(R)-salbutamol

(R)-salbutamol Uses, Dosage, Side Effects, Food Interaction and all others data.

(R)-salbutamol Nebuliser Solution is a sterile, clear, colorless, preservative-free solution of the hydrochloride salt of (R)-salbutamol, the (R)-enantiomer of the drug substance racemic salbutamol. (R)-salbutamol Hydrochloride is a relatively selective &beta 2 adrenergic receptor agonist.

Activation of &beta 2 adrenergic receptors on airway smooth muscle leads to the activation of adenylcyclase and to an increase in the intracellular concentration of cyclic AMP. This increase in cAMP leads to the activation of protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in relaxation. (R)-salbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. (R)-salbutamol acts as a functional antagonist to relax the airway irrespective of the spasmogen involved, thus protecting against all bronchoconstrictor.

It acts by relaxing smooth muscle in the bronchial tubes to increase air flow and relieve acute shortness of breath.

Trade Name (R)-salbutamol
Generic Levosalbutamol
Levosalbutamol Other Names (R)-salbutamol, Levalbuterol, Levosalbutamol, R-salbutamol
Type
Formula C13H21NO3
Weight Average: 239.3107
Monoisotopic: 239.152143543
Protein binding

plasma protein binding is relatively low.

Groups Approved, Investigational
Therapeutic Class Short-acting selective β2-adrenoceptor stimulants
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
(R)-salbutamol
(R)-salbutamol

Uses

(R)-salbutamol tablet is used for the treatment or prevention of bronchospasm in adults, adolescents, and children 6 years of age and older with reversible obstructive airway disease.

(R)-salbutamol Nebuliser Solution or Inhaler is used for the treatment or prevention of bronchospasm in adults, adolescents, and children with reversible obstructive airway disease.

(R)-salbutamol is also used to associated treatment for these conditions: Bronchospasm

How (R)-salbutamol works

β2 adrenergic receptors on airway smooth muscle are Gs coupled and their activation by levosalbutamol leads to activation of adenylate cyclase and to an increase in the intracellular concentration of 3',5'-cyclic adenosine monophosphate (cyclic AMP). Increased cyclic AMP activates protein kinase A which itself inhibits the phosphorylation of myosin produces lower intracellular ionic calcium concentrations, inducing muscle relaxation. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways, potentially contributing to its benefit in asthma attacks.

Dosage

(R)-salbutamol dosage

(R)-salbutamol Tablet-

  • Adults and children above 12 years: 1-2 mg three times daily.
  • Children (6 -11 years): 1 mg three times daily.

Syrup-

  • Adults and children above 12 years: 5-10 ml three times daily.
  • Children (6 -11 years): 5 ml three times daily.

(R)-salbutamol Nebuliser Solution-

This Nebuliser Solutionis supplied in unit-dose ampoules and requires no dilution before administration by nebulization.

  • Children (6 months-11 years): The recommended dosage is 0.31 mg administered three times a day, by nebulization. Routine dosing should not exceed 0.63 mg three times a day.
  • Adults and Adolescents above 12 years old: The recommended starting dosage is 0.63 mg administered three to four times a day, every 6 to 8 hours, by nebulization.
  • Patients 12 years of age and older with more severe asthma or patients who do not respond adequately: 0.63 mg of (R)-salbutamol Nebuliser Solution may benefit from a dosage of 1.25 mg three times a day.

(R)-salbutamol Inhaler-

You should take your (R)-salbutamol Inhaler as needed for an asthma attack at any time of day, with or without food, by taking 1-2 puffs up to 4 times daily and no more than 8 puffs in 24 hours. If you are using your (R)-salbutamol Inhaler more than 3-4 times a week this may indicate that your asthma is not well controlled and you may need to review your medication. You can also use your (R)-salbutamol Inhaler to prevent allergy or exercise induced asthma by taking 2 puffs 15 minutes before exercise or exposure to a known allergen.

