Akineton Side Effects & Drug Interactions SIDE EFFECTS Atropine-like side effects such as dry mouth; blurred

vision; drowsiness; euphoria or disorientation; urinary retention; postural hypotension; constipation; agitation; disturbed behavior may been seen. A case of generalized choreic movements has been reported in a Parkinson's disease patient when biperiden was added to carbidopa/levodopa. A reduction in rapid eye movement (REM) sleep, characterized by increased REM latency and decreased percentage of REM sleep, has been reported. There usually are no significant changes in blood pressure or heart rate in patients who have been given the parenteral form of AKINETON. Mild transient postural hypotension and bradycardia may occur. These side effects can be minimized or avoided by slow intravenous administration. No local tissue reactions have been reported following intramuscular injection. If gastric irritation occurs following oral administration, it can be avoided by administering the drug during or after meals. The central anticholinergic syndrome can occur as an adverse reaction to properly prescribed anticholinergic medication. See OVERDOSAGE section for signs and symptoms of the central anticholinergic syndrome, and for treatment. DRUG INTERACTIONS The central anticholinergic syndrome can occur when anticholinergic agents such as AKINETON are administered concomitantly with drugs that have secondary anticholinergic actions, e.g., certain narcotic analgesics such as meperidine, the phenothiazines and other antipsychotics, tricyclic antidepressants, certain antiarrhythmics such as the quinidine salts, and antihistamines. See OVERDOSAGE section for signs and symptoms of the central anticholinergic syndrome, and for treatment. CLINICAL PHARMACOLOGY AKINETON is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, AKINETON possesses nicotinolytic activity. 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 AKINETON is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance. The parenteral form of AKINETON 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 AKINETON, these drug-induced disturbances are rapidly brought under control. Subsequently, this can usually be maintained with oral doses which may be given with tranquilizer therapy in psychotic and other conditions requiring an uninterrupted therapeutic program. Pharmacokinetics and Metabolism Only limited pharmacokinetic studies of biperiden in humans are available. The serum concentration at 1 to 1.5 hours following a single, 4 mg oral dose was 4-5 ng/mL. Plasma levels (0.1-0.2 ng/mL) could be determined up to 48 hours after dosing. Six hours after an oral dose of 250 mg/kg in rats, 87% of the drug had been absorbed. The metabolism of AKINETON is also incompletely understood, but does involve

hydroxylation. In normal volunteers a single 10 mg intravenous dose of biperiden seemed to cause a transient rise in plasma cortisol and prolactin. No change in GH, LH, FSH, or TSH levels were seen. Biperiden lactate (10 mg/mL) was not irritating to the tissue of rabbits when injected intramuscularly (1.0 mL) into the sacrospinalis muscles and intradermally (0.25 mL) and subcutaneously (0.5 mL) into the shaved abdominal skin. AKINETON CONSUMER IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you. BIPERIDEN - ORAL (bye-PER-i-den) COMMON BRAND NAME(S): Akineton USES: Biperiden is used to treat symptoms of Parkinson's disease or involuntary movements due to the side effects of certain psychiatric drugs (antipsychotics such as chlorpromazine/haloperidol). Biperiden belongs to a class of medication called anticholinergics that work by blocking a certain natural substance (acetylcholine). This helps decrease muscle stiffness, sweating, and the production of saliva, and helps improve walking ability in people with Parkinson's disease. Anticholinergics can stop severe muscle spasms of the back, neck, and eyes that are sometimes caused by psychiatric drugs. It can also decrease other side effects such as muscle stiffness/rigidity (extrapyramidal signs-EPS). It is not helpful in treating movement problems caused by tardive dyskinesia and may worsen them. HOW TO USE: Take this medication by mouth, usually 1 to 4 times a day with meals and at bedtime or as directed by your doctor. Your doctor may start you at a low dose and increase your dose slowly to find the best dose for you. The usual maximum dose is 16 milligrams each day. The dosage is based on your medical condition and response to therapy. Take this medication regularly in order to get the most benefit from it. To help you remember, take it at the same times each day. Take this medication at least 1 hour before antacids containing magnesium, aluminum, or calcium. Allow at least 1-2 hours between doses of biperiden and certain drugs for diarrhea (adsorbent antidiarrheals such as kaolin, pectin, attapulgite). Take this medication at least 2 hours after ketoconazole. Antacids and some drugs for diarrhea may prevent the full absorption of biperiden, and this product may prevent the complete absorption of ketoconazole when these products are taken together.

If you are taking this medication for side effects from another medication, your doctor may instruct you to take it on a regular schedule or only as needed. If you are taking this medication for Parkinson's disease, your doctor may change the dose of your other medications (e.g., levodopa). Follow your doctor's instructions closely. When used for an extended period, this medication may not work as well and may require different dosing. Talk with your doctor if this medication stops working well. Rarely, abnormal drug-seeking behavior (addiction) is possible with this medication. Do not increase your dose, take it more frequently, or use it for a longer time than prescribed. Properly stop the medication when so directed. Some conditions may become worse when the drug is abruptly stopped. Your dose may need to be gradually decreased. Tell your doctor if your condition does not improve or if it worsens.

