Also known as 1,3,7-trimethylxanthine, 1-methyltheobromine, 7-methyltheophylline, Anhydrous caffeine, CAF, Cafeína, Caféine, Coffein, Guaranine, Koffein, Mateína, Methyltheobromine, Teina, Thein, Theine, Trimethylxanthine

A methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic and anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. This agent also promotes neurotransmitter release that further stimulates the CNS. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases (PDEs). Inhibition of PDEs raises the intracellular concentration of cyclic AMP (cAMP), activates protein kinase A, and inhibits leukotriene synthesis, which leads to reduced inflammation and innate immunity.

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

Can I take Caffeine while breastfeeding?

Caffeine appears in breastmilk rapidly after maternal ingestion. Fussiness, jitteriness and poor sleep patterns have been reported in the infants of mothers with very high caffeine intakes equivalent to about 10 or more cups of coffee daily. Studies in mothers taking 5 cups of coffee daily found no stimulatory effects on infants 3 weeks of age and older. Some experts feel that a maternal intake limit of 300 mg daily might be a safe level of intake.[1] However, preterm and younger newborn infants metabolize caffeine very slowly and may have serum levels of caffeine and other active caffeine metabolites similar to their mothers’ levels,[1][2][3] so a lower intake level preferable in the mothers of these infants. Other sources of caffeine, such as cola and energy drinks, yerba mate or guarana, will have similar dose-related effects on the breastfed infant. Coffee intake of more than 450 mL daily may decrease breastmilk iron concentrations and result in mild iron deficiency anemia in some breastfed infants.[4]

Drug levels

The half-life of caffeine in late pregnancy is much longer than in nonpregnant women; however, the maternal half-life returns to normal within the first week postpartum.[5] Smokers have more rapid clearance of caffeine and shorter half-lives than nonsmokers because smoking induces CYP1A2. Caffeine clearance is very low in preterm and newborn infants, but reaches adult values by 3 to 5 months of age.[2]

Maternal Levels. Caffeine appears in breastmilk with a peak usually occurring about 1 hour after a dose.[6][7][8] Most studies did not measure active metabolites in milk.

Five women who were 4 months to 1 year postpartum were given a dose of 150 mg of caffeine orally as caffeine sodium benzoate solution 2 hours after breakfast. Average caffeine levels at 30, 60 and 120 minutes after the dose were 1.6, 1.5, and 0.9 mg/L, respectively. One woman also received a 300 mg dose on a separate occasion and her milk caffeine levels were about double those after her 150 mg dose.[9]

Two nursing mothers who were 7 and 13 weeks postpartum ingested tablets containing a total of 128 mg of caffeine. Milk samples were taken over 12 and 48 hours in the 2 women, respectively. Peak milk levels of 1.3 and 1.6 mg/L occurred at 1.5 and 2 hours, respectively.[7]

A mother who drank 3 cups of coffee over a 1-hour period and then coffee at will throughout the day had milk caffeine concentrations ranging from 0.32 to 1.15 mg/L in 8 milk samples taken over a 10.5 hour period.[10]

Fifteen women ingested a caffeine-containing beverage of their choice (coffee or tea) containing caffeine in amounts ranging from 35 to 336 mg. Their breastfed infants ranged from 2 weeks to 9 months of age. Eleven of the women had caffeine detectable in their breastmilk with peak levels ranging from 2.1 to 7.2 mg/L. The 4 mothers with undetectable caffeine (<0.2 mg/L) had ingested less than 100 mg of caffeine. The mean half-life of caffeine in milk was 6.1 hours.[6] Nine nursing mothers ingested 750 mg of caffeine (5 doses of 150 mg) in instant coffee daily for 5 days. Pooled 24-hour milk samples were collected on days 5 and 9 after no caffeine had been taken for 4 days. Caffeine concentration in the mothers’ milk averaged 4.3 mg/L, ranging from undetectable (<0.25 mg/L) to 28.6 mg/L. By day 9, caffeine was undetectable in all milk samples. The authors estimated that at this caffeine intake, infants would receive 0.6 to 0.8 mg/kg daily.[11] Eleven nursing mothers randomly consumed 5 cups of decaffeinated coffee or 5 cups of decaffeinated coffee with a total of 500 mg of added caffeine daily for 5 days in a randomized, double- blinded study. Their infants averaged 47 days (range 22 to 71 days) of age. During a 24-hour collection period on day 5, milk of the women who consumed caffeine contained an average of 3.1 mg/L, which amounted to an average of 2.4 mg or 0.5 mg/kg daily intake for the infants.[12] Six women who were 3.5 to 17 weeks postpartum were given a single oral tablet of caffeine containing 100 mg of caffeine. Ten breastmilk samples from each breast were collected over the next 24 hours. The average peak milk levels from both breasts was 2.5 mg/L at 1 hour after the dose. Caffeine concentrations in milk from both breasts fell with an average half-life of 7.2 hours.[8] Using milk AUC data from 5 of the women, an exclusively breastfed infant would receive about 10% of the weight-adjusted maternal dose. Five nursing mothers who were 6 to 28 weeks postpartum received a single dose of 200 mg of caffeine as tablets. Blood and milk samples were taken over the next 24 hours for measurement of caffeine and 3 active caffeine metabolites, paraxanthine, theobromine, and theophylline. The peak caffeine levels in milk occurred at about 1 hour, but peak metabolite levels in milk occurred later at about 5 to 10 hours for paraxanthine and 10 to 15 hours for theobromine and theophylline. The authors estimated that an exclusively breastfed infant would receive a caffeine dose of 7% and a total xanthine dose of 18% of the maternal weight-adjusted dosage.[3] Infant Levels. Nine infants, aged 14 days to 19 weeks of age had saliva caffeine levels measured after maternal ingestion of 1 cup of coffee. All but 2 were completely breastfed. Among the 7 fully breastfed infants, saliva caffeine levels ranged from 0.21 to 0.75 mg/L between 1 and 6 hours after the maternal ingestion of caffeine.[13]

