Description

Simple

A medication used to treat the symptoms of allergies such as runny nose, red and watery eyes, as well as itchiness.

Clinical

A selective Histamine-1 antagonist drug used in allergic rhinitis and chronic urticaria.

Overview

Cetirizine, also commonly known as _Zyrtec_, is an orally active second-generation histamine H1 antagonist proven effective in the treatment of various allergic symptoms, such as sneezing, coughing, nasal congestion, hives, and other symptoms [1], [2].

One of the most common uses for this drug is for a condition called _allergic rhinitis_. The prevalence of allergic rhinitis in the United States is about 15% according to physician diagnoses, and up to 30%, according to self-reported nasal symptoms. Allergic rhinitis is associated with multiple missed or unproductive days at work and school, problems with sleep, and other difficulties with day to day activities for many individuals [3]. Furthermore, some antihistamine agents that are used to treat this condition cause undesirable, sedating effects [Read more

Pharmacology

Indication

**Seasonal Allergic Rhinitis**: Indicated for the relief of symptoms associated with seasonal allergic rhinitis caused by allergens such as ragweed, grass and tree pollens in adults and children 2 years of age and above. Symptoms treated effectively include sneezing, rhinorrhea, nasal pruritus, ocul... Read more

Pharmacodynamic

**General effects and respiratory effects**

Cetirizine, the active metabolite of the piperazine H1-receptor antagonist hydroxyzine, minimizes or eliminates the symptoms of chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical u... Read more

Mechanism of action

Cetirizine, a metabolite of _hydroxyzine_, is an antihistamine drug. Its main effects are achieved through selective inhibition of peripheral H1 receptors. The antihistamine activity of cetirizine has been shown in a variety of animal and human models. _In vivo_ and _ex vivo_ animal models have sho... Read more

Absorption

Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) of about 1 hour after oral administration of tablets or syrup formulation in adult volunteers [FDA label]. Bioavailability was found to be similar between the tablet and syrup dosage forms. When healthy study volunteers were... Read more

Protein binding

The mean plasma protein binding of cetirizine is 93% [FDA label].

Volume of distribution

Apparent volume of distribution: 0.44 +/- 0.19 L/kg [ Read more

Clearance

Apparent total body clearance: approximately 53 mL/min [FDA label].Cetirizine is mainly eliminated by the kidneys [ Read more

Half life

Plasma elimination half-life is 8.3 hours [FDA label].

Route of elimination

Mainly eliminated in the urine [FDA label], [1].

Betwe... Read more

Toxicity

Oral LD50 (rat): 365 mg/kg; Intraperitoneal LDLO (mouse): 138 mg/kg; Oral TDLO (rat): 50 mg/kg; Oral TDLO (mouse): 0.1 mg/kg [MSDS].

**Carcinogenesis and mutagenesis**: In a 2-year carcinogenicity study in rats, cetirizine was not shown to be carcinogenic at dietary doses up to 20 mg/kg (approxi... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Hypersensitivity to hydroxyzine
      • Drugbank Id: DBCOND0117551
  • Regions: US
  • Patient Conditions:
      • Name: Patients with known hypersensitivity to cetirizine
      • Drugbank Id: DBCOND0117550

Food Interactions

  • Avoid alcohol.
  • Take without regard to meals.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Cetirizine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Cetirizine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Cetirizine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Cetirizine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Abacavir
Cetirizine may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Cetirizine.
Abexinostat
The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Abexinostat.
Acarbose
Acarbose may decrease the excretion rate of Cetirizine which could result in a higher serum level.
Acebutolol
The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Cetirizine which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Cetirizine which could result in a higher serum level.
Acepromazine
The risk or severity of adverse effects can be increased when Cetirizine is combined with Acepromazine.
Aceprometazine
The risk or severity of adverse effects can be increased when Cetirizine is combined with Aceprometazine.
Acetaminophen
The serum concentration of Cetirizine can be increased when it is combined with Acetaminophen.
Acetazolamide
The risk or severity of adverse effects can be increased when Cetirizine is combined with Acetazolamide.
Acetophenazine
The risk or severity of adverse effects can be increased when Cetirizine is combined with Acetophenazine.
Acetyldigoxin
Cetirizine may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.
5 References
  1. 1 . Portnoy JM, Dinakar C: Review of cetirizine hydrochloride for the treatment of allergic disorders. Expert Opin Pharmacother. 2004 Jan;5(1):125-35. doi: 10.1517/14656566.5.1.125 .PubMed: 14680442
  2. 2 . Zhang L, Cheng L, Hong J: The clinical use of cetirizine in the treatment of allergic rhinitis. Pharmacology. 2013;92(1-2):14-25. doi: 10.1159/000351843. Epub 2013 Jul 18.PubMed: 23867423
  3. 3 . Wheatley LM, Togias A: Clinical practice. Allergic rhinitis. N Engl J Med. 2015 Jan 29;372(5):456-63. doi: 10.1056/NEJMcp1412282.PubMed: 25629743
  4. 4 . Church MK, Church DS: Pharmacology of antihistamines. Indian J Dermatol. 2013 May;58(3):219-24. doi: 10.4103/0019-5154.110832.PubMed: 23723474
  5. 5 . Spicak V, Dab I, Hulhoven R, Desager JP, Klanova M, de Longueville M, Harvengt C: Pharmacokinetics and pharmacodynamics of cetirizine in infants and toddlers. Clin Pharmacol Ther. 1997 Mar;61(3):325-30. doi: 10.1016/S0009-9236(97)90165-X.PubMed: 9084458