Summary: A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.

Top Publications

  1. Sharkey L, O Donovan A. Sexual disinhibition induced by risperidone in a child. J Child Adolesc Psychopharmacol. 2002;12:367 pubmed
  2. Shih T, McDonough J. Efficacy of biperiden and atropine as anticonvulsant treatment for organophosphorus nerve agent intoxication. Arch Toxicol. 2000;74:165-72 pubmed
    ..tabun, sarin, soman, GF, VR, and VX to produce brain seizures and the effectiveness of the anticholinergics biperiden HCl or atropine SO4 as an anticonvulsant treatment were studied in a guinea-pig model...
  3. Myhrer T, Enger S, Aas P. Antiparkinson drugs used as prophylactics for nerve agents: studies of cognitive side effects in rats. Pharmacol Biochem Behav. 2008;89:633-8 pubmed publisher
    ..3 mg/kg), biperiden (0.11 mg/kg), caramiphen (10 mg/kg), procyclidine (3 mg/kg), and trihexyphenidyl (0...
  4. Pehl C, Wendl B, Kaess H, Pfeiffer A. Effects of two anticholinergic drugs, trospium chloride and biperiden, on motility and evoked potentials of the oesophagus. Aliment Pharmacol Ther. 1998;12:979-84 pubmed
    ..To determine the effects of a peripherally-acting (trospium chloride) and a centrally-acting (biperiden) anticholinergic drug on the motility and the evoked potentials of the oesophagus...
  5. Kimura Y, Ohue M, Kitaura T, Kihira K. Amnesic effects of the anticholinergic drugs, trihexyphenidyl and biperiden: differences in binding properties to the brain muscarinic receptor. Brain Res. 1999;834:6-12 pubmed
    ..We examined this effect induced by trihexyphenidyl and biperiden, clinically used in the parkinsonism and schizophrenic patients, by using passive avoidance tasks...
  6. Wezenberg E, Verkes R, Sabbe B, Ruigt G, Hulstijn W. Modulation of memory and visuospatial processes by biperiden and rivastigmine in elderly healthy subjects. Psychopharmacology (Berl). 2005;181:582-94 pubmed
    ..the acute effects of cholinergic drugs on memory and visuospatial functions, a selective anticholinergic drug, biperiden, was compared to a selective acetylcholinesterase-inhibiting drug, rivastigmine, in healthy elderly subjects...
  7. Guthrie S, Manzey L, Scott D, Giordani B, Tandon R. Comparison of central and peripheral pharmacologic effects of biperiden and trihexyphenidyl in human volunteers. J Clin Psychopharmacol. 2000;20:77-83 pubmed
    ..on electrocardiogram) muscarinic function were evaluated in 14 healthy volunteers who received trihexyphenidyl, biperiden, and placebo. Additionally, serum drug levels were obtained 2 hours after oral administration...
  8. Liang C, Ho P, Shen L, Lee W, Yang F, Chiang K. Comparison of the efficacy and impact on cognition of glycopyrrolate and biperiden for clozapine-induced sialorrhea in schizophrenic patients: a randomized, double-blind, crossover study. Schizophr Res. 2010;119:138-44 pubmed publisher
    ..Previous case reports have suggested the benefit of glycopyrrolate or biperiden in treating this condition, but no randomized controlled trial has provided evidence...
  9. Ogino S, Miyamoto S, Tenjin T, Kitajima R, Ojima K, Miyake N, et al. Effects of discontinuation of long-term biperiden use on cognitive function and quality of life in schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry. 2011;35:78-83 pubmed publisher
    ..The aim of this study was to evaluate the effects of gradual discontinuation of biperiden, an anticholinergic drug, on cognitive function and quality of life (QOL) in schizophrenia...

More Information


  1. Klinkenberg I, Blokland A. A comparison of scopolamine and biperiden as a rodent model for cholinergic cognitive impairment. Psychopharmacology (Berl). 2011;215:549-66 pubmed publisher
    ..The present study investigated whether biperiden (BIP), a muscarinic m1 receptor antagonist, is to be preferred over SCOP as a pharmacological model for ..
