etophylline

Action and Spectrum

Actions and spectrum: 

Action: 

• Bronchodilation: theophylline relaxes the smooth muscles in the airways of the lungs, resulting in bronchodilation. This action helps to widen the air passages, improve airflow, and relieve bronchoconstriction. It is used to treat respiratory conditions like asthma and chronic obstructive pulmonary disease (COPD). 
• Anti-Inflammatory Effects: theophylline may have mild anti-inflammatory properties, which can help reduce the release of certain inflammatory mediators in the airways. 

Spectrum: 

• Asthma: etophylline can help manage and alleviate bronchoconstriction, which is a hallmark of asthma. It is used to relieve acute asthma symptoms and as a long-term maintenance therapy to prevent exacerbations. 
• Chronic Obstructive Pulmonary Disease (COPD): etophylline is also used in the treatment of COPD, including chronic bronchitis and emphysema, to improve breathing and reduce symptoms like shortness of breath and cough. 
• Other Respiratory Conditions: In some cases, etophylline may be prescribed to individuals with reversible airway obstruction due to other respiratory conditions, such as bronchiolitis or bronchiectasis. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Stomach pain 

Headache 

Insomnia 

Vomiting 

Irregular heartbeat 

Skin rash 

Diarrhea 

Restlessness 

Irritability 

Increased heart rate 

Seizures 

Black Box Warning

Black Box Warning: 

There is no specific black box warning for etophylline. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals who have a known hypersensitivity or allergy to theophylline, etophylline, or any of the medication’s components should not use it. 
• Active Peptic Ulcer: etophylline can stimulate gastric acid secretion, which may exacerbate symptoms of peptic ulcers. It is contraindicated in individuals with an active peptic ulcer. 
• Seizure Disorders: etophylline can lower the seizure threshold, and it should be used with caution or avoided in individuals with a history of seizure disorders. It may precipitate or worsen seizures. 
• Arrhythmias: Individuals with certain types of arrhythmias, especially ventricular arrhythmias, should avoid etophylline, as it can increase the risk of arrhythmias. 
• Heart Conditions: Individuals with severe heart conditions, especially those at risk of arrhythmias or congestive heart failure, should be cautious with etophylline use, as it can exacerbate these conditions. 
• Thyroid Disease: etophylline may affect thyroid hormone levels. It should be used with caution in individuals with hyperthyroidism (overactive thyroid) or hypothyroidism (underactive thyroid).

Caution: 

• Age and Weight: theophylline clearance can vary based on age and weight. Children and the elderly may require different dosing strategies. Age-appropriate dosing and monitoring are crucial. 
• Renal Impairment: theophylline is eliminated through the kidneys. Individuals with impaired renal function may require dose adjustments, as the drug may accumulate in the body. 
• Hepatic Impairment: theophylline is primarily metabolized in the liver. Individuals with liver disease, including cirrhosis, may metabolize the drug differently. Dose adjustments may be necessary. 
• Interactions: theophylline can interact with a wide range of medications and substances, including certain antibiotics, antifungal drugs, and herbal supplements. Healthcare providers should be informed of all medications and supplements the patient is taking to assess potential interactions. 
• Smoking and Caffeine: Smoking and caffeine can affect the metabolism of theophylline. Smokers may require higher doses, while reducing caffeine intake may help prevent side effects. 
• Hypertension: etophylline can cause an increase in blood pressure. It should be used cautiously in individuals with hypertension.

Comorbidities: 

• Gastroesophageal Reflux Disease (GERD): GERD is a common comorbidity in individuals with asthma. It can exacerbate respiratory symptoms and may need to be managed alongside etophylline therapy. 
• Osteoporosis: Chronic use of corticosteroids for respiratory conditions can increase the risk of osteoporosis. This may require monitoring and appropriate management strategies. 
• Diabetes: Diabetes may be a comorbidity in individuals with respiratory conditions. theophylline can affect glucose metabolism, and blood sugar levels may need to be monitored more closely. 
• Chronic Kidney Disease: theophylline is cleared from the body primarily through the kidneys. Individuals with chronic kidney disease may require dose adjustments to prevent drug accumulation. 
• Liver Disease: theophylline is metabolized in the liver. Individuals with liver disease, such as cirrhosis, may metabolize the drug differently, and dose adjustments may be necessary. 
• Obesity: Obesity is a common comorbidity in individuals with respiratory conditions and can impact dosing and treatment strategies. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

etophylline contains the active component theophylline, which is a bronchodilator with both anti-inflammatory and bronchodilating properties. It acts by relaxing smooth muscles of the airways, leading to bronchodilation, improved airflow, and relief from bronchoconstriction. theophylline also has mild anti-inflammatory effects.

