Sophafyllin

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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 Sophafyllin

Property Description
Active Ingredient Aminophylline (Theophylline ethylenediamine)
Pharmacological Class Xanthine derivative; Bronchodilator
Typical Form/Route Solution for injection (Intravenous/IV)
Manufacturer/Origin Sopharma Ad (Bulgaria/Eastern Europe)
Regulatory Status Prescription Only (Rx)

Sophafyllin is a prescription medication whose active component is aminophylline, a chemical compound known formally as theophylline ethylenediamine. This substance belongs to the pharmacological class of xanthine derivatives, which are clinically recognized for their ability to relax smooth muscles throughout the respiratory tract. This function establishes Sophafyllin as a systemic bronchodilator and respiratory stimulant.

Brand Differentiation

Sophafyllin, manufactured by Sopharma Ad, is typically presented as a solution for injection (ampoules). This formulation is crucial for its use in acute situations, as it allows for prompt intravenous (IV) delivery. The active compound, aminophylline, is a synthetic combination of theophylline and ethylenediamine; the latter component significantly enhances the drug’s solubility, which is necessary for effective IV administration. This feature makes it a primary choice for supportive care during severe respiratory conditions like acute exacerbations of asthma or Chronic Obstructive Pulmonary Disease (COPD). Pharmacological information confirms theophylline's established role in treating these long-term airway obstructive diseases.

Regulatory References

  1. Aminophylline - StatPearls - NCBI Bookshelf
  2. Theophylline - StatPearls - NCBI Bookshelf - NIH

What side effects are possible with Sophafyllin?

Possible Side Effects and Safety Information

The safety profile of Sophafyllin, whose active component is aminophylline, is strictly tied to its concentration-dependent toxicity, as documented in regulatory sources. Adverse reactions, particularly severe ones, significantly increase when the amount of the drug in the bloodstream exceeds a therapeutic threshold, often cited as 20 mu g/mL (FDA, EMA).


Systemic Safety Profile

Adverse reactions are organized into System-Organ Classes (SOC) and typically stem from the drug's systemic stimulatory effects. These effects are classified as Incidence Not Known in frequency for most common reactions, as their occurrence relates directly to serum concentration.

System-Organ Class Examples of Documented Effects
Nervous System Headache, restlessness, insomnia, tremors, seizures
Cardiac System Tachycardia (fast heart rate), palpitations, cardiac arrhythmias
Gastrointestinal Nausea, vomiting, abdominal pain, persistent vomiting
Metabolism & Nutrition Hypokalemia (low potassium), hyperglycemia (high blood sugar)

Serious Adverse Reactions and Restrictions

Regulatory documents highlight several severe adverse reactions, including Intractable Seizures, Ventricular Arrhythmias, and Cardiac Arrest, often linked to toxicity or overly rapid intravenous administration.

Population-Specific Risk: Official labeling identifies subsets of patients with reduced drug clearance, placing them at greater risk of toxicity. These groups include older adults (over 60), patients with liver impairment (e.g., cirrhosis), and those with heart failure. The drug is formally contraindicated in patients with a history of hypersensitivity to theophylline or ethylenediamine.

Overdose and Emergency Response

Overdose and When to Seek Help

The official regulatory description of Sophafyllin (Aminophylline) overdose focuses on serious systemic toxicity. Initial documented manifestations often include persistent nausea and vomiting, tremor, restlessness, and a fast heart rate (tachycardia).

Severe toxicity is officially documented to lead to life-threatening complications involving the Central Nervous System (CNS) and Cardiovascular System (CVS):

Regulatory Focus Documented Manifestation or Outcome
CNS/CVS Severity Seizures, status epilepticus, ventricular arrhythmias.
High-Risk Populations Infants, patients with hepatic impairment.
Antidote Status No specific antidote is known.

Due to the high risk of serious events like seizures and life-threatening cardiac arrhythmias, immediate medical attention or contact with emergency services is explicitly required upon suspicion of overdose. Management is symptomatic and supportive, often requiring hospitalization for intensive monitoring, including continuous ECG monitoring and frequent measurement of serum theophylline concentration. Procedures such as administering activated charcoal and, in severe cases, enhanced drug removal (e.g., hemodialysis) are described to manage the toxicity according to official protocols.

