Biperiden (Oral)

Biperiden is an anticholinergic drug used to manage the shaking and rigidity associated with Parkinson's disease.

Overview

In addition to managing Parksinon's symptoms, biperiden can also attenuate the musculoskeletal side effects of some other drugs, specifically phenothiazines, such as chlorpromazine, perphenazine and thioridazine. It is also sometimes taken by methadone users to reduce abnormal sweating.

Biperiden can help to significantly reduce the trembling and rigidity commonly seen during the early and middle stages of Parkinson's disease, though for patients suffering from the later stages of this degenerative condition, it may provide little relief. Treating Parksinson's disease typically involves both an anticholingergic drug, such as biperiden, to treat the muscoloskeletal symptoms, as well as a dopaminergic drug, such as levodopa, to slow the progression of the condition.

Biperiden is an anticholinergic drug. It works by reducing the effect of the neurotransmitter acetylcholine, resposible for muscle stimulation; attenuating this neurotransmitter thus causes muscles to relax. Anticholinergic drugs can be either nicotinic or muscarinic (targeting the body's nicotine or muscarine receptors of acetylcholine); biperiden is a muscarinic drug. Muscarinic anticholinergics typically target one of the five types of muscarine receptors, referred to as M1 through M5; biperiden binds primarily to M1. Each of the five muscarine receptors is located in different tissues throughout the body, so muscarinic anticholinergic drugs can treat a wide variety of conditions, depending on which receptor they bind with and thus which tissues they cause to receive less acetylcholine. The M1 receptors are located in exocrine glands, as well as the entire central nervous system, so like other anticholinergic drugs that bind with the M1 receptors, biperiden has a potent effect on the entire nervous and muscular system.

Biperiden was first discovered in 1953 in Germany and first patented in that country; several other countries soon followed as its benefits in treating Parkinson's disease became apparent. The drug was patented in the United States in 1957, but not approved by the Food and Drug Administration for another two years. Biperiden has been named to the World Health Organization's List of Essential Medicines, a list of drugs that are considered to be the safest and most effective drugs currently available. This list is used by many countries to develop their medical infrastructure.

In addition to its anticholinergic effects, biperiden also appears to act as a FIASMA, or functional inhibitor of acid sphingomyelinase; it indirectly inhibits a cellular enzyme influential in cell reproduction. A wide variety of drugs, many of them antidepressants, have this property, which seems to be largely clinically insignificant and is not responsible for any side effects observed during clinical trials. One study suggests that approximately 6 - 7% percent of all drugs licensed for human use have indirect FIASMA effects, and indicates that the effect may have pharmaceutical importance in the future, but currently does not.

Biperiden tablets are sold in the US as Akineton. It can also be absorbed intravenously or with an intramuscular injection, but oral tablets are currently the only form commercially available in the US. In the US, Akineton costs about $50 to $100 per month. In the developing world, generic versions of the drug are often considerably less expensive, typically less than $15 for a month's supply. Biperiden as Akineton is been manufactured by Abbott Laboratories and sold by Par Pharmaceutical.

Conditions treated

  • Parkinson's disease
  • Involuntary movement from phenothiazine drugs
  • Excessive sweating from methadone

Type of medicine

  • Anticholinergic

Side effects

Biperiden's side effects are most commonly related to the dosage taken; negative side effects are typically the result of a mild overdose, and will subside as the patient metabolizes the drug. Overdoses on biperiden can be very serious, and even mild symptoms demand immediate medical attention in order to ensure that they don't progress to more serious ones.

The most common side effects of biperiden include blurry vision, drowsiness, constipation and mild to moderate nausea. These side effects are usually not the sign of an overdose, and generally subside as the patient adjusts to the drug. However, if they are particularly bothersome or persistent, the patient should seek medical attention.

In excessive doses, biperiden can be a potent depressant of the central nervous system, and a mild overdose may somewhat resemble a drunken stupor. In cases of mild overdose, patients may feel euphoric, dizzy, lightheaded, irritable or very tired. Uncomfortable psychological side effects, including delirium, delusions, and paranoia, may also occur in cases of moderate overdose.

More serious cases of overdose can be very dangerous, and include confusion, including uncertainty about location and identity, memory loss, difficulty walking, shortness of breath, chills and a slow or irregular heartbeat. The most serious cases of overdose have included seizures, stopped breathing or heartbeat and complete loss of consciousness; an untreated overdose on biperiden could certainly be fatal, especially in children. Changes in consciousness are typically the first signs of an overdose, and patients should seek medical attention immediately if they begin to experience even mild signs of an overdose because they may rapidly progress to more serious symptoms.

Urinary side effects while taking biperiden may be a sign of kidney problems. Talk with your doctor immediately if you begin to urinate smaller volumes or less frequently, or have difficulty or pain when urinating.

Biperiden affects the exocrine glands, including glands and ducts for sweat, saliva, tears, and mucous. The most significant and dangerous consequence of this is hyperthermia, if the patient is not sweating enough to cool their body. Patients may also find that they produce less saliva or mucous while using biperiden, and may need to symptomatically treat dry mouth or eyes.

Dosage

Currently, the oral dose of biperiden is the only formulation commercially available. It is sold as 2 mg tablets.

