Drug Information: Albuterol
Albuterol is a short-acting selective beta2-adrenergic receptor agonist (sympathomimetic) class drug. It is used for the treatment and prevention of bronchospasms associated with asthma and chronic obstructive pulmonary disease (COPD). Albuterol aids bronchodilation by relaxing bronchial smooth muscles, thus increasing air flow into the lungs. Albuterol is a gold standard prescription drug with a proven track record. It is marketed in Canada under various brand names, such as Apo-Salvent, Ventolin Inhaler, Ventolin Nebules P.F., Ventolin Respirator and Ventolin Rotacaps.
Albuterol is a bronchodilator, which helps to open up the airways and make it easier for air to flow to the lungs. This inhaler is used to treat bronchospasms, or airway spasms, and is used in the treatment of asthma and chronic obstructive pulmonary disease, which is known as COPD.
Albuterol is classified as a beta-adrenergic receptor agonist, and helps to stimulate the muscles that surround the airways. During a bronchospasm, the muscles around the airways tighten and become constricted. Albuterol works by relaxing the muscles within the airways, which increases the amount of air that goes into the lungs.
Indication/Usage: Albuterol is primarily approved for the indication of bronchospasms associated with various medical conditions such as asthma and chronic obstructive pulmonary disease. Albuterol is also used, in combination with other drugs, for various other conditions like cystic fibrosis and congenital myasthenic syndrome subtypes.
Other uses for Albuterol include exercise-induced asthma, obstetrics, uterine smooth muscle relaxation, and the delay of premature labor.
Additionally, Albuterol may be used for emphysema or chronic bronchitis treatment if symptoms are related to airway obstruction.
Dose, Dosage forms and Administration: Albuterol is available in various dosage forms and strengths, such as disintegrating tablets, capsules, aerosol, syrup, solution, etc. Albuterol tablets are available in 2mg or 4mg strengths, while extended release tablets are available in 4mg and 8mg strengths. The recommended dose of disintegrating tablets or syrup is 2-4mg three to four times daily, while the extended release tablet dosage is 4-8 mg every 12 hours. The Albuterol aerosol recommended dosage is 1-2 inhalations every 4-6 hours for the prevention of general bronchospasms, and two inhalations 15 minutes prior to exercise for exercise induced bronchospasms. The recommended nebulizer is prescribed in different doses of 0.63 mg, 1.25mg or 2.5mg three to four times daily.
Albuterol tablets should be stored at room temperature (15 C to 30 C). The aerosol container must be kept away from heat and flame.
Mechanism of Action: Albuterol is a sympathomimetic class drug whose selective agonistic activity towards beta2-adrenergic receptors activates beta2 receptors present in the smooth muscles of the airway. This beta2 receptor activation further leads to the activation of adenylcyclase which results in increased concentration of intracellular cyclic AMP. Subsequently, the intracellular cyclic AMP activates protein kinase A and inhibits myosin phosphorylation, which results in decreased intracellular calcium concentration and ultimately results in smooth muscle relaxation. Albuterol relaxes smooth muscles from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations also help decrease the concentration of mast cell mediators in the respiratory tract.
Side-Effects and Safety Profile: Various non-serious side-effects associated with Albuterol usage include: headache, dry mouth, nausea, unusual taste, nervousness, vomiting, facial swelling, fingers or toes numbness, dizziness, skin rashes, etc.
Albuterol may cause various moderately-serious side-effects to include: anxiety, muscle cramps, sleep and behavior issues, unusual hoarseness, flushing, increased sweating, trembling.
Serious side-effects associated with Albuterol usage include: tremor, palpitation, tachycardia, arrhythmia, urticaria, myocardial ischemia, paradoxical bronchospasm, angioedema, hypotension, renal failure, hypokalemia, chest pain, wheezing, dyspnea etc. Patients experiencing any serious side-effects should receive immediate medical attention.
Warnings/Contraindications:
- Albuterol is contraindicated in patients who have an allergic history to it.
- Albuterol should be prescribed only after a careful examination of previous cardiac experiences such as high blood pressure, congestive heart failure (CHF), arrhythmia, coronary insufficiency, and other disorders such as epilepsy, diabetes, and overactive thyroid issues. These patients must be closely monitored while taking Albuterol.
- Albuterol is classified as pregnancy category C class drug which has shown teratogenic effects in preclinical studies. It has not yet been studied in pregnant women and therefore should not be prescribed to them.
- It is unknown whether Albuterol excretes via breast milk; therefore, it should not be prescribed to nursing women.
- Albuterol is reported to cause life threatening paradoxical bronchospasm.
- Cardiovascular events: Albuterol is reported to cause significant cardiovascular events, such as T wave flattening, QTc prolongation, and ST segment depression.
- Albuterol may deteriorate asthma acutely or chronically.
- Large doses of Albuterol have been reported to aggravate pre-existing diabetes, hypokalemia and ketoacidosis.
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