The long-acting beta-adrenergic agonists are very effective in the management of asthma . Most often, beta-adreneigic agonists are inhaled using metered-dose inhalers (handheld cartridges containing gas under pressure}. The pressure pumps the drug into a fine spray containing a measured dose of drug. Inhalation deposits the drug directly in the airways, so that it acts quickly, but the drug may not reach the airways that arc severely obstructed. For people who have difficulty using a metered-dose inhaler, spacers or holding chambers can be used. With any type of inhaler, proper technique is vital; if the device is not used properly, the drug will not reach the airways. A dry powder drug formulation is also available. The powder formulation is easier for some people to use, in part because it requires less coordination with breathing.
Beta-adrenergic agonists can also be delivered directly to the lungs by using a nebulizer. A nebulizer creates a mist of drug, and its use does not have to be coordinated with breathing. Nebulizers arc more portable than they were in the past; some units can even be plugged into a cigarette lighter in a car. Beta-adrenergic agonists can also be taken in liquid or tablet form or injected. However, the oral drugs tend to work slower than the inhaled or injected ones and are more likely to cause side effects. Side effects include abnormal heart rhythms, which may suggest excessive use. Other bronchodilators may be combined with beta-adrenergic agonists for acute attacks, including intravenous infusions of aminophylline (a type of theophylline) and nebulized ipratropium. Overusing these drugs can be very dangerous. The need for continuous use indicates severe bronchoconstriction, which can lead to respiratory failure and death.
There are currently around 26 Popular beta-adreneigic agonists molecules in the market. They are : Amibegron, Arformoterol, Bambuterol,Bitolterol, Bromoacetylalprenololmenthane, Carbuterol, Clenbuterol, Dopexamine, ormoterol, Hexoprenaline, Indacaterol,Levosalbutamol, Orciprenaline, Pirbuterol, Procaterol, Ractopamine, Reproterol, Rimiterol, Salbutamol, Salmeterol, Solabegron, Terbutaline and Tulobuterols.
Beta-adrenergic agonists can also be delivered directly to the lungs by using a nebulizer. A nebulizer creates a mist of drug, and its use does not have to be coordinated with breathing. Nebulizers arc more portable than they were in the past; some units can even be plugged into a cigarette lighter in a car. Beta-adrenergic agonists can also be taken in liquid or tablet form or injected. However, the oral drugs tend to work slower than the inhaled or injected ones and are more likely to cause side effects. Side effects include abnormal heart rhythms, which may suggest excessive use. Other bronchodilators may be combined with beta-adrenergic agonists for acute attacks, including intravenous infusions of aminophylline (a type of theophylline) and nebulized ipratropium. Overusing these drugs can be very dangerous. The need for continuous use indicates severe bronchoconstriction, which can lead to respiratory failure and death.
There are currently around 26 Popular beta-adreneigic agonists molecules in the market. They are : Amibegron, Arformoterol, Bambuterol,Bitolterol, Bromoacetylalprenololmenthane, Carbuterol, Clenbuterol, Dopexamine, ormoterol, Hexoprenaline, Indacaterol,Levosalbutamol, Orciprenaline, Pirbuterol, Procaterol, Ractopamine, Reproterol, Rimiterol, Salbutamol, Salmeterol, Solabegron, Terbutaline and Tulobuterols.
New Table of Contents
- Asthma Drug Therapy Amibegron, Arformoterol and Bambuterol
- Asthma Medications : Clenbuterol
- Asthma Drug Therapy : formoterol vs. salmeterol
- Asthma Medications: Indacaterol and xopenex
- Medicines For The Treatment Of Asthma
- Asthma Medications : metaproterenol and Maxair
- Asthma Drug Therapy : procaterol hydrochloride & Reproterol
- Salbutamol or albuterol is a short-acting beta-adrenergic receptor to treat asthma and COPD
- Salmeterol is a long-acting beta adrenergic drug that is prescribed for the treatment of asthma
- budesonide/formoterol Combination Therapy
- Advair
Asthma Drug Therapy Amibegron, Arformoterol and Bambuterol
long acting beta-adrenoceptor agonist used in the treatment of asthma
Amibegron is a drug developed by Sanofi-Aventis which acts as a selective agonist for the %u03B23 adrenergic receptor. It is the first orally active %u03B23 agonist developed that is capable of entering the Central Nervous System, and has antidepressant and anxiolytic effects.
