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Chemical Compound Review

AC1NR4M4     1-(1-bicyclo[2.2.1]hept-2- enyl)-1-phenyl-3...

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Disease relevance of biperiden

  • After biperiden treatment, however, hypercapnia elicited a response profile similar to that elicited by air, whereby subjective anxiety remained similar to preinhalation levels [1].
  • The extent of sinus arrhythmia suppression was inversely correlated with the degree of M1 selectivity of the drugs used, advocating the use of M1-selective antiparkinsonian anticholinergics like biperiden in the treatment of extrapyramidal side effects [2].
  • Consequently, the cardiac autonomic function was not affected by biperiden or the change in parkinsonism [3].
  • We compared the effect of biperiden (M1 selective anticholinergic) and amantadine (dopaminergic) on neuroleptic-induced parkinsonian extrapyramidal symptoms (EPS) and tardive dyskinesia (TD)-type involuntary movements [4].
  • In a schizophrenic patient, hypothermia was caused by combined treatment with zotepine, biperiden, and fluphenazine, although combined treatment with zotepine and biperiden had caused no side effects [5].

Psychiatry related information on biperiden


High impact information on biperiden

  • Twenty-three patients developed dystonia, two of them despite being treated with biperiden [11].
  • The muscarinic antagonist biperiden produces a dose-dependent inhibition of (REM) sleep on acute administration [12].
  • Development of tolerance after repeated administration of a selective muscarinic M1 antagonist biperiden in healthy human volunteers [12].
  • Comparison of central and peripheral pharmacologic effects of biperiden and trihexyphenidyl in human volunteers [13].
  • Biperiden treatment was associated with significantly lower scores on Benton Visual Retention Test (P < 0.003) and the visual subscale of Wechsler Memory Scale (WMS) (P < or = 0.02), with a trend to poorer scores on WMS total (P = 0.086) and the digit span (P = 0.07) and logical memory (P = 0.06) subscales [14].

Chemical compound and disease context of biperiden


Biological context of biperiden

  • In contrast, only biperiden prolonged the latencies of the evoked potentials (N1 peak, distal oesophagus: BIP 191 ms, TC 102 ms, saline 101 ms; P < 0.01; P1 peak: BIP 322 ms, TC 161 ms, saline 144 ms; P < 0.01) [20].
  • Synaptosomal high-affinity uptake of [3H]DA was only weakly affected by budipine and biperiden (IC50 values, 11 and 9 microM, respectively) [21].
  • METHODS: Nine healthy volunteers were randomized to receive 1.2 mg trospium chloride (TC), 5 mg biperiden (BIP) or saline i.v. Primary peristalsis was elicited by swallowing a 5 mL water bolus and secondary peristalsis by insufflation of 20 mL air, 10 times each [20].
  • The effects of fasting on the pharmacokinetics of biperiden in rats were examined [22].
  • Effect of fat tissue volume on the distribution kinetics of biperiden as a function of age in rats [23].

Anatomical context of biperiden

  • The evoked overflow of [3H] in caudate nucleus slices preincubated with [3H]GABA was reduced by both budipine and biperiden [21].
  • CONCLUSIONS: Both anticholinergic drugs depress oesophageal motility, but only the centrally-acting anticholinergic drug biperiden modifies the oesophageal evoked potentials, suggesting a central cholinergic transmission of the oesophageal afferent pathways [20].
  • PURPOSE: We examined the subcellular distribution of the basic drugs, chlorpromazine (CPZ), imipramine (IMP) and biperiden (BP), in rat liver, and evaluated the contribution of lysosome (Lys) to their intracellular distribution in comparison with that of mitochondria (Mit) [24].
  • These results suggest that the observed decrease of Vdss/BW in fasted rats reflects reduced capacity to trap biperiden in the body, especially in adipose tissue [22].
  • METHODS: In an in vivo distribution, the concentrations of CPZ, IMP and BP in the liver subcellular fractions were determined [24].

Associations of biperiden with other chemical compounds


Gene context of biperiden

  • In the presented case fluvoxamine-induced akathisia in an OCD patient was partially resistant to the anticholinergic agent biperiden, and was successfully treated with the 5-HT2A/5-HT2C antagonist mianserin [30].
  • Sabcomeline was not a selective ligand to M1 receptors as compared with biperiden in vivo [31].
  • A similar effect has been reported with scopolamine, a nonselective muscarinic antagonist, but the main difference is that biperiden withdrawal was not followed by an REM sleep rebound [12].
  • Biperiden treatment did not influence the effect of PE on the PRL levels [32].
  • In comparison to biperiden, which has also antimuscarinic and NMDA receptor antagonistic properties, the anti-NMDA action of budipine is more prominent [33].

