Recent Developments in the Treatment of People with Schizophrenia

By Robert W. Buchanan, MD

[Fall 2007; Vol. 34, No. 1; Pg 4, 10-11]

Over the past decade, the recovery movement has generated a growing appreciation of the need to improve the treatment of people with schizophrenia.  It emphasized that we need to move the focus of therapeutic interventions beyond the treatment of positive symptoms,  to enhance social and vocational functional role performance and outcomes.  There are multiple definitions of “recovery”.  They range from an emphasis on symptom amelioration and normative adaptation and functioning in the community to a focus on the “process” of recovery.  Its interventions impact upon not only external indicators of recovery, such as occupational functioning, but also enhance the sense of hope, autonomy/empowerment, and adaptation to the illness of the person with schizophrenia.

There are a number of roadblocks to the path of recovery. One is the lack of effective interventions for many of the primary and secondary problems that afflict people with schizophrenia.  Over the past 50 years, the major emphasis of drug development has been on “positive” psychotic symptoms, which has led to the development of a number of antipsychotic drugs with largely overlapping efficacy profiles.  They tend to be moderately effective for positive symptoms, but have limited effects on negative symptoms and cognitive impairments.  These limitations are critically important, because positive symptoms have little long-term impact on functional outcomes.  The Maryland Psychiatric Research Center has spent the last 30 years dedicated to the development of novel pharmacological treatments for not only positive psychotic symptoms, but also for the primary determinants of poor functional outcome: persistent negative symptoms and cognitive impairments, (as well as  co-occurring medical and psychiatric conditions). 

The following is a brief summary of some of our recent efforts to help develop better treatments..
Although conventional antipsychotics (e.g. fluphenazine , haloperidol  and perphenazine)  and second generation antipsychotics (e.g. risperidone , olanzapine ,quetiapine , ziprasidone , and aripiprazole)  are equally effective in the treatment of positive symptoms in treatment-responsive people, there are few options for those who fail to respond.  In fact, only clozapine has been shown to be effective in people with treatment-resistant positive symptoms, an observation that was recently replicated in the CATIE study.  The question that arises is,”What about the 40 – 60% of people who fail to adequately respond to clozapine?”  The most common practice is to add a second antipsychotic-- a practice for which there is little evidence.  We are currently in the last year of the largest study ever designed to evaluate the efficacy and safety of adding risperidone to clozapine in those   people who have not had an adequate response to clozapine alone.  The study will be the largest one yet.

Many studies have demonstrated the critical relationship between persistent (or enduring) negative symptoms and cognitive impairments, and poor social and vocational role outcome and performance.  We designed a series of investigations to evaluate various pharmacological approaches for the treatment of persistent negative symptoms. A number of studies in inpatients and outpatients with schizophrenia have shown that neither clozapine nor olanzapine is effective for these symptoms.  Rather, we believe the benefit of these drugs for negative symptoms is limited to their beneficial effect on depressive or extrapyramidal signs. We examined the efficacy of two drugs, D-cycloserine and glycine, which enhance glutamatergic function and have been shown in small pilot studies to improve negative symptoms when added to antipsychotics.  In the largest study to date, we found that these agents had limited effectiveness for persistent negative symptoms. 

The results of these and other studies have clearly demonstrated the limitations of currently available treatments, including second generation antipsychotics, and have led to ongoing NIMH  support for an  investigation of alternative approaches to the treatment of negative symptoms.  Although we continue to be interested in glutamatergic mechanisms, we are currently assessing the efficacy of rasagiline, a selective MAO-B inhibitor.  It is hypothesized that decreased dopamine in the prefrontal cortex plays a role in the pathophysiology of negative symptoms. The central role that the MAO-B enzyme plays in the deactivation of the dopamine signal in the prefrontal cortex may be important, too.

