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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
- Overactive thyroid gland
- Diabetes
- Ketoacidosis
- Excess Body Acid
- Low amount of potassium in the blood
- High blood pressure
- Diminished blood flow through arteries of the Heart
- Prolonged QT interval on EKG
- Abnormal heart rhythm
- Abnormal EKG with QT changes from Birth
- Kidney disease with the reduction in kidney function
- Seizures
- Paradoxical bronchospasm
- Allergies to Beta-Adrenergic Agents
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
Side Effects of Levosalbutamol/Levalbuterol
The most common
- Fast heartbeat
- Chest pain or tightness
- dry mouth
- trembling or shaking of the hands or feet
- stomach pain or cramping
- diarrhea
- a headache
- dizziness
- confusion
- stomach pain;
- back pain, joint or muscle pain.
- problems with your vision (including color vision);
- sudden chest pain or trouble breathing;
- pain or swelling in one or both legs;
- a pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine headache;
- pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
- feeling like you might pass out.
More common
- Abdominal or stomach pain, discomfort, or pain when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।" data-rx-term="tenderness" data-rx-definition="Tenderness means pain when an area is touched or pressed. সহজ বাংলা: চাপ দিলে ব্যথা।">tenderness
- chills or fever
- difficulty with moving
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- nervousness
Drug Interactions of Levosalbutamol/Levalbuterol
Levosalbutamol may interact with the following drugs, supplements & may change the efficacy of drugs
- antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- beta 2 agonists (e.g., salbutamol, formoterol, terbutaline)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- long-acting beta agonists (e.g., indacaterol, salmeterol)
- citalopram
- decongestant cold medications (e.g., phenylephrine, pseudoephedrine)
- decongestant eye drops and nose sprays (e.g., naphazoline, oxymetazoline, xylometazoline)
- diuretics (e.g., furosemide, hydrochlorothiazide)
- domperidone
- escitalopram
- ipratropium
- macrolide antibiotics (e.g., clarithromycin, erythromycin, telithromycin)
- methadone
- mirabegron
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
- narcotics (e.g., codeine, morphine, oxycodone)
- quinolone antibiotics (e.g., levofloxacin moxifloxacin ofloxacin)
- serotonin antagonists (anti-emetic medications; e.g., ondansetron granisetron, )
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
- tolterodine
- topiramate
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- aminophylline
- theophylline
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