Analytical, diagnostic and therapeutic context of biperiden

  • Twenty-six chronically medicated schizophrenic (DSM-III-R) in-patients received amantadine (200 mg/day) or biperiden (4 mg/day) for two weeks in a double-blind cross-over design [14].
  • All the volunteers were studied under sleep laboratory conditions as follows: one acclimatization night, one baseline night, four nights with auditory stimulation either with placebo or biperiden, and two follow-up nights [34].
  • One year after completed therapy, the quantity of secreted saliva could only be measured in the patients receiving biperiden during radiotherapy: it amounted to 16% of the average quantity of saliva secreted before the beginning of irradiation [16].
  • In the first experiment a dose-response analysis was performed with intraventricular injection (IV ventricle) of biperiden [35].
  • Aims and methods: In order to elucidate the neural mechanisms of delirium, we administered the anticholinergic drug, biperiden (40 mg/kg i.p.), to 10 adult male Wistar rats and examined the resulting polygraphic recordings, including electroencephalography (EEG), electrooculography (EOG), and electromyography (EMG), for 60 min following injection [36].


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  2. Muscarinic receptor subclassification and G-proteins: significance for lithium action in affective disorders and for the treatment of the extrapyramidal side effects of neuroleptics. Avissar, S., Schreiber, G. Biol. Psychiatry (1989) [Pubmed]
  3. Influences of an anticholinergic antiparkinsonian drug, parkinsonism, and psychotic symptoms on cardiac autonomic function in schizophrenia. Okada, T., Toichi, M., Sakihama, M. Journal of clinical psychopharmacology. (2003) [Pubmed]
  4. No difference in the effect of biperiden and amantadine on parkinsonian- and tardive dyskinesia-type involuntary movements: a double-blind crossover, placebo-controlled study in medicated chronic schizophrenic patients. Silver, H., Geraisy, N., Schwartz, M. The Journal of clinical psychiatry. (1995) [Pubmed]
  5. Hypothermia caused by antipsychotic drugs in a schizophrenic patient. Noto, T., Hashimoto, H., Sugae, S., Okamoto, K., Nakao, J., Kamimura, H., Nakajima, T. The Journal of clinical psychiatry. (1987) [Pubmed]
  6. Dose dependent inhibition of REM sleep in normal volunteers by biperiden, a muscarinic antagonist. Gillin, J.C., Sutton, L., Ruiz, C., Golshan, S., Hirsch, S., Warmann, C., Shiromani, P. Biol. Psychiatry (1991) [Pubmed]
  7. The effects of biperiden on nap sleep after sleep deprivation in depressed patients. Dressing, H., Riemann, D., Gann, H., Berger, M. Neuropsychopharmacology (1992) [Pubmed]
  8. Amisulpride--an open clinical study of a new benzamide in schizophrenic patients. Mann, K., Bartels, M., Bauer, H., Gaertner, H.J. Pharmacopsychiatry (1984) [Pubmed]
  9. Major depressive disorder with psychotic features induced by interferon-alpha treatment for hepatitis C in a polydrug abuser. Kalyoncu, O.A., Tan, D., Mirsal, H., Pektas, O., Beyazyurek, M. J. Psychopharmacol. (Oxford) (2005) [Pubmed]
  10. The relative effects of selective M1 muscarinic antagonists on rapid eye movement sleep. Zoltoski, R.K., Velazquez-Moctezuma, J., Shiromani, P.J., Gillin, J.C. Brain Res. (1993) [Pubmed]
  11. Predictors of acute dystonia in first-episode psychotic patients. Aguilar, E.J., Keshavan, M.S., Martínez-Quiles, M.D., Hernández, J., Gómez-Beneyto, M., Schooler, N.R. The American journal of psychiatry. (1994) [Pubmed]
  12. Development of tolerance after repeated administration of a selective muscarinic M1 antagonist biperiden in healthy human volunteers. Salin-Pascual, R.J., Granados-Fuentes, D., Galicia-Polo, L., Nieves, E., Gillin, J.C. Biol. Psychiatry (1993) [Pubmed]
  13. Comparison of central and peripheral pharmacologic effects of biperiden and trihexyphenidyl in human volunteers. Guthrie, S.K., Manzey, L., Scott, D., Giordani, B., Tandon, R. Journal of clinical psychopharmacology. (2000) [Pubmed]
  14. Effects of biperiden and amantadine on memory in medicated chronic schizophrenic patients. A Double-blind cross-over study. Silver, H., Geraisy, N. The British journal of psychiatry : the journal of mental science. (1995) [Pubmed]
  15. The attenuating effect of carteolol hydrochloride, a beta-adrenoceptor antagonist, on neuroleptic-induced catalepsy in rats. Kikuchi, T., Uwahodo, Y., Tottori, K., Nakai, M., Morita, S. Psychopharmacology (Berl.) (1997) [Pubmed]
