Albuterol

Albuterol is a bronchodilator that is widely used to relieve symptoms of asthma, chronic obstructive pulmonary disease (COPD), and other conditions accompanied by bronchospasm. The drug helps expand the airways quickly, making it easier to breathe and reducing shortness of breath.

Medicine is available in various forms, including inhalers, solutions for nebulizers and tablets, which allows you to choose a convenient option depending on the individual needs of the patient. The drug takes effect within minutes of use, providing rapid symptomatic relief.

Trade name

Albuterol is known by a variety of trade names depending on the country and manufacturer. The most common ones are:

• Ventolin
• Salbutamol
• ProAir
• Proventil

International Nonproprietary Name (INN)

Albuterol is the name adopted in the United States, but in international practice the term “salbutamol” is used.

Form of release

Albuterol is available in several forms depending on the route of administration:

• Aerosol for inhalation (metered-dose inhaler, such as Ventolin HFA)
• Inhalation solution (used with a nebulizer)
• Tablets (usually 2 mg or 4 mg)
• Cyrup (for oral administration, more commonly for children)
• Powder for inhalation (in disk inhaler form, such as AccuNeb)

Composition

Acting substance:

Salbutamol (in the form of sulfate - Salbutamol sulfate). It is a selective agonist of beta-2-adrenoreceptors, which relaxes bronchial smooth muscle, facilitating breathing.

Auxiliary components:

Aerosol for inhalation:

• Propellant (e.g., hydrofluoroalkane - HFA-134a)
• Ethanol (in some cases)
• Oleic acid (as a stabilizer)

Nebulizer solution:

• Sodium chloride (physiologic solution)
• Water for injection
• Sulfuric acid (for pH adjustment, if necessary)

Pills:

• Lactose
• Starch
• Magnesium stearate
• Cellulose and other fillers

Syrup:

• Sugar syrup
• Citric acid
• Flavorings (e.g. orange)
• Preservatives (sodium benzoate)

Pharmacologic properties

Pharmacodynamics (how the drug works)

Albuterol is a selective agonist of beta-2-adrenoreceptors. Its main mechanism of action:

• Bronchodilation: relaxes bronchial smooth muscle, dilating the airways.
• Fast onset of action: the effect occurs in 5-15 minutes and lasts 4-6 hours.
• Additional effects:
  • Reduces the release of inflammatory mediators (histamine, leukotrienes).
  • Improves mucociliary clearance (excretion of mucus).
• Selectivity: acts predominantly on beta-2 receptors, but at high doses may cause tachycardia or tremor.

Main use: relief and prophylaxis of bronchospasm.

Pharmacokinetics (absorption, distribution, metabolism, excretion)

Absorption

• Inhalation form: 10-20% of the dose reaches the lungs, maximum concentration - after 2-4 hours.
• Oral form: well absorbed, but bioavailability is reduced to 50% due to metabolism in the liver.

Distribution

• Volume of distribution is 0.2 liters/kg.
• It penetrates through the placenta and into breast milk in small amounts.
• Binding to plasma proteins - about 10%.

Metabolism

Metabolized in the liver to form inactive salbutamol-4'-O-sulfate During inhalation, most of the drug is excreted unchanged.

Excretion

• Half-life: 3-6 hours.
• It is excreted through the kidneys (70-80% within 24 hours), the rest - with feces.

Key features

• Inhalation form is preferred because it acts locally and reduces the risk of side effects.
• Peroral forms may cause systemic effects (tremor, tachycardia) due to entry into the blood.

