Albuterol 0.5% Conc(2.5mg/0.5ml)

Manufacturer NEPHRON PHARMACEUTICALS CORP. Active Ingredient Albuterol Inhalation Solution(al BYOO ter ole) Pronunciation al BYOO ter ole
It is used to open the airways in lung diseases where spasm may cause breathing problems.
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Drug Class
Bronchodilator
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Pharmacologic Class
Selective Beta2-Adrenergic Agonist
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Pregnancy Category
C
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FDA Approved
Sep 1981
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Albuterol is a 'rescue' inhaler used to quickly open up the airways in your lungs when you have trouble breathing due to asthma or COPD. It works by relaxing the muscles around your airways, making it easier to breathe. It's used for sudden breathing problems, not for daily prevention.
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How to Use This Medicine

Taking Your Medication Correctly

To use this medication safely and effectively, follow your doctor's instructions and read all the information provided. This medication is for inhalation only, using a special machine called a nebulizer, which delivers the liquid solution directly into your lungs.

Important Usage Guidelines

Do not use the solution if it appears cloudy, is leaking, or contains particles.
Do not use the solution if it has changed color.
Never mix other medications with this solution in the nebulizer.

Storing and Disposing of Your Medication

To maintain the quality and safety of your medication:
Store it at room temperature, protected from light.
Keep it in a dry place, avoiding storage in a bathroom.
Store unused containers in their original foil pouch until you are ready to use them.
Check the packaging for information on how long the vials can be stored after the pouch has been opened.
Keep all medications in a secure location, out of the reach of children and pets.

What to Do If You Miss a Dose

If you take this medication on a regular schedule:
Use a missed dose as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and return to your regular schedule.
* Do not take two doses at the same time or take extra doses.
If you use this medication as needed, do not use it more frequently than directed by your doctor.
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Lifestyle & Tips

  • Use exactly as prescribed by your doctor. Do not use more often or at higher doses than recommended.
  • Understand the difference between your 'rescue' inhaler (albuterol) and your 'controller' medications (if prescribed). Albuterol is for quick relief, not for daily maintenance.
  • Proper nebulizer technique is crucial for effective delivery. Follow instructions provided by your healthcare provider or pharmacist.
  • Rinse your mouth with water after each use to minimize dry mouth and potential for oral thrush (though less common with nebulized solution than inhaled corticosteroids).
  • Keep track of how often you use your albuterol. Increased use (e.g., more than twice a week for symptoms, not exercise-induced) may indicate worsening asthma and requires medical attention.
  • Avoid triggers that worsen your breathing problems (e.g., allergens, smoke, cold air).

Dosing & Administration

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Adult Dosing

Standard Dose: 2.5 mg (0.5 mL of 0.5% solution) administered 3 to 4 times daily by nebulization.
Dose Range: 2.5 - 5 mg

Condition-Specific Dosing:

acute_bronchospasm: 2.5 mg (0.5 mL of 0.5% solution) administered 3 to 4 times daily by nebulization. May be repeated every 4-6 hours as needed. For severe exacerbations, more frequent administration (e.g., every 20 minutes for 3 doses) may be used under medical supervision.
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Pediatric Dosing

Neonatal: Not established for routine use; use with extreme caution and under specialist guidance.
Infant: Not established for routine use; use with extreme caution and under specialist guidance. Some sources suggest 0.05-0.15 mg/kg/dose (minimum 1.25 mg) for infants >1 month, but typically 1.25 mg or 2.5 mg for children >2 years.
Child: For children 2-12 years: 2.5 mg (0.5 mL of 0.5% solution) administered 3 to 4 times daily by nebulization. For acute exacerbations, 1.25 mg or 2.5 mg every 20 minutes for 3 doses, then 2.5 mg every 1-4 hours as needed.
Adolescent: Same as adult dosing: 2.5 mg (0.5 mL of 0.5% solution) administered 3 to 4 times daily by nebulization.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment recommended for inhaled albuterol.
Moderate: No specific adjustment recommended for inhaled albuterol.
Severe: No specific adjustment recommended for inhaled albuterol. Monitor for increased systemic effects due to potential accumulation of albuterol and its metabolites.
Dialysis: No specific adjustment recommended. Albuterol is not significantly removed by dialysis.

Hepatic Impairment:

Mild: No specific adjustment recommended.
Moderate: No specific adjustment recommended.
Severe: No specific adjustment recommended. Monitor for increased systemic effects.

Pharmacology

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Mechanism of Action

Albuterol is a selective beta2-adrenergic agonist. It acts by stimulating beta2-adrenergic receptors in the smooth muscle of the bronchial tree, leading to activation of adenyl cyclase and an increase in intracellular cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels cause relaxation of bronchial smooth muscle, inhibition of mediator release from mast cells, and to a lesser extent, inhibition of microvascular leakage and enhancement of mucociliary clearance. This results in bronchodilation and relief of bronchospasm.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 10-20% of the inhaled dose reaches the lower airways. The remaining portion is deposited in the oropharynx and swallowed, leading to systemic absorption. Oral bioavailability is approximately 50%.
Tmax: Bronchodilation onset within 5-15 minutes. Peak bronchodilation typically occurs within 60-90 minutes.
FoodEffect: Not applicable for inhaled administration.