For the treatment of Parkinson's disease, most patients begin by taking a 2 mg tablet three or four times per day, with the dose increasing until the ideal reaction is achieved. However, dosage will only rarely exceed 16 mg per day.

Patients using biperiden to treat the side effects of phenothiazine drugs or methadone usually take a 2 mg tablet between one and three times each day, and should discuss its effectiveness with their doctor to determine an ideal dosage.

Biperiden is approved for use in children as young as one year old, but dosage guidelines are not clear for pediatric patients. Each child prescribed biperiden will have their dose uniquely determined by their doctor.

Biperiden doesn't necessarily need to be taken with food, but many patients prefer to take it with a meal or snack in order to reduce nausea; this does not reduce its effectiveness.

If a patient misses a dose of biperiden, they should take it as soon as they remember, unless it is nearly time for their next dose, in which case they should skip it and resume their regular dosing schedule. Patients should never take an extra or larger dose to make up for a missed dose.

Interactions

Patients should not use biperiden alongside other anticholinergic drugs, because this could create a dangerous disruption in the body's flow of the neurotransmitter acetylcholine, called anticholinergic syndrome. Anticholinergic syndrome is essentially synonymous with an overdose of biperiden, but can be even more dangerous if multiple different muscarine receptor types are being targeted simultaneously.

Biperiden should not be taken alongside supplemental potassium; this can cause a dangerous interaction in the stomach and intestines, leading to severe nausea and even, in rare cases, ulcers.

Biperiden can reduce the effectiveness of metoclopramide, a drug widely prescribed to manage gastrointestinal problems.

Biperiden should not be used alongside the antiarrythmia drug quinidine, because it may increase the anticholingergic action of biperiden and increase the likelihood of a dangerous overdose.

Patients should not drink alcohol in excess while taking biperiden, since this could amplify biperiden's effects as a central nervous system depressant and result in dangerous intoxication. Even amounts of alcohol that would have been modest before taking biperiden may become dangerous while using this medication. In addition to alcohol, all central nervous system depressants should be avoided while using biperiden, including not only drugs of abuse and anesthetics, but also several common over the counter drugs, such as cold medicines and antihistamines.

Warnings

Biperiden should not be used by patients who have ever had an allergic reaction to it. It is unclear whether or not patients who have had allergic reactions to other anticholinergic drugs would be similarly effected by biperiden, as there is little research into this, but if this is the case patients should proceed with caution and be monitored for symptoms of anaphylaxis while they begin a regimen of biperiden. Allergic reactions to biperiden are very rare, but can occur.

Patients who experience seizures or have heart problems should be extremely careful when using biperiden, since the drug could, in rare cases, severely exacerbate these conditions.

Biperiden should be used with caution or avoided by patients with com/health/coma/">glaucoma, because similar anticholinergic drugs are known to increase pressure on the eyes.

Biperiden should also be used with caution by patients with severe chronic constipation or an enlarged colon (megacolon), because its depressant effects could worsen these conditions.

Biperiden is classified as pregnancy category C, meaning it is unclear whether or not the drug will harm a developing fetus, since no study has carefully examined this. It has also not been studied in women who are breast feeding. Given the lack of available information, biperiden should be avoided by women who are pregnant or breast feeding, if possible.

Biperiden has the potential to be abused because of its effects as a depressant of the central nervous system, which can cause euphoria and relaxation. Patients with a history of drug or alcohol abuse should be very careful when using biperiden and may need to be closely monitored for signs of overuse.

Since biperiden can sometimes cause blurred vision, drowsiness or acute central nervous system depression, patients should avoid driving or operating machinery until they thoroughly understand how the drug effects them.

Biperiden is not recommended for patients suffering from tardive dyskinesia, a side effect of some medications that includes involuntarily motions and muscle tics; while tardive dyskinesia can sometimes resemble the movement-related drug side effects that biperiden can effectively treat, they are very different conditions, and should not be confused.

Storage

Biperiden should be stored at room temperature (approximately 59 to 77 degrees Fahrenheit, or 15 to 25 Celsius). It should be kept in a closed container and protected from excessive heat and direct light. It should also be protected from moisture, and thus not stored in a bathroom that becomes steamy while bathing. Biperiden should never be frozen.

Biperiden should be kept out of the reach of children.

If biperiden has expired or is no longer needed, it should properly disposed of at a drug drop off location, such as at a police station or fire department, rather than flushed or thrown in the trash where it could enter the ecosystem.

Summary

Biperiden can be a valuable tool for the management of Parkinson's disease, as well as the side effects of phenothiazine drugs and methadone. While it cannot control the neurological deterioration of Parkinson's disease, it is remarkably effective at managing the muscoloskeletal symptoms experienced at its earlier stages, including shaking, stiffness, and rigidity. When taken alongside a dopamingergic drug intended to slow the disease's progression, biperiden is a cornerstone of modern treatment for Parksinson's disease.

Patients using biperiden must not drink alcohol or use central nervous system depressants in excess, or take it alongside other anticholinergic drugs, and they should always be mindful of their consciousness in case they begin to experience signs of an overdose. While overdoses can be very dangerous, the drug's side effects are typically very mild if used as directed, and there appear to be no documented cases of death from biperiden use. Biperiden's inclusion on the World Health Organization's List of Essential Medicines attests to its safety and effectiveness.

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Last Reviewed:
December 25, 2017
Last Updated:
April 04, 2018
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