Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1997-11-19
2000-12-12
Weddington, Kevin E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 11, 514 30, 514450, A61K 3800, A61K 3170, A61K 31335
Patent
active
061599328
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to mixtures of avermectins, 22,23-dihydroavermectins B.sub.1 (ivermectins) and milbemycins from the class of the macrocyclic lactones in combination with cyclic depsipeptides, optionally in the presence of praziquantel or epsiprantel, for increasing the endoparasiticidal action in endoparasiticidal compositions.
Gastrointestinal nematode infections of dogs are in most cases brought about by species of the three nemadode families Ascarididae, Ancylostomatidae and Trichuridae. In cats, it is predominantly the two nemadode families Ascarididae and Ancylostomatidae which have spread worldwide. After passing through a number of development stages in a very great diversity of tissues of the host animals, patent infection of the gastrointestinal tract occurs. During the prepatency and patency of the infection, the parasitosis of roundworms, hookworms and whipworms causes considerable problems, especially in young, growing dogs, cats and also in humans. Therapy or prophylactic treatment is therefore an urgent necessity in order both to cure animals already affected and to maintain as yet uninfected animals in a healthy condition.
Consequently, the protection of dogs and cats against infection is of very great importance as prophylaxis against human infections, especially in children.
A series of nematicidal substances are already used as anthelminthics in animal breeding. In order to achieve effective protection, increasing use is being made not only of the pure compound but also of combinations of two or more substances.
Nevertheless, the effectiveness of these known combinations against parasites, especially at low dosages, is not always entirely satisfactory.
In addition to the gastrointestinal helminthic diseases in dogs and cats, as already mentioned, there are further severe parasitoses, for example filiarioses, which are highly host-specific.
The parasite Dirofilaria immitis--a filaria endemic in parts of North to South America, Africa, Asia and also Australia, is the cause of the important canine and feline cardiovascular dirofilariosis. The severe pathophysiological changes within the cardiovascular system which occur during the Dirofilaria immitis infection of dogs and cats can bring about a dramatic course of the disease in the host animal.
Among the known compounds with anthelmintic activity, only a few possess efficiency as a prophylactic against Dirofilaria immitis.
Anthelminthics such as, for example, diethylcarbamazine (DEC), although effective, must be administered daily during transmission (mosquito) of the pathogen. With the introduction of the anthelminthics ivermectin/milbemycin from the class of the macrocyclic lactones, it has been possible to reduce the prophylactic treatment of dogs and cats to one monthly administration.
Although there are endoparasiticidal agents having a high level of efficiency against gastrointestinal nematodes and other agents with an action against Dirofilaria immitis in dogs and cats, none of the known compounds has as yet shown the kind of broad-spectrum action which would make it suitable for use as a therapeutic agent against all gastrointestinal nematodes and as a prophylactic agent against Dirofilaria immitis.
For this reason, a variety of active substance combinations are employed which exhibit an improved action and have, moreover, reduced side-effects and toxicity in the host.
In the majority of cases, the monthly prophylaxis of Dirofilaria immitis is carried out with an avermectin, for example ivermectin, from the class of the macrocyclic lactones in combination with an anthelminthic, such as pyrantel or a benzimidazole, e.g. albendazole (cf W. C. Campbell, Ann. Rev. Microbiol. 45 (1991), pp. 445-474; J. N. Clark et al. Am. J. Vet. Res. 53(4), (1992), pp. 517-520).
A combination which may be mentioned by way of example is one consisting of 6.0 .mu.g/kg ivermectin and 5.0 mg/kg pyrantel pamoate. While this combination ensures treatment and control of Ascarides (T. canis and T. leonina) and of hookworms (A. canis and U. steneoce
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Harder Achim
Jeschke Peter
Kolbl Barbara
Mencke Norbert
Akorli Godfried R.
Bayer Aktiengesellschaft
Gil Joseph C.
Weddington Kevin E.
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