Albuterol Sulfate Inhalation Aerosol: Indications, Dosage, and Side Effects

Overview

Albuterol sulfate inhalation aerosol is also called Salbutamol. It is an FDA (Food and Drug Administration)--approved medication. They gave the green flag on 24 October 2004. If you are suffering from acute and severe bronchospasms with asthma, you can use this drug and take its benefits.

During an asthma attack, your airway channels get tight. You can take this drug, which will remove the tightness from your constricted airway channels. That is why it is called a bronchodilator drug. Your airway muscles will relax. This medication is inhaled through the mouth and is available by prescription in several dosage forms, including powder, solution, and suspension.

Dose Form and Strength:

Inhalational Aerosol: Each package contains an 8.5 g/200 actuator pressurized aluminum canister, a red plastic actuator, a dose counter, and a white dust cover. With each actuation, 108 mcg of Albuterol sulfate (or 90 mcg of Albuterol base) is delivered from the actuator mouthpiece and 120 mcg via the canister valve.

For Patients:

How Is Albuterol Sulfate Inhalation Aerosol Used for Bronchospasms?

The muscles around the lung airways get tightened, which you can call a bronchospasm. You may also feel tightness in the chest and breathing trouble. You may have bronchospasms with other respiratory conditions, like asthma, chronic obstructive pulmonary disease, or anaphylactic reactions.

If your child is between four and 12 years old and suffers from bronchospasms, you can take an Albuterol sulfate inhalation solution. When your child takes this drug, it relaxes their airway muscles. Your child will take proper breaths for up to six hours.

How Should You Take Albuterol Sulfate Inhalation Aerosol?

You should take the Albuterol sulfate inhalation solution by reading the instructions. These instructions should be kept alongside the medication for future reference. You should follow the dose as your doctor advises. But the drug has no color, and it is clear. It should not be mixed with other nebulizer medicines. But you should immediately go to your doctor if there is no change in breathing or your symptoms get worse after taking the medications. If you want to change your dose, you should contact your doctor. If you took a larger dose, then you should also immediately call your doctor.

What Are the Things to Inform the Doctor Before Taking Albuterol Sulfate Inhalation Aerosol?

Some points you should talk to your doctor about before taking Albuterol sulfate inhalation. If your kid is allergic to the drug or if your child suffers from any other medical condition, the parent should inform the doctor. Even if your child has taken any drug previously, you should tell your doctor because there can be drug interactions, which can pose a serious risk. Provide a list of the child's medications to the doctor and pharmacist with each new prescription.

What Are the Side Effects of Albuterol Sulfate Inhalation Aerosol?

Albuterol sulfate inhalation aerosol is suitable for its effective uses, but it has its bad side, too. The side effects you may feel after taking a drug are a fast or irregular heartbeat, tremors, confusion, chest pain, and shakiness in the limbs. Less common effects are chest discomfort, cough, difficulty breathing, dizziness, and swelling of the face or eyelids. Other side effects include hives, swelling of the face and throat, and noisy breathing.

Drug Dosage and Administration:

Missed Dose:

If you miss a dose, you should take the missed dose at that time. But if it is time for your next dose, there is no need to take a missed dose. If you have any confusion, you can go to your doctor.

Overdose:

Sometimes, you may take the drug dose in excess. You may experience angina, high and low blood pressure, and seizures. Other symptoms include palpitations, nausea, dizziness, fatigue, headache, tremors, malaise, insomnia, and an exaggeration of adverse pharmacological effects. Hypokalemia may also occur. In severe cases, abuse of Albuterol sulfate inhalation aerosol can lead to cardiac arrest and death.

Drug Storage:

You should be prepared before using this drug. Storage is important. Albuterol sulfate inhalation aerosol should be stored between 20 and 25 degrees Celsius (68 and 77 degrees Fahrenheit). You should place this drug in the freezer and avoid prolonged exposure to direct sunlight. If the drug gets exposed to temperatures above 120 degrees Fahrenheit, it will burst. It is important to keep the product out of the reach of children.