Distribution:

Vd: Approximately 150 L (in adults).
ProteinBinding: Approximately 10% bound to plasma proteins.
CnssPenetration: Limited, but can cause CNS effects (e.g., tremor, nervousness) at higher systemic concentrations.

Elimination:

HalfLife: Approximately 3.8 to 5 hours (systemic half-life).
Clearance: Not precisely quantified for inhaled route, but rapid systemic clearance.
ExcretionRoute: Primarily renal (80-100% of the dose excreted in urine within 24 hours, with 60% as unchanged drug and 20% as the sulfate conjugate).
Unchanged: Approximately 60% of the systemically absorbed dose is excreted unchanged in urine.
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Pharmacodynamics

OnsetOfAction: 5-15 minutes
PeakEffect: 60-90 minutes
DurationOfAction: 4-6 hours

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:

Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Fainting
+ Changes in eyesight
Signs of low potassium levels, such as:
+ Muscle pain or weakness
+ Muscle cramps
+ Abnormal heartbeat
Chest pain or pressure
Rapid or irregular heartbeat
Severe breathing problems, which can be life-threatening, especially when using an inhaler or liquid for breathing in. This may occur after the first use of a new canister or vial of this medication, or shortly after taking a dose. If you experience trouble breathing, worsening breathing, wheezing, or coughing, seek medical help immediately.

Other Possible Side Effects

As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, or if they bother you or persist, contact your doctor:

Feeling nervous or excitable
Dizziness or headache
Upset stomach or vomiting
Shakiness
Throat irritation
Runny nose

This is not an exhaustive list of possible side effects. If you have questions or concerns, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Worsening shortness of breath or wheezing after using albuterol (paradoxical bronchospasm). Seek immediate medical attention.
  • Chest pain or discomfort, fast or irregular heartbeat.
  • Severe dizziness or fainting.
  • Increased tremor or nervousness that is bothersome or interferes with daily activities.
  • Symptoms not improving or worsening after using the medication as directed.
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, any of its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you are currently taking another medication similar to this one. If you are unsure, consult your doctor or pharmacist for clarification.

Please note that this is not an exhaustive list of all potential interactions with this medication. To ensure your safety, it is crucial to discuss the following with your doctor and pharmacist:

All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Your existing health problems

Before starting, stopping, or modifying the dose of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. To ensure safe use, do not exceed the prescribed dose or frequency, as overdoses have been fatal. If you experience any concerns, consult your doctor immediately.

If you find that your usual dose is not providing adequate relief, your symptoms are worsening, or you need to use this medication more frequently than prescribed, notify your doctor right away.

If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels while taking this medication.

Before taking this medication, inform your doctor if you are pregnant, planning to become pregnant, or are breast-feeding. Your doctor will discuss the potential benefits and risks of using this medication during pregnancy or breast-feeding to ensure the best outcome for you and your baby.
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Overdose Information

Overdose Symptoms:

  • Tachycardia (fast heart rate)
  • Palpitations (pounding heart)
  • Tremor (shaking)
  • Nervousness
  • Headache
  • Dizziness
  • Nausea
  • Vomiting
  • Hyperglycemia (high blood sugar)
  • Hypokalemia (low potassium levels)
  • Metabolic acidosis

What to Do:

Seek immediate medical attention or call Poison Control. In the US, call 1-800-222-1222. Treatment is supportive and symptomatic. Consider cautious use of a cardioselective beta-blocker in severe cases, but only under strict medical supervision due to risk of bronchospasm.

Drug Interactions

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Major Interactions

  • Beta-blockers (non-selective, e.g., propranolol): May block the bronchodilatory effect of albuterol and produce severe bronchospasm in asthmatic patients. Avoid concomitant use.
  • Monoamine Oxidase Inhibitors (MAOIs) and Tricyclic Antidepressants (TCAs): May potentiate the cardiovascular effects of albuterol. Use with extreme caution or avoid within 14 days of discontinuing MAOIs/TCAs.
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Moderate Interactions

  • Diuretics (loop or thiazide): May exacerbate ECG changes and/or hypokalemia associated with beta-agonists, especially at high doses. Monitor potassium levels.
  • Digoxin: Albuterol may decrease serum digoxin levels. Monitor digoxin levels.
  • Other sympathomimetics: Concomitant use may potentiate adverse cardiovascular effects. Use with caution.

Monitoring

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Baseline Monitoring

Pulmonary Function Tests (e.g., FEV1, Peak Flow)

Rationale: To establish baseline lung function and assess severity of asthma/COPD.

Timing: Prior to initiation of therapy and periodically as part of routine asthma/COPD management.

