Theofar SR

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Theofar SR

Property Description
Active Ingredient Choline Theophyllinate (Oxtriphylline)
Form Sustained-Release (SR) Tablet (Oral formulation)
Pharmacological Class Bronchodilator / Methylxanthine
Common Use Improving breathing in chronic respiratory conditions
Origin Synthetic derivative of Theophylline

What Type of Medicine is Theofar SR?

Theofar SR is a prescription-only medicine classified as a bronchodilator that contains the active ingredient Choline Theophyllinate, also known as oxtriphylline. This substance is a synthetic derivative belonging to the methylxanthine class, which is a foundational group of agents in respiratory pharmacology. The efficacy of methylxanthines in providing long-term stabilization of respiratory function is recognized for chronic obstructive disorders. The drug is fundamentally designed to act on the airways in the lungs, where its core purpose is to relax the bronchial smooth muscles, thereby improving the flow of air into and out of the lungs.


Understanding the Sustained-Release (SR) Formulation

The SR in Theofar SR stands for Sustained-Release, meaning it is a modified-release oral formulation taken by mouth. This specialized dosage form is engineered to ensure that the Choline Theophyllinate is released slowly and steadily from the tablet matrix into the body over many hours. This mechanism is key because it maintains a consistent concentration of the active ingredient in the bloodstream, which is essential for providing continuous, reliable support for patients with chronic respiratory issues and avoiding the large fluctuations associated with immediate-release forms.


Choline Theophyllinate: General Therapeutic Purpose

The general therapeutic purpose of this bronchodilator is to ease the physical difficulty of breathing by reducing resistance in the respiratory tract. For example, it is typically used as a foundational maintenance therapy for patients experiencing persistent airway narrowing, which is a common characteristic of conditions managed by respiratory specialists. This chemical family serves as a core agent for airway disorders. The ultimate goal is to provide fundamental relief from persistent symptoms such as wheezing, chest tightness, and shortness of breath that restrict normal, effortless respiration.

What side effects are possible with Theofar SR?

The safety profile of Theofar SR (Choline Theophyllinate) is defined by officially documented adverse reactions, which are highly dependent on the medicine’s concentration in the bloodstream. The frequency and severity of side effects are noted in regulatory documents as increasing significantly at serum concentrations above 20 mu g/mL.


Documented Adverse Reactions by System

Adverse reactions are formally categorized by the physiological systems they affect, according to regulatory standards:

  • Nervous System Disorders: Common effects include headache, tremors, restlessness, and insomnia. Severe, clinically significant events, such as convulsions (seizures), are officially documented as serious adverse reactions

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  • Gastrointestinal Disorders: Effects frequently documented as early signs of toxicity include nausea, vomiting, and epigastric pain.
  • Cardiac Disorders: Adverse cardiovascular effects include palpitations, tachycardia (fast heart rate), and severe ventricular arrhythmias (irregular heart rhythms)

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Population-Specific Safety Considerations

Regulatory information requires particular caution for certain patient groups:

  • Older Adults: Individuals over 60 years may exhibit greater sensitivity to the effects and typically have reduced drug clearance.
  • Infants: Clearance is significantly reduced in infants, especially those under one year of age, increasing the risk of serious adverse effects.
  • Hepatic Impairment: Patients with liver disease (e.g., cirrhosis) have markedly reduced clearance of the medicine.

Safety Constraints and Monitoring

Conditions that reduce the medicine’s clearance, such as fever (ge 39 C), severe infection, or heart failure, are documented as increasing the risk of toxicity. For long-term therapy, the official label requires periodic monitoring of the serum theophylline concentration to maintain safety within the therapeutic range.

Overdose and Emergency Response

Overdose and When to Seek Help

Overdose with Theofar SR (theophylline) is a serious medical emergency that requires immediate attention. The overall profile of overdose is characterized by severe toxicity affecting the neurological and cardiovascular systems.

Documented Overdose Presentations

Initial signs of overdose often include vomiting (which may contain blood), tremor, anxiety, and tachycardia (rapid heart rate). Due to the sustained-release nature of Theofar SR, severe symptoms may be delayed 12 to 16 hours or more following ingestion, masking the true severity of the exposure.

Severe toxicity involves life-threatening events such as ventricular arrhythmias (serious heart rhythm disturbances), severe hypotension (low blood pressure), and seizures that may be difficult to control with standard treatments. These severe manifestations can lead to cardiac arrest or death.

When to Seek Immediate Medical Help

Immediate medical help must be sought right away following any suspected overdose of Theofar SR, regardless of how the person feels. This urgency is necessary because severe complications are known to occur after a significant delay. The risk of life-threatening events, including seizures and serious arrhythmias, remains high until medical management is initiated.

