SpringerLink
Log in

Repository Preparations

  • Chapter
Antimalarial Drug II

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 68 / 2))

  • 894 Accesses

Abstract

The nature and extent of the malaria problem and the details surrounding those agents both available and under development for treatment of active disease have been addressed in various sections of this volume. We propose to discuss here a specific need which exists in malaria chemotherapy, that is for agents with prolonged activity — the so-called repository drugs. This therapeutic requirement has only in recent years received attention, and it is certainly not yet attracting substantial research. Early efforts in this field were reviewed in 1969 (Elslager 1969) and again in 1974 (Elslager 1974). It is our intention to place in perspective both past and recent research in this brief survey.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution

Subscribe and save

Springer+ Basic
EUR 32.99 /Month
  • Get 10 units per month
  • Download Article/Chapter or Ebook
  • 1 Unit = 1 Article or 1 Chapter
  • Cancel anytime
Subscribe now

Buy Now

Chapter
GBP 19.95
Price includes VAT (United Kingdom)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
GBP 103.50
Price includes VAT (United Kingdom)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
GBP 129.99
Price includes VAT (United Kingdom)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free ship** worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

Similar content being viewed by others

References

  • Black RH, Hennessy WB, McMillian B (1966) Studies on depot antimalarials:2. The effect of a single injection of the depot antimalarial CI-564 on relapsing vivax malaria acquired in New Guinea. Med J Austr 2:808–811

    CAS  Google Scholar 

  • Bruce-Chwatt LJ (1977) Prolonged malaria prophylaxis. Br Med J 2:1287

    Article  PubMed  CAS  Google Scholar 

  • Chandrasekaran SK, Benson H, Urquhart J (1978) Methods to achieve controlled drug delivery, the biomedical approach. In: Robinson JR (ed) Sustained and controlled release drug delivery systems. Dekker, New York, pp 557–593

    Google Scholar 

  • Chien YW (1978) Methods to achieve sustained drug delivery. The physical approach:implants. In: Robinson JR (ed) Sustained and controlled release drug delivery systems. Dekker, New York, pp 211–349

    Google Scholar 

  • Chien YW, Lambert HJ, Grant DE (1974) Controlled release from polymeric devices I:Technique for rapid in vitro release studies. J Pharm Sci 63:365–369

    Article  PubMed  CAS  Google Scholar 

  • Chin W, Lunn JS, Buxbaum J, Contacos PG (1965) The effect of cycloguanil pamoate (CI-501) against a chlorguanide-resistant Chesson strain of Plasmodium vivax. Am J Trop Med Hyg 14:922–924

    PubMed  CAS  Google Scholar 

  • Chin W, Contacos PG, Coatney GR, Jeter MH, Alpert E (1967a) Evaluation of CI-564, a 1:1 mixture of cycloguanil pamoate (CI-501) and 4,4’-diacetylaminodiphenylsulfone (CI-556), against multiresistant falciparum malarias. Am J Trop Med Hyg 16:580–584

    PubMed  CAS  Google Scholar 

  • Chin W, Coatney GR, King HK (1967b) An evaluation of CI-564 against blood-induced chlorguanide-sensitive and chlorguanide-resistant strains of vivax malaria. Am J Trop Med Hyg 16:13–14

    PubMed  CAS  Google Scholar 

  • Choulis NH, Papadopoulos H (1975) Timed-release tablets containing quinine sulfate. J Pharm Sci 64:1033–1035

    Article  PubMed  CAS  Google Scholar 

  • Coatney GR, Contacos PG, Lunn JS, Kilpatrick JW, Elder HA (1963) The effect of a repository preparation of the dihydrotriazine metabolite of chlorguanide, CI-501, against the Chesson strain of Plasmodium vivax in man. Am J Trop Med Hyg 12:504–508

    PubMed  CAS  Google Scholar 

  • Coatney GR, Contacos PG, Lunn JS (1964) Further observations on the antimalarial activity of CI-501 (Camolar©) against the Chesson strain of vivax malaria. Am J Trop Med Hyg 13:383–385

    PubMed  CAS  Google Scholar 

  • Contacos PG, Coatney GR, Lunn JS, Kilpatrick JW (1964) The antimalarial activity of CI501(Camolar©) against falciparum malaria. Am J Trop Med Hyg 13:386–390

    PubMed  CAS  Google Scholar 

  • Contacos PG, Coatney GR, Lunn JS, Chin J (1965) Resistance to cycloguanil pamoate (CI-501) by falciparum malaria in West Pakistan. Am J Trop Med Hyg 14:925–926

