Bezac® (BEZAK®)

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: & nbsppills
    Composition:

    For one tablet:

    Active substance:


    Biperidena hydrochloride

    2 mg

    Excipients:


    MicrocristaAll-purposelulose

    192 mg

    TOarboximetistarch Mr.atriI

    5 mg

    Magnesium stearate

    1 mg
    Description:

    Round, flat-cylindrical tablets, almost white, with a facet and a risk.

    Pharmacotherapeutic group:Hollow block central
    ATX: & nbsp

    N.04.A.A.02   Biperiden

    Pharmacodynamics:

    Anticholinergic drug of central action. Biperiden selectively blocks central n-cholinergic receptors and peripheral m-cholinergic excitation transfer. By blocking the cholinergic receptors, the drug reduces the effect of acetylcholine on the cholinergic structures and levels the neurotransmitter balance between acetylcholine and dopamine. Peripheral anticholinergic action is less pronounced. Reduces tremors and stiffness. Biperiden causes psychomotor agitation, vegetative disorders.

    Pharmacokinetics:

    Quickly absorbed from the digestive tract. After taking the drug inside CmOh is achieved after 0.5-2 hours and is 1.01-6.53 ng / ml. Due to extensive metabolism during the initial passage through the liver, the bioavailability is 30%. Binding to plasma proteins - 91-94%, the volume of - (24±4.1) l / kg. Plasma clearance is 11.6 ± 0.8 ml / min / kg. Biperiden completely metabolized - subjected to hydroxylation; the main metabolites are bicycloheptane and piperidine. The excretion of biperidene occurs in two phases. T1/2 the first phase is 1.5 h, T1/2 second phase - 24 h. T1/2 - about 20 hours, however the concentration of drug in plasma 0.1-0.2 ng / ml can be determined later and 48 hr after administration. In elderly patients, T1/2 can increase up to 38 hours. Biperiden is excreted by the kidneys and through the intestine; penetrates into breast milk.

    Indications:

    Parkinsonism syndrome.

    Extrapyramidal symptoms (tremor, muscle rigidity, torsion dystonia, local forms of dystonia, including paroxysmal dyskinesia, hyperkinesia trochaic, tics of various shapes, myoclonus, and hyperkinesia, dystonia of the limbs, trunk, neck, face, akinesia, akathisia) caused by antipsychotic drugs or similarly acting drugs.

    Contraindications:

    Hypersensitivity to the drug components, ileus, prostatic hypertrophy with urinary retention, angle-closure glaucoma, mechanical narrowing or obstruction of the gastrointestinal tract, children under 18 years of age (data on the efficacy and safety of the drug in children are absent).

    Carefully:

    Elderly patients, myasthenia gravis, arrhythmia, patients with a tendency to convulsive attacks, including in the anamnesis, patients with arrhythmia, prostatic hypertrophy, congestive heart failure, IHD, arterial hypertension, ileostomy / colostomy, epilepsy.

    Pregnancy and lactation:

    Experience in the use of biperiden during pregnancy is limited, so prescribe the drug during pregnancy should be followed by a thorough evaluation of the benefit / risk to the mother and fetus, especially in the first trimester.

    When biperiden is prescribed, breastfeeding should be stopped, as the drug is excreted in breast milk and the child may develop anticholinergic effects.

    Dosing and Administration:

    Inside. Tablets should be taken during or after a meal, with a liquid.

    With parkinsonism syndrome adults the initial dose is 1 mg 1-2 times a day (1/2 tablet). The dose can be increased by 2 mg (1 tablet) every day. The maintenance dose is 3-16 mg / day (1 / 2-2 tablets 3-4 times a day). The maximum daily dose is 16 mg (8 tablets). The total daily dose should be evenly divided into doses during the day.

    With extrapyramidal symptoms, caused by neuroleptics or similarly acting drugs for of adults, the initial dose, depending on the severity of the symptoms, is 1-2 mg (1 / 2-1 tablet) 1-4 times a day as a corrector of neuroleptic therapy. A single dose, depending on the severity of the symptoms, can be increased to 4 mg, and the daily dose to 16 mg.

    Unwanted side effects from the gastrointestinal tract can be reduced by taking the pill right after eating. The duration of treatment depends on the nature and course of the disease. With the elimination of biperidene, its dose should be gradually reduced.

