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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]
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.
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]
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 ]
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 ...
This is the main receptor responsible for the anticholinergic side effects mentioned above. M 3: 25.9: 50: 1848: This receptor is believed to be partly responsible for the metabolic adverse effects of the atypical antipsychotics. σ: 300: 2000: 31.5: All three values are for binding to the guinea pig brain receptors.
It produces significantly less extrapyramidal side effects than most first-generation antipsychotics, likely due to its potent anticholinergic effect. [12] [13] Its use, along with the use of other typical antipsychotics, has been associated with degenerative retinopathies (specifically retinitis pigmentosa). [14]
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