Albuterol

What is Albuterol?

• Albuterol (Proventil; Ventolin; Volmax; VoSpire ER) is a beta2-adrenergic agonist used to prevent and treat wheezing, difficulty breathing, chest tightness, and coughing caused by lung diseases such as asthma and chronic obstructive pulmonary disease (COPD; a group of diseases that affect the lungs and airways).
• It is also known as Salbutamol.

Salbutamol

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What are the uses of this medicine?

Albuterol (Proventil; Ventolin; Volmax; VoSpire ER) is indicated for:

• the relief of bronchospasm in adults and children 6 years of age and older with reversible obstructive airway disease.

How does this medicine work?

• Albuterol is a beta2-adrenergic agonist.
• The beta adrenergic agonists are potent bronchodilators that are widely used in the management of bronchial asthma. These agents act by engaging the beta-2 adrenergic receptors on smooth muscle of bronchial tissue, relieving bronchospasm and reducing airway resistance.
• They also act on smooth muscle of the vascular system, intestines and uterus.
• Common forms of beta adrenergic agonists include albuterol, bitolterol, fenoterol, formoterol, levalbuterol, metaproterenol, salmeterol, pirbuterol and terbutaline, which all have similar mechanisms of action, chemical structure, side effects and efficacy, but somewhat different pharmacokinetics allowing for differences in dosing regimens and duration of action.
• Most of these agents are administered by inhalation (alone or in combination with other bronchodilators or corticosteroids), with only albuterol and terbutaline being available in oral forms in the United States.

• Albuterol stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3',5'-adenosine monophosphate (cAMP).
• Increased cAMP concentrations relax bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells.
• To a lesser extent albuterol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• Hypersensitivity to albuterol sulfate or any of the ingredients.

What drug interactions can this medicine cause?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Be sure to mention any of the following:

• beta blockers such as atenolol (Tenormin), labetalol (Normodyne), metoprolol (Lopressor, Toprol XL), nadolol (Corgard), and propranolol (Inderal)
• digoxin (Lanoxin)
• diuretics ('water pills')
• epinephrine (Epipen, Primatene Mist)
• other oral and inhaled medications for asthma and medications for colds.

Also tell your doctor or pharmacist if you are taking the following medications or have stopped taking them within the past two weeks:

• antidepressants such as amitriptyline (Elavil), amoxapine (Asendin), clomipramine (Anafranil), desipramine (Norpramin), doxepin (Adapin, Sinequan), imipramine (Tofranil), nortriptyline (Aventyl, Pamelor), protriptyline (Vivactil), and trimipramine (Surmontil)
• monoamine oxidase (MAO) inhibitors, including isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), and tranylcypromine (Parnate)

Is this medicine FDA approved?

• It was approved for medical use in the United States in 1982.

How should this medicine be used?

Recommended dosage: Adults and Children Over 12 Years of Age:

• The usual starting dosage for adults and children 12 years and older is 2 mg or 4 mg three or four times a day.
• For adults and children 12 years and older, a dosage above 4 mg four times a day should be used only when the patient fails to respond.
• If a favorable response does not occur with the 4 mg initial dosage, it should be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated.

Children 6 to 12 Years of Age:

• The usual starting dosage for children 6 to 12 years of age is 2 mg three or four times a day.
• For children from 6 to 12 years of age who fail to respond to the initial starting dosage of 2 mg four times a day, the dosage may be cautiously increased stepwise, but not to exceed 24 mg/day
• An initial dosage of 2 mg three or four times a day is recommended for elderly patients and for those with a history of unusual sensitivity to beta-adrenergic stimulators.
• If adequate bronchodilation is not obtained, dosage may be increased gradually to as much as 8 mg three or four times a day.

Administration:

• Albuterol comes as a tablet, a syrup, and an extended-release (long-acting) tablet to take by mouth.
• The tablets and syrup are usually taken three or four times a day.
• The extended-release tablets are usually taken once every 12 hours.
• Take albuterol at around the same times every day.
• Swallow the extended-release tablets whole with plenty of water or other liquid. Do not split, chew, or crush them.
• Your doctor may start you on a low dose of albuterol and gradually increase your dose.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As a tablet, a syrup, and an extended-release (long-acting) tablet

This medicine is available in fallowing brand namesː

• Proventil Syrup
• Proventil Tablets
• Ventolin Syrup
• Ventolin Tablets
• Volmax
• VoSpire ER

What side effects can this medication cause?

