Asthalin - General Information
A racemic mixture with a 1:1 ratio of the r-isomer, levalbuterol, and s-albuterol. It is a short-acting beta2-adrenergic agonist with its main clinical use in asthma.
Pharmacology of Asthalin
Asthalin (INN) or albuterol (USAN), a moderately selective beta(2)-receptor agonist similar in structure to terbutaline, is widely used as a bronchodilator to manage asthma and other chronic obstructive airway diseases. The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity. The R-enantiomer is sold in its pure form as Levalbuterol. The manufacturer of levalbuterol, Sepracor, has implied (although not directly claimed) that the presence of only the R-enantiomer produces fewer side-effects.
Asthalin for patients
The action of albuterol may last up to 6 hours or longer. Albuterol should not be used more frequently than recommended. Do not increase the dose or frequency of albuterol without consulting your physician. If you find that treatment with albuterol becomes less effective for symptomatic relief, your symptoms become worse, and/or you need to use the product more frequently than usual, you should seek medical attention immediately. While you are using albuterol, other inhaled drugs and asthma medications should be taken only as directed by your physician. Common adverse effects include palpitations, chest pain, rapid heart rate, and tremor or nervousness. If you are pregnant or nursing, contact your physician about use of albuterol. Effective and safe use of albuterol includes an understanding of the way that it should be administered.
Additional Information for Inhalation Aerosol: In general, the technique for administering albuterol inhalation aerosol to children is similar to that for adults, since children's smaller ventilatory exchange capacity automatically provides proportionally smaller aerosol intake. Children should use albuterol aerosol under adult supervision, as instructed by the patient's physician.
Additional Information for Inhalation Solutions: Drug compatibility (physical and chemical), efficacy, and safety of albuterol inhalation solution when mixed with other drugs in a nebulizer have not been established. 0.05% Solution Only: To avoid microbial contamination, proper aseptic techniques should be used each time the bottle is opened. Precautions should be taken to prevent contact of the dropper tip of the bottle with any surface, including the nebulizer reservoir and associated ventilatory equipment. In addition, if the solution changes color or becomes cloudy, it should not be used.
Additional Information for Capsules for Inhalation: Children should use albuterol capsules for inhalation under adult supervision, as instructed by the patient's physician.
Other short-acting sympathomimetic aerosol bronchodilators should not be used concomitantly with albuterol. If additional adrenergic drugs are to be administered by any route, they should be used with caution to avoid deleterious cardiovascular effects.
Monoamine Oxidase Inhibitors or Tricyclic Antidepressants: Albuterol should be administered with extreme caution to patients being treated with monoamine oxidase inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuation of such agents, because the action of albuterol on the vascular system may be potentiated.
Beta-Blockers: Beta-adrenergic receptor blocking agents not only block the pulmonary effect of beta-agonists, such as VENTOLIN Inhalation Aerosol, but may produce severe bronchospasm in patients with asthma. Therefore, patients with asthma should not normally be treated with beta-blockers. However, under certain circumstances, e.g., as prophylaxis after myocardial infarction, there may be no acceptable alternatives to the use of beta-adrenergic blocking agents in patients with asthma. In this setting, cardioselective beta-blockers could be considered, although they should be administered with caution.
Diuretics: The ECG changes and/or hypokalemia that may result from the administration of nonpotassium-sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded. Although the clinical significance of these effects is not known, caution is advised in the coadministration of beta-agonists with nonpotassium-sparing diuretics.
Digoxin: Mean decreases of 16% to 22% in serum digoxin levels were demonstrated after single-dose intravenous and oral administration of albuterol, respectively, to normal volunteers who had received digoxin for 10 days. The clinical significance of these findings for patients with obstructive airway disease who are receiving albuterol and digoxin on a chronic basis is unclear. Nevertheless, it would be prudent to carefully evaluate the serum digoxin levels in patients who are currently receiving digoxin and albuterol.
VENTOLIN Inhalation Aerosol is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.
Additional information about Asthalin
Asthalin Indication: For relief and prevention of bronchospasm due to asthma, emphysema, and chronic bronchitis.
Mechanism Of Action: Asthalin is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP production by activating adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered intracellular calcium concentration leads to a smooth muscle relaxation. Increased intracellular cyclic AMP concentrations also cause an inhibition of the release of mediators from mast cells in the airways.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Salbutamol
Synonyms: Albuterol; Albuterol Sulfate; Salbutamol Sulfate; Salbutamol Sulphate; Albuterol Sulphate; Levalbuterol
Drug Category: Adrenergic beta-Agonists; Tocolytic Agents; Bronchodilator Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Salbutamol: Accuneb; Aerolin; Asmaven; Broncovaleas; Cetsim; Cobutolin; Ecovent; Loftan; Proventil; Rotahaler; Salbulin; Salbutard; Salbutine; Salbuvent; Solbutamol; Sultanol; Venetlin; Ventalin Inhaler; Ventolin; Ventolin Inhaler; Ventolin Rotacaps; Volma; Volmax; Xopenex; Airomir; Asthalin; Asthavent; Asmol; Buventol; ProAir; Salamol;
Absorption: Systemic absorption is rapid following aerosol administration.
Toxicity (Overdose): LD50=1100 mg/kg (orally in mice)
Protein Binding: Not Available
Biotransformation: Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugatively metabolized to salbutamol 4'-O-sulfate.
Half Life: 1.6 hours
Dosage Forms of Asthalin: Liquid Oral
Aerosol, metered Respiratory (inhalation)
Powder Respiratory (inhalation)
Solution Respiratory (inhalation)
Chemical IUPAC Name: 4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
Chemical Formula: C13H21NO3
Salbutamol on Wikipedia: http://en.wikipedia.org/wiki/Salbutamol
Organisms Affected: Humans and other mammals