Antipsychotics Tranquilizers

In general, antipsychotics (tranquilizers) are primarily employed for the treatment of symptoms in mental diseases, their overall influenee being to free the mind from passion or disturbance and thus elam the mind i.e., they cause sedation without indueing sleep. 

Tranquilizers are drugs essentially used in the management and, treatment of psychoses and neuroses. They specifically exert their action on the lower brain areas to produce emotional calmness and relaxation without appreciable hypnosis sedation euphoria or motor impairment. In addition many of these drugs also display clinically beneficial actions, for instance skeletal muscle relaxants, antihypertensive, antiemetic and antiepileptic properties. 

One school of thought even suggested that these drugs may be divided into two categories, namely major tranquilizers (for psychoses) and minor tranquilizers (for neuroses) however, such an arbitrary categorization stands invalid because of their overlaping characteristic features. 

More recently antipsychotics may be defined as— drugs which ameliorate mental aberrations that are invariably characteristic feature of the psychoses. 

Positive symptoms of psychoses essentially comprise of a host of disorders, such as mild behavoural changes anxiety, delusions, hallucinations, and sclizzophrenias. Negative symptoms are usually designated by cognitive deficits, social withdrawl, apathy, and anhedonia. 

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Antipsychotic tranquilizers Increased sedation. Variable effects on respiratory depression. Accentuation of cardiovascular effects (antimuscarinic and -blocking actions). 

D-TR (4), 5HT-TR (40 nM), [T synaptic 5HT antiaddictive, anticonvulsant, CNS stimulant, hallucinogen] VMA-TR [antihypotensive, antipsychotic, tranquillizer] MA-TR, VM-TR VMAT1 (adrenal chromaffin granule), VMAT2 (brain, adrenal), I.-type Ca2+ CH-dependent NE release (6) (MDR-TR) [antihypertensive, antipsychotic, carcinogen, tranquillizer, neuroleptic CNS antidepressant] GABA-TR... 

Further chemical modification of the phenylpiperidine moiety has proven unusually fruitful in producing medicinal agents that affect the central nervous system. First, a series of compounds loosely related to the reversed meperidines produced several drugs with important antipsychotic activity. Further discussion of this pharmacologic activity, often referred to as major tranquilizer activity, will be found in the section on phenothiazines. The group led by Janssen took advantage of the chemistry of the... 

Chlorpromazine (33) can probably be considered the prototype of the phenothiazine major tranquilizers. The antipsychotic potential of the phenothiazines was in fact discovered in the course of research with this agent. It is of note that, despite the great number of alternate analogs now available to clinicians, the original agent still finds considerable use. The first recorded preparation of this compound relies on the sulfuration reaction. Thus, heating 3-chlorodiphenylamine (30) with sulfur and iodine affords the desired phenothiazine (31) as well as a lesser amount of the isomeric product (32) produced by reaction at the 2 position. The predominance of reaction at 6 is perhaps due to the sterically hindered nature of the 2 position. Alkylation with w-C3-chloropropyl)dimethylamine by means of sodium amide affords chlorpromazine (33). ... 

Major tranquilizer. A drug useful in the control of schizophrenia. Also referred to as neuroleptic or antipsychotic. 

Chlorpromazine had been shown to produce a tranquil state in animals and since it had a similar effect in humans it became known as a major tranquiliser but the term is rarely used today. Sometimes the drugs used to treat schizophrenia are called anti-psychotics but more commonly neuroleptics. Leptic means to activate (take hold of) and in animals these compounds produce a state of maintained motor tone known as catalepsy. This is an extrapyramidal effect and in schizophrenics the neuroleptics can cause a number of extrapyramidal side-effects (EPSs) including Parkinsonism. The new term neuroleptic is unsatisfactory as a description of clinically useful drugs. It really describes a condition (catalepsy) seen in animals and is more indicative of a compound s ability to produce EPSs than to treat schizophrenia. Antipsychotic is more descriptive but could imply a more general efficacy in psychoses than is the case. It would seem more appropriate to call a drug that is used to treat schizophrenia an antischizophrenic just as we use the terms antidepressant or antiepileptic irrespective of how the drug works. Despite such personal reservations, the term neuroleptic will be used in this text. 

As a group, these medications have been known by several names. They have been called major tranquilizers. This is not altogether inaccurate these medications do calm or tranquilize. Physicians still use this name sometimes, especially when they re reluctant to use the word psychotic in a discussion with a new patient or his/her family. These medications have also been called neuroleptic, literally meaning seize the nerve cell, in the original Greek. This term is derived from the potential for the medications to cause extrapyramidal side effects. Finally, and most accurately we contend, these medications are called antipsychotics. 

