Rupatadine

Registered South African indications:

• Symptomatic treatment of allergic rhinitis and urticaria

Contraindications

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Children below 2 years of age (sol)
• Children below 12 years of age (tab)
• Pregnancy
• Breastfeeding

Contraindications registered in other jurisdictions

• Hypersensitivity to the active ingredient or any of its excipients

Cautions

• Pregnancy (Recommendations in other jurisdictions)
• Breastfeeding (Recommendations in other jurisdictions)
• Renal impairment
• Hepatic impairment
• Elderly
• Known prolongation of QT interval
• Uncorrected hypokalaemia
• Ongoing proarrhythmic conditions
• Bradycardia
• Acute myocardial ischaemia
• Coadministration with any substrate for alcohol dehydrogenase (in children <5 years) (sol)
• Coadministration with grapefruit juice
• Coadministration with CYP3A4 inhibitors and substrates
• Galactose intolerance (tab)
• Total lactase deficiency (tab)
• Glucose-galactose malabsorption
• Fructose intolerance (sol)
• Sucrase-isomaltase insufficiency (sol)
• May impair ability to drive and operate machinery

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

South African registered indications and dosages

Symptomatic treatment of allergic rhinitis and urticaria

• Oral (tab): 10mg, dly with or without food

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

South African registered indications and dosages

Symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) and urticaria

Oral (sol)

• Younger than 2 years: Contraindicated
• Between 2-11 years: ≥10-<25kg: 2.5mg, dly with or without food
• Between 2-11 years: ≥25kg: 5mg, dly with or without food
• 12 years and older: Admin. of tablets more appropriate, see adult dosage

The administration of rupatadine solution to children under 2 years of age is not recommended due to the lack of data in this population

Symptomatic treatment of allergic rhinitis and urticaria

Oral (tab)

• Younger than 12 years: Contraindicated
• 12 years and older: See adult dosage

Rupatadine tablets are not recommended for use in children below 12 years of age

Pregnancy

South African recommendations

• Contraindicated (sol, tab)
• Data on a limited number (2) of exposed pregnancies indicate no adverse effects of rupatadine on pregnancy or on the health of the foetus/newborn child (sol)
• To date, no other relevant epidemiological data are available (sol)
• Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development (sol)
• As a precautionary measure, it is preferable to avoid the use of rupatadine during pregnancy (sol)

Recommendations in other jurisdictions

• Caution; not recommended (sol, tab) 
• There are limited amount of data from the use of rupatadine in pregnant women (tab)
• Data on a limited number (2) of exposed pregnancies indicate no adverse effects of rupatadine on pregnancy or on the health of the foetus/newborn child. To date, no other relevant epidemiological data are available (sol)
• Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/ foetal development, parturition or postnatal development. As a precautionary measure, it is preferable to avoid the use of rupatadine during pregnancy (sol, tab) 

Breastfeeding

South African recommendations

• Contraindicated (sol, tab)
• Rupatadine is excreted in animal milk. It is unknown whether rupatadine is excreted into breast milk (sol)
• Due to potential harmful effects in neonates, the use of rupatadine should be avoided during breastfeeding (tab)
• A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from rupatadine therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman (sol)

Recommendations in other jurisdictions

• Caution; not recommended (sol, tab) 
• Rupatadine is excreted in animal milk. It is unknown whether rupatadine is excreted into breast milk. A decision must be made whether to discontinue breastfeeding or to discontinue/ abstain from rupatadine therapy taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman (sol, tab)
• While propylene glycol has not been shown to cause reproductive or developmental toxicity in animals or humans, it was found in milk. As a consequence, administration of propylene glycol to breastfeeding patients should be considered on a case by case basis (sol)

Fertility

Recommendations below are applicable to South Africa and other jurisdictions

• There are no clinical data on fertility. Studies in animals have shown a significant reduction of fertility at exposure levels higher than those observed in humans at the maximum therapeutic dose

Recommendations below are applicable to South Africa and other jurisdictions

• Caution; not recommended
  As there is no clinical experience in patients with impaired kidney function, the use of rupatadine is at present not recommended in these patients

Recommendations below are applicable to South Africa and other jurisdictions

• Caution; not recommended
  As there is no clinical experience in patients with impaired  liver function, the use of rupatadine is at present not recommended in these patients

Recommendations below are applicable to South Africa and other jurisdictions

• Caution; no dose adjustment recommended
  Rupatadine should be used with caution in patients 65 years and older
  Although no overall differences in effectiveness or safety were reported in clinical trials, higher sensitivity of some older individuals cannot be excluded
   

Central Nervous System Disorder

• Somnolence
• Disturbance in attention
• Headache
• Dizziness
• Fatigue
• Irritability

Cardiovascular Disorders

• Tachycardia
• Palpitations

Respiratory Disorders

• Pharyngitis
• Nasopharyngitis
• Upper respiratory tract infection
• Rhinitis
• Cough
• Dry throat
• Epistaxis
• Nasal dryness
• Oropharyngeal pain

Gastrointestinal Disorders

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

Hepatobiliary Disorders

• Abnormal hepatic function tests
• Increased alanine aminotransferase
• Increased aspartate aminotransferase

Endocrine and Metabolic Disorders

• Increased appetite
• Thirst
• Increased weight

Musculoskeletal Disorders

• Back pain
• Arthralgia
• Myalgia
• Increased blood creatine phosphokinase

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reactions
• Anaphylactic reactions
• Fever
• Eosinophilia
• Neutropenia

Skin and Subcutaneous Tissue Disorders

• Rash
• Angioedema
• Urticaria
• Eczema

Others

• Influenza
• Night sweats

• CYP3A4 inhibitors
• Itraconazole
• Ketoconazole
• Voriconazole
• Posaconazole
• HIV protease inhibitors
• Clarithromycin
• Nefazodone
• Erythromycin
• Fluconazole
• Diltiazem
• CYP3A4 substrates
• Central nervous system depressants
• Midazolam
• Statins
• Simvastatin
• Lovastatin
• Ciclosporin
• Tacrolimus
• Sirolimus
• Everolimus
• Cisapride

Other interactions

• Alcohol
• Grapefruit juice

None routine. Specific cases may require

• Renal function
• Hepatic function

Rupatadine is a second-generation antihistamine, long-acting histamine antagonist, with selective peripheral H-receptor antagonist activity. Some of the metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug.

Tablet 10mg

• Raztrol (Ranbaxy Pharmaceuticals)
• Rupanase 10 (iNova Pharmaceuticals) originator
• Rupallerg 10 (iNova Pharmaceuticals)
• Zealargy (Pharma-Q)

Oral solution (per ml) 1mg

• Rupanase Junior (iNova Pharmaceuticals)) originator