Cetirizine

Registered South African indications:

• Symptomatic relief of allergic conditions

Contraindications

Registered South African contraindications

Film-coated tablets & Tablets

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to hydroxyzine
• Lactation
• Pregnancy
• Children under the age of 2 years

Syrup 1mg/ml

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to hydroxyzine
• Hypersensitivity to any piperazine derivatives
• Severe renal impairment creatinine clearance less than 30ml/min
• Asthma, as it may cause airway obstruction in patients who have previously experienced adverse reactions to antihistamines
• Pregnancy
• Lactation
• Children under the age of 2 years

Oral solution 1mg/ml & Oral drops 10mg/ml

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to hydroxyzine
• Hypersensitivity to any piperazine derivatives
• Severe renal impairment creatinine clearance less than 10ml/min
• Pregnancy
• Lactation
• Children under the age of 2 years

Contraindications registered in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to hydroxyzine
• Hypersensitivity to any piperazine derivatives
• Severe renal impairment creatinine clearance less than 10ml/min

Cautions

• Pregnancy (Recommendations in other jurisdictions)
• Breastfeeding (Recommendations in other jurisdictions)
• Renal impairment (South African recommendations)
  - CrCl<40ml/min  (fct)
  - CrCl 30-<40ml/min (syr)
  - CrCl 10-<40ml/min (drp, sol)
• Renal impairment (Recommendations in other jurisdictions)
  - CrCl 10-<50ml/min
• Moderate to severe hepatic impairment (South African recommendations) 
• Children between 2-6 years (tab)
• Predisposition to urinary retention
• Epilepsy
• Fructose intolerance (syr)
• Galactose intolerance (tab)
• Lapp lactase deficiency (tab) 
• Glucose-galactose malabsorption (tab)
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: drp, fct, sol, syr, tab

South African registered indications and dosages

Symptomatic relief of allergic conditions
- Allergic rhinitis
- Allergic skin conditions associated with pruritus such as urticaria
- Hay fever

• Oral (drp, fct, sol, syr, tab): 10mg, once daily

Drops: 10mg = 20 drops

Missed doses: Advise patients who forget to take cetirizine to take a dose as soon as possible and then continue with the normal dose. Patients should not take a double dose to compensate for the missed dose

Paed. forms avail. in SA and covered in this monograph: drp, fct, sol, syr, tab

South African registered indications and dosages

Symptomatic relief of allergic conditions
- Allergic rhinitis
- Allergic skin conditions associated with pruritus such as urticaria
- Hay fever

Oral (fct, tab)

• Younger than 2 years: Contraindicated
• Between 2-6 years: Not a suitable dosage form
• Between 6-12 years: 10mg, once daily OR 5mg, twice daily
• Older than 12 years: See adult dosage

Oral (drp, sol, syr)

• Younger than 2 years: Contraindicated
• Between 2-6 years: 5mg, once daily OR 2.5mg, in 2 divided doses (in the morning and in the evening)
• Between 6-12 years: 10mg, once daily OR 5mg, in 2 divided doses (in the morning and in the evening)
• Older than 12 years: See adult dosage

Drops: 10mg = 20 drops; 5mg = 10 drops; 2.5mg = 5 drops

Missed doses: Advise patients who forget to take cetirizine to take a dose as soon as possible and then continue with the normal dose. Patients should not take a double dose to compensate for the missed dose

Pregnancy

South African recommendations

• Contraindicated
• Safety in pregnancy has not been established

Recommendations in other jurisdictions

• Caution
• Data on a limited number of exposed pregnancies indicate no adverse effects of cetirizine on pregnancy or on the health of foetus/newborn child. To date no other relevant epidemiological data are available
• Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or post-natal development. Caution should be exercised when prescribing to pregnant women

Breastfeeding

South African recommendations

• Contraindicated
• Safety in breastfeeding women has not been established
• Caution should be exercised when prescribing cetirizine to lactating women
• Cetirizine is excreted in human milk at concentrations representing 25% to 90% of those measured in plasma, depending on sampling time after administration

Recommendations in other jurisdictions

• Caution
• Caution should be exercised when prescribing cetirizine to lactating women
• Cetirizine is excreted in human milk at concentrations representing 25% to 90% of those measured in plasma, depending on sampling time after administration

Fertility

Recommendations below are applicable to South Africa and other jurisdictions

• Limited data is available on human fertility but no safety concern has been identified. Animal data show no safety concern for human reproduction

South African recommendations

Film coated tablets & Tablets

• CrCl≥40ml/min: No dose adjustment recommended
• CrCl<40ml/min: Caution; dose adjustment recommended
  The recommended daily dose should be halved

