Typical antipsychotic

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Typical antipsychotics (sometimes referred to as conventional antipsychotics, classical neuroleptics or major tranquilizers) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia), and are generally being replaced by atypical antipsychotic drugs. Typical antipsychotics may also be used for the treatment of acute mania, agitation, and other conditions. The first typical antipsychotics to enter clinical use were the phenothiazines.

Contents

Traditional antipsychotics are broken down into low-potency and high-potency classifications:

Potency Examples Side effects
high-potency fluphenazine and haloperidol more extrapyramidal side effects (EPS) and less histaminic (e.g. sedation), alpha adrenergic (e.g. orthostasis) and anticholinergic (e.g. dry mouth)
low-potency chlorpromazine less EPS but more H1, alpha1, and muscarinic

Some of the high-potency antipsychotics have been formulated as the decanoate ester (e.g. fluphenazine decanoate) to allow for a slow release of the active drug when given as a deep, intramuscular injection. This has the advantage of providing reliable dosing for a person who doesn't want to be drugged. Depot injections can also be used for involuntary community treatment patients to ensure compliance with a community treatment order when the patient would refuse to take daily oral medication. Depot preparations were limited to high-potency antipsychotics so choice was limited . It is therefore preferable to use oral medications if the cooperation and compliance of the patient can be assured.

The oldest depots available were haloperidol and fluphenazine, with flupentixol and zuclopenthixol as more recent additions. All have a similar, predominantly extrapyramidal, side effect profile though there are some variations between patients. More recently a long acting preparation of the atypical antipsychotic risperidone has become available, offering a new choice. Risperidone still has a higher incidence of extrapyramidal effects than some other drugs available however.

Side effects vary among the various agents in this class of medications, but common side effects include: dry mouth, muscle stiffness, muscle cramping, tremors, EPS and weight-gain. EPS is a cluster of symptoms consisting of parkinsonism, dystonias, and akathisia. Anticholinergics such as benztropine and diphenhydramine are commonly prescribed to treat the symptoms of EPS.

There is a significant risk of the serious condition tardive dyskinesia developing as a side effect of typical antipsychotics. The risk of developing tardive dyskinesia after chronic typical antipsychotic usage varies on several factors, such as age and gender. The commonly reported incidence of TD among younger patients is about 5% per year. Among older patients incidence rates as high than 20% per year have been reported. The average prevalence is approximately 30%.[1] There are no treatments that have consistently been shown to be effective for the treatment of tardive dyskinesias, however branched chain amino acids, melatonin, and vitamin E have been suggested as possible treatments. The atypical antipsychotic clozapine has also been suggested as an alternative antipsychotic for patients experiencing tardive dyskinesia. Tardive dyskinesia may reverse upon discontinuation of the offending agent or it may be irreversible.

Neuroleptic malignant syndrome, or NMS, is a rare, but potentially fatal side effect of antipsychotic treatment. NMS is characterized by fever, muscle rigidity, autonomic dysfunction, and altered mental status. Treatment includes discontinuation of the offending agent and supportive care.

The role of typical antipsychotics has come into question recently as studies have suggested that atypical antipsychotics may increase the risk of death in elderly patients. A retrospective cohort study from the New England Journal of Medicine on Dec. 1, 2005 showed an increase in risk of death with the use of typical antipsychotics that was on par with the increase shown with atypical antipsychotics.[2] This has led some to question the common use of antipsychotics for the treatment of agitation in the elderly, particularly with the availability of alternatives such as mood stabilizing and antiepileptic drugs.

  1. ^ Llorca PM, Chereau I, Bayle FJ, Lancon C (2002). "Tardive dyskinesias and antipsychotics: a review". Eur. Psychiatry 17 (3): 129-38. PMID 12052573. 
  2. ^ Wang PS, Schneeweiss S, Avorn J, et al (2005). "Risk of death in elderly users of conventional vs. atypical antipsychotic medications". N. Engl. J. Med. 353 (22): 2335-41. doi:10.1056/NEJMoa052827. PMID 16319382. 


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