Get your patient on Albuterol Sulfate - Albuterol Sulfate solution (Albuterol Sulfate)

Albuterol inhalation solution is indicated for the relief of bronchospasm in patients 12 years of age and older with reversible obstructive airway disease and acute attacks of bronchospasm.

The usual dosage for adults and pediatric patients 12 years of age and older is 2.5 mg of albuterol (one unit-of-use vial) administered 3 to 4 times daily by nebulization. More frequent administration or higher doses are not recommended. To administer 2.5 mg of albuterol, dilute 0.5 mL of the 0.5% solution for inhalation to a total volume of 3 mL with sterile normal saline solution and administer by nebulization. The flow rate is regulated to suit the particular nebulizer so that albuterol inhalation solution will be delivered over approximately 5 to 15 minutes.

Drug compatibility (physical and chemical), efficacy, and safety of albuterol inhalation solution when mixed with other drugs in a nebulizer have not been established.

The use of albuterol inhalation solution can be continued as medically indicated to control recurring bouts of bronchospasm. During treatment, most patients gain optimum benefit from regular use of the nebulizer solution.

If a previously effective dosage regimen fails to provide the usual relief, medical advice should be sought immediately, as this is often a sign of seriously worsening asthma which would require reassessment of therapy.

The nebulizer should be cleaned in accordance with the manufacturer’s instructions. Failure to do so could lead to bacterial contamination of the nebulizer and possible infection.

Albuterol inhalation solution is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.

The results of clinical trials with albuterol inhalation solution in 135 patients showed the following side effects which were considered probably or possibly drug related:

No clinically relevant laboratory abnormalities related to albuterol inhalation solution were determined in these studies. Cases of urticaria, angioedema, rash, bronchospasm, hoarseness, oropharyngeal edema, and arrythmias (including atrial fibrillation, supraventricular tachycardia, and extrasystoles) have been reported after the use of albuterol inhalation solution.

Other short-acting sympathomimetic aerosol bronchodilators or epinephrine should not be used concomitantly with albuterol. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects.

Albuterol inhalation solution, USP 0.5% contains albuterol sulfate USP, the racemic form of albuterol and a relatively selective beta ₂ -adrenergic bronchodilator (see CLINICAL PHARMACOLOGY section below). Albuterol sulfate has the chemical name α ¹ -[( tert-Butylamino) methyl]-4-hydroxy- m-xylene-α,α′-diol sulfate (2:1) (salt) and the following chemical structure:

The molecular weight of albuterol sulfate is 576.7 and the empirical formula is (C ₁₃ H ₂₁ NO ₃ ) ₂ • H ₂ SO ₄

Albuterol sulfate USP is a white crystalline powder, soluble in water and slightly soluble in ethanol. The World Health Organization’s recommended name for albuterol base is salbutamol.

Albuterol inhalation solution, USP 0.5%, is in concentrated form. Dilute 0.5 mL of the solution to 3 mL with sterile normal saline solution prior to administration by nebulization (see DOSAGE AND ADMINISTRATION ).

Each 0.5 mL Unit-of-Use Vial Contains: ACTIVE: 2.5 mg of albuterol (equivalent to 3 mg of albuterol sulfate USP) in a sterile, aqueous solution; sulfuric acid is used to adjust the pH to between 3 and 5. Albuterol inhalation solution, USP contains no sulfiting agents or preservatives. It is supplied in 0.5 mL sterile Unit-of-Use Vials.

Albuterol inhalation solution, USP is a clear, colorless to light yellow solution.

In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta ₂ -adrenergic receptors compared with isoproterenol. While it is recognized that beta ₂ -adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta ₂ -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 ).

The pharmacologic effects of beta-adrenergic agonist drugs, including albuterol, are at least in part attributable to stimulation through beta-adrenergic receptors of 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. Albuterol has been shown in most controlled clinical trials to have more effect on the respiratory tract, in the form of bronchial smooth muscle relaxation, than isoproterenol at comparable doses while producing fewer cardiovascular effects. Controlled clinical studies and other clinical experience have shown that inhaled albuterol, like other beta-adrenergic agonist drugs, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic changes.