For Doctors:

Indications:

Albuterol sulfate inhalation aerosol is indicated for two main purposes. First, it can benefit children aged four and older with reversible obstructive airway disease. Second, it can also benefit exercise-induced bronchospasms in the same age group.

Dosage and Administration:

• For children aged 2 to 12, the usual starting dose of Albuterol sulfate inhalation solution is either 1.25 mg or 0.63 mg. This is administered with the help of a nebulizer (three to four times and not more than that). To give a dose of 1.25 mg or 0.63 mg, use the entire content of one unit-dose vial (three mL). Adjust the nebulizer flow rate to deliver the solution over five to 15 minutes.

• For children aged six to 12 with more severe asthma (baseline FEV1 less than 60 percent of the predicted value) and those weighing more than 40 kg, or for children aged 11 to 12, the higher 1.25 mg dose may provide a better initial response.

• For children aged six and above, about 2.5 mg of Albuterol per three mL is given.

Clinical Pharmacology:

1. Mechanism of Action: The drug acts as a beta 2-adrenergic agonist. It acts on the smooth muscle receptor. This increases cyclic AMP (adenosine monophosphate), leading to muscle relaxation by lowering intracellular calcium. It relaxes all your airway smooth muscles and inhibits mediator release from mast cells. Albuterol provides significant bronchial relaxation with fewer heart effects than Isoproterenol but may still cause heart side effects in some patients. Its action lasts longer.

2. Pharmacodynamics: Albuterol sulfate inhalation solution works by selectively stimulating beta-2-adrenergic receptors. It relaxes your airways' smooth muscles and dilates them. The R-isomer, Levalbuterol, is responsible for this bronchodilation, while the S-isomer may increase bronchial reactivity. Though primarily targeting beta-2 receptors, higher doses can also affect beta-1 receptors, causing heart effects like cardiac stimulation, vasodilation, hypotension, muscle tremor, and uterine relaxation. Metabolic effects may include hyperinsulinemia, hyperglycemia, and decreased serum potassium levels.

3. Pharmacokinetics: Albuterol sulfate inhalation solution shows low systemic levels after recommended doses. In healthy volunteers, high doses resulted in mean peak plasma concentrations (Cmax) of around 4,100 pg/mL (picograms per milliliter) and systemic exposure (AUCinf) of approximately 28,426 pg/mLhr (picograms per milliliter per hour), with a half-life of about six hours. Pediatric patients (ages four to 11) had a Cmax of 1,100 pg/mL and AUC0-∞ of 5,120 pg/mLhr, with a half-life of 166 minutes.

Albuterol is mainly metabolized by the enzyme SULTIA3 (sulfotransferase family 1A member 3), with (R)-Albuterol preferentially processed in the gastrointestinal tract. It is primarily excreted through the kidneys (80 to 100 percent), with less than 20 percent in feces. Renal impairment reduces Albuterol clearance by 67 percent but does not affect its half-life.

No pharmacokinetic studies exist for neonates, elderly subjects, or those with hepatic impairment. In asthmatic patients, less than 20 percent of an inhaled dose is absorbed, with most of it recovered from the nebulizer and expired air. The elimination half-life is five to six hours after oral administration.

What Are the Contraindications of Albuterol Sulfate Inhalation Aerosol?

Some people should avoid this drug. If you have a history of hypersensitivity to Albuterol or any other components of the aerosol, please do not take this drug. In rare cases, hypersensitivity reactions, such as urticaria, angioedema, and rash, have been noted following the use of Albuterol sulfate.

What Are the Adverse Effects of Albuterol Sulfate Inhalation Aerosol?

Before using this drug, you should know about its risks. The side effects associated with Albuterol sulfate inhalation aerosol, based on clinical trials and postmarketing reports, include several categories of reactions:

1. Common Adverse Effects (Clinical Trials):

• Tremor.

• Nervousness.

• Headache.

• Chest pain.

• Infection.

• Diarrhea.

• A tongue inflammation.

• Accidental injury (nervous system).

• Anxiety.

• Dyspnea.

• Ear disorder.

• Ear pain.

