Also known as 1,3-Dimethylxanthine Monohydrate, 1,3-dimethylxanthine, Constant-T, Elixophyllin, LaBID, Respbid, Slo-Phyllin, Slo-bid, Somophyllin-CRT, Somophyllin-T, T-Phyl, Theo-24, Theobid Duracap, Theochron, Theophyllin, Theophylline Monohydrate, Theophylline anhydrous, Theophylline, anhydrous, Uniphyl

A natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm. (NCI04)

Originator: NCI Thesaurus | Source: The website of the National Cancer Institute (http://www.cancer.gov)

Can I take Theophylline while breastfeeding?

An expert panel considers use of theophylline to be acceptable during breastfeeding.[1] Maternal theophylline use may occasionally cause stimulation and irritability and fretful sleep in infants. Newborn and especially preterm infants are most likely to be affected because of their slow elimination and low serum protein binding of theophylline. There is no need to avoid theophylline products; however, keep maternal serum concentrations in the lower part of the therapeutic range and monitor the infant for signs of theophylline side effects. Infant serum theophylline concentrations can help to determine if signs of agitation are due to theophylline. Avoiding breastfeeding for an 2 hours after intravenous or 4 hours after an immediate-release oral theophylline product can decrease the dose received by the breastfed infant. When theophylline is given as an oral sustained-release product, timing of nursing with respect to the dose is of little or no benefit.

Drug levels

Maternal Levels. Theophylline rapidly equilibrates between plasma and milk. Peak milk levels occur 1 to 3 hours after oral ingestion of immediate-release products and almost immediately after intravenous administration. Milk levels parallel serum levels closely and average about 70% of simultaneous maternal serum levels.[2][3] Assuming that each 1 mg/kg of maternal theophylline increases her serum level by 2 mg/L, an exclusively breastfed infant would receive about 21% of the maternal weight-adjusted dosage of theophylline or 17% of the maternal dosage of aminophyllline.

Infant Levels. Theophylline is found in the serum of breastfed infants.[4] In newborn infants with typical theophylline clearance rates, infant serum levels are expected to be between 1 and 4 mg/L with a maternal serum level in the therapeutic range of 10 to 20 mg/L.[2] Infant serum levels might occasionally accumulate to therapeutic levels in infants with slow clearance rates of the drug.[5]

Effects in breastfed infants

Maternal Levels. Theophylline rapidly equilibrates between plasma and milk. Peak milk levels occur 1 to 3 hours after oral ingestion of immediate-release products and almost immediately after intravenous administration. Milk levels parallel serum levels closely and average about 70% of simultaneous maternal serum levels.[2][3] Assuming that each 1 mg/kg of maternal theophylline increases her serum level by 2 mg/L, an exclusively breastfed infant would receive about 21% of the maternal weight-adjusted dosage of theophylline or 17% of the maternal dosage of aminophyllline.

Infant Levels. Theophylline is found in the serum of breastfed infants.[4] In newborn infants with typical theophylline clearance rates, infant serum levels are expected to be between 1 and 4 mg/L with a maternal serum level in the therapeutic range of 10 to 20 mg/L.[2] Infant serum levels might occasionally accumulate to therapeutic levels in infants with slow clearance rates of the drug.[5]

Possible effects on lactation

Relevant published information was not found as of the revision date.

Alternate drugs to consider

Terbutaline

References

1. National Heart, Lung, and Blood Institute, National Asthma Education and Prevention Program Asthma and Pregnancy Working Group. NAEPP expert panel report. Managing asthma during pregnancy: recommendations for pharmacologic treatment-2004 update. 2004;1-57.

2. Stec GP, Greenberger P, Ruo TI et al. Kinetics of theophylline transfer to breast milk. Clin Pharmacol Ther. 1980;28:404-8. PMID: 7408400

3. Yurchak AM, Jusko WJ. Theophylline secretion into breast milk. Pediatrics. 1976;57:518-25. PMID: 1264548

4. Gardner MJ, Schatz M, Cousins L et al. Longitudinal effects of pregnancy on the pharmacokinetics of theophylline. Eur J Clin Pharmacol. 1987;31:289-95. PMID: 3595701

5. Reinhardt D, Richter O, Brandenburg G. [Pharmacokinetics of drugs from the breast-feeding mother passing into the body of the infant, using theophylline as an example]. Monatsschr Kinderheilkd. 1983;131:66-70. PMID: 6843559

Last Revision Date

20130907

Disclaimer:Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

Source: LactMed – National Library of Medicine (NLM)

3D Model of the Theophylline molecule

MolView – data visualization platform