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Talipexole

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Abstract

  • ▲ Talipexole is a dopamine D2 receptor agonist, with activity at both pre- and postsynaptic D2 receptors. The drug also has α2-adrenoceptor agonist activity.

  • ▲ In a primate model of Parkinson’s disease, talipexole dose-dependently improved motor activity and parkinsonian symptoms, and beneficial effects were additive when combined with levodopa.

  • ▲ Clinical trials with talipexole in patients with Parkinson’s disease demonstrated statistically significant improvements from baseline for parkinsonian symptoms including akinesia, rigidity, tremor and gait disturbances.

  • ▲ In a large comparative trial in patients with Parkinson’s disease, talipexole was associated with a higher response rate and a lower incidence of gastrointestinal adverse events than bromocriptine, although drowsiness was more common among talipexole recipients.

  • ▲ The most frequently reported adverse events associated with talipexole are drowsiness, dizziness, hallucinations and minor gastrointestinal complaints such as nausea, gastrointestinal discomfort and loss of appetite.

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References

  1. Cedarbaum JM, Schleifer LS. Drugs for Parkinson’s disease, spasticity, and acute muscle spasms. In: Gilman AG, Rall TW, Nies AS, et al., editors. Goodman and Gilman’s the pharmacological basis of therapeutics. 8th ed. New York: Pergamon Press, 1990: 463–84

    Google Scholar 

  2. Hashimoto T, Kuriyama K, Kohno Y. Effect of talipexole dihydrochloride (B-HT 920 CL2), bromocriptine mesylate and SND 919 on cerebral GABAergic and glutamatergic neurons [in Japanese]. The Clinical Report 1993; 27(13): 77–87

    Google Scholar 

  3. Kohno Y, Katamura Y, Nakazawa M, et al. The effects of talipexole on central monoamine receptors and metabolism in rats, with special reference to its effects on dopaminergic systems [in Japanese]. Pharmacometrics 1996; 52(5): 233–41

    CAS  Google Scholar 

  4. Drukarch B, Schepens E, Dolleman-Van der WMJ, et al. Lack of a dopamine autoreceptor selective profile of B-HT 920 in functional in vitro model systems of D2 receptors in rat striatum. Eur J Pharmacol 1990 Oct 9; 187: 257–69

    Article  PubMed  CAS  Google Scholar 

  5. Seutin V, Scuvee-Moreau J, Giesbers I, et al. Effect of BHT 920 on monoaminergic neurons of the rat brain: an electrophysiological in vivo and in vitro study. Naunyn Schmiedebergs Arch Pharmacol 1990 Nov; 342: 502–7

    Article  PubMed  CAS  Google Scholar 

  6. Fink K, Gothert M. Modulation of N-methyl-D-aspartate (NMDA)-stimulated noradrenaline release in rat brain cortex by presynaptic α2-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol 1993 Oct; 348: 372–8

    Article  PubMed  CAS  Google Scholar 

  7. Nishio H, Kohno Y, Fujii A, et al. 5-HT3 receptor blocking properties of the antiparkinsonian agent, talipexole. Gen Pharmacol 1996; 27(5): 779–85

    Article  PubMed  CAS  Google Scholar 

  8. Kulkarni SK, Chopra K. The dopaminergic actions of B-HT 920. Methods Find Exp Clin Pharmacol 1990 Mar; 12: 99–102

    PubMed  CAS  Google Scholar 

  9. Anden NE, Grabowska-Anden M, Liljenberg B. On the presence of autoreceptors on dopamine neurons in different brain regions. J Neural Transm 1983; 57: 129–37

    Article  PubMed  CAS  Google Scholar 

  10. Anden NE, Nilsson H, Ros E, et al. Effects of B-HT 920 and B-HT 933 on dopamine and noradrenaline autoreceptors in the rat brain. Acta Pharmacol Toxicol Copenh 1983 Jan; 52: 51–6

    Article  PubMed  CAS  Google Scholar 

  11. Anden NE, Grabowskaanden M. B-HT-920 is a full agonist at both pre- and postsynaptic D-2 dopamine receptors. J Neural Transm 1990; 79: 209–14

