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Manufacturers: Knoll Australia Pty Ltd
Active ingredients
- Biperiden
Disease class
- Not indicated. See instructions
Clinical and pharmacological group
- Not indicated. See instructions
Pharmacological action
- Not indicated. See instructions
Pharmacological group
- n-Ancholinergics (ganglionic blockers)
pharmachologic effect
The main substance biperiden is a centrally acting anticholinergic blocker.
The effect suggests a suppressive ability on the activity of cholinergic neurons in the striatum, which is a structural unit of the extrapyramidal system.
The drug causes a ganglion-blocking effect, antispasmodic and a moderate m-anticholinergic effect on the periphery (spasmolytic).
The use of the drug helps eliminate limb tremor, which occurs when using cholinergic drugs (for example, pilocarpine), as well as catalepsy and muscle rigidity while taking antipsychotics. Has the ability to provoke psychomotor agitation.
Stock
diyucha rechovina:
biperiden hydrochloride;
1 tablet of biperiden hydrochloride 2 mg;
additional speeches:
cornstarch; lactose, monohydrate; microcrystalline cellulose; calcium hydrogen phosphate; potato starch; copovidon; talc; magnesium stearate
Medicine form
. Pills.
Main physical and chemical authorities:
adjacent to the white color, flat-cylindrical tablets with chamfers, on one side there is a cross-shaped mark.
Pharmacotherapeutic group.
Antiparkinsonian drugs. Anticholinergic properties. Tertiary Amens. ATX code N04A A02.
Pharmacological power.
Pharmacodynamics.
The drug Akineton has a central anticholinergic effect. Peripheral anticholinergic action is expressed to a lesser extent compared with that of atropine. Biperiden competitively binds to peripheral and central muscarinic receptors (most importantly M1).
In research on animals, biperiden is observed in Parkinson-like conditions (tremor, rigidity), caused by cholinergic effects of the central action.
Thus, biperiden flows into situations that are accompanied by cholinergic hyperactivity in the central nervous system, such as Parkinson's syndrome and extrapyramidal syndrome, dopamine deficiency as a result of neuronal degeneration, as well as other symptoms, is caused and antipsychotics, which can also lead to disruption of dopaminergic neurotransmission in the basal ganglia. In this way, the balance of dopaminergic and cholinergic functions is destroyed. Cholinergic activity is clearly enhanced and can be medicinally suppressed by anticholinergic drugs such as Akineton.
Pharmacokinetics.
Immersion
Biperiden hydrochloride is readily absorbed after oral administration of 4 mg and is detected in blood plasma after 27 minutes. The maximum concentration in blood plasma of 4-7 ng/ml is achieved after 1-2 years.
Bioavailability
The bioavailability of biperiden hydrochloride when administered orally is approximately 30%.
Rozpodil
The binding of biperiden to blood plasma proteins becomes approximately 95%. The obvious volume of distribution for biperiden is equal to 24±4.1 l/kg. Biperiden easily penetrates into tissue and has a dispersion period of 0.6 years in the tissue, with the transition from the central volume to the central volume of 9.6.
Information on how biperiden penetrates the placenta every day.
Biotransformation
Biperiden is almost completely metabolized. In the section without changes, biperiden is not detected. The main metabolite of biperiden is produced by hydroxylation of the bicycloheptane ring (60%), in addition, additional hydroxylation of the piperidine ring (40%) is often observed. Numerous metabolites (such as hydroxylation products and their conjugates) are excreted in a ratio of 50:50 from excrement and feces.
Vivedennya
The terminal period of plasma refilling after a single oral administration of biperiden hydrochloride in young healthy volunteers is 11–24 years, and plasma clearance is approximately 146 L/kg. At the same time, the period of recovery from blood plasma became 25±9 years.
Summer age patients
Bioavailability
Liver debris, blood circulation, and liver enzyme activity may be reduced; in patients with a summer age, there may be less fluidity in the metabolism of the liver, and therefore, increased liver function. Availability and decreased fluidity of excretion in comparison with younger age patients. In a consistent study, older patients had 3 to 5 times higher AUC values and 2 times longer treatment periods than younger volunteers.
Vivedennya
The terminal dosage period after a one-time oral administration of the drug in summer age patients became 30±6 years. The period of survival in the equal station became 39±12 years.
Pharmacokinetic data for patients with impaired liver function and on a daily basis.
Clinical characteristics.
Showing.
