2010/09/17

Akineton



Composition, structure and packing

Tablets ploskotsilindricheskie, almost white on one side there is the risk of cross-flats.

1 tab. biperidena hydrochloride 2 mg.

Excipients: corn starch, lactose monohydrate, microcrystalline cellulose, calcium hydrogen phosphate dihydrate, potato starch, kopovidon, talc, magnesium stearate, purified water. Solution for in / and / m the introduction of transparent, colorless.

1 ml biperidena lactate 5 mg.

Excipients: sodium lactate, water d / and.

Clinico-pharmacological group: antiparkinsonian drug - an inhibitor of cholinergic transmission in the CNS.

Pharmacological action

Anticholinergic drug central action, reduces the activity of cholinergic neurons in the striatum (the structural component of the extrapyramidal system). Peripheral anticholinergic effects expressed in a lesser degree. Reduces tremor and rigidity. Biperiden is psychomotor agitation, autonomic disorders.

Pharmacokinetics

Absorption and distribution

After taking the drug inside the Cmax is achieved through 0.5-2 h and is 1.01-6.53 ng / ml. Css after taking the drug orally at a dose of 2 mg 2 times / day is achieved through 15.7-40.7 h. Bioavailability after a single oral administration is about 33 ± 5%. Plasma protein binding after oral and parenteral administration - 91-94%. Plasma clearance was 11.6 ± 0.8 ml / min / kg body weight. Provided with breast milk.

Metabolism

Biperiden completely metabolized. The main metabolites - bitsiklogeptan and piperidine.

Withdrawal

Outputs in the form of metabolites in the urine and feces. Withdrawal is carried out in two phases.

T1 / 2 of the first phase is 1.5 h, T1 / 2 of the second phase - 24 hours

Pharmacokinetics in special cases klinchicheskih

In elderly patients T1 / 2 can be increased up to 38 hours

Statement
Parkinson's syndrome in adults;
Extrapyramidal symptoms in children and adults caused by neuroleptics or similarly acting drugs;
nicotinism or phosphorus in organic matter in adults (for a solution for i / m and / in the introduction).

Dosage regimen

In Parkinson's syndrome adults in severe cases, medication is introduced into the / m or / in slowly in a dose of 10-20 mg (2-4 ml), divided into 2-4 injections.

In the appointment of the drug inside treatment is usually started with small doses, gradually increasing them, depending on the therapeutic effects and side effects.

Adults appoint 1 mg 1-2 times / day. The dose may be increased by 2 mg every day. Maintenance dose is 3-16 mg / day (divided in 3-4 reception).

The maximum daily dose is 16 mg. The total daily dose should be spread evenly over the dose to receive during the day. After reaching the optimal dose patients should be transferred to receiving the drug Akineton retard.

When motor disorders caused by the influence of drugs, for the rapid achievement of therapeutic response in adult drug appoint / m or / in slowly in a dose of 2.5-5 mg (0.5-1 mL) once. If necessary, the same dose can re-enter after 30 minutes.

The maximum daily dose is 10-20 mg (2-4 ml).

Children under 1 year of drug administered in / in slowly in a dose of 1 mg (0.2 ml), under 6 years - 2 mg (0.4 ml) and in the age of 10 - 3 mg (0.6 ml). If necessary, this dose may re-enter after 30 minutes. The introduction of the drug should be discontinued if during the introduction of the side effects. In the appointment of the drug inside, depending on the severity of symptoms for adults appoint 1-4 mg 1-4 times / day as a proofreader neuroleptic therapy.

Children aged 3-15 years, prescribed 1-2 mg 1-3 times / day. Tablets should be taken during or after a meal, washed down with liquid.

Unwanted side effects from the gastrointestinal tract can be reduced by taking tablets after meals. Duration of treatment depends on the type of disease. If you cancel Akinetona, its dosage should be gradually reduced.