Arformoterol, also known as arformoterol tartrate is a long acting beta-adrenoceptor agonist drug indicated for the treatment of Chronic obstructive pulmonary disease. It is sold by Sepracor, under the tradename Brovana, as a solution to be administered twice daily (morning and evening) by nebulization.
It is the active (R,R)-enantiomer of formoterol and was approved by the United States Food and Drug Administration (FDA) on October 2006 for the treatment of COPD.
Bambuterol is marketed by AstraZeneca under the trade names Bambec and Oxeol. It is a long acting beta-adrenoceptor agonist used in the treatment of asthma. Bambuterol is converted into terbutaline in the body. Terbutaline acts by stimulating beta adrenergic receptors in many parts of the body. Stimulation of beta receptors in the lungs causes relaxation of the muscles surrounding the air passages (bronchioles), allowing the airways to open.
Arformoterol, also known as arformoterol tartrate is a long acting beta-adrenoceptor agonist drug indicated for the treatment of Chronic obstructive pulmonary disease. It is sold by Sepracor, under the tradename Brovana, as a solution to be administered twice daily (morning and evening) by nebulization.
It is the active (R,R)-enantiomer of formoterol and was approved by the United States Food and Drug Administration (FDA) on October 2006 for the treatment of COPD.
Bambuterol is marketed by AstraZeneca under the trade names Bambec and Oxeol. It is a long acting beta-adrenoceptor agonist used in the treatment of asthma. Bambuterol is converted into terbutaline in the body. Terbutaline acts by stimulating beta adrenergic receptors in many parts of the body. Stimulation of beta receptors in the lungs causes relaxation of the muscles surrounding the air passages (bronchioles), allowing the airways to open.
Asthma Medications : Clenbuterol
clenbuterol dosage and side effects
Clenbuterol is a drug to releive breathing disorders and acts as a decongestant and bronchodilator. People with chronic breathing disorders like asthma use this as a bronchodilator to make breathing easier. It is most commonly available in salt form as Clenbuterol hydrochloride.
Clenbuterol is a %u03B22 adrenergic agonist similar to ephedrine, but its effects are more potent and longer-lasting as a stimulant and thermogenic drug. It causes an increase in aerobic capacity, central nervous system stimulation, and an increase in blood pressure and oxygen transportation. It increases the rate at which fat and protein is used up in the body at the same time as slowing down the storage of glycogen. It is commonly used for smooth muscle relaxant properties. This means that it is a bronchodilator and tocolytic. It is usually used in dosages anywhere from 20-60 micrograms a day when
prescribed. A dose of about 150 %u03BCg should never be exceeded in a day. It is also prescribed for treatment of horses; however, equestrian usage is usually the liquid form of clenbuterol. Clenbuterol is also a sympathomimetic in the peripheral nervous system. Clenbuterol produced for human consumption is generally in tablet form. The most common veterinarian preparation is a syrup. Clenbuterol is not approved for human use in Australia and is also banned under the Olympic Movement's WorldAnti-Doping Code Prohibited Classes of Substances and Prohibited Methods.
Clenbuterol is approved for use in some countries as a bronchodilator for asthma patients. Recently though, the drug has been publicized for its off-label use as a weight loss drug. It is commonly used as a slimming aid despite lack of sufficient clinical evidence supporting such use. With many major diet review websites talking about clenbuterol, and given its accessibility via the internet, the drug is widely used as a "dietary supplement". In fact, nowadays it is recommended by many physical trainers as the primary solution for those body builders who desire to achieve sufficiently low body fat in order to look "cut". In many cases, it is introduced into the training regime not as an illegal drug, but simply as a weight loss aid. This reduces some of the negative connotations attached to illicit drug use and thereby decreases any hesitation to take the drug on the part of the trainee.
Clenbuterol is used worldwide for the treatment of allergic respiratory disease in horses, as it is a bronchodilator. A common trade name is Ventipulmin. It can be used both orally and intravenously. It is also a non-steroidal anabolic and metabolism accelerator, through a mechanism not well understood. Its ability to induce weight loss and a greater proportion of muscle to fat makes its illegal use in livestock popular.
The common side effects of clenbuterol include Headaches, Tremors, Cramps, Restlessness, Anxiety, Insomnia, Sweating, Increased appetite, Nausea, Palpitations, Nausea and Hypertension (high blood pressure). Clenbuterol is known to cause very high blood pressure resulting in serious cardiac problems. Unsupervised use of clenbuterol could exacerbate pre-existing heart conditions or hypertension. There is a risk of overdose and stroke when used at high doses. There have been reports of sudden deaths among bodybuilders on clenbuterol, although it is unclear whether this was the result of clenbuterol or other drug combinations. There are also some very negative effects on their hearts when used long term. The hearts of rats on clenbuterol increased in size due to the infiltration of collagen fibres into the heart wall. Collagen is a tough connective tissue that can stiffen the heart muscle, actually reducing cardiac output and possibly producing cardiac arrhythmias. Also, clenbuterol Rats suffered from noticeable cardiac-cell degeneration.