Therapeutic Uses of Sophafyllin

What Sophafyllin Treats: Main Uses and Benefits

This medication is commonly used to help with relief from symptoms associated with obstructive lung diseases.

Sophafyllin is applied in clinical settings that involve acute or unstable symptom patterns, particularly severe asthma and Chronic Obstructive Pulmonary Disease (COPD). It plays a role in managing symptoms that create noticeable interference with functional stability, such as intense wheezing and profound shortness of breath during a crisis. The active component is commonly used to address conditions presenting with acute episodes, including chronic bronchitis and emphysema.

“The therapy is relevant for assisting with maintaining functional stability during difficult episodes where symptoms may cause noticeable physiological strain.”

Beyond chronic conditions, the medication may be relevant in specialized contexts like the symptomatic management of Apnea of Prematurity in infants or addressing paroxysmal dyspnoea associated with acute pulmonary edema. This supportive therapeutic benefit assists with maintaining functional stability when symptoms fluctuate.


Quick Fact: Relevant for Easing Symptoms Related to Acute Breathing Difficulty


Regulatory References

  1. NIH MedlinePlus overview of Aminophylline uses

Eligibility and Restrictions for Use

Contraindications and Restrictions on Use

Sophafyllin's official eligibility profile is strictly defined by regulatory guidelines to prevent severe toxicity and adverse events. The medicine is contraindicated in patients with a known hypersensitivity to any xanthine derivative (such as theophylline or caffeine) or to the component ethylenediamine. Use is also prohibited concurrently with other xanthine medications [1.1, 1.6, 2.1].


Age and Comorbidity-Based Limitations

Eligibility is limited for specific patient groups who face a greater risk of toxicity due to altered drug clearance [1.2, 2.2].

Population Group Official Regulatory Status
Infants under 6 months Not Recommended due to immature metabolism [1.1, 2.1].
Elderly patients (ge 60 years) Use with Caution; may be more sensitive and require monitoring [1.1, 2.2].
Liver Disease / CHF Use with Caution; clearance is significantly decreased, increasing toxicity risk [1.1, 2.2].

Eligibility also requires caution in patients with a history of seizure disorders, active peptic ulcer disease, hyperthyroidism, or sustained acute fever, as these conditions can be exacerbated or reduce drug clearance [1.1, 4.3].


Pregnancy and Lactation Status

  • Pregnancy: Use is generally limited and should only be undertaken if considered clearly needed [1.6].
  • Lactation: The drug is excreted into breast milk and is not recommended for use by breastfeeding mothers due to the potential for mild infant toxicity [1.2, 1.6, 3.2].

What should I know about interactions with other medicines?

Sophafyllin's active ingredient is Theophylline, a medication with a narrow therapeutic index, meaning small changes in its blood level can lead to toxicity or loss of effect. Therefore, co-administration with other products must be managed carefully.

Significant Drug and Substance Interactions

1. Medicines that can increase Sophafyllin levels (Toxicity Risk): Sophafyllin is primarily metabolized (broken down) in the liver by the CYP1A2 enzyme. Medicines that inhibit this enzyme can lead to a rise in Sophafyllin's blood concentration and potential toxicity (e.g., nausea, seizures, cardiac arrhythmia). Key inhibitors include: Cimetidine, Ciprofloxacin, Erythromycin, and Fluvoxamine.

2. Medicines that can decrease Sophafyllin levels (Loss of Efficacy): Medicines that increase the activity of the CYP450 enzymes (inducers) can speed up Sophafyllin's metabolism, causing its blood level to drop. This can result in the loss of its therapeutic effect. Examples include Phenytoin, Carbamazepine, Phenobarbital, and Rifampicin.

3. Other Interactions and Lifestyle Factors:

  • Riociguat: Combination is generally contraindicated due to the risk of severe hypotension.
  • Beta-agonists (e.g., Albuterol): Concurrent use may increase the risk of side effects such as hypokalemia (low potassium).
  • Xanthine-containing products: Consumption of large amounts of caffeine-containing food, beverages, or supplements can lead to additive side effects because caffeine is chemically similar to Theophylline.
  • Smoking: Tobacco smoking is a potent enzyme inducer and increases Sophafyllin's clearance, often requiring a significant dose increase for smokers compared to non-smokers. Changes in smoking habits (starting or quitting) require immediate dose adjustment and monitoring.