It is used to treat respiratory conditions such as asthma and COPD. theophylline’s therapeutic range is narrow, so careful monitoring of blood levels is required to ensure both its effectiveness and the prevention of potential side effects and toxicity. Individualized dosing is often necessary to maintain the drug within the therapeutic range.  

Pharmacodynamics: 

• Bronchodilation: etophylline exerts its bronchodilatory effect by relaxing the smooth muscles of the bronchioles and bronchi in the lungs. This relaxation results in the widening of the airways, allowing for increased airflow and improved ventilation.  
• Anti-Inflammatory Effects: theophylline has mild anti-inflammatory properties. It can reduce the release of certain inflammatory mediators in the airways, potentially helping to control and manage the chronic inflammation associated with asthma and other respiratory diseases. These anti-inflammatory effects are part of what makes theophylline a valuable component in the treatment of these conditions. 
• Stimulation of the Respiratory Center: theophylline can stimulate the central respiratory center in the brain, resulting in an increase in the drive to breathe. This effect can be beneficial in conditions where respiratory drive is compromised, such as in some cases of COPD. 
• Enhanced Diaphragm Function: theophylline may enhance the strength of diaphragm, the primary muscle involved in breathing. This can lead to improved breathing patterns in certain situations. 
• Increased Heart Rate: theophylline can have a mild positive chronotropic effect, meaning it can increase heart rate. This effect is well-tolerated but can be a consideration, particularly in individuals with preexisting heart conditions.

Pharmacokinetics: 

Absorption 

etophylline is typically administered orally, and theophylline is absorbed from gastrointestinal tract after ingestion. The rate & extent of absorption can vary based on factors such as the specific formulation of the medication (e.g., immediate-release or sustained-release), the presence of food in the stomach, and individual patient factors. 

Distribution 

theophylline is distributed throughout the body, with a particular affinity for fatty tissues. It readily crosses cell membranes, including those in the central nervous system. The volume of distribution is large, meaning that the drug is distributed extensively in body tissues. 

Metabolism 

theophylline is primarily metabolized in the liver through a group of enzymes collectively known as the cytochrome P450 system, with a focus on the CYP1A2 enzyme. This metabolism leads to the formation of several metabolites. The rate of metabolism can vary between individuals, influenced by factors like genetics, age, and interactions with other medications. 

Elimination and excretion 

theophylline and its metabolites are primarily excreted through the kidneys. A small fraction may also be eliminated in the feces through biliary excretion. The clearance of theophylline depends on renal function, which can vary widely among individuals. In patients with impaired kidney function, the elimination half-life of theophylline may be prolonged, necessitating dose adjustments to prevent drug accumulation and potential toxicity. 

Adminstartion

Administration: 

• Dosing Schedule: The dosing schedule for etophylline is determined by healthcare provider and is based on patient’s specific condition, age, weight, and the specific product prescribed.  
• Oral Administration: etophylline is taken by mouth (orally). It is usually recommended to take it on an empty stomach, at least one hour before or 2 hours after a meal, to optimize absorption. Taking it with food can slow the absorption of theophylline and may lead to variations in drug levels. 
• Extended-Release Formulation: Some formulations of etophylline are extended-release (sustained-release) and are designed to release the medication slowly over time, allowing for less frequent dosing. It is important to follow the instructions for extended-release products carefully and not crush or chew them. 
• Individualized Dosing: theophylline has a narrow therapeutic range, and individualized dosing is common. The dosage is often adjusted based on the patient’s response to the medication and periodic monitoring of theophylline blood levels. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: etophylline 

Pronounced: (ee-TAW-fi-leen)  

Why do we use etophylline? 

etophylline is used in the management of asthma, a chronic respiratory condition characterized by recurrent episodes of wheezing, shortness of breath, coughing, and chest tightness. It helps relax the airway muscles and reduces airway inflammation, improving airflow and relieving bronchoconstriction. etophylline is used in the treatment of COPD, a progressive lung disease that includes chronic bronchitis and emphysema.

It helps alleviate symptoms such as breathlessness and cough by widening the airways and reducing inflammation. etophylline can be used to manage chronic bronchitis which is characterized by the inflammation of bronchial tubes and excessive mucus production. By promoting bronchodilation and reducing inflammation, it helps ease symptoms like cough and breathlessness.