Salbutamol

R03A - Adrenergics, inhalants ATC R03CC02 Small molecule approved 1981 Oral Topical Natural product Black-box warning

JFDA label: Asmanore 2mg tablet

⚠ Black-Box Warning

Mechanism of Action

Agonist of Beta-2 adrenergic receptor — Beta-2 adrenergic receptor agonist

Target	Action	Gene / class
Beta-2 adrenergic receptor efficacy	AGONIST	ADRB2

Indications

Approved

Bronchospasm
Exercise-induced bronchospasm

Off-label

Asthma (children younger than 4 years) (metered-dose inhaler)
Hyperkalemia (Inhalation)

Contraindications

Source: Lexicomp

Additional contraindications (not in US labeling): Injection: Ventolin: Hypersensitivity to albuterol or any component of the formulation Absolute
Inhalation, Oral: Hypersensitivity to albuterol or any component of the formulation Absolute
risk of abortion during first or second trimester Inhalation: Tocolytic use in patients at risk of premature labor or threatened abortion Absolute
severe hypersensitivity to milk proteins (dry powder inhalers) Absolute
tachyarrhythmias Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (3)

Common chest pain, headache, dizziness, diabetes mellitus, vomiting, unpleasant taste, gastroenteritis, increased appetite, viral gastroenteritis, diarrhea, difficulty in micturition · hypertension · Tachycardia

Nervous system disorders (2)

Very Common Excitement · nervousness

Hepatobiliary disorders (2)

Common Increased serum ALT · increased serum AST

Blood and lymphatic system disorders (4)

Common Decreased hematocrit · decreased hemoglobin · decreased white blood cell count · lymphadenopathy

Immune system disorders (1)

Common Hypersensitivity reaction

Musculoskeletal and connective tissue disorders (6)

Very Common Tremor

Common back pain · hyperkinesia · leg cramps · Muscle cramps · musculoskeletal pain

Ear and labyrinth disorders (2)

Common ear disease, viral upper respiratory tract infection, respiratory tract disease, nasopharyngitis, oropharyngeal pain, sinusitis, upper respiratory tract inflammation, cough, flu-like symptoms, dyspnea · Otitis media

Infections and infestations (2)

Common Cold symptoms · infection

Respiratory, thoracic and mediastinal disorders (5)

Very Common bronchospasm · exacerbation of asthma · pharyngitis · rhinitis · Upper respiratory tract infection

Dosing

Source: Lexicomp

Bronchospasm: Inhalation: Metered-dose inhaler (MDI) or dry powder inhaler (90 mcg/actuation): 2 inhalations every 4 to 6 hours as needed (NAEPP 2007) Metered-dose inhaler (100 mcg/actuation): Airomir [Canadian product]: Acute treatment: 1 to 2 inhalations; additional inhalations may be necessary every 4 to 6 hours as needed if inadequate relief however patients should be advised to promptly consult health care provider or seek medical attention if no relief from acute treatment (additional inhalations or more frequent administration is not recommended) Maintenance (in combination with corticosteroid therapy): 1 to 2 inhalations every 4 to 6 hours as needed (maximum: 8 inhalations daily) Dry powder inhaler (200 mcg/inhalation): Ventolin Diskus [Canadian product]: Acute treatment: 1 inhalation (200 mcg) as needed; maximum: 4 inhalations (800 mcg)/day; patient should be advised to promptly consult health care provider or seek medical attention if prior dose fails to provide adequate relief or if control of symptoms lasts Maintenance (in combination with corticosteroid therapy): 1 inhalation (200 mcg) every 4 to 6 hours; maximum: 4 inhalations (800 mcg)/day Nebulization solution: 2.5 mg 3 to 4 times daily as needed; Quick relief: 1.25 to 5 mg every 4 to 8 hours as needed (NAEPP 2007) Oral: Note: Oral is not the preferred route for treatment of asthma; inhalation via nebulization or MDI is preferred (NAEPP 2007). Regular release: 2 to 4 mg/dose 3 to 4 times daily; maximum dose not to exceed 32 mg daily (divided doses) Extended release: 8 mg every 12 hours; maximum dose not to exceed 32 mg/day (divided doses). A 4 mg dose every 12 hours may be sufficient in some patients, such as adults of low body weight. IV continuous infusion [Canadian product]: Severe bronchospasm and status asthmaticus: Initial: 5 mcg/minute; may increase up to 10 to 20 mcg/minute at 15- to 30-minute intervals if needed Exacerbation of asthma (acute, severe) (NAEPP 2007): Inhalation: Metered-dose inhaler or dry powder inhaler (90 mcg/actuation): 4 to 8 inhalations every 20 minutes for up to 4 hours, then every 1 to 4 hours as needed Nebulization solution: 2.5 to 5 mg every 20 minutes for 3 doses, then 2.5 to 10 mg every 1 to 4 hours as needed, or 10 to 15 mg/hour by continuous nebulization Exercise-induced bronchospasm (prevention): Inhalation: Metered-dose inhaler or dry powder inhaler (90 mcg/actuation): 2 inhalations 5 minutes prior to exercise (NAEPP 2007) Metered-dose inhaler (100 mcg/actuation): Airomir [Canadian product]: 2 inhalations 30 minutes prior to exercise Dry powder inhaler (200 mcg/inhalation): Ventolin Diskus [Canadian product]: 1 inhalation (200 mcg) 15 minutes before exercise Hyperkalemia (off-label use): Inhalation: Nebulization solution: 10 to 20 mg over 10 minutes in combination with other recommended therapies (Putcha 2007; Wong 1999)

