Levocetirizine

Registered South African indications:

• Seasonal allergic rhinitis
• Perennial allergic rhinitis
• Chronic idiopathic urticaria

Registered South African contraindications

Oral dispersible tablet

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to levocetirizine, to any piperazine derivative
• Pregnancy
• Breastfeeding
• End-stage renal disease (creatinine clearance < 10ml/min)
• In children under the age of 6 years

Solution

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to cetirizine, to hydroxyzine, to any piperazine derivative
• End stage renal disease, at less than 10ml/min creatinine clearance

Film-coated tablet

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to cetirizine, to hydroxyzine, to any piperazine derivative
• Patients with severe renal impairment at less than 10ml/min creatinine clearance and patients undergoing dialysis
• Infants and children under 2 years as safety and efficacy have not been demonstrated
• Children from ages 2 - 6 years as no dosage adjustment is possible with the film coated tablet formulation
• Pregnancy
• Breastfeeding

• Pregnancy (sol)
• Breastfeeding (sol)
• Renal impairment (paediatric patients)
• Moderate to severe renal impairment (CrCl ≥11-≤49ml/min)
• Predisposing factors of urinary retention
  - Spinal cord lesion
  - Prostatic hyperplasia
• Epilepsy and patients at risk of convulsion 
• Coadministration with alcohol
• Fructose intolerance (sol)
• 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: fct, odt, sol, tab

South African registered indications and dosages

Seasonal allergic rhinitis
Perennial allergic rhinitis
Chronic idiopathic urticaria

• Oral (fct, odt, sol): 5mg, dly

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Method of administration

The film-coated tablet must be taken orally, swallowed with liquid and may be taken with or without food. It is recommended to take the daily dose in one single intake

Oral dispersible tablet: To be placed on the tongue and sucked, not chewed, until completely disintegrated. The resulting suspension must be swallowed with saliva. Can be taken with or without water and may be taken with or without food. It is recommended to take the daily dose in one single intake

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Duration of use

Intermittent allergic rhinitis (symptoms < 4 days/week or during less than 4 weeks) has to be treated according to the disease and its history; it can be stopped once the symptoms have disappeared and can be restarted again when symptoms reappear. In case of persistent allergic rhinitis (symptoms > 4 days/week or during more than 4 weeks), continuous therapy can be proposed to the patient during the period of exposure to allergens

Clinical experience is currently available for a 6-month treatment period (fct, sol)

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

South African registered indications and dosages

Seasonal allergic rhinitis
Perennial allergic rhinitis
Chronic idiopathic urticaria

Children below 2 years

• Not recommended for use (see contraindications)

Between 2-6 years

• Oral (sol): 1.25mg, twice daily

Older than 6 years

• Oral (fct, odt, sol): 5mg, dly

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Film coated tablets is contraindicated in children aged less than 2 years and should not be used in children aged 2 - 6 years, as no adjusted dosage is possible with the film-coated tablet formulation

The oral dispersible tablet is contraindicated in children under the age of 6 years

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Method of administration

The film-coated tablet must be taken orally, swallowed with liquid and may be taken with or without food. It is recommended to take the daily dose in one single intake

Oral dispersible tablet: To be placed on the tongue and sucked, not chewed, until completely disintegrated. The resulting suspension must be swallowed with saliva. Can be taken with or without water and may be taken with or without food. It is recommended to take the daily dose in one single intake

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Duration of use

Intermittent allergic rhinitis (symptoms < 4 days/week or during less than 4 weeks) has to be treated according to the disease and its history; it can be stopped once the symptoms have disappeared and can be restarted again when symptoms reappear. In case of persistent allergic rhinitis (symptoms > 4 days/week or during more than 4 weeks), continuous therapy can be proposed to the patient during the period of exposure to allergens

Clinical experience is currently available for a 6-month treatment period (fct, sol)

Pregnancy

South African recommendations

• Contraindicated (fct, odt)
• Caution; not recommended (sol)
• Safety in pregnancy has not yet been established

Breastfeeding

South African recommendations

• Contraindicated (fct, odt)
• Caution; not recommended (sol)
• Not recommended in women who are breastfeeding their babies, since levocetirizine dihydrochloride is excreted in breast milk

Fertility

South African recommendations

• No information available

South African recommendations

• Mild (CrCl ≥ 50ml/min): No dose adjustment necessary
• Moderate to severe (CrCl ≥11-≤49ml/min): Caution; dose adjustment recommended (see table)
• End stage renal disease/ receiving dialysis (CrCl ≤10ml/min): Contraindicated
• Paediatric patients: Caution; dose adjustment recommended
  The dose will have to be adjusted on an individual basis taking into account the renal clearance of the patient and his/her body weight. There are no specific data for children with renal impairment

Group	CrCl (ml/min)	Adults
Normal	≥80	No adjustment necessary
Mild	50-79	No adjustment necessary
Moderate	30-49	5mg, once every 2 days
Severe	< 30	5mg, once every 3 days
End-stage renal disease – patients undergoing dialysis	< 10	Contraindicated

• No dose adjustment recommended

• No dose adjustment recommended
  Adjustment of the dose is recommended in elderly patients with moderate to severe renal impairment

Central Nervous System Disorders

• Headache
• Fatigue
• Somnolence
• Sleep disorder
• Aggression
• Agitation
• Hallucination
• Depression
• Insomnia
• Suicidal ideation
• Nightmare
• Seizures
• Paraesthesia
• Dizziness
• Syncope
• Tremor

Cardiovascular Disorders

• Tachycardia
• Palpitations

Respiratory Disorders

• Dyspnoea

Gastrointestinal Disorders

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

Hepatobiliary Disorders

• Hepatitis
• Abnormal hepatic function tests

Genitourinary Disorders

• Dysuria
• Urinary retention

Endocrine and Metabolic Disorders

• Increased appetite
• Increased weight

Musculoskeletal Disorders

• Myalgia
• Arthralgia

Skin and Subcutaneous Tissue Disorders

• Angioneurotic oedema
• Fixed drug eruption
• Pruritus
• Rash
• Urticaria

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity
  - Anaphylaxis
• Oedema

Sensory Disorders

• Vertigo
• Visual disturbances
• Blurred vision
• Oculogyration
• Dysgeusia

• Central nervous system depressants

Other interactions

• Alcohol
• Allergy skin tests (See additional prescribing points)

None routine. Specific cases may require

• Renal function

Allergy skin tests

• Response to allergy skin tests are inhibited by antihistamines and a wash-out period (of 3 days) is required before performing them

Levocetirizine, the (R) enantiomer of cetirizine, is a potent and selective antagonist of peripheral H1-receptors.

Solution (per ml) 0.5mg

• Xyzal oral solution (GSK) originator

Tablet 5mg

• Allerway (Dr Reddy)
• Cetaway (Pharma Dynamics)
• Cetizal (Ranbaxy)
• Cetlovo (Pharmacare)
• Glencet (Glenmark)
• Levogex (Adcock Ingram)
• Texamer fct (Pharma Dynamics)
• Xyzal (GSK) originator