Biperiden

Biperiden Oral

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.

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.

Uses

Biperiden is a muscarinic receptor antagonist used to treat parkinsonism and control extrapyramidal side effects of neuroleptic drugs.

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

Biperiden is also used to associated treatment for these conditions: Extrapyramidal disorder caused by neuroleptic drugs without Tardive dyskinesia, Parkinson's Disease (PD), Poisoning caused by Nicotine, Poisoning caused by organophosphorus pesticides, Extrapyramidal reaction

How Biperiden works

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.

Biperiden

Structure

Toxicity

LD₅₀=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.

Food Interaction

• Avoid alcohol.
• Take with food.

Biperiden Alcohol interaction

[Moderate] GENERALLY AVOID:

Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.

In addition, the potential for abuse may be increased with the combination.

The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.

No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.

However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.

Alcohol should generally be avoided during therapy with anticholinergic agents.

Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.

Biperiden Hypertension interaction

[Minor] Cardiovascular effects of anticholinergics may exacerbate hypertension.

Therapy with anticholinergic agents should be administered cautiously in patients with hypertension.

Biperiden Drug Interaction

Moderate: valproic acid, valproic acid

Minor: acetaminophen, acetaminophen

Unknown: aspirin, aspirin, charcoal, charcoal, epinephrine, epinephrine, lithium, lithium, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, cholecalciferol, cholecalciferol, phytonadione, phytonadione

Biperiden Disease Interaction

Major: autonomic neuropathy, GI obstruction, glaucoma, obstructive uropathy, tardive dyskinesia, infectious diarrhea

Moderate: cardiac disease, liver disease

Minor: hypertension, hyperthyroidism

Elimination Route

87% bioavailability

Innovators Monograph

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