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The Contribution of cocoa additive to cigarette smoking addiction

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Page 114 <strong>of</strong> 207 RIVM report 650270002<br />

Tryptamine<br />

after a tryp<strong>to</strong>phan load (28).<br />

Excretion<br />

No data are available for tryptamine excretion after tryptamine loading. Tryptamine is<br />

excreted in the urine after oral loading with L-tryp<strong>to</strong>phan (30 mg/kg body weight).<br />

<strong>The</strong> urinary excretion <strong>of</strong> tryptamine increases immediately after loading and reaches a<br />

maximum in approximately 45 min (29).Tryptamine in the unconjugated form in<br />

urine collected from human volunteers was 82 ± 11 µg/g creatinine (mean ± standard<br />

error <strong>of</strong> the mean) (30).<br />

Kinetic parameters<br />

Intraventricular injection in<strong>to</strong> the rat brain tryptamine resulted in rapid exponential<br />

decrease <strong>of</strong> it in the first 30 min after injection. Tryptamine showed a biphasic<br />

decrease with half-lives <strong>of</strong> 4.7 min (over the 5-10 min period) and 14.1 min (10-30<br />

min) (31). <strong>The</strong> turnover rate is high in the rat brain (38 ng/ g brain tissue/h) (12).<br />

Critical assessment<br />

Little is known about tryptamine pharmacokinetics in man from oral and respira<strong>to</strong>ry<br />

studies on tryptamine. <strong>The</strong> major route <strong>of</strong> catabolism for tryptamine is one <strong>of</strong><br />

enzymatic inactivation.<br />

Conclusion<br />

<strong>The</strong>re are no pharmacokinetic data available after tryptamine respira<strong>to</strong>ry and oral<br />

loading.<br />

TOXICOLOGY<br />

Acute <strong>to</strong>xicity<br />

Human<br />

Tryptamine produces pharmacological effects in man which are similar <strong>to</strong> those<br />

produced by LSD, mescaline, psilocin and other tryptamine derivatives. <strong>The</strong>se<br />

effects include tachycardia, tachypnea, mydriasis, hyperreflexia, behavioral changes<br />

and in man, hallucinations. No details were available on the tryptamine data in that<br />

study (19).<br />

Animal<br />

Tryptamine induced sero<strong>to</strong>nin (5-HT) syndrome (head weaving and hindlimb<br />

abduction) in rats through the 5-HT1A recep<strong>to</strong>r. <strong>The</strong> 5-HT syndrome may also be<br />

associated with the 5-HT1A recep<strong>to</strong>r in mice, as it is in rats (32). However, another<br />

study stated that the sero<strong>to</strong>nin syndrome was attributed <strong>to</strong> the binding <strong>of</strong> tryptamine<br />

<strong>to</strong> 5-HT2 recep<strong>to</strong>rs and subsequent agonistic actions. Intravenous doses <strong>of</strong> 25 mg/kg<br />

<strong>to</strong> mice induced the 5-HT syndrome <strong>of</strong> head weaving and hind limb abduction (33).<br />

<strong>The</strong> behavioural effects <strong>of</strong> intravenously administered tryptamine were examined in<br />

mice. Tryptamine in a dose greater than 15 mg/kg induced distinct head-weaving and<br />

hindlimb abduction. <strong>The</strong>se behavioural syndromes appeared immediately after the<br />

injection and disappeared within 3 min. <strong>The</strong> changes in time course <strong>of</strong> the behaviour<br />

induced by tryptamine were consistent with those <strong>of</strong> the levels <strong>of</strong> tryptamine in the<br />

brain (34).<br />

<strong>The</strong> effects <strong>of</strong> tryptamine on behavior were investigated in mice. Tryptamine at a

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