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

When nicotine poisoning adult in addition to standard therapy, a drug prescribed to / m at a dose of 5-10 mg (1-2 ml) and in / 5 mg in cases where the patient's life is threatened.

In case of poisoning by organic phosphate mixture was biperidena individual dosing, depending on the degree of poisoning. The drug is introduced into / in a dose of 5 mg with the re-introduction to the disappearance of signs of poisoning.

Side effect

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 spasms, and speech-impaired.

At increased excitation of the nervous system, particularly in patients with disorders of the brain, reduce the dose of the drug.

On the part of the digestive system: dry mouth, increased saliva, constipation, epigastric discomfort, nausea.

On the part of the organ of vision: paresis of accommodation, mydriasis, followed by photophobia, angle-closure glaucoma (should regularly monitor the intraocular pressure).

Since the cardiovascular system: tachycardia and bradycardia, blood pressure reduction.

From the urinary system: difficulty urinating, especially in patients with benign prostatic hyperplasia (in this case it is recommended to reduce the dose), more rarely - urinary retention.

Other: decrease perspiration, allergic reactions, drug dependence.

Contraindications
angle-closure glaucoma;
stenosis of the gastrointestinal tract;
megacolon;
obstruction of the gastrointestinal tract;
individual hypersensitivity to any component of the drug.

Precautions should be prescribed the drug for benign prostatic hyperplasia, delaying mochevyvedeniya, arrhythmias, elderly patients (especially in the presence of organic brain symptoms) and patients who are predisposed to epileptic seizures.

Pregnancy and lactation

As the experience of the drug Akineton pregnancy is limited, it should appoint, after careful assessment of the potential benefits of therapy for the mother and the possible risk to the fetus, especially in the I trimester. Biperiden excreted in breast milk, where its concentration can reach concentrations observed in blood plasma, so the period of treatment should stop breastfeeding.

Cautions

Side effects are observed, especially in the early stages of treatment and at too rapid increase in dose. Except in cases of life-threatening complications should avoid abrupt withdrawal of the drug. In elderly patients, particularly those with brain damage of vascular or degenerative nature, can often show sensitivity to the drug. Anticholinergic drugs of the central acts of a similar drug Akineton may increase susceptibility to epileptic seizures. Therefore, physicians should take this fact into account when treating patients with such a predisposition. Tardive dyskinesia caused by neuroleptics, may be intensified under the influence of the drug Akineton. Parkinson symptoms in a case which developed tardive dyskinesia in some cases are so severe that prevents the continuation of treatment of anticholinergic drugs.

Noted drug abuse Akineton. This phenomenon may be associated with improved mood and temporary euphoric effects of the drug, which are occasionally observed. When conducting a prolonged therapy with Akineton should regularly check the intraocular pressure.

Effects on ability to drive vehicles and management mechanisms

Admission drug Akineton and especially in combination with other drugs of the central action, anticholinergics can disrupt the ability of driving and working with machinery.

Overdose

Symptoms: advanced slowly reactive to light pupils (mydriasis), dry mucous membranes, reddening of the skin, heart palpitations, atony of bladder and bowel, hyperthermia, especially in children and the excitement, confusion, delirium, collapse.

Treatment: Antidote - acetylcholinesterase inhibitors and especially Physostigmine, if necessary, catheterization of the bladder. Spend symptomatically.

Drug Interactions

Use of the drug Akineton in combination with other anticholinergic psychotropic drugs with antihistamine, antiparkinsonian and antiepileptic drugs can enhance the central and peripheral side effects. Simultaneous reception quinidine may intensify anticholinergic cardiovascular effects (especially the violation of Av-conduction).

Simultaneous with the appointment of levodopa may exacerbate dyskinesia. Anticholinergic drugs can enhance the central side effects of pethidine. In the treatment of drug increases the inhibitory effect of ethanol on the CNS. Akineton weakens the effect of metoclopramide and the same operating funds for the digestive tract.

Terms and Conditions of storage

List A. The drug 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 or above 30 ° C.

Shelf life - 5 years.