albuterol 0.083 % Inhalant Solution

Generic Name: ALBUTEROL SULFATE
Brand Name: Albuterol Sulfate
  • Substance Name(s):
  • ALBUTEROL SULFATE

WARNINGS

As with other inhaled beta-adrenergic agonists, albuterol sulfate inhalation solution can produce paradoxical bronchospasm, which can be life threatening.

If it occurs, the preparation should be discontinued immediately and alternative therapy instituted.

Fatalities have been reported in association with excessive use of inhaled sympathomimetic drugs and with the home use of nebulizers.

It is, therefore, essential that the physician instruct the patient in the need for further evaluation, if his/her asthma becomes worse.

In individual patients, any beta2-adrenergic agonist, including albuterol solution for inhalation, may have a clinically significant cardiac effect.

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

DRUG INTERACTIONS

Drug Interactions Other sympathomimetic aerosol bronchodilators or epinephrine should not be used concomitantly with albuterol.

Albuterol should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, since the action of albuterol on the vascular system may be potentiated.

Beta-receptor blocking agents and albuterol inhibit the effect of each other.

OVERDOSAGE

Manifestations of overdosage may include seizures, anginal pain, hypertension, hypokalemia, tachycardia with rates up to 200 beats/min, and exaggeration of the pharmacological effects listed in ADVERSE REACTIONS.

In isolated cases in children 2 to 12 years of age, tachycardia with rates >200 beats/min has been observed.

The oral LD50 in rats and mice was greater than 2,000 mg/kg.

The inhalational LD50 could not be determined.

There is insufficient evidence to determine if dialysis is beneficial for overdosage of albuterol inhalation solution.

DESCRIPTION

Albuterol Sulfate Inhalation Solution is a relatively selective beta2-adrenergic bronchodilator (see CLINICAL PHARMACOLOGY section below).

Albuterol sulfate, the racemic form of albuterol, has the chemical name α1-[(tert-Butylamino)methyl]-4-hydroxy-m-xylene-α,α’-diol sulfate (2:1) (salt), and the following structural formula: Albuterol sulfate has a molecular weight of 576.70, and the molecular formula (C13H21NO3)2 • H2SO4.

Albuterol sulfate is a white or practically white powder, freely soluble in water and slightly soluble in alcohol.

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

Albuterol Sulfate Inhalation Solution 0.083% requires no dilution before administration.

Each milliliter of Albuterol Sulfate Inhalation Solution 0.083% contains 0.83 mg of albuterol (as 1 mg of albuterol sulfate) in an isotonic, sterile, aqueous solution containing sodium chloride; sulfuric acid is used to adjust the pH to between 3 and 5.

Albuterol Sulfate Inhalation Solution 0.083% contains no sulfiting agents or preservatives.

Albuterol Sulfate Inhalation Solution is a clear, colorless to light yellow solution.

Chemical Structure

HOW SUPPLIED

Unit-dose plastic vial containing Albuterol Sulfate Inhalation Solution 0.083%, 2.5 mg/3 mL(Potency expressed as albuterol, equivalent to 3 mg albuterol sulfate).

Equivalent to 0.5 mL albuterol (as the sulfate) 0.5% (2.5 mg albuterol) diluted to 3 mL.

Supplied in cartons as listed below.

NDC 33261-0789-01 25 vials per carton / 25 vials per foil pouch Storage PROTECT FROM LIGHT.

Store in pouch until time of use.

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

Rx only.

INDICATIONS AND USAGE

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

PEDIATRIC USE

Pediatric Use The safety and effectiveness of albuterol sulfate inhalation solution have been established in children 2 years of age or older.

Use of albuterol sulfate inhalation solution in these age-groups is supported by evidence from adequate and well-controlled studies of albuterol sulfate inhalation solution in adults; the likelihood that the disease course, pathophysiology, and the drug’s effect in pediatric and adult patients are substantially similar; and published reports of trials in pediatric patients 3 years of age or older.

The recommended dose for the pediatric population is based upon three published dose comparison studies of efficacy and safety in children aged 5 to 17 years, and on the safety profile in both adults and pediatric patients at doses equal to or higher than the recommended doses.

The safety and effectiveness of albuterol sulfate inhalation solution in children below 2 years of age have not been established.

PREGNANCY

Pregnancy Teratogenic Effects Pregnancy Category C Albuterol has been shown to be teratogenic in mice when given subcutaneously in doses corresponding to 1.25 times the human nebulization dose (based on a 50 kg human).

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.

A reproduction study in CD-1 mice with albuterol (0.025, 0.25, and 2.5 mg/kg subcutaneously, corresponding to 0.125, 1.25 and 12.5 times the maximum human nebulization dose, respectively) showed cleft palate formation in 5 of 111 (4.5%) fetuses at 0.25 mg/kg and in 10 of 108 (9.3%) fetuses at 2.5 mg/kg.

None were observed at 0.025 mg/kg.

Cleft palate also occurred in 22 of 72 (30.5%) fetuses from females treated with 2.5 mg/kg isoproterenol (positive control).

A reproduction study in Stride Dutch rabbits revealed cranioschisis in 7 of 19 (37%) fetuses at 50 mg/kg, corresponding to 250 times the maximum nebulization dose for a 50 kg human.

During worldwide marketing experience, various congenital anomalies, including cleft palate and limb defects, have been rarely reported in the offspring of patients being treated with albuterol.

Some of the mothers were taking multiple medications during their pregnancies.

No consistent pattern of defects can be discerned, and a relationship between albuterol use and congenital anomalies has not been established.

NUSRING MOTHERS

Nursing Mothers It is not known whether this drug is excreted in human milk.

Because of the potential for tumorigenicity shown for albuterol in some animal studies, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

INFORMATION FOR PATIENTS

Information For Patients The action of albuterol sulfate inhalation solution may last up to six hours, and therefore it should not be used more frequently than recommended.

Do not increase the dose or frequency of medication without medical consultation.

If symptoms get worse, medical consultation should be sought promptly.

While taking albuterol sulfate inhalation solution, other anti-asthma medicines should not be used unless prescribed.

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

See illustrated ” Patient’s Instructions for Use .”

DOSAGE AND ADMINISTRATION

Adults and Children 2 to 12 Years of Age The usual dosage for adults and for children weighing at least 15 kg is 2.5 mg of albuterol (one vial) administered three to four times daily by nebulization.

Children weighing < 15 kg who require < 2.5 mg/dose (i.e., less than a full vial) should use albuterol inhalation solution, 0.5% instead of albuterol inhalation solution, 0.083%.

More frequent administration or higher doses are not recommended.

To administer 2.5 mg of albuterol, administer the entire contents of one sterile unit dose vial (3 mL of 0.083% inhalation solution) 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.

The use of albuterol sulfate inhalation solution can be continued as medically indicated to control recurring bouts of bronchospasm.

During this time most patients gain optimum benefit from regular use of the inhalation 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.