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 nor for catechol- O -methyl transferase.

Pharmacokinetics : Studies in asthmatic patients have shown that less than 20% of a single albuterol dose was absorbed following either intermittent positive-pressure breathing (IPPB) or nebulizer administration; the remaining amount was recovered from the nebulizer and apparatus and expired air. Most of the absorbed dose was recovered in the urine 24 hours after drug administration. Following a 3 mg dose of nebulized albuterol, the maximum albuterol plasma level at 0.5 hour was 2.1 ng/mL (range 1.4 to 3.2 ng/mL). There was a significant dose-related response in FEV ₁ and peak flow rate. It has been demonstrated that following oral administration of 4 mg of albuterol, the elimination half-life was 5 to 6 hours.

Preclinical : Intravenous studies in rats with albuterol sulfate have demonstrated that albuterol crosses the blood-brain barrier and reaches brain concentrations that are amounting to approximately 5.0% of the plasma concentrations. In structures outside the brain barrier (pineal and pituitary glands), albuterol concentrations were found to be 100 times those in the whole brain.
Studies in laboratory animals (minipigs, rodents, and dogs) have demonstrated the occurrence of cardiac arrhythmias and sudden death (with histologic evidence of myocardial necrosis) when beta-agonists and methylxanthines were administered concurrently. The significance of these findings is unknown.

Clinical Trials : In controlled clinical trials in adults, most patients exhibited an onset of improvement in pulmonary function within 5 minutes as determined by FEV ₁ . FEV ₁ measurements also showed that the maximum average improvement in pulmonary function usually occurred at approximately 1 hour following inhalation of 2.5 mg of albuterol by compressor-nebulizer and remained close to peak for 2 hours.
Clinically significant improvement in pulmonary function (defined as maintenance of a 15% or more increase in FEV ₁ over baseline values) continued for 3 to 4 hours in most patients and in some patients continued up to 6 hours.
Published reports of trials in asthmatic children aged 3 years or older have demonstrated significant improvement in either FEV ₁ or PEFR within 2 to 20 minutes following single doses of albuterol inhalation solution. An increase of 15% or more in baseline FEV ₁ has been observed in children aged 5 to 11 years up to 6 hours after treatment with doses of 0.10 mg/kg or higher of albuterol inhalation solution. Single doses of 3, 4, or 10 mg resulted in improvement in baseline PEFR that was comparable in extent and duration to a 2 mg dose, but doses above 3 mg were associated with heart rate increases of more than 10%.

Albuterol inhalation solution, USP 0.5%, is a clear, colorless to light yellow solution, and is supplied in plastic sterile unit-of-use vials of 0.5 mL each, supplied in individual foil pouches:

NDC 0487-9901-30: 30 vials, each in an individual pouch.

1. Twist open the top of one Albuterol Inhalation Solution unit-of-use container (Figure 1).
2. Squeeze the solution into the nebulizer reservoir through the appropriate opening (Figure 2).
3. Add 2.5 mL of diluting fluid – sterile normal saline solution (as your doctor has directed).
4. Gently swirl the nebulizer to mix the contents and connect it with the mouthpiece or face mask (Figure 3).
5. Connect the nebulizer to the compressor.
6. Sit in a comfortable, upright position; place the mouthpiece in your mouth (Figure 4) (or put on the face mask); and turn the compressor on.
7. Breathe as calmly, deeply and evenly as possible until no more mist is formed in the nebulizer chamber (about 5 to 15 minutes). At this point, the treatment is finished.
8. Clean the nebulizer (see manufacturer’s instructions). Failure to clean the nebulizer in accordance with the manufacturer’s instructions could lead to bacterial contamination of the nebulizer, and possible infection.