Fifteen nursing mothers ingested a beverage containing caffeine in amounts ranging from 35 to 336 mg. Caffeine was not detected (<0.2 mg/L) in the urine of any of their infants over the 5-hour collection period that began 2 hours after the maternal caffeine intake.[6]

Effects in breastfed infants

The half-life of caffeine in late pregnancy is much longer than in nonpregnant women; however, the maternal half-life returns to normal within the first week postpartum.[5] Smokers have more rapid clearance of caffeine and shorter half-lives than nonsmokers because smoking induces CYP1A2. Caffeine clearance is very low in preterm and newborn infants, but reaches adult values by 3 to 5 months of age.[2]

Maternal Levels. Caffeine appears in breastmilk with a peak usually occurring about 1 hour after a dose.[6][7][8] Most studies did not measure active metabolites in milk.

Five women who were 4 months to 1 year postpartum were given a dose of 150 mg of caffeine orally as caffeine sodium benzoate solution 2 hours after breakfast. Average caffeine levels at 30, 60 and 120 minutes after the dose were 1.6, 1.5, and 0.9 mg/L, respectively. One woman also received a 300 mg dose on a separate occasion and her milk caffeine levels were about double those after her 150 mg dose.[9]

Two nursing mothers who were 7 and 13 weeks postpartum ingested tablets containing a total of 128 mg of caffeine. Milk samples were taken over 12 and 48 hours in the 2 women, respectively. Peak milk levels of 1.3 and 1.6 mg/L occurred at 1.5 and 2 hours, respectively.[7]

A mother who drank 3 cups of coffee over a 1-hour period and then coffee at will throughout the day had milk caffeine concentrations ranging from 0.32 to 1.15 mg/L in 8 milk samples taken over a 10.5 hour period.[10]

Fifteen women ingested a caffeine-containing beverage of their choice (coffee or tea) containing caffeine in amounts ranging from 35 to 336 mg. Their breastfed infants ranged from 2 weeks to 9 months of age. Eleven of the women had caffeine detectable in their breastmilk with peak levels ranging from 2.1 to 7.2 mg/L. The 4 mothers with undetectable caffeine (<0.2 mg/L) had ingested less than 100 mg of caffeine. The mean half-life of caffeine in milk was 6.1 hours.[6] Nine nursing mothers ingested 750 mg of caffeine (5 doses of 150 mg) in instant coffee daily for 5 days. Pooled 24-hour milk samples were collected on days 5 and 9 after no caffeine had been taken for 4 days. Caffeine concentration in the mothers’ milk averaged 4.3 mg/L, ranging from undetectable (<0.25 mg/L) to 28.6 mg/L. By day 9, caffeine was undetectable in all milk samples. The authors estimated that at this caffeine intake, infants would receive 0.6 to 0.8 mg/kg daily.[11] Eleven nursing mothers randomly consumed 5 cups of decaffeinated coffee or 5 cups of decaffeinated coffee with a total of 500 mg of added caffeine daily for 5 days in a randomized, double- blinded study. Their infants averaged 47 days (range 22 to 71 days) of age. During a 24-hour collection period on day 5, milk of the women who consumed caffeine contained an average of 3.1 mg/L, which amounted to an average of 2.4 mg or 0.5 mg/kg daily intake for the infants.[12] Six women who were 3.5 to 17 weeks postpartum were given a single oral tablet of caffeine containing 100 mg of caffeine. Ten breastmilk samples from each breast were collected over the next 24 hours. The average peak milk levels from both breasts was 2.5 mg/L at 1 hour after the dose. Caffeine concentrations in milk from both breasts fell with an average half-life of 7.2 hours.[8] Using milk AUC data from 5 of the women, an exclusively breastfed infant would receive about 10% of the weight-adjusted maternal dose. Five nursing mothers who were 6 to 28 weeks postpartum received a single dose of 200 mg of caffeine as tablets. Blood and milk samples were taken over the next 24 hours for measurement of caffeine and 3 active caffeine metabolites, paraxanthine, theobromine, and theophylline. The peak caffeine levels in milk occurred at about 1 hour, but peak metabolite levels in milk occurred later at about 5 to 10 hours for paraxanthine and 10 to 15 hours for theobromine and theophylline. The authors estimated that an exclusively breastfed infant would receive a caffeine dose of 7% and a total xanthine dose of 18% of the maternal weight-adjusted dosage.[3] Infant Levels. Nine infants, aged 14 days to 19 weeks of age had saliva caffeine levels measured after maternal ingestion of 1 cup of coffee. All but 2 were completely breastfed. Among the 7 fully breastfed infants, saliva caffeine levels ranged from 0.21 to 0.75 mg/L between 1 and 6 hours after the maternal ingestion of caffeine.[13]

