Haloperidol and Related Butyrophenones

Janßen, Paul

doi:10.1016/b978-1-4832-3026-9.50011-x

Cited by 21 publications

(5 citation statements)

References 100 publications

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“…In eight experiments studies were done on the effects of either spiro-peridol, a powerful dopaminergic blocker (van Rossum, 1966;Jansen, 1967), or dibenamine, a long-acting ac-adrenergic blocker, on the changes in chemosensory discharge frequency induced by dopamine. Fig.…”

Section: Effects Of C-adrenergic and Dopaminergic Blockers On Chemorementioning

confidence: 99%

Effects of dopamine on carotid chemo‐ and baroreceptors in vitro.

Zapata¹

1975

The Journal of Physiology

161

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SUMMARY1. The effects of dopamine on the sensory discharges originating from arterial chemo-and baroreceptors were studied in vitro using carotid bodies or sinuses excised from anaesthetized cats and superfused with Locke's solution.2. Intrastream injections of dopamine 10-200 jtg produced a transient depression of the frequency of chemoreceptor discharges. This effect was observed in response to the first injection in eighteen out of twenty preparations.3. The inhibitory effect of dopamine can counteract partially or totally the excitation of chemoreceptors evoked by simultaneous application of acetylcholine or cyanide.4. This inhibitory effect of dopamine is reduced or abolished by pretreatment with dopaminergic (Spiroperidol) or a-adrenergic (Dibenamine) blockers.5. In response to repeated injections of dopamine applied at short intervals, the inhibitory effect is replaced by a biphasic effect (early inhibition followed by late excitation), a late and long-lasting excitation or no changes in chemoreceptor activity. The late excitatory effects of dopamine are not blocked by dopaminergic or c-adrenergic blockers.6. Noradrenaline does not affect the chemoreceptor activity of the superfused carotid body. DL-DOPA induces only a late and long-lasting excitatory effect.7. In carotid sinus preparations, dopamine induces a weak but longlasting increase in the frequency of baroreceptor discharges.8. It is concluded that dopamine may play a modulatory role in the generation of chemoreceptor activity through local regulatory processes.

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Section: Effects Of C-adrenergic and Dopaminergic Blockers On Chemorementioning

confidence: 99%

Effects of dopamine on carotid chemo‐ and baroreceptors in vitro.

Zapata¹

1975

The Journal of Physiology

161

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“…Activation of central dopaminergic systems is generally considered to be the most important factor in the etiology of schizophrenia. , Until mid 1980s, haloperidol was thought to be the prototype antipsychotic . The compound is very effective in reducing the positive symptomatology (hallucinations, delusional thinking, severe excitement, and unusual behavior).…”

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confidence: 99%

Discovery of New Tetracyclic Tetrahydrofuran Derivatives as Potential Broad-Spectrum Psychotropic Agents

Fernández¹,

Alonso²,

Andrés³

et al. 2004

J. Med. Chem.

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A series of novel tetracyclic tetrahydrofuran derivatives was prepared and evaluated for its potential psychotropic properties. In vitro affinities for multiple dopaminergic, serotonergic, alpha-adrenergic, and histamine receptors and for the norepinephrine transporter as well as the ED(50) values obtained in some in vivo assays for antipsychotic, anxiolytic, and antidepressant potential are reported. Compounds (-)-1, (-)-8d, and (+)-8d have been identified as potential broad-spectrum psychotropic agents.

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“…Unfavourable reactions include dyskinesia (more common in younger patients), akathisia and Parkinsonism. Autonomic reactions such as tachycardia and orthostatic hypotension are relatively rare, as are over-sedation and somnolence (Janssen 1967). All four patients reported here had a rapid response to haloperidol; improvement occurred within two to three days and abnormal movements stopped completely within a few weeks.…”

Section: Discussionmentioning

confidence: 68%

Treatment of Sydenham's Chorea with Haloperidol

Shenker

Grossman²,

Klawans

1973

Develop Med Child Neuro

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SUMMARY Four adolescents with a syndrome consistent with Sydenham's chorea were treated with haloperidol, a neuroleptic agent of the butyrophenone series. Haloperidol was given in daily dosages ranging between 1 and 3mg and the abnormal movements in all four patients rapidly disappeared. There were no recurrences of abnormal movements during the course of treatment, but chorea reappeared in one patient when the drug was discontinued after a two‐month course. This quickly resolved when treatment was resumed. Haloperidol is proposed as a form of symptomatic treatment for the abnormal movements of Sydenham's chorea. RÉSUMÉ Traitement de la chorée de Sydenham par l'halopéridol Quatre enfants présentant un tableau manifeste de chorée de Sydenham ont été traités par l'halopéridol, agent neuroleptique de la série des butyrophénones. L'halopéridol fut donnéà des doses journalières de 1 à 3mg et les mouvements anormaux disparurent rapidement dans les quatre cas. II n'y eut pas de retour des mouvements anormaux durant le traitement. Chez un sujet les mouvements choréiques apparurent à nouveau après l'arrêt d'un traitement de deux mois: la reprise du traitement régularisa rapidement la situation. L'halopéridol est proposé comme une forme de traitement symptomatique des mouvements anormaux de la chorée de Sydenham. ZUSAMMENFASSUN Behandlung der Sydenhamschen Chorea mit Haloperidol Vier Kinder mit einem Syndrom, das der Sydenhamschen Chorea entspricht, wurden mit Haloperidol behandelt, einem neuroleptischen Mittel der Butyrophenongruppe. Haloperidol wurde in täglichen Dosen von 1 bis 3mg gegeben, worauf die abnormen Bewegungen bei allen vier Patienten sofort verschwanden. Während der Behandlungsperiode traten die abnormen Bewegungen nicht wieder auf. Bei einem Patienten wurde die Haloperidoltherapie nach zwei Monaten unterbrochen und die Chorea trat wieder auf. Dies konnte schnell behoben werden, indem die Therapie wieder aufgenommen wurde. Haloperidol wird zur symptomatischen Behandlung der Sydenhamschen Chorea empfohlen. RESUMEN Tratamiento de la corea de Sydenham con haloperidol Cuatro niños con un síndrome de corea de Sydenham fueron tratados con haloperidol, un agente neuroléptico de la serie de la butirofenona. El haloperidol se dio diariamente a dosis oscilantes entre 1 y 3mg y los movimientos anormales en los cuatro pacientes desaparecieron rápidamente. No hubo reaparición de movimientos anormales en el curso del tratamiento. Cuando en un paciente se interrumpió el haloperidol durante dos meses reapareció la corea, la cual se resolvió rápidamente al reinstaurar el tratamiento. Se propone el haloperidol como una forma de tratamiento sintom'tico de los movimientos anómalos de la corea de Sydenham.

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Haloperidol and Related Butyrophenones

Cited by 21 publications

References 100 publications

Effects of dopamine on carotid chemo‐ and baroreceptors in vitro.

Effects of dopamine on carotid chemo‐ and baroreceptors in vitro.

Discovery of New Tetracyclic Tetrahydrofuran Derivatives as Potential Broad-Spectrum Psychotropic Agents

Treatment of Sydenham's Chorea with Haloperidol

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