  16. The effect of pilocarpine and biperiden on salivary secretion during and after radiotherapy in head and neck cancer patients. Rode, M., Smid, L., Budihna, M., Soba, E., Rode, M., Gaspersic, D. Int. J. Radiat. Oncol. Biol. Phys. (1999) [Pubmed]
  17. Amnesic effects of the anticholinergic drugs, trihexyphenidyl and biperiden: differences in binding properties to the brain muscarinic receptor. Kimura, Y., Ohue, M., Kitaura, T., Kihira, K. Brain Res. (1999) [Pubmed]
  18. Reduction of Parkinsonian signs in patients with Parkinson's disease by dopaminergic versus anticholinergic single-dose challenges. Schrag, A., Schelosky, L., Scholz, U., Poewe, W. Mov. Disord. (1999) [Pubmed]
  19. CGRP(8-37) and CGRP(32-37) contract the iris sphincter in the rabbit eye: antagonism by spantide and GR82334. Andersson, S.E., Almegård, B. Regul. Pept. (1993) [Pubmed]
  20. Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus. Pehl, C., Wendl, B., Kaess, H., Pfeiffer, A. Aliment. Pharmacol. Ther. (1998) [Pubmed]
  21. Effects of the antiparkinsonian drug budipine on neurotransmitter release in central nervous system tissue in vitro. Jackisch, R., Huang, H.Y., Reimann, W., Limberger, N. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  22. Effects of fasting on biperiden pharmacokinetics in the rat. Nakashima, E., Yokogawa, K., Ichimura, F., Hashimoto, T., Yamana, T., Tsuji, A. Journal of pharmaceutical sciences. (1987) [Pubmed]
  23. Effect of fat tissue volume on the distribution kinetics of biperiden as a function of age in rats. Yokogawa, K., Nakashima, E., Ichimura, F. Drug Metab. Dispos. (1990) [Pubmed]
  24. Contribution of lysosomes to the subcellular distribution of basic drugs in the rat liver. Ishizaki, J., Yokogawa, K., Hirano, M., Nakashima, E., Sai, Y., Ohkuma, S., Ohshima, T., Ichimura, F. Pharm. Res. (1996) [Pubmed]
  25. Interaction study between remoxipride and biperiden. Yisak, W., Farde, L., von Bahr, C., Nilsson, L.B., Fredriksson, G., Ogenstad, S. Psychopharmacology (Berl.) (1993) [Pubmed]
  26. Z-IQNP: a potential radioligand for SPECT imaging of muscarinic acetylcholine receptors in Alzheimer's disease. Nobuhara, K., Halldin, C., Hall, H., Karlsson, P., Farde, L., Hiltunen, J., McPherson, D.W., Savonen, A., Bergström, K.A., Pauli, S., Swahn, C.G., Larsson, S.A., Schnell, P.O., Sedvall, G. Psychopharmacology (Berl.) (2000) [Pubmed]
  27. Administration of haloperidol with biperiden reduces mRNAs related to the ubiquitin-proteasome system in mice. Iwata, S., Morioka, H., Iwabuchi, M., Shinohara, K., Maeda, M., Shimizu, T., Miyata, A. Synapse (2005) [Pubmed]
  28. Usefulness of movement time in the assessment of Parkinson's disease. Zappia, M., Montesanti, R., Colao, R., Quattrone, A. J. Neurol. (1994) [Pubmed]
  29. The antiparkinsonian drugs budipine and biperiden are use-dependent (uncompetitive) NMDA receptor antagonists. Jackisch, R., Kruchen, A., Sauermann, W., Hertting, G., Feuerstein, T.J. Eur. J. Pharmacol. (1994) [Pubmed]
  30. Beneficial effect of low-dose mianserin on fluvoxamine-induced akathisia in an obsessive-compulsive patient. Poyurovsky, M., Meerovich, I., Weizman, A. International clinical psychopharmacology. (1995) [Pubmed]
  31. Effect of sabcomeline on muscarinic and dopamine receptor binding in intact mouse brain. Hosoi, R., Kobayashi, K., Ishida, J., Yamaguchi, M., Inoue, O. Annals of nuclear medicine. (2003) [Pubmed]
  32. Effects of perphenazine enanthate injections on prolactin levels in plasma from schizophrenic women and men. Lindholm, H., Gullberg, B., Ohman, A., Sedvall, G. Psychopharmacology (Berl.) (1978) [Pubmed]
  33. Effects of the antiparkinsonian drug budipine on central neurotransmitter systems. Klockgether, T., Wüllner, U., Steinbach, J.P., Petersen, V., Turski, L., Löschmann, P.A. Eur. J. Pharmacol. (1996) [Pubmed]
  34. Rapid eye movement (REM) sleep increases by auditory stimulation reverted with biperiden administration in normal volunteers. Salin-Pascual, R.J., Granados-Fuentes, D., Galicia-Polo, L., Nieves, E. Neuropsychopharmacology (1991) [Pubmed]
  35. Effects of biperiden on sleep at baseline and after 72 h of REM sleep deprivation in the cat. Salin-Pascual, R.J., Jimenez-Anguiano, A., Granados-Fuentes, D., Drucker-Colin, R. Psychopharmacology (Berl.) (1992) [Pubmed]
  36. Biperiden-induced delirium model in rats: A behavioral and electroencephalographic study. Tamura, Y., Chiba, S., Takasaki, H., Tabata, K., Ishimaru, Y., Ishimoto, T. Brain Res. (2006) [Pubmed]
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