(For additional information see "Albuterol (salbutamol): Pediatric drug information") Bronchospasm: Inhalation: Metered-dose inhaler or dry powder inhaler (90 mcg/actuation) (NAEPP 2007): Quick relief: Children and Adolescents: Refer to adult dosing. Metered-dose inhaler (100 mcg/actuation): Airomir [Canadian product]: Children 6 to 11 years: Acute treatment: 1 inhalation; additional inhalations may be necessary every 4 to 6 hours as needed if inadequate relief; however, patients should be advised to promptly consult health care provider or seek medical attention if no relief from acute treatment (additional inhalations or more frequent administration is not recommended) Maintenance (in combination with corticosteroid therapy): 1 inhalation every 4 to 6 hours as needed (maximum: 4 inhalations daily) Children ≥12 years and Adolescents: Refer to adult dosing. Dry powder inhaler (200 mcg/inhalation): Ventolin Diskus [Canadian product]: Children ≥4 years and Adolescents: Refer to adult dosing. Nebulization solution: Manufacturer's recommendations: Children 2 to 12 years: Initial: 10 to 15 kg: 0.63 to 1.25 mg 3 to 4 times daily as needed; titrate dose based on clinical response (maximum: 10 mg/day) >15 kg: 0.63 to 2.5 mg 3 to 4 times daily as needed; titrate dose based on clinical response (maximum: 10 mg/day) Children ≥12 years and Adolescents: 2.5 mg 3 to 4 times daily as needed Alternative recommendations (NAEPP 2007): Quick relief: Children ≤4 years of age: 0.63 to 2.5 mg every 4 to 6 hours as needed Children ≥5 years of age and Adolescents: Refer to adult dosing. Oral: Note: Oral is not the preferred route for treatment of asthma; inhalation via nebulization or MDI is preferred (NAEPP 2007). Regular release: Children 2 to 6 years: 0.1 to 0.2 mg/kg/dose 3 times daily (maximum: 12 mg daily) Children 6 to 12 years: 2 mg/dose 3 to 4 times daily (maximum: 24 mg daily) Children >12 years and Adolescents: 2 to 4 mg/dose 3 to 4 times daily (maximum: 32 mg daily) Extended release: Children 6 to 12 years: 4 mg every 12 hours (maximum: 24 mg daily) Children >12 years and Adolescents: 8 mg every 12 hours (maximum: 32 mg daily) Exacerbation of asthma (acute, severe) (NAEPP 2007): Inhalation: Metered-dose inhaler or dry powder inhaler (90 mcg/actuation): Children Children ≥12 years and Adolescents: Refer to adult dosing. Nebulization solution: Children or 0.5 mg/kg/hour by continuous nebulization Children ≥12 years and Adolescents: Refer to adult dosing. Exercise-induced bronchospasm (prevention): Inhalation: Metered-dose inhaler or dry powder inhaler (90 mcg/actuation): Children ≤4 years: 1 to 2 inhalations 5 minutes prior to exercise (NAEPP 2007) Children >4 years and Adolescents: 2 inhalations 5 minutes prior to exercise (NAEPP 2007) Metered-dose inhaler (100 mcg/actuation): Airomir [Canadian product]: Children 6 to 11 years: 1 inhalation 30 minutes prior to exercise Children ≥12 years and Adolescents: Refer to adult dosing. Dry powder inhaler (200 mcg/inha

Inhalation: Refer to adult dosing. Bronchospasm (treatment): Oral, regular release: 2 mg 3 to 4 times daily; maximum: 8 mg 4 times daily

There are no dosage adjustments provided in the manufacturer's labeling; use with caution. No dosage adjustment required in patients on hemodialysis, peritoneal dialysis, or CRRT (Aronoff 2007).