Indications for the use of Albuterol

Albuterol is used for the treatment and prevention of conditions associated with reversible airway obstruction. The main diseases and conditions for which the drug is prescribed include:

1. Bronchial asthma:
   • Counteracting acute attacks of bronchospasm (including inhaled administration for rapid relief of symptoms).
   • Prevention of attacks caused by exercise, allergens, or other triggers.
   • Supportive therapy as part of complex treatment (usually in combination with glucocorticosteroids).
2. Chronic obstructive pulmonary disease (COPD):
   • Ease symptoms of dyspnea and bronchospasm in patients with COPD, especially during exacerbations.
   • Use as a symptomatic treatment to improve respiratory function.
3. Bronchobstructive syndrome:
   • In various diseases (e.g., bronchitis, emphysema) accompanied by narrowing of the airways.
4. Prevention of exercise-induced bronchospasm:
   • Prescribed before physical activity in patients with exercise-induced asthma (inhalation 15-30 minutes before exercise).
5. Acute bronchospasm:
   • In allergic reactions, respiratory tract infections, or exposure to irritants resulting in sudden bronchoconstriction.
6. Other conditions (in some cases):
   • Treatment of hyperkalemia (in high doses via nebulizer, under medical supervision, as salbutamol stimulates potassium transport into cells).
   • Pediatric use for obstructive conditions such as bronchiolitis (as prescribed by a physician).

Notes

• Albuterol is most often used in inhaled form (aerosol or nebulizer solution), as this provides rapid action directly in the respiratory tract.
• Peroral forms (tablets, syrup) are used less frequently, usually when inhalation administration is not possible or in long-term therapy.

Contraindications for use

Albuterol has a number of contraindications in which its use is either completely prohibited (absolute contraindications) or requires caution (relative contraindications). Here are the main conditions:

Absolute contraindications

1. Hypersensitivity:
   • Allergic reaction to salbutamol or any of the drug's excipients (e.g., propellants in inhalers).
2. Tachyarrhythmias:
   • Severe cardiac rhythm disturbances (e.g., paroxysmal tachycardia, atrial fibrillation) in which beta-receptor stimulation may aggravate the condition.
3. Uncontrolled arterial hypertension:
   • Significant increase in blood pressure that cannot be corrected, as the drug may increase the burden on the cardiovascular system.
4. Severe heart failure:
   • Decompensated form, in which additional cardiac stimulation is undesirable.
5. Pheochromocytoma:
   • Adrenal tumor accompanied by excessive release of catecholamines, as albuterol may increase adrenergic effects.

Related contraindications (use with caution)

1. Diseases of the cardiovascular system:
   • Ischemic heart disease (angina pectoris, suffered myocardial infarction).
   • Arterial hypertension (controlled).
   • Cardiomyopathy (especially hypertrophic obstructive).
2. Diabetes mellitus:
   • Uncontrolled diabetes, as albuterol may increase blood glucose levels by activating glycogenolysis.
3. Hyperthyroidism:
   • Elevated thyroid function, in which increased adrenergic stimulation may exacerbate symptoms (tachycardia, tremor).
4. Convulsive disorders:
   • Epilepsy or susceptibility to seizures, as the drug may stimulate the central nervous system.
5. Pregnancy and lactation:
   • Albuterol penetrates the placental barrier and into breast milk. Use only for strict indications if the benefit to the mother outweighs the risk to the fetus or child. (Note: in obstetrics, salbutamol is sometimes used as a tocolytic to inhibit preterm labor, but this is a separate indication under strict supervision.)
6. Glaucoma:
   • Particularly the closed-angle form, as the drug may increase intraocular pressure.
7. Rnal or hepatic insufficiency:
   • Severe renal or hepatic dysfunction may slow the excretion of metabolites, requiring dosage adjustment.

Additional Remarks

• Paradoxical bronchospasm: In rare cases, inhalation of albuterol may cause worsening of breathing due to airway irritation. This is not a contraindication, but a side effect requiring withdrawal of the drug and medical attention.
• Children and the elderly: There are no absolute age contraindications, but the dosage should be carefully selected.

Method of administration and dosage

Method of administration and dosage depend on the form of drug release (inhalation, oral, etc.), age of the patient and severity of the condition. The following are general recommendations based on standard medical evidence. However, the exact dosage and regimen should be prescribed by a physician.

