PK-Merz

Active material: Amantadin
When ATH: N04BB01
CCF: Of anti-drug – blocker of glutamate NMDA-receptor
ICD-10 codes (testimony): B02.2, G20, G21
When CSF: 02.06.03
Manufacturer: Merz Pharma GmbH & Co. KGaA (Germany)

Pharmaceutical form, composition and packaging

Pills, Film-coated orange, round, lenticular, with a notch on one side, without smell.

Excipients: microcrystalline cellulose, potato starch, gelatin, lactose monohydrate, povidone, talc, magnesium stearate, colloidal silicon dioxide, Croscarmellose sodium, Titanium dioxide, butyl methacrylate copolymer, dye orange yellow.

10 PC. – blisters (3) – packs cardboard.

Solution for infusion colorless, clear.

Excipients: sodium chloride, water d / and.

500 ml – plastic bottles (1) – cardboard boxes.
500 ml – plastic bottles (2) – cardboard boxes.

Pharmacological action

Blocker of glutamate N-methyl-D-aspartate receptors (NMDA-receptor). Of anti-drug. Amantadine has indirect agonist activity at striatal dopamine receptors. Increases extracellular concentrations of dopamine, through both intensification of its production, and the blockade of dopamine reuptake by presynaptic neurons. At therapeutic concentrations amantadine and slows down the production of acetylcholine, thereby, anticholinergic effects.

Pharmacokinetics

Absorption

After administration of a single dose of C_max It achieved within approximately 2-8 no. Upon receiving a dose of amantadine sulfate 100 mg C_max is 0.15 ug / ml.

Average plasma concentrations of amantadine sulphate in the / infusion at a dose of 200 mg for 3 h is 0.54 l. At a dose of 200 mg / day average plasma concentration at the end of the 6th day of treatment is 0.76 l.

Distribution

Binding to plasma proteins is 67%. It penetrates through the BBB.

Deduction

T_1/2 – 10-30 no, average 10 no. Excreted by the kidneys virtually unchanged (90% single dose); a small amount of – with feces. Dialysis maloeffyektivyen (about 5% for one procedure).

The total clearance with on / in the introduction of 3.6 l /.

Testimony

Orally

- Parkinson's disease (muscle rigidity, tremor, Hypo- or akinesia);

- Extrapyramidal disorders, caused by the intake of neuroleptics, or other drugs;

- Neuralgia in opoyasыvayushtem gerpese.

For i / v administration

- Parkinson's disease, Parkinson's syndrome (akynetycheskyy crisis, acute decompensation);

- Violation of vigilance (initiative) in postkomatoznom period;

- Neuralgia in opoyasыvayushtem gerpese.

Dosage regimen

The drug is administered orally after meals, drinking a small amount of liquid, preferably in the first half of the day. First 3 days appoint 1 tab. / day, then increase the dose to 2 tab. / day, it being possible to further increase the dose to 1 tab. in Week. Typically, an effective dose of 1-3 tab. 2 times / day. The maximum daily dose – 600 mg (6 tab.). In case combination treatment is necessary to determine the dose individually. The last dose is recommended to take in the second half of the day no later 16 no.

In elderly patients, in particular, patients with the condition of excitement and confusion, preddeliriya and delirium, It requires a lower dosage.

B / appoint 500 ml 1-2 times / day. The dose can be increased to 3 time / day of 500 ml. The duration of infusion – 3 no (55 drops / min).

The average duration of therapy for neuralgia with herpes zoster is 1 week with a subsequent transition to the reception of the drug inside.

At renal impairment drug administered according to the glomerular filtration rate.

Side effect

The incidence of adverse reactions is classified as follows: Often (>1/10), often (>1/100, <1/10), infrequently (>1/1000, <1/100), rarely (>1/10 000, <1/1000), rarely (<1/10 000, including isolated reports).

From the central and peripheral nervous system: often – alarm, irritability, heteroptics, psychomotor agitation, dizziness, headache, reduced visual acuity, insomnia; rarely – seizures, perifericheskaya neuropathy, temporary loss of vision.