Mechanism of Action

The mechanism of Sophafyllin (Aminophylline) is driven by its active component, Theophylline, a multi-target molecule that modulates three distinct biological systems to influence the respiratory and neurological pathways.


Modulation of Airway Enzyme Systems

The primary action involves the non-selective inhibition of Phosphodiesterase (PDE) enzymes, particularly PDE3 and PDE4. This enzyme inhibition increases the concentration of the intracellular messenger cyclic AMP (cAMP), which directly promotes the relaxation of airway smooth muscles. This mechanism results in the dilation of the bronchial passages.


Regulation of Central and Peripheral Neuromodulation

A second key domain is the non-selective antagonism of Adenosine receptors ( A1 and A2B). By blocking these receptors, the drug interferes with the inhibitory action of Adenosine in the central nervous system (CNS), leading to increased central respiratory drive. Peripherally, this action enhances the contractility of the diaphragm muscle.


Suppression of Pro-Inflammatory Gene Transcription

The third domain involves the nucleus, where the drug acts to restore the activity of Histone Deacetylase 2 (HDAC2). This mechanism suppresses the transcription of genes, governed by pathways like NF-kappa B, that are responsible for creating pro-inflammatory mediators. This mechanism results in the downregulation of gene transcription for pro-inflammatory mediators within the airways.

Dosage and Administration Information

How to Use Sophafyllin

Sophafyllin is a prescription medication whose usage is governed by a precise, multi-step intravenous administration protocol, intended only for a controlled clinical setting with continuous supervision. The dosing is strictly individualized and is based on individualized clinical parameters.


Administration Guidelines

Property Instruction
Route of Administration Administered exclusively via Intravenous (IV) infusion or slow IV injection.
Dosing Schedule Therapy begins with a single calculated loading dose (e.g., 6 mg/kg IBW) followed by a continuous maintenance infusion.
Preparation The solution must be diluted in a compatible IV fluid (such as Sodium Chloride 0.9%) prior to infusion.
Procedural Constraint All dosing must be calculated using Ideal Body Weight (IBW), not total body weight.
Infusion Rate Limit The loading dose must be administered slowly, ensuring the rate does not exceed 25 mg per minute.
Prior Use Check The initial loading dose must be omitted or substantially reduced if the patient has received any theophylline-related product within the preceding 24 hours.

Population-Specific Adjustments

Dosage requires continuous monitoring and adjustment based on serum theophylline concentrations, aiming for a defined therapeutic range. Reduced maintenance infusion rates are applied for specific patient groups, including older adults and those with impaired drug clearance due to conditions like congestive heart failure or hepatic dysfunction. Conversely, a higher maintenance rate may be indicated for patients who smoke. The use of this drug is primarily short-term, intended for managing acute episodes until conversion to an oral therapy is feasible.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Sophafyllin

Research evidence for Sophafyllin is derived from studies of its active ingredient, aminophylline, which has been the focus of clinical evaluation in specific acute medical settings. This overview describes what the scientific literature reports, based on authoritative reviews and systematic research. Findings describe group patterns, not personal outcomes, and evidence quality varies across studies.


Evidence for Use in Acute Asthma Exacerbations

Research in children and adults with severe asthma exacerbations explored the addition of aminophylline to established treatments (like inhaled bronchodilators and systemic steroids). Studies monitored lung function changes and outcomes such as hospital stay. In some pediatric trials, research highlighted changes measured in lung function scores over the initial hours following administration. However, when combining data from many trials, findings were mixed concerning major clinical outcomes. Evidence remains limited for reducing the length of time patients spend in the hospital.


