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DOXOFYLLINE

DOXOFYLLINE 400 MG TABLETS

BIBEK SINGH MAHAT M.PHARM.

CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) :

Chronic obstructive pulmonary disease (COPD) is a disease state characterized by airflow limitation that is not fully reversible. This newest definition COPD, provided by the Global Initiative for Chrnonic Obstructive Lung Disease (GOLD), is a broad description that better explains this disorder and its signs and symptoms (GOLD, World Health Organization [WHO] & National Heart, Lung and Blood Institute [NHLBI], 2004).

CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) :

COPD may include diseases that cause airflow obstruction (e.g., Emphysema, chronic bronchitis) or any combination of these disorders. Other diseases as cystic fibrosis, bronchiectasis, and asthma that were previously classified as types of chronic obstructive lung disease are now classified as chronic pulmonary disorders. However, asthma is now considered as a separate disorder and is classified as an abnormal airway condition characterized primarily by reversible inflammation. COPD can co-exist with asthma.

CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) :

Currently, COPD is the fourth leading cause of mortality and the 12th leading cause of disability.

However, by the year 2020 it is estimated that COPD will be the third leading cause of death and the fourth leading cause of disability (Sin, McAlister, Man. Et al., 2003).

People with COPD commonly become symptomatic during the middle adult years, and the incidence of the disease increases with age.

CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) :

ANATOMY AND PHYSIOLOGY:

The respiratory system consists of all the organs involved in breathing. These include the nose, pharynx, larynx, trachea, bronchi and lungs.

The respiratory system does two very important things: it brings oxygen into our bodies, which we need for our cells to live and function properly; and it helps us get rid of carbon dioxide, which is a waste product of cellular function.
The nose, pharynx, larynx, trachea and bronchi all work like a system of pipes through which the air is funneled down into our lungs.

ANATOMY AND PHYSIOLOGY:

There, in very small air sacs called alveoli, oxygen is brought into the bloodstream and carbon dioxide is pushed from the blood out into the air. When something goes wrong with part of the respiratory system, such as an infection like pneumonia, chronic obstructive pulmonary diseases, it makes it harder for us to get the oxygen we need and to get rid of the waste product carbon dioxide. Common respiratory symptoms include breathlessness, cough, and chest pain.

ANATOMY AND PHYSIOLOGY:

ANATOMY AND PHYSIOLOGY:

ANATOMY AND PHYSIOLOGY:

ANATOMY AND PHYSIOLOGY:


How they work

Air enters your lungs through a system of pipes called the bronchi.
These pipes start from the bottom of the trachea as the left and right bronchi and branch many times throughout the lungs, until they eventually form little thin-walled air sacs or bubbles, known as the alveoli. The alveoli are where the important work of gas exchange takes place between the air and your blood. Covering each alveolus is a whole network of little blood vessel called capillaries, which are very small branches of the pulmonary arteries. It is important that the air in the alveoli and the blood in the capillaries are very close together, so that oxygen and carbon dioxide can move (or diffuse) between them.

ANATOMY AND PHYSIOLOGY:


How they work

In the capillaries are very close together, so that oxygen and carbon dioxide can move (or diffuse) between them.
So, when you breathe in, air comes down the trachea and through the bronchi into the alveoli. This fresh air has lots of oxygen in it, and some of this oxygen will travel across the walls of the alveoli into your bloodstream. Traveling in the opposite direction is carbon dioxide, which crosses from the blood in the capillaries into the air in the alveoli and is then breathed out. In this way, you bring in to your body the oxygen that you need to live, and get rid of the waste product carbon dioxide.

RISK FACTORS FOR COPD :

RISK FACTORS FOR COPD :


Risk factors for COPD include environmental exposures and host factors. The most important risk factor for COPD is cigarette smoking. Other risk factors are pipe, cigar, and other types of tobacco smoking. In addition, passive smoking contributes to respiratory symptoms and COPD.

Smoking depresses the activity of scavenger cells and affects the respiratory tracts ciliary cleansing mechanism, which keeps breathing passages free of inhaled irritants, bacteria, and other foreign matter.

RISK FACTORS FOR COPD :


When smoking damages this cleansing mechanism, airflow is obstructed and air becomes trapped behind the obstruction. The alveoli greatly distend, diminished lung capacity. Smoking also irritates the goblet cells and mucus glands, causing an increased accumulation of mucus, which in turn produces more irritation, infection, and damage to the lung. In addition, carbon monoxide (a by product of smoking) combines with hemoglobin to form carboxyhemoglobin. Hemoglobin that is bound by carboxyhemoglobin cannot carry oxygen efficiently.

RISK FACTORS FOR COPD :

ASTHMA
What Is Asthma? Asthma (AZ-ma) is a chronic (long-term) lung disease that inflames and narrows the airways. Asthma causes recurring periods of wheezing (a whistling sound when you breathe), chest tightness, shortness of breath, and coughing. The coughing often occurs at night or early in the morning.

Asthma affects people of all ages, but it most often starts during childhood. In the United States, more than 25 million people are known to have asthma. About 7 million of these people are children.

ASTHMA
To understand asthma, it helps to know how the airways work. The airways are tubes that carry air into and out of your lungs.