AKINETON CONSUMER IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you. BIPERIDEN - ORAL (bye-PER-i-den) COMMON BRAND NAME(S): Akineton USES: Biperiden is used to treat symptoms of Parkinson's disease or involuntary movements due to the side effects of certain psychiatric drugs (antipsychotics such as chlorpromazine/haloperidol). Biperiden belongs to a class of medication called anticholinergics that work by blocking a certain natural substance (acetylcholine). This helps decrease muscle stiffness, sweating, and the production of saliva, and helps improve walking ability in people with Parkinson's disease. Anticholinergics can stop severe muscle spasms of the back, neck, and eyes that are sometimes caused by psychiatric drugs. It can also decrease other side effects such as muscle stiffness/rigidity (extrapyramidal signs-EPS). It is not helpful in treating movement problems caused by tardive dyskinesia and may worsen them. HOW TO USE: Take this medication by mouth, usually 1 to 4 times a day with meals and at bedtime or as directed by your doctor. Your doctor may start you at a low dose and increase your dose slowly to find the best dose for you. The usual maximum dose is 16 milligrams each day. The dosage is based on your medical condition and response to therapy.

Take this medication regularly in order to get the most benefit from it. To help you remember, take it at the same times each day. Take this medication at least 1 hour before antacids containing magnesium, aluminum, or calcium. Allow at least 1-2 hours between doses of biperiden and certain drugs for diarrhea (adsorbent antidiarrheals such as kaolin, pectin, attapulgite). Take this medication at least 2 hours after ketoconazole. Antacids and some drugs for diarrhea may prevent the full absorption of biperiden, and this product may prevent the complete absorption of ketoconazole when these products are taken together. If you are taking this medication for side effects from another medication, your doctor may instruct you to take it on a regular schedule or only as needed. If you are taking this medication for Parkinson's disease, your doctor may change the dose of your other medications (e.g., levodopa). Follow your doctor's instructions closely. When used for an extended period, this medication may not work as well and may require different dosing. Talk with your doctor if this medication stops working well. Rarely, abnormal drug-seeking behavior (addiction) is possible with this medication. Do not increase your dose, take it more frequently, or use it for a longer time than prescribed. Properly stop the medication when so directed. Some conditions may become worse when the drug is abruptly stopped. Your dose may need to be gradually decreased. Tell your doctor if your condition does not improve or if it worsens.

AKINETON SUMMARY
AKINETON Tablets (biperiden hydrochloride) Each AKINETON tablet for oral administration contains 2 mg biperiden hydrochloride. Other ingredients may include corn syrup, lactose, magnesium stearate, potato starch and talc. AKINETON is an anticholinergic agent. Biperiden is -5-Norbornen-2-yl--phenyl-1-piperidinepropanol. It is a white, crystalline, odorless powder, slightly soluble in water and alcohol. It is stable in air at normal temperatures. AKINETON (biperiden) is indicated for the following: As an adjunct in the therapy of all forms of parkinsonism (idiopathic, postencephalitic, arteriosclerotic) Control of extrapyramidal disorders secondary to neuroleptic drug therapy (e.g., phenothiazines)
Typical antipsychotics (sometimes referred to as conventional antipsychotics or conventional neuroleptics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia), and are generally being replaced by atypical antipsychotic

drugs. Typical antipsychotics may also be used for the treatment of acute mania, agitation, and other conditions. Traditional antipsychotics are broken down into low-potency and high-potency classifications. Fluphenazine and haloperidol are examples of high-potency typical antipsychotics, and chlorpromazine is an example of a low potency antipsychotic. High-potency typical antipsychotics tend to be associated with more extrapyramidal side-effects (EPS) and less histaminic (e.g. sedation), alpha adrenergic (e.g. orthostasis) and anticholinergic (e.g. dry mouth) side effects, while low-potency typical antipsychotics tend to be associated with less EPS but more H1, alpha1, and muscarinic side effects. Depot injections Some of the high-potency antipsychotics, particularly haloperidol and fluphenazine, have been formulated as the decanoate ester(e.g. fluphenazine decanoate) to allow for a slow release of the active drug when given as a deep, intramuscular injection. This has the advantage of providing reliable dosing for a person who has trouble with compliance. Depot injections can also be used for involuntary community treatment patients to ensure compliance with a community treatment order when the patient would refuse to take daily oral medication. For practical reasons, depot preparations are limited to high-potency antipsychotics so the treating physician has a limited choice. It is therefore preferable to use oral medications if the cooperation and compliance of the patient can be obtained.

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Common side-effects Side effects vary among the various agents in this class of medications, but common side effects include: dry mouth, muscle stiffness, muscle cramping, tremors, EPS and weight-gain. EPS is a cluster of symptoms consisting of parkinsonism, dystonias, and akathisia. Anticholinergics such as benztropine and diphenhydramine are commonly prescribed to treat the symptoms of EPS. Risks of serious side-effects There is a significant risk of the serious condition tardive dyskinesia developing as a side-effect of typical antipsychotics. The risk of developing tardive dyskinesia after chronic typical antipsychotic usage varies on several factors, such as age and gender. The commonly reported incidence of TD among younger patients is about 5% per year. Among older patients incidence rates as high than 20%

per year have been reported. The average prevalence is approximately 30% [1]. There are no treatments that have consistently been shown to be effective for the treatment of tardive dyskinesias, however branched chain amino acids, melatonin, and vitamin E have been suggested as possible treatments. The atypical antipsychotic clozapine has also been suggested as an alternative antipsychotic for patients experiencing tardive dyskinesia. Tardive dyskinesia may reverse upon discontinuation of the offending agent or it may be irreversible. Neuroleptic malignant syndrome, or NMS, is a rare, but potentially fatal side effect of antipsychotic treatment. NMS is characterized by fever, muscle rigidity, autonomic dysfunction, and altered mental status. Treatment includes discontinuation of the offending agent and supportive care. Typical medications

Chlorpromazine

Fluphenazine (Prolixin) Haloperidol (Haldol)

Molindone Thiothixene Trifluoperazine Loxapine