    PubMed  CAS  Google Scholar 

  • Contacos PG, Coatney GR, Lunn JS, Chin W (1966) The urinary excretion and the antimalarial activity of CI-501 (Cycloguanil-pamoate, Camolar©) against vivax and falciparum malaria. Am J Trop Med Hyg 15:281–286

    PubMed  CAS  Google Scholar 

  • Desjardins RE, Canfield CJ, Haynes JD, Chulay JD (1979a) Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Antimicrob Agents Chemother 16:710–718

    PubMed  CAS  Google Scholar 

  • Desjardins RE, Pamplin CL, von Bredlow J, Berry KG, Canfield CJ (1979b) Kinetics of a new antimalarial, mefloquine. Clin Pharmacol Ther 26:372–379

    PubMed  CAS  Google Scholar 

  • Doberstyn EB, Phintuyothin P, Noeypatimanondh S, Teerakiartkamjorn (1979) Single-dose therapy of falciparum malaria with mefloquine or pyrimethamine-sulfadoxine. Bull WHO 57:275–279

    PubMed  CAS  Google Scholar 

  • Elslager EF (1969) Progress in malaria chemotherapy Part 1. Repository antimalarial drugs. Prog Drug Res 13:171–212

    Google Scholar 

  • Elslager EF (1974) New perspectives on the chemotherapy of malaria, filariasis, and leprosy. Prog Drug Res 18:99–172

    PubMed  CAS  Google Scholar 

  • Elslager EF, Worth DF (1966) Pyrimidine compounds. U.S. Patent 3,236,849

    Google Scholar 

  • Elslager EF, Gavrilis ZB, Phillips AA, Worth DF (1969a) Repository drugs. IV. 4′,4′-Sulfonylbisacetanilide (acedapsone, DADDS) and related sulfanilylanilides with prolonged antimalarial and antileprotic action. J Med Chem 12:357–363

    Article  CAS  Google Scholar 

  • Elslager EF, Phillips AA, Worth DF (1969b) Repository drugs. V.4’,4“’-[p-Phenylenebis(methylidyneimino p-phenylenesulfonyl)]bisacetanilide (PSBA) and related 4’,4”’[bis(imino-p-phenylenesulfonyl)]bisanilides, a novel class of long-acting antimalarial and antileprotic agents. J Med Chem 12:363–367

    Article  CAS  Google Scholar 

  • Elslager EF, Capps DB, Worth DF (1969c) Repository drugs. VII. N-Allylidene-4,4’-sulfonyldianiline and N-(benzylidene and -1-naphthylmethylene)-N’-methylene-4,4’-sulfonyldianiline polymers with prolonged antimalarial and antileprotic action. J Med Chem 12:597–599

    Article  PubMed  CAS  Google Scholar 

  • Elslager EF, Tendick FH, Werbel LM (1969d) Repository drugs. VIII. Ester and amide congeners of amodiaquine, hydroxychloroquine, oxychloroquine, primaquine, quinacrine, and related substances as potential long-acting antimalarial agents. J Med Chem 12:600–607

    Google Scholar 

  • Elslager EF, Hutt MP, Jacob P, Johnson J, Temporelli B, Werbel LM, Worth DF (1979) Folate antagonists. 15. 2,4-Diamino-6-(2-naphthylsulfonyl)quinazolines and related 2,4-diamino-6-[(phenyl and naphthyl)-sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity. J Med Chem 22:1247–1257

    Article  PubMed  CAS  Google Scholar 

  • Flynn GL, Smith EW (1971) Membrane diffusion I:design and testing of a new multi-featured diffusion cell. J Pharm Sci 60:1713–1717

    Article  PubMed  CAS  Google Scholar 

  • Fu JC, Kale AK, Moyer DL (1973) Drug-incorporated silicone discs as sustained release capsules. I. Chloroquine diphosphate. J Biomed Mater Res 7:71–78

    Google Scholar 

  • Grindel JM, Tilton PF, Shaffer RD (1977) Quantitation of the antimalarial agent, mefloquine, in blood, plasma, and urine using high-pressure liquid chromatography. J Pharm Sci 66:834–837

    Article  PubMed  CAS  Google Scholar 

  • Hawking F, Perry WLM (1948) Activation of paludrine. Br J Pharm 3:320–325

    CAS  Google Scholar 

  • Judge BM, Howells RE (1979a) A comparison of the response of Plasmodium berghei to primaquine diphosphate following drug administration by repeated daily injections and by a constant release system. Trans R Soc Trop Med Hyg 73:327–328

