Left lump

General characteristics. Structure:

Active ingredients: levodopas of 250 mg, karbidopa of 25 mg;

Excipients: starch corn, starch prezhelatinizirovanny, Indigotin dye, magnesium stearate, cellulose microcrystallic.

Pharmacological properties:

Pharmacodynamics. A left lump - the combined protivoparkinsonichesky drug which part are a levodopa – the metabolic predecessor of dopamine which unlike the last passes through a blood-brain barrier (GEB), and a karbidop - inhibitor of a decarboxylase of aromatic amino acids.
Owing to decarboxylation the levodopa in tissues of a brain is transformed to dopamine, filling up its deficit and weakening thereby parkinsonism symptoms. The levodopa reduces expressiveness of a large number of symptoms of a disease, especially rigidities and bradykinesias. Reduces the tremor of hands, a dysphagy, a sialorrhea, orthostatic instability connected with a disease and Parkinson's syndrome.
However a considerable part of the levodopa accepted inside will be transformed to dopamine outside a brain and does not pass through GEB.
Karbidopa who does not get through GEB interferes with ekstratserebralny decarboxylation of a levodopa, increasing thus the quantity of a levodopa getting into a brain and turning there into dopamine.
Advantages of the combined drug are the best in comparison with a levodopa therapeutic action and a susceptibility by patients; less expressed side effects as for achievement of therapeutic action smaller doses of a levodopa are used.
Drug provides therapeutic the effective level of a levodopa in a blood plasma throughout a long time. Karbidopa interferes with action of a pyridoxine of a hydrochloride (B6 vitamin) which accelerates peripheral metabolism of a levodopa.

Pharmacokinetics. The active components which are a part of drug undergo transformations inherent to them. The levodopa is well absorbed from the digestive channel, is preferential from a small intestine. It is distributed between bodies and fabrics. The levodopa is exposed to difficult metabolic transformations from which main thing is its decarboxylation with formation of dopamine, noradrenaline and adrenaline which are removed by kidneys. About 80% of a levodopa are allocated with urine, mainly in the form of dihydroxyalpha-toluic and gomovanilinovy acids. Less than 1% are removed in not changed look. The levodopa elimination half-life from plasma - about 1 hour, in the presence of a karbidopa an elimination half-life increases till 2 o'clock.

Karbidopa (alpha метилдофагидразин), after intake quickly, however not completely, is soaked up from the digestive channel. It is distributed in an organism, does not get through GEB. About 50% in not changed look and in the form of metabolites are removed by kidneys.

Indications to use:

- Parkinson's disease.
- Parkinson's syndrome.

Route of administration and doses:

To apply the adult inside.

The optimum daily dose of drug needs to be selected carefully for each patient. For patients who begin treatment with drug the initial dose makes 1/2 tablets 1-2 times a day after food. If necessary the dose is raised, gradually adding 1/2 tablets every day or every other day before obtaining optimum therapeutic effect.

The maximum daily dose of Levokom - 8 tablets (200 mg of a karbidopa and 2 g of a levodopa).

Features of use:

Use during pregnancy and feeding by a breast.
Drug is contraindicated during pregnancy and feeding by a breast. For prevention of emergence of negative reactions at children it is necessary to make the decision on feeding interruption by a breast or on the termination of administration of drug, considering importance of treatment for mother.

Children. Drug is not used to children.

The left lump is not applied to elimination of the extrapyramidal reactions caused by medicines.
Drug is shown to patients with parkinsonism who accept the vitamin drugs containing a pyridoxine a hydrochloride (B6 vitamin).

All patients accepting drug have to be under careful observation for identification of mental changes, a depressive syndrome. Patients with psychosis (including in the anamnesis) need special observation of the doctor during treatment.

Patients should appoint drug carefully with cardiovascular diseases, a serious illness of lungs, bronchial asthma, a diabetes mellitus, mental disturbances, a convulsive syndrome, an open angle glaucoma, a peptic ulcer of a stomach and/or duodenum in the anamnesis (because of possibility of bleedings from upper parts of a digestive tract), at diseases of kidneys, a liver and bodies of endocrine system. With care appoint also to patients who had a myocardial infarction, in the presence of sinus ciliary or ventricular arrhythmias recently. At such patients observation of a condition of cardiovascular system is necessary, especially when determining an initial dose.

Under observation there have to be patients who at use of drug had hyperkinesias of choreoathetoid type. The left lump in certain cases can cause a recurrence of hyperkinesias that can be an effect of increase in dopamine in a brain and demands a drug dose decline. If it is necessary to appoint psychotropic drugs, it is necessary to consider a possibility of easing in such cases of protivoparkinsonichesky effect of Levokom. Patients with a chronic open angle glaucoma can use drug on condition of systematic ophthalmologic control.

If it is necessary to perform operation under anesthetic, Levok the day before cancel. Administration of drug is resumed after operation as soon as the patient is able to accept drug orally.

In case of drug withdrawal the dose is reduced gradually, at the same time it is necessary to watch a condition of the patient carefully.

