[Activity of the anthelmintic agent trichlorophen on the models of human helminthiasis]. / Aktivnost' otechestvennogo antigel'mintika trikhlofena na modeliakh gel'mintozov cheloveka.

Trials of trichlorophen have shown its high efficacy on models of cestode infections: hymenolepiasis (at the adult and cysticercoid stages of development on three types of animals: outbred albino mice, albino rats and golden hamsters), preimaginal echinococciasis alveolaris, larval alveolar echinococciasis (at the early stage of development of the parasite in experiments on cotton rats). The high nematodical activity of trichlorophen was first found on models of trichocephaliasis in DBA/2y mice, nippostrongyloidiasis (in in vitro experiments), and aspiculuriasis in outbred mice. The agent proved to be ineffective at the tissue developmental stage of Hymenolepsis nana (H. nana), the dwarf tapeworm, in albino mice, during experimental opisthorchiasis in golden hamsters. It showed a low efficacy in treating trichinosis in outbred albino mice. Unlike carbamatebenzimidazoles, trichlorophen was inactive at the tissue stage of H. nana; it exerted no effects on the eggs of a dwarf tapeworm in trichinosis. Trichlorophen was also inactive in treating experimental opisthorchiasis in golden hamsters.

[Experimental rationale for the use of medapec as the drug of choice in treating echinococcosis]. / Eksperimental'noe obosnovanie prigodnosti medapeka v kachestve preparata vybora dlia lecheniia ékhinokokkozov.

The dosage form of medamine-medapec was found to have a high antiechinococcal activity in experiments on laboratory animals. Its efficacy was shown in treating larval alveolar echinococciasis in mice and cotton rats with different doses and courses as compared with medamine and albendazole. It was ascertained that for its high larvicidal activity, medapec should be given to animals regularly during a day. The daily dose of the drug should be gradually increased. In complying with these conditions, the duration of effective courses of therapy drastically reduces.

[The pharmacokinetics of medamine and its solid polymeric form (medapek) in experimental larval alveolar echinococcosis in cotton rats]. / Farmakinetika medamina i ego tverdoi polimernoi formy (medapek) pri éksperimental'nom larval'nom al'veoliarnom ékhinokokkoze khlopkovykh krys.

Our study has shown that after single administration of its substance or its polymer formulation, medamine rapidly absorbs into blood, by penetrating into the host's viscera and tissues and parasitic larvocysts and excretes from the experimental animals' body at hour 24. Examining the distribution of medamine in the viscera and tissues has revealed that it penetrates into the rat viscera and tissue with blood and accumulated in the tissues. At the same time medamine given as a substance accumulates more in the excretory organs and medapec retains in the muscle tissue and brain longer. Medapec shows higher maximum concentrations at lower values of the pharmacokinetic curve area. Noticeable accumulation of medamine in the larvocysts of experimental animals confirms its chemotherapeutical activity.

[The experimental chemotherapy of larval alveolar echinococcosis. The search for an optimal regimen of albendazole use]. / Eksperimental'naia khimioterapiia larval'nogo al'veoliarnogo ékhinokokkoza. Poisk optimal'nogo rezhima primeneniia al'bendazola.

The antiechinococcal activity of albendazole resynthesized at the E. I. Martsinovskii Institute of Medical Parasitology and Tropical Medicine was studied on infection models in rats and mouse in different experimental modifications. The efficiency of the therapy was determined in relation to the dose of the drug and its routes administrations, to the single or intermittent daily dose, to the presence or absence of intervals in the treatment regimen, to dosage forms. The trials indicated that albendazole was most active against larval alveolar echinococcosis of mice or cotton rats when it was used with their feed, i.e. through the gastrointestinal tract.

[The search for new antiparasitic agents. 17. The synthesis and study of the anti-echinococcal activity of the new preparation G-1697]. / Izyskanie novykh protivoparazitarnykh sredstv. 17. Sintez i izuchenie protivoékhinokokkovoi aktivnosti novogo preparata G-1697.

The paper describes the synthesis of the new agent G-1697 which is 4-[(benzo-2,1,3-thiadiazolyl-4)amino]-5, 6,7,8-tetrahydrobenzothieno [2,3-d] pyrimidine and the results of testing its acute toxicity and antiparasitic activity on a model of Echinococcus multilocularis invasion at the larval stage in cotton rats. The maximum nonlethal dose of G-1697 was 4.0 g/kg for outbred mice of both sexes whose weight was 14-16 g. Adult cotton rats (males) received the agent with their feed in increasing daily doses for 3 weeks continuously on days 8 to 28 after infection. The daily dose of its active ingredient varied from 0.03 to 0.35 g/kg and averaged 0.12 g/kg (the mean total dose per session was 2.47 g/kg). The baseline weight of parasitic larvocysts (PL) per animal averaged 0.28 g at the baseline. In the treated and control rats sacrificed 34 days following infection, the mean mass of PL per animal was 0.95 and 7.51 g, respectively. In the cotton rats treated with G-1697, the suppressed growth index calculated by three parameters (moderate, maximum, and minimum mass of PL in the animals of the comparable groups after treatment with regard to the similar baseline variables) was 90.8, 91.0 and 92.7, respectively, versus the controls. Among all PL found in each animal, its death was approximately 70-90% in the treated rats.