    Google Scholar 

  • Judge BM, Howells RE (1979b) The use of drug polymer mixture implants for sustained antimalarial effects in mice. Br Soc Parasitol Proc 79:2–3

    Google Scholar 

  • Korolkovas A, Ferreira EI, Lima JD, Krettli AU (1978) Antimalarial activity of saccharidic polymers of dapsone and sulfadimethoxine. Chemotherapy 24:231–235

    Article  PubMed  CAS  Google Scholar 

  • Laboratory of Malaria Research, Shanghai Institute of Parasitic Diseases (1975) Preliminary studies on tripiperaquine (M 1020). Chin Med J (Engl) 1:419–424

    Google Scholar 

  • Peters W (1978) Medical aspects — comments and discussion II. Symp Br Soc Parasitol 16:25–40

    Google Scholar 

  • Pinazzi C, Rabadeux JC, Pleurdeau A, Niviere P, Paubel JP, Benoit JP (1978) Synthesis and polymerization of polymethacrylates containing the quinine residue. Comparative study of the toxicity and immunogenicity of the free and polymeric form. Makromol Chem 179:1699–1706

    Google Scholar 

  • Powell RD, Brewer GJ, DeGowin RL, Alving AS (1964) Studies on a strain of chloroquineresistant Plasmodium falciparum from Vietnam. Bull WHO 31:379–392

    PubMed  CAS  Google Scholar 

  • Powell RD, DeGowin RL, Eppes RB (1965) Studies on the antimalarial effects of cycloguanil pamoate (CI-501) in man. Am J Trop Med Hyg 14:913–921

    PubMed  CAS  Google Scholar 

  • Rieckmann KH, Trenholme GM, Williams RL, Carson PE, Frischer H, Desjardins RE (1974) Prophylactic activity of mefloquine hydrochloride (WR 142490) in drug-resistant malaria. Bull WHO 51:375–377

    PubMed  CAS  Google Scholar 

  • Ritschel WA, Hammer GV, Thompson GA (1978) Pharmacokinetics of antimalarials and proposals for dosage regimens. Int J Clin Pharmacol 16:395–401

    CAS  Google Scholar 

  • Robinson JR (1978) Sustained and controlled release drug delivery systems. Dekker, New York

    Google Scholar 

  • Rozman RS, Canfield CJ (1979) New experimental antimalarial drugs. In: Garattini S, Goldin A, Hawking F, Kopkin IJ (eds) Advances in pharmacology and chemotherapy, vol 16. Academic, New York, pp 31–32

    Google Scholar 

  • Russell DA, Worth RM, Jano B, Fasal P, Shepard C (1979) Acedapsone in the prevention of leprosy:field trial in three high prevalence villages in Micronesia. Am J Trop Hyg 28:559–563

    CAS  Google Scholar 

  • Schmidt LH (1973) Infections with Plasmodium falciparum and Plasmodium vivax in the owl monkey — model systems for basic biological and chemotherapeutic studies. Trans R Soc Trop Med Hyg 67:446–470

    Article  PubMed  CAS  Google Scholar 

  • Schmidt LH, Rossan RN, Fisher KF (1963) The activity of a repository form of 4,6-diamino-l-(p-chlorophenyl)-1,2-dihydro-2,2-dimethyl-s-triazine against infections with Plasmodium cynomolgi. Am J Trop Med Hyg 12:494–503

    PubMed  CAS  Google Scholar 

  • Schneider J, Bonury M, Le Quellac J (1965) Plasmodium berghei et chimiotherapie. Ann Soc Belg Med Trop 45:435–439

    Google Scholar 

  • Schofield P, Howells RE, Peters W (1981) A technique for the selection of long-acting antimalarial compounds using a rodent malarial model. Ann Trop Med Parasitol 74:521–531

    Google Scholar 

  • Sodeman TM, Contacos PG, Collins WE, Smith CS, Jumper JR (1972) Studies on the prophylactic and radical curative activity of RC-12 against Plasmodium cynomolgi in Ma-caca mulatta. Bull WHO 47:425–428

    PubMed  CAS  Google Scholar 

  • Thompson PE, Olszewski BJ, Elslager EF, Worth DF (1963) Laboratory studies on 4,6-diamino-l-(p-chlorophenyl)- 1,2-dihydro-2,2-dimethyl-s-triazine pamoate (CI-501) as a repository antimalarial drug. Am J Trop Med Hyg 12:481–493