Clenbuterol is a %u03B22 adrenergic agonist similar to ephedrine, but its effects are more potent and longer-lasting as a stimulant and thermogenic drug. It causes an increase in aerobic capacity, central nervous system stimulation, and an increase in blood pressure and oxygen transportation. It increases the rate at which fat and protein is used up in the body at the same time as slowing down the storage of glycogen. It is commonly used for smooth muscle relaxant properties. This means that it is a bronchodilator and tocolytic. It is usually used in dosages anywhere from 20-60 micrograms a day when
prescribed. A dose of about 150 %u03BCg should never be exceeded in a day. It is also prescribed for treatment of horses; however, equestrian usage is usually the liquid form of clenbuterol. Clenbuterol is also a sympathomimetic in the peripheral nervous system. Clenbuterol produced for human consumption is generally in tablet form. The most common veterinarian preparation is a syrup. Clenbuterol is not approved for human use in Australia and is also banned under the Olympic Movement's WorldAnti-Doping Code Prohibited Classes of Substances and Prohibited Methods.
Clenbuterol is approved for use in some countries as a bronchodilator for asthma patients. Recently though, the drug has been publicized for its off-label use as a weight loss drug. It is commonly used as a slimming aid despite lack of sufficient clinical evidence supporting such use. With many major diet review websites talking about clenbuterol, and given its accessibility via the internet, the drug is widely used as a "dietary supplement". In fact, nowadays it is recommended by many physical trainers as the primary solution for those body builders who desire to achieve sufficiently low body fat in order to look "cut". In many cases, it is introduced into the training regime not as an illegal drug, but simply as a weight loss aid. This reduces some of the negative connotations attached to illicit drug use and thereby decreases any hesitation to take the drug on the part of the trainee.
Clenbuterol is used worldwide for the treatment of allergic respiratory disease in horses, as it is a bronchodilator. A common trade name is Ventipulmin. It can be used both orally and intravenously. It is also a non-steroidal anabolic and metabolism accelerator, through a mechanism not well understood. Its ability to induce weight loss and a greater proportion of muscle to fat makes its illegal use in livestock popular.
The common side effects of clenbuterol include Headaches, Tremors, Cramps, Restlessness, Anxiety, Insomnia, Sweating, Increased appetite, Nausea, Palpitations, Nausea and Hypertension (high blood pressure). Clenbuterol is known to cause very high blood pressure resulting in serious cardiac problems. Unsupervised use of clenbuterol could exacerbate pre-existing heart conditions or hypertension. There is a risk of overdose and stroke when used at high doses. There have been reports of sudden deaths among bodybuilders on clenbuterol, although it is unclear whether this was the result of clenbuterol or other drug combinations. There are also some very negative effects on their hearts when used long term. The hearts of rats on clenbuterol increased in size due to the infiltration of collagen fibres into the heart wall. Collagen is a tough connective tissue that can stiffen the heart muscle, actually reducing cardiac output and possibly producing cardiac arrhythmias. Also, clenbuterol Rats suffered from noticeable cardiac-cell degeneration.
Asthma Drug Therapy : formoterol vs. salmeterol
Do not use formoterol if you have asthma that is quickly getting worse
Formoterol or eformoterol is a long-acting beta agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD). It is marketed in four forms: a dry-powder inhaler (DPI), metered dose inhaler (MDI), an oral tablet, and as an inhalation solution, under various trade names including Foradil/Foradile (Novartis), Oxis (AstraZeneca), Atock (Astellas) and Perforomist (Dey).
Formoterol is a long-acting %u03B22 agonist (LABA), which has an extended duration of action (up to 12 hours) compared to short-acting %u03B22 agonists such as salbutamol, which have are effective for 4-6 hours. LABAs such as formoterol are used as "symptom controllers" to supplement "preventer" corticosteroid therapy (e.g. fluticasone). A "reliever" short-acting %u03B22 agonist (e.g. salbutamol) is still required, since LABAs are not recommended for the treatment of acute asthma.
