dyphylline

Action and Spectrum

Actions and Spectrum: 

dyphylline is a medication that belongs to the xanthine class of drugs and is used primarily for treating respiratory conditions, like asthma and chronic obstructive pulmonary disease (COPD). It is a bronchodilator, which helps relax and open the airways, making breathing easier. 

The action of dyphylline is similar to other xanthines, such as theophylline and caffeine. It works by inhibiting the enzyme phosphodiesterase, which enhances the levels of cyclic adenosine monophosphate (cAMP) in smooth muscle cells. Elevated cAMP levels promote smooth muscle relaxation and bronchodilation, widening the airways and improving airflow. 

dyphylline also has a mild stimulant effect on the central nervous system, similar to caffeine, although it is less potent. This stimulant effect can help to increase respiratory drive and reduce fatigue in some individuals with respiratory conditions. 

In terms of its spectrum, dyphylline primarily acts on the smooth muscles of the respiratory system, including the bronchioles and bronchial muscles. Relaxing these muscles can alleviate bronchospasms and improve airflow, making breathing easier for individuals with asthma or COPD. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Extrasystoles 

Nausea 

Albuminuria 

Tachypnea 

Hypotension 

Ventricular arrhythmia 

Circulatory failure 

Hematuria 

Tachycardia 

Headache 

Seizure 

Muscle twitching 

Restlessness 

Upset stomach 

Hyperglycemia 

Palpitation 

Insomnia 

Irritability 

Diuresis 

Black Box Warning

Black Box Warning: 

The black box warning for dyphylline highlights the potential for severe and life-threatening adverse reactions associated with its use. The warning advises that dyphylline should be reserved for patients who generally do not respond to other asthma and chronic obstructive pulmonary disease therapies. 

The specific risks associated with dyphylline use that are highlighted in the black box warning include: 

• Cardiac arrhythmias: dyphylline can cause changes in the heart’s electrical activity, leading to potentially dangerous arrhythmias. These can occur even in patients without a history of heart disease or arrhythmias. Patients with pre-existing heart conditions are at higher risk. 
• Seizures: dyphylline can lower the seizure threshold and increase the risk of seizures. This risk is more in patients with a prior history of seizures or other risk factors for seizures, such as head injury or brain tumor. 
• Gastrointestinal bleeding: dyphylline can cause irritation and damage the lining of the stomach, intestines, leading to gastrointestinal bleeding.  
• Hypersensitivity reactions: Some patients may develop allergic reactions to dyphylline, which can be severe and even life-threatening in some cases. 
• Use in pregnancy and breastfeeding: Using dyphylline during pregnancy condition and breastfeeding is not recommended, as it can cause fetal harm and may be passed into breast milk. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

dyphylline has several contraindications, meaning there are specific conditions or circumstances in which its use is not recommended. These contraindications include: 

• Hypersensitivity: dyphylline should not be used in individuals with known hypersensitivity or allergy to dyphylline or its components. 
• Active peptic ulcer: dyphylline can irritate and potentially worsen peptic ulcers in the stomach or intestines. Therefore, it is contraindicated in individuals with active peptic ulcer disease. 
• Seizure disorders: dyphylline can lower the seizure threshold, making it contraindicated in individuals with a history of seizures or those at an increased risk of seizures, such as those with a head injury or brain tumor. 
• Cardiac arrhythmias: dyphylline can cause changes in heart rhythm and potentially lead to cardiac arrhythmias. It is contraindicated in individuals with pre-existing cardiac arrhythmias or those at a high risk of developing arrhythmias. 
• Porphyria: dyphylline may worsen symptoms or trigger an acute attack in individuals with porphyria, a group of rare genetic disorders affecting heme production, a hemoglobin component. 
• Concurrent use of other xanthine derivatives: Simultaneous use of dyphylline with other xanthine derivatives, such as theophylline or caffeine, is contraindicated due to the potential for additive effects and increased risk of adverse reactions. 