    PubMed  CAS  Google Scholar 

  • Thompson PE, Olszewski B, Waitz JA (1965a) Laboratory studies on the repository antimalarial activity of 4,4’-diacetylaminodiphenylsulfone, alone and mixed with cycloguanil pamoate (CI-501). Am J Trop Med Hyg 14:343–353

    PubMed  CAS  Google Scholar 

  • Thompson PE, Bayles A, Olszewski B, Waitz JA (1965b) Studies on a dihydrotriazine and sulfone, alone and in combination, against Plasmodium berghei in mice. Am J Trop Med Hyg 14:198–206

    PubMed  CAS  Google Scholar 

  • Thompson PE, Waitz JA, Olszewski B (1965c) The repository antimalarial activities of 4,4′diacetylaminodiphenylsulfone and cycloguanil pamoate (CI-501) in monkeys relative to local release following parenteral administration. J Parasitol 51:343–349

    Google Scholar 

  • Thompson PE, Bayles A, Olszewski B (1970) Antimalarial activity of 2,4-diamino-6-[(3,4dichlorobenzyl)nitros-amino]quinazoline (CI-679 base) and CI-679 acetate, laboratory studies in mice and rhesus monkeys. Am J Trop Med Hyg 19:12–26

    PubMed  CAS  Google Scholar 

  • Werbel LM, Jacobs RL, Steinkampf RW, Worth DF (1981) Repository effects of 2,4-di-amino-6-(2-naphthylsulfonyl)quinazoline in mice. Personal observations

    Google Scholar 

  • Werbel LM, Jacobs RL, Steinkampf RW, Worth DF ( 1981 b) Repository antimalarial activity of pyrimethamine pamoate. Am J Trop Med Hyg, Submitted for publication

    Google Scholar 

  • Wise DL, McCormick GJ, Willet GP, Anderson LC (1976) Sustained release of an antimalarial drug using a copolymer of glycolic/lactic acid. Life Sci 19:867–874

    Article  PubMed  CAS  Google Scholar 

  • Wise DL, McCormick GJ, Willet GP, Anderson LC, Howes JF (1978) Sustained release of sulfadiazine. J Pharm Pharmac 30:686–689

    Article  CAS  Google Scholar 

  • Wise DL, Gresser JD, McCormick GJ (1979a) Sustained release of a dual antimalarial system. J Pharm Pharmacol 31:201–204

    Article  PubMed  CAS  Google Scholar 

  • Wise DL, Fellman TD, Sanderson JE, Wentworth RL (1979b) Lactic/glycolic acid polymers. In: Gregoriades G (ed) Drug carriers in biology and medicine. Academic, London, pp 237–270

    Google Scholar 

  • Wiselogle FY (1946) A survey of antimalarial drugs, 1941–1945, 2 Vols. Ann Arbor, Michigan

    Google Scholar 

  • World Health Organization (1967) Chemotherapy of malaria, Report of a WHO scientific group. WHO Tech Rept Ser No 375

    Google Scholar 

  • Worth DF, Elslager EF, Phillips AA (1969) Repository drugs. VI. 4′-[N-(aralkylidene-, -benzylidene-, and -naphthylidene)sulfanilyl]anilides, 4′-[N-[(dimethylamino)methylene]sulfanilyl]anilides, and related sulfanilylanilides with prolonged antimalarial and leprotic action. J Med Chem 12:591–596

    Article  PubMed  CAS  Google Scholar 

Download references

Authors
  1. D. F. Worth
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. L. M. Werbel
    View author publications

    You can also search for this author in PubMed Google Scholar

Editor information

Editors and Affiliations

  1. London School of Hygiene and Tropical Medicine, Keppel Street, London, WC1E 7HT, Great Britain

    Wallace Peters M.D., DSc, FRCP, DTM & H (Professor of Medical Protozoology) (Professor of Medical Protozoology)

  2. Wellcome Research Laboratories, Ravens Lane, Berkhamsted, Herts., HP4 2DY, Great Britain

    William H. G. Richards BSc, Ph. D. (Manager, Scientific Advisory Services) (Manager, Scientific Advisory Services)

Rights and permissions

Reprints and permissions

Copyright information

© 1984 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Worth, D.F., Werbel, L.M. (1984). Repository Preparations. In: Peters, W., Richards, W.H.G. (eds) Antimalarial Drug II. Handbook of Experimental Pharmacology, vol 68 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-69254-3_7

Download citation

  • DOI: https://doi.org/10.1007/978-3-642-69254-3_7

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-69256-7

  • Online ISBN: 978-3-642-69254-3

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics

Search

Navigation