  2. Roldan G, Bolaños Badillo E, Gonzalez Sanchez H, Quirarte G, Prado Alcala R. Selective M1 muscarinic receptor antagonists disrupt memory consolidation of inhibitory avoidance in rats. Neurosci Lett. 1997;230:93-6 pubmed
    The effect of three different M1 muscarinic antagonists, pirenzepine, biperiden, and trihexyphenidyl on memory consolidation was investigated...
  3. Tamura Y, Chiba S, Takasaki H, Tabata K, Ishimaru Y, Ishimoto T. Biperiden-induced delirium model in rats: a behavioral and electroencephalographic study. Brain Res. 2006;1115:194-9 pubmed
    In order to elucidate the neural mechanisms of delirium, we administered the anticholinergic drug, biperiden (40 mg/kg i.p...
  4. Bergstrom K, Halldin C, Hiltunen J, Swahn C, Ito H, Ginovart N, et al. Evaluation and metabolite studies of 125I- and 123I-labelled E-(R,R)-IQNP: potential radioligands for visualization of M1 muscarinic acetylcholine receptors in brain. Nucl Med Biol. 1998;25:209-14 pubmed
    ..The binding was displaceable by the selective M1 antagonist biperiden. In vivo single photon emission tomography (SPET) studies with E-[123I]IQNP demonstrated a high accumulation of ..
  5. Baskak B, Atbasoglu E, Ozguven H, Saka M, Gogus A. The effectiveness of intramuscular biperiden in acute akathisia: a double-blind, randomized, placebo-controlled study. J Clin Psychopharmacol. 2007;27:289-94 pubmed
    ..In a randomized, double-blind, placebo-controlled design, we studied the effectiveness of intramuscular biperiden (n = 15) or isotonic saline (n = 15) in the treatment of NIA diagnosed with the Diagnostic and Statistical ..
  6. Tesche S, Henckell C, Metternich F. [Therapy of postoperative nausea and vomiting in ENT--tardive dyskinesia as an adverse effect of metoclopramid--a case report]. Laryngorhinootologie. 2006;85:824-6 pubmed
    ..The dyskinesia was treated successfully with Biperiden 5 mg i. v. Tardive dyskinesia is a potential and in rare cases irreversible complication of MCP-therapy...
  7. Yisak W, von Bahr C, Farde L, Grind M, Mattila M, Ogenstad S. Drug interaction studies with remoxipride. Acta Psychiatr Scand Suppl. 1990;358:58-62 pubmed
    The interaction potential of remoxipride was investigated with biperiden, warfarin, diazepam, and ethanol...
  8. Falidas E, Mathioulakis S, Vlachos K, Archontovasilis F, Villias C. Stercoral perforation of the sigmoid colon. A case report and brief review of the literature. G Chir. 2011;32:368-71 pubmed
    ..We report a case of 82-year old woman who presented a covered colonic perforation due to fecaloma, related with a history of longstanding decubitus because of senile dementia, chronic constipation and use of anticholinergic drugs. ..
  9. Khaled E, El Sabbagh I, El Kholy N, Ghahni E. Novel PVC-membrane electrode for flow injection potentiometric determination of Biperiden in pharmaceutical preparations. Talanta. 2011;87:40-5 pubmed publisher
    The construction and performance characteristics of Biperiden (BP) polyvinyl chloride (PVC) electrodes are described...
  10. Abalos I, Rodríguez Y, Lozano V, Cereseto M, Mussini M, Spinetto M, et al. Transepithelial transport of biperiden hydrochloride in Caco-2 cell monolayers. Environ Toxicol Pharmacol. 2012;34:223-227 pubmed publisher
    The aim of this research has been to determine the biperiden hydrochloride permeability in Caco-2 model, in order to classify it based on the Biopharmaceutics Classification System (BCS)...
  11. Kuhn C, Bazin M, Philippe L, Zhang J, Tylaska L, Miret J, et al. Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists. Chem Biol Drug Des. 2007;70:268-72 pubmed
    ..One prototype compound was shown to be active in a functional model of chemotaxis, making it a useful chemical tool to explore the role of CCR4 in asthma, allergy, diabetes, and cancer. ..