Parkinson's syndrome: treatment of symptoms of Parkinson's disease, such as rigidity, tremors.
Extraramidal side effects of neuroleptics and other medications: early dyskinesia, akathisia and parkinsonism.
Contraindicated.
Increased individual sensitivity to any of the components of the drug, closed-cuta glaucoma, mechanical sounding (stenosis) of the scilicointestinal tract, megacolon, obstruction of the scilicointestinal tract.
Pharmacokinetics
«Akineton" binds to plasma proteins by 91-94%. Plasma clearance will be 11.6 ± 0.8 ml/min/kg body weight. A single dose of the oral form has a bioavailability of about 33 ± 5%.
Able to pass into breast milk.
Biperiden is completely metabolized in the human body. This substance is not detected in urine unchanged. The main metabolites are bicycloheptane and piperidine, which are excreted in feces and urine.
Elimination occurs in two phases, with a half-life (T 1/2) of 90 minutes during the first phase and 24 hours during the second phase. In elderly patients, the half-life may increase significantly.
Indications and restrictions for the drug Akineton
The drug is prescribed if there are special indications. Among them:
- Parkinson's syndrome itself. This pathology most often occurs in older people for no apparent reason.
- Secondary parkinsonism. The occurrence of the disease is associated with infectious lesions, encephalitis, and intoxication of the body with certain chemicals.
- Violation of the extrapyramidal system due to taking antipsychotics and drugs with similar effects.
- Nicotine or phosphorus poisoning. In this case, an injectable form of the drug is used.
Parkinson's disease
It is strictly forbidden to use the drug if there are such contraindications:
- individual intolerance to the active substance or auxiliary components;
- damage to the colon associated with its enlargement;
- narrowing of the lumen or obstruction of the digestive tract;
- glaucoma.
With extreme caution and under supervision, Akineton can be prescribed to patients with prostatic hyperplasia, urinary retention, and heart rhythm disturbances. Also limitations are advanced age and a tendency to epileptic seizures.
The drug can be prescribed to children. There are examples of its use during pregnancy, but in this case the expected benefits and possible risks to the fetus should be assessed (especially in the first weeks after conception). The substance may pass into breast milk. Therefore, breastfeeding should be avoided during its use.
Contraindications
The purpose of this drug is not indicated in case of individual intolerance to the active substance of the drug "Akineton".
The instructions for use inform that you should avoid prescribing the drug when diagnosing a patient with a pathology such as prostate enlargement, closed-angle glaucoma, obstructive changes in the gastrointestinal tract (pyloric stenosis, intestinal obstruction of paralytic origin).
Arrhythmias, epilepsy, breastfeeding, old age of the patient, pregnancy are factors in which Akineton is prescribed with great caution.
Interactions with other medicinal drugs and other types of interactions.
Peculiarities of stastosuvaniya
Due to episodes of life-threatening complications, it is necessary to avoid sudden administration of the drug due to the risk of an over-the-top reversal effect. Anticholinergic drugs of central action, similar to the drug Akineton, may predispose to epileptic attacks. Therefore, doctors should take into account this fact when treating patients with such variability and the drug Akineton should be administered with caution (section “Adverse reactions”). Late dyskinesia caused by neuroleptics can be enhanced by the drug Akineton. Parkinsonian symptoms in advanced tardive dyskinesia in various episodes can be so severe that they outweigh continued treatment with anticholinergic drugs. They reported about the incidence of improper intake and retention while taking biperiden, which may be associated with heightened mood and euphoric effects as a result of this medicinal procedure, which is sometimes guarded huddle.
When carrying out treatment with Akineton, it is necessary to regularly check the internal eye pressure (section “Adverse reactions”). Also, be careful when using the drug for signs of glaucoma.
Be careful when using the drug for hyperplasia of the anterior ovary, congestion. In case of bruising, patients should clear the bruising and first take the appropriate dose of biperiden. Biperiden can sometimes lead to difficulty in cutting the cut, especially in patients with hyperplasia of the anterior pelvis, and sometimes before the cut is closed.
The use of the drug Akineton in patients with myasthenia gravis is possible only with the utmost care.
For patients with illnesses that may lead to tachycardia, Akineton should be administered with caution.
In case of severe dryness in the mouth, it can be changed by frequently drinking a small amount of ripe or chewing gum without rind.
