By E. W. McChesney, C. D. Fitch (auth.), Wallace Peters M.D., DSc, FRCP, DTM & H, William H. G. Richards BSc, Ph. D. (eds.)
The development of this quantity has been guided via own convictions. event within the box of experimental chemotherapy, either within the pharmaceutical and academia, has confident us that contemporary quantum technological advances in biochemistry, molecular biology, and immunology will enable and, certainly, necessitate an more and more better use of rational drug improvement sooner or later than has been the customized prior to now. partially l, for that reason, we requested our members to supply exact stories masking the biology of the malaria parasites and their relation with their hosts, the experimental approaches together with tradition innovations which are essential to take a drug from basic screening to scientific trial, and an account of antimalarial drug resistance. Our moment conviction is that many learn employees are all too loath to benefit from the teachings of the prior. consequently we requested the individuals to half 2 of this quantity to check very completely the commonly scattered yet voluminous literature on these few chemical teams that experience supplied the antimalarial medicines in scientific use this day. a lot should be realized from the historical past in their improvement and the issues that experience arisen with them in guy. a few certainly should still have a lot to supply in the event that they should be deployed in higher methods than they're at this time. this query has been taken up by way of a number of authors.
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3. Ear DENCKER and LINDQUIST (1975) have studied the accumulation of CQ in the melanin-bearing tissues of albino and pigmented rats, following injection of the 14C-labelled compound. Large accumulations were found in the stria vascularis and planum semilunatum of the inner ear, but in the pigmented animals only. This accumulation persisted even after an interval of 13 days post-injection. 4. Brain It has been pointed out frequently above (see Tables 3-5) that brain is a minor repository for CQ in all species.
It has been recommended (TANENBAUM and TUFFANELLI 34 E. W. MCCHESNEY and C. D. FITCH 1980) that the patients' ocular functions (EOG), in any case, should be monitored at about 4-monthly intervals. This is certainly a reasonable precaution; however, GRANIEWSKI-WIJNANDS et al. (1979) doubt that such a precaution is really necessary, providing that the dosage ofCQ or its equivalent does not exceed 75 g/year. 3. Ear DENCKER and LINDQUIST (1975) have studied the accumulation of CQ in the melanin-bearing tissues of albino and pigmented rats, following injection of the 14C-labelled compound.
It is of particular interest, in connection with the retinopathy problem, to note the very high affinity of CQ for retina choroid, and the comparatively low affinity for sclera (line 16). Results on the one squirrel monkey (line 17) are notable for the fact that the concentration in heart exceeded that in all of the other tissues analysed; otherwise, the relative affinities were much the same as in the rhesus strain. In all of these animals, except the one listed in line 19, the analyses were based on 14C content, but it may be assumed that at least 80% of the 14C was present in the form of unchanged CQ.
Antimalarial Drug II: Current Antimalarial and New Drug Developments by E. W. McChesney, C. D. Fitch (auth.), Wallace Peters M.D., DSc, FRCP, DTM & H, William H. G. Richards BSc, Ph. D. (eds.)
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