Scribd Logo
Upload

Welcome to Scribd!

  • 6 views

    Mechanisms Anthelmintic Action

    Uploaded by

    semere demissie
    Solution dosage form

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd

    Mechanisms Anthelmintic Action

    Uploaded by

    semere demissie
    6 views2 pages
    Solution dosage form

    Original Title

    978-3-0348-7090-0_19

    Copyright

    © © All Rights Reserved

    Available Formats

    PDF, TXT or read online from Scribd

    Did you find this document useful?

    Is this content inappropriate?

    Solution dosage form

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    6 views2 pages

    Mechanisms Anthelmintic Action

    Uploaded by

    semere demissie
    Solution dosage form

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 2

    Mechanisms of Anthelmintic Action

    By Dr. U. K. SHETH, M.D., B.Sc., F.C.P.S., F.C.P.C. (USA), F.A.M.S.


    Professor and Director, Department of Pharmacology and Clinical Pharmacology
    Seth G.S. Medical College and K.E.M. Hospital, Parel, Bombay 400012, India.

    I Introduction ............................................................ 147


    2 Neuromuscular Mechanisms.......................................... ..... 148
    2.1 Santonin. . . . . ... . ... . ... . .. . . . . . . . . . . .. . . . .. .. . . . . . . . . . .. ... . . . . . . .. . .. 149
    2.2 Piperazine .............................................................. 149
    2.3 Methyridine. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .. 150
    2.4 Tetramisole ...................................... . . . . . . . . . . . . . . . . . . . . . .. 150
    2.5 Organophosphorous Compounds .......................................... 150
    2.6 Tris-Carbonium Salts. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 150
    2.7 Diethylcarbamazine. .... .. . . . .... .. .. . . . .. . . .. . . . ... .. .. . . . . . . .... .. . .. . . lSI
    3 Energy Metabolism ...................................................... 151
    3.1 Mebendazole... .. .. . . .. . . . . . .. .. .. . . . . . . . . . .. .. .. . . . . . . . . . .... . .. . .. . .. 152
    3.2 Thiabendazole .......................................................... 152
    3.3 Pyrvinium Pamoate ...................................................... 152
    3.4 Trivalent Organic Antimonials ............................................ 153
    3.5 Niridazole .............................................................. 153
    3.6 Desperidine . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .. 153
    3.7 Tetrachlorethylene. . .. . . . .. .. . . . . . . . . . . . .... . .. . . . .. . .. .. . . .. . . . . . .. .... 154
    3.8 Suramin. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .. 155
    3.9 Combination of Drugs ................................................... 155
    4 Immunological Considerations ............................................. 155
    5 Conclusion ............................................................. 156
    References .................. "............................................ 156

    Introduction

    In the vast field of medical sciences, parasitology constitutes a small segment


    and has received comparatively scant attention, though wqrm infestation is a
    medical and public health problem of great magnitude, both in man and
    domesticated animals. The economic loss in terms of morbidity in man, loss of
    man-hours of work, and poor quality of animals, is exorbitant. Increasing the
    areas under cultivation, and quick and extensive modem transport system has
    contributed to the spread of worm infection beyond its traditional tropical and
    sub-tropical habitat. Drugs used as anthelmintics prior to World War II were
    mostly developed on empirical basis. Advances in the knowledge of physiolo-
    gy and biochemistry of parasites in last few years, have helped to a certain
    extent, in understanding the mechanism of action of known drugs, and
    development of newer chemotherapeutic agents. Understanding the mechan-
    isms of action of anthelmintics, requires a more complete understanding of
    helminth physiology, biochemistry, effect of environment, and role played by
    immunological processes in parasitic diseases, than is available at present.
    Till recently, mechanism of action of anthelmintics was described purely on
    the basis of gross effects of drugs on parasites - in terms of removal of the

    147

    E. Jucker (ed.), Progress in Drug Research / Fortschritte der Arzneimittelforschung /


    Progrès des recherches pharmaceutiques
    © Birkhäuser Verlag Basel 1975
    U. K. Sheth

    parasite either dead or paralysed, from the host, or fu terms of decrease in the
    excretion of eggs or circulating microfilaria. Structure activity relationship of
    related chemical analogues has also been described in terms of comparative
    gross effects on parasites. Majority of text books and monograms on chemo-
    therapy, while descnbing anthelmintic action of a drug often mention that
    'mechanism of action of the drug is not known'. In recent years two main
    approaches have been made towards elucidating these mechanisms. The first
    approach is derived from the observation that many of the anthelmintics have
    an effect on the neuromuscular system of helminths, leading to either increase
    or decrease in their activity. The other approach has been on the basis of the
    knowledge that most of the helminths utilize carbohydrate as a source of
    energy. Studies on the possibility of interfering with the utilisation of carbohy-
    drate for energy, by selectively interfering with the functional integrity of the
    enzymes of the parasites without affecting those catalysing the same reactions
    in the hosts, has been an interesting approach in developing newer anthelmin-
    tics.
    I do not plan to discuss in detail all the drugs available for treatment of
    various helminths. I propose to indicate briefly, some of the well documented
    mechanisms of action of few anthelmintics, and indicate the present trends of
    thoughts in this field, based on which, the future anthelmintics are likely to be
    developed. The helminths of clinical importance in our country are, hook-
    worms, ascaris, pinworm, and in some areas tapeworms. I will however, refer
    to certain other infections, like schistosomiasis which though not prevalent
    here, is of great importance in other parts of the world and has been a subject
    of many interesting studies. These studies are of great help in bringing out
    various mechanisms of action of anthelmintics.

    2 Neuromuscular Mechanisms

    Survival of most of the parasitic helminths in their natural habitat depends on


    their ability to maintain themselves 'in situ' in the face of peristaltic move-
    ments of intestines or movement of blood or lymph. Most of the parasites
    exhibit well co-ordinated rhythmic movements which help them to maintain
    their position in the hosts, or have specialized sucker like organs or hooks, the
    movements of which help them to attach themselves to the hosts. The neuro-
    muscular system is fairly well developed in various helminths. Platyhelminths
    have a well defined sub-cuticular musculature consisting of an outer circular, a
    middle longitudinal, and inner diagonal layer. Parasitic nematodes have
    underneath the cuticle a single layer of muscles consisting exclusively of
    longitudinal fibres. The movements of these muscles are controlled by a
    primitive sort of nervous system, consisting of ganglia and nerve fibres. The
    nervous system operates through release of neurotransmitters. Occurrance of
    acetylcholine in helminths was first described by BULBRING et al. [13]. Acetyl-
    choline and both its synthesising and hydrolysing enzymes have been demon-

    148

    You might also like