Pharmacotherapeutic Group: Selective β2-adrenoreceptor agonists. ATC Code: R03AC02.
Pharmacology: Pharmacodynamics: The pharmacologic effects of Levolin are at least in part attributable to stimulation through β-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle. Bronchial effects of inhaled Levolin can be detected after few minutes and duration of action is normally 4-6 hrs.
Like other β2-adrenoceptor agonists also Levolin has cardiovascular effects in some patients as measured by changes in pulse rate, blood pressure, symptoms and electrocardiogram (ECG) changes. These effects can especially be detected after oral and IV administration of Levolin. In addition, Levolin has some metabolic effects. Especially IV and nebulized Levolin decreases serum potassium concentrations although the effect is generally mild and transient.
Pharmacokinetics: After administration of Levolin by the inhaled route between 10 and 25% of the dose reaches the lung. The remainder is retained in the delivery system or is deposited in the oropharynx from where it is swallowed. The fraction deposited in the airways is absorbed into the pulmonary tissues and circulation, but is not metabolised by the lung. On reaching the systemic circulation it becomes accessible to hepatic metabolism and is excreted primarily in the urine. The swallowed portion of an inhaled dose is absorbed from the gastrointestinal tract and undergoes considerable first-pass metabolism. Both unchanged drug and conjugate are excreted primarily in the urine. The elimination half-life (t½) of Levolin is 2.7-5.5 hrs after oral and inhaled administration.
Toxicology: Preclinical Safety Data: Acute toxicity of Levolin is low in the mouse, rat and dog. Lethal dosage (LD50) values in these species have exceeded several thousand fold the intended human therapeutic doses. Reported findings in repeated-dose studies eg, tachycardia, increases in heart weights and hypertrophy of muscle fibres are common to all potent selective β2-agonists and are an expression of excessive β-stimulant action. Cleft palate has been reported in mice but not in rats or rabbits after SC administration. Levolin is not mutagenic. Mesovarian leiomyomas, benign tumours of smooth muscle, occur particularly in Sprague-Dawley rats, but not in other species.
This section provides information on the proper use of a number of products that contain albuterol. It may not be specific to Levolin. Please read with care.
Use this medicine only as directed by your doctor. Do not use more of it and do not use it more often than your doctor ordered. Also, do not stop using this medicine or any asthma medicine without telling your doctor. To do so may increase the chance for breathing problems.
The albuterol inhalation solution (eg, Accuneb®) should be used with a jet nebulizer that is connected to an air compressor with good air flow. The inhalation solution and nebulizer will come with patient instructions. Read and follow these instructions carefully. Ask your doctor if you have any questions.
To use the inhalation solution in the nebulizer:
The albuterol inhalation aerosol (eg, Proair® HFA) and albuterol inhalation powder (eg, Proair® Respiclick™) is used with a special inhaler that comes with patient instructions. Read the directions carefully before using this medicine. If you or your child do not understand the directions or are not sure how to use the inhaler, ask your doctor to show you what to do. Also, ask your doctor to check you or your child on a regular basis to make sure you are using it properly.
To use the inhalation aerosol:
To use the inhalation powder:
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the canister at room temperature, away from heat and direct light. Do not freeze. Do not keep this medicine inside a car where it could be exposed to extreme heat or cold. Do not poke holes in the canister or throw it into a fire, even if the canister is empty.
Keep the medicine in the foil pouch until you are ready to use it. Store at room temperature, away from heat and direct light. Do not freeze.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Throw away Proair® Respiclick™ 13 months after opening the foil pouch, when the dose counter reaches "0", or after the expiration date, whichever comes first.
Should be taken on an empty stomach. Take 1 hr before or 2 hr after meals.
When using an aerosol there is a rapid absorption of albuterol (Levolin) in the blood, but its concentration in plasma when used in recommended doses are very low or below detection limit.
After oral administration Levolin Cyclocaps 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. Levolin 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 Levolin and unintentionally swallowed.
T1/2 from plasma is 2-7 hours. albuterol (Levolin) is rapidly excreted in the urine as metabolites and unchanged substance, in small amounts excreted in the feces.
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Information checked by Dr. Sachin Kumar, MD Pharmacology