1. Inhalation form (aerosol, nebulizer solution)

How to use:

• Aerosol (metered-dose inhaler):
  • Before use, shake the canister. Take a deep breath in through the mouth while pressing the inhaler to release the dose. Hold your breath for 10 seconds, then exhale slowly. Between inhalations - an interval of 1-2 minutes.
  • It does not depend on food intake.
• Solution for nebulizer:
  • Diluted with saline solution (if indicated in the instructions) and used through a nebulizer. The treatment lasts 5-15 minutes. Does not require association with food.

Dosages for adults:

• Cupping of acute bronchospasm:
  • Aerosol: 1-2 breaths (100-200 mcg salbutamol) once, repeated 4-6 hours later if necessary.
  • Nebulizer: 2.5-5 mg once, up to 4 times a day.
• Prophylaxis (e.g., before exertion):
  • Aerosol: 2 breaths (200 mcg) 15-30 minutes before activity.

Dosages for children:

• Aerosol:
  • Children 2-12 years of age: 1-2 breaths (100-200 mcg) as needed, not more than 4 times a day.
  • Under 2 years of age: only as prescribed by a physician.
• Nebulizer:
  • Children 2-12 years of age: 0.1-0.15 mg/kg body weight (usually 1.25-2.5 mg) per inhalation, up to 3-4 times per day.
  • Under 2 years of age: individualized (e.g., 0.625-1.25 mg).

2. Oral form (tablets, syrup)

How to take:

• Pills:
  • Taken orally, drinking a small amount of water. Meal time is not affected, but to reduce gastric irritation it is better to take after meals.
• Syrup:
  • Taken orally with a measuring spoon or syringe. May be taken with water, preferably after meals.

Dosages for adults:

• Tablets: 2-4 mg 3 to 4 times daily. The maximum daily dose is 32 mg.
• Syrup: 5-10 ml (2-4 mg) 3-4 times a day.

Dosages for children:

• Tablets (usually from 6 years of age):
  • 2 mg 3 to 4 times daily.
• Cyrup:
  • 2-6 years: 1-2 mg (2.5-5 mL) 3 times daily.
  • 6-12 years: 2 mg (5 ml) 3-4 times a day.
  • Under 2 years: 0.1 mg/kg body weight 3 times a day (strictly as prescribed by a doctor).

Dose adjustment in certain conditions

1. Rnal insufficiency:
   • Inhalation form: No correction is usually necessary, since the main action is local and systemic absorption is minimal.
   • Oral form: In severe renal impairment (creatinine clearance < 30 mL / min), the dose should be reduced (e.g., to 2 mg twice daily) because of delayed excretion of metabolites. Physician supervision is required.
2. Hepatic insufficiency:
   • Inhalation form: No correction is necessary because metabolism in the liver plays a minor role.
   • Oral form: In severe hepatic insufficiency (e.g., cirrhosis) the dose is reduced (e.g., to 2 mg 2-3 times a day), since the drug is metabolized in the liver via sulfation. Cumulation is possible.
3. Elderly patients:
   • Frequently start with the lowest dose (e.g., 1 inh or 2 mg orally) due to hypersensitivity to side effects (tachycardia, tremor).
4. Pregnancy:
   • Use the standard dosage only for strict indications. Excessive doses are undesirable due to the risk of tachycardia in the fetus.

General recommendations

• Frequency of use: Do not exceed 4 times daily without medical advice to avoid tolerance or side effects.
• Control: If attacks become more frequent or dose increases are necessary, therapy should be revised (possibly adding glucocorticosteroids).
• Inhalation technique: For children and the elderly, a spacer (additional device for the inhaler) may be required for proper delivery of the drug.

