AKINETON (tablets, solution)
Active material: Biperiden
When ATH: N04AA02
CCF: Of anti-drug – transmission in the CNS holinergicescoy inhibitor
ICD-10 codes (testimony): G20, G21, T 57.1, T 65.2
Manufacturer: DESMA GmbH (Germany)
Pharmaceutical form, composition and packaging
Pills Valium, nearly white; on one side there is a Phillips risk with chamfers.
1 tab. | |
biperiden hydrochloride | 2 mg |
Excipients: corn starch, lactose monohydrate, microcrystalline cellulose, calcium hydrogen phosphate dihydrate, potato starch, kopovydon, talc, magnesium stearate, Purified water.
20 PC. – blisters (5) – packs cardboard.
Solution for in / and the / m clear, colorless.
1 ml | |
biperiden lactate | 5 mg |
Excipients: sodium lactate, water d / and.
1 ml – ampoule (5) – packs of cardboard dividers partitions.
Pharmacological action
Malignant drug central action, reduces the activity of cholinergic neurons of the striped body (structural component of extrapyramidal system). Peripheral antiholinergicescoe effect expressed in lesser extent. Decreases tremor and rigidity. Biperiden causes agitation, autonomic disorders.
Pharmacokinetics
Absorption and distribution
After taking the drug inside Cmax achieved through 0.5-2 h and is 1.01-6.53 ng / ml. Css After taking the drug inside the dose 2 mg 2 times / day achieved through 15.7-40.7 no. Bioavailability after single intake is about 5% ± 33.
Linking blood plasma after ingestion and injecting – 91-94%. Plasma clearance is 11.6 ± 0.8 mL/min/kg.
Provided with breast milk.
Metabolism
Biperiden is fully metabolized. The main metabolites – biciklogeptan and piperidine.
Deduction
Appears in the form of metabolites in urine and feces.
Excretion is performed in two phases. T1/2 the first phase is 1.5 no, T1/2 Phase II – 24 no.
Pharmacokinetics in special cases klinchicheskih
Older patients t1/2 may increase to 38 no.
Testimony
Parkinson's syndrome in adults;
-extrapyramidal symptoms in children and adults, caused neiroleptikami or similarly acting drugs;
— nicotine poisoning or fosforosoderzhashhimi organic substances in adults (for a solution to the in/m and/in the).
Dosage regimen
At Parkinsonian syndrome adult in severe cases, medication is injected in the/m or/in slowly in the dose 10-20 mg (2-4 ml), razdelennoy of 2-4 injection.
In appointing the drug inside treatments usually start with small doses of, gradually their increasing, Depending on the therapeutic actions and side effects. Adults appoint 1 mg 1-2 times / day. Dose can be increased to 2 mg every day. The maintenance dose is 3-16 mg / day (razdelennaya of 3-4 admission). The maximum daily dose is 16 mg. The total daily dose should be spread evenly over the dose for admission within 24 hours. After reaching the optimal dose patients should be transferred to the receiving medication Akineton® retard.
At propulsion violations, caused by the action of medicines, for the speedy achievement of a therapeutic response adult the drug is prescribed in the/m or/in slowly in the dose 2.5-5 mg (0.5-1 ml) single. If necessary, the dose can be re-entered through 30 m. The maximum daily dose is 10-20 mg (2-4 ml).
Children under 1 year the drug is prescribed in/in slowly in the dose 1 mg (0.2 ml), in Up to 6 years – 2 mg (0.4 ml) and in Up to 10 years – 3 mg (0.6 ml). If necessary, the dose can be re-entered through 30 m. The introduction of the drug should be discontinued, If at the time of the introduction of developing side effects.
In appointing the drug inside, depending on the severity of symptoms adult appoint 1-4 mg 1-4 times per day as a neuroleptic therapy. For children 3-15 years appointed 1-2 mg 1-3 times / day.
The tablets should be taken during or after a meal, with some liquid.
Unwanted side effects from the stomach can be reduced, taking a pill immediately after eating. Duration of treatment depends on the type of illness. If you cancel Akinetona®, the dose should be gradually reduce.
Experience in application of Akineton® When drug dystonia in children is restricted to conduct short courses of drug treatment.
At nicotine poisoning adult In addition to standard therapy, the drug is prescribed at a dose of 5-10 mg (1-2 ml) and in/in the dose 5 mg in cases, When a patient's life is threatened.