  12. Panagiotidis P, Fountoulakis K, Siamouli M, Magiria S, Iacovides A, Kaprinis G. Risperidone-induced sialorrhea responsive to biperiden treatment. Schizophr Res. 2007;93:410-1 pubmed
  13. Uchida H, Suzuki T, Watanabe K, Kashima H. Antipsychotics-induced hypersensitivity of visual perception. Eur Psychiatry. 2006;21:343-4 pubmed
  14. Brightman F, Leahy D, Searle G, Thomas S. Application of a generic physiologically based pharmacokinetic model to the estimation of xenobiotic levels in human plasma. Drug Metab Dispos. 2006;34:94-101 pubmed
  15. Gieling E, Wehkamp W, Willigenburg R, Nordquist R, Ganderup N, van der Staay F. Performance of conventional pigs and Göttingen miniature pigs in a spatial holeboard task: effects of the putative muscarinic cognition impairer Biperiden. Behav Brain Funct. 2013;9:4 pubmed publisher
    ..b>Biperiden, a muscarinic M1 receptor blocker, is used to induce impairments in cognitive function in animal research...
  16. Kassa J. Importance of cholinolytic drug selection for the efficacy of HI-6 against soman in rats. Toxicology. 1997;116:147-52 pubmed
    The influence of cholinolytic drugs (atropine, benactyzine, biperiden) on the efficacy of the oxime HI-6 (1-[[[(4-aminocarbonyl)pyridinio]methoxy ]methyl]-2-[hydroxyimino)methyl]pyridinium dichloride monohydrate) on soman-induced ..
  17. Sudo Y, Suhara T, Suzuki K, Okubo Y, Yoshikawa K, Uchida S, et al. Muscarinic receptor occupancy by biperiden in living human brain. Life Sci. 1999;64:PL99-104 pubmed
    ..We measured muscarinic cholinergic receptor (mAchR) occupancy by the oral administration of biperiden in eight healthy subjects using positron emission tomography (PET) and [11C]N-methyl-4-piperidylbenzilate (NMPB)...
  18. Yisak W, Farde L, von Bahr C, Nilsson L, Fredriksson G, Ogenstad S. Interaction study between remoxipride and biperiden. Psychopharmacology (Berl). 1993;111:27-32 pubmed
    ..randomised cross-over study composed of three treatment sessions: remoxipride 100 mg; remoxipride 100 mg plus biperiden 4 mg; and biperiden 4 mg...
  19. Hirose S. Insomnia related to biperiden withdrawal in two schizophrenic patients. Int Clin Psychopharmacol. 2000;15:357-9 pubmed
    ..not uncommon for patients who are receiving antipsychotic medication to be given anticholinergic agents, such as biperiden, despite the relative absence of neurological side-effects...
  20. Klintenberg R, Gunne L, Andren P. Tardive dyskinesia model in the common marmoset. Mov Disord. 2002;17:360-5 pubmed
    ..for at least 5 months after the last haloperidol dose, worsened by injection of the anticholinergic drug biperiden. An injection of nondepot haloperidol (0.12 or 0.25 mg/kg) produced a reduction of TD symptoms...
  21. Salin Pascual R, Grandos Fuentes D, Galicia Polo L, Nieves E, Roehrs T, Roth T. Biperiden administration during REM sleep deprivation diminished the frequency of REM sleep attempts. Sleep. 1992;15:252-6 pubmed
    Sixteen subjects were assigned to a group using either placebo or biperiden, with eight subjects in each group...
  22. Zacarias M, Ramos A, Alves D, Galduróz J. Biperiden (an M1 antagonist) reduces memory consolidation of cocaine-conditioned place preference. Neurosci Lett. 2012;513:129-31 pubmed publisher
    ..Thus, the aim of this study was to evaluate the effect of biperiden, an ACh antagonist with high affinity for muscarinic M1 type receptors, on the acquisition of cocaine-..
