medications
 
 
                                    
Typical (first generation) Antipsychotics



What They Are and Are Not

These antipsychotic medications were the first to become available for the treatment of schizophrenia.  They are also known as conventional antipsychotics, neuroleptics, and “major tranquilizers”.  This later term stems from the fact that early agents in the class, chlorpromazine, mesoridazine and thioridazine) often produced profound sedation.

This term also serves to distinguish them from the class of drugs that we refer to as “minor tranquilizers”.  They are part of a classification of drugs referred to as “sedative-hypnotics”; drugs employed to calm or induce sleep.

Sedative-hypnotics include the “anxiolytic” (anti-anxiety) benzodiazapines:  diazepam (Valium), lorazepam (Ativan) and others; and a number of unrelated medications such as meprobamate (Miltown), methaqualone (Qualude), ethchlorvynol (Placidyl), chloral hydrate (Noctec), hydroxazine (Atarax or Vistaril), buspirone (Buspar) and others).

Some benzodiazapines that are hypnotics (drugs generally used to induce sleep) include flurazepam (Dalmane), temazepan (Restoril) and others.

Another related, but much more dangerous, category is the barbiturates; secobarbital (Seconal) and pentobarbital (Nembutal), used to induce sleep; amobarbital (Amytal) and phenobarbital.  Some are used to treat seizures.  All are particularly dangerous when combined with alcohol.

All of these drugs are unrelated to either class of antipsychotic medications.


Categories

Conventional antipsychotics can be divided into low potency drugs (such as chlorpromazine, mesoridazine and thioridazine) and high potency drugs (such as haloperidal and fluphenazine).  Low potency drugs are less likely to produce EPSE (extrapyramidal side effects) and more likely to produce H1, or histamine, side effects such as sedation; anticholineregic (muscarinic) and alpha1 side effects.  High potency drugs are more likely to produce EPSE, including Tardive Dyskinesia, and less likely to produce histamine, alpha 1 and anticholinergic side effects.

Antipsychotic medications can also be considered based upon their chemical make-up 1. (http://en.wikopedia.org/wiki/Typical_antipsychotic):

aliphatic compounds: the group with the most members, which include chlorpromazine (Thorazine), promazine (Sparine), triflupromazine (Vesprin), and levomeprozine (Nozinan).
piperidines: mesoridazine (Serentil) and thioridazine (Mellaril).
piperazines: fluphenazine (Prolixin), perphenazine (Trilafon), prochlorperazine (Compazine), and trifluoperazine (Stelazine).

Other groups include:

butyrophenones: haloperidal (Haldol).
thioxanthines: thiothixine (Navane).
dihydroindolones: molindone (Moban).
dibenzoxazepines: this is a subclass of tricyclic antipsychotic agents that includes loxapine (Loxitane).
diphenylbutylpiperidine derivatives: pimozide (Orap).

Aliphatic compounds exhibit moderate to strong sedation, moderate autonomic effects (effects on pulse and blood pressure), and moderate EPSE.

Piperidines exhibit strong sedation, strong autonomic effects, and weak EPSE.

Piperazines exhibit weak to moderate sedation, weak autonomic effects, and strong EPSE.


Indications and Treatment Goals

The indications and goals for treatment are similar to those of the atypical antipsychotics.


Mechanism of Action

The mechanism of action is similar to that of atypical antipsychotics with the exceptions that typicals may have less effects on neurotransmitters that affect mood, such as serotonin, and they may be more likely to worsen negative symptoms.


History

These agents began to enter the marketplace in the 1950s.  While clozapine (Clozaril), an atypical antipsychotic, was developed at that time, it did not appear until the 1970s.  Therefore, modern psychiatrists waited for decades for newer antipsychotics, drugs which offered similar beneficial effects, but with more attractive side effect profiles.


1 http://en.wikopedia.org/wiki/Typical_antipsychotic


(Sources: The author’s knowledge base, unless otherwise noted.)______________________________________________________________________

Related Articles:

Atypical (second generation) Antipsychotics

Antipsychotics That Are Not FDA Approved

Medications Used To Treat Side Effects

Should Atypical Antipsychotics Be Abandoned?
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