequate. If concurrent use is necessary, use the lowest effective doses and minimum treatment durations needed to achieve desired clinical effect. Acetaminophen; Pentazocine: concurrent use of cetirizine / levocetirizine with Pentazocine should generally be avoid. Coadministration may increase the risk of CNS depressant-related side effects. If concurrent use is necessary, monitor for excessive sedation and somnolence. Acetaminophen; Propoxyphene: concomitant use of opioid agonists with cetirizine may cause excessive sedation and somnolence. Limit use of opioid pain medication with cetirizine to only patients for whom alternative treatment options are inadequate. If concurrent use is necessary, use the lowest effective doses and minimum treatment durations needed to achieve desired clinical effect. Acetaminophen; Tramadol: concomitant use of opioid agonists with cetirizine may cause excessive sedation and somnolence. Limit use of opioid pain medication with cetirizine to only patients for whom alternative treatment options are inadequate.

* 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

How to take levocetirizine

Before you start treatment, read the manufacturer's printed information leaflet from inside the pack. It will give you more information about levocetirizine, and will also provide you with a full list of side-effects which you could experience from taking it. The usual dose for adults and older children is one tablet daily. If it is for younger child, they are likely to be prescribed liquid medicine, so check the label on the bottle carefully to make sure you give the correct dose for the age of your child. Most people take levocetirizine in the morning, but you can take it at whatever time of day you find easiest to remember. Try to take your doses at same time of day, each day, as this will help you to remember to take them regularly. You can take levocetirizine either before or after a meal. Tablets are best swallow with a drink of water. If you have been given liquid medicine, oral dose syringe will be included in the pack. This is to measure out dose. Put tip of syringe into the medicine and draw a plunger up to mark which corresponds to the dose prescribed. Remove the syringe from the bottle and empty its contents on to spoon or into a small glassful of water. Medicine can be swallow either undiluted, or diluted with water. Remember to rinse the syringe with water after using it. If you forget to take dose at your usual time, take it as soon as you remember. If you do not remember until the following day, then leave out forgotten dose from the previous day and take the dose that is due that day. Do not take two doses at same time to make up for miss 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

Clinical Trials Experience

In addition to adverse reactions reported during clinical trials and list above, following adverse reactions have also been identified during postapproval use of Xyzal. Because these reactions are reported voluntarily from population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Cardiac disorders: palpitations, tachycardia Ear and labyrinth disorders: vertigo Eye disorders: blur vision, visual disturbances Gastrointestinal disorders: nausea, vomiting General disorders and administration site conditions: edema Hepatobiliary disorders: hepatitis Immune system disorders: anaphylaxis and hypersensitivity Metabolism and nutrition disorders: increased appetite Musculoskeletal, connective tissues, and bone disorders: arthralgia, myalgia Nervous system disorders: dizziness, dysgeusia, febrile seizure, movement disorders, paresthesia, seizure, tremor Psychiatric disorders: aggression and agitation, depression, hallucinations, insomnia, nightmare, suicidal ideation Renal and urinary disorders: dysuria, urinary retention Respiratory, thoracic, and mediastinal disorders: dyspnea Skin and subcutaneous tissue disorders: angioedema, fix drug eruption, pruritus, rash and urticaria besides these reactions report under treatment with Xyzal, other potentially severe adverse events have been report from postmarketing experience with cetirizine. Since levocetirizine is the principal pharmacologically active component of cetirizine, one should take into account the fact that following adverse events could also potentially occur under treatment with Xyzal. Cardiac disorders: severe hypotension Gastrointestinal disorders: cholestasis Nervous system disorders: extrapyramidal symptoms, myoclonus, orofacial dyskinesia, tic Pregnancy, puerperium and perinatal conditions: stillbirth Renal and urinary disorders: glomerulonephritis Skin and subcutaneous tissue disorders: acute generalize exanthematous pustulosis; rebound pruritus-pruritus within few days after discontinuation of cetirizine, usually after long-term use of cetirizine.

* 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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