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Fluids Hypertension Syndromes: Migraines, Headaches, Normal ...

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<strong>Fluids</strong> <strong>Hypertension</strong> <strong>Syndromes</strong> – Dr. Leonardo Izecksohn – page 292<br />

“Emulsion with Siloxanetriol alginate caffeine was considered more indicated to promote the lipolytic<br />

action on fatty tissue, acting as a complement to treat cellulite.” (Velasco M V, and others).<br />

XVII- 49 -To enhance seizure duration in electroconvulsive therapy.<br />

XVII- 50 -To determine the enzymatic capacity for its degradation and elimination by the patient,<br />

together with other intoxicants.<br />

“Cytochrome P4501A2 (CYP1A2) and N-acetyltransferase 2 (NAT2) are key enzymes in the metabolism<br />

of caffeine. Gluthatione S-transferase alpha1 may also be active in the metabolism of caffeine.”<br />

(Bech B H, and others).<br />

Individuals who are homozygous for the Cytochrome P4501A2*1A allele are "rapid" caffeine metabolizers,<br />

whereas carriers of the variant Cytochrome P4501A2*1F are "slow" caffeine metabolizers,<br />

ascribed to differences in the activities of the arylamine acetylating enzymes (isozymic N-acetyltransferase<br />

variants) of the liver, intestinal mucosa and other tissues. The acetylator status is determined by<br />

measuring the peak height ratio of two urinary caffeine metabolites, 5-acetylamino-6-formylamino-3methyluracil<br />

and 1-methylxanthine, one to four hours after drinking a strong cup of coffee.<br />

The classification of the patient as slow or rapid acetylator has statistical correlations with many diseases.<br />

“The slow acetylator (N-acetyltransferase phenotype) status is related with:<br />

Increased risk of certain side effects in slow acetylators treated with isoniazid (particularly peripheral<br />

neuropathies and lupus erythematosus).<br />

Hypersensibility reactions with sulfonamides (including Lyell and Stevens-Johnson syndromes),<br />

Poor tolerance to sulfasalazine and dapsone.<br />

Risk of developing primitive liver cancer.<br />

Predisposition to mesothelioma in subjects exposed to asbestos.<br />

Predisposition to atopic diseases.<br />

Increased frequency of Parkinson's disease.<br />

The fast acetylator status is related with:<br />

Myelotoxicity induced by amonafide.<br />

Increased risk of nephropathy on non-smoking type 1 diabetics.” (Furet Y, and others).<br />

“Significant differences in the proportion of rapid acetylators were observed between type 1 (53.6%)<br />

and type 2 (33.7%) diabetics, and between the control group (26%).” (el-Yazigi A, and others).<br />

“Women with slow N-acetyltransferase 2 (NAT2) and rapid cytochrome P450 1A2 (CYP1A2) activity<br />

were at highest risk relative to women with rapid NAT2 and slow Cytochrome P4501A2 activity, for<br />

lung adenocarcinoma.” (Seow A, and others).<br />

“Cytochrome P450 (CYP1A2) enzyme activity was determined in healthy Swedish and Korean subjects,<br />

on the basis of the 4-h plasma paraxanthine/caffeine ratio. The mean ratio was 1.54-fold higher in<br />

Swedes than in Koreans. Smokers had a significantly higher ratio (higher CYP1A2 activity) than nonsmokers,<br />

while Swedish oral contraceptive users had a significantly lower ratio than non-users.<br />

Koreans displayed a significantly lower mean ratio than Swedes having the same CYP1A2 genotype,<br />

smoking habit and oral contraceptive use. None of the investigated CYP1A2 haplotypes are critical in<br />

inducing variations in enzyme activity, with the exception of CYP1A2*1F.” (Ghotbi R, and others).<br />

“Daily consumption of at least three cups of coffee significantly increased Cytochrome P450 1A2 enzyme<br />

activity in both Serbs (P = 0.0002) and Swedes…Significantly higher plasma paraxanthine/caffeine<br />

(17X/137X) ratio was detected in Serbian smokers compared to non-smokers…Habitual heavy<br />

coffee consumption increases Cytochrome P450 1A2 activity. Polycyclic aromatic hydrocarbons<br />

formed during roasting of coffee beans might partly be responsible for this effect.” (Djordjevic N, and<br />

others).<br />

XVII -51- To improve the endurance performance in competitions (ergogenic effect):<br />

“Caffeine improves performance and endurance during prolonged, exhaustive exercise. To a lesser<br />

degree, it also enhances short-term, high-intensity athletic performance. Caffeine improves concentration,<br />

reduces fatigue, and enhances alertness.” (Paluska S A).

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