Albuterol side effects

Albuterol, like any medicine, can cause undesirable reactions of the body. The frequency and severity of side effects depend on the form of administration (inhalation or oral), dosage and individual sensitivity of the patient. The following are the main possible side effects, categorized by body system:

Frequently occurring side effects

1. Nervous system:
   • Tremor (hand tremor) - especially at high doses.
   • Headache.
   • Nervousness, restlessness.
2. Cardiovascular system:
   • Tachycardia (rapid heartbeat).
   • Sensation of palpitations (palpitation).
   • Elevation of blood pressure (less common).
3. Repiratory system:
   • Irritation of the throat or dry mouth (due to inhalation administration).
   • Cough (sometimes due to inhalation administration).
4. Muscular:
   • Muscle spasms or cramps (usually mild).

Less frequent side effects

1. Gastrointestinal tract (more common with oral administration):
   • Nausea.
   • Vomiting.
   • Gastric discomfort.
2. Metabolism:
   • Hypokalemia (decreased blood potassium levels) - at high doses, especially with nebulizer use.
   • Hyperglycemia (increased blood sugar levels) - in diabetic patients.
3. Skin reactions:
   • Rash.
   • Itching.
   • Eczema (in case of allergic reaction).
4. Cardiovascular system:
   • Arrhythmias (rare, in overdose or in predisposed patients).

Rare but serious side effects

1. Paradoxical bronchospasm:
   • Deterioration of breathing immediately after inhalation due to airway irritation. Requires immediate withdrawal of the drug and medical attention.
2. Anaphylactic reactions:
   • Allergic shock, Quincke's edema (extremely rare, in case of hypersensitivity).
3. Central nervous system:
   • Dizziness.
   • insomnia.
   • In rare cases - confusion or hallucinations (in overdose).

Special features

• Inhalation form: Side effects are usually less severe because the drug acts locally and systemic absorption is minimal.
• Oral form (tablets, syrup): Systemic effects (tachycardia, tremor) are more common due to greater absorption into the bloodstream.
• Children: Tremor and agitation are more common.
• Elderly: Increased risk of tachycardia and arrhythmias.

Risk Factors

• Exceeding the recommended dose increases the likelihood of side effects (especially hypokalemia and tachycardia).
• Combination with other beta-adrenomimetics or stimulants (eg, caffeine) may increase adverse reactions.

Overdose

Albuterol overdose can occur when the recommended doses are exceeded, especially with frequent use of an inhaler or taking large amounts of oral forms (tablets, syrup). This condition requires immediate attention as it can lead to serious complications.

An overdose of this medication may occur if you exceed the recommended dosage.

Symptoms of overdose

Symptoms of overdose are associated with overstimulation of beta-2-adrenoreceptors and, in some cases, beta-1-receptors. They may include:

1. Cardiovascular system:
   • Pronounced tachycardia (rapid heartbeat, pulse >120 beats per minute).
   • Arrhythmias (irregular heart rhythm).
   • Elevated or, less commonly, decreased blood pressure.
   • Chest pain (a sign of ischemia in predisposed patients).
2. Nervous system:
   • Tremor (severe shaking of the hands or whole body).
   • Nervousness, anxiety, or panic.
   • Dizziness.
   • Headache.
   • In severe cases, confusion or seizures.
3. Repiratory system:
   • Faster breathing (tachypnea).
   • Sense of shortness of breath (due to overexcitement).
4. Metabolic disorders:
   • Hypokalemia (decreased blood potassium levels) - manifested by weakness, muscle spasms, or arrhythmias.
   • Hyperglycemia (increased blood sugar levels).
   • Lactoacidosis (accumulation of lactic acid, a rare symptom, accompanied by weakness and shortness of breath).
5. General symptoms:
   • Dry mouth.
   • Sweating.
   • Nausea or vomiting (more common in oral overdose).
   • Faintness or fatigue.

