Salbutamol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Inhalation/Respiratory
Acute bronchospasm
Adult: Treatment and prevention in patient with reversible obstructive airway disease: As metered-dose aerosol or dry powder inhaler (90 or 100 mcg/actuation): 1 or 2 inhalations every 4-6 hours. Max: 800 mcg daily.
Child: As metered-dose aerosol or dry powder inhaler: 4-11 years 1 or 2 inhalations; ≥12 years Same as adult dose.

Inhalation/Respiratory
Prophylaxis of exercise-induced bronchospasm
Adult: As metered-dose aerosol or dry powder inhaler (90 or 100 mcg/actuation): 2 inhalations 15-30 minutes prior to exercise.
Child: As metered-dose aerosol or dry powder inhaler (90 or 100 mcg/actuation): 4-11 years 1 or 2 inhalations 15-30 minutes prior to exercise; ≥12 years Same as adult dose.

Inhalation/Respiratory
Chronic bronchospasm
Adult: Via nebuliser: 2.5-5 mg up to 3-4 times daily.
Child: ≥4 years Same as adult dose.

Intravenous
Severe bronchospasm
Adult: As 50 mcg/mL solution: 250 mcg (4 mcg/kg) via slow inj. May be repeated if necessary. As 10mcg/mL solution via infusion: Usual rate of 3-20 mcg/min, adjusted according to patient needs.
Child: ≥12 years Same as adult dose.

Intravenous
Uncomplicated premature labour
Adult: For arrest of preterm labour between 22 and 37 weeks of gestation: Initially, 10 mcg/min, increased at 10-minute intervals until there is response; then increase infusion rate slowly until contractions cease. Usual dose: 10-45 mcg/min. Maintain infusion at rate at which contractions stop for 1 hour, then reduce by decrements of 50% at intervals of 6 hours. Max treatment duration: 48 hours.

Oral
Bronchospasm
Adult: Treatment and prevention in patient with reversible obstructive airway disease: As syr/immediate-release tab: 2-4 mg 3-4 times daily, may be increased up to max 8 mg 3-4 times daily as tolerated. As extended-release tab: 4-8 mg 12 hourly.
Elderly: As syr/immediate-release tab: Initially, 2 mg 3 or 4 times daily.
Child: As syr/immediate-release tab: 2-6 years 1-2 mg; >6-12 years 2 mg; >12 years Same as adult dose. All doses are given 3 or 4 times daily. As extended-release tab: 6-12 years 4 mg 12 hourly.