Acute overdoses of more than 50 mg/kg are potentially associated with severe toxicity, and very young infants and elderly patients are particularly susceptible to chronic intoxication at lower exposure levels. Contact emergency services or poison control immediately and be ready to provide details about the medicine name, time of ingestion, and the amount swallowed.

Therapeutic Uses of Theofar SR

What Theofar SR Treats: Main Uses and Benefits

Theofar SR (Theophylline Sustained-Release) may offer supportive symptomatic relief primarily within the domain of chronic respiratory conditions. It is used as maintenance therapy to help manage and ease the burden of symptoms associated with compromised airflow. The medication is applied in managing distressing manifestations such as wheezing, shortness of breath, and chest tightness associated with lung diseases.


Key Therapeutic Focus

Theofar SR is commonly used across conditions characterized by periods of heightened symptoms, relevant for chronic obstructive conditions like chronic bronchitis and emphysema. It is applied in addressing symptom clusters that may become intense or disruptive, helping patients cope more steadily with difficult episodes. Use of this medication may support the patient during difficult episodes by helping ease symptom load and assists with maintaining functional stability when symptoms become temporarily overwhelming.

“The sustained-release formulation is commonly used to help with easing the overall symptom burden of chronic conditions.”

Quick Fact: Addresses Symptoms of Persistent Breathing Strain


Role in Symptom Management

The sustained-release formulation is applied across domains where continuous, round-the-clock support for symptom management is needed. It helps to address underlying symptom patterns that interfere with routine activities. This continuous relief may assist with easing the overall symptom burden of chronic conditions, supporting general well-being during symptomatic periods.

Regulatory References

  1. NIH MedlinePlus Drug Information

Eligibility and Restrictions for Use

Official Eligibility Rules for Theofar SR

Regulatory documents define specific populations allowed to use Theofar SR (Choline Theophyllinate sustained release), as well as groups for whom use is strictly contraindicated or requires restriction. This eligibility is based on official government prescribing information.


Contraindicated Populations (Must Not Use):

  • Patients with known hypersensitivity to xanthines (including Theofar SR's active ingredient) or any components.
  • Individuals with active peptic ulcer disease or a history of recent ulceration.
  • Patients with Coronary Artery Disease where heart stimulation is deemed harmful.

Age and Conditional Use Restrictions:

Population Group Regulatory Status
Children under 12 years Not Recommended (Use not established for some sustained-release forms).
Older Adults (>60 years) Use with Caution (Due to slower drug clearance and increased sensitivity).
Hepatic or Severe Cardiac Impairment Use with Caution (Due to decreased clearance; requires monitoring).
Pregnancy and Lactation Use is Conditional/Restricted; the drug is excreted into breast milk and is classified as FDA Category C.

Eligibility also requires caution for patients with a history of seizure disorders, hyperthyroidism, or persistent high fever, as these conditions may affect drug safety or clearance.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documents identify several classes of medicinal products and specific drugs that interact with Theofar SR, primarily by affecting its concentrations in the body. These pharmacokinetic interactions are categorized based on their mechanism, which involves specific metabolizing enzymes and drug transporters.

Co-administration with strong enzyme inducers is a critical restriction. Official labeling advises against using Theofar SR with agents such as Rifampin, as these drugs are expected to significantly decrease the level of Theofar SR in the bloodstream. This reduction in exposure may lead to a loss of the medication's intended effect.

Conversely, drugs classified as strong enzyme inhibitors or P-glycoprotein (P-gp) inhibitors are known to increase Theofar SR exposure. Specific examples include the antifungal agent Ketoconazole. The combination with these inhibitors requires close monitoring and possible dosage modifications to manage the elevated concentrations, which could increase the potential for effects related to the drug's activity.

Additionally, Theofar SR may influence the exposure of other medicinal products. It has been documented to increase the plasma concentration of other drugs that are substrates of the P-gp transporter. This complex interaction profile mandates that healthcare providers carefully review all concurrent medications and manage therapy according to official constraints to ensure safe use.

Mechanism of Action

Enzyme-Mediated Bronchial Lumen Dilation

The primary mechanism involves the non-selective inhibition of Phosphodiesterase (PDE) enzymes ( PDE3 and PDE4) in bronchial smooth muscle. By blocking PDE, the drug prevents the hydrolysis of the secondary messenger cyclic adenosine monophosphate ( cAMP), leading to its cellular accumulation. This cascade initiates a reduction in cellular calcium flux, which results in the relaxation of the smooth muscle tissue and induces a reduction in the resistance to airflow.


