Интересно, как обычно на этом блоге! Статья с http://scienceblogs.com/corpuscallosum/2009/09/iloperidone_approved_for_treat.php?utm_source=combinedfeed&utm_medium=rss
The new drug is called iloperidone; the brand name in the USA will be Fanapt. It is yet another antipsychotic that blocks D2 and 5HT2 receptors. Although there is no universally accepted way of classifying drugs into families, it will be referred to as an atypical or second-generation antipsychotic. This designation will indicate a loose kind of similarity to risperidone, aripiperazole, ziprasidone, quetiapine, olanzapine, clozapine, and paliperidone.
It turns out that there is a Wikipedia page for iloperidone. It is not one of the better pages on Wikipedia.
Iloperidone is a monoamine directed towards acting upon and antagonizing specific neurotransmitters.
Iloperidone does act upon the transmitter. It blocks the receptor, which causes the transmitter to be ineffective, or less effective, at transmitting whatever message it otherwise would have transmitted.
There are several other quibbles I have with the Wikipedia page. If I were unemployed, I would edit it. But it is going to take a lot of work.
Anyway, I could write the kind of blog post that I usually have written when potentially-interesting new drugs come out. But it turns out that there is already a good, concise article in an open-access journal. It says all the things I would have said.
Iloperidone for schizophrenia
Peter J. Weiden, MD, and Jeffrey R. Bishop, PharmD, BCPP
Current Psychiatry Online
Vol. 8, No. 9 / September 2009
Iloperidone is a second-generation (atypical) antipsychotic the FDA approved in May 2009 for treating acute schizophrenia in adults (Table 1). Iloperidone is not a derivative (metabolite, isomer, or different formulation) of any other antipsychotic. Clinical trials have shown that iloperidone is efficacious and suggest that for some patients its side-effect profile may be more favorable than that of other antipsychotics.
It is expected to be available later this year. It is not possible for me, or anyone else, to say exactly when this will be.
The high points are: oral bioavailability 95%, half-life about 18 hours, protein binding about 95%, high affinity for D2 and 5HT2A, low for H1, minimal for muscarinic, and moderate for NEα1. The cost will be too high, but I don't know exactly how high. The manufacturer, Vanda Pharmaceuticals, reportedly is working on a long-acting injectable product.
The one sort of interesting thing has to do with the alpha-1 antagonism. This is a nuisance sometimes, because it can cause orthostatic hypotension (dizziness upon standing up, due to drop in blood pressure). This is a side effect, which may or may not happen in a given individual. It is potentially an adverse effect.
Prazosin is an antihypertensive drug that blocks alpha-1 receptors. Prazosin has been used, off-label, to reduce nightmares in persons with PTSD.
Could iloperidone have a similar effect? If so, it would be a side effect, but not an adverse effect. It would be a beneficial side effect. It remains to be seen whether this will turn out to be the case. In general, it is tricky to anticipate clinical effects, based upon the in vitro pharmacology of a drug, when it comes to the effects in the brain.
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