IN case of poisoning by organic phosphoric mixture conduct individual dosing biperiden, Depending on the degree of poisoning. The drug is injected in/in the dose 5 mg with repeated introduction to the disappearance of signs of poisoning.
Side effect
CNS: dizziness, drowsiness, weakness, fatigue, alarm, confusion, euphoria, impaired memory and in some cases hallucinations, deliriosnye disorders; nervousness, headache, insomnia, dyskinesia, ataxia, muscle cramps and speech. At high excitation of the central 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, salivary gland enlargement, constipation, discomfort in epigastria, nausea.
On the part of the organ of vision: Parez akkomodacii, midriaz, accompanied by fotofobiej, zakrыtougolynaya glaucoma (should regularly monitor the inner pressure).
Cardio-vascular system: tachycardia and bradycardia, decrease in blood pressure.
From the urinary system: strangury, especially in patients with hyperplasia of prostate (in this case it is recommended to reduce the dose); more rarely – urinary retention.
Other: decreased sweating, allergic reactions, drug dependence.
Contraindications
- Zakrыtougolynaya glaucoma;
-DIGESTIVE TRACT stenosis;
- Megacolon;
-obstruction of the DIGESTIVE TRACT;
-individual hypersensitivity to any component of the drug.
FROM caution should be prescribed the drug for benign prostatic hyperplasia, delay mochevyvedenija, violations heart rhythm, older patients (especially if you have organic brain syndrome) and patients, prone to seizures and obstructed.
Pregnancy and lactation
As experience in application of Akineton® during pregnancy is limited, then assign it should, after careful assessment of the potential benefit of therapy to the mother and the potential risk to the fetus, especially in the I trimester.
Biperiden is excreted in breast milk, in which its concentration can reach concentrations, observed in plasma, Therefore, in the period of treatment should stop breast-feeding.
Cautions
Side effects are observed, primarily, in the early stages of treatment and when the dose too quickly.
Except in cases of life-threatening complications should avoid abrupt cancellation of the drug.
In elderly patients, especially with cerebral vascular or degenerative forms of violations, can often manifested hypersensitivity to the drug.
Anticholinergic medicines central action, similar drug Akineton®, may increase susceptibility to obstructed seizures. Therefore, physicians should take this fact into consideration when treating patients with such a predisposition.
Pozdnyaya dyskinesia, neuroleptic-induced, can grow under the influence of medication Akineton®.
Parkinsonicheskie symptoms in case grew late psoriasis in some cases are so severe, that impede the continuation of the treatment of anticholinergic drugs.
Noted drug abuse Akineton®. This phenomenon is possibly related to improvements in mood and time jejforicheskimi effects of the medicinal product, which occasionally are observed.
When conducting a prolonged drug therapy Akineton® You should regularly check the intraocular pressure.
Effects on ability to drive vehicles and management mechanisms
Admission drug Akineton®, particularly in combination with other drugs central action, antiholinergicakimi means, can disrupt the ability to driving and working with machinery.
Overdose
Symptoms: extended, slow reacting to light the pupils (midriaz), dryness of mucous membranes, erythema, cardiopalmus, atony bladder and bowel, hyperthermia, especially in children and the excitement, confusion, delirium, collapse.
Treatment: Antidote – Acetylcholinesterase inhibitor and primarily Physostigmine, if necessary – bladder catheterization. Symptomatic therapy.
Drug Interactions
Application of Akineton® in conjunction with other antiholinergicakimi psychotropic drugs, with antihistamines, protivoparkinsonicheskimi and antiepileptic drugs can contribute to the strengthening of Central and peripheral side effects.
Simultaneous reception hinidina can cause increased anticholinergic and cardiovascular effects (especially violation of atrioventricular conduction).
The simultaneous appointment with levodopa it may exacerbate hypertension diskineziu.
Antiholinergicakie funds may increase Central side effects of pethidine.
When drug treatment is enhanced by the dampening effect of ethanol on the central nervous system.
Akineton® ters of metoclopramide and is similar to existing funds in the DIGESTIVE TRACT.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
A List. The drug is in the form of tablets should be stored out of reach of children at or above 25 ° C, in the form of solution for injection – at a temperature no higher than 30 ° C. Shelf life - 5 years.