Cognitive impairments play a major role in determining functional outcome.  People with schizophrenia often have a broad range of cognitive impairments, including abnormalities of attention/information processing, problem-solving, processing speed, verbal and visual learning and memory, and working memory. Despite appropriate treatment, many people with schizophrenia continue to exhibit pronounced cognitive impairments, which has led to the investigation of adjunctive co-therapy of these impairments.  In particular, we have been interested in the potential benefit of drugs that act through the cholinergic system.  We have conducted a series of studies that have demonstrated that acute nicotine is effective in reversing eye-tracking, sensory gating and visual memory impairments in people with schizophrenia.  We have recently completed a large randomized clinical trial of adjunctive galantamine, an acetylcholinesterase inhibitor and allosteric modulator of nicotinic receptors.  We found that it had selective benefits for processing speed and verbal memory-- both cognitive processes linked to functional outcome.  We have also been involved in NIMH- sponsored efforts to facilitate the development of new treatments.  The Measurement and Treatment Research to Improve Cognition in Schizophrenia (MATRICS) and Treatment Units for Research on Neurocognition and Schizophrenia (TURNS) initiatives have stimulated efforts to develop new targets.  The TURNS project, a consortium of seven academic sites, is charged with the selection and evaluation of new pharmacological agents, which may help in  the treatment of cognitive impairments.  We are currently conducting three “proof of concept” studies to evaluate novel GABAergic, nicotinic, and serotonergic mechanisms.

People with schizophrenia are also often afflicted with multiple co-occurring disorders.  These include medical disorders secondary to the drugs that are used to treat their condition, and also substance abuse disorders.  These further complicate their treatment  and their efforts to recover.  The advent of second-generation antipsychotics and the increased incidence of weight gain, metabolic abnormalities and concern about cardiac complications, combined with the recent documentation of the poor quality of medical care provided to people with schizophrenia, has led to an increased awareness. We need: 1) more effective strategies for ensuring sufficient medical monitoring and 2) interventions for the treatment of co-occurring medical conditions.  Should we encourage people with schizophrenia who have gained weight or have developed hyperlipidemias or glucose dysregulation  to switch to a different antipsychotic, or treat the secondary medical condition?  We are currently conducting a study on the efficacy of adjunctive rimonabant, a cannabinoid (CB)1 antagonist, for weight gain and metabolic abnormalities.

The primary focus of our efforts to develop treatments for co-occurring substance use disorders has been on nicotine dependence.  We have conducted a pilot study and clinical trial examining the efficacy of combining bupropion and group therapy.  We have documented the efficacy of the group therapy component and have also shown that bupropion (compared to placebo) provides additional benefit in helping people with schizophrenia to stop smoking cigarettes.  However, only 22% of subjects did quit smoking by the end of the 14-week study.  This cessation rate is considerably lower than what is seen in smoking cessation studies with controls. The results suggest that a different approach may be required in people with schizophrenia.  Therefore, we have designed a study to examine the efficacy of varenicline, which is a partial agonist of the "4$2 nicotinic receptor, which may be abnormal in schizophrenia. Thus, it may serve to reverse an underlying pathophysiological impairment as well as treat nicotine dependence.

Although alcohol abuse is a major problem, pharmacological interventions that benefit primary alcohol abusers have not been widely studied in schizophrenia.  There are three FDA-approved medications for treatment of alcohol use disorders: disulfiram, naltrexone, and acamprosate.  There is reason to believe that acamprosate may provide a unique benefit to people with schizophrenia and co-occurring alcohol use disorders. It may enhance glutamatergic functioning when the system is under-stimulated and decrease glutamatergic functioning when  it is over-stimulated.  We plan to assess its safety and tolerability  in people who have schizophrenia.

In conclusion, we hope to enter a new era of pharmacological treatment of schizophrenia.  Recent advances in molecular biology have markedly increased our understanding of how the brain works and what may be wrong with it in people who suffer from schizophrenia.  If these recent advances can be translated into novel drugs with mechanisms that extend beyond simple dopamine receptor blockade,  we should be able to offer our patients more effective treatments that target those aspects of their illness that  most importantly determine whether they will really recover.