Composition, form of production and packaging
Tablets are almost white, round, flat-cylindrical, with a facet and a risk.
biperidene hydrochloride 2 mg
Excipients: microcrystalline cellulose - 192 mg, sodium carboxymethyl starch - 5 mg, magnesium stearate - 1 mg.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (5) - packs cardboard.
10 pieces. - packings cellular planimetric (10) - packs cardboard.
20 pcs. - packings cellular planimetric (2) - packs cardboard.
20 pcs. - packings cellular planimetric (5) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
Anticholinergic drug of central action. Biperiden selectively blocks central n-cholinergic receptors and peripheral m-holipergic transmission of excitation. By blocking 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.
Quickly absorbed from the digestive tract. After taking the drug inside C max is achieved after 0.5-2 h and is 1.01-6.53 ng / ml. Thanks to the extensive metabolism during the primary passage through the liver, bioavailability is 30%. Binding to plasma proteins - 91-94%, V d - (24 В± 4.1) l / kg. Plasma clearance is 11.6 В± 0.8 ml / min / kg. Biperiden is completely metabolized - subjected to hydroxylation; the main metabolites are bicycloheptane and piperidine. The excretion of biperidene occurs in two phases. T 1/2 of the first phase is 1.5 h, T 1/2 of the second phase is 24 h. T 1/2 - about 20 h; therefore, the concentration of the drug in the plasma is 0.1-0.2 ng / ml and can be determined 48 hours after its administration. In elderly patients, T 1/2 may increase to 38 hours. Biperiden is excreted by the kidneys and through the intestine; penetrates and breast milk.
- Parkinsonism syndrome;
- extrapyramidal symptoms (tremor, muscle rigidity, torsion dystonia, local forms of dystopia, including paroxysmal dyskinesias, hyperkinesia of chorea, tics of various forms, myoclonia and hyperkinesia, dystonia of the muscles of the extremities, trunk, neck, face, akinesia, akathisia); caused by neuroleptics or similarly acting drugs.
Inside. Tablets should be taken during or after a meal, with a liquid.
In Parkinson's syndrome, the initial dose for adults is 1 mg 1-2 times / day (1/2 tab.). The dose can be increased by 2 mg (1 tab.) Every 24 hours. The maintenance dose is 3-16 mg / day (1 / 2-2 tablets 3-4 times / day). The maximum daily dose is 16 mg (8 tablets). The total daily dose should be evenly divided into doses during the day.
In case of extrapyramidal symptoms caused by neuroleptics or similarly acting drugs for adults , the initial dose, depending on the severity of the symptoms, is 1-2 mg (1 / 2-1 tab.) 1-4 times / 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. When biperidenum is withdrawn, its dose should be gradually reduced.
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 effect of the drug.
From the nervous system and sense organs: fatigue, dizziness, speech disorders, headache, mydriasis, paresis of accommodation, snotty, anxiety, confusion, memory impairment, hallucinations, euphoria, angle-closure glaucoma, photophobia, disorientation in time and space, activity, motor excitement, catalepsy.
From the cardiovascular system: rarely - tachycardia, lowering blood pressure; very rarely - a bradycardia.
On the part of the intestine: 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.
hypersensitivity to the components of the drug;
- hypertrophy of the prostate with a delay in urine;
- an angle-closure glaucoma;
- mechanical narrowing or obstruction of the gastrointestinal tract;
- Children under 18 years of age (data on the effectiveness and safety of the drug in children are absent).
Elderly patients, myasthenia gravis, arrhythmia, patients with a tendency to convulsive seizures, incl. 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 biperidepa is appointed, it is necessary to stop breastfeeding, as the drug is excreted in breast milk and the child may develop aichicholinergic effects.
APPLICATION FOR CHILDREN
The use of the drug for children and adolescents under the age of 18 is contraindicated (there is no data on the efficacy and safety of the drug in children).
APPLICATION IN ELDERLY PATIENTS
With caution apply the drug to elderly patients.
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, can be intensified by biperidene. Parkinsonichsky symptoms in the case of advanced tardive dyskinesia in some cases are so severe that they prevent continuation of treatment with anticholinergic drugs.
Abuse of drugs containing biperiden was noted. 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, the intraocular pressure should be checked regularly.
With dry mouth, symptomatic therapy is performed and, if necessary, the dose is adjusted.
Influence on ability to drive vehicles, mechanisms
The drug has a strong effect on psychomotor reactions, so patients. taking a 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 anticholinergic drugs, can disrupt the ability to drive and work with machinery.
Symptoms (similar to symptoms of atropine poisoning): mydriasis, dry skin, facial hyperemia, dry mouth. dryness of the upper respiratory tract, increased body temperature, tachycardia, cardiac arrhythmias, impaired intestinal motility, urinary retention, delirium, disorientation, anxiety, hallucinations, confusion, ataxia, aggressiveness and convulsions. In severe poisoning, stupor, coma, stopping breathing and heart and death can occur.
Treatment: gastric lavage, symptomatic therapy. As a specific antagonist, physiostigmia 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.
With the simultaneous use of biperidene:
- with anticholinergic drugs, it is possible to strengthen central and peripheral anticholinergic effects;
- with antipsychotic drugs (neuroleptics), the risk of developing tardive dyskinesia increases;
- with levodopa, m-holin-blocking action and dyskinesia may be enhanced;
- with quinidine, the risk of dyskinesia increases (increases cholinolytic effect);
- the action of blockers of histamine III receptors is enhanced;
- the effect of anticonvulsants increases;
- decreases the effectiveness of metoclopramide.
Biperiden potentiates the action of ethanol.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a place protected from light and inaccessible to children at a temperature of no higher than 30 В° C.
Shelf life - 3 years.
Do not use after the expiration date indicated on the package.