[The search for new antiparasitic agents. 12. The synthesis and study of the anti-Echinococcus and anti-Hymenolepis activity of 6-[4-(4-alkylpiperazinyl-1)-phenylamino]-1,2,5-thiadazolo[3 ,4-h] quinolines]. / Izyskanie novykh protivoparazitarnykh sredstv. 12. Sintez i izuchenie protivoékhinokokkoznoi i protivogimenolepidoznoi aktivnosti 6-[4-(4-alkilpiperazinil-1)-fenilamino]-1,2,5-tiadiazolo[3,4-h] khinolinov.

The paper describes the synthesis of 6-[4-alkylpiperazinyl-1)phenylamino]-1,2,5-thiadiazolo[3,4-h ]quinolines where methyl (Drug G-1574) and ethyl (Drug G-1569) are alkyls. The two agents are as effective as mebendazole against the larval stage of Echinococcus multilocularis infection. Drug G-1574 has been demonstrated to ensure 100% recovery of spontaneously Hymenolepis nana-infected albino mice given doses 2.5-5 times lower than the effective dose of phenasal (niclosamide).

[Experimental chemotherapy of echinococcosis. 13. The effect of mebendazole in combination with a vegetable oil on the larval cysts of Echinococcus multilocularis and the reaction of the infested host to long-term administration of the preparation]. / Eksperimental'naia khimioterapiia ékhinokokkozov. Soobshchenie 13. Vliianie mebendazola v sochetanii s rastitel'nym maslom na larvotsisty mnogokamernogo ékhinokokka i reaktsiia invazirovannogo khoziaina na dlitel'noe vvedenie preparata.

The use of mebendazole as a suspension in vegetable oil enhanced the efficiency of treating experimental Echinococcus granulosus infection in outbred albino rats without increasing the dose of the drug. A sharp reduction in platelet count in the blood of the infected animals treated and untreated suggests that thrombohemorrhagic complications might be in echinococcosis. Thrombopenia in the treated animals appeared to be steady-state. A decrease in a rapid immune response in the mebendazole-treated rats, as compared to the untreated ones, is likely to be a consequence of a significant fall of antigenic immune stimulation due to suppression of the parasite's viability with the drug and to be an indicator of therapeutical efficiency.

[Differences in the infectivity and chemotherapy susceptibility of Kamchatka and Kazakhstan isolates of Echinococcus multilocularis in laboratory animals (a study of echinococcosis on Kamchatka Peninsula)]. / Razlichiia invazionnosti i podatlivosti khimioterapii kamchatskogo i kazakhstanskogo izoliatov Echinococcus multilocularis u laboratornykh zhivotnykh (k izucheniiu ékhinokokkozov na Kamchatskom poluostrove).

Describes specific features of development of larval multi-cystic echinococcosis in some laboratory animals infected with the Kamchatka and Kazakhstan strains of E. multilocularis. Analyses the efficacy of chemotherapy in animals infected with various strains of E. multilocularis.

[The search for new antiparasitic agents. 11. The acute toxicity and anticestodal activity of the new anthelmintic Tizanox compared with Azinox]. / Poisk novykh protivoparazitarnykh sredstv. 11. Ostraia toksichnost' i protivotsestodnaia aktivnost' novogo antigel'mintika tizanoksa v sravnenii s azinoksom.

A synthesis is described and the results of toxicological trial of the potential anthelmintic agent G-1587 are presented. The agent is 2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-2H-[1, 2,5] thiadiazino [3,2-a] isoquinoline-4,4-dioxide. The agent was shown to have a low toxicity, the maximal sublethal dose for mice being 4.0 g/kg when given per os.

[The search for new antiparasitic agents. 8. The synthesis and study of the acute toxicity, anti-alveolar hydatid and antihymenolepiasis activity of 1-alkyl-4[4-(heterylamino)phenyl]piperazines]. / Izyskanie novykh protivoparazitarnykh sredstv. 8. Sintez i issledovanie ostroi toksichnosti, protivoal'veokokkoznoi i protivogimenolepidoznoi aktivnosti nekotorykh 1-alkil-4[4-(geterilamino)fenil]piperazinov.

The synthesis and the acute toxicity and anticestodal activity of l-alkyl-4-[-(heterylamino)phenyl]-piperazines are presented. These compounds were found to be able to suppress the growth of larvocysts of Echinococcus multilocularis in cotton rats when injected intraperitoneally in a single dose of 0.25 g/kg, close to capacity of mebendazole. The tested compounds were also highly effective against the adult stage of Hymenolepis nana. Experimentally infected mice given an oral single dose of 0.2-0.5 g/kg of the drug were radically cured.

[The search for new antiparasitic agents. 7. A study of the relationship between the structure and the anthelmintic activity of new halogen-containing benzamides]. / Izyskanie novykh protivoparazitarnykh sredstv. 8. Izuchenie sviazi mezhdu stroeniem i protivogel'mintnoi aktivnost'iu novykh galoidsoderzhashchikh benzamidov.

Anthelminthic properties of new series of haloid-containing benzamides have been studied. The anthelminthic activity-structure relationships of the compounds under study has been examined. A number of highly active compounds promising for further investigations have been identified.

[Experimental chemotherapy of alveolar hydatid disease. 12. The efficacy of drug forms of mebendazole and nocodazole with high bioavailability]. / Eksperimental'naia khimioterapiia al'veokokkoza. Soobshchenie 12. Effektivnost' lekarstvennykh form mebendazola i nokodazola s povyshennoi biostupnost'iu.

New formulations have been designed to increase the efficacy and bioavailability of the oral drugs mebendazole and nocodazole and were tested in CBA mice. A considerable increase in efficacy was established for a solid disperse formulation of certain composition with a relatively lower toxicity than in aqueous suspensions of the drugs.