Information for Healthcare Providers

What is VoSpire ER^®?

VoSpire ER^® is relatively selective β₂-adrenergic bronchodilator that contains the racemic form of albuterol in an extended-release formulation. Each 4mg and 8mg tablet of VoSpire ER^® contains albuterol as 4.8 mg or 9.6 mg, respectively, of albuterol sulfate in a cellulosic material that serves as a diffusion-release membrane. 

VoSpire ER^® Extended-Release tablets are indicated for the relief of bronchospasm in adults and children 6 years of age and older with Reversible Obstructive Airway Disease.

How does VoSpire ER^® work?

Albuterol is a β₂-adrenergic agonist. The binding of albuterol molecules to β₂-receptors in the lungs results in relaxation of bronchial smooth muscles. The pharmacologic effects of β-adrenergic agonist drugs, including albuterol, are at least in part attributable to stimulation through β-adrenergic receptors on intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. While it is recognized that β₂-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicates that there is a population of β₂-receptors in the human heart existing in a concentration between 10% and 50%. The precise function of these receptors has not been established. (See Warnings Section Below) In-vitro studies and in-vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on the respiratory tract, in the form of bronchial smooth muscle relaxation, while producing fewer cardiovascular effects than isoproterenol at comparable doses.

Albuterol is longer acting than isoproterenol in most patients by any route of administration because it is not a substrate for the cellular uptake processes for catecholamines or for catechol-O-methyl transferase.

What is VoSpire ER^®’s Duration of Action?

VoSpire ER^® (Albuterol Sulfate) Extended-Release Tablets have been formulated to provide duration of action of up to 12 hours. In an 8-day, multiple-dose, crossover study, 15 normal adult male volunteers were given 8 mg albuterol extended-release tablets every 12 hours or 4 mg albuterol tablets, USP every 6 hours. Each dose of albuterol extended-release tablets and the corresponding doses of albuterol tablets, USP were administered in the postprandial state. Steady-state plasma concentrations were reached within 2 days for both formulations. Fluctuations (C_max-C_min/C_average) in plasma concentrations were similar for albuterol extended-release tablets administered at 12-hour intervals and albuterol tablets, USP administered every 6 hours. In addition, the relative bioavailability of albuterol extended-release tablets was approximately 100% of the immediate-release tablet at steady state. 

How should VoSpire ER^® be taken?

VoSpire ER^® Tablets are taken by mouth twice daily, usually once in the morning and once in the evening. VoSpire ER^® Tablets MUST NOT BE CHEWED OR CRUSHED.  Albuterol extended-release tablets must be swallowed whole with the aid of liquids.

VoSpire ER^® (Albuterol Sulfate) Extended-Release Tablets should not be used more frequently than recommended. Patients must not increase the dose or frequency of albuterol extended-release tablets without consulting their physician. If patient find that treatment with albuterol extended-release tablets becomes less effective for symptomatic relief, and/or symptoms become worse, and/or they need to use the product more frequently than usual, they should seek medical attention immediately. While using albuterol extended-release tablets, other inhaled drugs and asthma medications should be taken only as directed by a physician.

Pharmacokinetics and Disposition: In a single-dose study comparing one 8 mg albuterol extended-release tablet with two 4 mg immediate-release albuterol tablets, USP in 17 normal adult volunteers, the extent of availability of albuterol extended-release tablets was shown to be about 80% of albuterol tablets, USP with or without food. In addition, lower mean peak plasma concentration and longer time to reach the peak level were observed with albuterol extended-release tablets as compared with albuterol tablets, USP. The single-dose study results also showed that food decreases the rate of absorption of albuterol from albuterol extended-release tablets without altering the extent of bioavailability.

In another single-dose study in adults, 8 mg and 4 mg albuterol extended-release tablets were shown to deliver dose-proportional plasma concentrations in the fasting state. Definitive studies for the effect of food on 4 mg albuterol extended-release tablets have not been conducted. However, since food lowers the rate of absorption of 8 mg albuterol extended-release tablets, it is expected that food reduces the rate of absorption of 4 mg albuterol extended-release tablets also.

What are the most Common Reactions Associated with VoSpire ER^®?

The most common adverse reactions (>3%) reported in clinical trials of adult patients were: tremor (24.2%); headache (18.8%); nervousness (8.5%); nausea and vomiting (4.2%).  Patients who are pregnant or nursing should contact their physician about using VoSpire ER^®. Effective and safe use of albuterol extended-release tablets includes an understanding of the way that it should be administered.

How are additional warnings and precautions associated with VoSpire ER^®?

WARNINGS: Immediate hypersensitivity reactions may occur after administration of albuterol, as demonstrated by rare cases of urticaria, angioedema, rash, bronchospasm, and oropharyngeal edema.

Cardiovascular Effects: Albuterol extended-release 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. Although such effects are uncommon after administration of albuterol extended-release tablets at recommended doses, if they occur, the drug may need to be discontinued. In addition, beta-agonists have been reported to produce electrocardiogram (ECG) changes, such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression. The clinical significance of these findings is unknown. Therefore, albuterol extended-release tablets, like all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension.

Deterioration of Asthma: Asthma may deteriorate acutely over a period of hours or chronically over several days or longer. If the patient needs more doses of albuterol extended-release tablets than usual, this may be a marker of destabilization of asthma and requires reevaluation of the patient and the treatment regimen, giving special consideration to the possible need for anti-inflammatory treatment; e.g., corticosteroids.

Use of Anti-Inflammatory Agents: 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.

Paradoxical Bronchospasm: Albuterol extended-release tablets can produce paradoxical bronchospasm, which may be life threatening. If paradoxical bronchospasm occurs, albuterol extended-release tablets should be discontinued immediately and alternative therapy instituted.
Rarely, erythema multiforme and Stevens-Johnson syndrome have been associated with the administration of oral albuterol in children.

PRECAUTIONS: General: Albuterol, as with all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias, and hypertension; in patients with convulsive disorders, hyperthyroidism, or diabetes mellitus; and in patients who are unusually responsive to sympathomimetic amines. Clinically significant changes in systolic and diastolic blood pressure have been seen and could be expected to occur in some patients after use of any beta-adrenergic bronchodilator.

For additional detailed information, please see the VoSpire ER^® Full Prescribing Information.