• Urinary tract infection.

2. Adverse Effects in Kids (Ages Four to 11): Similar to those seen in adults and adolescents, these occur at a low incidence rate (no more significant than two percent).

3. Less Common Adverse Effects (Reported by Less than Three Percent of Patients): These include chest pain, infection, diarrhea, glossitis, accidental injury, anxiety, dyspnea, ear disorder, ear pain, and urinary tract infection.

4. Postmarketing Adverse Effects:

• Other observed effects include urticaria, angioedema, rash, bronchospasm, hoarseness, oropharyngeal edema, and arrhythmias (such as atrial fibrillation, supraventricular tachycardia, and extrasystoles).

• Additional potential reactions include angina, hypertension or hypotension, palpitations, central nervous system stimulation, insomnia, pharyngeal irritation, and high sugar levels.

5. Heart Effects: Albuterol sulfate inhalation aerosol can produce significant heart effects, including pulse rate changes, blood pressure fluctuations, and electrocardiogram changes (such as flattening of the T wave, prolongation of the QTc interval, and ST segment depression).

Warnings and Precautions:

• Paradoxical Bronchospasm: The condition where your airways constrict rather than relax after taking a bronchodilator. You may experience this condition after taking the drug. If it occurs, discontinue immediately and switch to any other drug.

• Deterioration of Asthma: If you are taking an excessive dose of Albuterol, it may affect your asthma. For this, there is a need for re-evaluation and some other treatment.

• Use of Anti-Inflammatory Agents: These drugs may not effectively control asthma. So, you should add anti-inflammatory agents early.

• Heart Effects: Albuterol can cause heart effects, including changes in pulse rate, blood pressure, and ECG readings.

• Do Not Exceed Recommended Dose: If you are taking this dose in excess, it can lead to cardiac arrest following severe asthma attacks and hypoxia.

• Immediate Hypersensitivity Reactions: Hypersensitivity reactions, including urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema, may occur.

• Coexisting Conditions: You should use caution if you are suffering from heart disorders, convulsive disorders, hyperthyroidism, or diabetes mellitus or if you are unusually responsive to sympathomimetic amines. Beta-agonists can aggravate these conditions.

• Hypokalemia: Significant hypokalemia may occur, potentially causing adverse cardiovascular effects.

What Are the Drug Interactions of Albuterol Sulfate Inhalation Aerosol?

If you are taking any other drug to cure asthma or are suffering from any other medical condition. In that case, you should immediately tell your doctor because there can be a drug interaction, which can cause complications. Drug interactions of Albuterol sulfate inhalation aerosol involve several categories, including other bronchodilators, beta-blockers, diuretics, digoxin, and certain antidepressants. Here are the detailed interactions:

• Other Sympathomimetic Aerosol Bronchodilators: The use of short-acting sympathomimetic aerosol bronchodilators or epinephrine should be avoided.

• Beta-Blockers: Beta-adrenergic-receptor blocking agents can negate the pulmonary effects of Albuterol sulfate and may induce severe bronchospasm in asthmatic patients. Typically, asthmatic patients should not be treated with beta-blockers. If necessary, cardioselective beta-blockers should be used with caution.

• Diuretics: Non-potassium-sparing diuretics (e.g., loop or thiazide diuretics) can cause ECG changes and/or hypokalemia, which can be exacerbated by beta-agonists like Albuterol, especially if the beta-agonist dose is exceeded. Co-administration requires caution, and potassium levels should be monitored.

• Digoxin: Albuterol has been shown to decrease serum digoxin levels by 16 percent to 22 percent following single-dose administration. Although the clinical significance of chronic use in obstructive airway disease patients is unclear, monitoring serum digoxin levels in these patients is advisable.

• Monoamine Oxidase Inhibitors (MAOIs) and Tricyclic Antidepressants: The drug should be taken with care in people who are currently on monoamine oxidase inhibitors (MAOIs) or tricyclic antidepressants or within two weeks of discontinuing these medications, as the heart effects of Albuterol may be potentiated.

