Treatment FAQ

xanthines are no longer the first-line treatment as bronchodilators for what reason

by Geovanni Ziemann Published 2 years ago Updated 1 year ago

What are beta 2 agonist bronchodilators?

Beta 2 agonists are a type of bronchodilator used in the treatment of asthma. Beta 2 agonist medications stimulate beta cells, which relax the smooth muscles of your airways that tighten as part of the pathophysiology of asthma to cause symptoms such as: Wheezing Chest tightness Shortness of breath Chronic cough

What is the first-line therapy for asthma?

Thus, in 1914, anticholinergics by injection or inhalation were considered as first-line asthma therapies. Osler also made the important observation of the intraindividual differences in the response to asthma treatment.

How effective are ß2-agonist medications for treating asthma?

ß2-agonist medications are considered highly effective at relieving symptoms of asthma. Modern ß2-agonists are the result of more than a century of intensive research into asthma treatments. 4 SABAs provide almost instant relief of symptoms, but the effect only lasts for between four and six hours.

Which study had the biggest impact on the use of inhaled corticosteroids?

The study that had the biggest impact on the use of inhaled corticosteroids was that of Haahtela and coworkers ( 33 ). In this trial, patients with newly diagnosed asthma were randomly assigned to receive inhaled corticosteroids or an inhaled β 2 agonist as their primary asthma treatment for 2 years.

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.

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.

Why theophylline is not recommended?

However, at clinically effective blood concentrations of around 10–20 mg/L, theophylline is frequently associated with adverse effects, such as nausea and other gastrointestinal disturbances, cardiac arrhythmias, and CNS excitation, leading to a narrow therapeutic window.

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 is xanthine used for?

The major use of xanthine derivatives are for relief of bronchospasm caused by asthma or chronic obstructive lung disease. The most widely used xanthine is theophylline.

Which is the bronchodilator drug related to xanthine?

A bronchodilator consisting of theophylline that is used for the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis....Xanthine derivatives.DrugTargetTypeTheophyllineAdenosine receptor A2atargetTheophyllineCytochrome P450 1A2enzymeTheophyllineAdenosine deaminaseenzyme124 more rows

Who should not take theophylline?

Kidney disease in infants younger than 3 months of age or. Liver disease (e.g., cirrhosis, hepatitis) or. Pulmonary edema (lung condition) or. Shock (serious condition with very little blood flow in the body)—Use with caution.

What is theophylline toxicity?

Therefore, Theophylline toxicity occurs when serum theophylline levels surpass the levels in the therapeutic range. This can occur by intentional overdose or unintentionally when metabolism and/or clearance of theophylline is altered due to certain physiological stressors.

What is the side effect of theophylline?

Nausea/vomiting, stomach/abdominal pain, headache, trouble sleeping, diarrhea, irritability, restlessness, nervousness, shaking, or increased urination may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.

How do xanthines work in asthma?

Xanthine derivatives are a group of alkaloids that work as mild stimulants and bronchodilators. Xanthine derivatives ease symptoms of bronchospasm and make breathing easier by relaxing the smooth muscles of the respiratory tract and reducing the airway's hypersensitive response to stimuli.

What are the side effects of xanthine derivatives?

SIDE EFFECTS: Dizziness, headache, lightheadedness, heartburn, stomach pain, loss of appetite, restlessness, nervousness, sleeplessness or increased urination may occur as your body adjusts to the medication. If these symptoms persist or worsen, inform your doctor.

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 are the three types of bronchodilators?

For treating asthma symptoms, there are three types of bronchodilators: beta-agonists, anticholinergics, and theophylline. You can get these bronchodilators as tablets, liquids, and shots, but the preferred way to take beta-agonists and anticholinergics is inhaling them.

What are the bronchodilator drugs?

The 3 most widely used bronchodilators are:beta-2 agonists, such as salbutamol, salmeterol, formoterol and vilanterol.anticholinergics, such as ipratropium, tiotropium, aclidinium and glycopyrronium.theophylline.

Is terbutaline a xanthine bronchodilator?

Terbutaline is a beta-2 adrenergic agonist used as a bronchodilator and to prevent premature labor. Terbutaline was first synthesized in 1966 12 and described in the literature in the late 1960s and early 1970s. It is a selective beta-2 adrenergic agonist used as a bronchodilator in asthmatic patients.

Which drug is a xanthine oxidase inhibitor?

Allopurinol. Allopurinol, a xanthine oxidase inhibitor, is commonly used for the treatment of hyperuricemia and gout.

How long does a bronchodilator last?

These agents had rapid onset of action, produced bronchodilation lasting 4 to 6 hours, and became the “bronchodilator of choice.”. Since the mid-1980s, bronchoconstriction that could be relieved by the inhalation of a specific β 2 agonist was commonly included as a diagnostic criterion of asthma.

How effective are corticosteroids for asthma?

Inhaled corticosteroids have been recommended and used in the treatment of asthma for just over 30 years; they are very effective as “asthma-controller” therapies, but there are no convincing data that they are disease-modifying treatments.

When did corticosteroids start being used?

