What is Biperiden?
Biperiden, sold under the brand name Akineton, is an anticholinergic medication [1.6.2]. It was first approved for medical use in the United States in 1959 [1.4.1]. The drug works by blocking central cholinergic receptors, which helps to re-balance neurotransmitter activity in the brain [1.6.3]. Its primary function was as an adjunct therapy for all forms of parkinsonism, including Parkinson's disease, to improve muscle control, reduce stiffness, and allow for more normal body movements [1.2.1, 1.2.6].
Additionally, biperiden was prescribed to manage extrapyramidal symptoms (EPS). These are drug-induced movement disorders that can occur as side effects of certain antipsychotic (neuroleptic) medications [1.2.1, 1.4.5]. It was effective in relieving muscle rigidity and reducing issues like abnormal sweating and salivation [1.6.2].
The Discontinuation of Biperiden in the United States
Despite its long history, biperiden is no longer marketed or commercially available in the United States [1.2.2, 1.2.4, 1.3.2]. The medication, which was sold by Abbott, has been officially discontinued [1.2.1]. While it remains on the World Health Organization's List of Essential Medicines, its availability in the U.S. has ceased [1.2.3]. Reports indicated it was not commercially available as early as 2017, and it was noted as no longer being marketed by 2020 [1.2.2].
Mechanism of Action
Biperiden is a muscarinic antagonist that affects both the central and peripheral nervous systems [1.4.2]. In conditions like Parkinson's disease, there is an imbalance between the neurotransmitters dopamine and acetylcholine. Biperiden works by blocking M1 muscarinic acetylcholine receptors, which helps to decrease cholinergic activity, thereby helping to restore the balance and alleviate motor symptoms [1.6.1, 1.6.5]. It may also block the reuptake of dopamine, which further increases dopaminergic activity [1.6.3]. This dual action made it useful for treating rigidity and tremors associated with Parkinson's and similar conditions [1.4.3].
Common Side Effects and Risks
Like other anticholinergic medications, biperiden came with a range of potential side effects. The most common ones were related to its primary mechanism and included:
- Dry mouth [1.6.2]
- Blurred vision [1.6.2]
- Drowsiness and sleepiness [1.2.2, 1.6.3]
- Confusion, especially in elderly patients [1.6.2]
- Constipation [1.6.3]
- Urinary retention [1.6.3]
- Dizziness [1.6.1]
High doses could lead to more severe central nervous system effects like agitation, confusion, and hallucinations [1.6.1]. Due to these risks, it was not recommended for individuals with conditions like bowel obstruction or narrow-angle glaucoma [1.2.2].
Alternatives to Biperiden
With biperiden no longer available in the US, clinicians rely on other anticholinergic agents and different classes of medication to manage Parkinson's disease and extrapyramidal symptoms. The two most common anticholinergic alternatives are Benztropine and Trihexyphenidyl [1.7.1].
- Benztropine (Cogentin): This medication has both anticholinergic and antihistaminic properties [1.7.3]. It is often preferred for geriatric patients because it causes a lower level of CNS stimulation compared to trihexyphenidyl [1.7.4].
- Trihexyphenidyl (Artane): This is a potent anticholinergic used for the same indications as biperiden was [1.7.1, 1.7.6].
- Diphenhydramine (Benadryl): An antihistamine with significant anticholinergic effects, it can also be used to treat acute extrapyramidal reactions [1.5.2, 1.5.3].
- Amantadine: This drug is a dopamine agonist and can be an alternative for managing drug-induced parkinsonism, with fewer anticholinergic effects [1.5.5, 1.5.6].
Comparison of Biperiden Alternatives
| Feature | Biperiden (Discontinued) | Benztropine | Trihexyphenidyl |
|---|---|---|---|
| Primary Mechanism | Anticholinergic (M1 antagonist) [1.6.1] | Anticholinergic & Antihistaminic [1.7.3] | Anticholinergic (central antimuscarinic) [1.7.3] |
| Primary Uses | Parkinson's, Drug-induced EPS [1.2.1] | Parkinson's, Drug-induced EPS [1.7.4] | Parkinson's, Drug-induced EPS [1.7.6] |
| Common Side Effects | Dry mouth, blurred vision, confusion [1.6.2] | Dry mouth, blurred vision, constipation, urinary retention [1.7.3] | Anxiety, confusion, agitation, dry mouth [1.7.3] |
| US Availability | No, discontinued [1.2.4] | Yes, as a generic [1.7.1] | Yes, as a generic [1.7.1] |
| Geriatric Use | Caution advised due to confusion risk [1.6.2] | Often preferred due to less CNS stimulation [1.7.4] | Used with caution, can cause more stimulation [1.7.4] |
Conclusion
To summarize, the answer to the question 'Is biperiden available in the US?' is a definitive no. While it was once an effective treatment for Parkinson's disease and medication-induced movement disorders, it has been discontinued and is no longer marketed in the United States [1.3.1, 1.3.2]. Patients and healthcare providers now utilize alternative anticholinergic medications like benztropine and trihexyphenidyl, among other drug classes, to manage these conditions [1.7.1]. These alternatives have similar efficacy but also carry their own profiles of side effects that require careful management by a healthcare professional.
For more information on medications for Parkinson's disease, an authoritative source is the National Institute of Neurological Disorders and Stroke.
