Cetirizine


Description

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 [

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Pharmacology

Indication

**Seasonal Allergic Rhinitis**: Indicated for the relief of symptoms associated with seasonal allerg... Read more

Pharmacodynamic

**General effects and respiratory effects**

Cetirizine, the active metabolite of the piperazine H...
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Mechanism of action

Cetirizine, a metabolite of _hydroxyzine_, is an antihistamine drug. Its main effects are achieved... Read more

Absorption

Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) of about 1 hour after or... 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 b... Read more

Half life

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

Route of elimination

Mainly eliminated in the urine [FDA label], [ Read more

Toxicity

Oral LD50 (rat): 365 mg/kg; Intraperitoneal LDLO (mouse): 138 mg/kg; Oral TDLO (rat): 50 mg/kg; Oral... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • pediatric
  • Kind: experimental
    • Percent: 11.0-14.0%
  • Kind: placebo
    • Percent: 12.3%
  • Clinical Trial
    Pharyngitis US
    • pediatric
  • Kind: experimental
    • Percent: 2.8-6.2%
  • Kind: placebo
    • Percent: 2.9%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 5.9
  • Clinical Trial
    Abdominal Pain US
    • pediatric
  • Kind: experimental
    • Percent: 4.4-5.6%
  • Kind: placebo
    • Percent: 1.9%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 5
  • Clinical Trial
    Cough US
    • pediatric
  • Kind: experimental
    • Percent: 2.8-4.4%
  • Kind: placebo
    • Percent: 3.9%
  • Clinical Trial
    Somnolence US
    • pediatric
  • Kind: experimental
    • Percent: 1.2-4.2%
  • Kind: placebo
    • Percent: 1.3%
  • Clinical Trial
    Epistaxis US
    • pediatric
  • Kind: experimental
    • Percent: 1.9-3.7%
  • Kind: placebo
    • Percent: 2.9%
  • Clinical Trial
    Diarrhea US
    • pediatric
  • Kind: experimental
    • Percent: 1.9-3.1%
  • Kind: placebo
    • Percent: 1.3%
  • Clinical Trial
    Bronchospasm US
    • pediatric
  • Kind: experimental
    • Percent: 1.9-3.1%
  • Kind: placebo
    • Percent: 1.9%
  • Clinical Trial
    Nausea US
    • pediatric
  • Kind: experimental
    • Percent: 1.9-2.8%
  • Kind: placebo
    • Percent: 1.9%
  • Clinical Trial
    Vomiting US
    • pediatric
  • Kind: experimental
    • Percent: 2.3-2.5%
  • Kind: placebo
    • Percent: 1.0%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 2
  • Dizziness US
  • Kind: experimental
    • Percent: 2
  • Clinical Trial
    Photosensitivity reaction US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Maculopapular rash US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Increases sweating US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Toxic photosensitivity reaction US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Seborrhea US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Purpura US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Urticaria US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Skin nodule US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Skin disorder US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Angioedema US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Acne US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Alopecia US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dermatitis US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Dry Skin US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Bullous eruption US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Erythematous rash US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Eczema US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Hypertrichosis US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Furunculosis US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Hyperkeratosis US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Enlarged abdomen US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Facial edema US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Generalized edema US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Hot Flashes US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Leg edema US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Increased weight US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Parosmia US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Taste loss US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial
    Taste perversion US
  • Kind: experimental
    • Percent: <2%
  • Clinical Trial

    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

    Type in a drug name to check for interaction with Cetirizine

    2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
    2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
    4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with 4-Methoxyamphetamine.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with 5-methoxy-N,N-dimethyltryptamine.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with 7-Nitroindazole.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
    Cetirizine may decrease the excretion rate of Abacavir which could result in a higher serum level.
    The serum concentration of Abemaciclib can be increased when it is combined with Cetirizine.
    The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Abexinostat.
    Acarbose may decrease the excretion rate of Cetirizine which could result in a higher serum level.
    The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Acebutolol.
    Aceclofenac may decrease the excretion rate of Cetirizine which could result in a higher serum level.
    Acemetacin may decrease the excretion rate of Cetirizine which could result in a higher serum level.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with Acepromazine.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with Aceprometazine.
    The serum concentration of Cetirizine can be increased when it is combined with Acetaminophen.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with Acetazolamide.
    The risk or severity of adverse effects can be increased when Cetirizine is combined with Acetophenazine.
    Cetirizine may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.

    References

    • 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 . 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 . 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 . 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 . 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]

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