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Typical antipsychotics (also known as major tranquilizers, and first generation antipsychotics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia). Typical antipsychotics may also be used for the treatment of acute mania, agitation, and other conditions.
The difference between first- and second-generation antipsychotics is a subject of debate. The second-generation antipsychotics are generally distinguishable by the presence of 5HT2A receptor antagonism and a corresponding lower propensity for extrapyramidal side effects compared to first-generation antipsychotics. [15]
First generation antipsychotics are used to treat schizophrenia and are often accompanied by extrapyramidal side effects. [1] They inhibit dopaminergic neurotransmission in the brain by blocking about 72% of the D2 dopamine receptors. [15] They can also block noradrenergic, cholinergic, and histaminergic activity. [15]
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These side effects are serious and some of them are permanent, and many remain a crucial concern for companies and healthcare professionals and substantial efforts are being encouraged to reduce the potential risks for future antipsychotics through more clinical trials and drug development.
Neuroleptic malignant syndrome (NMS) is a rare [5] [6] but life-threatening reaction that can occur in response to antipsychotics (neuroleptic) or other drugs that block the effects of dopamine. [ 1 ] [ 7 ] Symptoms include high fever , confusion, rigid muscles, variable blood pressure, sweating, and fast heart rate. [ 1 ]
Second-generation antipsychotics, including risperidone, are effective in the treatment of manic symptoms in acute manic or mixed exacerbations of bipolar disorder. [25] [26] [27] In children and adolescents, risperidone may be more effective than lithium or valproate, but has more metabolic side effects. [28]
Penfluridol (Semap, Micefal, Longoperidol) is a highly potent, first generation diphenylbutylpiperidine antipsychotic. [2] It was discovered at Janssen Pharmaceutica in 1968. [ 3 ] Related to other diphenylbutylpiperidine antipsychotics, pimozide and fluspirilene , penfluridol has an extremely long elimination half-life and its effects last for ...