During use of drug it is regularly necessary to control a functional condition of a liver, kidneys, cardiovascular system and system of a hemopoiesis. Levodopa drugs from karbidopy can cause pseudo-positive reaction to ketonic bodies in urine, and also deviations of results of different laboratory indicators – hepatic tests, an alkaline phosphatase, alaninaminotranspherase, aspartate aminotransferase, a lactate dehydrogenase, bilirubin, test on presence of blood at urine and Koombs's reaction. Lozhnopozitivny results can be received when using a glyukozooksidazny method of definition of a glucosuria.

Ability to influence speed of response at control of motor transport or work with other mechanisms.
It is necessary to consider individual reaction of the patient to treatment as some side effects (dizziness, drowsiness, dyskinesia) observed at Levokom's use, influence ability to manage motor transport or to work with mechanisms.

Side effects:

Most often there are side effects caused by the central neuropharmacological activity of dopamine – dyskinesia (including choreoid), dystonic and other involuntary movements, twitching of muscles and a nictitating spasm. These side effects disappear at a drug dose decline.
Other serious side effects - change of the mental status (including paranoid effects and a psychotic episode), a depression with development of suicide intentions or without them, dementia.
Infrequently disturbances of a cordial rhythm, strong heartbeat, orthostatic hypotension, the phenomena of block and disinhibition, anorexia, nausea, vomiting, dizziness, drowsiness meet.
Seldom there are gastrointestinal bleeding, a duodenum ulcer, arterial hypertension, phlebitis, a leukopenia, hemolitic and not hemolitic anemias, thrombocytopenia, an agranulocytosis, pain behind a breast, short wind and paresthesias, spasms.
At treatment by levodopa drugs from karbidopy deviations from norms of various laboratory tests - hepatic tests, an alkaline phosphatase, aspartate - and alaninaminotranspherases, lactate dehydrogenases, bilirubin, positive reaction of Koombs can be observed. Decrease in level of hemoglobin and indicators of a hematocrit, increase in level of glucose in blood serum, quantities of leukocytes and bacteria in urine is possible.
Other side effects:
- from a nervous system – an ataxy, numbness and a tremor of hands, twitching of muscles, a tonic nictitating spasm, a lockjaw, activation of the hidden syndrome of Bernard-Horner; falling, gait disturbances;
- from mentality – confusion of consciousness, sleeplessness, nightmares, hallucinations, nonsense, excitement, concern, euphoria;
- from a digestive tract – feeling of dryness and bitterness in a mouth, burning of language, a sialorrhea, a dysphagy; bruxism, hiccups attacks, abdominal cavity pain, lock, diarrhea, meteorism;
- from a metabolism – decrease or increase in body weight, hypostases;
- from integuments - rushes of blood to the person, the increased perspiration, rash, coloring of sweat in dark color, a hair loss;
- from urinogenital system – an urination delay, an urine incontience, coloring of urine in dark color, a priapism;
- from sense bodys - a diplopia, a mydriasis, oculomotor crisis;
- other complications - weakness, an indisposition, a headache, hoarseness of a voice, a bruxism, inflows, диспноэ, a malignant antipsychotic syndrome, a malignant melanoma.

Interaction with other medicines:

Levok can cause symptoms of orthostatic hypotension in patients who receive some antihypertensives that demands dose adjustment of antihypertensives in an initiation of treatment drug.

At simultaneous use of Levokom with tricyclic antidepressants negative reactions, including allergic hypertensia and dyskinesia are possible.

It is not necessary to accept drug along with MAO inhibitors. These drugs need to be cancelled in two weeks prior to Levokom's appointment.

Fenotiazina and phenyl propyl ketones can reduce therapeutic effect of Levokom.

The papaverine and Phenytoinum can eliminate protivoparkinsonichesky effect of Levokom.

Metoclopramidum increases concentration of a levodopa in a blood plasma.

Iron preparations can suppress absorption of a levodopa.

The left lump can be applied with other protivoparkinsonichesky means which are not containing a levodopa.

At the patients adhering to a diet with the high content of proteins drug absorption reduction is noted.

Contraindications:

- Established by hypersensitivity to any of drug components.
- Closed-angle glaucoma.
- Simultaneous treatment with MAO inhibitors.
- Not diagnosed skin diseases or a melanoma in the anamnesis.
- Pregnancy and feeding by a breast.
- Children's age.

Overdose:

Symptoms: precursory symptoms - twitching of muscles, a nictitating spasm; arterial hypertension, increase in heart rate, deterioration in appetite. Confusion of consciousness, alarming excitement, sleeplessness, alarm.

Treatment: it is artificial to cause vomiting, to urgently wash out a stomach.

Symptomatic therapy: infusions are appointed with care, pay attention to passability of respiratory tracts, at emergence of arrhythmias apply the corresponding treatment under control of an ECG. Value of dialysis for treatment of the phenomena of overdose is not studied. Use of a pyridoxine is not effective.

Storage conditions:

To store in original packaging in the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in the blister; on 3 and 10 blisters in a pack from a cardboard.