Syrup 1mg/ml

• CrCl≥40ml/min: No dose adjustment recommended
• CrCl 30-<40ml/min: Caution; dose adjustment recommended
  The recommended daily dose should be halved
• CrCl<30ml/min: Contraindicated

Oral solution 1mg/ml & Oral drops 10mg/ml

• CrCl≥40ml/min: No dose adjustment recommended
• CrCl 10-<40ml/min: Caution; dose adjustment recommended
  The recommended daily dose should be halved
• CrCl<10ml/min: Contraindicated

Recommendations in other jurisdictions

• CrCl≥50ml/min: No dose adjustment recommended
• CrCl 10-<50ml/min: Caution; dose adjustment recommended
• CrCl<10ml/min: Contraindicated

In paediatric patients suffering from renal impairment, the dose will have to be adjusted on an individual basis taking into account the renal clearance of the patient, their age and body weight

South African recommendations

• Mild: No dose adjustment recommended
• Moderate to severe: Caution; dose adjustment recommended
  The recommended daily dose should be halved

Recommendations in other jurisdictions

• No dose adjustment recommended

Recommendations below are applicable to South Africa and other jurisdictions

• No dose adjustment recommended
  No dose adjustment is necessary in healthy elderly patients with normal renal function

Central Nervous System Disorders

• Dizziness
• Headache
• Somnolence
• Agitation
• Aggression
• Confusion
• Depression
• Hallucinations
• Insomnia
• Tic
• Paraesthesia
• Incoordination
• Tremors
• Nightmares
• Convulsions
• Hallucinations
• Malaise

Cardiovascular Disorders

• Tachycardia
• Hypotension
• Oedema

Respiratory Disorders

• Pharyngitis
• Rhinitis

Gastrointestinal Disorders

• Abdominal pain
• Dry mouth
• Nausea and vomiting
• Diarrhoea
• Constipation
• Jaundice

Hepatobiliary Disorders

• Abnormal hepatic function 

Genitourinary Disorders

• Dysuria
• Enuresis

Endocrine and Metabolic Disorders

• Increased appetite
• Increased weight

Skin and Subcutaneous Tissue Disorders

• Pruritus
• Rash
• Urticaria
• Angioedema
• Fixed drug eruption
• Photosensitivity

Immune, Blood and Lymphatic System Disorders

• Thrombocytopenia
• Hypersensitivity
• Anaphylactic shock
• Haemolytic anaemia
• Agranulocytosis
• Leucopenia

Sensory Disorders

• Accommodation disorder
• Blurred vision
• Oculogyration
• Vertigo
• Tinnitis

• Central nervous system depressants

Other interactions

• Alcohol

None routine. Specific cases may require

• Renal function

Cetirizine competes with histamine for binding at H1-receptor sites, resulting in suppression of histaminic oedema, flare, and pruritus. It has limited penetration into the central nervous system, as a result of the less lipophilic carboxyl group on the ethylamine side chain, thus a low incidence of sedation.

Tablet 5mg

• Austell Cetirizine (Austell)

Tablet 10mg

• Acuzyrt (Cipla Medpro)
• Adco-Cetirizine (Adcock Ingram)
• Allecet (Cipla Medpro)
• Allermine (Trinity Pharma)
• Allesoothe (Forrester Pharma)
• Aspen Cetirizine (Pharmacare)
• Austell Cetirizine (Austell)
• Betek (Be-Tabs)
• Ceticit (Adcock Ingram)
• Cetirizine Dis-chem (Dezzo)
• Cetirizine-Hexal (Sandoz)
• Dezzo Cetirizine fct (Dezzo)
• Gulf Cetirizine (Gulf Drug)
• Sandoz Cetirizine (Sandoz)
• Sensahist (Oethmaan Biosims)
• Sinutab Sinus Allergy (Johnson & Johnson)
• Texa (Pharma Dynamics)
• Trantrin (Aurobindo)
• Zelary (Camox)
• Zetop (Pharma-Q)
• Zinallerg (Oethmaan Biosims))
• Zyncet (Unichem)
• Zyrtec (GSK) originator

Drops (per ml) 10mg

• Zyrtec Oral Drops (GSK) originator

Syrup (per ml) 1mg

• Acuzyrt (Cipla Medpro)
• Allecet (Cipla Medpro)
• Aspen Cetirizine (Pharmacare)
• Ceticit (Adcock)
• Cetirizine-Hexal (Sandoz)
• Sinutab Sinus Allergy Solution (Johnson & Johnson)
• Texa (Pharma Dynamics)
• Zelary (Unicorn)
• Zetop (Pharma-Q)
• Zyrtec Oral Solution (GSK) originator