Astmerole - General Information
Astmerole is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD.
Pharmacology of Astmerole
Astmerole is a long acting beta2-adrenoceptor agonist (LABA), usually only prescribed for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed concurrently with a corticosteroid, such as beclometasone. The primary noticable difference of salmeterol to salbutamol is that the duration of action lasts approximately 12 hours in comparison with 4-6 hours of salbutamol. When used regularly every day as presecribed, inhaled salmeterol decreases the number and severity of asthma attacks. However, it is not for use for relieving an asthma attack that has already started. Inhaled salmeterol works like other beta 2-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. Astmerole is similar in action to formoterol, however formoterol has been demonstrated to have a faster onset of action than salmeterol as a result of a lower lipophilicity, and has also been demonstrated to be more potent - a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol.
Astmerole for patients
Patients should be instructed to read the accompanying Medication Guide with each new prescription and refill.
Patients being treated with SEREVENT DISKUS should receive the following information and instructions. This information is intended to aid them in the safe and effective use of this medication. It is not a disclosure of all possible adverse or intended effects.
It is important that patients understand how to use the DISKUS appropriately and how to use SEREVENT DISKUS in relation to other asthma or COPD medications they are taking. Patients should be given the following information:
1. Patients should be informed that salmeterol may increase the risk of asthma-related death.
2. SEREVENT DISKUS is not meant to relieve acute asthma or COPD symptoms and extra doses should not be used for that purpose. Acute symptoms should be treated with an inhaled, short-acting bronchodilator (the physician should provide the patient with such medication and instruct the patient in how it should be used).
3. The physician should be notified immediately if any of the following signs of seriously worsening asthma or COPD occur:
· Decreasing effectiveness of inhaled, short-acting beta2-agonists
· Need for more inhalations than usual of inhaled, short-acting beta2-agonists
· Significant decrease in PEF or lung function as outlined by the physician
· Use of 4 or more inhalations per day of a short-acting beta2-agonist for 2 or more days consecutively
· Use of more than 1 canister (200 inhalations per canister) of an inhaled, short-acting beta2-agonist in an 8-week period.
4. Patients should not stop therapy with SEREVENT DISKUS for asthma or COPD without physician/provider guidance since symptoms may worsen after discontinuation.
5. SEREVENT DISKUS should not be used as a substitute for oral or inhaled corticosteroids. The dosage of these medications should not be changed and they should not be stopped without consulting the physician, even if the patient feels better after initiating treatment with SEREVENT DISKUS.
6. Patients should be cautioned regarding adverse effects associated with beta2-agonists, such as palpitations, chest pain, rapid heart rate, tremor, or nervousness.
7. When patients are prescribed SEREVENT DISKUS, other medications for asthma and COPD should be used only as directed by the physician.
8. SEREVENT DISKUS should not be used with a spacer device.
9. Patients who are pregnant or nursing should contact the physician about the use of SEREVENT DISKUS.
10. The action of SEREVENT DISKUS may last up to 12 hours or longer. The recommended dosage (1 inhalation twice daily, morning and evening) should not be exceeded.
11. When used for the treatment of EIB, 1 inhalation of SEREVENT DISKUS should be taken 30 minutes before exercise.
· Additional doses of SEREVENT should not be used for 12 hours.
· Patients who are receiving SEREVENT DISKUS twice daily should not use additional SEREVENT for prevention of EIB.
12. Effective and safe use of SEREVENT DISKUS includes an understanding of the way that it should be used:
Never exhale into the DISKUS.
· Never attempt to take the DISKUS apart.
· Always activate and use the DISKUS in a level, horizontal position.
· Never wash the mouthpiece or any part of the DISKUS. KEEP IT DRY.
· Always keep the DISKUS in a dry place.
· Discard 6 weeks after removal from the moisture-protective foil overwrap pouch or after all blisters have been used (when the dose indicator reads "0"), whichever comes first.
13. For the proper use of SEREVENT DISKUS and to attain maximum benefit, the patient should read and follow carefully the Instructions for Using SEREVENT DISKUS in the Medication Guide accompanying the product.
14. Most patients are able to taste or feel a dose delivered from SEREVENT DISKUS. However, whether or not patients are able to sense delivery of a dose, they should not exceed the recommended dose of 1 inhalation twice daily, morning and evening. Patients should contact a physician or pharmacist if they have questions.
