NAC

General characteristics. Structure:

Active agents: levodopa of 250 mg; karbidopa of 25 mg;

excipients: starch prezhelatinizirovanny — 45 mg; starch corn — 6,5 mg; blue dye (E132 indigotin) — 0,-72 mg; magnesium stearate — 4,2 mg; MKTs — to 380 mg.

Description. Tablets of a biconvex oval form of blue color with white impregnations and separate impregnations of dark-blue color with a notch on one party.

Pharmacological properties:

The NAC — the combined protivoparkinsonichesky drug containing a karbidopa (inhibitor of a decarboxylase of aromatic amino acids) and a levodopa (the metabolic predecessor of a dopamine).

Possibly, symptoms of a disease of Parkinson are connected with insufficiency of a dopamine. Normal the dopamine performs function of a neurotransmitter and is developed in the cells of a brain controlling muscular activity. It is considered that motive disturbances are a consequence of dopamine insufficiency.

The levodopa reduces expressiveness of symptoms of a disease of Parkinson due to transformation it in a dopamine in a head brain by decarboxylation. Karbidopa who is not getting through GEB interferes with ekstratserebralny decarboxylation of a levodopa. Thereby the quantity of a levodopa coming to a brain and which is transformed there to a dopamine increases that leads to reduction of expressiveness of symptoms of a disease of Parkinson at many patients.

The levodopa is quickly soaked up in a GIT. Generally it turns into a dopamine, adrenaline, noradrenaline and, in a net result, into hydroxyalpha-toluic, gomovanilinovy and vanilmindalny acids. In a blood plasma and SMZh is defined 3-O-metildopa. Т½ levodopas of a blood plasma are made by about 50 min.

If the karbidopa and a levodopa are removed together, Т½ increases to 1,5 h.

Indications to use:

Parkinson's disease, Parkinson's syndrome.

Route of administration and doses:

The mode of dosing is set individually depending on the disease severity accompanying pathology and reaction to treatment. Usually initial dose makes ½ tablets the NAC 1 or 2 times a day after meal. For achievement of the optimum response to treatment it is possible to raise a dose gradual addition on ½ tablets every day or every other day. Most of patients have enough 3–6 tablets of drug a day. The daily dose should not exceed 8 tablets (200 mg of a karbidopa and 2 g of a levodopa) for patients with the body weight of 70 kg. 

The therapeutic effect is shown within 1 day, sometimes — after reception of 1 dose. The full effect is usually reached within 7 days.

Patients who accept other protivoparkinsonichesky drugs along with Nakom perhaps, will require dose adjustment. Tablets can be halved.

For achievement of optimum effect it is better to accept drug daily, without doing breaks.

Features of use:

Drug is not recommended to be accepted for elimination of the extrapyramidal effects caused by medicines.

Patients need to appoint drug with care with a serious illness of cardiovascular system and lungs, OH, diseases of kidneys, a liver and endocrine system, with a round ulcer or spasms in the anamnesis. With care appoint also to patients who had a myocardial infarction, in the presence of atrial, nodal or ventricular arrhythmia recently. At such patients it is necessary to watch a condition of cardiovascular system, especially during definition of an initial dose.

It is necessary to watch carefully patients timely to reveal at them development of a depression with the accompanying suicide intentions. Patients with psychoses (including in the anamnesis) require special attention.

The NAC, as well as other drugs of a levodopa, can serve as the reason of involuntary movements and mental disorders. It is assumed that such reactions are caused by increase in concentration of a dopamine in a brain after purpose of a levodopa. The dose decline can be necessary.

Patients with a chronic open angle glaucoma need to appoint drug with care on condition of constant control of intraocular pressure and careful observation of its changes during treatment.

At sudden drug withdrawal the complex of symptoms, similar to a malignant antipsychotic syndrome with manifestations of muscle tension, hyperthermia, changes in mentality and increase in the KFK level in blood serum was observed. Careful observation of a condition of patients which reduce a dose of drug is necessary or carry out its cancellation, especially if the patient at the same time applies neuroleptics.

During prolonged treatment it is necessary to control periodically a functional condition of a liver, kidneys, cardiovascular system and system of a krovoobrazovaniye.

Karbidopa drugs with a levodopa can cause false positive reaction to ketonic bodies in urine if for definition of a ketonuria use an indicator tape. This reaction does not change after boiling of tests of urine.

False-negative results can be received when using a glyukozooksidazny method of testing of a glucosuria.

Use during pregnancy and feeding by a breast. As influence of drug on the course of pregnancy at the person is unknown, and the levodopa combination with karbidopy can cause disturbance of development of internals and a skeleton in animals, use of drug is possible only in case the expected advantage for mother exceeds potential risk for a fruit. 

In need of purpose of drug the woman in the period of a lactation needs to resolve an issue concerning expediency of the termination of feeding by a breast or treatments by drug.