Side Effects

Potentially serious side effects like hypokalamia may result from ß-2 agonist therapy. This effect may be potentiated by hypoxia. The other likely side effects are gastrointestinal disturbances such as nausea, vomiting, burning substernal or epigastric pain and diarrhoea. In some cases nervousness, headache, dizziness, fatigue and sleeplessness may occur.

Precaution

Particular caution is advised in acute severe asthma as this effect may be potentiated by hypoxia and by concomitant treatment with xanthine derivatives, steroids and diuretics. Serum potassium levels should be monitored in such situations. Oral (R)-salbutamol should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, cardiac arrhythmias or hypertension. (R)-salbutamol can be used with caution after myocardial infarction.

(R)-salbutamol Hydrochloride, like all sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency, hypertension, and cardiac arrhythmias; in patients with convulsive disorders, hyperthyroidism, or diabetes mellitus; and in patients who are unusually responsive to sympathomimetic amines. (R)-salbutamol Nebuliser Solution or Inhaler must not be injected.

Interaction

Other short-acting sympathomimetic bronchodilators or epinephrine should be used with caution with (R)-salbutamol. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects.

Food Interaction

No interactions found.

Elimination Route

Inhalation delivers the medication directly into the airways and lungs, thereby minimizing side effects because of reduced systemic absorption of the inhaled medications.

Half Life

3.3 - 4 hours

Elimination Route

excreted into the urine.

Pregnancy & Breastfeeding use

Use in pregnancy: Use of oral (R)-salbutamol in pregnant women should be considered only if the expected benefit to the mother is greater than any possible risk to the foetus or the infant.

Use in lactation: It is not known whether (R)-salbutamol is excreted in human milk. Caution should be exercised when oral (R)-salbutamol is administered to a nursing woman.

Pregnancy: There are no adequate and well-controlled studies of (R)-salbutamol Nebuliser Solution in pregnant women. (R)-salbutamol Solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: It is not known whether (R)-salbutamol is excreted in human milk. Caution should be exercised when (R)-salbutamol Nebuliser Solution is administered to a nursing woman.

Contraindication

(R)-salbutamol Nebuliser Solution is contraindicated in patients with a history of hypersensitivity to (R)-salbutamol Hydrochloride or racemic salbutamol.

Acute Overdose

The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under side effects e.g., tachycardia, nervousness, headache, tremor, nausea, dizziness, fatigue and sleeplessness. Hypokalaemia also may occur. Treatment consists of discontinuation of oral (R)-salbutamol together with appropriate symptomatic therapy. In the event of serious poisoning, the stomach should be emptied and, if necessary, a beta-blocker administered with caution in patients with a history of bronchospasm.

Storage Condition

Store at cool and dry place. Protected from light and moisture. Keep out of the reach of children.

Innovators Monograph

You find simplified version here (R)-salbutamol

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0002448
http://classyfire.wishartlab.com/tax_nodes/C0002279
http://classyfire.wishartlab.com/tax_nodes/C0000033
http://classyfire.wishartlab.com/tax_nodes/C0000033
http://classyfire.wishartlab.com/tax_nodes/C0003899
http://classyfire.wishartlab.com/tax_nodes/C0004646
http://classyfire.wishartlab.com/tax_nodes/C0001661
http://classyfire.wishartlab.com/tax_nodes/C0001897
http://classyfire.wishartlab.com/tax_nodes/C0002228
http://classyfire.wishartlab.com/tax_nodes/C0000286
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0004150
http://classyfire.wishartlab.com/tax_nodes/C0003073
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8746
http://www.genome.jp/dbget-bin/www_bget?drug:D08124
http://www.genome.jp/dbget-bin/www_bget?cpd:C11770
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=123600
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=347829257
https://www.chemspider.com/Chemical-Structure.110192.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50361247
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=237159
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=8746
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1002
https://zinc.docking.org/substances/ZINC000000007601
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/68H
https://en.wikipedia.org/wiki/Levosalbutamol
*** Taking medicines without doctor's advice can cause long-term problems.
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