People who have asthma have inflamed airways. This makes them swollen and very sensitive. They tend to react strongly to certain inhaled substances.
When the airways react, the muscles around them tighten. This narrows the airways, causing less air to flow into the lungs. The swelling also can worsen, making the airways even narrower. Cells in the airways might make more mucus than usual. Mucus is a sticky, thick liquid that can further narrow the airways. This chain reaction can result in asthma symptoms. Symptoms can happen each time the airways are inflamed.

ASTHMA

ASTHMA

ASTHMA

DOXOFYLLINE TABLETS

Doxofylline (also known as doxophylline) is a xanthine derivative drug used in the treatment of asthma. It has antitussive and bronchodilator effects, and acts as a phosphodiesterase inhibitor. In animal and human studies, it has shown similar efficacy to theophylline but with significantly less side effects. Unlike other xanthines, doxofylline lacks any significant affinity for adenosine receptors and does not produce stimulant effects. This suggests that its antiasthmatic effects are mediated by another mechanism, perhaps its actions on phosphodiesterase.

DOXOFYLLINE TABLETS

Doxofylline is a type of enzyme inhibitor drugs that is used to treat Asthma and COPD. Doxofylline belongs to category of enzyme inhibitor activity drugs. Specifically, Doxofylline is a new generation long acting oral methylxanthine derivative. Methylxanthines are phosphodiesterase inhibitors. Doxofylline is available as the Brand Name, DOXOFYLLINE. Doxofylline also has antitussive and bronchodilator affects.

DOXOFYLLINE TABLETS

Indication for use of Doxofylline:-

For maintenance therapy in patients suffering with Asthma and Chronic Obstructive Pulmonary Disease (COPD). Side Effects :No CNS and CVS side effects. Doxofylline has a prolonged bronchodilator effect and unlike theophylline it has least adenosine interactions. It is highly safe in smokers. There is no sleep disturbances and no effects on gastric secretions with doxofylline.

DOXOFYLLINE TABLETS

Dosages of Doxofylline:Adult:400mg once a day. Single dose, administration in the evening reduces nocturnal, symptoms and helps to keep the patients complaint free during the day. However, in certain cases, 400mg twice daily is recommended on the basis of the clinical response. Doses as high as 1200mg/day (400mg 3 times day) may also be prescribed .

DOXOFYLLINE TABLETS ARTICLES


Med Sci Monit. 2002 Apr;8(4):CR297-304. Efficacy and safety of doxofylline compared to theophylline in chronic reversible asthma -- a double-blind randomized placebo-controlled multicentre clinical trial. Goldstein MF, Chervinsky P. Source:-The Asthma Center, Philadelphia, PA 19107-1578, USA. Gpike35@aol.com BACKGROUND: Experimental studies have shown that doxofylline is endowed with a remarkable bronchodilator activity with less extra-respiratory effects than theophylline. This trial was designed to compare the efficacy and safety of doxofylline, theophylline, and placebo in patients with chronic reversible bronchial asthma.

DOXOFYLLINE TABLETS ARTICLES DOXOFYLLINE TABLETS

CONCLUSIONS: This study provides evidence that doxofylline 400 mg t.i.d. is an effective treatment for relieving airway obstruction and displays a better safety profile with respect to theophylline 250 mg t.i.d. with a favorable risk-to-benefit ratio.

DOXOFYLLINE TABLETS ARTICLES DOXOFYLLINE TABLETS


Expert Opin Pharmacother. 2009 Oct;10(14):2343-56. Doxofylline: a promising methylxanthine derivative for the treatment of asthma and chronic obstructive pulmonary disease. Shukla D, Chakraborty S, Singh S, Mishra B. Source:- Banaras Hindu University, Institute of Technology, Department of Pharmaceutics, Varanasi, India. BACKGROUND: Doxofylline, a methylxanthine derivative, has recently drawn attention because of its better safety profile and similar efficacy over the most widely prescribed analogue, theophylline, indicated for asthma and chronic obstructive pulmonary disease.

DOXOFYLLINE TABLETS PATIENT INFORMATION:


Uses It is used to treat Asthma and Chronic Obstructive Pulmonary Disease (COPD). It is a type of enzyme inhibitor and is designed to be used to manage these conditions. Please note that this product is not designed for use as an emergency treatment during an asthma attack. Dosage and Administration Adult patients are usually advised to dose 1 to 3 times a day (400mg per time). Your dosage depends on your response to the medication. If you have been advised to dose once a day, you may be directed to do so in the evenings to reduce nocturnal symptoms.

DOXOFYLLINE TABLETS PATIENT INFORMATION:


Side effects Doxobid (Doxofylline) rarely causes serious side effects, however possible symptoms are similar to taking excess amount of caffeine. These include:

Upset stomach Heartburn Difficulty sleeping (insomnia) Headaches Mood changes

MECHANISM OF ACTION:

Doxofylline is a theophylline derivative. Its mechanism of action is related to the inhibition of phosphodiesterase activities, resulting in bronchodilating effects. Doxofylline has a prolonged bronchodilator effects and unlike theophylline it has least adenosine interactions i.e., no CNS and CVS side effects. There is no sleep disturbances and no effects on gastric secretions with doxofylline. It is highly safe in smokers.

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