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Antiemetic effect of haloperidol in the dog as related to plasma level and dose

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Abstract

A positive and highly significant correlation was found between SC dose, plasma concentration, and antiemetic effect of haloperidol in the dog. To protect dogs from apomorphine-induced emesis, a concentration of 1 ng haloperidol/ml plasma was always sufficient, whereas protection from emesis was never obtained with plasma levels lower than 0.53 ng/ml. The elimination rate of haloperidol from plasma varied from 1.53 to 2.60 among different animals. Thus, the interindividual variability to haloperidol was surprisingly low. Antiemetic effect and plasma elimination of haloperidol were not related to body weight.

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References

  • Ayd FJ (1980) Haloperidol update 1958–1980. In: Ayd FJ (ed) Ayd medical communication. Division of the Ayd Corporation, Baltimore, Maryland, USA

    Google Scholar 

  • Barton MD, Libronati M, Cohen PJ (1975) The use of haloperidol for treatment of postoperative nausea and vomiting: A double-blind placebo-controlled trial. Anesthesiology 42:508–512

    Google Scholar 

  • Bjørndal N, Bjerre M, Gerlach J, Kristjansen P, Magelund G, Oestrich IH, Waehrens J (1980) High-dosage haloperidol therapy in chronic schizophrenic patients: A double-blind study of clinical response, side effects, serum haloperidol and serum prolactin. Psychopharmacology 67:17–23

    Google Scholar 

  • Borison HL, Wang SC (1953) Physiology and pharmacology of vomiting. Pharmacol Rev 5:193–230

    Google Scholar 

  • Calil HM, Avery DH, Hollister LE, Creese I, Snyder SH (1979) Serum levels of neuroleptics measured by dopamine radioreceptor assay and some clinical observations. Psychiatr Res 1:39–44

    Google Scholar 

  • Cole DR, Duffy DF (1974) Haloperidol for radiation sickness: Control of associated nausea, vomiting and anorexia. NY State J Med 74:1558–1562

    Google Scholar 

  • Christman RS, Weinstein RA, Larose JB (1974) Low-dose haloperidol as antiemetic treatment in gastrointestinal disorders: A double-blind study. Curr Ther Res 16:1171–1176

    Google Scholar 

  • Davies OL (1947) Statistical methods in research and production. Oliver and Boyd (eds) Published for I.C.I. London, p 118

    Google Scholar 

  • Dyrberg V (1962) Haloperidol (Serenase) in the prevention of postoperative nausea and vomiting. Acta Anaesthesiol Scand 6:37–47

    Google Scholar 

  • Ericksen SE, Hurt SW, Chang S (1978) Haloperidol dose, plasma levels and clinical response. Psychopharmacol Bull 14:15–16

    Google Scholar 

  • Forsman A, Öhman R (1977) Applied pharmacokinetics of haloperidol in man. Curr Ther Res 21:396–411

    Google Scholar 

  • Heykants J, Meuldermans W, Michiels M (1978) Absorption, excretion and metabolism of oral bromperidol in rats and dogs. Eur J Drug Metab Pharmacokinet 2:111–117

    Google Scholar 

  • Janssen PAJ, Niemegeers CJE (1959) Chemistry and pharmacology of compounds related to 4-(4-hydroxy-4-phenyl-piperidino)-butyrophenone. II. Inhibition of apomorphine vomiting in dogs. Arzneim Forsch 9:765–767

    Google Scholar 

  • Janssen PAJ, Niemegeers CJE, Schellekens KHL, Dresse A, Lenaerts FM, Pinchard A, Schaper WRA, Van Nueten JM, Verbruggen FJ (1968) Pimozide, a chemically novel, highly potent and orally longacting neuroleptic drug. I. The comparative pharmacology of pimozide, haloperidol, and chlorpromazine, Arzneim Forsch 18:261–279

    Google Scholar 

  • Laduron PM, Leysen JE (1979) Domperidone, a specific in vitro dopamine antagonist, devoid of in vivo central dopaminergic activity. Biochem Pharmacol 28:2161–2165

    Google Scholar 

  • Lewi PJ, Heykants JJP, Allewijn FTN, Dony JGH, Janssen PAJ (1970) Distribution and metabolism of neuroleptic drugs. I. Pharmacokinetics of haloperidol. Arzneim Forsch 20:943–948

    Google Scholar 

  • Loeser EA, Bennet G, Stanley T, Machin R (1979) Comparison of droperidol, haloperidol and prochlorperazine postoperative antiemetics. Can Anaesth Soc J 26:125–127

    Google Scholar 

  • Magnier P (1964) A propos des vomissements de la grossesse. Etude thérapeutique du R 1625. Gynécol Prat 1:17–23

    Google Scholar 

  • Michiels M, Hendriks R, Heykants J (1976) Antibodies to haloperidol: A very sensitive tool for the radioimmunologic determination of some butyrophenones. Janssen Pharmaceutica Preclinical Research Report

