Dilatrane

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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 Dilatrane

Quick Facts

Property Description
Active ingredient Choline Theophyllinate (Oxtriphylline)
Form Tablet, Capsule, Syrup, Nebulization Solution
Pharmacological class Xanthine Derivative, Bronchodilator Agent
General purpose Long-term control of restricted airflow
Origin Synthetic Salt

Dilatrane is the trade name for the medication containing the active ingredient Choline Theophyllinate, which is classified as a Bronchodilator Agent belonging to the Xanthine Derivative group. This medication is a synthetic single-entity product utilized for the stable, long-term management of conditions characterized by restricted airflow in the bronchial passages. Its distinction lies in its specialized salt composition and availability across multiple administration routes.

What is Dilatrane and its Pharmacological Class?

Dilatrane's identity is chemically defined by Choline Theophyllinate (INN), also known as Oxtriphylline. This compound is a synthetic salt created by combining the therapeutic component, Theophylline, with Choline. It is classified within the Xanthine Derivative class of Bronchodilator Agents. Its classification as a bronchodilator relates to its primary role in assisting pulmonary function. The choline salt form is specifically prepared to offer improved solubility and gastrointestinal tolerance compared to the basic anhydrous Theophylline, which is a key differentiating feature supporting its reliable systemic absorption.

Composition and Available Forms of Choline Theophyllinate

The composition of this medication consists solely of the active ingredient Choline Theophyllinate as a single-entity product. It is prepared for systemic administration through various dosage forms, notably including tablets, capsules, and an oral solution (syrup). The medication is supplied either in standard forms or as sustained-release preparations, where the drug is engineered for slow and consistent release over an extended duration. The extended-release formulation helps to minimize fluctuations in the drug's concentration in the bloodstream, thereby maintaining steady therapeutic levels.

General Purpose: Why is Dilatrane Used?

The general purpose of Dilatrane is to ease breathing difficulty by promoting the relaxation of the smooth muscle surrounding the air passages. Its action as a bronchodilator helps to widen the airways, counteracting the restrictive narrowing process. This mechanism is primarily utilized in scenarios requiring long-term stabilization of lung function, where maintaining continuous patency of the bronchial passages is critical for routine health management.

What side effects are possible with Dilatrane?

Possible Side Effects and Safety Information

This section outlines the officially documented adverse effects and safety characteristics of Dilatrane (Choline Theophyllinate), based strictly on government regulatory documents.

Adverse effects are often concentration-dependent, meaning their frequency and severity increase significantly when the active ingredient's serum concentration exceeds 20 mu g/ mL, a documented risk in regulatory labeling.


Documented Adverse Reactions and Organ Systems

Adverse reactions are classified by the body system affected, as noted in official regulatory documents:

System-Organ Class Common Adverse Reactions Serious Adverse Reactions
Gastrointestinal Nausea, Vomiting, Abdominal Pain, Diarrhea Severe Toxicity
Nervous System Headache, Restlessness, Insomnia, Tremor Seizures (Convulsions)
Cardiac Tachycardia, Palpitations, Arrhythmias Ventricular Arrhythmias

Safety Restrictions and Population Considerations

The regulatory safety profile includes specific limitations and warnings for certain conditions and populations:

  • Absolute Restrictions: The medication is contraindicated for individuals with a known peptic ulcer, an underlying seizure disorder, or where concurrent use with other xanthine derivatives is involved.
  • Hepatic and Cardiovascular Safety: Caution is advised, and clearance is reduced in patients with impaired liver function or certain cardiovascular conditions (e.g., congestive heart failure), increasing the risk of toxicity.
  • Age and Exposure: Clearance of the active substance is generally slower in the elderly (over 60 years) and neonates. Less serious effects like nausea and restlessness may be transient upon initiation of therapy but persistent reactions suggest elevated concentrations.

Note: Severe and potentially fatal theophylline toxicity is a critical safety consideration, as serious events (such as seizures or ventricular arrhythmias) may occur as the first sign of toxicity.