Inhaled formoterol works like other %u03B22-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. The long duration of formoterol action occurs because the formoterol molecules initially diffuse into the plasma membrane of the lung cells, and then are slowly released back outside, where they can come into contact with %u03B22 adrenergic receptors. Formoterol has been demonstrated to have a faster onset of action than salmeterol as a result of 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.
In November 2005, the American FDA released a health advisory, alerting the public to findings that show the use of long-acting %u03B22-agonists could lead to a worsening of symptoms. In a large clinical study, more patients who used an asthma medication similar to formoterol died of asthma problems than patients who did not use the medication. If you have asthma, use of formoterol may increase the chance that you will experience serious or fatal asthma problems. Your doctor will only prescribe formoterol if other medications have not controlled your asthma or if your asthma is so severe that two medications are needed to control it. Formoterol should not be the first or the only medication that you use to treat your asthma.
Do not use formoterol if you have asthma that is quickly getting worse. Tell your doctor if you have had many severe asthma attacks or if you have ever been hospitalized because of asthma symptoms. If you have any of the following signs of worsening asthma, call your doctor immediately:
Currently available long-acting beta 2 agonists include salmeterol, formoterol, bambuterol, and sustained-release oral salbutamol. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread - combination preparations include fluticasone/salmeterol and budesonide/ formoterol.
Formoterol is a long-acting %u03B22 agonist (LABA), which has an extended duration of action (up to 12 hours) compared to short-acting %u03B22 agonists such as salbutamol, which have are effective for 4-6 hours. LABAs such as formoterol are used as "symptom controllers" to supplement "preventer" corticosteroid therapy (e.g. fluticasone). A "reliever" short-acting %u03B22 agonist (e.g. salbutamol) is still required, since LABAs are not recommended for the treatment of acute asthma.
Inhaled formoterol works like other %u03B22-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. The long duration of formoterol action occurs because the formoterol molecules initially diffuse into the plasma membrane of the lung cells, and then are slowly released back outside, where they can come into contact with %u03B22 adrenergic receptors. Formoterol has been demonstrated to have a faster onset of action than salmeterol as a result of 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.
In November 2005, the American FDA released a health advisory, alerting the public to findings that show the use of long-acting %u03B22-agonists could lead to a worsening of symptoms. In a large clinical study, more patients who used an asthma medication similar to formoterol died of asthma problems than patients who did not use the medication. If you have asthma, use of formoterol may increase the chance that you will experience serious or fatal asthma problems. Your doctor will only prescribe formoterol if other medications have not controlled your asthma or if your asthma is so severe that two medications are needed to control it. Formoterol should not be the first or the only medication that you use to treat your asthma.
Do not use formoterol if you have asthma that is quickly getting worse. Tell your doctor if you have had many severe asthma attacks or if you have ever been hospitalized because of asthma symptoms. If you have any of the following signs of worsening asthma, call your doctor immediately:
Currently available long-acting beta 2 agonists include salmeterol, formoterol, bambuterol, and sustained-release oral salbutamol. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread - combination preparations include fluticasone/salmeterol and budesonide/ formoterol.
Asthma Medications: Indacaterol and xopenex
xopenex as a bronchodilator is used to treat asthma and COPD
Indacaterol is an ultra long acting beta-adrenoceptor agonist currently undergoing research. It needs only be taken once a day, unlike the currently available Formoterol and Salmeterol. Such drugs are used in the treatment of chronic obstructive pulmonary disease and asthma.
Indacaterol by Novartis is an effective and well-tolerated treatment of asthma and chronic obstructive pulmonary disease (COPD) over 24 hours with a rapid onset of action. The combination of 24-hour efficacy and a reassuring safety profile suggests that in time, a once-daily dose of indacaterol could become a new standard of care for bronchodilation in asthma and COPD. Indacaterol could be the first beta2-agonist to be taken only once-daily providing full 24 hour symptom control with a single administration, in contrast to currently-available long-acting beta2-agonists (LABAs) such as salmeterol and formoterol which have to be taken twice-daily.
Xopenex as a bronchodilator is used to treat asthma and COPD. In general, xopenex has similar pharmacokinetic and pharmacodynamic properties to albuterol; however, its manufacturer, Sepracor, has implied (although not directly claimed) that the presence of only the R-enantiomer produces fewer side effects.
Physicians sometimes elect to use xopenex in patients with a history of supraventricular tachycardia or other arrhythmias because it is thought that xopenex may produce less direct effects on beta 2 adrenergic receptors in the heart. For similar reasons, some pediatricians also use xopenex for patients who experience hyperactivity or jitteriness from racemic albuterol.