The most common side effects of this medicine include:

• Nervousness
• Tremor
• Headache
• Sleeplessness
• Weakness
• Dizziness
• Drowsiness
• Restlessness
• Irritability
• Tachycardia
• Palpitations
• Chest discomfort
• Flushing
• Muscle cramps
• Nausea
• Difficulty in micturition

• Rare cases of urticaria, angioedema, rash, bronchospasm, and oropharyngeal edema have been reported after the use of albuterol.

What special precautions should I follow?

• Albuterol tablets can produce paradoxical bronchospasm, which may be life threatening. If paradoxical bronchospasm occurs, albuterol tablets should be discontinued immediately and alternative therapy instituted.
• Albuterol tablets, like all other beta-adrenergic agonists, can produce a clinically significant cardiovascular effect in some patients as measured by pulse rate, blood pressure, and/or symptoms. Therefore, albuterol tablets, like all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.
• Asthma may deteriorate acutely over a period of hours or chronically over several days or longer. Reevaluation of the patient and treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment, e.g., corticosteroids.
• The use of beta-adrenergic agonist bronchodilators alone may not be adequate to control asthma in many patients. Early consideration should be given to adding anti-inflammatory agents, e.g., corticosteroids.
• Immediate hypersensitivity reactions may occur after administration of albuterol, as demonstrated by rare cases of urticaria, angioedema, rash, bronchospasm, and oropharyngeal edema. Rarely, erythema multiforme and Stevens-Johnson syndrome have been associated with the administration of oral albuterol sulfate in children.
• The action of albuterol tablets may last up to 8 hours or longer. Albuterol tablets should not be taken more frequently than recommended.
• While you are taking albuterol tablets, other asthma medications and inhaled drugs should be taken only as directed by your physician
• Do not increase the dose or frequency of albuterol tablets without consulting your physician.
• It is not known whether this drug is excreted in human milk. Adecision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
• The use of beta adrenergic agonists in asthma has not been associated with elevations in serum aminotransferase or alkaline phosphatase levels or in causing clinically apparent liver disease. When given in large doses or after intentional overdose, beta adrenergic agonists can cause liver injury. Most case reports of liver damage from these agents have been associated with their use in control of premature labor (for their effects on relaxation of uterine smooth muscle). The liver injury typically arises within a few days of starting high dose intravenous beta adrenergic agonists, is usually asymptomatic, not associated with jaundice, and rapidly reversed once the medication is stopped.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• seizures
• angina
• hypertension or hypotension
• tachycardia with rates up to 200 beats/min
• arrhythmias
• nervousness
• headache
• tremor
• dry mouth
• palpitation
• nausea
• dizziness
• fatigue
• malaise
• sleeplessness
• Hypokalemia

As with all sympathomimetic medications, cardiac arrest and even death may be associated with abuse of albuterol tablets

Management of overdosage:

• Treatment consists of discontinuation of albuterol tablets together with appropriate symptomatic therapy.
• There is insufficient evidence to determine if dialysis is beneficial for overdosage of albuterol tablets.
• A cardioselective beta-receptor blocker may be considered, bearing in mind that such medication can produce bronchospasm.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• There are no adequate and well-controlled studies in pregnant women. Albuterol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• Safety and effectiveness in children below 6 years of age have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredients:

• ALBUTEROL SULFATE

Inactive Ingredients:

• LACTOSE MONOHYDRATE
• MAGNESIUM STEARATE
• STARCH, CORN
• SODIUM STARCH GLYCOLATE TYPE A POTATO

Who manufactures and distributes this medicine?

Distributed by:

• Aurobindo Pharma USA, Inc.
• 279 Princeton-Hightstown Road
• East Windsor, NJ

Manufactured by:

• Aurobindo Pharma Limited
• Hyderabad, India

What should I know about storage and disposal of this medication?

• Store at 20° to 25°C (68° to 77°F).

Beta-2 Adrenergic Agonists

Albuterol, Bitolterol, Formoterol, Metaproterenol, Pirbuterol, Salbutamol, Salmeterol, Terbutaline

Leukotriene Receptor Antagonists

Montelukast, Zafirlukast

Monoclonal Antibodies

Benralizumab, Mepolizumab, Omalizumab, Reslizumab

Xanthine Derivatives

Theophylline Zileuton

• Dailymed label info on Albuterol
• FDA Albuterol

Albuterol Resources
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