Doxofylline, Discovery, Action, Effective Uses, Dosage, side effects, precautions and 8 Brands

Introduction

Doxofylline is a bronchodilator medication used to treat respiratory conditions such as asthma, chronic bronchitis, and chronic obstructive pulmonary disease (COPD). It’s a member of the xanthine class of drugs, which also includes caffeine and theophylline.

Doxofylline works by relaxing the smooth muscles in the airways, making it easier to breathe. Opening up the airways helps to relieve symptoms such as shortness of breath, wheezing, and coughing, making it a viable therapeutic choice for people with respiratory disorders.

Discovery of Doxofylline

 Doxofylline was indeed first synthesized in the 1970s by a team of scientists at Italfarmaco, an Italian pharmaceutical company, The company was researching new compounds with bronchodilatory activity, and Doxofylline was identified as a potential candidate.

Initial Development

Clinical Trials

Marketing and Availability

Mechanism of action

The mechanism of action of doxofylline includes several pathways that contribute to its bronchodilator effects. Here are the main components:

1. Inhibition of Phosphodiesterase

2. Increase in cAMP Levels

3. Relaxation of Smooth Muscle

4. Anti-Inflammatory Effects

5. Increase in Mucociliary Clearance

Uses of Doxofylline

Doxofylline, a potent bronchodilator medication, is essential for the treatment of a variety of respiratory conditions. Its multifaceted therapeutic profile addresses a spectrum of respiratory ailments, offering relief and restoration to individuals grappling with bronchospasm, inflammation, and impaired lung function. The various medical uses include the following:

Asthma Management:

Doxofylline emerges as a frontline therapy in the battle against asthma, a chronic inflammatory condition characterized by airway hyperresponsiveness and bronchospasm. By dilating the bronchial passages and curbing inflammation, doxofylline alleviates wheezing, dyspnea, and chest tightness, empowering individuals to breathe more freely and reclaim control over their respiratory health.

Chronic Obstructive Pulmonary Disease (COPD):

In the complex landscape of COPD, which includes chronic bronchitis and emphysema, it is a reliable ally in improving lung function and relieving symptoms. By relaxing bronchial smooth muscles and reducing airway inflammation, doxofylline fosters enhanced airflow, facilitating easier breathing and enhancing the quality of life for individuals grappling with this debilitating respiratory condition.

Bronchiectasis Treatment:

Doxofylline extends its therapeutic embrace to individuals afflicted by bronchiectasis, a condition characterized by abnormal bronchial dilation and chronic inflammation. By promoting bronchodilation and mitigating inflammation, doxofylline offers relief from chronic mucus production, recurrent infections, and respiratory distress, fostering a newfound sense of respiratory well-being.

Chronic Bronchitis Relief:

Chronic bronchitis, marked by persistent cough, mucus production, and breathlessness, finds solace in the bronchodilatory effects of it. By relieving bronchospasm and lowering airway inflammation, symptomatic relief, allows individuals to breathe more comfortably and engage in daily activities with greater ease.

Emphysema Treatment:

In the realm of emphysema, characterized by irreversible damage to the lung’s air sacs, or alveoli, it offers a ray of hope. Enhancing bronchial patency and attenuating inflammation, it helps alleviate breathlessness and improve exercise tolerance, empowering individuals to navigate the challenges posed by this progressive respiratory condition.

Acute Bronchitis Management:

Doxofylline can be used to treat acute bronchitis, which is characterized by transient inflammation of the bronchial tubes. By easing bronchospasm and reducing airway inflammation, it offers symptomatic relief, hastening the resolution of symptoms and restoring respiratory comfort.

COPD Exacerbation Control:

Doxofylline emerges as an important drug tool during COPD exacerbations, which are characterized by episodes of worsened symptoms and lung function. By promoting bronchodilation and mitigating inflammation, It helps alleviate acute respiratory distress and facilitates recovery, guiding individuals through turbulent respiratory episodes with greater ease.

Dosage

Doxofylline, a bronchodilator medication, must be dosed carefully to maximize therapeutic benefits while minimizing potential side effects. The appropriate dosage varies depending on the patient’s age, condition, and response to treatment. The following are general dosage guidelines for doxofylline in various contexts.

General Dosage for Adults

• Standard Dose: 200 to 400 mg taken orally two to three times daily.
• Administration: To reduce gastrointestinal discomfort, it is best taken with or after meals.

Dosage for Specific Conditions

1. Asthma: 200 to 400 mg taken orally two to three times daily. Adjustments are made based on the intensity of the condition and the patient’s response.
2. Chronic Obstructive Pulmonary Disease (COPD): 200 to 400 mg taken orally two to three times daily, tailored to the severity of symptoms and lung function.
3. Bronchiectasis: 200 to 400 mg taken orally two to three times daily. The dosage is adjusted based on clinical response and tolerance.
4. Chronic Bronchitis: 200 to 400 mg taken orally two to three times daily. Dosage adjustments is necessary based on symptom severity and patient response.
5. Emphysema: 200 to 400 mg taken orally two to three times daily, with dosage adjustments made according to clinical response.

