
1.
Caffeine is able to penetrate
the blood brain barrier and directly influence the
CNS
Lamarine (1994) notes caffeine is able to penetrate the blood brain
barrier and directly influence
the CNS. Ochs,
Holmes, and Karst (1992) report as a chemical, caffeine is a methylated
xanthine, a powerful central nervous system (CNS) stimulant which can
arouse all levels of the
rain and the skeletal muscles.
2.
4-quinolones inhibit
biotransformation of caffeine.
The pharmacokinetics of caffeine, including formation of its major
metabolite paraxanthine in plasma, has been investigated in 12 healthy
males (age 20-40 years) alone and during co-administration of the
4-quinolones ofloxacin, norfloxacin, pipemidic acid, ciprofloxacin,
and
enoxacin; ciprofloxacin and enoxacin were given in 3 different
dose levels. The naphthyridine
derivative enoxacin and the
pyrido-pyrimidine derivative pipemidic acid had caused marked
inhibition of caffeine and paraxanthine metabolism
3. Ciprofloxacin-caffeine: a drug interaction established using in vivo
and in vitro
investigations.
The inhibitory effects of ciprofloxacin and other quinolone
derivatives on the hepatic cytochrome P450-dependent metabolism of
caffeine have been investigated in humans. In vivo studies involved an
intraindividual comparison of the single-dose kinetics of caffeine
before and during quinolone
administration in 12
healthy men.