Salbutamol

Registered South African indications:

• Relief of bronchospasm
  - Bronchial asthma of all types
  - Chronic bronchitis
  - Emphysema
• Prophylaxis of bronchospasm in exercise-induced asthma

Contraindications

International manufacturer recommendations

• Hypersensitivity to the active ingredient or any of its excipients
• Use to arrest uncomplicated premature labour or threatened abortion (non-IV salbutamol formulations)
• Severe milk-protein allergy (acc)

South African manufacturer recommendations

• Hypersensitivity to the active ingredient or any of its excipients
• Managing premature labour or threatened abortion 
• Severe milk-protein allergy (acc)

Cautions

International manufacturer recommendations

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Only or main treatment in patients with severe or unstable asthma
• Increase in dosage or frequency
• Underlying severe heart disease
  - Ischaemic heart disease (including myocardial ischaemia)
  - Arrhythmia (including tachyarrhythmia)
  - Severe heart failure
  - Cardiac insufficiency
  - Hypertrophic obstructive cardiomyopathy
• Thyrotoxicosis
• Hypokalaemia
• Acute severe asthma
• Diabetes mellitus
• Hypoxia
• Coadministration with xanthine derivatives, corticosteroids or diuretics
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

South African manufacturer recommendations

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly (inh)
• Thyrotoxicosis
• Hyperthyroidism
• Cardiovascular disorders/ underlying severe heart disease
  - Ischaemic heart disease
  - Angina pectoris
  - Tachycardia
  - Dysrhythmias
  - Hypertension
• Increase in dosage or frequency
• Acute severe asthma
• Hypokalaemia
• Hypoxia
• Presence of acidosis
• Coadministration with other sympathomimetic medicines
• Coadministration with xanthine derivatives, corticosteroids or diuretics
• Coadministration with beta blockers
• Galactose intolerance (acc)
• Lapp lactase deficiency (acc)
• Glucose-galactose malabsorption (acc)
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: acc, inh

Dosages below include:

• International manufacturer recommendations
• South African manufacturer recommendations

International manufacturer recommendations

100μg inhaler

Asthma - mild, moderate or severe
- Relief of acute asthma symptoms including bronchospasm

• Inhaled (inh): Initial: 100μg, as a single minimum starting dose; Increase to 200μg, if needed

- Prevention of allergen- or exercise-induced symptoms

• Inhaled (inh): 200μg, taken 10-15mins before challenge

- Chronic therapy

• Inhaled (inh): 200μg, up to 6hrly; Max: 800μg/24hrs

200μg inhaler

Asthma - mild, moderate or severe
- Relief of acute bronchospasm
- Managing intermittent episodes of asthma

• Inhaled (inh): 200μg, as a single dose; Increase to 400μg, if needed

- Prevention of exercise-induced bronchospasm or allergen bronchospasm

• Inhaled (inh): 200μg, before challenge; Repeat dose if needed

200μg accuhaler

Management of asthma and/or bronchospasm
Reversible airways obstruction
- Relief of acute bronchospasm

• Inhaled (acc): 200μg, as a single dose; Max: 200μg, 6hrly OR 800μg/24hrs

- Prevention of allergen- or exercise-induced symptoms

• Inhaled (acc): 200μg, taken 10-15mins before challenge

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It should be used to relieve symptoms when they occur, and to prevent them in those circumstances recognised by the patient to precipitate an asthma attack (e.g. before exercise or unavoidable allergen exposure)

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On-demand use of salbutamol inhaler should not exceed 8 inhalations in any 24hrs. Reliance on such frequent supplementary use, or a sudden increase in dose, indicates poorly controlled or deteriorating asthma

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Salbutamol is particularly valuable as relief medication in mild, moderate or severe asthma, provided that reliance on it does not delay the introduction and use of regular inhaled corticosteroid therapy

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Salbutamol inhaler may be used with a volumatic spacer device by patients who find it difficult to synchronise aerosol actuation with inspiration of breath

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South African manufacturer recommendations

Relief of bronchospasm
- Bronchial asthma of all types
- Chronic bronchitis
- Emphysema

• Inhaled (inh): 100-200μg, 4hrly, as required
• Inhaled (acc): 200μg, 6hrly, as required; Max: 800μg/24hrs

