Biperiden: Uses, Dosage, Side Effects & Interactions

Introduction to Biperiden

Biperiden is an anticholinergic agent used primarily as a symptomatic therapy for Parkinson’s disease and other movement disorders. It is an oral medication available under various brand names, such as Akineton. Biperiden works by antagonizing muscarinic receptors in the brain, improving muscle control and reducing stiffness associated with parkinsonism.

Medical Uses of Biperiden

Biperiden is prescribed alone or together with other medicines like levodopa to treat Parkinson’s disease . It is effective in improving muscle control, reducing stiffness, and managing tremors and spasms. Biperiden is also used to control extrapyramidal side effects induced by neuroleptic drugs, such as antipsychotics. ¹

Mechanism of Action

As a muscarinic receptor antagonist, biperiden blocks the action of acetylcholine in the brain. This antimuscarinic effect leads to a reduction in the excessive activity of cholinergic neurons, which is thought to contribute to the motor symptoms of Parkinson’s disease. By restoring the balance of neurotransmitters, biperiden helps alleviate rigidity, tremors, and akinesia associated with parkinsonism. ²

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Biperiden is well absorbed orally, with peak plasma concentrations reached within 1-2 hours after administration. It undergoes extensive first-pass metabolism in the liver and is primarily excreted in the urine as metabolites. The elimination half-life of biperiden ranges from 18 to 24 hours. The onset of action is usually observed within 30-60 minutes, and the duration of effect can last up to 6-12 hours. ¹

Side Effects and Adverse Reactions

Common side effects of biperiden include dry mouth, blurred vision, constipation, urinary retention, and tachycardia. In higher doses, it may cause confusion, disorientation, hallucinations, and memory impairment. Serious adverse reactions, such as acute glaucoma, paralytic ileus, and heat stroke, have been reported rarely. Patients should be monitored for any signs of toxicity or adverse effects. ³

Safety and Warnings

Biperiden is contraindicated in patients with narrow-angle glaucoma, pyloric stenosis, and prostatic hypertrophy. It should be used with caution in elderly patients and those with cardiovascular disorders, renal impairment, or liver disease. Biperiden may interact with other anticholinergic drugs, levodopa, and alcohol, potentiating their effects. Patients should be advised about the potential for drowsiness and impaired cognitive function while taking biperiden. ¹

Usage Guidelines

The recommended starting dose of biperiden for Parkinson’s disease is 2 mg orally two to three times daily, which can be gradually increased based on the patient’s response and tolerability. The maximum daily dose should not exceed 16 mg. For extrapyramidal symptoms, the usual dose is 2 mg one to three times daily. Dosage adjustments may be necessary for elderly patients or those with renal or hepatic impairment. Missed doses should be taken as soon as remembered unless it is close to the next scheduled dose. ⁴

Side Effects and Toxicity Management

Overdose symptoms of biperiden may include excessive dry mouth, dilated pupils, flushing, fever, tachycardia, agitation, and hallucinations. In case of suspected overdose, supportive care should be provided, including monitoring of vital signs, maintaining airway patency, and administering intravenous fluids if needed. Gastric lavage and activated charcoal may be considered in cases of recent ingestion. Physostigmine, a cholinesterase inhibitor, can be used as an antidote in severe cases of anticholinergic toxicity. ¹

Clinical Studies and Efficacy

Several clinical trials have demonstrated the efficacy of biperiden in improving motor function and reducing disability in patients with Parkinson’s disease. A randomized, double-blind study compared biperiden with placebo in 60 patients and found significant improvements in rigidity, tremor, and bradykinesia scores in the biperiden group. ⁵ Another study evaluated the long-term efficacy and safety of biperiden in 50 patients over a 12-month period and reported sustained benefits in motor function and activities of daily living. ⁶

Conclusion

Biperiden is an effective antiparkinson drug that offers symptomatic relief for patients with Parkinson’s disease and drug-induced extrapyramidal symptoms. As an anticholinergic agent, it improves motor function by antagonizing muscarinic receptors in the brain. While generally well-tolerated, biperiden may cause side effects related to its antimuscarinic properties. Proper use, dosage adjustment, and monitoring are essential to optimize therapeutic benefits and minimize adverse reactions. Patients should consult their healthcare provider for personalized treatment plans and follow the prescribed regimen for the best outcomes.