Esketamine , also known as ( S ) - ketamine or S () - ketamine and sold under the brand name Ketanest and Ketanest S among others, are general anesthesia and dissociative hallucinogens. This is an S () enantiomer of ketamine, which is the same anesthetic and dissociative. This is given by intravenous infusion.
Esketamine acts primarily as a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist. It also acts to some extent as a dopamine reuptake inhibitor but, unlike ketamine, does not interact with sigma receptors.
Esketamine was introduced for medical use in 1997. In addition to its anesthetic effects, the drug exhibits properties as a rapid-acting antidepressant, and is being developed for such use. In November 2017, Phase III has completed a Phase III trials for treatment-resistant depression (TRD) in the United States, with results to be announced in the second quarter of 2018. Johnson & Johnson plans to submit a New Drug Application (NDA) for Administration and Medicines (FDA) for approval by 2018. It can be approved as soon as early 2019.
Video Esketamine
Medical use
Eskethamine is a general anesthetic and is used for the same indication as ketamine. Such uses include induction of anesthesia in high-risk patients such as patients with hemorrhagic shock, anaphylactic shock, septic shock, severe bronchospasm, severe liver insufficiency, cardiac tamponade, and constrictive pericarditis; anesthesia in the cesarean section; use of some anesthesia on burns; and as a supplement to regional anesthesia with incomplete nerve blocks.
Maps Esketamine
Pharmacology
Esketamine is about twice as strong as an anesthetic as is the racemic ketamine. This is removed from the human body faster than arketamin ( R (-) - ketamine) or racemine ketamine, although arketamin slows elimination.
Numerous studies have shown that esketamin has pharmacological actions that are more medically beneficial than arketamine or rasemic ketamine. However, in mice found that the effect of rapid antidepressants from arketamine is greater and lasts longer than esketamine. Thus, as antidepressants, the opposite has been stated ("R ketamine appears to be a potent antidepressant and is safe relative to S ketamine", "(2R, 6R) -HNK (hydroxynorketamine), major metabolites of (R) - ketamine", "R- ketamine as a durable antidepressant compared to rapastinel ").
Esketamine inhibits dopamine transport eight times more than arketamin. This increases the activity of dopamine in the brain. At doses that cause the same intensity of effect, esketamine is generally considered more pleasurable by the patient. Patients also generally restore mental function more quickly after being treated with pure esketamine, which may be a result of the fact that it is cleared of their system faster. However this is contrary to R-ketamine which has no psychotomimetic side effects.
Esketamine has an affinity for PCM receptor binding sites of NMDA 3 to 4 times higher than arkethamine. Unlike arketamine, esketamine does not significantly bind sigma receptors. Esketamine increases glucose metabolism in the frontal cortex, while arketamine lowers the glucose metabolism in the brain. This difference may be responsible for the fact that esketamine generally has a more dissociative or hallucinogenic effect while arketamine is reported to be more relaxed. However, other studies found no difference between racemic and (S) -ketamin on the patient's alert level. The interpretation of these findings is complicated by the fact that ketamic racemates comprise 50% (S) -ketamin.
History
Esketamine was introduced for medical use in Germany in 1997.
Society and culture
Common names
Esketamine is the generic name of the drug and INN and BAN , while esketamine hydrochloride is BANM . It is also known as S () - ketamine , (S) -ketamin , or (-) - ketamine , as well as by the developmental code name < i> JNJ-54135419 .
Brand name
Esketamine is marketed under the brand name Ketanest, Ketanest S, Ketanest-S, and Keta-S (animals) among others.
Availability
Esketamine is marketed in Europe, including in Austria, Denmark, Estonia, Finland, Germany, Netherlands, Norway, Slovenia, Sweden, and Switzerland.
Research
Depression
Similarly for ketamine, esketamine shows a profile as a fast-acting antidepressant. Thus, currently being developed by Johnson & amp; Johnson in a nasal spray formulation under the name development code JNJ-54135419 for the treatment of major depressive disorder (MDD). These drugs are being studied specifically for use in combination with oral antidepressants in patients with TRD who are unresponsive to treatment. In June 2017, it was in Phase III clinical trials for this indication, with six ongoing trials. Esketamine has received a breakthrough appointment of the FDA for two-time depression, specifically for TRD in November 2013 and for MDD with an accompanying suicide idea in August 2016. It has been said recently, recently that esketamine appears to be the closest novel and fast-acting antidepressant for approval for the treatment of depression.
See also
- List of antidepressants studied
References
External links
- Esketamine - Johnson & amp; Johnson - AdisInsight
Source of the article : Wikipedia
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