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November 2019, Week 4


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Gerardo Gutierrez <[log in to unmask]>
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Gerardo Gutierrez <[log in to unmask]>
Tue, 26 Nov 2019 11:35:24 -0600
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Please your help

Drugs Today (Barc)


, 36 (11), 735-57
 Nov 2000Epinastine: An Update of Its Pharmacology, Metabolism, Clinical
Efficacy and Tolerability in the Treatment of Allergic Diseases
K Tasaka

   - PMID: 12845334
   - DOI: 10.1358/dot.2000.36.11.1136048


Epinastine is a potent antiallergic agent that has not only antihistaminic
(H(1)) properties but also provides antileukotriene, anti-PAF and
antibradykinin activities, which are associated with its antiallergic
actions. Moreover, epinastine is very effective in inhibiting the release
of chemical mediators from mast cells exposed to antigen. In addition, IL-8
release from eosinophils was inhibited by epinastine posttranscriptionally.
Chemotatic movement of eosinophils was also blocked by epinastine. The
increase in EEG power spectrum at low frequency region detected at frontal
cortex is associated with drowsiness. No such change was induced by
epinastine, while a marked increase was observed after ketotifen. In
agreement with this, when the amount of H(1) blockers that penetrated
through the BBB into the brain was estimated by means of PET, it was
apparent that epinastine hardly penetrated the BBB. With regard to the
current-voltage relationship of HERG currents, epinastine did not affect
I(Kr), while a marked inhibition was seen after terfenadine or astemizole.
These results indicated that epinastine does not suppress delayed rectifier
potassium current of the heart and, consequently, no cardiotoxic action of
epinastine was postulated. In man, epinastine is readily absorbed after
oral administration and no significant change in pharmacokinetics was found
during chronic administration. In teratological studies in rats,
malformation and variation were not observed even at high doses of
epinastine. In the clinical application of epinastine, it was shown that
this drug is remarkably effective in the treatment of various
dermatological diseases, such as chronic urticaria, psoriasis vulgaris and
other pruritic dermatoses. Moreover, epinastine provides excellent clinical
efficacy in the treatment of allergic rhinitis. Although efficacy of H(1)
blockers in bronchial asthma is somewhat doubtful, the overall improvement
rate in asthmatic patients was significantly higher in epinastine-treated
patients (53.7%) compared to those treated with ketotifen (25%).


Gerardo Gutierrez

Medical librarian EDUFARM