Short-Acting Beta2-Agonists:In two 12-week, repetitive-dose adolescent and adult clinical trials in patients with asthma (N = 149), the mean daily need for additional beta2-agonist in patients using SEREVENT DISKUS was approximately 1½ inhalations/day. Twenty-six percent (26%) of the patients in these trials used between 8 and 24 inhalations of short-acting beta-agonist per day on 1 or more occasions. Nine percent (9%) of the patients in these trials averaged over 4 inhalations/day over the course of the 12-week trials. No increase in frequency of cardiovascular events was observed among the 3 patients who averaged 8 to 11 inhalations/day; however, the safety of concomitant use of more than 8 inhalations/day of short-acting beta2-agonist with SEREVENT DISKUS has not been established. In 29 patients who experienced worsening of asthma while receiving SEREVENT DISKUS during these trials, albuterol therapy administered via either nebulizer or inhalation aerosol (1 dose in most cases) led to improvement in FEV1 and no increase in occurrence of cardiovascular adverse events.
In 2 clinical trials in patients with COPD, the mean daily need for additional beta2-agonist for patients using SEREVENT DISKUS was approximately 4 inhalations/day. Twenty-four percent (24%) of the patients using SEREVENT DISKUS in these trials averaged 6 or more inhalations of albuterol per day over the course of the 24-week trials. No increase in frequency of cardiovascular events was observed among patients who averaged 6 or more inhalations per day.
Monoamine Oxidase Inhibitors and Tricyclic Antidepressants: Salmeterol 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 salmeterol on the vascular system may be potentiated by these agents.
Corticosteroids and Cromoglycate: In clinical trials, inhaled corticosteroids and/or inhaled cromolyn sodium did not alter the safety profile of salmeterol when administered concurrently.
Methylxanthines: The concurrent use of intravenously or orally administered methylxanthines (e.g., aminophylline, theophylline) by patients receiving salmeterol has not been completely evaluated. In 1 clinical asthma trial, 87 patients receiving SEREVENT Inhalation Aerosol 42 mcg twice daily concurrently with a theophylline product had adverse event rates similar to those in 71 patients receiving SEREVENT Inhalation Aerosol without theophylline. Resting heart rates were slightly higher in the patients on theophylline but were little affected by therapy with SEREVENT Inhalation Aerosol.
In 2 clinical trials in patients with COPD, 39 subjects receiving SEREVENT DISKUS concurrently with a theophylline product had adverse event rates similar to those in 302 patients receiving SEREVENT DISKUS without theophylline. Based on the available data, the concomitant administration of methylxanthines with SEREVENT DISKUS did not alter the observed adverse event profile.
Beta-Adrenergic Receptor Blocking Agents: Beta-blockers not only block the pulmonary effect of beta-agonists, such as SEREVENT DISKUS, but may also produce severe bronchospasm in patients with asthma or COPD. Therefore, patients with asthma or COPD 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 or COPD. 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.
SEREVENT DISKUS is contraindicated in patients with a history of hypersensitivity to salmeterol or any other component of the drug product.
Additional information about Astmerole
Astmerole Indication: For the treatment of asthma and chronic obstructive pulmonary disease (COPD).
Mechanism Of Action: Astmerole's long, lipophilic side chain binds to exosites near beta(2)-receptors in the lungs and on bronchiolar smooth muscle, allowing the active portion of the molecule to remain at the receptor site, continually binding and releasing. Beta(2)-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and increased bronchial airflow.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Salmeterol
Synonyms: Salmeterolum [Latin]
Drug Category: Bronchodilator Agents; Sympathomimetic; Adrenergic beta-Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Salmeterol: Aeromax; Arial; Astmerole; Fujimycin; Salmetedur; Serevent;
Absorption: Because of the small therapeutic dose, systemic levels of salmeterol are low or undetectable after inhalation of recommended doses.
Toxicity (Overdose): Symptoms of overdose include angina (chest pain), dizziness, dry mouth, fatigue, flu-like symptoms, headache, heart irregularities, high or low blood pressure, high blood sugar, insomnia, muscle cramps, nausea, nervousness, rapid heartbeat, seizures, and tremor. By the oral route, no deaths occurred in rats at 1,000 mg/kg (approximately 81,000 times the maximum recommended daily inhalation dose in adults and approximately 38,000 times the maximum recommended daily inhalation dose in children on a mg/m2 basis).
Protein Binding: 96%
Biotransformation: Hepatic, metabolized by hydroxylation via CYP3A4
Half Life: 5.5 hours
Dosage Forms of Astmerole: Powder Respiratory (inhalation)
Powder Respiratory (inhalation)
Chemical IUPAC Name: 2-(hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenol
Chemical Formula: C25H37NO4
Salmeterol on Wikipedia: http://en.wikipedia.org/wiki/Salmeterol
Organisms Affected: Humans and other mammals