Overdose and Emergency Response

The official prescribing information for Choline Theophyllinate (Dilatrane) explicitly details the clinical manifestations and required emergency actions in the event of an overdose. Documented initial symptoms may include intractable vomiting, nausea, abdominal pain, restlessness, headache, tremor, and a rapid heart rate (tachycardia). These systemic manifestations can rapidly progress to severe, life-threatening events.

Severe Outcomes and Emergency Response

Overdose is associated with severe or life-threatening outcomes affecting the central nervous system and cardiovascular function, including seizures (convulsions), ventricular arrhythmias, and cardiac arrest. The regulatory labeling mandates that individuals must seek immediate medical attention following any suspected overdose. Emergency services must be contacted immediately if severe manifestations, such as seizures or profound cardiac symptoms, occur.

Management described in regulatory documents is focused on symptomatic and supportive treatment. No specific antidote is known. Hospitalization and continuous monitoring are required, specifically including Electrocardiogram (ECG) monitoring and frequent measurement of serum Theophylline concentration and key electrolytes. The official documents also note that the risk of severe toxicity is increased in the elderly and in patients with known hepatic or cardiac impairment.

Therapeutic Uses of Dilatrane

What Dilatrane Treats: Main Uses and Benefits

Dilatrane (Choline Theophyllinate) is commonly used for managing breathing difficulties associated with chronic lung diseases. The medication is commonly used to help with the long-term stabilization of chronic respiratory diseases, including Bronchial Asthma, Chronic Obstructive Pulmonary Disease (COPD), Chronic Bronchitis, and Emphysema. It is utilized in clinical settings marked by persistent airflow restriction, providing supportive relief from symptoms related to noticeable physiological strain for routine health management.

The medication targets key symptoms of airflow restriction, which include wheezing, persistent shortness of breath (dyspnea), and chest tightness. The primary benefit is to help ease the overall symptom load, supporting general well-being and stability during symptomatic phases.

Quick Fact: Relief for Airflow Restriction

Symptom Domain Key Benefit
Wheezing and Dyspnea Helps ease the overall symptom load; assists with maintaining functional stability
Nocturnal Symptoms May assist in managing symptom recurrence; contributes to improved comfort
Chronic Restriction Supports the long-term stabilization of respiratory conditions

Regulatory References

  1. National Institutes of Health (NIH)

Eligibility and Restrictions for Use

Dilatrane (Choline Theophyllinate) eligibility is strictly defined by regulatory documents, distinguishing between absolute prohibitions and conditional use.

Contraindications: Who Must Not Use Use is contraindicated in patients with a known hypersensitivity or allergy to xanthine derivatives (like Theophylline) and in individuals with active peptic ulcer disease (PUD). Patients with severe coronary artery disease or uncontrolled seizure disorders must also officially avoid this medication.

Conditional Use: Special Populations This medicine requires caution and close monitoring in several populations due to documented reduced drug clearance. This includes older adults (generally over 55 years) and infants under one year of age. Patients with impaired liver function (hepatic impairment) are at risk for toxicity. Caution is also mandatory for those with severe cardiac conditions (e.g., arrhythmias, severe hypertension).

Pregnancy and Lactation During pregnancy, the drug is classified as Category C; clearance significantly decreases in the third trimester, requiring monitoring. For lactation, the drug is excreted in human milk, and official guidance suggests discontinuing either the drug or nursing.

What should I know about interactions with other medicines?

Dilatrane (Choline Theophyllinate) Interactions with other medicines and products are primarily defined by the clearance of its active moiety, Theophylline, through the hepatic CYP enzyme system. All interaction statements are derived from official regulatory documentation.