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Reliance on supplementary use or a sudden increase in dose indicates deteriorating asthma

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The bronchodilator effect of each administration of salbutamol lasts for ≥4hrs and more frequent use should not be necessary

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The patient can readily recognise any reduction in the length of action and should be instructed to consult a doctor if the effect of a previously adequate dose lasts for <3hrs

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See additional prescribing points

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Prevention of allergen or exercise-induced bronchospasm

• Inhaled (acc): 200μg, before exercise

Chronic therapy

• Inhaled (acc): 200μg, 6hrly; Max: 800μg/24hrs

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No information available for 200μg inhaler 

Paed. forms avail. in SA and covered in this monograph: acc, inh

Paed. dosages below include:

• International manufacturer recommendations
• South African manufacturer recommendations

International manufacturer recommendations

100μg inhaler

Asthma - mild, moderate or severe
- Relief of acute bronchospasm

Younger than 12 years

• Inhaled (inh): Initial: 100μg, as a single minimum starting dose; Increase to 200μg, if needed

12 years and older

• See adult dosage

- Prevention of allergen- or exercise-induced bronchospasm

Younger than 12 years

• Inhaled (inh): 100μg, before challenge or exertion; Increase to 200μg, if needed

12 years and older

• See adult dosage

- Chronic therapy

Younger than 12 years

• Inhaled (inh): 100-200μg, up to 6hrly; Max: 800μg/24hrs

12 years and older

• See adult dosage

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The baby spacer device may be used to facilitate administration to children under 5 years of age

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200μg inhaler, 200μg accuhaler

Relief of acute bronchospasm

Younger than 4 years

• No information available

Between 4-11 years

• Inhaled (inh): 200μg, as needed

12 years and older

• See adult dosage

Prevention of exercise-induced bronchospasm or allergen bronchospasm

Younger than 4 years

• No information available

Between 4-11 years

• Inhaled (inh): 200μg, before challenge or exertion

12 years and older

• See adult dosage

Chronic therapy

Younger than 4 years

• No information available

Between 4-11 years

• Inhaled (inh): 200μg, 6hrly; Max:800μg/24hrs

12 years and older

• See adult dosage

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100μg and 200μg inhaler: On-demand use of salbutamol inhaler should not exceed 8 inhalations in any 24hrs. Reliance on such frequent supplementary use, or a sudden increase in dose, indicates poorly controlled or deteriorating asthma

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For optimum results in most patients salbutamol inhaler should be used regularly during asthmatic attacks. The bronchodilator effect of each administration of inhaled salbutamol lasts for 4 hours, except in patients whose asthma is becoming worse. Such patients should be warned not to increase their usage of salbutamol, but should seek medical advice in case treatment with an inhaled and/or systemic glucocorticosteroid is indicated

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South African manufacturer recommendations

100μg inhaler

Relief of bronchospasm
- Bronchial asthma of all types
- Chronic bronchitis
- Emphysema

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No specific paediatric recommendations are available in SA manufacturer recommendations

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200μg accuhaler

Relief of bronchospasm
- Bronchial asthma of all types
- Chronic bronchitis
- Emphysema
Prevention of allergen or exercise-induced bronchospasm
Chronic therapy

Younger than 5 years

• No information available

5 years and older

• See adult dosage

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No information available for 200μg inhaler 

Pregnancy

International manufacturer recommendations

• Caution
• Administration of drugs during pregnancy should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus
• As with the majority of drugs, there is little published evidence of the safety of salbutamol in the early stages of human pregnancy, but in animal studies there was evidence of some harmful effects on the foetus at very high dose levels

South African manufacturer recommendations

• Caution
• Safety in pregnant women has not been established
• No controlled clinical trials with salbutamol have been conducted in pregnant women
• Reports of various congenital anomalies following intrauterine exposure to salbutamol (including cleft palate, limb defects and cardiac disorders) have been received. Studies in animals have shown reproductive toxicity

Breastfeeding

International manufacturer recommendations

• Caution
• As salbutamol is probably secreted in breast milk, its use in breastfeeding mothers requires careful consideration
• It is not known whether salbutamol has a harmful effect on the neonate, and so its use should be restricted to situations where it is felt that the expected benefit to the mother is likely to outweigh any potential risk to the neonate

