PENFLURIDOL

Product Description

Penfluridol tablets(Semap,Micefal,Longoperidol) is a highly potent, first generationdiphenylbutylpiperidineantipsychotic. It was discovered atJanssen Pharmaceutica in 1968.Related to other diphenylbutylpiperidine antipsychotics,pimozideandfluspirilene, penfluridol has an extremely long elimination half-life and its effects last for many days after single oral dose. Its antipsychotic potency, in terms of dose needed to produce comparable effects, is similar to bothhaloperidoland pimozide. It is only slightlysedative, but often causesextrapyramidalside-effects, such asakathisia,dyskinesiaeand pseudo-Parkinsonism.

Penfluridol is indicated for antipsychotic treatment of chronicschizophreniaand similarpsychotic disorders, it is, however, like most typical antipsychotics, being increasingly replaced by theatypical antipsychotics. Due to its extremely long-lasting effects, it is often prescribed to be taken orally as tablets only once a week (q 7 days). The once-weekly dose is usually 1060mg. A 2006systematic review examined the use of penfluridol for people with schizophrenia.

Typical antipsychotics(also known asfirst generation antipsychotics, orFGAs) are a class ofantipsychoticdrugs first developed in the 1950s and used to treatpsychosis(in particular,schizophrenia). Typical antipsychotics may also be used for the treatment of acute mania, agitation, and other conditions. The first typical antipsychotics to come into medical use were thephenothiazines, namelychlorpromazinewhich was discoveredserendipitously. Another prominent grouping of antipsychotics are thebutyrophenones, an example of which would behaloperidol. The newer, second-generation antipsychotics, also known asatypical antipsychotics, have largely supplanted the use of typical antipsychotics as first-line agents due to the higher risk of movement disorders in the latter.

Both generations of medication tend to block receptors in the brain’sdopamine pathways, but atypicals at the time of marketing were claimed to differ from typical antipsychotics in that they are less likely to causeextrapyramidal symptoms(EPS), which include unsteadyParkinson’s disease-type movements,internal restlessness, and other involuntary movements (e.g.tardive dyskinesia, which can persist after stopping the medication). More recent research has demonstrated the side effect profile of these drugs is similar to older drugs, causing the leading medical journalThe Lancet to write in its editorial “the time has come to abandon the terms first-generation and second-generation antipsychotics, as they do not merit this distinction.”While typical antipsychotics are more likely to cause EPS, atypicals are more likely to cause metabolic side effects, such asweight gainand increase the risk fortype II diabetes.
Source: Wikipedia

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