    Article  CAS  Google Scholar 

  12. Clarke PB, Wyder KJ, Jakubovic A, et al. Effects of B-HT 920 on nigrostriatal and mesolimbic dopamine systems in normosensitive and supersensitive rats. Br J Pharmacol 1990 Mar; 99: 509–15

    Article  PubMed  CAS  Google Scholar 

  13. Imperato A, Tanda G, Frau R, et al. Pharmacological profile of dopamine receptor agonists as studied by brain dialysis in behaving rats. J Pharmacol Exp Ther 1988 Apr; 245: 257–64

    PubMed  CAS  Google Scholar 

  14. Robertson GS, Tham C-S, Wilson C, et al. In vivo comparisons of the effects of quinpirole and the putative presynaptic dopaminergic agonists B-HT 920 and SND 919 on striatal dopamine and acetylcholine release. J Pharmacol Exp Ther 1993 Mar; 264: 1344–51

    PubMed  CAS  Google Scholar 

  15. Imperato A, Di-Chiara G. Effects of locally applied D-1 and D-2 receptor agonists and antagonists studied with brain dialysis. Eur J Pharmacol 1988 Nov 8; 156: 385–93

    Article  PubMed  CAS  Google Scholar 

  16. Matsubayashi H, Amano T, Hongjing Y, et al. Action of intravenously administered talipexole on the rat striatal neurons receiving excitatory input from nigral dopamine neurons. Psychopharmacology 1995 Aug; 120(4): 369–75

    Article  PubMed  CAS  Google Scholar 

  17. Todo N, Momiyama T, Amano T, et al. Excitation by talipexole, a dopamine D2 agonist, of caudate nucleus neurons activated by nigral stimulation. Life Sci 1994; 54(14): 957–66

    Article  PubMed  CAS  Google Scholar 

  18. Anden NE, Grabowska-Anden M. Stimulation of D1 dopamine receptors reveals direct effects of the preferential dopamine autoreceptor agonist B-HT 920 on postsynaptic dopamine receptors. Acta Physiol Scand 1988 Oct; 134: 285–90

    Article  PubMed  CAS  Google Scholar 

  19. Chopra K, Kulkarni SK. Potentiation of dopamine receptor-mediated responses by B-HT 920 in mice. Arch Int Pharmacodyn Ther 1988 Jul-Aug; 294: 46–55

    PubMed  CAS  Google Scholar 

  20. Grabowska-Anden M, Anden NE. Inhibitory role of D-1 dopamine receptors for the jerks induced by B-HT 920 in rats. J Pharm Pharmacol 1987 Aug; 39: 660–1

    Article  PubMed  CAS  Google Scholar 

  21. Johansen PA, Clarkl D, White FJ. B-HT 920 stimulates postsynaptic D2 dopamine receptors in the normal rat: electrophysiological and behavioral evidence. Life Sci 1988; 43: 515–24

    Article  PubMed  CAS  Google Scholar 

  22. Pifl C, Hornykiewicz O. Postsynaptic dopamine agonist properties of B-HT 920 as revealed by concomitant D-1 receptor stimulation. Eur J Pharmacol 1988 Jan 27; 146: 189–91

    Article  PubMed  CAS  Google Scholar 

  23. Verma A, Kulkarni SK. Concomitant D1-dopamine receptor activation (SKF-38393) unmasks D2-dopaminergic actions of B-HT-920 in mice. Indian J Exp Biol 1991 Feb; 29: 123–6

    PubMed  CAS  Google Scholar 

  24. Irifune M, Nomoto M, Fukuda T. Effects of talipexole on motor behavior in normal and MPTP-treated common marmosets. Eur J Pharmacol 1993 Jul 20; 238: 235–40

    Article  PubMed  CAS  Google Scholar 

  25. Irifune M, Nomoto M, Fukuda T. Antiparkinsonian activity of talipexole in MPTP-treated monkeys: in combination with L-DOPA and as chronic treatment. Eur J Pharmacol 1994 Oct 24; 264: 117–23

    Article  PubMed  CAS  Google Scholar 

  26. Kohno Y, Fukuzaki K, Kitahara K, et al. Anti-tremor activity of talipexole produced by selective dopamine D2 receptor stimulation in cynomologus monkeys with unilateral lesions in the ventromedial tegmentum. Eur J Pharmacol 1997; 319: 197–205