South African manufacturer recommendations

• Caution
• As salbutamol is probably secreted in breast milk, its use in breastfeeding mothers requires careful consideration. It is not known whether salbutamol has a harmful effect on the neonate, safety in breastfeeding has not been established

Fertility

• There is no information on the effects of salbutamol on human fertility. There were no adverse effects on fertility in animals

Renal Impairment

• Caution; no information available

Hepatic Impairment

• Caution; no information available

Elderly

International manufacturer recommendations

• No dose adjustment recommended

South African manufacturer recommendations

• No dose adjustment recommended (acc)
• Caution; no information available (inh)

Porphyria Information

• Not porphyrinogenic (NP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Tremor
• Headache
• Hyperactivity
• Restlessness
• Dizziness

Cardiovascular Disorders

• Tachycardia
• Palpitations
• Cardiac arrhythmias
  - Atrial fibrillation
  - Supraventricular tachycardia
  - Extrasystoles
• Myocardial ischaemia
• Peripheral vasodilatation

Respiratory Disorders

• Paradoxical bronchospasm
• Cough

Gastrointestinal Disorders

• Mouth and throat irritation

Endocrine and Metabolic Disorders

• Hypokalaemia (Potentially serious hypokalaemia may result from beta₂ agonist therapy)

Musculoskeletal Disorders

• Muscle cramps

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity reactions
  - Angioedema
  - Urticaria
  - Bronchospasm
  - Hypotension
  - Collapse

• Non-selective beta blocking agents
• Propanolol

• Pulmonary function tests
  - Forced expiratory volume (FEV1)
  - Peak flow
• Blood pressure
• Heart rate
• Serum glucose
• Serum potassium
• Serum creatinine

Additional observations

• CNS stimulation
• Asthma symptoms
• Arterial or capillary blood gases

Important considerations for use

South African manufacturer recommendations

• Salbutamol acts rapidly and may be used when necessary to relieve attacks of acute dyspnoea. Doses may be taken prophylactically before exertion to prevent exercise-induced asthma
• Bronchodilators should not be the only or main treatment in patients with severe or unstable asthma. Severe asthma requires regular medical assessment as the condition is potentially life-threatening
• Patients with severe asthma have constant symptoms and frequent exacerbations, with limited physical capacity, and PEF values below 60% predicted at baseline with greater than 30% variability, usually not returning entirely to normal after a bronchodilator. These patients will require inhaled corticosteroid therapy
• Failure to respond promptly or fully to such rescue medicine signals a need for urgent medical advice and treatment

Salbutamol is a selective beta₂-adrenoceptor agonist. At therapeutic doses it acts on the beta₂-adrenoceptors of bronchial muscle, with little or no action on the beta₁-adrenoceptors of cardiac muscle. Salbutamol provides short-acting (4-6hr) bronchodilation with a fast onset (within 5mins) in reversible airways obstruction

Inhaler 100μg

• Asthavent Inhaler (Cipla Medpro)
• Asthavent Ecohaler (Cipla Medpro)
• Airomir Inhaler (iNova) originator
• Azmaler (Forrester Pharma)
• Glenbute (Glenmark Pharmaceuticals South Africa)
• Ventimax CFC Free (Biotec)
• Venteze CFC free (Pharmacare)
• Venteze Ecohaler (Pharmacare)
• Venteze Inhaler (Pharmacare)
• Venteze Complete (Pharmacare)

Inhaler 200μg

• Ventolin CFC-Free (GSK) originator

Accuhaler 200μg

• Ventolin Accuhaler (GSK) originator

Also available in the following forms: Nebule, solution, syrup, tablet and injection.

COMBINATION PREPARATIONS

Salbutamol/ Ipratropium bromide anhydrous

Solution U.D.V (per 2.5ml) 2.5mg/0.5mg

• Combivent U.D.V (Ingelheim) originator

Solution (per 2.5ml) 2.5mg/0.5mg

• Sabax Combined (Adcock) 

Solution U.D.V (per 2.5ml) 3mg/0.5mg

• Co-iprasal Solution (Arrow)

Inhaler 100μg/20μg

• Duolin Hfa (Cipla)