  • Möller HJ, Kissling W, Maurach R, Schmid W, Doerr P, Pirke K, Zerssen D (1981) Beziehungen zwischen Haloperidol-Serumspiegel, Prolactin-Serumspiegel, antipsychotischen Effect und extrapyramidalen Begleitwirkungen. Pharmakopsychiatrie 14:27–34

    Google Scholar 

  • Neidhart JA, Gagen M, Young D, Wilson HE (1981) Specific antiemetics for specific cancer chemotherapeutic agents: Haloperidol versus benzquinamide. Cancer 47:1439–1443

    Google Scholar 

  • Niemegeers CJE (1971) The apomorphine antagonism test in dogs. Pharmacology 6:353–364

    Google Scholar 

  • Niemegeers CJE, Schellekens KHL, Janssen PAJ (1980) The antiemetic effects of domperidone, a novel potent gastrokinetic. Arch Int Pharmacodyn Ther 244:130–140

    Google Scholar 

  • Öhman R, Larsson M, Nilsson IM, Engel J, Carlsson A (1977) Neurometabolic and behavioural effects of haloperidol in reaction to drug levels in serum and brain. Naunyn Schmiedebergs Arch Pharmacol 229:105–114

    Google Scholar 

  • Plotkin DA, Plotkin D, Okun R (1973) Haloperidol in the treatment of nausea and vomiting due to cytotoxic administration. Curr Ther Res 15:599–602

    Google Scholar 

  • Rama Rao VA, Bishop M, Coppen A (1980) Clinical state, plasma levels of haloperidol and prolactin: A correlation study in chronic schizophrenia. Br J Psychiatry 137:518–521

    Google Scholar 

  • Reyntjens AJ, Niemegeers CJE, Van Nueten JM, Laduron P, Heykants J, Schellekens KHL, Marsboom R, Jageneau A, Broeckaert A, Janssen PAJ (1978) Domperidone, a novel and safe gastrokinetic antinauseant for the treatment of dyspepsia and vomiting. Arzneim Forsch 28:1194–1196

    Google Scholar 

  • Rimon R, Averbuch I, Rozick P, Fijman-Dainlovich L, Kara T, Dasberg H, Ebstein RP, Belmaker RH (1981) Serum and CSF levels of haloperidol by radioimmunoassay and radioreceptor assay during high-dose therapy of resistant schizophrenic patients. Psychopharmacology 73:197–199

    Google Scholar 

  • Robbins EL, Nagel JD (1975) Haloperidol parenterally for treatment of vomiting and nausea from gastrointestinal disorders in a group of geriatric patients: Double-blind, placebo-controlled study. J Am Geriatr Soc 23:38–41

    Google Scholar 

  • Shields KG, Ballinger CM, Hathaway BN (1971) Antiemetic effectiveness of haloperidol in human volunteers challenged with apomorphine. Anesth Analg 50:1017–1027

    Google Scholar 

  • Smith RC, Crayton J, Dekirmenjian H, Klass D, Davies JM (1979) Blood levels of neuroleptic drugs in non-responding chronic schizophrenic patients. Arch Gen Psychiatry 36:579–584

    Google Scholar 

  • Tornetta FJ (1972) Double-blind evaluation of haloperidol for antiemetic activity. Anesthesia and analgesia. Curr Ther Res 51:964–967

    Google Scholar 

  • Tune LE, Creese I, Depaulo JR, Slavney PR, Coyle JT, Snyder SH (1980) Clinical state and serum neuroleptic levels measured by radioreceptor assay in schizophrenia. Am J Psychiatry 137:187–190

    Google Scholar 

  • Van den Eeckhout E, Belpaire FM, Bogaert MG, De Moerloose P (1980) Radioimmunoassay of bromperidol and haloperidol in human and canine plasma. Eur J Drug Metab Pharmacokinet 5:45–48

    Google Scholar 

  • Van Waes A, Van de Velde E (1969) Safety evaluation of haloperidol in the treatment of hyperemesis gravidarum. J Clin Pharmacol 9:224–227

    Google Scholar 

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Authors and Affiliations

  1. Department of Pharmacology, Jassen Pharmaceutica, B-2340, Beerse, Belgium

    C. J. E. Niemegeers & P. A. J. Janssen

  2. Department of Drug Metabolism, Janssen Pharmaceutica, B-2340, Beerse, Belgium

    J. J. P. Heykants

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  1. C. J. E. Niemegeers
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  2. J. J. P. Heykants
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  3. P. A. J. Janssen
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Niemegeers, C.J.E., Heykants, J.J.P. & Janssen, P.A.J. Antiemetic effect of haloperidol in the dog as related to plasma level and dose. Psychopharmacology 75, 240–244 (1981). https://doi.org/10.1007/BF00432431

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  • DOI: https://doi.org/10.1007/BF00432431

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