PC Mertz

General characteristics. Structure:

Active ingredient: 200 mg of active agent of an amantadin of sulfate (1-damantanamin sulfate).

Excipients: sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Amantadin has indirect agonistic effect on striatal dopamine receptors. Increases extracellular concentration of a dopamine, by means of both an intensification of its development, and blockade of the return capture of a dopamii presynaptic neurons.

In therapeutic concentration амантадин slows down development of acetylcholine and, thereby, has anticholinergic effect.

Pharmacokinetics. Average plasma concentration of an amantadin of sulfate after its infusions in number of 200 mg within 3 hours makes 0,54 мкл. At a dosage of 200 mg a day average plasma concentration by the end of introduction of the 6th day of treatment makes 0,76 мкл. The general clearance makes 3,6 l/h; an elimination half-life - from 10 to 30 hours, on average about 10 hours.

Amantadin approximately for 67% contacts proteins of a blood plasma. Gets through a blood-brain barrier. It is allocated with kidneys practically in an invariable look (90% of a single dose); its small amount is distinguished with excrements. Dialysis is ineffective (about 5% for one procedure).

Indications to use:

• Parkinson's disease, parkinsonism syndrome (akinetic crisis, acute decompensation).
• Disturbance of a vigilnost (initiative) in the post-coma period.
• Neuralgia at the surrounding herpes.

Route of administration and doses:

Intravenously. 1-2 times a day on 500 ml; it is possible to increase a dose to 3 times a day on 500 ml. Duration of injection is 3 hours (55 drops a minute). The average duration of therapy at neuralgia at the surrounding herpes makes 1 week with the subsequent transition to oral administration of drug.

At renal failures:

Glomerular speed of filtering (GFR) of ml/min.	Dosage (mg)	Interval of a dosage (p)
80-60	100	12
60-50	200 and 100 alternately	every other day
50-40	100	24
30-20	200	2 times a week
20-10	100	3 times a week
<10	200 and 100	weekly and in a week

Features of use:

Treatment PC Mertz cannot be stopped suddenly as it can lead to deterioration in symptomatology.

The patients having cardiovascular diseases have to be under constant medical control at purpose of drug PC Mertz.

Against the background of treatment alcohol intake is contraindicated.

With care to apply in operating time to drivers of vehicles and people whose profession is connected with the increased concentration of attention.

Side effects:

Very often	(> 1/10)
Often	(> 1/100, <1/10)
Not often	(> 1/1000, <1/100)
Seldom	(> 1/10000, <1/1000)
Very seldom	(<1/10000), including separate messages.

From a nervous system, sense bodys and mentality. Often: alarm, irritability, visual hallucinations, psychomotor arousing, dizziness, headache, decrease in visual acuity, insomnia. Very seldom: epileptic seizures, peripheral neuropathy, temporary loss of sight.

From cardiovascular system. Very seldom: arrhythmia, tachycardia, fibrillation of ventricles, lengthening of an interval of QT, development or aggravation of heart failure, orthostatic hypotension. Often: a syndrome of marble skin in combination with hypostasis of anklebones and shins.

From bodies of digestive tract. Often: nausea, vomiting, dryness in a mouth, a loss of appetite, dyspepsia.

Others. Often: an ischuria at patients with prostate adenoma. Very seldom: skin allergic reactions, dermatosis, fotosensebilization, polyuria, nocturia, leukopenia, thrombocytopenia.

Interaction with other medicines:

The concomitant use of an amantadin and drugs causing increase in an interval of QT, in particular is contraindicated:
- some antiarrhytmic drugs of a class 1A (for example, Kinidinum, Disopyramidum, procaineamide), and class III (for example, Amiodaronum and соталол);
- some antipsychotic drugs (for example, thioridazine, Chlorpromazinum, Pimozidum);
- some tricyclic and tetracyclic antidepressants (for example, amitriptyline);
- some antihistaminic drugs (for example, астемизол, терфенадин);
- some makrolidny antibiotics (for example, erythromycin, кларитромицин);
- some inhibitors of a giraza (for example, спарфлоксасин);
- antifungal means of group of azoles, and other drugs, in particular, бидупин, галофантрин, co-trimoxazole, pentamidine, цизаприд also bepridit.

The concomitant use of the diuretics representing a combination of Triamterenum/Hydrochlorthiazidum can lead to increase in concentration of an amantadin in plasma.

At a concomitant use with other protivoparkinsonichesky drugs (such as a levodopa, Bromocriptinum, мемантин, trigeksifenidit) it can be necessary to lower a dose of at the same time accepted drug, or both drugs in avoidance of undesirable effects, in particular, of psychotic reactions.

Anticholinergics, sympathomimetics and мемантин: strengthen side effects.

The means stimulating the central nervous system (including psychostimulants), ethanol increase risk of development of side effects.

Contraindications:

• Hypersensitivity to any of drug components;
• heavy congestive heart failure (the IV class on a scale of the New York Cardiological Association), a cardiomyopathy, myocarditis, atrioventricular blockade of II and III degrees, bradycardia with heart rate less than 55 beats/min, lengthening of an interval of QT more than 420 ms, ventricular arrhythmia (including tremblings of ventricles);
• pregnancy and period of breastfeeding;
• the lowered content in blood of potassium and magnesium;
• a concomitant use with the drugs extending QT interval;
• the expressed renal failure (clearance of creatinine less than 10 ml/min.),
• children's age,
• hereditary galaktozny insufficiency, lactose deficit,
• glucosic галактозная malabsorption, fenilketonuriya, sakharozo-isomaltose insufficiency, hereditary fructose insufficiency.

With care: A prostate hyperplasia, a narrow angle glaucoma, a renal failure of varying severity (there is a risk of cumulation of drug), agitation, a delirium, oppression of the central nervous system, exogenous psychosis (including in the anamnesis), joint reception with memantiny, a Triamterenum/hydrochlorothiazide.

Overdose:

Symptoms: nausea, vomiting, tremor, ataxy, decrease in visual acuity, lethargic state, dysarthtia, epileptic seizures, arrhythmia.

Treatment: gastric lavage, reception of absorbent carbon, symptomatic therapy.

Storage conditions:

At a temperature not above 25 °C. To store in the places unavailable to children. A period of validity - 5 years. Not to apply after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions of 200 mg / 500мл. On 500 ml in the bottle from polymeric material supplied with the special device for fastening. The bottle is hermetically corked by a cover from polymer a material leg.