Pediatric Dosage

• Children: The dosage is usually adjusted according to body weight and specific clinical needs. Typically, the dose ranges from 6 mg/kg/day to 12 mg/kg/day, divided into two or three doses.

Special Populations

• Elderly Patients: Dosage adjustment is necessary due to potential age-related changes in drug metabolism and increased sensitivity to side effects. It is recommended to start at the lower end of the dosing range.
• Patients with Renal or Hepatic Impairment: Due to abnormal drug clearance, careful consideration and potential dosage adjustments are required. Monitoring of drug levels and clinical response is essential.

Dosage Adjustments

• In Case of Side Effects: If adverse effects such as nausea, headache, or gastrointestinal discomfort occur, the dosage may be reduced. Close monitoring is necessary to balance efficacy and tolerability.
• Therapeutic Drug Monitoring: Although therapeutic drug monitoring is not required for all patients, it can be useful in certain situations to ensure optimal drug levels and minimize toxicity.

Administration Tips

• Timing: It should be taken at evenly spaced intervals to maintain consistent drug levels in the bloodstream.
• Food: Taking it with or after meals can help reduce gastrointestinal side effects.

Doxofylline Side Effects

Doxofylline is safe well-tolerated and effective in treating a variety of respiratory conditions, some people will experience Understanding these potential side effects can assist patients and healthcare providers in effectively managing them and achieving a favourable benefit-risk balance.

Common Side Effects

• Gastrointestinal Disturbances: Nausea, vomiting, and stomach pain are common gastrointestinal side effects. Taking it with food may help mitigate these symptoms.
• Headache: Mild to moderate headaches are common and can usually be treated with over-the-counter pain relievers or by themselves.
• Insomnia: Difficulty sleeping or restlessness is experienced, particularly if doxofylline is taken later in the day.

Less Common Side Effects

• Dizziness: Some patients experience dizziness or lightheadedness, especially when standing up quickly.
• Palpitations: Increased heart rate or palpitations can occur, particularly in sensitive individuals or those on higher doses.
• Muscle Cramps: Muscle cramps or spasms are reported, which can be uncomfortable but are typically not severe.

Rare Side Effects

• Allergic Reactions: Although rare, allergic reactions such as rash, itching, swelling, or difficulty breathing require immediate medical attention.
• Severe Gastrointestinal Symptoms: Severe abdominal pain, persistent nausea or vomiting, or blood in stools are rare but warrant prompt medical evaluation.
• Central Nervous System Effects: Rarely, do patients experience anxiety, tremors, or seizures, especially at high doses or with underlying conditions predisposing to these effects.

Doxofylline Precautions

Doxofylline, a bronchodilator medication renowned for its efficacy in managing respiratory conditions, requires careful consideration and adherence to precautions to maximize therapeutic benefits while minimizing potential risks. By heeding these precautions, patients and healthcare providers can foster a safe and effective treatment experience.

Hypersensitivity Reactions

• Allergic Predisposition: Patients with a history of hypersensitivity reactions to doxofylline or xanthine derivatives should exercise caution.
• Immediate Evaluation: Any signs of allergic reactions, such as rash, itching, swelling, or difficulty breathing, warrant immediate medical evaluation.

Cardiovascular Considerations

• Cardiovascular Conditions: Patients with pre-existing cardiovascular conditions, such as arrhythmias or heart failure, should be closely monitored during the therapy.
• Risk Assessment: Healthcare providers should assess the cardiovascular risk profile of patients before initiating treatment and consider alternative therapies if deemed necessary.

Renal and Hepatic Impairment

• Impaired Renal Function: Patients with renal impairment may require dosage adjustments or closer monitoring to avoid drug accumulation and potential toxicity.
• Hepatic Dysfunction: Liver function should be assessed before initiating doxofylline therapy, and dosage adjustments are necessary in patients with hepatic impairment.

Drug Interactions

• Concomitant Medications: It can interact with other medications, potentially altering their efficacy or increasing the risk of side effects.
• Review Medication Regimen: Healthcare providers should conduct a comprehensive review of the patient’s medication regimen to identify potential interactions and adjust dosages as needed.

Pregnancy and Lactation

• Pregnancy: The safety of doxofylline during pregnancy has not been established, and its use should be carefully considered based on the potential risks and benefits.
• Lactation: It is unknown whether doxofylline is excreted in human breast milk, and caution should be exercised when administering it to nursing mothers.

Doxofylline Brands in Pakistan

The list of brands of Doxofylline in Pakistan along with their manufacturers are as follows:

1. Doxofyllne syrup
2. AGOLIX – Hiranis Pharmaceuticals Pvt Ltd
3. BRONAXE – Opal Laboratories (Pvt) Ltd.
4. DOXFREE – EG Pharma
5. OFYLIN – S.J. & G. Fazul Ellahie (Pvt) Ltd.
6. PROFYLLINE – Kaizen Pharmaceuticals Pvt Ltd.
7. SYNSMA – Medisure Laboratories Pakistan (Pvt.) Ltd.
8. THEOZAM – Cirin Pharmaceuticals (Pvt) Ltd.
9. UNIFYLINE – Platinum Pharmaceuticals (Pvt.) Ltd.