Cardio-vascular system: rarely – arrhythmia, tachycardia, ventricular fibrillation, prolongation of the interval QT, development or exacerbation of congestive heart failure, orthostatic hypotension; often – marble skin syndrome in combination with swelling of the ankles and shins.

From the digestive system: often – nausea, vomiting, dry mouth, decreased appetite, dyspepsia.

From the urinary system: often – urinary retention in patients with benign prostatic hyperplasia; rarely – polyuria, nocturia.

Dermatological reactions: rarely – allergic skin reactions, dermatosis, photosensitivity.

From the hematopoietic system: leukopenia, thrombocytopenia.

Contraindications

- Severe congestive heart failure (IV functional class NYHA classification);

- Cardiomyopathy;

- Miokardit;

— AV-blockade II and III degrees;

- Bradycardia (HR less 55 u. / min);

- Prolongation of the interval QT more 420 ms;

- Ventricular fibrillation (incl. ventricular flutter);

- Hypokalemia;

- Gipomagniemiya;

- Concomitant use of drugs with, prolonging the QT interval;

- Severe renal insufficiency (CC < 10 ml / min);

- Children's age;

- Only Pill – hereditary deficiency galaktazy, lactase deficiency, malabsorption syndrome glucose / galactose, lack of sucrase / isomaltase, hereditary fructose intolerance;

- Phenylketonuria;

- Pregnancy;

- Breastfeeding;

- Hypersensitivity to any component of the drug.

FROM caution should be prescribed the drug for benign prostatic hyperplasia, angle-closure glaucoma, renal failure of varying severity (there is a risk of cumulation of the drug), ažitacii, delirium, CNS depression, ékzogennom psychosis (incl. history), when co-administered with memantine, triamterene / hydrochlorothiazide.

Pregnancy and lactation

The drug is contraindicated in pregnancy and lactation (breast-feeding).

Cautions

Treatment with PK-Merz can not be stopped suddenly, tk. this can lead to deterioration of the disease.

Patients with cardiovascular disease should be under constant medical supervision in the appointment of PK-Merz.

The treatment is contraindicated alcohol intake.

Effects on ability to drive vehicles and management mechanisms

Precautions should use the drug during the drivers of vehicles and people, skills relate to the high concentration of attention.

Overdose

Symptoms: nausea, vomiting, tremor, ataxia, reduced visual acuity, lethargic, dysarthria, seizures, arrhythmia.

Treatment: gastric lavage, administration of activated charcoal. Symptomatic therapy.

Drug Interactions

Concomitant intake of amantadine and drugs, causing an increase in the QT interval, in particular:

- Class I antiarrhythmic drugs A (eg, quinidine, disopyramide, prokaynamyd) and class III (eg, amiodarone and sotalol);

- Antipsychotics (eg, tioridazin, chlorpromazine, pimozid);

- Tricyclic and tetracyclic antidepressants (eg, Amitriptyline);

- Antihistamines (eg, astemizol, terfenadine);

- Macrolide antibiotics (eg, Erythromycin, clarithromycin);

- Gyrase inhibitors (eg, sparfloxacine);

- Azole antifungals;

- Other preparations (bidupin, galofantrin, co-trimoxazole, pentamidine, cisapride and bepridil).

Simultaneous administration of diuretics, representing a combination of triamterene / hydrochlorothiazide may lead to increased concentrations of amantadine in plasma.

At simultaneous reception with other antiparkinsonian drugs (levodopa, bromocriptine, Memantine, trigeksifenidil) it may be necessary to lower the dose of the drug at the same time received, or both drugs in order to avoid unwanted effects, in particular, psychotic reactions.

Anticholinergic agents, sympathomimetic and memantine increase the side effects of amantadine.

Funds, stimulating the central nervous system (incl. psychostimulants), Ethanol increases the risk of side effects of amantadine.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 5 years.