Mizolastine

Registered South African indications:

• Rhinoconjunctivitis
• Urticaria

Contraindications 

• Hypersensitivity to the active ingredient or any of its excipients
• Severe hepatic impairment
• Clinically significant cardiac disease
• History of symptomatic arrhythmias
• Known or suspected QT prolongation or with electrolyte imbalance, in particular hypokalaemia
• Clinically significant bradycardia
• Coadministration with macrolide antibiotics
• Coadministration with systemic imidazole antifungals
• Coadministration with QT prolonging agents e.g. Class I and III antiarrhythmics

Cautions 

• Pregnancy
• Breastfeeding
• Renal impairment
• Mild to moderate hepatic impairment
• Elderly
• Asthma
• Diabetes
• Patients susceptible to electrolyte imbalance
• Patients susceptible to cardiac arrhythmias
• Galactose intolerance
• Total lactose deficiency
• Glucose-galactose malabsorption
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: tab

Symptomatic treatment of seasonal and perennial allergic rhinoconjunctivitis
Urticaria

• Oral (tab): 10mg, dly

Paed. forms avail. in SA and covered in this monograph: tab

Symptomatic treatment of seasonal and perennial allergic rhinoconjunctivitis
Urticaria

Younger than 12 years

• No information available

Older than 12 years

• Oral (tab): See adult dosage

Pregnancy

• Caution
• The safety of mizolastine for use in human pregnancy has not been established
• The evaluation of experimental animal studies does not indicate direct or indirect harmful effects with respect to the development of the embryo or foetus, the course of gestation and pre-and post-natal development
• However, as with all medicinal products, mizolastine should be avoided in pregnancy, particularly during the first trimester

Breastfeeding

• Caution; not recommended
• Mizolastine is excreted into breast milk, therefore its use in breastfeeding women is not recommended

Renal Impairment

• Caution; no information available 

Hepatic Impairment

• Mild to moderate: Caution; no information available
• Severe: Contraindicated

Elderly

• No dose adjustment recommended
  Elderly may be particularly susceptible to the sedative effects of mizolastine and the potential effects of mizolastine on cardiac repolarisation
  

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Drowsiness
• Headache
• Dizziness
• Anxiety
• Depression
• Asthenia

Cardiovascular Disorders

• Hypotension
• Tachycardia
• Palpitations
• Vasovagal attack
• Prolonged QT interval

Respiratory Disorders

• Aggravation of asthma
• Bronchospasm

Gastrointestinal Disorders 

• Dry mouth
• Diarrhoea
• Abdominal pain
• Dyspepsia
• Nausea and vomiting
• Increased appetite

Hepatobiliary Disorders

• Increased hepatic enzymes

Endocrine and Metabolic Disorders

• Increased weight
• Minor changes in electrolytes
• Minor changes in blood sugar

Musculoskeletal Disorders

• Arthralgia
• Myalgia

Immune, Blood and Lymphatic System Disorders

• Low neutrophil count
• Allergic reactions
  - Anaphylaxis
  - Angioedema
  - Generalized rash/urticaria
  - Pruritis
  - Hypotension

• Macrolide antibiotics
• Systemic imidazole antifungals
• QT prolonging agents
• Class I and III antiarrhythmics
• CYP3A4 inhibitors
• Cimetidine
• Ciclosporin
• Nifedipine

None routine

Mizolastine possesses antihistamine and antiallergic properties due to a specific and selective antagonism of peripheral histamine H receptors. It has also been shown to inhibit histamine release from mast cells (at 0.3 mg/kg orally) and the migration of neutrophils (at 3 mg/kg orally) in animal models of allergic reactions.

Tablet 10mg

• Mizollen (Adcock Ingram) originator