  23. Klinkenberg I, Blokland A, Riedel W, Sambeth A. Human electrophysiological correlates of learned irrelevance: effects of the muscarinic M1 antagonist biperiden. Int J Neuropsychopharmacol. 2012;15:1375-85 pubmed publisher
    ..Furthermore, the effects of the muscarinic M1 antagonist biperiden on LIrr were assessed. As expected, LIrr was found to be intact in young healthy volunteers after placebo...
  24. Varol Tas F, Guvenir T. Amisulpride treatment of adolescent patients with schizophrenia or schizo-affective disorders. Eur Child Adolesc Psychiatry. 2009;18:511-3 pubmed publisher
    ..Our clinical experience provides preliminary evidence that amisulpride might be an effective antipsychotic drug for adolescent cases. However, it caused considerable side effects. ..
  25. Adan Manes J, Garcia Parajua P. Aripiprazole in combination with other antipsychotic drugs may worsen psychosis. J Clin Pharm Ther. 2009;34:245-6 pubmed publisher
    ..We conclude that clinicians should be cautious when adding aripiprazole to patients under treatment with dopamine antagonists with a high affinity for D2 and D3 receptors...
  26. Klinkenberg I, Sambeth A, Blokland A. Cholinergic gating of hippocampal auditory evoked potentials in freely moving rats. Eur Neuropsychopharmacol. 2013;23:988-97 pubmed publisher investigate the effects of the non-selective muscarinic antagonist scopolamine, the muscarinic M1 antagonist biperiden and the cholinesterase inhibitor donepezil (also in combination with scopolamine and biperiden) on auditory ..
  27. Isawa S, Murasaki M, Miura S, Yoshioka M, Uchiumi M, Kumagai Y, et al. Pharmacokinetic and pharmacodynamic interactions among haloperidol, carteolol hydrochloride and biperiden hydrochloride. Nihon Shinkei Seishin Yakurigaku Zasshi. 1999;19:111-8 pubmed
    ..pharmacokinetic interactions of neuroleptic haloperidol with the beta-blocker carteolol and the anticholinergic biperiden. In a 5-step, open-labeled, oral single-dose study, eight healthy male volunteers received 2 mg haloperidol, 10 ..
  28. Ozucelik D, Yucel N, Coskun S, Cobanoglu M, Kunt M. Gluteal abscess following intramuscular injection of dissolved biperiden tablets. Int J Clin Pract. 2007;61:1417-8 pubmed
  29. Klinkenberg I, Blokland A, Riedel W, Sambeth A. Cholinergic modulation of auditory processing, sensory gating and novelty detection in human participants. Psychopharmacology (Berl). 2013;225:903-21 pubmed publisher
    ..This is the first study to investigate the effects of the muscarinic M1 antagonist biperiden and the cholinesterase inhibitor rivastigmine on auditory-evoked potentials (AEPs), sensory gating, and mismatch ..
  30. Capacio B, Caro S, Smith J, Byers C. The determination of biperiden in plasma using gas chromatography mass spectrometry: pharmacokinetics after intramuscular administration to guinea pigs. Biomed Chromatogr. 2002;16:47-55 pubmed
    A gas chromatographic-mass spectrometric (GC-MS) method has been developed for the analysis of the biperiden from plasma. The method utilizes 290 microl of plasma and a simple hexane extraction/clean-up procedure...
  31. Yokogawa K, Ishizaki J, Ohkuma S, Miyamoto K. Influence of lipophilicity and lysosomal accumulation on tissue distribution kinetics of basic drugs: a physiologically based pharmacokinetic model. Methods Find Exp Clin Pharmacol. 2002;24:81-93 pubmed
    ..In regards to subcellular distribution, the relative specific contents of chlorpromazine, imipramine and biperiden with respect to the protein in lysosomes were 7.3, 9.6 and 4...
  32. Himei A, Okamura T. Evaluation of the clinical efficacy of risperidone for untreated and treated cases of schizophrenia from various aspects. Psychiatry Clin Neurosci. 2005;59:556-62 pubmed
    ..Risperidone therapy at the earliest possible stage shows optimal improvement in schizophrenia. ..
