What is the structure of Benperidol?

Benperidol is a typical first-generation neuroleptic with the chemical name 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2- a]pyrimidin-4-one. It is a piperazine phenylisoxazole derivative.

Benperidol consists of a central piperazine ring attached at one side to a phenylisoxazole unit and at the other side to a tetrahydropyridopyrimidine. The phenylene ring of the phenylisoxazole is substituted with fluorine at the 6-position. This chemical structure, particularly the phenylisoxazole unit and tetrahydropyridopyrimidine, gives benperidol its dopaminergic properties.

Benperidol binds with high affinity to dopamine D2 receptors in the dopaminergic pathways of the mesolimbic system, mesocortical system and nigrostriatal system. This leads to blockade of postsynaptic dopamine receptors, which in turn reduces dopaminergic neurochemical transmission. This is the primary mechanism by which benperidol exerts its antipsychotic effect.

Although benperidol binds highly to dopamine receptors, it also has moderate affinity for other receptors such as 5-HT2A, muscarinic M1, histamine H1 and noradrenaline α1 receptors. These additional pharmacological properties are responsible for many of the side effects of benperidol such as sedation, muscle twitching and dry mouth.

The complex chemical structure combined with the broad spectrum of activity contributes to the potential benefits of benperidol in treating psychoses such as schizophrenia, but is also causative of its significant side effects. Despite its historical importance, the clinical use of benperidol has been largely replaced today by newer atypical antipsychotics with a more favorable side effect profile.

There are various forms of drugs available, such as tablets or liquids, and each may have a separate patient information leaflet (PIL) for different doses. It is important to refer to the PIL for the specific form and dose of the drug that you have been prescribed.

You can search for further information and PILs on websites such as:

  • The British National Formulary (BNF)
  • Electronic medicines compendium (emc)
  • The National Library of Medicine's DailyMed
  • The Food and Drug Administration (FDA) 
  • Different drug forms like tablets or liquids have specific patient information leaflets (PIL) for various doses. Refer to the PIL for your prescribed drug form and dose.

    Search for PILs on websites like:


    • ANSM (Agence nationale de sécurité du médicament et des produits de santé): ansm.sante.fr


    • AEMPS (Agencia Española de Medicamentos y Productos Sanitarios): aemps.gob.es


    • BfArM (Bundesinstitut für Arzneimittel und Medizinprodukte): bfarm.de


    For questions about your medication:

    • Consult your doctor, a healthcare professional, or a pharmacist


    • Contact SOS Médecins: 3624
    • For mental health support, contact SOS Suicide: 01 45 39 40 00

    Belgium (French)

    Switzerland (French)

    • La Main Tendue: 143
    • Website: 143.ch

    Canada (French)

    • Centre de prévention du suicide du Québec: 1 866 APPELLE (1 866 277-3553)
    • Website: cpsquebec.ca


    • Contact emergency number: 112
    • For mental health support, contact Teléfono de la Esperanza: 717 003 717


    • Contact emergency number: 112
    • For mental health support, contact Telefonseelsorge: 0800 111 0 111 or 0800 111 0 222


    • Contact emergency number: 112
    • For mental health support, contact Telefono Amico: 199 284 284


    • Contact emergency number: 112
    • For mental health support, contact 113 Zelfmoordpreventie: 0800 0113


    • Contact emergency number: 112
    • For mental health support, contact Sos Voz Amiga: 21 354 45 45, 91 280 26 69, or 96 352 46 60

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