Confinement for special groups of patients
It is necessary to administer the drug with care to late-age patients who have symptoms of organic brain damage. In late-life patients, especially quiet ones, who suffer from cerebral disorders of a vascular or degenerative nature, they often experience increased sensitivity to speech when the drug is administered at therapeutic doses.
The evidence of stagnation of biperiden in children and children up to 18 years of age is limited and is expanded with a head rank for stagnation during the interim period in episodes of dystonia caused by medicinal means (for example, antipsychotics or labels lopramide and similar drugs), which may result as a side effect or symptom of intoxication.
If you take biperiden, there may be a loss of memory (see also section “Adverse reactions”).
Special notes
The drug contains lactose and should not be prescribed to patients with rare spasmodic forms of fructose intolerance, galactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome or sucrase-isomaltase deficiency.
Suspension during pregnancy or breastfeeding.
Vaginism
The fragments of the drug have been frozen for Akineton during the period of gestation, and the drug must be frozen after a thorough assessment of the risk/corrosiveness for the vagina and fetus.
Anniversary breastfeeding
Anticholinergic drugs may suppress lactation. Looking at the chemical structure of this substance, it can be assumed that it is readily excreted in breast milk, which is likely to occur during breastfeeding.
Reproductive function
It is important to use the drug Akineton on reproductive function every day.
This is due to the fluidity of the reaction during treatment with vehicles or other mechanisms.
Through side effects on the side of the central and peripheral nervous systems, such as, for example, confusion and drowsiness, when properly infused, this drug can also contribute to the fluidity of the reaction in such a world, but not carefully from the degeneration caused by the main illnesses, as it continues Cleanliness, construction and repair are actively involved in road traffic and working with electrical tools or tools with motors, and other mechanisms are even more damaged. This, zocrema, should be avoided when combined with other central nervous system drugs, anticholinergic drugs, and especially with alcohol.
Patients taking the drug should avoid potentially unsafe activities that may require a strong mental and emotional reaction.
Side effects
On the part of the central nervous system, they are manifested by asthenia, increased fatigue, drowsiness, weakness, stupor, dizziness, feelings of concern, anxiety, memory impairment, confusion, hallucinations, catalepsy, drug dependence on the drug "Akineton".
The instructions for use talk about side effects on the organ of vision - mydriasis, disturbance of accommodation.
On the part of the cardiovascular system, it is characterized by an increase in heart rate (tachycardia); sometimes - slowdown (bradycardia); when using the injection form of the drug - a decrease in blood pressure (hypotension).
From the digestive system - dry mouth, dyspeptic symptoms, constipation.
From the side of metabolic processes - a decrease in sweating.
From the urinary system - in patients with enlargement (hypertrophy) of the prostate gland - possible difficulty urinating.
Allergic manifestations: rash on the skin, itching.
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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Akineton SR, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.
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Methods of application
For intramuscular, intravenous administration, as well as oral administration of the tablet form, the drug “Akineton” is suitable.
The instructions for use indicate that Akineton therapy usually starts with small doses, then the dose of the drug is gradually increased depending on the required therapeutic effect and the presence of side effects.
Adults using the oral form of the drug begin treatment with a dose of 1 mg in 1-2 doses throughout the day or 2 mg divided into two doses per day. Further, the dosage can be increased to 8 mg in two to four doses. However, you should not increase the dose by more than 2 mg per day. Do not exceed the maximum dosage of 6-16 mg per day. A single dose of the injection form of the drug should not exceed 2.5-5 mg. This dose can be re-administered after half an hour, but the number of injections per day should not exceed 4 times. The maximum dose of the drug in injection form is 20 mg per day. When the optimal dose of the drug is reached, it is possible to switch to taking Akineton retard.
However, one should not forget about an individual approach to each specific patient when prescribing biperiden therapy.
Extrapyramidal pathology that occurs as a result of taking certain medications (antipsychotics or neuroleptics) requires the administration of this substance in a single dose of 2 mg orally or parenterally. The specified dose can be repeated every half hour. However, as stated above, the number of injections should not exceed 4 times. The oral dose of the drug should be divided into one to three doses.
Parkinson's disease involves prescribing this drug at a dose of 6-8 mg orally in 2-4 doses per day, gradually the dose can be increased to 6-16 mg.
