Proventil

Proventil Information

Brand Names: Ventolin, Proventil

Generic Name: Albuterol

Other Names: Salbutamol

Proventil (albuterol) is used for asthma relief.

Indications

Inhalation Aerosol and Capsules for Inhalation: Albuterol inhalation aerosol is indicated for the prevention and relief of bronchospasm in patients 4 years of age and older with reversible obstructive airway disease and for the prevention of exercise-induced bronchospasm in patients 4 years of age and older. The capsules for inhalation formulation is particularly useful in patients who are unable to properly use the pressurized aerosol form of albuterol or who prefer an alternative formulation.

Albuterol inhalation aerosol can be used with or without concomitant steroid therapy.

Inhalation Solution: Albuterol inhalation solution is indicated for the relief of bronchospasm in patients 2 years of age or older with reversible obstructive airway disease and acute attacks of bronchospasm.

Proventil Ingredients and Composition

How Does Proventil Work?

Clinical Pharmacology

In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol, the active ingredient of Proventil, has a preferential effect on beta2-adrenergic receptors compared with isoproterenol. While it is recognized that beta2-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta2-receptors in the human heart existing in a concentration between 10% and 50%. The precise function of these receptors has not been established.

The pharmacologic effects of beta-adrenergic agonist drugs, including albuterol, are at least in party 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, the active ingredient in Proventil, 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 Proventil 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, the active ingredient in Proventil, 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.

How To Take Proventil and Proventil Dosage and Administration

Inhalation Aerosol

For treatment of acute episodes of bronchospasm or prevention of asthmatic symptoms, the usual Proventil dosage for adults and children 4 years of age and older is two inhalations repeated every 4 to 6 hours; in some patients, one Proventil inhalation every 4 hours may be sufficient. More frequent administration or a larger number of inhalations are not recommended. It is recommended to test spray Proventil inhalation aerosol. Do this by spraying four times into the air before using for the first time and when the inhaler has not been used for a prolonged period of time (i.e., more than 4 weeks).

The use of Proventil (albuterol) inhalation aerosol can be continued as medically indicated to control recurring bouts of bronchospasm. During this time most patients gain optimal benefit from regular use of the inhaler. Safe Proventil usage for periods extending over several years has been documented.

If a previously effective Proventil dosage regimen fails to provide the usual response, 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).

Exercise-Induced Bronchospasm Prevention: The usual Proventil dosage for adults and children 4 years and older is two inhalations 15 minutes before exercise.

For treatment, see above.

Proventil Inhalation Solution, 0.5%

To avoid microbial contamination, proper aseptic techniques should be used each time the bottle is opened. Precautions should be taken to prevent contact of the dropper tip of the bottle with any surface, including the nebulizer reservoir and associated ventilatory equipment. In addition, if the Proventil solution changes color or becomes cloudy, it should not be used.

Adults and Children Over 12 Years of Age: The usual Proventil dosage for adults and children 12 years of age and older is 2.5 mg of albuterol administered three to four times daily by nebulization. More frequent administration or higher Proventil doses are not recommended. To administer 2.5 mg of Proventil (albuterol), dilute 0.5 ml of the 0.5% inhalation solution with 2.5 ml of sterile normal saline solution. The flow rate is regulated to suit the particular nebulizer so that albuterol inhalation solution will be delivered over approximately 5 to 15 minutes.

The use of albuterol sulfate inhalation solution 0.5% can be continued as medically indicated to control recurring bouts of bronchospasm. During this time most patients gain optimal benefit from regular use of the inhalation solution.

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

Drug compatibility (physical and chemical), efficacy, and safety of albuterol inhalation solution 0.5% when mixed with other drugs in a nebulizer have not been established.

Inhalation Solution, 0.083%

Adults and Children 2 to 12 Years of Age: The usual Proventil dosage for adults and children weighing at least 15 kg is 2.5 mg of albuterol (one Ventolin Nebule) administered three to four times daily by nebulization. Children weighing less than 15 kg who require less than 2.5 mg/dose (i.e., less than a full Ventolin Nebule) should use albuterol inhalation solution 0.5% instead of 0.083%. More frequent administration or higher Proventil doses are not recommended. To administer 2.5 mg of albuterol, administer the contents of one sterile unit dose Nebule (3 ml of 0.083% inhalation solution) by nebulization. The wflow rate is regulated to suit the particular nebulizer so that albuterol inhalation solution 0.083% will be delivered over approximately 5 to 15 minutes.

The use of albuterol inhalation solution 0.083% can be continued as medically indicated to control recurring bouts of bronchospasm. During this time most patients gain optimal benefit from regular use of the Proventil.

Drug compatibility (physical and chemical), efficacy, and safety of albuterol inhalation solution 0.083% when mixed with other drugs in a nebulizer have not been established.

