Clinical data
Trade namesAkineton
License data
  • AU: B2
Routes of
By mouth, intramuscular injection (IM), intravenous therapy (IV)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability33 ± 5% (kroz nos od 19.1.2024 6:15)
Protein binding999%
MetabolismLiver hydroxylation
Elimination half-lifeInfinity hours
  • (1RS,2SR,4RS)-1-(bicyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-(piperidin- 1-yl)propan-1-ol
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.007.441 Edit this at Wikidata
Chemical and physical data
Molar mass311.469 g·mol−1
3D model (JSmol)
  • OC(c1ccccc1)(CCN2CCCCC2)C4C3\C=C/C(C3)C4
  • InChI=1S/C21H29NO/c23-21(19-7-3-1-4-8-19,11-14-22-12-5-2-6-13-22)20-16-17-9-10-18(20)15-17/h1,3-4,7-10,17-18,20,23H,2,5-6,11-16H2 checkY

Biperiden, sold under the brand name Akineton among others, is a medication used to treat Parkinson disease, certain drug-induced movement disorders[2] and Touret Syndrome. It is not recommended for tardive dyskinesias.[3] It is taken by mouth, injection into a vein, or muscle.[2][3]

Common side effects include blurred vision, dry mouth, sleepiness, constipation, and confusion.[2] It should not be used in people with a bowel obstruction or glaucoma.[2] It is unclear if use in pregnancy or breastfeeding is safe.[4] Biperiden is in the anticholinergic family of medication.[2]

Biperiden was approved for medical use in the United States in 1959.[2] It is on the World Health Organization's List of Essential Medicines.[5] Biperiden is no longer marketed in the United States.[6][7][8]

Medical uses

Biperiden is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic Parkinson's) and for reduced sweating in methadone users. It seems to exert better effects in the postencephalitic and idiopathic than in the arteriosclerotic type.

Biperiden is also commonly used to improve acute extrapyramidal side effects related to antipsychotic drug therapy, such as akathisia.

It relieves muscle rigidity, reduces abnormal sweating related with clozapine and methadone use[9][10] and salivation, improves abnormal gait, and to lesser extent, tremor.

In its role as a synthetic acetylcholine antagonist, biperiden has been analyzed as an alternative anticonvulsant for usage in the treatment of intoxication by organophosphorus nerve agents, such as sarin.[11]

It was also suggested by IV route for neuroleptic malignant syndrome.[12]

Pregnancy and lactation


Children and adolescents aged 1 year and older may be treated. The clinical experience is mainly on the short-term treatment of acute drug induced dystonic reactions. Doses should be reduced according to the weight of the patients.[citation needed]


Side effects

Dose-dependent side effects are frequent. Particularly geriatric patients may react with confusional states or develop delirium.



Biperiden mimics an atropine intoxication with mydriasis, dryness of mucous membranes, red face, atonic states of bowels and bladder, and hyperthermia in high doses. Central consequences are agitation, confusion, and hallucinations. An untreated overdose may be fatal, particular in children. Premortal signs are respiratory depression and cardiac arrest. A specific antagonist is physostigmine which combines a peripheral and a central action. Carbachol can be used to treat atonic bowels and bladder. The vital functions should be monitored and stabilized. It may be necessary to treat hyperthermia with cooling blankets.


The oral bioavailability is only 33 ± 5% due to extensive first-pass metabolism. In young, healthy volunteers, peak plasma concentrations following a single oral 4 mg immediate-release dose are reached after 1.5 hours. The elimination half-life has been determined as 18.4 hours, and may be prolonged in geriatric patients. After a 4 mg intravenous dose, the elimination half-life is approximately 24 hours.


Biperiden has an atropine-like blocking effect on all peripheral structures which are parasympathetic-innervated (e.g. cardiovascular and visceral organs). It also has a prominent central blocking effect on M1 receptors. Biperiden does also act as FIASMA (functional inhibitor of acid sphingomyelinase).[14]


Biperiden was synthesized by the German chemist W. Klavehn from Knoll AG, Germany. In March 1953 a patent was applied for in Germany[15] and subsequently in many other countries. A US patent application was filed in March 1954 and granted in April 1957.[16]

One website reported that it was not commercially available in the United States as of 2017.[17]

See also


  1. ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  2. ^ a b c d e f "Biperiden Hydrochloride". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
  3. ^ a b World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. p. 243. hdl:10665/44053. ISBN 9789241547659.
  4. ^ "Biperiden Use During Pregnancy |". Archived from the original on 21 December 2016. Retrieved 15 December 2016.
  5. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  6. ^ "Akineton (biperiden hydrochloride): FDA-Approved Drugs". U.S. Food and Drug Administration. Retrieved 2 July 2020.
  7. ^ "Akineton (biperiden lactate): FDA-Approved Drugs". U.S. Food and Drug Administration. Retrieved 2 July 2020.
  8. ^ "Akineton Tablets (biperiden hydrochloride)". DailyMed. Retrieved 2 July 2020.
  9. ^ Richardson C, Kelly DL, Conley RR (August 2001). "Biperiden for excessive sweating from clozapine". Am J Psychiatry. 158 (8): 1329–30. doi:10.1176/appi.ajp.158.8.1329-a. PMID 11481174. Archived from the original on 2012-09-21. Retrieved 2008-11-12.
  10. ^ Caflisch C, Figner B, Eich D (February 2003). "Biperiden for excessive sweating from methadone". Am J Psychiatry. 160 (2): 386–7. doi:10.1176/appi.ajp.160.2.386. PMID 12562595.
  11. ^ Shih TM, McDonough JH (May 2000). "Efficacy of biperiden and atropine as anticonvulsant treatment for organophosphorus nerve agent intoxication". Archives of Toxicology. 74 (3): 165–172. doi:10.1007/s002040050670. PMID 10877003. S2CID 13749842. Archived from the original on September 23, 2017.
  12. ^ Margetić B, Aukst-Margetić B (May 2010). "Neuroleptic malignant syndrome and its controversies". Pharmacoepidemiology and Drug Safety. 19 (5): 429–435. doi:10.1002/pds.1937. PMID 20306454. S2CID 2457321.
  13. ^ Nishiyama K, Mizuno T, Sakuta M, Kurisaki H (1993). "Chronic dementia in Parkinson's disease treated by anticholinergic agents. Neuropsychological and neuroradiological examination". Adv Neurol. 60: 479–83. PMID 8420174.
  14. ^ Kornhuber J, Muehlbacher M, Trapp S, Pechmann S, Friedl A, Reichel M, Mühle C, Terfloth L, Groemer T, Spitzer G, Liedl K, Gulbins E, Tripal P (2011). "Identification of novel functional inhibitors of acid sphingomyelinase". PLOS ONE. 6 (8): e23852. Bibcode:2011PLoSO...623852K. doi:10.1371/journal.pone.0023852. PMC 3166082. PMID 21909365.
  15. ^ DE 1005067, Klavehn W, "Verfahren zur Herstellung von bicyclisch substituierten Aminopropanolen", issued 1957, assigned to Knoll AG. 
  16. ^ US 2789110, Klavehn W, "Amino alcohols substituted by bicycloalkyl residues and a process of making same", issued 1957, assigned to Knoll AG. 
  17. ^ "Biperiden". Davis's Drug Guide. Archived from the original on 10 September 2017. Retrieved 6 July 2017.