Product Name: Levalbuterol
Common Brand Names: Xopenex
Pharmaceutical Category: Anti-Allergic / Asthma
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There is an additional general information about this medication active ingredient albuterol (salbutamol):
Levalbuterol is a beta adrenoagonists with a predominant effect on beta2-adrenergic receptors (localized, particularly in the bronchi, myometrium, blood vessels).
This medication prevents and reduces or eliminates bronchospasm, reduces the resistance in the airways, increases the vital capacity. It prevents the release of histamine, slow reacting substance from mast cells and factors chemotaxis of neutrophils. Compared with other drugs of this group has a less pronounced positive chrono-and inotropic effect on myocardium. It widen of coronary arteries, practically does not reduce blood pressure. Has tocolytic effect, lowering the tone and the contractile activity of the myometrium.
When using an aerosol there is a rapid absorption of albuterol (salbutamol) in the blood, but its concentration in plasma when used in recommended doses are very low or below detection limit.
After oral administration Levalbuterol is well absorbed from the gastrointestinal tract. Plasma protein binding is 10%. Metabolised with "first pass" through the liver and possibly in the wall of the intestine, the main metabolite - inactive sulfate conjugate. salbutamol is not metabolised in the lungs, thus its ultimate metabolism and excretion following inhalation depends on the method of application, which defines the relationship between inhaled salbutamol and unintentionally swallowed.
T1/2 from plasma is 2-7 hours. albuterol (salbutamol) is rapidly excreted in the urine as metabolites and unchanged substance, in small amounts excreted in the feces.
Why is Levalbuterol prescribed?
The prevention and relief of bronchospasm in all forms of bronchial asthma. Reversible airway obstruction in chronic bronchitis and emphysema, bronchial obstruction in children.
Threatening preterm labor with uterine contractions; birth to 37-38 weeks of pregnancy; isthmic-cervical insufficiency, decrease in fetal heart rate, depending on uterine contractions during opening of the cervix and expulsion. As a preventive measure during surgery on the pregnant uterus (the imposition of a circular suture with the lack of internal os of the uterus).
Dosage and administration
Levalbuterol for oral use as a means of extending the broncho adults and children over 12 years - 2.4 mg 3-4 times / day; if necessary, the dose may be increased to 8 mg 4 times / day. Children aged 6-12 years - 2 mg 3-4 times / day; children 2-6 years - 1-2 mg 3 times / day.
Levalbuterol for inhalation use dose depends on the applied dosage form, frequency of use depends on the testimony and the clinical situation.
As a tocolytic agent used as IV infusion in dose of 1-2 mg.
Levalbuterol side effects
Cardiovascular system: a transient expansion of peripheral blood vessels, a moderate tachycardia.
Central nervous system: headache, dizziness, nausea, vomiting.
Allergic reactions: in a few cases - angioedema, allergic reactions in the form of skin rashes, urticaria, hypotension, collapse.
Other: Tremor of hands, inner trembling, tension, rarely - paradoxical bronchoconstriction, muscle cramps.
The threat of miscarriage in I and II trimesters of pregnancy, premature placental abruption, bleeding or toxemia in the III trimester of pregnancy, infancy to 2 years; hypersensitivity to salbutamol.
Using during pregnancy and breastfeeding
Category of the fetus by FDA - C.
Levalbuterol is contraindicated in threatened miscarriage in I and II trimesters of pregnancy, premature detachment of the placenta, bleeding, or toxicosis in the III trimester of pregnancy. If necessary, the use of salbutamol during pregnancy should be related to the expected benefits of treatment for the mother and the potential risk to the fetus. Currently is insufficient data on the safety of salbutamol in early pregnancy. salbutamol is excreted in breast milk, so if you need to use during lactation should also assess the potential benefits of treatment for the mother and the potential risk to the child.
With caution used Levalbuterol when tachyarrhythmia and other cardiac arrhythmias, arterial hypertension, myocarditis, heart defects, aortic stenosis, diabetes, thyrotoxicosis, glaucoma, acute heart failure (with careful medical supervision).
Increase doses or frequency of receiving albuterol (salbutamol) should be under the supervision of a doctor. Reducing the interval may be only in exceptional cases and should be strictly justified.
In the application of salbutamol there was a risk of hypokalemia, so the period of treatment in patients with severe asthma should monitor the flow levels of potassium in the blood. The risk of hypokalemia increases with hypoxia.
To increase the effectiveness of therapy the patient should be trained in the proper use of inhalers and the beginning of treatment to use an inhaler under the supervision of medical personnel. Receiving high doses of salbutamol in patients with acute asthma leads to the fact that each subsequent attack of breathlessness becomes more intense the previous syndrome (rebound). In severe asthma interval between inhalations should be at least 20 minutes. In the absence of the minimal effect of inhalation or the appearance of pronounced tremor, tachycardia, cardiac arrhythmias continued uncontrolled use of the inhaler is contraindicated, and should appeal to the doctor. The risk of complications increases as in the long duration of treatment, and at a sharp lifting of the drug.
Levalbuterol drug interactions
With simultaneous use of albuterol (salbutamol) with not cardioselective beta-blockers may suppress mutual therapeutic effects; with theophylline - increases the risk of tachycardia and arrhythmia, in particular, supraventricular extrasystoles.
With simultaneous use of salbutamol and xanthine derivatives, SCS or diuretics increases the risk of hypokalemia.
Levalbuterol in case of emergency / overdose
Symptoms: tachycardia (heart rate to 200 bpm), ventricular flutter, reducing blood pressure, increased cardiac output, hypoxemia, acidosis, hypokalemia, hyperglycemia, muscle tremors, headache, agitation, hallucinations, convulsions.
Treatment: removal of preparation and holding of symptomatic therapy of beta-blockers (selective) in patients with bronchial asthma requires extreme caution because of the risk of severe bronchospasm reaction.