First aid measures

If an Albuterol overdose is suspected, it is important to act quickly to minimize the risk of complications:

1. Stop using the drug:
   • Stop using the inhaler, nebulizer, or taking the tablets/syrup immediately.
2. Provide rest:
   • Lay or sit the casualty in a comfortable position, avoid physical activity to reduce stress on the heart.
3. Call an ambulance:
   • Seek medical attention immediately (e.g. call 112 or the local emergency number), especially if tachycardia, arrhythmia, seizures or loss of consciousness are observed.
4. Provide access to fresh air:
   • Open a window or get the person out into fresh air, if safe to do so, to facilitate breathing.
5. Condition Control:
   • Monitor breathing and pulse. If breathing or cardiac arrest occurs, start resuscitative measures (indirect cardiac massage, artificial respiration) if trained.
6. Do not give food or drink:
   • Avoid giving water or food until the doctor arrives to avoid aggravating nausea or vomiting.

Treatment in a medical setting

• Antidote: Beta-blockers (e.g., propranolol) may be used to relieve excessive receptor stimulation, but only under physician supervision.
• Correction of hypokalemia: Administration of potassium preparations (intravenously) if potassium levels are low.
• Symptomatic therapy: Sedatives for anxiety, oxygen for breathing difficulties.
• Monitoring: ECG, blood tests (potassium, glucose, acid-base balance).

Notes

• Overdose is more likely to occur with inhalation use if the patient exceeds the inhalation rate (e.g., >10-20 breaths in a short period of time).
• In children and the elderly, symptoms may occur more rapidly and be more severe.
• Self-treatment in case of overdose is inadmissible - professional medical assistance is required.

Albuterol Interaction with Other Drugs

Influence on the effect of other drugs:

• Beta-blockers (e.g., propranolol, atenolol) - may decrease the effectiveness of albuterol and cause bronchospasm.
• Other β2-adrenoreceptor agonists (e.g., formoterol, salmeterol) - increased risk of side effects such as tachycardia and hypokalemia.
• Diuretics (e.g., furosemide, hydrochlorothiazide) - co-administration may increase potassium loss, which increases the risk of cardiac arrhythmias.
• Xanthines (theophylline, aminophylline) - may increase cardiovascular stimulation, which increases the risk of tachycardia and arrhythmias.
• Monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants (e.g., amitriptyline, nortriptyline) - may increase the cardiovascular effects of albuterol (hypertension, tachycardia).
• Glucocorticosteroids (e.g., prednisolone, dexamethasone) - may increase the risk of hypokalemia with prolonged use.

Compatibility with alcohol and food:

• Alcohol - may increase side effects of albuterol such as palpitations, dizziness and nervousness. Alcohol consumption is not recommended.
• Food - does not significantly affect the effect of the drug, but should be washed down with water. It is advisable to avoid foods with high caffeine content (coffee, energy drinks, chocolate), as they can increase nervousness and tachycardia.

If you are taking any other medications, it is better to consult your doctor before using albuterol.

Special indications

Use of Albuterol in pregnancy and breastfeeding

• Pregnancy:

  Albuterol is FDA Category C (risk to the fetus has not been ruled out, but data are insufficient). Use only when the expected benefit to the mother exceeds the potential risk to the fetus.

  • The drug penetrates the placental barrier. In high doses, it may cause tachycardia in the fetus or mother, and potentially inhibit uterine contractile activity (which is sometimes used in obstetrics as a tocolytic to prevent preterm labor, but under strict control).
  • It is recommended to use the lowest effective doses and preferably the inhaled form to reduce systemic exposure. Medical advice is required before use.
• Breastfeeding:

  Albuterol is excreted in small amounts with breast milk. There are no data on significant harm to the child, but the effect on newborns has not been fully studied. Allbuterol is excreted with breast milk in small amounts.

  • If the drug is necessary, preference is given to the inhaled form, as it penetrates less into the systemic bloodstream and, consequently, into the milk.
  • The child should be monitored for possible signs of agitation or tachycardia. The decision to continue breastfeeding is made by a doctor.