Parenteral
Severe bronchospasm
Adult: 50 mcg given via SC or IM injection given 4 hourly, as required.
Child: ≥12 years Same as adult dose.
Hướng dẫn pha thuốc
IV inj: Dilute ampoule labelled as containing 500 mcg/mL with 10 mL of water for injection to provide a solution containing 50 mcg/mL. IV infusion: Dilute 5 mL salbutamol inj with 500 mL NaCl or dextrose inj to a concentration of 10 mcg/mL.
Chống chỉ định
IV (in the treatment of premature labour): Pre-existing or risk factors for ischaemic heart disease, gestational age <22 weeks, conditions in which prolongation of pregnancy is hazardous, intrauterine foetal death, known lethal congenital or lethal chromosomal malformation, pulmonary hypertension. Non-IV formulation is not indicated for use in uncomplicated premature labour or threatened abortion.
Thận trọng
Patient with CV disease (e.g. arrythmia, coronary insufficiency, hypertension, heart failure), diabetes mellitus, glaucoma, hyperthyroidism, hypokalaemia, seizures. Renal impairment. Children and elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Hypersensitivity reactions (e.g. urticaria, angioedema, rash, bronchospasm, oropharyngeal oedema), hypokalaemia (high doses).
Cardiac disorders: Tachycardia, palpitations, chest pain. Rarely, cardiac arrythmias (e.g. atrial fibrillation, supraventricular tachycardia, extrasystoles), myocardial ischaemia.
Gastrointestinal disorders: Nausea, vomiting, mouth and throat irritation (inhalation).
General disorders and administration site conditions: Weakness.
Metabolism and nutrition disorders: Hyperglycaemia. Rarely, lactic acidosis (high doses).
Musculoskeletal and connective tissue disorders: Muscle cramps.
Nervous system disorders: Tremor, headache, dizziness, drowsiness, restlessness.
Psychiatric disorders: Nervousness, irritability, insomnia.
Respiratory, thoracic and mediastinal disorders: Pharyngitis, rhinitis, pulmonary oedema (parenteral).
Vascular disorders: Peripheral vasodilation, flushing.
Potentially Fatal: Rarely, paradoxical bronchospasm.
Inhalation/Respiratory/IV/Parenteral/PO: C
Chỉ số theo dõi
Monitor FEV1 peak flow, and/or other pulmonary function tests; blood pressure, heart rate, CNS stimulation; serum glucose, K and creatinine; asthma symptoms; arterial or capillary blood gases if needed; lactate, and ECG (IV).
Quá liều
Symptoms: Tachycardia, tremor, hyperactivity, metabolic effects (e.g. hypokalaemia, lactic acidosis), headache, nervousness, dry mouth, palpitations, dizziness, fatigue, malaise, insomnia, arrhythmias, anginal pain, seizures. Children may experience nausea, vomiting, hyperglycaemia when taken orally. Management: Symptomatic treatment. Monitor serum K and lactate levels. May give cardioselective β-blocker with caution. May give oral or IV potassium for hypokalaemia as needed.
Tương tác
Increased risk of hypokalaemia with corticosteroids, diuretics (e.g. loop, thiazide) and xanthines (e.g. theophylline). Increased vascular effects with MAOIs, tricyclic antidepressants (TCAs). May cause severe bronchospasm when used with β-blockers (e.g. propranolol). May decrease serum concentrations of digoxin.
Tác dụng
Description:
Mechanism of Action: Salbutamol is a direct-acting sympathomimetic that acts on β2-receptors to relax bronchial smooth muscle with less prominent effect on the heart. It activates adenyl cyclase, the enzyme that stimulates the production of cyclic adenosine-3', 5'-monophosphate (cAMP). Increased cAMP leads to activation of protein kinase A, which inhibits phosphorylation of myosin and lowers intracellular ionic Ca concentrations, resulting in muscle relaxation.
Synonym: albuterol
Onset: ≤5 minutes (inhalation); 5.4-8.2 minutes (oral inhalation); ≤30 minutes (oral).
Duration: Inhalation: 3-6 hours. Oral inhalation: Approx 2-6 hours. Oral: 6-8 hours (immediate-release); up to 12 hours (extended-release).
Pharmacokinetics:
Absorption: Readily absorbed from the gastrointestinal tract. Time to peak plasma concentration: Inhalation: 30 minutes. Oral inhalation: 25-30 minutes. Oral: ≤2 hours (immediate-release); 6 hours (extended release). Bioavailability: Approx 50%.
Distribution: Crosses the placenta. Plasma protein binding: 10%.
Metabolism: Metabolised in the liver to an inactive sulfate conjugate.
Excretion: Mainly via urine (80-100% [oral inhalation]; 76% over 3 days, [60% as metabolite; oral]); faeces (<20% [oral inhalation]; 4% [oral]). Elimination half-life: Oral inhalation: 3.8 to approx 5 hours. Oral: 5-6 hours (immediate-release); 9.3 hours (extended-release). IV: 4-6 hours.
Đặc tính

Chemical Structure Image
Salbutamol

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2083, Salbutamol. https://pubchem.ncbi.nlm.nih.gov/compound/Salbutamol. Accessed Oct. 24, 2023.

Bảo quản
Dry powder or metered dose inhalers/tab/syr: Store below 25°C. Solution for inj/nebule: Store below 30°C. Protect from light.
Phân loại MIMS
Thuốc trị hen & bệnh phổi tắc nghẽn mạn tính / Thuốc tác dụng lên tử cung
Tài liệu tham khảo
Albuterol Sulfate Aerosol, Metered (Perrigo New York Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/05/2020.

Albuterol Sulfate Inhalant (Cipla USA Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/05/2020.

Albuterol Sulfate Inhalation Solution (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/05/2020.

Albuterol Sulfate Syrup (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/05/2020.

Albuterol Sulfate Tablet (Dash Pharmaceutical LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/05/2020.

Albuterol Sulfate Tablet, Film Coated, Extended Release (Mylan Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/06/2020.

Anon. Albuterol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/05/2020.

Buckingham R (ed). Salbutamol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/05/2020.

Easyhaler Salbutamol Sulfate 200 mcg per Actuation Inhalation Powder (Orion Corporation). MHRA. https://products.mhra.gov.uk/. Accessed 05/05/2020.

GlaxoSmithKline NZ Limited. Ventolin Injection 500 mcg/mL, Ventolin Solution for Intravenous Infusion 5 mg/5 mL data sheet 17 December 2018. Medsafe. http://www.medsafe.govt.nz/. Accessed 05/05/2020.

Joint Formulary Committee. Salbutamol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/05/2020.

Salbutamol Syrup 2 mg/5 mL (Pinewood Laboratories Limited). MHRA. https://products.mhra.gov.uk/. Accessed 05/05/2020.

Salbutamol Tablets BP 4 mg (Accord-UK Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 05/05/2020.

Ventolin Injection 500 mcg in 1 mL (Glaxo Wellcome UK Ltd.). MHRA. https://products.mhra.gov.uk/. Accessed 05/05/2020.

Ventolin Nebules 5 mg (Glaxo Wellcome UK Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 05/05/2020.

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