There are no dosage adjustments provided in the manufacturer's labeling.

Warnings & Precautions

Source: Lexicomp

Bronchospasm

Rarely, paradoxical bronchospasm may occur with use of inhaled bronchodilating agents (may be fatal); this should be distinguished from inadequate response.

Hypersensitivity reactions

Immediate hypersensitivity reactions (urticaria, angioedema, rash, bronchospasm, oropharyngeal edema), including anaphylaxis, have been reported. Disease-related concerns:

Asthma

Albuterol is a short-acting beta2-agonist (SABA) that should be used as needed for quick relief of asthma symptoms. Based on a step-wise treatment approach using asthma guidelines, monotherapy without concurrent use of a long-term controller medication should only be reserved for patients with mild, intermittent forms of asthma without the presence of risk factors (Step 1 and/or exercise-induced) (GINA 2016; NAEPP 2007).

Cardiovascular disease

Use with caution in patients with cardiovascular disease (arrhythmia, coronary insufficiency, hypertension, heart failure); beta-agonists may produce ECG changes (flattening of the T wave, prolongation of the QTc interval, ST segment depression) and/or cause elevation in blood pressure, heart rate and result in CNS stimulation/excitation. Beta2-agonists may also increase risk of arrhythmias. In a scientific statement from the American Heart Association, albuterol has been determined to be an agent that may either cause direct myocardial toxicity or exacerbate underlying myocardial dysfunction (magnitude: moderate to major) (AHA [Page 2016]).

Diabetes

Use with caution in patients with diabetes mellitus; beta2-agonists may increase serum glucose and aggravate preexisting diabetes and ketoacidosis.

Glaucoma

Use with caution in patients with glaucoma; may elevate intraocular pressure.

Hyperthyroidism

Use with caution in hyperthyroidism; may stimulate thyroid activity.

Hypokalemia

Use with caution in patients with hypokalemia; beta2-agonists may decrease serum potassium.

Renal impairment

Use with caution in patients with renal impairment.

Seizures

Use with caution in patients with seizure disorders; beta-agonists may result in CNS stimulation/excitation. Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Special populations:

Pediatric

Use spacer for children Dosage form specific issues:

Benzyl alcohol and derivatives

Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.

Lactose

Powder for oral inhalation contains lactose; hypersensitivity reactions (eg, anaphylaxis, angioedema, pruritus, and rash) have been reported in patients with milk protein allergy. Other warnings/precautions:

Appropriate use

Do not exceed recommended dose; serious adverse events, including fatalities, have been associated with excessive use of inhaled sympathomimetics.

Patient information

Patients must be instructed to seek medical attention in cases where acute symptoms are not relieved or a previous level of response is diminished. The need to increase frequency of use may indicate deterioration of asthma, and treatment must not be delayed. A spacer device or valved holding chamber is recommended when using a metered-dose inhaler.

Pregnancy & Lactation

Pregnancy

FDA category C

Safe

Continue asthma inhaler therapy unchanged. Uncontrolled asthma (hypoxia, acidosis) is far more harmful than the drug. Parenteral salbutamol for tocolysis causes neonatal metabolic effects

Lactation

Compatible

It is not known if albuterol is present in breast milk. The amount of albuterol available systemically following inhalation is significantly less in comparison to oral doses. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of exposure to the infant and the benefits of treatment to the mother. Women with asthma should be encouraged to breastfeed (GINA 2016). Use of albuterol is generally considered acceptable

Monitoring

Clinical pearl	FEV1, peak flow, and/or other pulmonary function tests; blood pressure, heart rate; CNS stimulation; serum glucose, serum potassium, serum creatinine; asthma symptoms; arterial or capillary blood gases (if patients condition warrants)

Chemistry & Properties

Formula	C13H21NO3
Molecular weight	239.31 g/mol
IUPAC name	4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
CAS	18559-94-9
PubChem CID	2083
InChIKey	`NDAUXUAQIAJITI-UHFFFAOYSA-N`
logP	1.31 (XLogP 0.3)
Polar surface area	72.72 Å²
H-bond acceptors / donors	4 / 4
Drug-likeness (QED)	0.64
Lipinski violations	0

SMILES

CC(C)(C)NCC(O)c1ccc(O)c(CO)c1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	No (logBB -1.3)

Enzyme interactions

Enzyme	Role	Detail
CYP2C19	Substrate	—
CYP2D6	Substrate	—
CYP3A4	Substrate	—

Receptor binding (top 3)