    Side effects:

    The incidence of adverse events following the use of the drug is classified according to WHO recommendations: very frequent -> 10%; frequent -> 1% and <10%; infrequent -> 0.1% and <1%; rare -> 0.01% and <0.1%; very rare - <0.01%.

    In general, side effects develop as a result of the anticholinergic action of the drug.

    From the nervous system and sensory organs: fatigue, dizziness, speech disorders, headache, mydriasis, paresis of accommodation, drowsiness, anxiety, confusion, memory impairment, hallucinations, euphoria, angle-closure glaucoma, photophobia, disorientation in time and space, increased convulsive activity, motor agitation, catalepsy.

    From the cardiovascular system: rarely - tachycardia, lowering blood pressure; very rarely - a bradycardia.

    On the part of the digestive system: often - dry mouth; rarely - constipation, dyspepsia, nausea.

    From the genitourinary system: rarely - urine retention.

    Other: rarely - drug dependence, allergic reactions (skin rash), decreased sweating, twitching in the muscles, parotitis, side reactions from the psyche.

    Except for life-threatening complications, abrupt withdrawal should be avoided.

    Overdose:

    Symptoms (similar to the symptoms of atropine poisoning): mydriasis, dry skin, hyperemia of the face, dry mouth, dryness of the upper respiratory tract, fever, tachycardia, cardiac arrhythmias, impaired intestinal motility, urinary retention, delirium, disorientation, anxiety, hallucinations, confusion consciousness, ataxia, aggression and cramps.In severe poisoning, stupor, coma, stopping breathing and heart and death can occur.

    Treatment: gastric lavage, symptomatic therapy. As a specific antagonist, physiostigmine is recommended (1 mg IM or by slow intravenous infusion every 20 minutes, but not more than 4 mg / day). Since physiostigmine is rapidly metabolized, additional injections are sometimes necessary every 1-2 hours. For children and elderly patients, it is recommended to administer half of the standard dose. The patient should be under the supervision of the doctor at least 8-12 hours after the last appearance of the symptoms.

    Interaction:

    With the simultaneous use of biperidene:

    - with anticholinergic drugs, it is possible to strengthen central and peripheral anticholinergic effects;

    - with antipsychotic drugs (neuroleptics) increases the risk of developing tardive dyskinesia;

    - with levodopa, there may be an increase in m-cholinoblocking action and dyskinesia;

    - with quinidine increases the risk of dyskinesia (increases cholinolytic effect);

    - the action of histamine blockers is increased III-receptors;

    - the effect of anticonvulsant drugs increases;

    - decreases the effectiveness of metoclopramide.

    Biperiden potentiates the action of ethanol.

    Special instructions:

    It is necessary to avoid sudden discontinuation of treatment because of the high probability of development of withdrawal symptoms. Treatment is stopped gradually.

    To prevent the occurrence of side effects it is not recommended to increase the dose of the drug too quickly at the beginning of treatment.

    May cause neuromuscular blockade followed by muscle weakness and paralysis.

    During the treatment should not drink alcohol.

    In susceptible patients with the appointment of anticholinergic drugs at recommended therapeutic doses, confusion, euphoria, motor excitement are observed.

    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 biperiden, 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 biperidene.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 drugs containing biperidene. This phenomenon may be due to the improvement in mood and the temporary euphoric effects of this drug, which are occasionally observed.

    When carrying out long-term therapy with the drug should regularly check the intraocular pressure.

    With dry mouth, symptomatic therapy is performed and, if necessary, the dose is adjusted.

    Effect on the ability to drive transp. cf. and fur:

    The drug has a strong effect on psychomotor reactions, so patients taking the drug should refrain from engaging in potentially dangerous activities that require rapid mental and motor reactions.

    The administration of the drug, especially in combination with other central-action drugs, with anticholinergics, may impair the ability to driving and working with machinery.

    Form release / dosage:Tablets, 2 mg.
    Packaging:

    For 10 or 20 tablets in a planar cell pack.

    For 2, 5 contour cell packs (10 or 20 tablets) or 10 contour cell packs (30 tablets) together with instructions for use in a pack of cardboard.

    Storage conditions:

    In the dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.
    Shelf life:

    3 years.

    Do not use after the expiration date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002994
    Date of registration:14.05.2015 / 12.12.2016
    Expiration Date:14.05.2020
    Date of cancellation:2020-05-14
    The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp21.01.2017
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