Western medicine began to use adrenergic stimulants approximately 100 years ago, but they were likely used in Asian medicine long before that. Systemic treatment with corticosteroids was introduced into the treatment of asthma in the mid-20th century; inhaled corticosteroids have been in use for over 35 years.

What was the general approach to asthma treatment?

Thus, more than 100 years ago, the general approach to asthma treatment was then as it is now: acute rescue treatment, controller treatment, and prevention of long-term complications. This article examines the evolution of the treatment of asthma by environmental manipulation and drug treatments over the past 100 years. Because we want to identify the most commonly used general practices until the late 20th century, we take most of our guidance from generally accepted textbooks of medicine. We also have tried to identify the key contributions that led to the evolution of asthma treatment.

How to treat asthma?

The treatment of asthma involves the treatment of the patient during fits and between the fits. The general indications are: 1 To allay the spasm during the paroxysm; 2 To find out and remove the exciting cause … 3 To treat complications and sequelae and to improve the general health.

What advice did Stewart and Gibson give to patients with asthma?

In the 1896 textbook of Stedman, as noted previously, Stewart and Gibson ( 3) offer advice for the management of the patient with asthma based on removal of the offending allergens from the environment: “This may be the avoidance of certain foods, the avoidance of exposure to dust or pollen or flowers … or other specific irritants . It may be the correction of a gastric … disorder … or it may be the removal of nasal polyps.”

How many types of pharmacologic treatments are there for asthma?

There are four general types of pharmacologic treatment that have been used for asthma over the past 100 years. Interestingly, most of the treatments, once introduced, have remained in the pharmacopeia, although the specific entities and methods of delivery have changed. These four overlapping epochs of the pharmacologic treatment ...

When did metformin become known as dimethyl-biguanide?

Rediscovery of dimethyl-biguanide. In the 1940s , metformin inadvertently gained recognition for its ability to lower blood glucose—an observation noted when used to treat influenza.4In 1957, a French physician, Jean Sterne,5published data which indicated metformin’s superior ability to safely lower blood-glucose levels.

What is the first line of treatment for type 2 diabetes?

Keywords: first-line therapy, metformin, type 2 diabetes. Introduction. Metformin is a biguanide that is used as first-line treatment of type 2 diabetes mellitus and is effective as monotherapy and in combination with other glucose-lowering medications.

What is metformin used for?

Within a year, metformin was prescribed in Europe for the treatment of type 2 diabetes mellitus, and Sterne dubbed the drug “glucophage” for its perceived ability to devour blood glucose.3.

Is metformin a good antihyperglycemic?

There are few studies comparing metformin with newer anti-hyperglycemic agents. A recent study compared different doses of canagliflozin (100/300 mg) with metformin and combination therapy. While the results indicated that combination therapy was superior in glucose-lowering to the other treatment groups, both doses of the canagliflozin were found to be non-inferior to metformin. However, the canagliflozin groups achieved greater weight loss.29This study suggests that there might be an additional benefit to choosing a sodium-glucose cotransporter-2 (SGLT-2) inhibitor as first-line therapy or considering combination therapy as initial treatment of type 2 diabetes in certain individuals.

Does metformin decrease HBA1C?

Metformin monotherapy has been shown to decrease mean HbA1c by 1.3% , compared with a 0.4% increase in the placebo group after 29 weeks.8The United Kingdom Prospective Diabetes Study (UKPDS) not only found a greater improvement in glycemic control in patients taking metformin compared with the conventional treatment arm but also showed that metformin therapy resulted in a reduction in hypoglycemic events and weight gain compared with sulfonylureas and insulin.26

Is metformin good for diabetes?

Metformin is a biguanide that is used as first-line treatment of type 2 diabetes mellitus and is effective as monotherapy and in combination with other glucose-lowering medications. It is generally well-tolerated with minimal side effects and is affordable. Although the safety and efficacy of metformin have been well-established, there is discussion regarding whether metformin should continue to be the first choice for therapy as other anti-hyperglycemic medications exhibit additional advantages in certain populations. Despite a long-standing history of metformin use, there are limited cardiovascular outcomes data for metformin. Furthermore, the available studies fail to provide strong evidence due to either small sample size or short duration. Recent data from glucagon-like peptide-1 receptor agonist and sodium-glucose cotransporter-2 inhibitor cardiovascular and renal outcomes trials demonstrated additional protection from diabetes complications for some high-risk patients, which has impacted the guidelines for diabetes management. Post-hoc analyses comparing hazard ratios for participants taking metformin at baseline versusnot taking metformin are inconclusive for these two groups. There are no data to suggest that metformin should not be initiated soon after the diagnosis of diabetes. Furthermore, the initiation of newer glycemic-lowering medications with cardiovascular benefits should be considered in high-risk patients regardless of glycemic control or target HbA1c. However, cost remains a major factor in determining appropriate treatment.

Is there a placebo controlled trial for metformin?

Unfortunately, there has never been and likely will never be a placebo-controlled cardiovascular outcomes trial with metformin in patients with type 2 diabetes . However, the ongoing VA-IMPACT trial will examine the effect of metformin on MACEs in individuals with pre-diabetes and established ASCVD.38

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