Are xanthines effective bronchodilators for COPD?
Doxofylline, another xanthine, is an effective bronchodilator and displays a better safety profile than theophylline. Therefore, we performed a quantitative synthesis to compare the efficacy and safety profile of different xanthines in COPD.The primary end-point of this meta-analysis was the impact of xanthines on lung function.
What is xanthine in pharmacology?
Group of alkaline substances taken from plants, which react with acids to form salts (e.g., theophylline). Methylxanthines Chemical group of drugs derived from xanthines. There are three methylated (CH3) xanthines: caffeine, theophylline, and theobromine. Phosphodiesterase (PDE) Group of enzymes that change intracellular signaling. Xanthine
What are the benefits of xanthine inhalers?
Xanthines also inhibit the release of slow-reacting substance of anaphylaxis and histamine, decreasing the bronchial swelling and narrowing that occurs as a result of these two chemicals. Relief of symptoms or prevention of bronchial asthma. Reversal of bronchospasm associated with COPD. Co-morbidities.
When should caution be taken when taking xanthines?
Caution should be taken with any patient with GI problems, coronary disease, respiratory dysfunction, renal or hepatic disease, alcoholism, or hyperthyroidism because these conditions can be exacerbated by the systemic effects of xanthines.
Why is theophylline no longer used?
Oral theophylline has been used as a bronchodilator to treat chronic obstructive pulmonary disease (COPD) for decades, but it has fallen out of favor due to the side effects that come with the higher doses that are required to achieve any beneficial effect, as well as the advancement of improved drug treatment.
Why aminophylline is not recommended?
In the adult literature, a Cochrane review from 2012 recommends that aminophylline should not be considered for use in acute asthma due to serious side-effects and limited efficacy [17].
Is xanthine a bronchodilator?
Mechanism of Action. A xanthine derivative that acts as a bronchodilator by directly relaxing smooth muscle of the bronchial airway and pulmonary blood vessels similar to theophylline.
Are xanthine drugs used to treat asthma?
Xanthines have been used in the treatment of asthma as a bronchodilator, though they may also have anti‐inflammatory effects.
What are the negative effects of aminophylline?
Aminophylline side effects fast or irregular heartbeats; a seizure; high blood sugar--increased thirst, increased urination, dry mouth, fruity breath odor; or. low potassium level--leg cramps, constipation, irregular heartbeats, fluttering in your chest, numbness or tingling, muscle weakness or limp feeling.
Why is theophylline no longer commonly used in the treatment of asthma?
For maintenance therapy of asthma, theophylline may be obsolete because it is merely a relatively weak bronchodilator that adds little but side effects to dose- optimized inhaled ~2-agents ... and does not address the underlying inflammation, a fundamental charac- teristic of the disease.
What are the effects of xanthine drugs?
Xanthines also stimulate muscle and cardiac cells and neurons. Xanthines can cause a mild diuresis. The xanthines have many minor side effects (anxiety, nervousness, tremor, headache, dizziness) but are largely well tolerated in the doses used to treat asthma and chronic bronchitis.
Which is the bronchodilator drug related to xanthine?
Theophylline is a bronchodilator that is used in patients with reversible bronchospasm associated with asthma or chronic obstructive pulmonary disease.
What are side effects of xanthine derivatives?
What are side effects of xanthine derivatives?Central nervous system excitement.Headache.Insomnia.Irritability.Restlessness.Skeletal muscle tremors.Seizure.Seizures that are resistant to anticonvulsants.More items...
Which drugs are contraindications with administration of xanthine derivatives?
Methylxanthines are contraindicated in any patient with a history of hypersensitivity reaction to any medication with a xanthine-derivative component (including aminophylline, theophylline, ethylenediamine).
What kind of drugs are xanthines?
Derivatives of xanthine (known collectively as xanthines) are a group of alkaloids commonly used for their effects as mild stimulants and as bronchodilators, notably in the treatment of asthma or influenza symptoms....Pharmacology.NameTheophyllineR2CH3R3HR8HIUPAC nomenclature1,3-Dimethyl-7H-purine-2,6-dione9 more columns
What is the function of xanthine oxidase?
Xanthine oxidase (XO) is an important enzyme catalyzing the hydroxylation of hypoxanthine to xanthine and xanthine to uric acid which is excreted by kidneys. Excessive production and/or inadequate excretion of uric acid results in hyperuricemia.
What are xanthine derivatives used for?
Four types of xanthine derivatives used as bronchodilators in obstructive airway diseases
What stimuli reduce airway responsiveness?
reduced airway responsiveness to stimuli such as histamine and methacholine
Is theophylline always equivalent?
different forms of theophylline are not always equivalent,
Which has a higher therapeutic index, caffeine or theophylline?
Caffeine citrate has a higher therapeutic index and fewer side effects compared with theophylline.
Does theophylline help with bronchitis?
Because of the diuretic effect of theophylline, ensure that patients with excess airway secretions (e.g., those with bronchitis or cystic fibrosis) receive adequate fluid replacement to prevent dehydration and thickening of secretions.
Can you use theophylline for COPD?
Yes or No: Theophylline can be used for maintenance therapy in COPD if anticholinergics (ipratropium bromide) and b agonists cannot control the disease.
How do xanthines work?
A theory suggests that xanthines work by directly affecting the mobilization of calcium within the cell.
Why are anticholinergics used as bronchodilators?