The use of xopenex over the more traditionally used racemic albuterol is controversial among health care professionals. That using xopenex instead of albuterol produces less direct effect on beta 2-adrenergic receptors and/or fewer cardiac side effects has been suggested, but not consistently demonstrated by long term, well-designed clinical trials.
There are differing opinions on whether there is sufficient therapeutic benefit to using xopenex that outweighs the 5-10 times higher price tag. In general, it appears that if a clinician and patient feel that a low dose of racemic mixture is causing undesirable side effects, xopenex may be a viable alternative. xopenex was originally available only as a solution for nebulizer and eventually become available as a CFC-free metered dose inhaler under the trade name Xopenex HFA (xopenex tartrate) Inhalation Aerosol.
Indacaterol by Novartis is an effective and well-tolerated treatment of asthma and chronic obstructive pulmonary disease (COPD) over 24 hours with a rapid onset of action. The combination of 24-hour efficacy and a reassuring safety profile suggests that in time, a once-daily dose of indacaterol could become a new standard of care for bronchodilation in asthma and COPD. Indacaterol could be the first beta2-agonist to be taken only once-daily providing full 24 hour symptom control with a single administration, in contrast to currently-available long-acting beta2-agonists (LABAs) such as salmeterol and formoterol which have to be taken twice-daily.
Xopenex as a bronchodilator is used to treat asthma and COPD. In general, xopenex has similar pharmacokinetic and pharmacodynamic properties to albuterol; however, its manufacturer, Sepracor, has implied (although not directly claimed) that the presence of only the R-enantiomer produces fewer side effects.
Physicians sometimes elect to use xopenex in patients with a history of supraventricular tachycardia or other arrhythmias because it is thought that xopenex may produce less direct effects on beta 2 adrenergic receptors in the heart. For similar reasons, some pediatricians also use xopenex for patients who experience hyperactivity or jitteriness from racemic albuterol.
The use of xopenex over the more traditionally used racemic albuterol is controversial among health care professionals. That using xopenex instead of albuterol produces less direct effect on beta 2-adrenergic receptors and/or fewer cardiac side effects has been suggested, but not consistently demonstrated by long term, well-designed clinical trials.
There are differing opinions on whether there is sufficient therapeutic benefit to using xopenex that outweighs the 5-10 times higher price tag. In general, it appears that if a clinician and patient feel that a low dose of racemic mixture is causing undesirable side effects, xopenex may be a viable alternative. xopenex was originally available only as a solution for nebulizer and eventually become available as a CFC-free metered dose inhaler under the trade name Xopenex HFA (xopenex tartrate) Inhalation Aerosol.
Medicines For The Treatment Of Asthma
New Treatment Of Asthma
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Asthma Medications : metaproterenol and Maxair
Maxair is an adrenergic bronchodilator used in the treatment of asthma
Orciprenaline also known as metaproterenol is a bronchodilator used in the treatment of asthma. Orciprenaline is a moderately selective beta 2-adrenergic receptor agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle, with minimal or no effect on alpha-adrenergic receptors. The pharmacologic effects of beta adrenergic agonist drugs, such as orciprenaline, are at least in part attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of ATP to cAMP. Increased cAMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from many cells, especially from mast cells.
Pirbuterol commercially available as Maxair is a beta-2 adrenergic bronchodilator used in the treatment of asthma, available (as perbuterol acetate) as a breath-activated metered-dose inhaler. MAXAIR AUTOHALER is a pressurized metered-dose aerosol unit for oral inhalation. It provides a fine-particle suspension of maxair acetate in the propellant mixture of trichioro-monofluoromethane and dichlorodifluoromethane, with sorbitan trioleate. Each actuation delivers 253 mcg of maxair (as maxair acetate) from the valve and 200 mcg of maxair (as maxair acetate) from the mouthpiece. The unit is breath-actuated such that the medication is delivered automatically during inspiration without the need for the patient to coordinate actuation with inspiration
maxair is used to treat wheezing and shortness of breath that commonly occur with lung problems (e.g., asthma, chronic obstructive pulmonary disease-COPD). Controlling these symptoms can decrease time lost from work or school. maxair is a bronchodilator (beta-2 receptor agonist) that works by opening breathing passages to make breathing easier. This medicine comes in an inhaler that automatically releases a puff of medicine when you inhale. The inhaler allows the drug to reach deep into the lungs for the most benefit. Because this type of inhaler is used differently than other types, be sure to follow directions closely.