Caution 

While no specific cautions are associated with dyphylline, it is essential to exercise caution and consider certain factors when using this medication. These cautions include: 

• Renal impairment: dyphylline is primarily excreted through the kidneys. Individuals with impaired kidney function may experience slower drug clearance, leading to higher levels in the body. Adjustments in dosage or careful monitoring may be necessary in such cases. 
• Hepatic impairment: dyphylline is metabolized in the liver. Patients with liver disease or impaired liver function may have slower metabolism of the drug, leading to increased levels in the body. Dose adjustments or close monitoring may be required. 
• Elderly population: Elderly individuals may be more susceptible to the effects of dyphylline due to age-related changes in drug metabolism and clearance. Careful monitoring and adjustments in dosage may be necessary. 
• Cardiovascular conditions: dyphylline may affect the cardiovascular system, including potential cardiac arrhythmias. Patients with underlying cardiovascular conditions, such as heart disease or hypertension, should be closely monitored while taking dyphylline. 
• Seizure threshold: dyphylline can lower the seizure threshold and may increase the risk of seizures. Individuals with a prior history of seizures or those at a higher risk of developing seizures should use dyphylline cautiously and be closely monitored. 
• Pregnancy and breastfeeding: Using dyphylline during pregnancy and breastfeeding should be cautiously approached.  
• Drug interactions: dyphylline may interact with other medications, including but not limited to cimetidine, fluvoxamine, erythromycin, and certain fluoroquinolone antibiotics. To avoid potential interactions, you must inform your healthcare provider about all your medications, supplements, and herbal products. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: C 

Lactation:   

Excreted into human milk: Yes. 

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: 

dyphylline is a xanthine derivative with pharmacological properties contributing to its therapeutic effects. Here are some critical aspects of the pharmacology of dyphylline: 

• Bronchodilation: dyphylline acts as a bronchodilator by relaxing the smooth muscles of the bronchioles and bronchial tubes in the lungs. It achieves this by inhibiting the enzyme phosphodiesterase, which leads to increased levels of cyclic adenosine monophosphate (cAMP) in smooth muscle cells. Elevated cAMP levels promote smooth muscle relaxation and bronchodilation, improving airflow. 
• Anti-inflammatory effects: dyphylline possesses mild anti-inflammatory properties, which can help reduce inflammation in the airways. This effect may improve respiratory symptoms in conditions like asthma and COPD. 
• Central nervous system stimulation: dyphylline has a mild stimulant effect on the CNS (central nervous system), similar to caffeine. This stimulation can enhance respiratory drive and reduce fatigue in individuals with respiratory conditions. 
• Adenosine receptor antagonism: dyphylline antagonizes adenosine receptors, notably the A1 and A2A subtypes. By blocking these receptors, it inhibits the bronchoconstrictive effects of adenosine, further promoting bronchodilation. 
• Pharmacokinetics: dyphylline is well-absorbed after oral administration. It undergoes hepatic metabolism, primarily through demethylation and hydroxylation, resulting in the formation of metabolites such as 5-methyl-7-(2,3-dihydroxypropyl)-1H-purine-2,6-dione (methylandioxydyphylline) and 7-(2,3-dihydroxypropyl)-1H-purine-2,6-dione (methyldyphylline). The elimination half-life of dyphylline is around 5 to 8 hours, but it can vary among individuals. The drug and its metabolites are mainly excreted through the kidneys. 
• Drug interactions: dyphylline may interact with other medications, including but not limited to cimetidine, fluvoxamine, erythromycin, and certain fluoroquinolone antibiotics. These interactions can affect the metabolism and clearance of dyphylline, leading to potential drug interactions and adverse effects. To avoid potential interactions, you must inform your healthcare professional about all your medications, supplements, and herbal products. 

Remember, the pharmacology of dyphylline is complex, and its effects can vary among individuals. Following the prescribed dosage and consulting your healthcare professional for personalized advice and guidance regarding using dyphylline based on your specific condition and medical history is essential. 

