Montelukast

Registered South African indications:

• Atopic asthma
  - Prophylaxis and chronic treatment

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Children under the age of 2 years as safety and efficacy has not been demonstrated (4mg chu, gra)
• Children under the age of 6 years, as safety and efficacy has not been demonstrated (5mg chu)
• Children under the age of 15 years (10mg tab)
• Pregnancy (chu, fct)
• Breastfeeding (chu, fct)

Additional contraindications related to certain formulations

• Allergy to peanut or soya as montelukast 10mg tablet contains soy lecithin (E-322) (peanut oil)

• Pregnancy (gra)
• Breastfeeding (gra)
• Severe hepatic impairment 
• Acute bronchospasm
• Abrupt withdrawal 
• Galactose intolerance
• Lapp lactase deficient
• Glucose-galactose malabsorption
• May influence ability to drive and operate machinery

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

South African registered indications and dosages

Atopic asthma
- Prophylaxis and chronic treatment

• Oral (fct, tab): 10mg, dly to be taken in the evening

Tablets may be taken with or without food. Advise patients to continue taking montelukast while their asthma is controlled, as well as during periods of worsening asthma

In those adult asthmatic patients, in whom montelukast is indicated for asthma, this may also provide some symptomatic relief of seasonal allergic rhinitis

Paed. forms avail. in SA and covered in this monograph: chu, gra, fct, tab

South African registered indications and dosages

Atopic asthma
- Prophylaxis and chronic treatment

Younger than 2 years

• Not established for use (see Contraindications)

Between 2-5 years

• Oral (gra): 4mg, dly to be taken in the evening

Between 6-14 years

• Oral (chu): 5mg, dly

Older than 15 years

• Oral (fct, tab): See adult dosage

Method of administration

Montelukast granules can be administered either directly in the mouth or mixed with a spoonful of cold or room temperature soft food (e.g., applesauce, ice cream, carrots and rice)
The sachet should not be opened until ready to use. After opening the sachet, the full dose of must be administered immediately (within 15 minutes). If mixed with food, montelukast granules must not be stored for future use. Montelukast granules are not intended to be dissolved in liquid for administration. However, liquids may be taken subsequent to administration. Montelukast granules can be administered without regard to the timing of food ingestion

Chewable tablet can be taken with or without food

In relation to other treatments for asthma montelukast granules can be added to a patient’s existing treatment regimen

The therapeutic effect of montelukast on parameters of asthma control occurs within one day. Advise patients to continue taking montelukast even if their asthma is under control, as well as during periods of worsening asthma

Montelukast chewable tablet 5mg has not been studied in seasonal allergic rhinitis in children with asthma

Pregnancy

South African recommendations

• Chu, fct: Contraindicated
• Gra: Caution; not recommended
• The safety of montelukast in pregnant women has not been established. Montelukast should not be used during pregnancy
• During worldwide marketing experience, congenital limb defects have been reported in offspring of women treated with montelukast during pregnancy. A causal relationship between these events and montelukast has not been established

Breastfeeding

South African recommendations

• Chu, fct: Contraindicated
• Gra: Caution; not recommended
• The safety of montelukast in lactating women has not been established
• It is unknown whether montelukast/metabolites are excreted in human milk
• Montelukast should not be used in breastfeeding mothers
• Studies in rats have shown that montelukast is excreted in milk

Fertility

South African recommendations

• No information available

• No dose adjustment recommended

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no dose adjustment recommended

• No dose adjustment recommended

Central Nervous System Disorders

• Headache
• Dizziness
• Drowsiness
• Paraesthesia
• Hypoesthesia
• Seizure
• Insomnia
• Somnambulism
• Anxiety
• Agitation
• Depression
• Psychomotor hyperactivity
• Disturbances in attention
• Memory impairment
• Hallucinations
• Disorientation
• Suicidal thinking and behaviour
• Fatigue
• Malaise

Cardiovascular Disorders

• Palpitations

Respiratory Disorders

• Epistaxis
• Churg-Strauss Syndrome
• Pulmonary eosinophilia
• Upper respiratory tract infection

Gastrointestinal Disorders

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

Hepatobiliary Disorders

• Elevated levels of serum transaminases
• Hepatitis

Musculoskeletal Disorders

• Arthralgia
• Myalgia

Skin and Subcutaneous Tissue Disorders

• Rash
• Bruising
• Urticaria
• Pruritus
• Angiooedema
• Erythema nodosum
• Erythema multiforme

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reactions
• Anaphylaxis
• Hepatic eosinophilic infiltration
• Increased bleeding tendency

• CYP3A4 inducers
• CYP3A4 inhibitors  

None routine

Montelukast is a selective leukotriene receptor antagonist that inhibits the cysteinyl leukotriene-1 (CysLT-1) receptor. Cysteinyl leukotrienes bind to CysLT receptors found in the airway and have been correlated with pathophysiology of asthma and allergic rhinitis, including bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitmentIn allergic rhinitis, CysLT is released from the nasal mucosa after allergen exposure.

Sprinkles 4mg

• Monte-Air (MSD)
• Singulair (MSD) originator

Tablet chew 4mg

• Belair (Camox)
• Dilair (Ranbaxy)
• Glenmont (Glenmark)
• Kulair (Brimpharm) 
• Lumont (Zydus)
• Minair (Akacia)
• Monte-Air (MSD)
• Montelukast Chew Biotech (Biotech)
• Montelukast Cipla (Cipla)
• Montelukast Specpharm (Specpharm)
• Montelukast Unicorn (Sandoz)
• Monteflo (Trinity)
• Sintair (Pharma Dynamics)
• Sintrine (Sandoz)
• Singulair (MSD) originator
• Topraz (Dr Reddy Lab)

Tablet chew 5mg

• Belair (Camox)
• Dilair (Ranbaxy)
• Glenmont (Glenmark)
• Kulair (Brimpharm) 
• Lumont (Zydus)
• Minair  (Akacia)
• Monte-Air (MSD)
• Montelukast Chew Biotech (Biotech)
• Montelukast Cipla (Cipla)
• Montelukast Specpharm (Specpharm)
• Montelukast Unicorn (Sandoz)
• Monteflo (Trinity)
• Sintair (Pharma Dynamics)
• Sintrine (Sandoz)
• Singulair (MSD) originator
• Topraz (Dr Reddy)

Tablet 10mg

• Belair (Camox)
• Dilair (Ranbaxy)
• Glenmont (Glenmark)
• Kulair (Brimpharm) 
• Lumont (Zydus)
• Minair (Akacia)
• Monte-Air (MSD)
• Montelukast Biotech (Biotech)
• Montelukast Cipla (Cipla)
• Montelukast LCH 10 (LHC Pharmaceuticals)
• Montelukast Specpharm (Specpharm)
• Montelukast Unicorn (Sandoz)
• Monteflo (Trinity Pharm)
• Sintair (Pharma Dynamics)
• Sintrine (Sandoz)
• Singulair (MSD) originator
• Topraz (Dr Reddy)