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Less painful all around

People can often become very anxious when they need to visit the vet and worried that their pet will find the experience unpleasant as well. Orion’s Dexdomitor®, a new-generation sedative and analgesic, helps veterinarians handle and treat animals more easily, making things easier for animals and people alike.
Orion Corporation

Dexdomitor®, which uses dexmedetomidine as its active ingredient, is the latest addition to Orion’s family of alpha2-adrenoceptor agonists used in veterinary medicine. Designed for the sedation, analgesia, and preanesthesia of small animals such as dogs and cats, the product is now being launched in key global markets as a successor to Domitor® (medetomidine), Orion’s first-generation sedative for small animals.

Dexdomitor® differs from Domitor® in that its active ingredient contains only the pure and active form of the molecule. The same compound is used in Orion’s Precedex®, a sedative for intensive care patients. The active ingredient in Domitor® – medetomidine – is a molecule that contains mirror images of itself, known as enantiomers. The right-handed enantiomer, dexmedetomidine, has clinically important sedative, analgesic, and preanesthetic effects, whereas the left-handed enantiomer, levomedetomidine, has no sedative or analgesic properties.

The pure form used in Dexdomitor® makes the drug more predictable and its effects simpler to control. The fact that Dexdomitor® contains only half the amount of the active ingredient of Domitor® makes life easier for animals and veterinarians alike. This places less of a burden on an animal’s metabolism, and they tend to recover faster and are less woozy after operations.

Inserting an intravenous catheter would be very difficult or impossible without first sedating an animal. Mikael Granholm, seen here, uses Dexdomitor® for sedating and anaesthetising dogs and cats at his clinic in Raisio in Finland.

Pure compounds are better

The combined use of several sedative substances has become more and more commonplace in recent years, bringing benefits such as smaller total doses and a safer overall anaesthetic protocol. Multimodal anaesthesia using up to six different drugs administered simultaneously works best with pure compounds, as this reduces the risk of adverse drug interactions.

No fewer than 11 separate studies – primarily in Germany, France, Britain, and the US, and involving over 1,000 dogs and cats – were conducted with Dexdomitor® to show that the drug formulation, which includes only the active enantiomer, is therapeutically better than one containing both enantiomers.

These indicated that dexmedetomidine has a shorter duration of action and a better safety profile than other alpha2-agonists. One clinical trial on cats, for example, confirmed that the animals recovered from anaesthesia more rapidly when Dexdomitor® was used as a premedication prior to ketamine anaesthesia. Dexdomitor® was also shown to exhibit fewer side-effects than xylazine, a much older and less selective alpha2-agonist.

Used at relatively low doses, Dexdomitor® typically results in cooperative sedation, making it easier for vets to interact with animals, while still reaping the product’s analgesic effects.

The clinically important sedative, analgesic, and pre-anaesthetic effects in Dexdomitor® are provided by dexmedetomidine, the right-handed enantiomer of medetomidine. The left-handed enantiomer is inactive.

The right enantiomer

Many pharmaceuticals used today are racemic mixtures, containing equal amounts of left- and right-handed enantiomers. Because a pharmaceutical compound binds to its target molecule on the basis of physical shape as well as chemical properties, only one of the enantiomers involved normally functions as the active ingredient. The other enantiomer either has no effect at all or, in some cases, may have an adverse one.

Even when an enantiomer does not have any clinically relevant or useful effects, it can still place an unnecessary burden on the patient’s metabolism – and this is why modern drug development focuses on products containing only the pure, active enantiomer.

 

Already used in over 30 countries

Dexdomitor® has been approved in Europe and the US for use as a sedative and analgesic for dogs and cats to facilitate examinations and minor surgical procedures at veterinary clinics. Typical applications include grooming, bathing and nail clipping, oral and ear examinations, bandage changes, and skin biopsies.

The ability to use Dexdomitor® as a preanesthetic prior to general anaesthesia is a particular plus when dealing with dogs. In Europe, the drug has also been approved for use in conjunction with butorphanol on dogs for deeper sedation and analgesia when more painful procedures are expected; while cats benefit from vets being able to use Dexdomitor® as a preanesthetic prior to ketamine anaesthesia.

The global marketing and sales of Dexdomitor®, which is already in use in over 30 countries worldwide, is being shared by Orion and its partner, Pfizer Animal Health; with Orion covering Finland and the other Nordic countries and Pfizer the rest of the world, with the exception of Japan.

> Anne Allo
(Published in HighTech Finland 2009)