Effects on driving and operating machinery

Albuterol usually has no significant effect on the ability to drive vehicles or operate machinery. However, individual reactions are possible:

• Side effects such as tremor, dizziness, or nervousness may temporarily impair concentration and coordination, especially at the initiation of therapy or when the dose is exceeded.
• If the patient experiences such symptoms, one should refrain from driving or operating machinery until they disappear.

It is recommended to evaluate individual reaction to the drug before performing tasks requiring high accuracy or attention.

Particularities of use in elderly people and children

• Elderly persons:
  • Elderly patients are more likely to have comorbidities (e.g., hypertension, coronary heart disease), which increases the risk of side effects such as tachycardia or arrhythmias.
  • It is recommended to start with the lowest doses (e.g., 1 inh 100 mcg for the inhaler or 2 mg for the oral form) and monitor the condition closely.
  • Dose adjustment may be necessary if renal or hepatic dysfunction occurs, as excretion of the drug is slowed.
  • The use of a spacer with the inhaler facilitates use in the elderly with limited coordination.
• Children:
  • Albuterol is approved for use in children, subject to age-appropriate dosages (see previous answers about dosages).
  • Children are more likely to experience side effects such as tremor or agitation due to greater sensitivity to beta-adrenomimetics.
  • For toddlers (younger than 2 years of age), the drug is prescribed only by a physician, often through a nebulizer with minimal doses (e.g., 0.625-1.25 mg).
  • Inhalation technique in children requires supervision: a spacer or nebulizer mask is recommended to ensure proper delivery of the drug.
  • Parents should monitor the frequency of administration to avoid overdose.

Supplementary remarks

• Patients with chronic conditions (diabetes, hyperthyroidism) require special monitoring, as Albuterol may affect glucose levels or increase the symptoms of these conditions.
• Regularly excessive doses or increased frequency of attacks indicates inadequate control of underlying disease (e.g. asthma) - physician consultation for revision of therapy is required.

Storage conditions

Correct storage of Albuterol is important to maintain its effectiveness and safety. Conditions depend on the form of release (inhalers, solutions, tablets, syrup), but there are general recommendations.

Temperature regime

• General range: Most forms of Albuterol are stored between 15°C and 30°C (room temperature).
  • Avoid freezing and exposure to high temperatures (above 40°C).
• Specific forms:
  • Aerosol inhalers (e.g., Ventolin HFA): Store at 15-25°C. Do not leave in a car or in the sun, as heat may damage the canister or reduce effectiveness.
  • Nebulizer solution: Normally store at 15-30°C. After opening the ampoule, use immediately, do not store residue.
  • Pills: 15-30°C, in a dry place.
  • Syrup: 15-30°C, do not freeze. After opening the vial, the shelf life may be limited (usually 1 month, specify in the instructions).

Protect from light, moisture, children

• Light protection:
  • The drug should be stored in the original packaging (box, bottle or blister), which protects from direct sunlight.
  • Particularly important for syrup and solutions, as light may reduce the stability of the active ingredient.
• Protection against moisture:
  • Store in a dry place, away from bathrooms or other moist areas.
  • Inhalers and tablets are sensitive to moisture - do not open packaging before use.
  • After using the inhaler, close the protective cap to prevent the ingress of moisture.
• Child protection:
  • Store out of the reach of children, preferably in a locked cabinet or on a high shelf.
  • Inhalers and syrup may be dangerous if used accidentally by children (risk of overdose or suffocation from small parts).

Additional recommendations

• Do not store the preparation in the refrigerator, unless specified in the instructions (for example, for some solutions after opening).
• Do not use the drug after the expiration date (usually indicated on the package, is 2-3 years from the date of manufacture).
• Dispose of used inhalers or empty bottles in accordance with local regulations - do not puncture or burn aerosol cans.