Levocom

Levocom is an antiparkinsonian drug from the group of dopaminergic medications.

Indications Levocoma

It is used for parkinsonism and Parkinson's disease.

Release form

The medicine is released in tablets, 10 pieces inside a blister plate. There are 3 or 10 such plates in a box.

Pharmacodynamics

Levokom is a complex antiparkinsonian drug, the constituent elements of which are carbidopa (a component that slows down aromatic amino acid decarboxylase) and levodopa (a metabolic element that precedes dopamine and is capable, unlike dopamine itself, of passing through the BBB).

As a result of the decarboxylation process, levodopa located inside the brain tissue is transformed into dopamine, replenishing its deficiency and thus reducing the manifestations of Parkinsonism. Levodopa reduces the severity of many signs of the disease, especially rigidity, and also bradykinesia. At the same time, it reduces dysphagia with tremor, ptylysis and orthostatic instability, which arise due to Parkinson's disease and Parkinsonism.

But most of the orally consumed levodopa is transformed into dopamine in the extracerebral environment, without penetrating the BBB.

Carbidopa cannot pass through the BBB. It prevents the process of extracerebral decarboxylation of the levodopa element, thereby increasing the volume of levodopa penetrating into the brain, which is converted into dopamine inside it.

Among the advantages of the combination drug are a stronger medicinal effect, compared to levodopa, and better patient susceptibility. In addition, side effects are less pronounced, because lower doses of levodopa are used to obtain the medicinal effect.

Levokom helps to ensure long-term maintenance of medicinal concentration of levodopa in blood plasma. Carbidopa prevents the activity of pyridoxine hydrochloride, which allows to increase the rate of peripheral metabolic processes of levodopa.

Pharmacokinetics

The active ingredients that are part of the drug undergo their inherent transformations. Levodopa is perfectly absorbed inside the gastrointestinal tract (most of it inside the small intestine).

The distribution of the substance is carried out inside the tissues together with the organs. Levodopa undergoes complex metabolic transformations (the main one is decarboxylation, during which it is transformed into norepinephrine, dopamine with adrenaline). Metabolic products are excreted by the kidneys.

About 80% of levodopa is excreted in urine, most of it in the form of homovanillic and 2-hydroxyphenylacetic acids. Less than 1% of the drug is excreted unchanged. The half-life of the substance from plasma is approximately 1 hour (with the participation of carbidopa, this period is extended to 2 hours).

Carbidopa (α-methyldofahydrazine) is rapidly, although not completely, absorbed in the gastrointestinal tract when administered orally. It is distributed within the body but does not pass through the blood-brain barrier. About 50% of the drug in the form of an unchanged component and its decay products is excreted by the kidneys.

Dosing and administration

The medicine is taken orally. Each individual patient needs to select the appropriate daily dose individually.

People who are just starting therapy should be prescribed a dosage of 0.5 tablets taken 1-2 times a day after meals. If necessary, the dosage can be gradually increased - daily or every other day by 0.5 tablets until the desired medicinal result is achieved.

It is allowed to take no more than 8 tablets of Levokoma per day (0.2 g of carbidopa, as well as 2 g of levodopa).

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Use Levocoma during pregnancy

The medicine should not be prescribed to pregnant or breastfeeding mothers.

To prevent the development of negative symptoms in the infant, it is necessary to either stop breastfeeding or stop using the medication - the choice is made based on an assessment of the importance of taking the drug for the mother.

Contraindications

Main contraindications:

• the presence of hypersensitivity to any element of the drug;
• glaucoma.
• use in combination with MAOIs;
• skin diseases that have not been diagnosed, or a history of melanoma.

Side effects Levocoma

After using Levokom, negative effects often appear, related to the central neuropharmacological effect of dopamine - such as dyskinesia (including choreiform), muscle twitching, dystonic and other involuntary movements, as well as blepharospasm. Such side effects disappear after reducing the dose of the drug.

Other serious negative symptoms include dementia, changes in mental status (including paranoid symptoms and transient psychosis), and depression, which can lead to suicidal tendencies.