Fifteen nursing mothers ingested a beverage containing caffeine in amounts ranging from 35 to 336 mg. Caffeine was not detected (<0.2 mg/L) in the urine of any of their infants over the 5-hour collection period that began 2 hours after the maternal caffeine intake.[6]

Possible effects on lactation

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

References

1. James J, Lawrence R. Can consuming caffeine while breastfeeding harm your baby? An interview with Ruth Lawrence, PhD. J Caffeine Res. 2011;1:192-4.

2. McNamara PJ, Abbassi M. Neonatal exposure to drugs in breast milk. Pharm Res. 2004;21:555-66. PMID: 15139511

3. Oo CY, Burgio DE, Kuhn RC et al. Pharmacokinetics of caffeine and its demethylated metabolites in lactation: predictions of milk to serum concentration ratios. Pharm Res. 1995;12:313-6. PMID: 7784352

4. Munoz LM, Lonnerdal B, Keen CL, Dewey KG. Coffee consumption as a factor in iron deficiency anemia among pregnant women and their infants in Costa Rica. Am J Clin Nutr. 1988;48:645-51. PMID: 3414579

5. Knutti R, Rothweiler H, Schlatter CH. Effect of pregnancy on the pharmacokinetics of caffeine. Eur J Clin Pharmacol. 1981;21:121-6. PMID: 7341280

6. Berlin CM Jr, Denson HM, Daniel CH, Ward RM. Disposition of dietary caffeine in milk, saliva, and plasma of lactating women. Pediatrics. 1984;73:59-63. PMID: 6691042

7. Findlay JW, DeAngelis RL, Kearney MF et al. Analgesic drugs in breast milk and plasma. Clin Pharmacol Ther. 1981;29:625-33. PMID: 7214793

8. Stavchansky S, Combs A, Sagraves R et al. Pharmacokinetics of caffeine in breast milk and plasma after single oral administration of caffeine to lactating mothers. Biopharm Drug Dispos. 1988;9:285-99. PMID: 3395670

9. Tyrala EE, Dodson WE. Caffeine secretion into breast milk. Arch Dis Child. 1979;54:787-800. PMID: 507903

10. Bailey DN, Welbert RT, Naylor A. A study of salicylate and caffeine excretion in the breast milk of two nursing mothers. J Anal Toxicol. 1982;6:64-8. PMID: 7098450

11. Ryu JE. Caffeine in human milk and in serum of breast-fed infants. Dev Pharmacol Ther. 1985;8:329-37. PMID: 4075932

12. Ryu JE. Effect of maternal caffeine consumption on heart rate and sleep time of breast-fed infants. Dev Pharmacol Ther. 1985;8:355-63. PMID: 4075934

13. Hildebrandt R, Gundert-Remy U. Lack of pharmacological active saliva levels of caffeine in breast-fed infants. Pediatr Pharmacol (New York). 1983;3:237-44. PMID: 6677875

14. Rivera-Calimlim L. Drugs in breast milk. Drug Ther (NY). 1977;7:59-6. PMID: 12336945

15. Clement MI. Personl view: Caffeine and babies. Br Med J. 1989;298:1461.

16. Rustin J. Caffeine and babies. Br Med J. 1989;299:121. Letter.

17. Martin I, Lopez-Vilchez MA, Mur A et al. Neonatal withdrawal syndrome after chronic maternal drinking of mate. Ther Drug Monit. 2007;29:127-9. PMID: 17304161

18. Santos IS, Matijasevich A, Domingues MR. Maternal caffeine consumption and infant nighttime waking: prospective cohort study. Pediatrics. 2012;129:860-8. PMID: 22473365

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 Caffeine molecule

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