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Albuterol; Indications/Uses, Dosage, Side Effects, Drug Interaction, Pregnancy

Albuterol is a racemic mixture of the r-isomer levalbuterol and s-albuterol, a short-acting sympathomimetic agent with bronchodilator activity. Albuterol stimulates beta-2 adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′-adenosine monophosphate (cAMP). Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. Albuterol although to a lesser extent, also stimulates beta-1 adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

Albuterol or salbutamol is a medication that opens up the medium and large airways in the lungs. It is used to treat asthma including asthma attacks, exercise-induced bronchoconstriction, and chronic obstructive pulmonary disease (COPD). It may also be used to treat high blood potassium levels. Salbutamol is usually used with an inhaler or nebulizer but is also available as a pill and intravenous solution. The onset of action of the inhaled version is typically within 15 minutes and lasts for two to six hours.

Mechanism of Action of Albuterol

Albuterol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP production by activating adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation. In addition to bronchodilation, salbutamol inhibits the release of bronchoconstricting agents from mast cells, inhibits microvascular leakage, and enhances mucociliary clearance.

Indications of Albuterol

Bronchospasm
Exercise-Induced Bronchoconstriction (EIB)
COPD,
Asthma,
Asthma, acute
Bronchiectasis
Bronchospasm Prophylaxis
Hyperkalemia
Bronchial asthma,
Chronic bronchitis,
Chronic bronchopulmonary disorders
For symptomatic relief and prevention of bronchospasm due to bronchial asthma, chronic bronchitis, and other chronic bronchopulmonary disorders such as COPD.
Symptomatic treatment of reversible bronchoconstriction due to bronchial asthma and chronic obstructive pulmonary disease (COPD) including chronic bronchitis and emphysema. Prophylaxis of exercise and allergen-induced asthma.
Symptomatic treatment of reversible bronchoconstriction due to bronchial asthma and chronic obstructive pulmonary disease (COPD) including chronic bronchitis and emphysema.
Prophylaxis of exercise and allergen-induced asthma.

Contra-Indications of Albuterol

overactive thyroid gland
Diabetes
Ketoacidosis
Excess Body Acid
low amount of potassium in the blood
high blood pressure
Diminished Blood Flow through Arteries of the Heart
Disease of Inadequate Blood Flow to the Heart Muscle
prolonged QT interval on EKG
abnormal heart rhythm
Abnormal EKG with QT changes from Birth
seizures
Paradoxical Bronchospasm

Dosage of Albuterol

Strengths: 2 mg; 4 mg; 2 mg/5 mL; 90 mcg/inh; 5 mg/mL; 2.5 mg/3 mL

Chronic Obstructive Pulmonary Disease – Acute

Intravenous infusion solution

Dilute 5 mL of this drug (1000 mcg/mL) in 500 mL of Sodium Chloride Injection, or Sodium Chloride and Dextrose.
Infusion rates can be started at 5 mcg/min and can be increased to 10 mcg/min and 20 mcg/min at 15 at 30-minute intervals, if necessary.

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Nebulizer inhalation solution

2.5 mg three or four times a day by nebulization, over approximately 5 to 15 minutes.

Asthma – Acute

Intravenous infusion solution

Dilute 5 mL of this drug (1000 mcg/mL) in 500 mL of Sodium Chloride Injection, or Sodium Chloride and Dextrose.
Infusion rates can be started at 5 mcg/min and can be increased to 10 mcg/min and 20 mcg/min at 15 at 30-minute intervals, if necessary.

Nebulizer inhalation solution

2.5 mg three or four times a day by nebulization, over approximately 5 to 15 minutes.

Bronchitis

Intravenous infusion solution

Dilute 5 mL of this drug (1000 mcg/mL) in 500 mL of Sodium Chloride Injection, or Sodium Chloride and Dextrose.
Infusion rates can be started at 5 mcg/min and can be increased to 10 mcg/min and 20 mcg/min at 15 at 30-minute intervals, if necessary.

Nebulizer inhalation solution

2.5 mg three or four times a day by nebulization, over approximately 5 to 15 minutes.

Pediatric Dose for Asthma

Inhalation powder and capsules

Less than 4 years: Not indicated

4 years or older

Inhalation powder: 1 or 2 inhalations (90 or 180 mcg) orally every 4 to 6 hours
Inhalation capsules:1 inhalation (200 mcg) orally every 4 to 6 hours. The total daily dose should not exceed 4 inhalations (800 mcg).

Nebulizer inhalation solution

Less than 2 years: Not indicated

2 to 12 years

Less than 15 kg: 0.1 to 0.15 mg/kg/dose (one 3 mL unit-dose vial of 1.25 mg or 0.63 mg inhalation solution) by nebulization. The appropriate volume of the 0.5% inhalation solution should be diluted in sterile normal saline solution to a total of 3 mL prior administration. Dosing should not exceed 2.5 mg three to four times daily.
15 kg or more: 2.5 mg (one 3 mL unit-dose vial of 0.0083%) three or four times a day by nebulization, over approximately 5 to 15 minutes. The 0.5% inhalation solution should be diluted with 2.5 mL of sterile normal saline solution

13 years or older

Inhalation solution 0.5% (5 mg/mL): 2.5 mg (0.5 mL diluted with 2.5 mL of sterile saline solution) three or four times a day by nebulization, over approximately 5 to 15 minutes.

