Note: Descriptions are shown in the official language in which they were submitted.
25,643
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SU~ ~RY OF THE INVENTION
This invention relates to an animal feed
composition comprising, a nutrionally balanced feed
containing a cyclopropanecarboxylic acid of the formula:
R- ~ -CO-0-CH 2
CH3- /
l ~H3 O ~
wherein R is 2,2-dichlorovinyl- or 2-methyl-propenyl- in
an amount of from 0.01% to 2.5~ by weight of the feed.
BAC~GR~UND OF THE INVENTION
1. Field of the Invention: The field of the
invention is the use of cyclopropanecarboxylates for
systemic control of ectoparasites on animals.
2. The Prior Art: Ixodidae, or hard ticks, are
generally categorized as one-host, two-host or three-host
ticks. They sustain themselves and their species by attach-
ing to a host animal and feeding the blood and body fluids
thereof. Engorged females drop from the host animal and lay
their eggs (2,000 to 20,000) in a niche on the ground or in
some sheltered area where hatching occurs. The larvae then
seek a host from which to obtain a blood meal and depending
on whether the tick is a one, two or three-host tick may
drop off the host to molt.
Ixodid ticks are responsible for the transmission
and propagation of a great many human and animal diseases
throughout the world. Those ticks of major economic impor-
tance include Boophilus spp., Rhipicephalus spp., Ixodes
spp., Hyalomma spp., Amblyomma spp. and Dermacentor spp.
They are vectors for disease, tick paralysis and tick toxi-
cosis. A single tick species can cause paralysis of several
different mammals, and several tick species can cause pa-
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ralysis in a particular host. Tick-borne diseases, such
as Sweating Sickness, Babesiosis, Anaplasmosis, Theileriosis
and Heartwater, have been and are responsible for the death
and/or debilitation of a vast number of animals throughout
the world each year. Ticks are responsible for great eco-
nomic losses in livestock production in the world today.
Such losses are, of course, attributable not only to death,
but also to damaged hides, loss in growth rate, reduction
in milk production and reduced grade of meat animals.
Although the debiiitating effects of tick and
other pest infestation of animals has been recognized for
years, and tremendous strides have been made in tick con-
trol programs, no entirely satisfactory method for con-
trolling or eradicating these parasites has been forth-
coming. Topical treatment of tick-infested and other ecto-
parasite plagued animals with chemical ectoparasital agents,
such as the chlorinated hydrocarbons, including benzene
hexachloride (BHC), DDT, toxaphene, chlordane and aldrin;
the organophosphorus compounds, including Delnav, ethion
and coumaphos, have been partially successful in controlling
ectoparasite populations. However, certain speeies of eeto-
parasites have become resistant to the ehlorinated hydro-
carbons and the organophosphates.
Netherlands Patent No. 7,307,130, issued Nov. 27,
1973, describes a broad class of cyclopropanecarboxylic acid
ester derivatives which include the compounds I have found
to be effective agalnst ectoparasites. The patentee does
not, of course, suggest the systemic method of the present
invention.
DETAILED DESCRIPTION
The invention provides a method for the systemic
control of insecticidal and acaracidal agents which attack
warm-blooded or homothermic animals by employing systemic
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cyclopropanecarboxylates that provide excellent control of
ectoparasites. In the invention, cyclopropanecarboxylates
of the formula:
ClzC=CH-
\ > co-o-c~24
CH3- ,H3 0 ~
Cyclopropanecarboxylic acid,
3-(2,2-dichlorovinyl)-2,2-dimethyl-
m-phenoxybenzyl ester, cis and trans isomer
(GH3)2C=CH- ~ r--~
> -C0-0-CH 2 y \>
CH3-
or CH3 ~
Cyclopropanecarboxylic acid,
2,2-dimethyl-3-(2-methyl-propenyl)-
3'-phenoxybenzyl ester, c1s and trans isomer
are administered to the animals orally or parenterally in
amounts ranging from 0.01 to about 600 mg per kilogram
animal body weight and preferably from about 100 mg to 400
mg per kilogram animal body weight.
As indicated above, the systemic insecticidal and
acaricidal agents of the invention may be administered
orally or parenterally. When given orally, they may be in
any convenient oral form of medication, such as a capsule,
tablet or as an oral drench.
