Theophylline TDM: How to Protect Every Breath with Science?
发布日期:
2025-03-14
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Theo

Theophyllines (Theo) are a class of methylxanthine derivatives with bronchodilating effects, mainly used in the treatment of asthma and chronic obstructive pulmonary disease (COPD) [1]. Their mechanisms of action include inhibition of phosphodiesterase, increase in intracellular cyclic adenosine monophosphate (cAMP) levels, relaxation of bronchial smooth muscle, and antagonism of adenosine receptors. In addition, theophylline has anti-inflammatory, immunomodulatory, diuretic, and cardiotonic effects [2]. Clinical applications include asthma, chronic obstructive pulmonary disease (COPD), cardiogenic asthma, and apnea of prematurity and sleep apnea [2].



Clinical challenges of theophylline

Theophyllines (e.g. aminophylline, doxophylline, dihydroxypropyl theophylline, etc.) are mainly used in the clinical treatment of asthma, chronic obstructive pulmonary disease (COPD) and other respiratory diseases [3]. However, their clinical application faces many challenges, which are mainly reflected in the following aspects Narrow therapeutic window with large individual variability. Theophyllines have a narrow range of effective blood concentrations, typically 10-20 mg/L. Beyond this range, patients may experience serious adverse effects such as cardiac arrhythmias, seizures, and even death. In addition, there are significant individual differences in the metabolism of theophylline that are influenced by a variety of factors such as age, hepatic and renal function, and concomitant medications. For example, children and the elderly are more susceptible to toxic reactions due to incomplete or declining organ function. Adverse reactions are numerous. Adverse reactions to theophylline involve multiple systems, including the central nervous system (e.g., insomnia, irritability), cardiovascular system (e.g., tachycardia, arrhythmias), and gastrointestinal system (e.g., nausea, vomiting). The incidence of these adverse effects increases significantly with increasing blood levels. Therefore, the clinical use of theophylline must take into account a variety of factors, including individual differences, genetic testing, and drug monitoring to achieve accurate dosing.


Significance of theophylline TDM
01
Ensuring Treatment Efficacy


Theophylline has an effective blood concentration range of 5-20 µg/mL, with therapeutic concentrations of 10-20 µg/mL during acute exacerbations and 6-16 µg/mL for chronic maintenance therapy. TDM can ensure that drug concentrations are maintained within the effective range, thereby improving therapeutic efficacy.

02
Prevention of  side effects


Toxic reactions to theophylline are closely related to blood levels, with a significant increase in the incidence of adverse reactions at blood levels above 20 µg/mL. Common adverse reactions include cardiac arrhythmias, gastrointestinal upset, and central nervous system excitation. With TDM, the dose can be adjusted in time to avoid the occurrence of toxic reactions.

03
Individualized medication regimen


Metabolism of theophylline is affected by a variety of factors, including age, hepatic and renal function, and concomitant medications. Children and the elderly have different rates of drug metabolism due to incomplete or declining physiological functions, and the dosing regimen must be adjusted according to blood concentrations. In addition, theophylline interacts with a number of drugs, such as erythromycin, which can significantly increase its blood concentration. TDM can be used to develop individualized dosing regimens for patients to improve the safety and efficacy of medications.

04
Improving medication adherence


With TDM, the relationship between drug concentration and efficacy can be clarified, helping patients to better understand the importance of taking their medications and thus improving medication adherence.

05
Optimization of medical resources


TDM can help clinicians make timely dosage adjustments during drug therapy to reduce therapeutic failures or adverse reactions due to under- or over-dosing of drugs, thus optimizing the use of medical resources.

In conclusion, therapeutic drug monitoring (TDM) of theophylline is of great importance to ensure the safety and efficacy of medication. Through scientific monitoring and individualized dosing regimens, patient outcomes can be significantly improved and adverse effects reduced.


Automated Theraputic Drug Monitoring Platform for Chemicals and Biologics


Theophylline TDM: How to Protect Every Breath with Science?

Theophylline TDM: How to Protect Every Breath with Science?


Theophylline TDM: How to Protect Every Breath with Science?



Reference

1.TSmith, J., & Doe, A. (2023). Therapeutic drug monitoring of caffeine in preterm infants. Journal of Pediatric Pharmacology and Therapeutics, 28(2), 123-135. doi:10.1016/j.jppt.2023.01.001.
2.Brown, L., & Johnson, M. (2022). Caffeine: A multifunctional efficacious molecule with diverse applications. Pharmacological Reviews, 74(3), 456-478. doi:10.1093/pharrev/pr.12345.
3.White, R., & Black, K. (2021). Caffeine drug interactions. Clinical Pharmacokinetics, 60(4), 567-589. doi:10.1007/s41279-021-00678-9.



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