Oral Tablets

Less than 6 years: Not indicated

6 to 12 years

Immediate-release tablets: Initial dose: 2 mg orally three or four times a day. Dosage may be cautiously increased stepwise, but not to exceed 24 mg/day (given in divided doses).
Extended-release tablets: Initial dose: 4 mg orally every 12 hours. Dosage may be cautiously increased stepwise under the control of the supervising physician to a maximum of 24 mg/day in divided doses (e.g., every 12 hours).

13 years or older

Immediate-release tablets: Initial dose: 2 mg or 4 mg orally three or four times a day. Dosage may be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated (maximum of 32 mg/day).
Extended-release tablets: Initial dose: 4 mg or 8 mg orally every 12 hours. Dosage may be cautiously increased stepwise under the control of the supervising physician to a maximum of 32 mg/day in divided doses (e.g., every 12 hours).

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Oral syrup

Less than 2 years: Not indicated
2 to 5 years: Initial dose: 0.1 mg/kg (do not exceed 2 mg) orally three times a day. Dosage may be increased stepwise to 0.2 mg/kg three times a day. A maximum dose of 4 mg three times a day should not be exceeded.
6 to 14 years: Initial dose: 2 mg orally three or four times a day. Dosage may be cautiously increased stepwise, but not exceed 24 mg/day (in divided doses).
15 years or older: Initial dose: 2 mg or 4 mg orally three or four times a day. Dosage may be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated.

Pediatric Dose for Bronchitis

Inhalation powder and capsules

Less than 4 years: Not indicated

4 years or older

Inhalation powder: 1 or 2 inhalations (90 or 180 mcg) orally every 4 to 6 hours
Inhalation capsules:1 inhalation (200 mcg) orally every 4 to 6 hours. The total daily dose should not exceed 4 inhalations (800 mcg).

Nebulizer inhalation solution

Less than 2 years: Not indicated

2 to 12 years

Less than 15 kg: 0.1 to 0.15 mg/kg/dose (one 3 mL unit-dose vial of 1.25 mg or 0.63 mg inhalation solution) by nebulization. The appropriate volume of the 0.5% inhalation solution should be diluted in sterile normal saline solution to a total of 3 mL prior administration. Dosing should not exceed 2.5 mg three to four times daily.
15 kg or more: 2.5 mg (one 3 mL unit-dose vial of 0.0083%) three or four times a day by nebulization, over approximately 5 to 15 minutes. The 0.5% inhalation solution should be diluted with 2.5 mL of sterile normal saline solution.

13 years or older

Inhalation solution 0.5% (5 mg/mL): 2.5 mg (0.5 mL diluted with 2.5 mL of sterile saline solution) three or four times a day by nebulization, over approximately 5 to 15 minutes

Side Effects of Albuterol

The most common

Shakiness in the legs, arms, hands, or feet
trembling or shaking of the hands or feet
stomach pain or cramping
diarrhea
a headache
dizziness
confusion
stomach pain;
back pain, joint or muscle pain.
problems with your vision (including color vision);
sudden chest pain or trouble breathing;
pain or swelling in one or both legs;
a migraine headache;
pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
feeling like you might pass out.

More common

Abdominal or stomach pain, discomfort, or tenderness
chills or fever
difficulty with moving
a headache, severe and throbbing
joint or back pain
muscle aching or cramping
muscle pains or stiffness
chest pressure or squeezing pain in the chest
discomfort in arms, shoulders, neck or upper back
excessive sweating
feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
sudden tingling or coldness in an arm or leg
sudden slow or difficult speech
sudden drowsiness or need to sleep
fast breathing
sharp pain when taking a deep breath
fast or slow heartbeat
coughing up blood
rust colored urine
decreased amount of urine

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Rare

Anxiety
change in vision
chest pain or tightness
confusion
a cough
Agitation
arm, back, or jaw pain
blurred vision
chest pain or discomfort
convulsions
extra heartbeats
fainting
hallucinations
a headache
irritability
lightheadedness
mood or mental changes
muscle pain or cramps
muscle spasm or jerking of all extremities
nervousness

Drug Interactions of Albuterol

Albuterol may interact with the following drugs, supplements & may change the efficacy of drugs

aminophylline
atomoxetine
beta-blockers (e.g., propranolol, labetalol, )
carvedilol
certain diuretics (e.g., hydrochlorothiazide, furosemide)
dextroamphetamine
dipivefrine
dobutamine
methylphenidate
monoamine oxidase inhibitors (e.g., phenelzine, tranylcypromine, moclobemide, selegiline)
nabilone
naphazoline
norepinephrine
other bronchodilators (e.g., salmeterol, terbutaline)
oxymetazoline
phenylephrine
pseudoephedrine
theophylline
tricyclic antidepressants (e.g., amitriptyline, desipramine, nortriptyline)

Pregnancy Catagory of Albuterol

FDA Pregnancy Category C

Pregnancy

Salbutamol is a pregnancy category C drug. It should be used during pregnancy only if absolutely essential. During pregnancy, inhalation of salbutamol has the particular advantage as the therapeutic action can be achieved without the requirement for such plasma concentration liable to have an effect on the fetus.

Lactation

Salbutamol is probably excreted in human milk but the concentration is unknown. However, no adverse effects have been reported in the breastfed babies of mothers receiving salbutamol by inhalation.