Interaction Category Regulatory Statement
Contraindicated Combinations The co-administration of Dilatrane with other xanthine-containing preparations is prohibited. The combination with Ephedrine is contraindicated in children.
Pharmacokinetic Alterations Concomitant use with CYP inhibitors like Ciprofloxacin and Enasidenib is documented to increase Theophylline plasma concentrations and the risk of serious adverse reactions. Conversely, CYP inducers such as Rifampicin and Carbamazepine are documented to decrease Theophylline levels by increasing its metabolic clearance.
Pharmacodynamic Effects Theophylline may potentiate the risk of hypokalemia when administered with beta-agonists, corticosteroids, or diuretics. Co-administration has also resulted in documented effects like arrhythmias ( Halothane) and antagonism of sedative effects ( Benzodiazepines).
Non-Drug Substance Interactions Cigarette smoking and marijuana are documented to increase Theophylline clearance. The herbal product St. John's Wort is also documented to reduce blood levels. Specific dietary components, such as charcoal-broiled beef, are officially noted to alter Theophylline clearance.
Timing Rules and Cautions Doses must be separated by at least 4 or 12 hours following the use of other xanthine preparations. Reduced Theophylline clearance is documented in populations including the elderly, patients with cardiac failure, or liver impairment, increasing their susceptibility to adverse interaction outcomes.

Mechanism of Action

Dual Mechanism: PDE Inhibition and Adenosine Antagonism

Dilatrane (Theophylline) exerts its primary mechanism of action through two distinct molecular pathways. First, it functions as a non-selective inhibitor of phosphodiesterase (PDE) enzymes, particularly PDE type III and IV. This inhibition prevents the breakdown of the second messenger cyclic AMP (cAMP), leading to increased intracellular cAMP levels within smooth muscle cells. Second, it acts as a non-selective antagonist of adenosine receptors. This dual action modulates bronchial smooth muscle tone and influences central nervous system activity.


Modulating Inflammatory Gene Expression

Beyond its immediate effects on muscle tone, the drug influences the long-term regulation of cellular processes by affecting gene transcription. This mechanism involves the restoration of activity in Histone Deacetylase 2 (HDAC2), which assists in suppressing the transcription of genes regulated by factors such as NF-kappaB, leading to the suppression of pro-inflammatory protein synthesis within airway cells.


Modulating Respiratory Drive and Muscle Function

The drug's antagonism of adenosine receptors also extends to the respiratory system. By modulating adenosine signaling, the compound acts on the brain's respiratory center and directly influences the contractility of respiratory muscles, including the diaphragm. This results in a modulation of the rate and force of respiratory muscle contraction.

Dosage and Administration Information

Dilatrane (Choline Theophyllinate) is utilized as a long-term oral maintenance therapy for chronic conditions characterized by restricted airflow. The medication is available in both immediate-release (oral solution) and extended-release (tablets or capsules) forms, which dictates the required dosing frequency.


Standard Administration and Dosing

The medicine is typically initiated with a lower starting dose, generally around 300 mg per day (Theophylline equivalent), which may be administered in divided doses if using immediate-release forms. The standard adult maintenance range commonly falls between 400 mg and 600 mg per day, with the total daily dose not usually exceeding the upper limit. Dosing must be taken at the same time each day to maintain consistent blood levels.

Titration and Special Handling

A fundamental principle of use involves slow titration where dose adjustments are implemented only after a minimum of three days. This interval allows the concentration of the drug in the bloodstream to stabilize before making further adjustments. For extended-release forms, the tablets or capsules must be swallowed whole and must not be crushed, broken, or chewed; this is necessary to preserve the intended slow-release characteristic.

Population-Specific Use

Specific administration rules apply to certain patient groups. For older adults (aged ge 60 years), the total daily dose is typically restricted to a maximum of 400 mg due to slower drug processing. For pediatric patients (weighing le 45 kg), the dose is calculated based on body weight. If a dose is missed, it is generally advised to avoid taking a double dose; the patient should take the next scheduled dose as planned.

Recent Clinical Evidence

Dilatrane: Recent Clinical Evidence

Evidence for Use in Chronic Obstructive Pulmonary Disease (COPD)

Research has examined Dilatrane (Choline Theophyllinate) in adults with stable Chronic Obstructive Pulmonary Disease (COPD) through Randomized Controlled Trials (RCTs) and systematic reviews. Studies explored patient response over defined intervals, monitoring objective functional measures, such as air movement in the lungs, and physiological parameters. Research has described patterns related to lung function values following administration and short-term changes in patient-reported outcomes describing perceived discomfort compared to control groups.

