COFFEE
Coffea arabica, C. canephora, C. robusta, C. liberica
Synonyms/common names/related substances1
Cafe, caffea, espresso, java, mocha
Indications
Increases mental alertness and performance:2,3 Evidence grade B1
Decreases risk of Parkinson disease:4,5 Evidence grade C
Decreases risk of symptomatic gallbladder Evidence grade C
disease in men:6
Decreases risk of gallstones in women:7 Evidence grade C
Rectal cancer prevention:8 Evidence grade C
Pregnancy
Spontaneous abortion:9,10 Evidence level 1b
A case–control study of 3149 pregnant women reported that serum paraxanthine,
a caffeine metabolite, concentration was higher in the women who had spontaneous
abortions than in the controls.9 Drinking more that six cups of coffee per
day increases the risk of spontaneous abortions and that only extremely high
serum paraxanthine concentrations are associated with spontaneous abortion.9
A case–control study of 1498 pregnant women reported that the consumption
of 375 mg or more caffeine per day during pregnancy may increase the risk of
spontaneous abortion.10
Increased risk of stillbirth:11 Evidence level 1b
A prospective follow-up study on 18 478 singleton pregnancies in women with
valid information about coffee consumption during pregnancy11 reported that
pregnant women who drink eight or more cups of coffee per day have double
the risk of stillbirth, when compared to women who do not drink coffee during
pregnancy.11
Low birthweight infants:12,13 Evidence level 1b
A large prospective study on 2291 mothers reported that women consuming more
than 600 mg of caffeine per day are at greater risk for having low birthweight
infants.13 A prospective study on 63 women reported that pregnant non-smokers
consuming caffeine more than 300 mg/day had statistically significant lower
weights of newborns and placentas (p 0.05).12
72 Herbal medicines
Teratogenic compounds:14–17 Evidence level 3
Elevated caffeine intake causes histopathologically teratogenic effects on newborn
rat cornea.14 A study on the effects of coffee during pregnancy on mice
reported long-term teratopharmacologic and behavioral alterations in the offspring
of pregnant mice that consumed coffee.15 A similar study on mice
reported teratogenic effects associated with coffee ingestion during pregnancy.17
A review study, however, reported that when caffeine is administered in
fractioned quantities during the day, as it is the case with human caffeine intake,
caffeine is no longer a teratogen in animals.18
Impairs trace mineral absorption in fetus:19 Evidence level 3
A study on the effect of coffee consumption on pregnancy and lactation in
mice19 reported that maternal coffee intake may impair mobilization of trace
elements from liver reserves in early life and that this may result in reduced
hemoglobin synthesis.19
Harmful to the fetus:20 Evidence level 4
Crosses the placenta:20 Evidence level 4
A compendium on the safety of drugs in pregnancy and lactation reported that
over three cups of coffee a day (300 mg of caffeine) may be harmful to the
fetus.20 The compendium also reported that caffeine crosses the human placenta
where fetal blood and tissue levels are similar to maternal concentrations.20
Three cups of coffee throughout the day – Evidence level 4
possibly safe:21,22
A drug compendium and a review study reported that three cups of coffee
(approximately 300 mg of caffeine) consumed throughout the day seems safe
during pregnancy.21,22
Estrogenic:23 Evidence level 4
A review article on the potential value of plants as sources of anti-fertility
agents reported that coffee has estrogenic activity.23
Lactation
Teratogenic compounds:14–17 Evidence level 3
Two studies reported teratogenic and behavioral alterations in animals whose
mothers were fed coffee.14,15 A similar study on mice reported teratogenic effects
associated with coffee ingestion during pregnancy.17 Since caffeine appears in
breast milk at half the concentration as in the mother’s plasma, newborns may
Herbal medicines 73
be exposed to teratogenic compounds.24 A review study, however, reported that
when caffeine is administered in fractioned quantities during the day, as it is the
case with human caffeine intake, caffeine is no longer a teratogen in animals.18
Impairs trace mineral absorption in newborn:19 Evidence level 3
A study on the effects of coffee consumption on pregnancy and lactation in
mice reported that maternal coffee intake may impair mobilization of trace
elements from liver reserves in early life and that this may result in reduced
hemoglobin synthesis.19
May cause sleeping disorders:25 Evidence level 4
A compendium on herbal medicine reported that nursing mothers who consume
caffeine may have infants with sleeping disorders.25
Stimulates breast milk production:22 Evidence level 4
A review study reported that coffee consumption stimulates breast milk production
in women and that it does not change breast milk composition.22
Contraindications
Cardiac problems16
Kidney disease16
Hyperthyroidism16
Caution
People who have a predisposition to convulsion or anxiety should not drink
more than five cups or 500 mg of caffeine per day.16
Toxic constituents
Methylxanthine alkaloid: caffeine16
Polyphenolic acid: chlorogenic acid16
Caffeol1
Diterpenes1
Toxicity
● Toxic dose of caffeine: 1 g16
● Lethal dose of caffeine: 10 g (adult) and 5.3 g (child)16,26
Pharmacology
● Caffeine is a powerful stimulant of the central nervous system, respiration,
and skeletal muscles.16,26
● Caffeine causes cardiac stimulation, coronary dilation, smooth muscle relaxation,
increases blood pressure, increases heart rate and contractility, and
diuresis.1,26,27
74 Herbal medicines
● Coffee stimulates gastric secretions.28
● Caffeine crosses the human placenta where fetal blood and tissue levels are
similar to maternal concentrations.20
● Chlorogenic acid, a constituent in coffee, is reported to have stimulant,
diuretic, choleretic properties and allergenic properties.26,29
● Chlorogenic acid may raise homocysteine levels.30
● Cafestol, a diterpene in unfiltered coffee, was shown to raise plasma
triacylglycerol levels in humans.31
● Caffeine has anti-platelet activity.32,33
Drug interactions
Acetaminophen (paracetamol)34
Alendronate35
Anti-coagulant/anti-platelet drugs32,33
Anti-diabetic drugs34
Aspirin32,33,36
Benzodiazepines35
b-Adrenergic agonists37
Cimetidine35
Clozapine38,39
Central nervous system stimulants38,40
Disulfiram37
Ephedrine34,41
Ergotamine37
Estrogen42
Lithium43,44
Mexiletine35
Monoamine oxidase inhibitors34
Oral contraceptives35
Phenylpropanolamine35
Quinolones45–47
Riluzole35
Terbinafine35
Theophylline35
Verapamil35
Part used16
Dried ripe seed
References
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Herbal medicines 75
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Giovannucci E. A prospective study of coffee consumption and the risk of
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abortion. Acta Obstet Gynecol Scand 2003; 82:182–188.
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76 Herbal medicines
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acid, present in coffee, or of black tea increases plasma total homocysteine
concentrations in humans. Am J Clin Nutr 2001; 73:532–538.
31. de Roos B, Caslake MJ, Stalenhoef A et al. The coffee diterpene cafestol increases
plasma triacylglycerol by increasing the production rate of large VLDL
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38. Hagg S, Spigset O, Mjorndal T, Dahlqvist R. Effect of caffeine on clozapine pharmacokinetics
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44. Jefferson JW. Lithium tremor and caffeine intake: two cases of drinking less and
shaking more. J Clin Psychiatry 1988; 49:72–73.
45. Harder S, Fuhr U, Staib AH, Wolff T. Ciprofloxacin-caffeine: a drug interaction
established using in vivo and in vitro investigations. Am J Med 1989; 87:89S–91S.
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