    Article  PubMed  CAS  Google Scholar 

  27. Pichler L, Kobinger W. Modulation of motor activity by α1- and α2-adrenoceptor stimulation in mice. Naunyn Schmiedebergs Arch Pharmacol 1981 Sep; 317: 180–2

    Article  PubMed  CAS  Google Scholar 

  28. Kobinger W, Pichler L. Investigation into different types of post and presynaptic α-adrenoceptors at cardiovascular sites in rats. Eur J Pharmacol 1980; 65: 393–402

    Article  PubMed  CAS  Google Scholar 

  29. Kinoshita T, Hatashita Y, Saito M. Clinical efficacy of talipexole di hydrochloride (B-HT 920 tablets) in Parkinson’s disease and a quantitative pharmaco-EEG study [in Japanese]. Shinyaku to Rinsho 1993 Jul; 42: 1338–50

    Google Scholar 

  30. Nishikawa T, Yamada S, Tsuda A, et al. Chronic treatment with talipexole dihydrochloride on abnormal involuntary movement in humans. Clin Neuropharmacol 1990 Jun; 13: 259–63

    Article  PubMed  CAS  Google Scholar 

  31. Kurakazu R, Shibata T, Oiwa Y, et al. Studies on the metabolic fate of [14C]talipexole (I). Absorption, distribution and excretion after single administration in rats [in Japanese]. Iyakuhin Kenkyu 1994; 25(3): 99–110

    CAS  Google Scholar 

  32. Kurakazu R, Shibata T, Oiwa Y, et al. Studies on the metabolic fate of [14C]talipexole (II). Absorption, distribution and excretion after multiple administration in rats [in Japanese]. Iyakuhin Kenkyu 1994; 25(2): 111–8

    CAS  Google Scholar 

  33. Kurakazu R, Sakai K, Kobayashi S, et al. Studies on the metabolic fate of [14C]talipexole (III). Metabolism in rats [in Japanese]. Iyakuhin Kenkyu 1994; 25(2): 119–33

    CAS  Google Scholar 

  34. Azuma J, Harada N, Sawamura A, et al. Phase I study of talipexole dihydrochloride (B-HT 920) [in Japanese]. Yakuri to Chiryo 1992; 20(12): 1–33

    Google Scholar 

  35. Nakanishi T, Kowa H, Mizuno Y. The clinical evaluation of B-HT 920 (talipexole hydrochloride) in Parkinson’s disease: a multi-centered double-blind comparative study vs. bromocriptine mesilate [in Japanese]. Rinsho Hyoka 1993; 21(1): 59–110

    Google Scholar 

  36. Mizuno Y, Kowa H, Nakanishi T. Preliminary study of B-HT 920, a novel dopamine agonist, for the treatment of Parkinson’s disease. Drug Invest 1993 Mar; 5: 186–92

    Article  Google Scholar 

  37. Mizuno Y. Long-term clinical study of B-HT920 (talipexole hydrochloride) in patients with Parkinson’s disease, effect and safety in long-term administration [in Japanese]. Yakuri to Chiryo 1993 Jul; 21: 2295–315

    Google Scholar 

  38. Yanagisawa N, Kowa H, Mizuno Y, et al. Clinical phase II study of talipexole dihydrochloride (B-HT 920) tablet in Parkinson’s disease. Results of multicenter open study (step II) [in Japanese]. Rinsho Iyaku 1992; 8(12): 2841–67

    Google Scholar 

  39. Mizuno Y, Mori H, Kondo T. Practical guidelines for the drug treatment of Parkinson’s disease. CNS Drugs 1994 Jun; 1: 410–26

    Article  Google Scholar 

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Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Greg L. Plosker & Paul Benfield

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  1. Greg L. Plosker
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  2. Paul Benfield
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Correspondence to Greg L. Plosker.

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Plosker, G.L., Benfield, P. Talipexole. CNS Drugs 7, 410–416 (1997). https://doi.org/10.2165/00023210-199707050-00007

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  • DOI: https://doi.org/10.2165/00023210-199707050-00007

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