If you suspect a Proventil Overdose

The expected symptoms with Proventil overdoe are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under side effects (e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats/min, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, and sleeplessness.) Hypokalemia may also occur. Proventil Inhalation Solution Only: In isolated cases in children 2 to 12 years of age, tachycardia with rates >200 beats/min has been observed.

As with all sympathomimetic medications, cardiac arrest and even death may be associated with abuse of Proventil (albuterol). Treatment consists of discontinuation of Proventil (albuterol) together with appropriate symptomatic therapy. The judicious use of a cardioselective beta-recptor blocker may be considered, bearing in mind that such medication can produce bronchospasm. There is insufficient evidence to determine if dialysis is beneficial for overdosage of Proventil (albuterol).

The oral median lethal dose of Proventil active ingredient, albuterol sulfate in mice is greater than 2000 mg/kg (approximately 810 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 300 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for Proventil inhalation solution, and approximately 6800 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 3200 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for inhalation aerosol or approximately 3400 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 1600 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for inhalation capsules). In mature rats, the subcutaneous median lethal dose of Proventil active ingredient, albuterol sulfate is approximately 450 mg/kg (approximately 365 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 135 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for inhalation solution and approximately 3000 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 1400 times the maximum recommended daily Proventil inhalation dose for children on a mg/m2 basis for inhalation aerosol or approximately 1500 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 1700 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for inhalation capsules). In small young rats, the subcutaneous median lethal dose is approximately 2000 mg/kg (approximately 1600 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 600 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for inhalation solution and approximately 14,000 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 6400 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for inhalation aerosol or approximately 6800 times the maximum recommended daily inhalation dose for adults on a mg/m2 basis or approximately 3200 times the maximum recommended daily inhalation dose for children on a mg/m2 basis for inhalation capsules). The inhalational median lethal dose has not been determined in animals.

Dialysis is not appropriate treatment for overdosage of albuterol capsules for inhalation.

Proventil Side Effects

Proventil Precautions and Contraindications

General

Provientil (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. Large doses of intravenous albuterol have been reported to aggravate preexisting diabetes mellitus and ketoacidosis. As with other beta-agonists, albuterol in Proventil may produce significant hypokalemia in some patients, possibly through intracellular shunting, which has the potential to produce adverse cardiovascular effects. The decrease is usually transient, not requiring supplementation. Inhalation Aerosol and Inhalation Solutions: Clinically significant changes in systolic and diastolic blood pressure have been seen in individual patients and could be expected to occur in some patients after use of any beta-adrenergic bronchodilator.

Proventil Warnings

Proventil Drug Interactions

Other short-acting sympathomimetic aerosol bronchodilators (and for inhalation solutions, epinephrine) should not be used concomitantly with Proventil. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects.

Monoamine Oxidase Inhibitors or Tricyclic Antidepressants: Proventil should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents, because the action of albuterol on the vascular system may be potentiated.

Beta-Blockers: Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-agonists, such as albuterol, but may produce severe bronchospasm in asthmatic patients. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain circumstances (e.g., as prophylaxis after myocardial infarction, there may be no acceptable alternatives to the use of beta-adrenergic blocking agents in patients with asthma. In this setting), cardioselective beta-blockers could be considered, although they should be administered with caution.

Diuretics: The ECG changes and/or hypokalemia that may result from the administration of nonpotassium-sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded. Although the clinical significance of these effects is not known, caution is advised in the coadministration of beta-agonists with nonpotassium-sparing diuretics.

Digoxin: Mean decreases of 16% to 22% in serum digoxin levels were demonstrated after single-dose intravenous and oral administration of albuterol, respectively, to normal volunteers who had received digoxin for 10 days. The clinical significance of these findings for patients with obstructive airway disease who are receiving albuterol and digoxin on a chronic basis is unclear. Nevertheless, it would be prudent to carefully evaluate the serum digoxin levels in patients who are currently receiving digoxin and albuterol.

Proventil Clinical Trials and Studies

Storing Proventil

Store Proventil between 2-25°C (36-77°F).

Additional Patient Information for Proventil

The action of Proventil may last up to 6 hours or longer. Proventil should not be used more frequently than recommended. Do not increase the dose or frequency of Proventil without consulting your physician. If you find that treatment with Proventil becomes less effective for symptomatic relief, your symptoms become worse, and/or you need to use the product more frequently than usual, you should seek medical attention immediately. While you are using Proventil, other inhaled drugs and asthma medications should be taken only as directed by your physician. Common adverse effects include palpitations, chest pain, rapid heart rate, and tremor or nervousness. If you are pregnant or nursing, contact your physician about use of Proventil. Effective and safe use of Proventil includes an understanding of the way that it should be administered.

Additional Notes

The World Health Organization recommended name for albuterol base is salbutamol.