What remains uncertain is the full extent of the impact on long-term outcomes beyond the trial periods, as follow-up durations were limited in many studies. Additionally, data for certain subgroups of patients with different degrees of disease severity remain insufficient, and evidence quality varies across studies concerning functional measures like exercise capacity.


Evidence for Use in Bronchial Asthma

The medication was studied for chronic bronchial asthma using short-term to intermediate-term RCTs and comparative studies. Research monitored outcomes such as objective lung function and patient-reported outcomes describing perceived discomfort from daytime and nocturnal symptoms. Trials reported measurements showing differences in lung function parameters over short observation periods, and early research described patterns related to lung function values in the studied populations.

Evidence for Chronic Bronchitis and Emphysema Subgroups

Specific research examined chronic bronchitis and emphysema largely within the context of the broader COPD studies. The evidence for these subgroups often relies on analyses derived from general trial populations, monitoring general measures of airflow restriction. Dedicated research focusing solely on these isolated conditions is not frequently published in recent systematic reviews.


Long-Term Studies and Follow-up Data

Studies have been conducted over various durations, but there is limited information for long-term outcomes that look at the durability of the response over multiple years. Research was evaluated in specific patient groups, including children with chronic asthma and older adults within COPD trials, although data for certain groups remain insufficient. Follow-up durations were limited in many of the key trials.


What is Still Uncertain About Dilatrane Research

The research landscape highlights what is known—and what is still uncertain. Evidence quality varies across studies, and the effect seen in clinical trials may not apply universally, as research does not determine whether an individual will respond similarly. Certainty remains low regarding the long-term impact on disease progression. Furthermore, comparative evidence is lacking in recent trials against other established maintenance therapies, and the research needs further clarification across certain subgroups.

Frequently Asked Questions (FAQ)

Common questions about Dilatrane (FAQ)

Q: What should I do if I accidentally miss a dose?

If a dose is forgotten, official instructions advise taking the next scheduled dose as planned. Regulatory instructions state that a double dose should not be taken to make up for a missed dose. Maintaining consistent timing is key to helping keep the level of the medicine stable in the bloodstream.

Q: What are the most common side effects of Dilatrane?

Regulatory documents state that common adverse reactions are often those with a caffeine-like effect, including nausea, vomiting, headache, restlessness, insomnia, and tremor. The severity and frequency of adverse effects are officially noted to increase significantly when the concentration of the active ingredient exceeds a documented level.

Q: How long does it typically take for Dilatrane to start working?

Dilatrane is officially approved as a long-term maintenance therapy, not as an immediate-relief medicine for sudden breathing issues. Studies indicate that sustained therapeutic improvement usually requires the drug's concentration to be stable in the target range. Because of this, it is utilized for chronic, stable management rather than for a rapid effect.

Q: Is Dilatrane used to treat sudden asthma attacks?

Official product labeling states that Dilatrane (Choline Theophyllinate) is not a rescue medicine and should not be used to treat sudden, acute asthma attacks or bronchospasms. The medication is specifically for the stable, long-term management of chronic breathing conditions.

Q: Are there any specific foods I should avoid while taking this medicine?

Regulatory information notes that certain dietary components, such as charcoal-broiled beef, may change how quickly the medicine is cleared from the body. Official guidance suggests limiting or avoiding foods and beverages containing caffeine (like coffee, tea, and chocolate) because combining them may increase the risk of experiencing caffeine-like side effects such as restlessness or insomnia.

How should Dilatrane be stored and disposed of?

Dilatrane (Choline Theophyllinate) must be stored and handled according to specific conditions defined in regulatory product labeling to maintain its stability and effectiveness.

Storage Conditions

Requirement Official Labeled Condition
Temperature Store at controlled room temperature (20 C to 25 C).
Protection Product must be protected from light and protected from moisture.
Packaging Keep the container tightly closed; some liquid forms require discarding the unused portion after a single use.

All forms of the medicine must be kept out of the sight and reach of children. Avoid exposure to temperatures above 25 C, as this can affect stability in certain containers.

Disposal

Disposal of unused or expired Dilatrane and its container must be carried out in accordance with local, regional, and national regulations. To protect the environment, steps must be taken to avoid improper release of the product into wastewater or chemical run-off.

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

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