Biperiden - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Anti-Parkinsonics

Included in the formulation

Akineton®

solution w / m in / in

Desma GmbH Germany

Akineton®

pills inwards

Desma GmbH Germany

Bezac®

pills inwards

VALENTA PHARM, PAO Russia

Mendilex®

pills inwards

Alkaloid, JSC Macedonia

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

ONLS

АТХ:

N.04.A.A.02 Biperiden

Pharmacodynamics:

It is an anticholinergic drug of 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.

Pharmacokinetics:

Suction and distribution

After taking the drug inside C_max is achieved after 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 a day is reached after 15.7-40.7 hours Bioavailability after a single oral intake is about 33 ± 5%.

Binding to plasma proteins after ingestion and parenteral administration is 91-94%. Plasma clearance is 11.6 ± 0.8 ml / min / kg.

Excreted in breast milk.

Metabolism

Biperiden is completely metabolized. The main metabolites are bicycloheptane and piperidine.

Excretion

It is excreted in the form of metabolites with urine and feces.

Excretion is carried out in two phases.The half-life of the first phase is 1.5 hours, the second phase is 24 hours.

Pharmacokinetics in special clinical cases

In elderly patients, the half-life may increase to 38 hours.

Indications:

Parkinson's syndrome in adults; extrapyramidal symptoms in children and adults caused by neuroleptics or similarly acting drugs.

ICD-10

VI.G20-G26.G20 Parkinson's disease

VI.G20-G26.G21 Secondary Parkinsonism

VI.G20-G26.G25 Other extrapyramidal and motor disorders

XX.Y40-Y59.Y49 Psychotropic drugs, not elsewhere classified

Contraindications:

Closed-angle glaucoma; stenosis of the gastrointestinal tract; megacolon; GI tract obstruction; children up to 3 years; increased individual sensitivity to any of the components of the drug.

Carefully:

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 in pregnancy is limited, it should be prescribed after a careful 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.

Dosing and Administration:

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 appoint 1 mg 1-2 times a day. The dose can be increased by 2 mg every 24 hours. The maintenance dose is 3-16 mg per 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, patients should be transferred to the administration of the prolonged-release preparation.

When motor disorders caused by the action of drugs, depending on the severity of the symptoms adults appoint 1-4 mg 1-4 times a day as a corrector of neuroleptic therapy, children aged 3-15 years 1-2 mg 1-3 times a 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. If you cancel the drug, its dose should be gradually reduced.

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

Side effects:

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.

From 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 (regular monitoring of intraocular pressure).

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 lower the dose); more rarely - urinary retention.

Other: reducing sweating, allergic reactions, drug dependence.

Overdose:

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, agitation, confusion, delirium, collapse.

Treatment: antidote - inhibitors of acetylcholinesterase and, above all, physostigmine, if necessary - catheterization of the bladder. Conduction of symptomatic therapy.

Interaction:

The use of the drug 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.

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

Biperiden weakens the effect of metoclopramide and similarly acting remedies on the digestive tract.

Special instructions:

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.

Late dyskinesia caused by neuroleptics may be intensified by the drug.

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.

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

When carrying out long-term therapy with the drug, the intraocular pressure should be checked regularly.

Impact on the ability to drive vehicles and manage mechanisms

The administration of the drug, especially in combination with other central-action drugs, with anticholinergic drugs, can disrupt the ability to drive and work with machinery.

Instructions

Biperiden (Biperidenum)