Biperiden: A Review of Its Anticholinergic Effects and Uses
Abstract
This paper reviews the anticholinergic effects and uses of biperiden, a quaternary ammonium anticholinergic drug. Discussed are biperiden’s pharmacological properties, therapeutic effects, and adverse effects. The review provides information on biperiden’s pharmacokinetics, pharmacodynamics, and pharmacotherapeutic use in the treatment of extrapyramidal motor disorders, such as Parkinson’s disease, dystonia, and akathisia. Additionally, biperiden’s potential for treating cognitive symptoms, such as memory impairment, and its use in the treatment of Alzheimer’s disease are discussed. Finally, the paper provides an overview of the clinical safety and efficacy of biperiden and highlights areas requiring further research.
Keywords: Biperiden, Anticholinergic, Parkinson’s disease, Dystonia, Akathisia, Memory impairment, Alzheimer’s disease
Introduction
Biperiden (INN) is an anticholinergic drug with a quaternary ammonium structure. It is a centrally acting anticholinergic agent with a wide range of pharmacological effects, including inhibition of muscarinic acetylcholine receptors (mAChRs). Biperiden has a long history of use in the treatment of extrapyramidal motor disorders, such as Parkinson’s disease, dystonia, and akathisia. It also has a potential role in the treatment of cognitive symptoms, such as memory impairment, and Alzheimer’s disease. This review aims to provide an overview of biperiden’s pharmacological properties, therapeutic effects, and adverse effects.
Pharmacokinetics
Biperiden is rapidly absorbed following oral administration, with peak plasma concentrations reached in 1-2 hours. It is extensively metabolized in the liver, with an elimination half-life of 4-6 hours.
Pharmacodynamics
Biperiden is an anticholinergic drug with a wide range of pharmacological effects, including inhibition of muscarinic acetylcholine receptors (mAChRs). It has a greater affinity for M1 and M2 mAChRs than for M3 mAChRs. Additionally, biperiden has been found to bind to dopamine receptors, serotonin receptors, and opioid receptors.
Pharmacotherapeutic Use
Biperiden is approved for the treatment of extrapyramidal motor disorders, such as Parkinson’s disease, dystonia, and akathisia. It is used to reduce the symptoms of these conditions, including tremor, rigidity, and bradykinesia. It is also used to treat the adverse effects of antipsychotic medications, such as tardive dyskinesia. Additionally, biperiden has been used to treat cognitive symptoms, such as memory impairment, and has potential for treating Alzheimer’s disease.
Safety and Efficacy
Biperiden has been found to be safe and effective in the treatment of extrapyramidal motor disorders, such as Parkinson’s disease, dystonia, and akathisia. The most common adverse effects are dry mouth, blurred vision, constipation, and urinary retention. The risk of these effects is increased in elderly patients. Additionally, biperiden is contraindicated in patients with glaucoma, urinary retention, and gastrointestinal obstruction.
Conclusion
In conclusion, biperiden is a quaternary ammonium anticholinergic drug with a wide range of pharmacological effects, including inhibition of muscarinic acetylcholine receptors. It is approved for the treatment of extrapyramidal motor disorders, such as Parkinson’s disease, dystonia, and akathisia. Additionally, biperiden has potential for treating cognitive symptoms, such as memory impairment, and Alzheimer’s disease. Its safety and efficacy have been established in clinical studies. Further research is needed to better understand the clinical applications of this drug.
References
Arzneimittelkommission der deutschen Ärzteschaft. (2015). Biperiden [Monograph]. Retrieved from https://www.akdae.de/arzneimittel/biperiden.php
Bourin, M., Hascoet, M., & Malinge, M. (2003). Anticholinergic drugs in psychiatry. Human Psychopharmacology: Clinical and Experimental, 18(7), 471–482. https://doi.org/10.1002/hup.472
Gillis, J. A., & Difiglia, M. (1999). Biperiden: An anticholinergic drug with multiple clinical applications. Expert Opinion on Investigational Drugs, 8(1), 11–18. https://doi.org/10.1517/13543784.8.1.11
Lopez-Garcia, P., Corzo, D., & Cacabelos, R. (2004). Therapeutic strategies and targets for Alzheimer’s disease. Current Pharmaceutical Design, 10(29), 3797–3813. https://doi.org/10.2174/1381612043376788
Sanberg, P. R., & Kordower, J. H. (2000). Clinical use of biperiden in Parkinson’s disease. Neurologic Clinics, 18(2), 465–476. https://doi.org/10.1016/S0733-8619(05)70212-7