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Analogues of Ketamine

总结
Novel ester analogues of ketamine that combine the similar anaesthetic/analgesic properties of ketamine with a much shorter half-life, overcoming ketamine’s major drawbacks
技术优势
The expected medical advantages of short-acting analogues include:
• Short action and reduced adverse effect profile enabling increased use compared to ketamine
• Reduced use of potentially dangerous adjunctive sedatives or hypnotics
• Potential for downstream benefits such as resource savings associated with improved patient recovery times. Some ester analogues show evidence of prolonged analgesic effects, suggesting potential use as non-hallucinogenic analgesic (anti-nociceptive) drugs.

Potential as a rapid-onset antidepressantAlso opportunity to develop analgesics only compounds and compounds for mood disorders.
技术应用
The ketamine esters have wide potential application in the management of both acute (e.g., surgery) and chronic pain, without the drawbacks of ketamine. In the longer term, the analogues may have a new application as anti-depressants.
申请日期
41555
申请号码
PCT/IB2013/059191
其他
Use of ketamine is associated with significant adverse effects that impact on the patient and the healthcare system, the most important of which are its hallucinogenic properties. It has a relatively long elimination half-life (2-3 hours) and so is usually administered together with sedative or hypnotic drugs to try and reduce hallucinations; however, this greatly increases the risk of respiratory depression and loss of the patient’s airway. Therefore, ketamine analogues with much shorter half-lives would be preferred and could avoid the concomitant use of sedatives and hypnotics.
Key advantages of short acting ketamine analogues are anticipated to include:
• Short action and reduced adverse effect profile enables increased use compared to ketamine
• The very rapid recovery would limit the hallucination period to a maximum of 1-2 minutes (compared to 20-120 minutes of hallucinations seen with ketamine)
• Reduced use of adjunctive sedatives or hypnotics, with their potentially dangerous compromisation of airway and breathing
• Potential for downstream benefits such as resource savings associated with improved patient recovery times
ID号码
30165
国家/地区
新西兰

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