Levosalbutamol/Levalbuterol; Indications, Dosage, Side Effects, Drug Interactions

Levosalbutamol/Levalbuterol; Indications, Dosage, Side Effects, Drug Interactions

Levosalbutamol/Levalbuterol also known as levalbuterol is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Salbutamol has been marketed as a racemic mixture, although beta2-agonist activity resides almost exclusively in the (R)-enantiomer. The enantioselective disposition of salbutamol and the possibility that (S)-salbutamol has adverse effects have led to the development of an enantiomerically pure (R)-salbutamol formulation known as levosalbutamol (levalbuterol). Evidence does not show that levosalbutamol works better than salbutamol, thus there may not be sufficient justification for prescribing it.

Mechanism of action of Levosalbutamol/Levalbuterol

Activation of β2 adrenergic receptors on airway smooth muscle leads to the activation of adenylate cyclase and to an increase in the intracellular concentration of 3′,5′-cyclic adenosine monophosphate (cyclic AMP). The increase in cyclic AMP is associated with the activation of protein kinase A, which in turn, inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in muscle relaxation.

Levosalbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways. Levosalbutamol acts as a functional agonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges. While it is recognized that β2 adrenergic receptors are the predominant receptors on bronchial smooth muscle, data indicate that there are beta receptors in the human heart, 10–50% of which are β2 adrenergic receptors. The precise function of these receptors has not been established. However, all β adrenergic agonist drugs can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, and restlessness symptoms, and/or electrocardiographic (ECG) changes.

Indications of Levosalbutamol/Levalbuterol

  • Bronchospasm
  • Asthma, 
  • Asthma, acute
  • Bronchiectasis
  • Bronchospasm Prophylaxis
  • Bronchial asthma,
  • Chronic bronchitis,
  • Chronic bronchopulmonary disorders
  • Levosalbutamol’s bronchodilator properties give it indications in treatment of COPD (chronic obstructive pulmonary disease, also known as chronic obstructive lung disease) and asthma.

Contra-Indications of Levosalbutamol/Levalbuterol

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The dosage of Levosalbutamol/Levalbuterol

Strengths: 0.31 mg/3 mL; 0.63 mg/3 mL; 1.25 mg/0.5 mL; 1.25 mg/3 mL; 45 mcg/inh

Chronic Obstructive Pulmonary Disease

Inhalation Aerosol

  • rust colored urine
  • 2 inhalations (90 mcg) orally every 4 to 6 hours or
  • 1 inhalation (45 mcg) orally every 4 hours

Inhalation Solution

  • Initial dose: 0.63 mg inhaled orally by nebulization three times a day (every 6 to 8 hours)
  • For severe asthma, or if not responding to initial dose: 1.25 mg inhaled orally, by nebulization, three times a day

Asthma

Inhalation Aerosol

  • 2 inhalations (90 mcg) orally every 4 to 6 hours or
  • 1 inhalation (45 mcg) orally every 4 hours

Inhalation Solution

  • Initial dose: 0.63 mg inhaled orally by nebulization three times a day (every 6 to 8 hours)
  • For severe asthma, or if not responding to initial dose: 1.25 mg inhaled orally, by nebulization, three times a day

Pediatric Chronic Obstructive Pulmonary Disease

Inhalation Aerosol

  • Less than 4 years: Not approved

4 years or older

  • 2 inhalations (90 mcg) orally every 4 to 6 hours or
  • 1 inhalation (45 mcg) orally every 4 hours

Inhalation Solution

  • Less than 6 years old: Not approved

6 to 11 years

  • Recommended dose: 0.31 mg inhaled orally by nebulization three times a day
  • Maximum dose: 0.63 mg inhaled orally three times a day

12 years or older

  • Initial dose: 0.63 mg inhaled orally by nebulization three times a day (every 6 to 8 hours)
  • For severe asthma, or if not responding to initial dose: 1.25 mg inhaled orally, by nebulization, three times a day

Pediatric Dose for Asthma

Inhalation Aerosol

  • Less than 4 years: Not approved

4 years or older

  • 2 inhalations (90 mcg) orally every 4 to 6 hours or
  • 1 inhalation (45 mcg) orally every 4 hours

Inhalation Solution

  • Less than 6 years old: Not approved

6 to 11 years

  • Recommended dose: 0.31 mg inhaled orally by nebulization three times a day
  • Maximum dose: 0.63 mg inhaled orally three times a day

12 years or older

  • Initial dose: 0.63 mg inhaled orally by nebulization three times a day (every 6 to 8 hours)
  • For severe asthma, or if not responding to initial dose: 1.25 mg inhaled orally, by nebulization, three times a day
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Side Effects of Levosalbutamol/Levalbuterol

The most common

More common

Rare

Drug Interactions of Levosalbutamol/Levalbuterol

Levosalbutamol may interact with the following drugs, supplements & may change the efficacy of drugs

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Pregnancy Catagory of Levosalbutamol/Levalbuterol

FDA Pregnancy Category C

Pregnancy

Levalbuterol falls into category C. There are no good studies that have been done in humans with levalbuterol. But in animal studies, pregnant animals were given this medication, and the babies did not show any medical issues related to this medication.

Lactation

Levalbuterol is the R-enantiomer of the beta-2 adrenergic agonist, albuterol. Although no published data exist on the use of levalbuterol by mouth or inhaler during lactation, data from the related drug, terbutaline, indicate that very little is expected to be excreted into breastmilk.

References

  1. https://pubchem.ncbi.nlm.nih.gov

Levosalbutamol/Levalbuterol

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