USE OF A SUBSTITUTED IMIDAZOLE FOR THE MANUFACTURE OF A MEDICAMENT USEFUL AS A SEDATIVE OR ANALGESIC

Abstract: 4-[(α-Methyl)-2,3-dimethyl-benzyl]imidazole is useful as a veterinary sedative-analgetic agent, especially in small mammals.

Description: This invention relates to sedative and analgesic agents useful in the veterinary field. 4-[(α-Methyl)-2,3-dimethyl-benzyl]imidazole of the formula has been disclosed in the European Patent Publication No. 72615 as an antihypertensive agent. 4-(2,3-Dimethylbenzyl)imidazole, or detomidine, is a known sedative and analgesic agent useful in horses and cattle. Detomidine is used in veterinary medicine as a pharmacological restraint to keep the animal sedated before investigation, treatment and difficult medical operations. Even a small surgical operation cannot be carried without the use of a sedative agent. The effect of detomidine in horses and cattle has been described in the literature, e.g. O. Vainio: "Detomidine hydrochloride - a novel imidazole-type sedative-analgesic". Pharmacologie et Toxicologie Veterinaires, INRA Publ. Paris, 1982, Les Colloques de I'INRA, No. 8. There is also a great need for sedative-analgesic agents as pharmacological restraints in the treatment of dogs, cats and other small animals, but no useful effect was, however, observed. We have now surprisingly found that the above-mentioned detomidine analogue, 4-[(α-methyl)-2,3-dimethylbenzyl] imidazole (compound (I)) is very effective as a sedative-analgesic in the treatment of small animals, especially dogs and cats, but also, e.g., guinea pits and rabbits. Intramuscular or intravenous administration of this compound at a dose of 10 to 160 µg/kg (in dogs and cats) or 200 to 400 µg/kg (in guinea pigs and rabbits) induces a sedative effect which appears in 2 to 10 minutes after intramuscular (i.m.) administration or in 0.5 to 1 min. after intravenous (i.v.) administration. Both the strength and the duration of the effects are clearly dose dependant. Higher doses have a hypnotic effect during which the animals do not react to external stimuli such as sounds, pain etc. The duration of the effect is about 1 to 4 hours in dogs and 0.5 to 2 hours in cats. Sedation is accompanied by an analgesic effect, especially at higher doses. This compound possesses both a sedative and an analgesic effect, which are clearly superior to those of xylazine, which is a known compound commonly used as sedative in the treatment of small animals. The following test data illustrate the invention. The tests were carried out using six beagle dogs per group. The study was carried out using a cross-over-design. Different doses of compound (I) were given i.m. or i.v.. The reactions observed were compared to those obtained by xylazine.

Claims: The use of 4-[(α-methyl)-2,3-dimethylbenzyl]imidazole for the manufacture of a medicament for use in veterinary therapy of small mammals as a sedative/analgesic agent. The use according to claim 1 for the manufacture of a medicament for use in therapy as a sedative/analgesic agent in dogs, cats, guinea pigs and rabbits.

Inventors: KARJALAINEN, ARTO JOHANNES, KURKELA, KAUKO OIVA ANTERO, VAHA-VAHE, ANTTI TAPANI, VAINIO-KIVINEN, OUTI MARITTA, VIRTANEN, RAIMO EINARI
Applicants: ORION-YHTYMAE OY
Application year: 1985
Main classification: A61K31
IPC codes: C07D233, A61P25, A61K31