Sometimes there are disturbances in the heart rhythm, increased heartbeat, orthostatic collapse, signs of disinhibition or inhibition, as well as vomiting, a feeling of drowsiness, the appearance of dizziness or nausea and the development of anorexia.

Occasionally, bleeding in the gastrointestinal tract, development of intestinal ulcers, phlebitis, anemia (hemolytic or non-hemolytic), leukopenia or thrombocytopenia, and agranulocytosis are observed. In addition, convulsions, dyspnea, pain behind the breastbone, and paresthesia appear, and blood pressure values increase.

During therapy with levodopa, as well as carbidopa, deviations from normal values of various laboratory tests may be observed - for example, alkaline phosphatase, liver function tests, LDH, ALT and AST, as well as bilirubin, and in addition, a positive result of the Coombs test. Hemoglobin with hematocrit values may also decrease, the level of glucose in the blood serum and the number of bacteria with leukocytes in the urine may increase.

Other negative effects:

• disorders of the nervous system: numbness, muscle twitching, ataxia, tremor affecting the hands, as well as trismus, blepharospasm of a tonic nature, gait disorder and activation of latent Horner's syndrome;
• mental disorders: insomnia, feelings of anxiety, confusion, euphoria and excitement. Hallucinations, delirium and nightmares also appear;
• problems with digestive function: burning in the tongue, dry mouth and bitterness in the mouth, dysphagia and hypersalivation. In addition, there are painful sensations in the peritoneum, hiccups, diarrhea, constipation and bloating;
• metabolic disorders: the appearance of swelling, as well as an increase or decrease in weight;
• skin surface lesions: hyperhidrosis, flushing of the skin on the face, alopecia and rashes. Sweat can also be colored dark;
• disorders of the urogenital system: urinary incontinence or retention, dark urine and priapism;
• disturbances in the functioning of the sense organs: mydriasis and diplopia, as well as oculomotor crisis;
• Other symptoms: feeling of malaise and weakness, hot flashes, hoarseness, dyspnea, headaches, teeth grinding, malignant melanoma and NMS.

Overdose

Signs of poisoning: early symptoms include muscle twitching and blepharospasm. Heart rate also increases, blood pressure rises, and appetite decreases. There is a feeling of restlessness, anxiety, and agitation, as well as confusion, and insomnia.

Emergency gastric lavage and induction of vomiting are required to relieve symptoms.

Symptomatic measures are also taken: infusions are carefully performed, the level of patency of the respiratory ducts is monitored, and if arrhythmia develops, appropriate procedures are performed, while monitoring the ECG. There is no data on the effect of dialysis on these disorders. The use of pyridoxine will not have an effect.

Interactions with other drugs

In people who use antihypertensive drugs, the drug can provoke the development of manifestations of orthostatic collapse. In this regard, it is necessary to correct the doses of antihypertensive drugs at the initial stage of therapy using Levokom.

When combined with tricyclics, negative symptoms may develop, including dyskinesia and increased blood pressure.

It is prohibited to combine the drug with MAOIs. These drugs must be discontinued 14 days before starting to use Levokom.

Butyrophenones with phenothiazines may reduce the medicinal effect of the drug.

Phenytoin with papaverine are able to eliminate the antiparkinsonian effect of the drug.

Metoclopramide increases plasma levodopa levels.

Iron preparations can inhibit the absorption of levodopa.

The drug can be combined with other antiparkinsonian drugs that do not contain levodopa.

People who eat a high-protein diet may experience decreased absorption of the drug.

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Storage conditions

Levokom should be stored in a place closed to small children. The temperature level should not exceed 25°C.

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Shelf life

Levokom can be used for 3 years from the date of manufacture of the medicinal product.

Application for children

Prescribing Levokom to children is prohibited.

Analogues

The following drugs are analogs of the drug: Levocarbhexal with Duodopa and Madopar, as well as Carbidopa and Levodopa, Nakom, Levokom retard and Stalevo.