Wednesday, January 28, 2009

NEw schizophrenia medications

NEW SCHIZOPHRENIA DRUGS
Talnetant and Osanetant are both NK3 (neurokinin 3, a neurotransmitter receptor in the brain) antagonists, being independently developed by GlaxoSmithKline and Sanofi-Synthelabo, respectively. Talnetant is in phase II FDA clinical trials, and Osanetant is in phase III. Neurokinin receptors play a role in movement; therefore, both medications may potentially alleviate some of the movement side effects caused by other neuroeptics. Early date for Talnetant, according to a GlaxoSmithKlilne press release, showed that a small subset of patients on a high dose of the drug had a positive response with good tolerability, and a minimum of side effects such as weight gain. Talnetant may also have a beneficial impact on cognitive deficits. Journal articles on the effects of NK3 antagonists (not not on Talnetant or Osanetant specifically) report some positive improvements in subjects with schizophrenia.
Paliperidone ER is the active metabolite of antipsychotic medication Risperdal (risperidone). It fully blocks serotonin receptors, and partially blocks D2 dopamine receptors. It is being developed by Johnson and Johnson. The metabolite may end up beling clinically beneficial for patients who don't respond to convential treatment with risperidone. No research information was found on this specific compound.
RG1068 is a synthetaic human secretin compoundd, developed by Repligen. It has already proven helpful for auatistic patients (the same drug is in phase III trials for treating autism), and Repligen is conducting phase II trials to determine whether it might be useful for treating some of the autistic-type symptoms in schizophrenia patients. Early research indicates preliminary promise for the compound as an adjunct treatment; patients given the drug in placebo-controlled trials show modest, although transient, symptom improvement.
Seromycin (d-cycloserine) is a partial NMDA receptor agonist, or a glutamatergic agent. It acts to enhance glutamate receptor responses in certain areas of the brain. Because esearch has suggesed that glutamate dysfunction may be a cause of negative symptoms, seromycin and other glutamatergic agents are being tested for their therapeutic effects. Early studies with such agents have shown mixed results – some studies show ono effects (although small sample size and high drop-out rates are noted as possible confounding factors), while others indicate that schizophrenia medications. It is in phase III clinical trials.
AMPAkines are a series of related compounds designed to improve memory and cognition. Some compounds designed to improve memory and cognition. Some compounds (notably CX-516 for schizophrenia) are currently in phase II clinical trials. Research indicates that ampakines may help to enhance the effects of typical and atypical antipsychotics, although they may not be therapeutically effective on their own.
Galantimine is a compound that enhances cholinergic function (the activity of acetycholine) in the hippocampal and cortex regions of the brain. Perliminary research shows that it may improve negative and cognitive symptoms of schixophrenia. It is currently in phase II clinical trials to establish effects on cognitive and learning deficits.
Memantine is an NMDA receptor antoganist, designed to address the cognitive symptoms of schizophrenia. Research shows that NMDA hyperactivity in some areas of the brain may cause some of the cognitive dysfunction seen in schizophrenia patients. It is currently in Phase II clinical trails. No further research information was found regarding the compound.
Modafinil, a drug currently used to treat narcolepsy, is now being examined for its potential to improve cognitive symptoms and working memory in schizophrenia patients wit certain genotypes. The mechanism of action is still not entirely clear, although it appears that the medication induces wakefulness through act ivation of sleep-wake centers in the hypothalamus, and increases dopamine levels in the pre-frontal cortex. Modafinil is currently in Phase II clinical trials, to test whether it improves working memory in schizophrenia patients with particular gene variations.
Ocaperidone is a D2 dopamine ant agonist, as well as serotonin antagonist. Due to the dual-action mechanism of the drug, early research reports it to have “haloperidol-like effects” on the positive symptoms of schizophrenia, but with a lower incidence of extrapyramidal side effects (more like the side-effect profile of risperidone). Neuro3d, the France, based developers of the medication, report that they are nearing the end of phase II clinical trials. They expect further results to be released in March or April of this year.
Tolcapone is a COMT gene inhibitor that acts in the midial prefrontal cortex of the brain. Its measurable effects in rat brains include an increase of dopamine neurotransmitter levels in the prefrontal cortex. This medication augments some of the actions of clozapine, and may be helpful for relieving some of the cognitive deficits associated with antipsycotic treatment (esp. working memory deficits). It is currently in Phase II clinical trials.
Http://www.schizophrenia.com/newmeds2004.html

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