Children. Safety and efficiency of drug at children are not established therefore its use for patients aged up to 18 years is not recommended.

Ability to influence speed of response at control of vehicles or work with other mechanisms. During treatment by drug at some patients frustration of a nervous system can be observed. It should be considered at control of vehicles or work with the difficult mechanisms demanding concentration of attention.

Side effects:

The side effects arising at treatment by drug by the NAC disappear at a dose decline or in the course of treatment.

The most frequent side effect at use of drug is dyskinesia (motility disturbance).

Other side effects about which it was reported in connection with use of a levodopa or its combination with karbidopy, the following:

from TsNS: bradykinetic episodes, ataxy, adynamy, disorientation, numbness, tremor of hands, twitching of muscles, nictitating spasm, lockjaw, euphoria, dizziness, drowsiness, paresthesia, hallucinations, depression, dementia, excitement, confusion of consciousness, increase libido, sleeplessness, incoordination, fatigue, weakness, headache, respiratory depression, activation of a latent syndrome of the Corner, faint, anorexia; 

from cardiovascular system: disturbance of a cordial rhythm / heart consciousness, arterial hypotension, stethalgia, phlebitis, asthma; 

from a GIT: nausea, diarrhea, a lock, dark saliva, dyspepsia, dryness in a mouth, hypersalivation, a dysphagy, a bruxism, hiccups attacks, gastrointestinal bleeding, a meteorism, a language burning sensation, development of an ulcer of a duodenum;

disorders of metabolism: increase or loss of body weight, hypostases;

from integuments: rushes of blood to the person, the increased sweating, coloring of sweat in dark color, a hair loss, rash;

allergic reactions: a Quincke's disease, a small tortoiseshell, Shenleyn's disease — Genokh;

from urinogenital system: an urination delay, an urine incontience, coloring of urine in dark color, a priapism;

from system of blood: leukopenia, hemolitic and not hemolitic anemias, thrombocytopenia, agranulocytosis;

from sense bodys: diplopia, mydriasis, oculomotor crisis, sight opacification;

others: general weakness and indisposition, hoarseness, inflows, excitement, диспноэ, AG, malignant antipsychotic syndrome, malignant melanoma; 

laboratory indicators: increase in indicators of function of a liver, such as ShchF, ALAT, ASAT, LDG, bilirubin, blood urea nitrogen, creatinine, uric acid, positive test of Koombs.

In isolated cases spasms developed, however the causal relationship using a levodopa or its combination from karbidopy is not established.

Seldom noted decrease in hemoglobin and a hematocrit, increase in level of glucose in serum, a leukocytosis, a bacteriuria, a hamaturia.

Interaction with other medicines:

It is necessary to observe precautionary measures at simultaneous use of drug by the NAC with other medicines.

Hypotensive medicines. Orthostatic hypotension can arise at patients who combined with drug the NAC apply other antihypertensives. In that case dose adjustment of an antihypertensive can be necessary.

Antidepressants. There were separate messages on emergence of negative reactions, including AG and dyskinesia caused by simultaneous use of tricyclic antidepressants and drug by the NAC (for the patients applying MAO inhibitors (see CONTRAINDICATIONS)).

Iron. Pilot studies showed decrease in bioavailability of drug by the NAC if it was applied together with ferrous sulfate or a gluconate of iron.

Other medicines. Antagonists of receptors of a dopamine of D2 (for example fenotiazina, phenyl propyl ketones and рисперидон) and an isoniazid can reduce therapeutic effect of a levodopa. It is noted that positive effects of drug at Parkinson's disease can be reversible at use of Phenytoinum and papaverine. For the patients applying such medicines combined with drug the NAC careful observation of the doctor is necessary for identification of decrease in therapeutic effect.

The combined therapy with selegiliny can lead to the heavy orthostatic hypotension not characteristic of drug. 

As the levodopa competes with some amino acids, at the patients who are on a high-protein diet absorption of a levodopa can increase.

Influence of simultaneous use of antacids with drug by the NAC on bioavailability of a levodopa was not studied.

The NAC patients can accept with a disease and Parkinson's syndrome which use the drugs containing a pyridoxine.

Contraindications:

Hypersensitivity to any of drug components, heavy psychoses, the suspicious not diagnosed educations on skin (dermatosis) or a melanoma in the anamnesis; simultaneous use of the MAO non-selective inhibitors; closed-angle glaucoma. Children aged up to 18 years.

Overdose:

Symptoms: disturbance of a cordial rhythm, involuntary movements, nictitating spasm.

Symptomatic treatment.

The pyridoxine is inefficient for prevention of effect of drug.

ECG monitoring and careful control of the patient regarding a possibility of development of arrhythmia is necessary. It is necessary to consider also that together with drug the NAC the patient can apply other medicines. Experience of use of dialysis is absent.

Storage conditions:

In the dry dark place at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets in the blister of 100 pieces.