Pharmacodynamics: 

Mechanism of action: dyphylline works by inhibiting the enzyme phosphodiesterase (PDE), specifically PDE III and PDE IV. By inhibiting PDE, dyphylline increases intracellular cyclic adenosine monophosphate (cAMP) levels, relaxing bronchial smooth muscles and bronchodilation. It also has weak adenosine receptor antagonistic activity. 

Pharmacokinetics: 

Absorption 

dyphylline is well-absorbed after oral administration. It is wholly and rapidly absorbed from the gastrointestinal tract (GIT), with peak plasma concentrations achieved within 30 minutes- two hours after ingestion. 

Distribution 

dyphylline is distributed widely throughout the body, including the lungs and other tissues. It readily crosses cell membranes and has a relatively large volume of distribution, indicating extensive tissue distribution. 

Metabolism 

dyphylline undergoes hepatic metabolism. The primary metabolic pathways include demethylation and hydroxylation. These metabolic processes lead to the formation of active metabolites, such as methylandioxydyphylline and methyldyphylline. These metabolites also contribute to the pharmacological activity of dyphylline. 

Elimination and Excretion 

The elimination of dyphylline and its metabolites occurs mainly through the kidneys. Renal excretion accounts for the primary route of elimination. The elimination half-life of dyphylline is around 5 to 8 hours, but it can vary among individuals. 

Adminstartion

Administration: 

Oral administration 

dyphylline is available in various forms, including oral tablets and extended-release capsules. The administration of dyphylline typically involves the following guidelines: 

• Dosage: The dosage of dyphylline is determined by the prescribing healthcare professional based on factors such as the individual’s age, weight, medical condition, and response to treatment. It is key to follow the prescribed dosage and any specific instructions provided. 
• Timing: dyphylline is usually taken orally, and the timing of administration may vary depending on the formulation. Immediate-release tablets are typically taken every 6 to 8 hours, while extended-release capsules are usually taken once or twice daily. Follow the specific instructions your healthcare professional provides or the medication’s label. 
• Swallowing: Swallow the tablets or capsules whole with a glass of water. Do not crush, chew, or break them unless instructed by your healthcare professional. 
• Food and beverage: dyphylline can be taken with or without food. However, certain substances like alcohol, tobacco, or caffeine-containing products may interact with dyphylline, affect its efficacy, or increase the risk of side effects. It’s best to consult your healthcare professional regarding specific dietary restrictions or considerations. 
• Compliance: Taking dyphylline regularly and as your healthcare professional prescribes is crucial. Missing doses or stopping the medication abruptly may result in inadequate symptom control or other complications. If you have any concerns/experience side effects, discuss them with your healthcare provider before changing your medication regimen. 
• Duration of treatment: The duration of dyphylline treatment varies depending on the individual’s condition and response to therapy. It is key to follow the treatment plan outlined by your healthcare professional and only discontinue the medication with their guidance. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: dyphylline 

Pronounced: [ DYE-fi-lin ] 

Why do we use dyphylline? 

dyphylline is primarily used to manage and treat respiratory conditions, particularly asthma and chronic obstructive pulmonary disease (COPD). Its main uses include: 

• Bronchodilation: dyphylline is a bronchodilator that helps relax and widen the airways, making breathing easier. It relieves symptoms such as wheezing, shortness of breath, and chest tightness associated with asthma and COPD. 
• Asthma: dyphylline may be prescribed for the maintenance treatment of asthma, helping to prevent or reduce the frequency and severity of asthma attacks. 
• Chronic Obstructive Pulmonary Disease (COPD): dyphylline can be used as a maintenance treatment for COPD, including chronic bronchitis and emphysema. It helps to alleviate symptoms and improve airflow in the lungs. 
• Chronic Bronchitis: dyphylline may be used to manage chronic bronchitis, long-term inflammation of the bronchial tubes characterized by a persistent cough and excessive mucus production. 
• Emphysema: dyphylline can be prescribed as part of the treatment plan for emphysema, a condition where the air sacs in lungs are damaged, leading to reduced lung function. 

A healthcare professional should determine the specific use and dosage of dyphylline based on individual patient factors and needs.