Children under one year of age suggest the possibility of administering this drug in injection form slowly, a single dose is 1 mg or 0.2 ml. For ages from one to 6 years, 2 mg or 0.4 ml is prescribed. From 6 to 10 years - 3 mg or 0.6 ml. If necessary, this dose can be re-administered after half an hour. If there are side effects on the administration of the drug, the injection should be stopped. When carrying out therapy with the oral form of the drug at the age of 3 to 15 years, take a dosage of 1-2 mg in 1-3 doses during the day.
The tablets should not be taken on an empty stomach, but should be taken with a moderate amount of water. If unwanted side effects from the digestive system occur, you should take the drug immediately after a meal, which reduces the severity of the adverse effects of Akineton.
The instructions for use indicate that in case of nicotine poisoning in adults, this medicine is also prescribed as part of standard therapy, and its dose is 5-10 mg for injection forms, but only in cases that pose a threat to the patient’s life.
In case of poisoning with organic phosphorus mixtures, dosing of biperiden is carried out individually, which depends on the severity of the lesion. Start with a dose of 5 mg in the case of intravenous administration, repeated administrations continue until the signs of poisoning disappear.
Practical application experience
Reviews from practicing doctors and patients who have taken or are taking Akineton.
I prescribe this drug to my patients without any fear. During my medical practice, side effects were very rare. Since they were minor (nausea), we did not stop taking the drug.
Elena Igorevna, neurologist
I always prescribe Biperidine for Parkinson's disease. Side effects were present, but the therapeutic effect was also visible.
Valentin Sergeevich, neurologist
I take one tablet three times a day daily. I have been doing this for three years now and have had no side effects. Personally, this medication helps me.
Evgeniy, 41
I started taking the medicine with small doses. The effect was immediately noticeable, but when I started increasing the doses, I thought that they would put me in a psychiatric hospital. Everything around me was cloudy, I was slow to think, so I had to interrupt the course of treatment.
Alexandra Valerievna, 56
From the reviews of doctors and patients, we can conclude that the drug has a positive therapeutic effect. But the disadvantages include the presence of a number of side effects.
Interaction
«Akineton" when used simultaneously with m-anticholinergics, drugs with antihistamine and antiepileptic effects increases the severity of the latter. However, simultaneous use with metoclopramide weakens its therapeutic effect. The drug is strictly incompatible with ethanol. Prescribing quinidine significantly increases the risk of developing manifestations of dyskinesia. The M-cholinergic effect is enhanced by the use of levodopa.
special instructions
The prescription of biperiden during pregnancy and breastfeeding (lactation) requires strict indications.
Biperiden can enter the baby's body through breast milk, which is the reason for temporary refusal of breastfeeding until about
The description of the drug draws attention to the fact that when deciding whether to prescribe biperiden during pregnancy and lactation, the possible risk to the newborn and fetus is taken into account.
The elderly age of the patient becomes a risk factor when treated with this drug. Therefore, Akineton is prescribed to this category of people with great caution.
The absence of any data indicating the safety of use in childhood is the reason why the drug Akineton is not used for children.
The description of the drug (instructions for use) indicates the fact that caution is necessary when using this drug in patients with epilepsy or arrhythmia.
With prolonged use, drug dependence may develop.
The risk of developing withdrawal syndrome involves gradual cessation of Akineton therapy.
During therapy, you should avoid drinking alcohol-containing drinks.
Therapy with this drug involves the need to refrain from driving vehicles and engaging in activities that require increased concentration and rapid psychomotor reactions, as this carries a potential danger due to the risk of dizziness.
Overdose
Symptoms:
similar signs of toxicity to atropine with peripheral anticholinergic signs: dilation of the zone that responds strongly to light (mydriasis); dryness of the mucous membranes, redness of the skin, increased heart rate, atony of the mucous membranes and intestines, increased temperature (more often seen in children) and damage to the side of the central nervous system (such as: awakening , delirium, confusion and/or hallucinations). In cases of severe toxicity, there is a risk of circulatory collapse and central paralysis of the respiratory muscles.
Likuvannya:
As an antidote, it is recommended to take acetylcholinesterase inhibitors and immediately before physostigmine, which can penetrate the spinal cord and can also interfere with symptoms of central origin (and/or physostigmine salicylate in cases of a positive test for physostigmine in). Supporting the function of the cardiovascular and respiratory systems (uniform ventilation of the legs with acid), reduced heat transfer with elevated body temperature, catheterization of the urinary tract - depending on the type of symptoms.
In addition, if necessary, you can wash the pouch or change the position of the pouch in the intestinal tract.