Pirbuterol commercially available as Maxair is a beta-2 adrenergic bronchodilator used in the treatment of asthma, available (as perbuterol acetate) as a breath-activated metered-dose inhaler. MAXAIR AUTOHALER is a pressurized metered-dose aerosol unit for oral inhalation. It provides a fine-particle suspension of maxair acetate in the propellant mixture of trichioro-monofluoromethane and dichlorodifluoromethane, with sorbitan trioleate. Each actuation delivers 253 mcg of maxair (as maxair acetate) from the valve and 200 mcg of maxair (as maxair acetate) from the mouthpiece. The unit is breath-actuated such that the medication is delivered automatically during inspiration without the need for the patient to coordinate actuation with inspiration
maxair is used to treat wheezing and shortness of breath that commonly occur with lung problems (e.g., asthma, chronic obstructive pulmonary disease-COPD). Controlling these symptoms can decrease time lost from work or school. maxair is a bronchodilator (beta-2 receptor agonist) that works by opening breathing passages to make breathing easier. This medicine comes in an inhaler that automatically releases a puff of medicine when you inhale. The inhaler allows the drug to reach deep into the lungs for the most benefit. Because this type of inhaler is used differently than other types, be sure to follow directions closely.
Asthma Drug Therapy : procaterol hydrochloride & Reproterol
Reproterol is an adrenergic agonist used in the treatment of asthma
Procaterol, also known as procaterol hydrochloride (USAN), is a short-acting beta adrenergic receptor agonist used for the treatment of asthma. Procaterol has not been filed for FDA evaluation in the United States. So it is not available in the USA. Procaterol was developed in Japan and has been approved there for the treatment of asthma.
Reproterol (INN) is a %u03B22-adrenergic receptor agonist used in the treatment of asthma. In a number of countries reproterol has been used for many years as a bronchodilator in the treatment of asthma. Its mode of action has been attributed to a more or less selective stimulation of 2-receptors. Reproterol has gained wide use when it was licensed as a fixed combination therapy with cromoglycate. Until today, the bronchodilator effects of reproterol and the bronchoprotective and anti-inflammatory actions of cromoglycate combined in one inhaler remain the only successful fixed combination of a disease-modifying and symptomatic drug for the treatment of asthma.
Reproterol (INN) is a %u03B22-adrenergic receptor agonist used in the treatment of asthma. In a number of countries reproterol has been used for many years as a bronchodilator in the treatment of asthma. Its mode of action has been attributed to a more or less selective stimulation of 2-receptors. Reproterol has gained wide use when it was licensed as a fixed combination therapy with cromoglycate. Until today, the bronchodilator effects of reproterol and the bronchoprotective and anti-inflammatory actions of cromoglycate combined in one inhaler remain the only successful fixed combination of a disease-modifying and symptomatic drug for the treatment of asthma.
Salbutamol or albuterol is a short-acting beta-adrenergic receptor to treat asthma and COPD
Salbutamol is specifically indicated in the following conditions: acute asthma
Salbutamol or albuterol is a short-acting beta-adrenergic receptor agonist used to treat bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease.
Salbutamol sulfate is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is done by a metered dose inhaler (MDI), nebuliser or other delivery devices. In these forms of delivery, the Salbutamol can start effecting within five to twenty minutes of dosing, though some immediate rekeif too is seen. Salbutamol can also be given orally as an inhalant or intravenously. However, some asthma patients do not have the required DNA base sequence in a specific gene and may not respond to these medications. Salbutamol became available in the United Kingdom in 1969 and in the United States in 1980 under the trade name Ventolin.
Salbutamol is specifically indicated in the following conditions:
Acute asthma: Symptomatic relief during maintenance therapy of asthma and other conditions with reversible airways obstruction (including COPD) and Protection against exercise-induced asthma. Salbutamol Can induce Hypokalaemia, especially in patients with renal failure. As a ß2-agonist, salbutamol also finds use in obstetrics. Intravenous salbutamol can be used to relax the uterine smooth muscle to delay premature labour.
Side Effects of Salbutamol include: Tachycardia, Tremors, Shakiness, nervousness, Hyperkinesis, Headache, Insomnia, Nausea, Vomiting and Reactive bronchospasm. The U.S. Food & Drug Administration in April of 2005 mandated that all (including albuterol) inhalers containing chlorofluorocarbons (CFCs) will be prohibited in the United States as of 12/31/2008. CFC inhalers had previously been given "essential use" status, exempting it from a CFC-production ban, however in accordance with the Montreal Protocol they will be phased out; in many other countries patients have been transitioned to non-CFC based inhalers using hydrofluoroalkane (HFA) propellant. Pharmaceutical manufacturers are expected to produce adequate supplies of alternative (HFA) inhalers by 2009.[citation needed]
One drawback of this transition to HFA inhalers is that due to patent restrictions all of the HFA albuterol inhalers are "brand-name" (ProAir, Proventil, and Ventolin). They cost approximately $20 more per inhaler than existing generic CFC albuterol inhalers. Three of the four available albuterol/ levalbuterol HFA inhalers on the market also contain 10-14% ethanol by weight. Ventolin HFA is the exception.
