Biperiden is one of the most important antiparkinsonian drugs. The basis of its action is based on the inhibition of acetylcholine. The active ingredient has been on the market since 1953 under the trade name Akneton.
What is biperiden?
Biperiden is one of the most important antiparkinsonian drugs. The active ingredient has been on the market since 1953 under the trade name Akneton. Biperiden is an anticholinergic. It acts on the muscarinic acetylcholine receptors in such a way that the effectiveness of acetylcholine is reduced, especially in the parasympathetic nervous system. The active ingredient is used, among other things, for the symptomatic treatment of Parkinson’s disease. Biperiden has also been shown to be successful in attenuating the side effects of psychotropic drugs and is therefore also used in this field. In drugs, the active ingredient is present as biperidene hydrochloride. Chemically, this is a white, crystalline powder that dissolves only with difficulty in water. In addition to its anticholinergic influence, biperiden also has mood-lifting and euphoric effects. Therefore, there is a risk of abuse. Biperiden is administered in tablet form and, in emergency cases of poisoning, as a solution for injection.
Pharmacologic effects
Biperiden exerts its effects by inhibiting muscarinic receptors for acetylcholine in the parasympathetic nervous system. In this process, the action of acetylcholine is suppressed with the consequence of reducing important body functions related to the parasympathetic nervous system. So what is the mechanism by which the symptoms of Parkinson’s can be treated? It is necessary to know that Parkinson’s is caused by a deficiency of the neurotransmitter dopamine. This deficiency results from the death of dopamine-producing nerve cells. Dopamine is responsible for the coordination of movement sequences. However, in addition to dopamine, other neurotransmitters are responsible for the transmission of stimuli in the nerve cells, including acetylcholine. However, due to dopamine deficiency, there is an imbalance between acetylcholine and dopamine. Thus, acetylcholine is now present in relative excess and thus amplifies the uncoordinated conduction of stimuli. Various options are now available for the treatment of Parkinson’s disease. Either dopamine precursors b. w. Dopamine degradation inhibitors are used or the relative excess of acetylcholine is reduced. A combination treatment is also possible. Anticholinergics, such as biperides, are considered for inhibition of acetylcholine action. However, when treated with anticholinergics, one must simultaneously accept the side effects associated with the inhibition of acetylcholine.
Medical application and use
The most important use of biperiden, as already stated, is in the treatment of the symptoms of Parkinson’s disease. Parkinson’s is generally characterized by increasingly uncoordinated and involuntary movements. A major symptom is the lack of movement. Dexterity decreases during rapid movements. Tremor (trembling) and muscle stiffness (rigor) are also present. Furthermore, there is gait and stance insecurity. As already mentioned, Parkinson’s is caused by an imbalance of dopamine and acetylcholine. One way of influencing this is treatment with anticholinergics, such as biperides. When choosing a drug, the relationship between treatment success and side effects must of course also be considered. In the case of Parkinson’s, anticholinergics do less well in this regard compared to other agents. The side effects due to acetylcholine inhibition do play a significant role. More commonly, anticholinergics, such as biperiden, are now used in secondary PD due to treatment with psychotropic drugs. So-called dyskinesias can occur during this treatment. These are disturbances in the physiological movement of organs, parts of the body or an entire region of the body. These often occur in the form of cramps, spasmodic movements or tics. Here, the use of biperides shows good results. Other areas of application are still poisoning with pesticides or nicotine.
Risks and side effects
Due to its anticholinergic properties, the use of biperiden elicits several typical side effects. These include dry mouth due to reduction of secretion and saliva production, constipation, indigestion, urinary retention, and decreased sweating. Visual disturbances and increase in heart rate may also occur.Furthermore, central nervous disorders such as dizziness, fatigue, excitability or even hallucinations are also observed. These side effects are the result of a reduced acetylcholine effect. However, as with all drugs, there are also direct hypersensitivities to biperiden. In this case, in epilepsy, in dementia, and in gastrointestinal tract obstruction, its use is contraindicated. This also applies in cardiac arrhythmias and muscle weakness. During pregnancy and lactation, biperiden should be taken only under medical supervision.