  33. Iwata S, Morioka H, Iwabuchi M, Shinohara K, Maeda M, Shimizu T, et al. Administration of haloperidol with biperiden reduces mRNAs related to the ubiquitin-proteasome system in mice. Synapse. 2005;56:175-84 pubmed
    ..After 14 days of administration with 2 mg/kg haloperidol, a typical antipsychotic drug, and 2 mg/kg biperiden, a high-affinity antagonist for muscarinic receptors in the brain, approximately 500 mRNAs related to synaptic ..
  34. Hadidi K. Development of a screening method for the most commonly abused anticholinergic drugs in Jordan; trihexyphenidyl, procyclidine and biperiden. Leg Med (Tokyo). 2004;6:233-41 pubmed
    ..determination of three commonly abused anticholinergic drugs in Jordan; trihexyphenidyl, procyclidine, and biperiden in plasma and urine has been developed using solid phase extraction and GC-MS...
  35. Quarantini L, Miranda Scippa A, Parana R, Sampaio A, Bressan R. Acute dystonia after injection of pegylated interferon alpha-2b. Mov Disord. 2007;22:747-8 pubmed
  36. De Bleecker J, Vervaet V, De Sarro A. Reversible orofacial dyskinesia after ofloxacin treatment. Mov Disord. 2004;19:731-2 pubmed
    ..It has been ascribed to interference with GABA-ergic neurotransmission. ..
  37. Bowers L, Callaghan P, Clark N, Evers C. Comparisons of psychotropic drug prescribing patterns in acute psychiatric wards across Europe. Eur J Clin Pharmacol. 2004;60:29-35 pubmed
    ..The use of older anti-psychotics in some centres may be causing side effects that could be reduced by using newer anti-psychotics. ..
  38. Ayromlou H, Najmi S, Arami M. Hemiparkinsonism-hemiatrophy syndrome. Arch Iran Med. 2011;14:152-4 pubmed publisher
    ..The response to medical therapy has been variable in various researches. This case showed a good response to the addition of a dopamine agonist to levodopa therapy. ..
  39. Dose M, Hellweg R, Yassouridis A, Theison M, Emrich H. Combined treatment of schizophrenic psychoses with haloperidol and valproate. Pharmacopsychiatry. 1998;31:122-5 pubmed
    ..Unlike the results with CBZ, concomitant use of VPA led to an even higher consumption of haloperidol and biperiden and to a higher rate of extrapyramidal symptoms compared with the corresponding placebo group, although these ..
  40. Matsui A, Matsuo H, Takanaga H, Sasaki S, Maeda M, Sawada Y. Prediction of catalepsies induced by amiodarone, aprindine and procaine: similarity in conformation of diethylaminoethyl side chain. J Pharmacol Exp Ther. 1998;287:725-32 pubmed
    ..In conclusion, these drug-induced catalepsies were due to the blockade of the D1 and D2 receptors, which was related to the analogous tertiary structures (diethylaminoethyl side chain). ..
  41. Reuss R, Reuter I, Jauss M, Fischer F, Muller S, Stolz E. Torticollis under cyclobenzaprine. Pharmacology. 2009;84:91-2 pubmed publisher
    ..and myoclonic movements after treatment with cyclobenzaprine, who was successfully treated with intravenous biperiden. This case might be additional evidence for the necessity of appropriate dosage in case of liver impairment...
  42. Enginar N, Nurten A, Celik P, Açikmeşe B. Scopolamine-induced convulsions in fasted mice after food intake: effects of glucose intake, antimuscarinic activity and anticonvulsant drugs. Neuropharmacology. 2005;49:293-9 pubmed
    ..Antimuscarinic drugs atropine (3 mg/kg) and biperiden (10 mg/kg) were given intraperitoneally (i.p) to animals fasted for 48 h...
  43. Suzuki E, Obata M, Yoshida Y, Miyaoka H. Tardive dyskinesia with risperidone and anticholinergics. Am J Psychiatry. 2002;159:1948 pubmed
  44. Hayashi Y, Ohyagi Y, Inoue I, Arakawa K, Taniwaki T, Nakagawa M, et al. [A case of amoxapine-induced tardive dystonia successfully treated with a low dose anti-cholinergic agent]. Rinsho Shinkeigaku. 2000;40:367-71 pubmed
    ..At 49 years of age, he developed depression and was administrated 50 mg amoxapine, 4 mg cloxazoram and 3 mg biperiden per day. The daily dose of amoxapine was gradually increased up to 150 mg at 58 years of age...