Evidence for Use in Acute Exacerbations of COPD

Sophafyllin was evaluated in adults and older adults experiencing flare-ups of Chronic Obstructive Pulmonary Disease (COPD). Studies monitored physiological markers (like blood gas levels) and patient-reported discomfort (dyspnea scores). Research observed in some studies that the drug was associated with modest changes in certain physiological markers and small improvements in dyspnea scores. However, systematic reviews consistently note that the evidence is insufficient to demonstrate a clinical advantage in reducing the length of hospital stay or ICU admission.


Evidence for Use in Apnea of Prematurity (AOP)

The active component of Sophafyllin was studied for its use in preterm infants to manage recurrent breathing pauses (apnea). Research indicates that the drugs in this class may help reduce the number of apneic episodes compared to no treatment. Studies evaluated whether aminophylline and the alternative agent, caffeine, demonstrated similar patterns on respiratory function. However, trials reported that the use of aminophylline was associated with a higher occurrence of temporary cardiac changes compared to caffeine.

What remains uncertain is the drug's long-term profile in this young population, as data are still emerging regarding developmental outcomes years after treatment.

Key Studies & References Aminophylline for acute severe asthma in children over two years receiving inhaled beta2-agonists and systemic corticosteroids

Frequently Asked Questions (FAQ)

Common questions about Sophafyllin (FAQ)

Q: Is Sophafyllin the same type of drug as [Similar Drug Name]?

Sophafyllin belongs to a class of medicines called xanthine derivatives. Official information states it works by modulating three systems, including blocking adenosine receptors and inhibiting PDE enzymes. This multi-target mechanism is different from how many other common respiratory medicines function.

Q: How long does it usually take to notice an effect from Sophafyllin?

Sophafyllin is given directly into a vein (intravenously) only for acute, severe episodes. Due to this method of administration in a clinical setting, its onset of effect in the body is considered rapid.

Q: Can children take Sophafyllin?

Regulatory documents indicate that use in children requires careful monitoring. Infants under 6 months are generally not recommended for treatment due to their immature metabolism. Official information notes that older children may need relatively higher doses than adults because the drug is cleared faster from their bodies.

Q: Are there any long-term effects of taking Sophafyllin?

The official documents describe Sophafyllin as being primarily intended for short-term use to manage acute episodes. The goal is often to stabilize the patient until they can transition to an oral treatment. Therefore, its long-term safety profile is not the main focus of its current regulatory designation for acute care.

Q: What are the most common reasons someone might stop using Sophafyllin?

The treatment is typically stopped when the acute episode has resolved or when the patient is ready to transition to a maintenance medicine taken by mouth. Additionally, the drug may be discontinued under medical supervision if serious adverse reactions occur or if signs of drug toxicity are detected during monitoring.

Q: How is Sophafyllin different from other medicines for the same condition?

The active ingredient in Sophafyllin acts on multiple pathways, which is unique among medications for this condition. Regulatory information defines its action as inhibiting PDE enzymes, blocking Adenosine receptors, and restoring certain anti-inflammatory activity. This combination of effects sets it apart from other single-action respiratory drugs.

Q: Is it possible for Sophafyllin to stop working over time?

The drug's effectiveness can be reduced by certain factors that cause its level in the blood to drop too low. Official documents note that smoking tobacco and taking certain other medicines can speed up the way the body processes Sophafyllin, potentially leading to a loss of therapeutic effect.

Q: Is it common to feel stomach upset when starting Sophafyllin?

According to summaries of clinical data, some of the most commonly reported temporary side effects observed at therapeutic blood levels include gastrointestinal issues such as nausea and vomiting. Headache and insomnia are also frequently reported stimulatory effects.

Q: Do you have to take Sophafyllin at a specific time of day?

No, this medication is a liquid solution administered only by intravenous infusion or slow injection in a controlled clinical setting. It is not a tablet or capsule that a patient would take at home at a specific time of day.

Q: Are there any specific warnings about using Sophafyllin with herbal products?

Official labeling cautions against taking herbal products or supplements that contain xanthine derivatives, which are similar to the active ingredient in Sophafyllin. Combining these products may result in increased stimulatory side effects, such as nervousness or a fast heart rate.

Q: Do regulatory bodies classify Sophafyllin as a high-risk medication?