Salbutamol sulfate is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is done by a metered dose inhaler (MDI), nebuliser or other delivery devices. In these forms of delivery, the Salbutamol can start effecting within five to twenty minutes of dosing, though some immediate rekeif too is seen. Salbutamol can also be given orally as an inhalant or intravenously. However, some asthma patients do not have the required DNA base sequence in a specific gene and may not respond to these medications. Salbutamol became available in the United Kingdom in 1969 and in the United States in 1980 under the trade name Ventolin.
Salbutamol is specifically indicated in the following conditions:
Acute asthma: Symptomatic relief during maintenance therapy of asthma and other conditions with reversible airways obstruction (including COPD) and Protection against exercise-induced asthma. Salbutamol Can induce Hypokalaemia, especially in patients with renal failure. As a ß2-agonist, salbutamol also finds use in obstetrics. Intravenous salbutamol can be used to relax the uterine smooth muscle to delay premature labour.
Side Effects of Salbutamol include: Tachycardia, Tremors, Shakiness, nervousness, Hyperkinesis, Headache, Insomnia, Nausea, Vomiting and Reactive bronchospasm. The U.S. Food & Drug Administration in April of 2005 mandated that all (including albuterol) inhalers containing chlorofluorocarbons (CFCs) will be prohibited in the United States as of 12/31/2008. CFC inhalers had previously been given "essential use" status, exempting it from a CFC-production ban, however in accordance with the Montreal Protocol they will be phased out; in many other countries patients have been transitioned to non-CFC based inhalers using hydrofluoroalkane (HFA) propellant. Pharmaceutical manufacturers are expected to produce adequate supplies of alternative (HFA) inhalers by 2009.[citation needed]
One drawback of this transition to HFA inhalers is that due to patent restrictions all of the HFA albuterol inhalers are "brand-name" (ProAir, Proventil, and Ventolin). They cost approximately $20 more per inhaler than existing generic CFC albuterol inhalers. Three of the four available albuterol/ levalbuterol HFA inhalers on the market also contain 10-14% ethanol by weight. Ventolin HFA is the exception.
www.healasthma.com
Generic HFA albuterol inhalers are not expected on the market until 2017 due to existing patents, although some pharmaceutical companies will offer discounts for those who cannot afford the HFA inhalers. Another drawback that is coming to light now as the use of HFA/HFA+ethanol inhalers is expanding seems to be a far higher intolerance of the new inhalers compared to CFC propellant in patients. Registered complaints run the gamut from "doesn't seem to work as well" all the way to serious anaphylaxis in response to using an HFA or HFA+ ethanol inhaler.
Albuterol is widely used, and accounts for anywhere from 80% of all bronchodilator prescriptions in 2006 to 88% in 2008. However, patients in the United States who cannot tolerate the HFA albuterol inhalers will not have a single albuterol alternative available to them domestically after December 31, 2008. The FDA did not approve any alternatives to HFA and there are few standard inhaled lung medications in the United States that come in Dry Powder Inhaler (DPI) versions. Noticibly missing is albuterol in DPI form in the United States, although it is available in most of the rest of the world in salbutamol DPIs.
The benefits of transitioning to HFA inhalers include increased drug deposition in the distal airways, more consistent drug delivery from nearly empty canisters, and more consistent drug delivery at a greater range of canister temperatures. It should be noted that the spray force of HFA inhalers is less than that of CFC inhalers, which may mislead some patients to believe that they may not be receiving enough albuterol when in fact they are seeing the benefits as outlined above.
Salmeterol is a long-acting beta adrenergic drug that is prescribed for the treatment of asthma
inhaled salmeterol decreases the number and severity of asthma attacks
Salmeterol is a long-acting beta adrenergic receptor agonist drug that is prescribed for the treatment of asthma and chronic obstructive pulmonary disease (COPD). It is currently available as a metered-dose inhaler in powdered form of the drug.
