Drug/Small Molecule:
biperiden

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB contains no drug labels with pharmacogenomic information for this drug/small molecule. To report a drug label with PGx, click here.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

? = Mouse-over for quick help

This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Beperiden
  • Biperiden Hydrochloride
  • Biperiden [Usan:Ban:Inn:Jan]
  • Biperidene Hydrochloride
  • Biperidene [INN-French]
  • Biperideno [INN-Spanish]
  • Biperidenum [INN-Latin]
  • Biperidine
  • Biperidine Hydrochloride
Trade Names
  • Akineton
  • Akinophyl
Brand Mixture Names

PharmGKB Accession Id:
PA448626

Description

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.

Source: Drug Bank

Indication

For use as an adjunct in the therapy of all forms of parkinsonism and control of extrapyramidal disorders secondary to neuroleptic drug therapy.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance.

Source: Drug Bank

Pharmacology

Biperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. The parenteral form of biperiden is an effective and reliable agent for the treatment of acute episodes of extrapyramidal disturbances sometimes seen during treatment with neuroleptic agents. Akathisia, akinesia, dyskinetic tremors, rigor, oculogyric crisis, spasmodic torticollis, and profuse sweating are markedly reduced or eliminated. With parenteral biperiden, these drug-induced disturbances are rapidly brought under control.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

The metabolism of biperiden is not completely understood, but does involve hydroxylation.

Source: Drug Bank

Protein Binding

60%

Source: Drug Bank

Absorption

87% bioavailability

Source: Drug Bank

Toxicity

LD 50=760 mg/kg (Orally in rats). Signs of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.

Source: Drug Bank

Chemical Properties

Chemical Formula

C21H29NO

Source: Drug Bank

Isomeric SMILES

C1CCN(CC1)CC[C@]([C@@H]2C[C@H]3C[C@@H]2C=C3)(C4=CC=CC=C4)O

Source: Drug Bank

OC(CCN1CCCCC1)(C1CC2CC1C=C2)C1=CC=CC=C1

Source: Drug Bank

Canonical SMILES

OC(CCN1CCCCC1)(C1CC2CC1C=C2)C1=CC=CC=C1

Source: Drug Bank

Average Molecular Weight

311.4611

Source: Drug Bank

Monoisotopic Molecular Weight

311.224914555

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
CHRM1 (source: Drug Bank)
CHRNA2 (source: Drug Bank)

Drug Interactions

Drug Description
donepezil Possible antagonism of action (source: Drug Bank)
donepezil Possible antagonism of action (source: Drug Bank)
galantamine Possible antagonism of action (source: Drug Bank)
galantamine Possible antagonism of action (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
rivastigmine Possible antagonism of action (source: Drug Bank)
rivastigmine Possible antagonism of action (source: Drug Bank)
biperiden Possible antagonism of action (source: Drug Bank)
biperiden Possible antagonism of action (source: Drug Bank)
biperiden Possible antagonism of action (source: Drug Bank)
biperiden Possible antagonism of action (source: Drug Bank)
biperiden The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
biperiden The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
biperiden The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Biperidin, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents. (source: Drug Bank)
biperiden The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Biperidin, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents. (source: Drug Bank)
biperiden Trimethobenzamide and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
biperiden Triprolidine and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
biperiden Triprolidine and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)
biperiden Trospium and Biperiden, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects. (source: Drug Bank)

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to biperiden: 1

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Anti-Parkinson's disease drugs and pharmacogenetic considerations. Expert opinion on drug metabolism & toxicology. 2013. AgĂșndez JosĂ© A G, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
49884-693-01
DrugBank:
DB00810
ChEBI:
3112
KEGG Compound:
C07941
KEGG Drug:
D00779
PubChem Compound:
2381
PubChem Substance:
153864
46508325
Drugs Product Database (DPD):
124982
BindingDB:
50240680
ChemSpider:
2289
Therapeutic Targets Database:
DAP001125
FDA Drug Label at DailyMed:
b4dc473f-fbd3-4ad9-83af-5ed2a33e6eae

Clinical Trials

These are trials that mention biperiden and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.