Regulatory documents emphasize that this drug has a narrow therapeutic index. This means there is only a small difference between the amount of the drug that provides a benefit and the amount that can cause serious toxicity, which is why continuous patient monitoring is required during administration.

Q: Is it true that Sophafyllin can affect my blood pressure?

Official documents state that the drug is associated with changes in the cardiac system, including the potential for tachycardia (fast heart rate) and arrhythmias. Caution is also advised when the drug is used in patients with pre-existing conditions like hypertension.

Q: Is Sophafyllin approved in countries outside the US?

Yes, the active component of Sophafyllin is a globally recognized medicine (aminophylline). The drug is manufactured in Bulgaria and has regulatory status in multiple territories outside the US, including countries that follow the European Medicines Agency (EMA) guidelines.

Q: Is there a generic version of Sophafyllin available?

The active ingredient in Sophafyllin is aminophylline. This substance is widely available from various manufacturers and is often utilized as the generic form for oral tablets and other preparations.

Q: What information about Sophafyllin is included in the official patient leaflet?

Patient information approved by regulatory bodies covers the drug's purpose, the conditions for its intravenous administration, the need for continuous monitoring, potential side effects, and important warnings for specific patient groups. This information ensures patients are fully informed about the treatment protocol.

Q: Are there any specific supplements that interact with Sophafyllin?

The official labeling specifically cautions against supplements that contain high amounts of xanthine derivatives, which are similar to Sophafyllin's active component. Combining these can increase the risk of stimulatory side effects. No other specific interaction risks are listed for non-caffeine-containing supplements.

Q: How long does Sophafyllin stay in your system after stopping it?

The time it takes for the active drug to be cleared from the body varies significantly based on factors like age, whether the person smokes, and other medical conditions. Scientific information reports that the average drug clearance in adults is studied to be around 57 mL/hr/kg.

Q: Is Sophafyllin known to cause any mood changes or anxiety?

Official safety information documents stimulatory effects on the nervous system. These documented effects include restlessness, nervousness, and irritability.

Q: Does Sophafyllin affect fertility?

Non-clinical research, which involves animal studies, has suggested that the active ingredient may impair fertility at very high doses compared to the human therapeutic range. This evidence comes from decreases in reproduction outcomes observed in mice.

Q: Can people with kidney disease safely use Sophafyllin?

Official documents state that use in patients with impaired kidney function requires caution and close monitoring. There is a risk that the drug's byproducts (metabolites) may accumulate in these patients, potentially leading to increased toxicity risk.

Q: Can Sophafyllin be taken with vitamins?

No specific interaction between Sophafyllin and common vitamins (such as A, C, or D) is documented in the official labeling. The official information emphasizes that all concurrent supplements, including vitamins, should be disclosed to the healthcare team.

Q: How does Sophafyllin affect the ability to drive or operate machinery?

Adverse effects on the nervous system, including tremors, headache, and restlessness, are documented in the safety information. The documented effects may influence the ability to safely perform activities that require concentration and coordination.

Q: Does Sophafyllin interact with birth control pills?

Yes, the official label warns of a documented interaction where contraceptive steroids (hormonal birth control pills) can increase the amount of Sophafyllin in the bloodstream. This interaction can raise the risk of drug toxicity, meaning monitoring is necessary when starting or stopping hormonal contraceptives.

Q: What if I experience a rare side effect mentioned in the documentation?

Official guidance stresses the importance of immediate communication with the healthcare team is necessary if a severe or persistent reaction is experienced. Due to the risk of concentration-dependent toxicity, prompt evaluation and management are necessary for all adverse events.

How should Sophafyllin be stored and disposed of?

Official Storage and Disposal Requirements

Sophafyllin must be stored according to regulatory labeling to maintain its efficacy and safety. The product requires storage at controlled room temperature, typically 20 C to 25 C (68 F to 77 F). It is mandatory to protect the medicine from moisture and excessive heat and to avoid freezing the product.

Keep Sophafyllin in its original, tightly closed container and ensure it is stored out of the sight and reach of children.

For disposal, do not place unused or expired Sophafyllin in household trash or flush it down the toilet or drain. Unused medication must be disposed of through an authorized pharmaceutical take-back program or a drug collection box as designated by local regulations.

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

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