Salmeterol is a long acting beta-adrenoceptor agonist (LABA), usually prescribed for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed together with a corticosteroid, such as beclomethasone. The primary noticeable difference of salmeterol to salbutamol is that the duration of action lasts approximately 12 hours in comparison with 6 hours of salbutamol.
When used regularly every day as prescribed, 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 bronchodialation by relaxing the smooth muscle in the airway so as to treat the aggaravating asthma conditions. The long duration of formoterol action occurs by the formoterol molecules initially diffusing into the plasma membrane of the lung cells, and then slowly being released back outside the cell where they can come into contact with the beta 2 adrenoceptors. 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 than a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol.
Currently available long-acting beta 2 adrenoceptor agonists include salmeterol, formoterol, bambuterol, and sustained-release oral albuterol. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread; the most common combination currently in use is fluticasone/salmeterol available as Advair in the United States and Seretide in the UK.
Serevent (salmeterol) is marketed and manufactured by GlaxoSmithKline and was released as Serevent in 1990. However, the product is under license from Allen & Hanburys.(UK). In November of 2005, the American FDA released a health advisory, alerting the public to findings that show the use of Long-acting ßeta-agonists could lead to a worsening of symptoms, and in some cases death.
Whilst the use of inhaled LABAs are still recommended in asthma guidelines for the resulting improved symptom control, further concerns have been raised, by a large meta-analysis of the pooled results from 20 trials with 34,826 participants, that salmeterol may increase the small risks of asthma deaths and this additional risk is not reduced with the additional use of inhaled steroids. This seems to occur because although LABAs relieve asthma symptoms, they also promote bronchial inflammation and sensitivity without warning.
Salmeterol is a long acting beta-adrenoceptor agonist (LABA), usually prescribed for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed together with a corticosteroid, such as beclomethasone. The primary noticeable difference of salmeterol to salbutamol is that the duration of action lasts approximately 12 hours in comparison with 6 hours of salbutamol.
When used regularly every day as prescribed, 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 bronchodialation by relaxing the smooth muscle in the airway so as to treat the aggaravating asthma conditions. The long duration of formoterol action occurs by the formoterol molecules initially diffusing into the plasma membrane of the lung cells, and then slowly being released back outside the cell where they can come into contact with the beta 2 adrenoceptors. 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 than a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol.
Currently available long-acting beta 2 adrenoceptor agonists include salmeterol, formoterol, bambuterol, and sustained-release oral albuterol. Combinations of inhaled steroids and long-acting bronchodilators are becoming more widespread; the most common combination currently in use is fluticasone/salmeterol available as Advair in the United States and Seretide in the UK.
Serevent (salmeterol) is marketed and manufactured by GlaxoSmithKline and was released as Serevent in 1990. However, the product is under license from Allen & Hanburys.(UK). In November of 2005, the American FDA released a health advisory, alerting the public to findings that show the use of Long-acting ßeta-agonists could lead to a worsening of symptoms, and in some cases death.
Whilst the use of inhaled LABAs are still recommended in asthma guidelines for the resulting improved symptom control, further concerns have been raised, by a large meta-analysis of the pooled results from 20 trials with 34,826 participants, that salmeterol may increase the small risks of asthma deaths and this additional risk is not reduced with the additional use of inhaled steroids. This seems to occur because although LABAs relieve asthma symptoms, they also promote bronchial inflammation and sensitivity without warning.
budesonide/formoterol Combination Therapy
fluticasone/salmeterol Combination Therapy in Adults With Asthma
A new open-label study evaluated patient satisfaction with budesonide/formoterol combination therapy and fluticasone/salmeterol combination therapy, as measured by the Asthma Treatment Satisfaction Measure (ATSM)(1). Patients participating in the study were ages 18 years and older with moderate to severe asthma(1) and had been previously treated with inhaled corticosteroids(1). Results were presented today at the International Conference of the American Thoracic Society
Advair
advair inhaler
The combination preparation fluticasone/salmeterol is a formulation containing fluticasone propionate and salmeterol xinafoate used in the management of asthma and chronic obstructive pulmonary disease (COPD). It is marketed by GlaxoSmithKline under various trade names including Advair (US, CA), Seretide (EU, Australia), Viani (Germany), Adoair (Japan), and ForAir (India). Annual sales approx $3.8B. Patent expires 2010.
Fluticasone, a corticosteroid, is the anti-inflammatory component of the combination, while salmeterol treats constriction of the airways. Together, they relieve the symptoms of coughing, wheezing and shortness of breath better than either fluticasone or salmeterol taken on its own.
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