Akineton® (Akineton®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceBiperidenBiperiden
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    • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    Per 1 ml of the preparation:

    active substance: biperidene lactate 5.0 mg;

    Excipients: sodium lactate 14.0 mg, water for injection 989.0 mg.

    Description:A clear, colorless solution.
    Pharmacotherapeutic group:Hollow block central
    ATX: & nbsp

    N.04.A.A.02   Biperiden

    Pharmacodynamics:

    Biperiden is the central anticholinergic agent, 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.

    Pharmacokinetics:

    The connection with plasma proteins is 91-94%. Plasma clearance is 11.6 ± 0.8 ml / min / kg of body weight. Penetrates into breast milk.

    Biperiden is completely metabolized. The main metabolites, bicycloheptane and piperidine, are excreted in urine and feces.

    Excretion is carried out in two phases with a half-life (T1/2) 1,5 h in the first phase and 24 h - in the second, in elderly patients the half-life may increase.

    Indications:

    - Parkinsonism syndrome in adults;

    - extrapyramidal symptoms in children and adults caused by neuroleptics or similarly acting drugs;

    - poisoning with nicotine or phosphorus-containing organic substances in adults.

    Contraindications:

    RaisewIndividual sensitivity to any of the drug components, angle-closure glaucoma, mechanical constriction (stenosis) of the gastrointestinal tract, megacolon, gastrointestinal obstruction.

    Carefully:When the drug is prescribed for prostatic hyperplasia, urinary retention, heart rhythm disturbances, elderly patients (especially when there is organic brain symptoms) and patients predisposed to epileptic seizures.
    Pregnancy and lactation:Since the experience of using the drug Akineton ® during pregnancy is limited, the drug should be prescribed after a thorough evaluation of the risk / benefit for the mother and fetus, especially in the first trimester.
    The drug Akineton® is excreted in breast milk in which its concentrations mayto reach the concentrations observed in the blood plasma, so you should stop breastfeeding.
    Dosing and Administration:

    Parkinson's Syndrome the of adults:

    In severe cases, treatment can be initiated with a dose of 10-20 mg of the drug Akineton® (2-4 ml injection solution) divided into several injections (two to four) that are injected intramuscularly or in the form of slow intravenous fluids throughout the day.

    Movement disorders caused by the action of drugs:

    To quickly achieve a therapeutic response, adults can be given 2.5-5 mg of the drug Akineton® (0.5-1 ml injection solution) as a single dose, administered intramuscularly or in the form of a slow intravenous injection. If necessary, the same dose can be re-entered after 30 minutes. The maximum daily dose is 10-20 mg of the drug Akineton ® (2-4 ml solution for injection).

    Children under the age of 1 year it is possible to prescribe 1 mg (0.2 ml) of the drug Akineton ®, under 6 years of age can be administered 2 mg (0.4 ml) and under 10 years of age can be administered 3 mg (0.6 ml) as a slow intravenous injection. If necessary, this dose can be re-entered after 30 minutes. Injection should be discontinued if side effects develop during administration.

    The experience with the drug Akineton ® in the treatment of dystonia in children is limited to short courses of treatment with the drug.

    Poisoning with nicotine the of adults:

    In addition to standard therapy, intramuscular injections of 5-10 mg (1-2 ml) and intravenous administration of 5 mg are recommended in cases where the patient's life is at risk.

    In case of poisoning with an organic phosphoric mixture, individual dosing of biperidene is performed, depending on the degree of poisoning. Intramuscularly 5 mg of biperidene lactate is injected with repeated injection until the symptoms of poisoning disappear.

    Side effects:

    From the central nervous system (CNS): 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 disorders. With increased excitation of the nervous system, especially in patients with impaired cerebral function, it is necessary to reduce the dose of the drug.

    Other side effects: dry mouth, salivary gland enlargement, paresis of accommodation, mydriasis accompanied by photophobia, decreased sweating, constipation, epigastric discomfort, nausea, tachycardia and bradycardia, lowering of arterial pressure, difficulty urinating, especially in patients with prostatic hyperplasia (in this case it is recommended reduce the dose) and, more rarely, urine retention, angle-closure glaucoma (should regularly monitor intraocular pressure), allergic reactions, drug dependence.

    Overdose:

    Symptoms: dilated, slowly reacting to light pupils (mydriasis); dryness of mucous membranes; redness 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. Symptomatic therapy.

    Interaction:

    The use of the drug Akineton ® in combination with other anticholinergic psychotropic drugs, with antihistamines,antiparkinsonian and antiepileptic drugs can contribute to the strengthening of central and peripheral side effects.

    Simultaneous administration of quinidine may cause an increase in anticholinergic cardiovascular effects (especially atrioventricular conduction).

    Simultaneous administration with levodopa may increase dyskinesia.

    Anticholinergics can increase the central side effects of pethidine.

    When treating the drug, the oppressive effect of alcohol on the central nervous system increases.

    Akineton ® weakens the effect of metoclopramide and similarly acting agents on the gastrointestinal tract.

    Special instructions:

    Warnings:

    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 of drug treatment 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®, 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 action of the drug Akineton®.

    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 ® was noted. This phenomenon is possibly associated with improved mood and temporary euphoric effects of this drug, which are occasionally observed.

    For prolonged therapy with the drug Akineton®, intraocular pressure should be checked regularly.

    Effect on the ability to drive transp. cf. and fur:Admission of the drug Akineton ® and especially in combination with other central drugs, anticholinergics can disrupt the ability to drive and work with machinery.
    Form release / dosage:

    Solution for intravenous and intramuscular injection, 5 mg / ml.

    Packaging:

    1 ml of the drug in an ampoule (2 ml capacity) of colorless glass, hydrolytic type I, with an impression and a white point on the top of the ampoule or a colored ring of fracture. Ampoules can be labeled in two ways: sticking labels or marking by color printing on glass.

    5 ampoules are placed in a deep-drawing film (in an open form or sealed), which, together with the instruction for use, is placed in a cardboard box.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N015243 / 02
    Date of registration:15.08.2007 / 29.11.2012
    Expiration Date:Unlimited
    The owner of the registration certificate: Desma GmbH Desma GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspSVYCH LLC SVYCH LLC Russia
    Information update date: & nbsp24.06.2017
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