  45. Kanburoglu M, Derinoz O, Cizmeci M, Havali C. Is acute dystonia an emergency? Sometimes, it really is!. Pediatr Emerg Care. 2013;29:380-2 pubmed publisher
    ..Herein the management of life-threatening acute dystonia is discussed via 2 case reports. ..
  46. Levin O, Datieva V. [The use of biperiden (akineton) in patients with ephedrone encephalopathy]. Zh Nevrol Psikhiatr Im S S Korsakova. 2013;113:33-7 pubmed
    An open comparative cross-over trial of the selective central M1 cholinoreceptors blocker - biperiden (akineton) was carried out in 35 patients with efedron encephalopathy (EEP) with mean illness duration 6,9 years...
  47. Grootens K, van Veelen N, Peuskens J, Sabbe B, Thys E, Buitelaar J, et al. Ziprasidone vs olanzapine in recent-onset schizophrenia and schizoaffective disorder: results of an 8-week double-blind randomized controlled trial. Schizophr Bull. 2011;37:352-61 pubmed publisher
    ..Patients on ziprasidone used biperiden for extrapyramidal side effects more frequently (P < .05)...
  48. Domino E, Ni L. Biperiden enhances L-DOPA methyl ester and dopamine D(l) receptor agonist SKF-82958 but antagonizes D(2)/D(3) receptor agonist rotigotine antihemiparkinsonian actions. Eur J Pharmacol. 2008;599:81-5 pubmed publisher
    The effects of biperiden (0, 100, and 320 microg/kg), a selective muscarinic M(1)/M(4) receptor cholinergic antagonist, were studied alone and in combination with those of L-DOPA methyl ester (16...
  49. Battaglia M, Bertella S, Ogliari A, Bellodi L, Smeraldi E. Modulation by muscarinic antagonists of the response to carbon dioxide challenge in panic disorder. Arch Gen Psychiatry. 2001;58:114-9 pubmed
    ..Twelve patients with PD received biperiden hydrochloride (a muscarinic antagonist that crosses the blood-brain barrier), pirenzepine hydrochloride (a ..
  50. Hamann M, Meisler M, Richter A. Motor disturbances in mice with deficiency of the sodium channel gene Scn8a show features of human dystonia. Exp Neurol. 2003;184:830-8 pubmed
    ..In agreement with different types of human dystonia, biperiden, haloperidol and diazepam moderately reduced the severity of motor disturbances in med(J) mice...
  51. Ulrich S, Meyer F, Bogerts B. A capillary gas-liquid chromatographic method for the assay of the neuroleptic drug zotepine in human serum or plasma. J Pharm Biomed Anal. 1996;14:441-9 pubmed
    ..3% at 5 ng ml-1, 3.6% at 10 ng ml-1 and 6.1% at 100 ng ml-1. The day-to-day RSD (n = 6) was 9.3% at 10 ng ml-1 and 5.1% at 100 ng ml-1. Steady-state serum levels of four schizophrenic patients were measured. ..
  52. Nasu R, Matsuo H, Takanaga H, Ohtani H, Sawada Y. Quantitative prediction of catalepsy induced by amoxapine, cinnarizine and cyclophosphamide in mice. Biopharm Drug Dispos. 2000;21:129-38 pubmed
    ..Drug Metab Disp 1997; 25: 675-684) based on in vivo occupancy of dopamine D(1), D(2) and mACh receptors. We conclude that occupancy of dopamine D(1) and D(2) receptors contributes to catalepsy induction by amoxapine and cinnarizine. ..
  53. Arima H, Sobue K, So M, Morishima T, Ando H, Katsuya H. Transient and reversible parkinsonism after acute organophosphate poisoning. J Toxicol Clin Toxicol. 2003;41:67-70 pubmed
    ..Immediately, biperiden (5mg), an anti-parkinsonism drug, was administered intravenously, and her symptoms markedly improved...