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Cetirizine is a second-generation antihistamine used in the treatment of hay fever, allergies, angioedema, and urticaria. It is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist.
Pharmacology
Cetirizine crosses the blood–brain barrier only slightly, reducing the sedative side-effect common with older antihistamines. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. found that it inhibited the expression of VCAM-1 in patients with atopic dermatitis.Unlike many other antihistamines, Cetirizine does not exhibit anticholinergic properties.
The levorotary enantiomer of cetirizine, known as levocetirizine, is the more active form.
Administration method and metabolism
Chewable, non-chewable, and syrup forms of cetirizine are similarly absorbed rapidly and effectively, with absorbed food minutely affecting the absorption rate which yields a peak serum level one hour after administration;in a study of healthy volunteers prescribed 10 mg tablets, once daily for 10 days, a mean peak serum level of 311 ng/mL was observed. The metabolic effects of cetirizine are long acting, remaining in the system for a maximum of 21 hours before being excreted; the average elimination half-life is 8 hours. About 70% of the drug is removed through urination, of which half is observed as unchanged cetirizine compound. Another 10% is excreted.
Like many other antihistamine medications, cetirizine is commonly prescribed in combination with pseudoephedrine hydrochloride, a decongestant. These combinations are marketed using the same brand name as the cetirizine with a "-D" suffix (Zyrtec-D, Virlix-D, etc.)
Allergies
Cetirizine's primary indication is for hay fever and other allergies. Because the symptoms of itching and redness in these conditions are caused by histamine acting on the H1 receptor, blocking those receptors temporarily relieves those symptoms.
Cetirizine is also commonly prescribed to treat acute and (in particular cases) chronic urticaria, more efficiently than any other second-generation antihistamine. It is preferred over diphenhydramine in many countries because, while being as effective as it for treating hives-related skin diseases, cetirizine does not affect the regular functioning of the brain.
Rhinovirus infection
Interleukin 6 and interleukin 8 have been shown to be elevated in acute respiratory distress syndrome. Cetirizine contains L- and D-stereoisomers. Chemically, levocetirizine is the active L-enantiomer of cetirizine. One recent study of airway epithelial cells showed that Levocetirizine may have beneficial effects on the pathophysiologic changes related to human rhinovirus (HRV) infection.Airway inflammation caused from a cytokine storm secondary to acute respiratory distress syndrome could also theoretically benefit.
Kimura's disease
Cetirizine is an effective agent in treating the symptoms of Kimura's disease, which mostly occurs in young Asian men, affecting the lymph nodes and soft tissue of the head and neck in the form of tumor-like lesions. Cetirizine's properties of being effective both in the treatment of pruritus (itching) and as an anti-inflammatory agent make it suitable for the treatment of the pruritus associated with these lesions.
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This medication is used to relieve allergy symptoms such as watery eyes, runny/stuffy nose, itching eyes/nose, and sneezing. It contains 2 medications: cetirizine and pseudoephedrine. Cetirizine is an antihistamine and works by blocking a certain natural substance (histamine) that your body makes during an allergic reaction. Pseudoephedrine is a decongestant and works by narrowing the blood vessels in the nose to decrease swelling and congestion.
This medication is not recommended for use in children under 12 years of age due to the large amount of pseudoephedrine in it.
How to use Aller-Tec D Oral
If you are taking the over-the-counter product to self-treat, read all directions on the product package before taking this medication. If you have any questions, consult your pharmacist. If your doctor has prescribed this medication, take it as directed with or without food, usually twice daily (every 12 hours).
Do not crush or chew extended-release tablets. Doing so can release all of the drug at once, increasing the risk of side effects. Also, do not split the tablets unless they have a score line and your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing or chewing.
The dosage is based on your age, medical condition, and response to treatment. Do not increase your dose or take this medication more often than directed.
Tell your doctor if your symptoms do not improve after 1 week, if they worsen, or if they occur with a fever.
Drowsiness, dizziness, tiredness, dry mouth, nausea, headache, or trouble sleeping may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
If your doctor has prescribed this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Tell your doctor right away if you have any serious side effects, including: difficulty urinating, fast/irregular/pounding heartbeat, shaking (tremor), mental/mood changes (such as anxiety, confusion, nervousness, restlessness), weakness.
Get medical help right away if you have any very serious side effects, including: seizures.
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
Before taking this medication, tell your doctor or pharmacist if you are allergic to cetirizine or pseudoephedrine; or to hydroxyzine; or to levocetirizine; or if you have any other allergies. Also, tell your doctor if you have had serious side effects from similar medications (such as other decongestants, including phenylephrine). This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: glaucoma, difficulty urinating (such as due to an enlarged prostate), high blood pressure (hypertension), heart/blood vessel disease (such as coronary artery disease), overactive thyroid (hyperthyroidism), diabetes, kidney disease, liver disease.
This drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Avoid alcoholic beverages.
Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).
Older adults may be more sensitive to the side effects of this drug, especially fast/irregular heartbeat, dizziness, problems urinating, trouble sleeping, or confusion.
During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
This medication passes into breast milk. Consult your doctor before breast-feeding.
Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
Taking MAO inhibitors with this medication may cause a serious (possibly fatal) drug interaction. Avoid taking MAO inhibitors (isocarboxazid, linezolid, methylene blue, moclobemide, phenelzine, procarbazine, rasagiline, selegiline, tranylcypromine) during treatment with this medication. Most MAO inhibitors should also not be taken for two weeks before treatment with this medication. Ask your doctor when to start or stop taking this medication.
Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, other antihistamines (such as diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and narcotic pain relievers (such as codeine).
Check the labels on all your medicines (such as cough-and-cold products) because they may contain ingredients that cause drowsiness or they may contain similar ingredients (decongestants such as phenylephrine). Ask your pharmacist about using those products safely.
Do not use with any other antihistamines applied to the skin (such as diphenhydramine cream, ointment, spray) because increased side effects may occur.
Cetirizine is very similar to hydroxyzine and levocetirizine. Do not use these medications while using cetirizine.
This medication may interfere with certain laboratory tests (including allergy skin testing), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
If overdose is suspected, contact a poison control center or emergency room immediately. Symptoms of overdose may include: severe drowsiness, fast/irregular heartbeat, mental/mood changes (such as anxiety, restlessness), seizures.
Notes
Keep all regular medical and laboratory appointments.
Missed Dose
If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.
Storage
Store at room temperature away from light and moisture. Do not store in the bathroom. Different brands of this medication may have different storage needs. Check the product package for instructions on how to store your brand, or ask your pharmacist. Keep all medications away from children and pets.
Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised November 2013. Copyright(c) 2013 First Databank, Inc.
