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Albuterol

Albuterol opens up the medium and large airways in the lungs, and is used to treat asthma, exercise-induced bronchoconstriction, and chronic obstructive pulmonary disease (COPD).

It may also be used to treat high blood potassium levels.

Usually used with an inhaler or nebulizer, but it is also available in a pill, liquid, and intravenous solution.

Onset of action with inhalation is typically within 15 minutes and lasts for two to six hours.

Ventolin, Proventil, are trade names.

Pregnancy category US: C (Risk not ruled out)

Routes of administration by mouth, inhalational, IV

Metabolism occurs in the liver.

Onset of action <15 min by inhalation, and less than 30 min by pill.

Elimination half-life 3.8–6 hours.

Duration of action2–6 hrs

Excretion by Kidney

Common side effects include: tremulousness, headache, fast heart rate, dizziness, and feeling anxious.

Serious side effects may include: worsening bronchospasm, irregular heartbeat, and low blood potassium levels.

It can be used during pregnancy and breastfeeding.

It is a short-acting β2 adrenergic receptor agonist which works by causing relaxation of airway smooth muscle.

Typically used to treat bronchospasm as well as chronic obstructive pulmonary disease.

One of the most common medicines used in rescue inhalers, as a short-term bronchodilator to alleviate asthma attacks.

Intravenous albuterol can be used as a tocolytic to relax the uterine smooth muscle to delay premature labor.

iIs role as a tocolytic has largely been replaced by the calcium channel blocker nifedipine, which is more effective and better tolerated.

Can be be used to treat acute hyperkalemia, as it stimulates potassium flow into cells, thus lowering the potassium in the blood.

Albuterol side effects include: fine tremor, anxiety, headache, muscle cramps, dry mouth, and palpitation,tachycardia, arrhythmia, flushing of the skin, myocardial ischemia, disturbances of sleep and behaviour.

Rarely occurring are allergic reactions of paradoxical bronchospasms, urticaria, angioedema, hypotension, and collapse.

High doses may cause hypokalemia.

It is more selective for β2 receptors, which are the predominant receptors on the bronchial smooth muscles.

When β2 receptors are activated , it causes adenylyl cyclase to convert ATP to cAMP,

Activation of these receptors causes adenylyl cyclase to convert ATP to cAMP, beginning the signalling cascade that ends with the inhibition of myosin phosphorylation and lowering the intracellular concentration of calcium ions.

Myosin phosphorylation and calcium ions are necessary for muscle contractions

The increased levels of cAMP inhibits inflammatory cells in the airway, such as basophils, eosinophils, and especially mast cells, from releasing inflammatory mediators and cytokines.

The albuterol β2 receptor agonist also increases the conductance of channels sensitive to calcium and potassium ions, leading to hyperpolarization and relaxation of bronchial smooth muscles.

It is either filtered out by the kidneys directly, a metabolite is excreted in the urine.

It is a racemic mixture.

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