What are the potential interactions between theophylline and letrozole (aromatase inhibitor)?

Medical Advisory BoardAll articles are reviewed for accuracy by our Medical Advisory Board
Educational purpose only • Exercise caution as content is pending human review
Article Review Status
Submitted
Under Review
Approved

Last updated: November 14, 2025View editorial policy

Personalize

Help us tailor your experience

Which best describes you? Your choice helps us use language that's most understandable for you.

Drug Interaction Between Theophylline and Letrozole

Direct Answer

There is no documented clinically significant drug interaction between theophylline and letrozole based on available evidence. These medications can be co-administered without specific dose adjustments or enhanced monitoring beyond what is routinely recommended for each drug individually.

Mechanistic Considerations

Letrozole Metabolism and Drug Interactions

  • Letrozole is a nonsteroidal aromatase inhibitor that is generally well-tolerated with minimal drug interaction potential 1
  • The drug has been studied extensively in combination with other agents (including tamoxifen) without evidence of significant metabolic interference 2
  • No CYP450-mediated interactions with theophylline have been reported in clinical trials or post-marketing surveillance 1, 3

Theophylline Interaction Profile

  • Theophylline has well-documented interactions with specific drug classes, particularly macrolide antibiotics (erythromycin), fluoroquinolones (ciprofloxacin), calcium channel blockers (verapamil), and H2-blockers (cimetidine) 4, 5
  • These interactions typically involve CYP1A2 inhibition, leading to elevated theophylline levels and potential toxicity 4
  • Aromatase inhibitors like letrozole are not known to affect CYP1A2 activity, the primary enzyme responsible for theophylline metabolism 1

Clinical Management

Standard Monitoring Approach

  • Continue routine theophylline monitoring based on clinical indication (typically targeting serum levels of 5-15 mcg/mL for chronic therapy)
  • Monitor for letrozole-specific adverse effects including hot flushes, arthralgia, and potential effects on lipid profile and bone mineral density 1, 3
  • No additional theophylline level monitoring is required solely due to letrozole co-administration

Important Caveats

  • Be vigilant for true theophylline-interacting drugs that may be prescribed concurrently, as patients on theophylline are exposed to adversely interacting drugs approximately 17.8% of the time they receive theophylline 5
  • If theophylline toxicity develops (seizures, arrhythmias, gastrointestinal symptoms), investigate other potential drug interactions or dosing errors rather than attributing it to letrozole 4

Patient Population Considerations

  • Both medications are commonly used in postmenopausal women (letrozole for breast cancer, theophylline for respiratory conditions) 6
  • No dose adjustment of either medication is required based on co-administration alone

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

Have a follow-up question?

Our Medical A.I. is used by practicing medical doctors at top research institutions around the world. Ask any follow up question and get world-class guideline-backed answers instantly.