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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

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

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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

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 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 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

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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.