Typical Antipsychotics. The high potency antipsychotic haloperidol (Haldol) and low potency antipsychotics chlorpromazine (Thorazine) and thioridazine (Mellaril) have also been used to treat ADHD. Although they provide a tranquilizing effect (they are in fact sometimes called major tranquilizers ) that can reduce hyperactivity and impulsivity, antipsychotics remain markedly less effective than stimulants. Antipsychotics do not noticeably improve attention in patients with ADHD, and at this time the typical antipsychotics cannot be considered a reasonable monotherapy in uncomplicated ADHD. 

Antipsychotics. Antipsychotic medications are also called major tranquilizers. It is for the tranquilizing effect that they have been used to treat agitation. The earliest antipsychotics, especially thioridazine (Mellaril), proved to be effective in reducing agitation however, this comes at the price of further impairing cognition due to its profound anticholinergic effects. 

Benzodiazepines. These medications are also known as minor tranquilizers. In general, they have been found less effective than antipsychotics in treating agitation over the long term. However, their relatively quick onset of action makes them effective for acute episodic agitation. 

Carbamazepine is more widely used for treating chronically agitated dementia patients. Its onset of action is delayed by several days to a couple of weeks therefore, other tranquilizing medications such as antipsychotics may need to be used when first starting carbamazepine. Carbamazepine doses have problematic side effects that require blood monitoring, and it also interacts with many medications. 

Delusions/Psychosis. Demented patients who are acutely psychotic and agitated should be treated in much the same manner as demented patients with delirium. Low doses of a high potency conventional antipsychotic like haloperidol were once preferred. This was mainly because it can be given both orally and by injection. In recent years, the atypical antipsychotic ziprasidone, which is now also available in oral and injectable forms, has superseded haloperidol as the preferred agent when treating the acutely psychotic and agitated patient with dementia. As previously noted, ziprasidone affords the same tranquilizing benefit as haloperidol, it can now be administered via injection when necessary, and it avoids the problematic extrapyramidal symptoms of haloperidol to which patients with dementia are often keenly sensitive. 

Nevertheless, patients with severe BPD may be especially vulnerable to repeated psychotic decompensation and therefore arguably need prophylactic treatment with an antipsychotic. In addition to their proven ability to treat psychotic symptoms, antipsychotics also have tranquilizing effects that can counteract impulsivity and mood lability. They do so while avoiding the potential disinhibition that can be caused by benzodiazepines. 

Antipsychotics are drugs that have a specific sedative effect, and which improve the attitude and calm the behavior of psychotic patients. They do not cause dependence, and have been proposed for treating psychotic disorders (elimination of psychotic symptomatology— delirium, hallucinations) and schizophrenic patients. Drugs of this group are also frequently referred to as neuroleptics. The term major tranquilizer was used previously to distinguish them from minor tranquilizers/anxiolytics. 

Some patients have attacks of confusion even without taking the substances for variable periods after excessive, so called flash-backs . The use of tranquillizers and antipsychotics may be needed. 

Antipsychotic medications, previously referred to as major tranquilizers or neuroleptics, are effective for the treatment of a variety of psychotic symptoms—such as hallucinations, delusions, and thought disorders—regardless of etiology. The term major tranquilizer is a misnomer because sedation is generally a side effect, and not the principal treatment effect. Similarly, the term neuroleptic is based on the neurological side effects characteristic of older antipsychotic drugs, such as catalepsy in animals and extrapyramidal side effects (EPS) in humans. 

Antipsychotics for the symptomatic treatment of schizophrenia and states of agitation occurring in other psychiatric syndromes these medicines are also occasionally called neuroleptics or major tranquillizers. 

In Chapter 1 of this book, psychopharmaceuticals were introduced as effective medicines that primarily have a symptomatic action but are problematic in several respects. Antipsvchotics can cause serious side effects and antidepressants often exert their therapeutic effects only after a delay of weeks and in many cases have unpleasant side effects. With anxiolytics, hypnotics and, in particular, psychostimulants, there are problems with habituation and the potential of dependency. It is therefore not surprising that psychopharmaceuticals do not enjoy a very high reputation among many doctors and the general public (see Box 8.1) and have been given names such as chemical strait-jackets for the older neuroleptics (Szasz, 1957) or chemical blinkers for the mind for tranquillizers. Elomaa (1993) even posed the question of whether the long-tom use of conventional antipsychotics should be considered a crime against humanity. 

Antipsychotic drugs or major tranquillizers used in all types of psychosis mainly schizophrenia. 

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