Receptor Antagonism and Respiratory System Modulation

The drug acts as an antagonist against Adenosine Receptors ( A1 and A2 B), countering the bronchoconstrictive signal mediated by endogenous adenosine. This antagonism contributes to the maintenance of reduced smooth muscle tone and modulates the sensitivity of the medullary respiratory center in the CNS via A1 receptor effects.


Modulation of Inflammatory Gene Pathways

At sustained concentrations, the drug modulates the enzyme Histone Deacetylase ( HDAC2) and inhibits the NF-kappa B transcription factor. This action contributes to the restoration of HDAC2 function, thereby increasing the suppression of pro-inflammatory gene expression (e.g., cytokine synthesis). This effect alters inflammatory signaling and decreases the production of pro-inflammatory mediators within the respiratory tract.

Dosage and Administration Information

How to Use Theofar SR

Theofar SR, which contains Choline Theophyllinate in a sustained-release form, is strictly administered via the oral route as a high-level maintenance strategy for chronic respiratory conditions. It is not indicated for use in reversing sudden or acute breathing problems. The administration pattern is structured to maintain a constant level of the active ingredient over a 12-hour or 24-hour period, depending on the specific extended-release formulation used.


Official Dosing and Administration Principles

Specific parameters for proper use include:

  • Frequency and Timing: The medicine is typically taken once daily (q24h) or twice daily (q12h) to maintain round-the-clock support. It may be ingested with or without food.
  • Standard Dosing: The general initial adult dose ranges from 300 mg to 400 mg per day, with a usual maintenance range between 400 mg and 600 mg per day in otherwise healthy adults. Dose calculations are often based on ideal body weight.
  • Dose Titration: Any required dose adjustment must be done conservatively, in intervals of no less than three days, allowing the body to reach a stable state.

Administration Constraints and Adjustments

The sustained-release nature of Theofar SR dictates procedural constraints. The tablets must be swallowed whole and not broken, crushed, or chewed; altering the tablet can disrupt the intended slow-release mechanism.

Furthermore, specific high-level adjustments are required for certain populations. The maximum dose for older adults (over 60 years) is typically limited to 400 mg per day. Similarly, patients with risk factors for impaired drug clearance, such as liver disease or congestive heart failure, require a dose reduction.

Recent Clinical Evidence

Research evidence / Overview of studies for Theofar SR

Evidence in Chronic Respiratory Conditions (COPD and Asthma)

Theophylline, the active component of Theofar SR, was evaluated in the context of Chronic Obstructive Pulmonary Disease (COPD) and Chronic Asthma. Research has included Randomized Controlled Trials (RCTs) and Meta-analyses to examine how symptoms change over time and to monitor physiological strain. Studies primarily focused on objective measures of lung function, such as how much air a person can exhale in one second (FEV1), and patient-reported outcomes describing perceived discomfort.

Findings describe patterns observed in the studies where lung function measurements were monitored for changes. Research explored whether it was associated with patterns when used as an add-on therapy to existing inhaled treatments.


Long-Term Research and Study Limitations

Research examined the effects over different defined time intervals, ranging from short crossover studies to long-term observational cohorts. The research focused on the sustained nature of observed patterns, but certainty remains low for many of the most important long-term clinical endpoints. For instance, data show patterns related to symptom scores reported by patients, but findings were mixed regarding major outcomes like the frequency of severe COPD flare-ups or hospitalizations.

Evidence in Special Populations and Uncertainty

The study populations have included older adults and children/adolescents with chronic asthma, where research examined outcomes related to systemic or functional imbalance. However, the data for certain groups remain insufficient when it comes to long-term follow-up. The comparative evidence is lacking against many newer, inhaled bronchodilators, and long-term effects are not fully established for certain critical endpoints. Findings were mixed across large observational data sets when assessing the association with all-cause mortality.

How should Theofar SR be stored and disposed of?

How to Store and Dispose of Theofar SR

Official regulatory guidance dictates specific conditions for storing Theofar SR (Theophylline Extended-Release) to maintain its labeled quality and stability.


Storage Requirements

Condition Requirement
Temperature Store at controlled room temperature, 20 C to 25 C (68 F to 77 F).
Protection Keep the container tightly closed and protect the tablets from light and moisture.
Child Safety The medication must be kept out of the sight and reach of children and pets.

Disposal Instructions

Disposal of unused or expired Theofar SR must be carried out according to local regulations. The preferred method is typically an authorized drug take-back program. The medication must not be flushed down a toilet or disposed of in wastewater unless specifically instructed by the regulatory documents for the product.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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