Clinical Studies

1. Bronchospasm Associated With Asthma

Adult and Adolescent Patients (12 Years and Older): A six-week, randomized, double-blind, placebo-controlled trial compared Albuterol sulfate inhalation aerosol (58 patients) to a matched placebo hydrofluoroalkane (HFA) inhalation aerosol (58 patients) in asthmatic patients aged 12 to 76 years at a dose of 180 mcg (microgram) four times daily. Additionally, a marketed active comparator, the HFA-134a Albuterol inhaler (56 patients), was included.

Results showed that two inhalations of Albuterol sulfate showed an improvement in forced expiratory volume in 1 second over pre-treatment values compared to placebo, with effects comparable to the active comparator. Specifically, 31 of the 58 patients treated with Albuterol sulfate achieved a 15 percent. The median times for onset, peak effect, and duration of effect were 8.2 minutes, 47 minutes, and approximately 3 hours, respectively. Some patients experienced effects lasting up to six hours.

A single-dose, placebo-controlled, crossover study demonstrated that Albuterol sulfate inhalation aerosol, at doses of 90, 180, and 270 mcg, produced bronchodilator responses significantly greater than placebo and comparable to the marketed active comparator.

Pediatric Patients (Four to 11 Years): A 3-week, randomized, double-blind, placebo-controlled trial compared the same formulation of Albuterol as in Albuterol sulfate inhalation aerosol (50 patients) to a matched placebo HFA inhalation aerosol (45 patients) in asthmatic children aged four to 11 years at a dose of 180 mcg four times daily. FEV1 measurements demonstrated that two inhalations of Albuterol produced a greater improvement in FEV1 compared to placebo.

In this study, 21 of 50 pediatric patients achieved a 15 percent increase in FEV1 within 30 minutes post-dose on day 1. The median times for onset, peak effect, and duration of effect were 10 minutes, 31 minutes, and approximately four hours, respectively. Some pediatric patients experienced effects lasting up to six hours.

A single-dose, placebo-controlled, crossover study in 55 pediatric patients aged four to 11 years showed that Albuterol sulfate inhalation aerosol at doses of 90 and 180 mcg produced significantly greater bronchodilator responses than placebo.

2. Exercise-Induced Bronchospasm

A randomized, single-dose, crossover study in 24 adults and adolescents with exercise-induced bronchospasm (EIB) demonstrated that two inhalations of Albuterol sulfate inhalation aerosol were taken half an hour before exercise. Specifically, 83 percent (20 of 24) of patients maintained FEV1 within 80 percent of post-dose, pre-exercise baseline values, compared to 25 percent (six of 24) of patients when they received a placebo.

Usage In Specific Population:

Pregnancy: The research studies do not show a risk of significant birth defects or miscarriage. However, animal studies show that the drug can cause cleft palate in mice and cranioschisis in rabbits at high doses.

If you are pregnant with poorly or moderately controlled asthma, you face increased risks of prematurity, low birth weight, and preeclampsia. So, you should go to your doctor for early monitoring. You should not use this drug during labor because it may interfere with uterine contractility.

Lactation: There is no data on the presence of Albuterol in human milk or its effects. Any presence in breast milk would likely have low oral bioavailability.

Pediatric Use: If your child is 12 years or older, you can give this drug. This is based on clinical trials comparing doses with a placebo. A clinical trial showing the bronchodilatory effect of Albuterol supports safety in children aged 4 to 11. However, the effectiveness for this age group is extrapolated from trials in older children and adults. The safety and efficacy of Albuterol sulfate inhalation aerosol in children below four years have not been established.

Geriatric Use: People over the age of 65 years are not included. Adults should use this drug with care. As the kidney substantially excretes Albuterol, patients with impaired renal function may face a greater risk of toxic reactions, necessitating careful dose selection and potential monitoring of renal function

Key Takeaway From iCliniq

Albuterol sulfate inhalation aerosol may relax your muscles. It dilates the tight muscles and provides relief. Children above 12 years of age are safe when using this drug under their physician’s supervision. If you want to know more about this drug, you can contact our doctor at icliniq.com.