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 |
| 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. PubChem (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)
ATC Therapeutic Category
- N04AA:Tertiary amines
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 Interactions
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<sub>50</sub>=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)
Isomeric SMILES Code:
C1CCN(CC1)CC[C@]([C@@H]2C[C@H]3C[C@@H]2C=C3)(C4=CC=CC=C4)O (source: Drug Bank)
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| CHRM1 |
|
(source: Drug Bank) |
| CHRNA2 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| donepezil |
|
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) |
| rivastigmine |
|
Possible antagonism of action (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.