Composition, form of production and packaging
Tablets are almost white, flat-cylindrical, on one side of which there is a cruciform risk, with chamfers.
biperidene hydrochloride 2 mg
Auxiliary substances: corn starch, lactose monohydrate, microcrystalline cellulose, calcium hydrophosphate dihydrate, potato starch, copovidone, talc, magnesium stearate, purified water.
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
20 pcs. - blisters (2) - packs of cardboard.
20 pcs. - blisters (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
The anticholinergic drug of the central action reduces the activity of the cholinergic neurons of the striatum (the structural component of the extrapyramidal system).Peripheral anticholinergic action is less pronounced. Reduces tremors and stiffness. Biperiden causes psychomotor agitation, vegetative disorders.
Suction and distribution
After taking the drug inside C max is achieved in 0.5-2 hours and is 1.01-6.53 ng / ml. C ss after taking the drug inside at a dose of 2 mg 2 times / day is achieved through 15.7-40.7 hours Bioavailability after a single oral intake is about 33 В± 5%.
Binding to plasma proteins after ingestion and parenteral administration is 91-94%. Plasma clearance is 11.6 В± 0.8 ml / min / kg.
Excreted in breast milk.
Biperiden is completely metabolized. The main metabolites are bicycloheptane and piperidine.
It is excreted in the form of metabolites with urine and feces.
Excretion is carried out in two phases. T 1/2 of the first phase is 1.5 h, T 1/2 of the second phase is 24 h.
Pharmacokinetics in special clinical cases
In elderly patients, T 1/2 may increase to 38 hours.
- Parkinsonism syndrome in adults;
- extrapyramidal symptoms in children and adults caused by neuroleptics or similarly acting drugs.
When the drug is administered internally, treatment usually begins with small doses, gradually increasing them, depending on the therapeutic effect and side effects.
When Parkinsonism adults are prescribed 1 mg 1-2 times / day. The dose can be increased by 2 mg every 24 hours. The maintenance dose is 3-16 mg / day (divided into 3-4 doses). The maximum daily dose is 16 mg. The total daily dose should be evenly divided into doses for use during the day. After reaching the optimal dose of patients should be transferred to the drug Akineton В® retard.
For motor disorders caused by the action of drugs, depending on the severity of symptoms, adults are prescribed 1-4 mg 1-4 times / day as a corrector of neuroleptic therapy, children aged 3-15 years 1-2 mg 1-3 times / day.
Tablets should be taken during or after a meal, with a liquid.
Unwanted side effects from the gastrointestinal tract can be reduced by taking the pill right after eating. The duration of treatment depends on the type of disease.When canceling Akinetton, its dose should be gradually reduced.
The experience of using the drug Akineton В® with drug dystonia in children is limited to short courses of treatment with the drug.
From the side of the central nervous system: dizziness, drowsiness, weakness, fatigue, anxiety, confusion, euphoria, memory impairment and in some cases hallucinations, delirious disorders; nervousness, headache, insomnia, dyskinesia, ataxia, muscle cramps and speech impairment. With increased excitation of the nervous system, especially in patients with impaired cerebral function, it is necessary to reduce the dose of the drug.
On the part of the digestive system: dry mouth, increased salivary glands, constipation, epigastric discomfort, nausea.
From the side of the organ of vision: paresis of accommodation, mydriasis, accompanied by photophobia, angle-closure glaucoma (the intraocular pressure should be regularly monitored).
From the cardiovascular system: tachycardia and bradycardia, lowering blood pressure.
From the urinary system: difficulty urinating, especially in patients with prostatic hyperplasia (in this case, it is recommended to reduce the dose); more rarely - urinary retention.
Other : decreased sweating, allergic reactions, drug dependence.
- an angle-closure glaucoma;
- stenosis of the gastrointestinal tract;
- obstruction of the digestive tract;
- children's age till 3 years;
- increased individual sensitivity to any of the components of the drug.
With caution should prescribe the drug for prostatic hyperplasia, urinary retention, heart rhythm disorders, elderly patients (especially in the presence of organic brain symptoms) and patients predisposed to epileptic seizures.
PREGNANCY AND LACTATION
Since the experience of using the drug Akineton В® in pregnancy is limited, it should be prescribed after a thorough assessment of the potential benefits of therapy for the mother and the possible risk to the fetus, especially in the first trimester.
Biperiden is excreted in breast milk, in which its concentrations can reach the concentrations observed in the blood plasma, therefore, during the treatment period, breastfeeding should be stopped.
APPLICATION FOR CHILDREN
Contraindicated in childhood up to 3 years.
APPLICATION IN ELDERLY PATIENTS
Caution should be given to the drug in elderly patients (especially in the presence of organic cerebral symptoms).
Side effects are observed, especially in the early stages of treatment and with too rapid a rise in the dose.
Except for life-threatening complications, abrupt withdrawal should be avoided.
In elderly patients, especially those having cerebral vascular or degenerative disorders, an increased sensitivity to the drug may often appear.
Anticholinergic drugs of central action, similar to the drug Akineton В® , may increase the predisposition to epileptic seizures. Therefore, doctors should take this fact into consideration when treating patients with this predisposition.
Late dyskinesia caused by neuroleptics may be intensified by the drug Akineton В® .
Parkinsonian symptoms in the case of advanced tardive dyskinesia in some cases are so severe that they prevent the continuation of treatment with anticholinergic drugs.
Abuse of the drug Akineton В® was noted. This phenomenon is possibly associated with improved mood and temporary euphoric effects of this drug, which are occasionally observed.
During prolonged therapy with the drug Akineton В® , intraocular pressure should be checked regularly.
Impact on the ability to drive vehicles and manage mechanisms
The administration of the drug Akineton В® , especially in combination with other central-action drugs, with anticholinergics, may impair the ability to drive and work with machinery.
Symptoms: dilated, slowly reacting to light pupils (mydriasis), dry mucous membranes, reddening of the skin, palpitations, atony of the bladder and intestines, hyperthermia, especially in children and agitation, confusion, delirium, collapse.
Treatment: antidote - inhibitors of acetylcholinesterase and, above all, physostigmine, if necessary - catheterization of the bladder. Conduction of symptomatic therapy.
The use of the drug Akineton В® in combination with other anticholinergic psychotropic drugs, with antihistamine, antiparkinsonian and antiepileptic medicines can contribute to the strengthening of central and peripheral side effects.
Simultaneous administration of quinidine can cause an increase in anticholinergic cardiovascular effects (especially AV violation).
Simultaneous administration with levodopa may increase dyskinesia.
Anticholinergics can increase the central side effects of pethidine.
When treating the drug, the oppressive effect of ethanol on the central nervous system increases.
Akineton В® weakens the effect of metoclopramide and similarly acting remedies on the digestive tract.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List A. The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C. Shelf life - 5 years.