Cetirizine

JFDA label: Cetolerg Tab

Mechanism of Action

Mechanism of Actions Cetirizine, a human metabolite of hydroxyzine, is an antihistamine; its principal effects are mediated via selective inhibition of peripheral H 1 receptors. The antihistaminic activity of cetirizine has been clearly documented in a variety of animal and human models. In vivo and ex vivo animal models have shown negligible anticholinergic and antiserotonergic activity. In clinical studies, however, dry mouth was more common with cetirizine than with placebo. In vitro receptor binding studies have shown no measurable affinity for other than H 1 receptors. Autoradiographic studies with radiolabeled cetirizine in the rat have shown negligible penetration into the brain. Ex vivo experiments in the mouse have shown that systemically administered cetirizine does not significantly occupy cerebral H 1 receptors.

Indications

Approved

• Eye Manifestations — eye allergy
• Hypersensitivity — allergic disease

Off-label

• Alopecia
• Conjunctivitis, Allergic
• Dermatitis
• Eczema
• Multiple Sclerosis
• Pemphigus
• Pruritus
• Rhinitis
• Rhinitis, Allergic, Perennial
• Rhinitis, Allergic, Seasonal
• Severe Acute Respiratory Syndrome

Contraindications

Source: openFDA

• Cetirizine hydrochloride oral solution, USP is contraindicated in those patients with a known hypersensitivity to it or any of its ingredients or hydroxyzine. Absolute

Adverse Reactions

Cardiac disorders (3)

Rare Cardiac disorder · Palpitations · Tachycardia

Vascular disorders (1)

Rare Hypotension

Nervous system disorders (11)

Very Common Headache · Somnolence

Common Dizziness

Uncommon Loss of consciousness · Syncope

Rare Amnesia · Convulsion · Dyskinesia · Memory impairment · Paraesthesia · Tremor

Hepatobiliary disorders (5)

Rare Blood bilirubin increased · Cholestasis · Hepatic function abnormal · Hepatitis · Transaminases increased

Renal and urinary disorders (4)

Rare Dysuria · Glomerulonephritis · Urinary retention · Urinary tract disorder

Blood and lymphatic system disorders (2)

Rare Haemolytic anaemia · Thrombocytopenia

Immune system disorders (3)

Rare Anaphylactic shock · Hypersensitivity · Immune system disorder

Gastrointestinal disorders (9)

Common Abdominal pain · Diarrhoea · Dry mouth · Dyspepsia · Gastrointestinal pain · Nausea · Vomiting

Uncommon Gastrointestinal disorder

Rare Increased appetite

Skin and subcutaneous tissue disorders (6)

Common Pruritus

Rare Angioedema · Dermatitis · Rash · Skin disorder · Urticaria

Musculoskeletal and connective tissue disorders (2)

Rare Musculoskeletal discomfort · Myalgia

Psychiatric disorders (7)

Common Insomnia

Rare Aggression · Agitation · Confusional state · Hallucination · Mental disorder · Suicidal ideation

Eye disorders (3)

Rare Eye disorder · Vision blurred · Visual impairment

Ear and labyrinth disorders (1)

Rare Vertigo

Infections and infestations (2)

Common Nasopharyngitis · Pharyngitis

Investigations (5)

Common Body temperature increased

Uncommon Weight increased

Rare Blood alkaline phosphatase increased · Feeling abnormal · Gamma-glutamyltransferase increased

General disorders and administration site conditions (20)

Common Asthenia · Fatigue · Otitis media

Uncommon Shock

Rare Accommodation disorder · Completed suicide · Discomfort · Drug eruption · Dysgeusia · Enuresis · Extrapyramidal disorder · Ill-defined disorder · Malaise · Movement disorder · Myoclonus · Nervous system disorder · Oculogyric crisis · Oedema · Stillbirth · Urethral disorder

Respiratory, thoracic and mediastinal disorders (4)

Common Bronchospasm · Cough · Epistaxis

Rare Dyspnoea

Dosing

Source: openFDA

Pregnancy & Lactation

Chemistry & Properties

Biology & Pharmacokinetics

Pharmacokinetics

Enzyme interactions

Receptor binding (top 2)

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MATE1 (Inhibitor)MATE2 (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OATP2B1 (Inhibitor)OCT1 (Inhibitor)OCTN2 (Inhibitor)P-gp (Inhibitor)MDR1 (Substrate)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Showing 40 of 100+.

Registered Products (39)