Target	Action	Affinity
adrenergic Beta3 (ADRB3)	Binding	pKi 8.3
adrenergic Beta1 (ADRB1)	Binding	pKi 6.9
adrenergic Beta2 (ADRB2)	Binding	pKi 6.4

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP3 (Inhibitor)MRP4 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)MATE1 (Substrate)MATE2 (Substrate)OCT1 (Substrate)OCT2 (Substrate)OCT3 (Substrate)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drug	Severity	Management
Carteolol	major
Carteolol (ophthalmic)	major
Carvedilol	major
Cocaine (nasal)	major
Cocaine (topical)	major
Labetalol	major
Levobunolol (ophthalmic)	major
Macimorelin	major
Metipranolol (ophthalmic)	major
Mifepristone	major
Nadolol	major
Ozanimod	major
Papaverine	major
Penbutolol	major
Pindolol	major
Propranolol	major
Ribociclib	major
Sotalol	major
Timolol	major
Timolol (ophthalmic)	major
Abarelix	moderate
Abiraterone	moderate
Acarbose	moderate
Acebutolol	moderate
Acetazolamide	moderate
Acetohexamide	moderate
Adenosine	moderate
Albiglutide	moderate
Alfuzosin	moderate
Alimemazine	moderate
Alogliptin	moderate
Aminophylline	moderate
Amiodarone	moderate
Amisulpride	moderate
Amitriptyline	moderate
Amoxapine	moderate
Amphetamine	moderate
Anagrelide	moderate
Apalutamide	moderate
Apomorphine	moderate

Showing 40 of 100+.

Registered Products (25)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Asmanore syrup	Syrup 2 mg/5 ml	100 ml	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	0.530
Asmadil Tablets	Tablet 2 mg	30 tab pack varies	The Arab Pharmaceutical Manufactruing Co.	0.550
Asmanore	Tablet 2 mg	30 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	0.550
Butalin Syrup	Syrup 2 mg/5 ml	120 ml	Professional Drug Store	0.650
Ventol Syrup	Syrup 2 mg/5 ml	120 ml	Sun Set Drug Store	0.650
Asmadil Syrup	Syrup 2 mg/5 ml	120 ml	The Arab Pharmaceutical Manufactruing Co.	0.730
Asmanore	Tablet 4 mg	30 tab	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	0.810
MEDOLIN TAB	Tablet 2 mg	50 tab pack varies	Khoury Drug Store	0.900
VENTOGEED SYRUP	Syrup Salbutamol Sulfate 2.4 mg/5 ml	100 ml	AlGadeed Pharmaceutical Industries	1.000
MEDOLIN TAB	Tablet 2 mg	100 tab pack varies	Khoury Drug Store	1.720
Salbutamol Sol For Inhalation	Solution 0.5 %	30 ml	AL-Faiasel Drug Store	1.760
Asthalin CFC Free	Inhaler 100 mcg	200 MD	ORIENT DRUG STORE CO	1.780
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp	Solution 2.5 mg, 0.5 mg	10 ampoule pack varies	Al Hilal Drug Store	2.270
Butalin	Solution as sulphate 0.5 %	20 ml	Professional Drug Store	2.370
Asthalin Respules	Ampoule 2.5 mg/2.5 ml	20 amp	ORIENT DRUG STORE CO	2.590
Ventolin Injection	Injection 0.5 mg/ml	1 ml	Suleiman Tannous & Sons Co. Ltd	3.070
Ventolin Evohaler	Inhaler 100 mcg	200 Actuations	Suleiman Tannous & Sons Co. Ltd	3.150
Ventolin Resp. Solution	Solution (as sulphate)0.5 %	20 ml	Suleiman Tannous & Sons Co. Ltd	3.310
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp	Solution 2.5 mg, 0.5 mg	20 ampoule pack varies	Al Hilal Drug Store	4.280
Duolin Respules	Ampoule 500 mcg/2.5 mg	20 amp	ORIENT DRUG STORE CO	4.640
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp	Solution 2.5 mg, 0.5 mg	30 ampoule pack varies	Al Hilal Drug Store	6.420
Combivent Unit Dose Vial	Vial 3 mg, anhydrous 500 mcg dose	2.5 ml	The Jordan Drugstore Co	9.750
Demoren nebulizer solution (0.5+ 2.5)mg/2.5 ml amp	Solution 2.5 mg, 0.5 mg	50 ampoule pack varies	Al Hilal Drug Store	10.700
Asmanore	Tablet 2 mg	1005 tab pack varies	THE JORDANIAN PHARMACEUTICAL MANUFACTURING COMPANY/JORDAN	14.740
Asmadil Tablets	Tablet 2 mg	1000 tab pack varies	The Arab Pharmaceutical Manufactruing Co.	15.580