The agents may also be incorporated in a nu-
tritionally balanced animal feed in the range of 0.01% to
2.5~ by weight of feed and preferably 0.01% to 1.0% by weight
of feed. They may also be added to the animal drlnking water
with the aid of a pharmaceutically acceptable dispersing
or emulsifying agent.
- 30 If desired, the systemic agents may be intro-
duced into the body of the animal by subcutaneous, intra-
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muscular or intraperitoneal injection. The manner of admin-
istration of the systemic agents is not particularly
important, so long as the prescribed amounts of systemic
agents are introduced into the body of the animal where it
may be distributed by the action of the circulatory system.
Advantageously, the above-identified compounds are
highly effective systemic ixodicidal agents. They have re-
latively low mammalian toxicity and are effective for pro-
tecting animals, particularly dom~stic and farm animals,
such as dogs, cats, cattle, sheep, horses and the like,
from attack by ticks. They can be used to control a wide
variety of ixodid ticks, including Boophilus spp., Amblyomma
spp., Rhipicephalus ~., Dermacentor ~., and Hyalomma
spp .
The invention is exemplified by the following
non-limiting examples.
Example l
_etermination of Systemic Ixodicidal Activity of Cyclopro-
panecarboxylic acid, 3-(2,2-dichlorovinyl)-2,2-dimethyl-m-
phenoxybenzyl ester (mixture of cis- trans isomers) Against
the three-host tick Rhipicephalus anguineus
Albino guinea pigs are housed individually and
fed guinea pig chow and water ad libitum. One leaf of cab-
bage per day is also given to each guinea pig.
The diet employed in these tests is as follows:
Crude protein not less than 18.0%
Crude fat not less than4.0%
Crude fiber not more than16.0%
Added minerals not more than 3.5%
Ash not more than 7.0%
and consists of the following ingredients: Ground wheat,
ground yellow corn, drled skimmed milk, soybean meal, de-
hydrated alfalfa meal, cane molasses, wheat middlings,
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animal fat preserved with BHA, vitamin B12 supplement,
riboflavin supplement, cholin chloride, calcium pantothe-
nate, thiamin, niacin, folic acid, ascorbic acid, vitamin A
supplement, D activated sterol (source of vitamin D3),
methionine hydroxy analogue calcium, pyridoxine hydrochloride,
vitamin E supplement, dicalcium phosphate, calcium carbonate,
iodized salt, copper oxide, copper sulfate, iron sulfate,
iron oxide, manganous oxide, cobalt carbonate, zinc oxide.
To the shaved back of each guinea pig, a capsule
made from a 2 inch spud gasket, with the base ground down
to provide greater flexibility, is glued using 3M adhesive
no. 8001. Five male and five female adult Rhipicephalus
sanguineus ticks are placed inside the capsule and allowed
to attach to the guinea pig. A gauze material is fastened
over the top of the gasket to prevent the ticks from escaping.
The yuinea pigs are given a daily oral dose by
gelatin capsule of either 400 or 100 mg per kilogram body
weight of the test compound. The ticks do not appear to be
affected for about 3 days after the initial treatment except
for slight color changes and some reduction in size, but
become moribund and die shortly thereafter. The following
test data are obtained:
~Tick
Daily oral dose (mg/kg) Mortality
25400 100
100 80
control 0
Example 2
Determination of ~ystemic Ixodicidal Activity of Cyclopro-
30 panecarboxylic acid, 3-(2,2-dichlorovinyl)-2,2-dimethyl-,
. . .
m-phenoxybenzyl ester, cis -trans (23% - 77%) against the
~ .... _ . ...
Three-host Tick Dermacentor variabilis.
_
By the method of Example 1 the efficacy of the
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test compound for controlling the above-identified tick
species is demonstrated. The Dermacentor variabilis ticks
are somewhat less susceptible to the test compound and after
about 5 days become moribund and die shortly thereafter.
The data obtained are as follows:
% Tick
Daily oral dose (mg/kg) Mortality
400 80
100 0
Control 0
Results comparable to those in the Examples are obtained
with the ixodicide, cyclopropanecarboxylic acid, 2,2-di-
methyl-3-(2-methylpropenyl)-3-phenoxybenzyl ester, trans
and cls.
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