Anticholinergics are used as bronchodilators because of their effect on the vagus nerve, which sis to block or antagonize the action of the neurotransmitter acetylcholine at vagal-mediated receptor sites. By blocking the vagal effect, relaxation of smooth muscle in the bronchi occurs, leading to bronchodilation.
What is bronchodilator used for?
Bronchodilators or antiasthmatics are medications used to facilitate respiration by dilating the airways. They are helpful in symptomatic relief or prevention of bronchial asthma and for bronchospasm associated with COPD. Contents. Therapeutic actions of Xanthines. Indications.
What anticholinergics are not as effective as sympathomimetics?
Patients who cannot tolerate the sympathetic effects of sympathomimetics might respond to the anticholinergic drugs ipratropium (Atrovent) and tiotropium (Spiriva). These drugs are not as effective as the sympathomimetics but can provide some relief to those patients who cannot tolerate the other drugs.
What is the effect of sympathomimetics on the bronchi?
One of the actions of the sympathetic nervous system is dilation of the bronchi with increased rate and depth of respiration. This is the desired effect when selecting a sympathomimetic as a bronchodilator.
What is the best bronchodilator for asthma?
Option D: Beta-adrenergic agonists, such as albuterol, are highly effective bronchodilators and are used to dilate the narrow airways associated with asthma.
Why do drugs interact with xanthines?
Because of the mechanism of xanthine metabolism in the liver, many drugs interact with xanthines.
What is the clinical use of xanthines?
Clinical indications for the use of xanthines. ! KEY POINT. Clinical uses of theophylline include the management of asthma, COPD, and apnea of prematurity in neonates. Theophylline has traditionally been used in the management of asthma and COPD. Theophylline and caffeine have been used to treat apnea of prematurity.
What is xanthine used for?
Chapter 8 reviews the pharmacology of the xanthine drugs, such as theophylline. Theophylline traditionally has been used to treat patients with asthma and chronic obstructive pulmonary disease (COPD) in stable and acute phases.
What is the best med for apnea?
If pharmacologic therapy is needed to stimulate breathing in apnea of prematurity, methylxanthines are considered the first-line agents of choice. Theophylline has been used most extensively, but Bhatia6suggested that caffeine citrate may be the agent of choice. Caffeine citrate penetrates the cerebrospinal fluid better and has a higher therapeutic index with fewer side effects compared with theophylline. Caffeine citrate (Cafcit) has been approved for administration either intravenously or orally.
What is theophylline used for?
Sustained-release theophylline is indicated as an alternative for maintenance (step 2) therapy of mild, persistent asthma and higher in patients older than 5 years of age and is listed as an alternative in step 3 and higher for patients older than 5 years of age in combination with an inhaled corticosteroid (ICS). Sustained-release theophylline is considered a less preferred alternative to low-dose ICS, cromolynlike agents, or antileukotrienes as second-line maintenance drug therapy in stable asthma. Theophylline is not recommended in the guidelines for children younger than 5 years or for any person with acute exacerbation of asthma. 1
Where is xanthine found?
Another xanthine is theobromine. All three agents are found as alkaloids in plant species. Caffeine is found in coffee beans and kola nuts. Caffeine and theophylline are contained in tea leaves, and caffeine and theobromine are in cocoa seeds or beans.
What group is theophylline in?
Theophylline,and its salt, aminophylline,are members of the methylxanthinegroup of drugs, which also includes dyphylline.
Is theophylline a precursor to uric acid?
Theophylline is related chemically to the natural metabolite xanthine, which is a precursor of uric acid. Figure 8-1 shows the general xanthine structure and the structures of theophylline (1,3-dimethylxanthine) and caffeine (1,3,7-trimethylxanthine). Because of their methyl attachments, these agents are often referred to as methylxanthines. Another xanthine is theobromine. All three agents are found as alkaloids in plant species. Caffeine is found in coffee beans and kola nuts. Caffeine and theophylline are contained in tea leaves, and caffeine and theobromine are in cocoa seeds or beans. Historically, these natural plant substances have been used as brews for their stimulant effect.
Where is the 6Dept of Experimental Medicine?
6Dept of Experimental Medicine, Unit of Pharmacology , University of Campania Luigi Vanvitelli, Naples, Italy.
Is xanthine safe for COPD?
Doxofylline, another xanthine, is an effective bronchodilator ...
Is theophylline a good bronchodilator?
Doxofylline, another xanthine, is an effective bronchodilator and displays a better safety profile than theophy ….
Is doxofylline better than theophylline?
Theophylline can still have a role in the management of stable chronic obstructive pulmonary disease (COPD), but its use remains controversial, mainly due to its narrow therapeutic window. Doxofylline, another xanthine, is an effective bronchodilator and displays a better safety profile than theophylline. Therefore, we performed a quantitative synthesis to compare the efficacy and safety profile of different xanthines in COPD.The primary end-point of this meta-analysis was the impact of xanthines on lung function. In addition, we assessed the risk of adverse events by normalising data on safety as a function of person-weeks. Data obtained from 998 COPD patients were selected from 14 studies and meta-analysed using a network approach.The combined surface under the cumulative ranking curve (SUCRA) analysis of efficacy (change from baseline in forced expiratory volume in 1 s) and safety (risk of adverse events) showed that doxofylline was superior to aminophylline (comparable efficacy and significantly better safety), bamiphylline (significantly better efficacy and comparable safety), and theophylline (comparable efficacy and significantly better safety).Considering the overall efficacy/safety profile of the investigated agents, the results of this quantitative synthesis suggest that doxofylline seems to be the best xanthine for the treatment of COPD.