Heart Rate and Blood Pressure

Rationale: Albuterol can cause cardiovascular effects (tachycardia, palpitations, hypertension).

Timing: Prior to initiation, especially in patients with pre-existing cardiovascular disease.

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Routine Monitoring

Frequency of Albuterol Use

Frequency: Daily patient self-monitoring

Target: As needed, typically not more than 2 days a week for symptom control (excluding exercise-induced bronchospasm). Increased use indicates worsening asthma control.

Action Threshold: Use of albuterol more than twice a week (excluding exercise-induced bronchospasm) suggests inadequate asthma control and warrants re-evaluation of therapy.

Symptoms of Bronchospasm (wheezing, shortness of breath, cough, chest tightness)

Frequency: Daily patient self-monitoring

Target: Resolution or significant improvement of symptoms.

Action Threshold: Persistent or worsening symptoms, or increased need for rescue inhaler, indicates inadequate control or worsening condition.

Adverse Effects (tremor, nervousness, palpitations, tachycardia)

Frequency: Regularly, especially during initial therapy or dose adjustments.

Target: Absence or mild, tolerable effects.

Action Threshold: Persistent or severe adverse effects warrant dose reduction or alternative therapy.

Serum Potassium (if high doses or concomitant diuretics)

Frequency: Periodically, as clinically indicated.

Target: 3.5-5.0 mEq/L

Action Threshold: Hypokalemia (<3.5 mEq/L) warrants intervention.

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Symptom Monitoring

  • Wheezing
  • Shortness of breath (dyspnea)
  • Cough
  • Chest tightness
  • Increased work of breathing
  • Paradoxical bronchospasm (rare, but severe worsening of breathing immediately after use)

Special Patient Groups

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Pregnancy

Albuterol is Pregnancy Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Studies in animals have shown adverse effects, but there are no adequate and well-controlled studies in pregnant women. Untreated asthma can pose significant risks to both mother and fetus.

Trimester-Specific Risks:

First Trimester: Potential for teratogenicity, though human data are limited and generally reassuring for inhaled beta-agonists.
Second Trimester: Generally considered safer than first trimester, but still weigh risks vs. benefits.
Third Trimester: May inhibit uterine contractions (tocolytic effect) at high doses, though unlikely with typical inhaled doses. Monitor for maternal tachycardia and hyperglycemia.
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Lactation

Albuterol is excreted into human milk. However, due to its low oral bioavailability and the small amount transferred into milk, significant systemic effects on the breastfed infant are unlikely. Use with caution and monitor the infant for adverse effects (e.g., irritability, tremor).

Infant Risk: Low risk (L3 - Moderately Safe).
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Pediatric Use

Albuterol inhalation solution is approved for children 2 years of age and older. Dosing for children under 2 years is not well-established and should be done under strict medical supervision. Children may be more susceptible to systemic adverse effects (e.g., tremor, tachycardia) at higher doses.

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Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Start with the lowest effective dose and monitor closely for adverse cardiovascular effects (e.g., tachycardia, arrhythmias) and tremor, especially in patients with co-morbidities.

Clinical Information

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Clinical Pearls

  • Albuterol is a rescue medication; it should not be used for daily maintenance unless specifically prescribed for exercise-induced bronchospasm or as part of a specific treatment plan.
  • Increased frequency of albuterol use (more than twice a week for symptom control) is a key indicator of worsening asthma control and necessitates re-evaluation of the patient's asthma action plan and controller therapy.
  • Educate patients on proper nebulizer technique to ensure optimal drug delivery to the lungs.
  • Paradoxical bronchospasm is a rare but serious adverse effect; instruct patients to seek immediate medical attention if their breathing worsens immediately after using albuterol.
  • Monitor for hypokalemia, especially in patients receiving high doses, concomitant diuretics, or corticosteroids.
  • Caution should be exercised in patients with cardiovascular disorders (e.g., coronary insufficiency, arrhythmias, hypertension), hyperthyroidism, diabetes mellitus, or convulsive disorders.
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Alternative Therapies

  • Other Short-Acting Beta-Agonists (SABAs): Levalbuterol (Xopenex) - R-isomer of albuterol, potentially fewer side effects.
  • Long-Acting Beta-Agonists (LABAs): Salmeterol, Formoterol, Arformoterol, Indacaterol, Olodaterol (used for maintenance, not rescue).
  • Short-Acting Muscarinic Antagonists (SAMAs): Ipratropium (Atrovent HFA) - for COPD or as an alternative for patients intolerant to SABAs.
  • Inhaled Corticosteroids (ICS): Budesonide, Fluticasone, Mometasone (for maintenance/prevention of asthma exacerbations).
  • Systemic Corticosteroids: Prednisone, Methylprednisolone (for acute severe exacerbations).
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Cost & Coverage

Average Cost: $10 - $50 per 25 x 2.5 mg/0.5 mL unit-dose vials
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.