Pharmacological group of levodopa substance

Nonological Classification (ICD-10)

CAS code

Characteristics of the substance of Legodopa

White crystalline powder. Little soluble in water, insoluble in alcohol.

Pharmacology

It is a predecessor of dopamine. It penetrates through the BBB, accumulates in the basal ganglia and turns into dopamine, igniteing the lack of the latter in the extrapyramidal system. As a result, the rigidity of muscles and hypokinesia decreases. Well absorbed when taking inside; C MAX is determined after 1-2 hours, some of it is transformed into dopamine already in the blood and does not fall into the basal kernels (dopamine does not pass BGB). Excaped mainly kidneys.

Application of the substance of Levodopopia

Parkinson's disease, symptomatic Parkinsonism.

Contraindications

Hypersensitivity, pronounced atherosclerosis, hypertonic disease, diseases of the liver, kidneys, blood, glaucoma, melanoma, bronchial asthma, mental diseases, noncompensated pathology of cardiovascular, respiratory, endocrine systems.

Restrictions on application

Pregnancy, breast-feeding, childhood (up to 12 years), myocardial infarction in history.

Side effects of the substance levodop

Horoiatethyoid hypercines, arrhythmia, psychotic and paranoid reactions, dyspeptic phenomena, ultraceration of the gastrointestinal tract, headache, dizziness, violation, hemolytic anemia, agranulocytosis and leukopenia, alopecia, allergic reactions.

Interaction

The effect relaxes vitamin B 6. Enhances the action of Mao inhibitors.

Anti-parkinsonic.
The active substance of the drug: Levodopa / Levodopopia

Pharmacological effect of levodopa / Levodopa

Anti-parkinsonic. It is the left-handing isomer of Dopa - the predecessor of dopamine, in which the levodopa turns under the influence of the Dopa-Decarboxylase enzyme. The anti-parkinsonic effect of Leveodopa is due to its transformation into dopamine directly into the central nervous system, which leads to replenishing dopamine deficiency in the CNS. However, most of the levodopa entered the body turns into dopamine in peripheral tissues. The dopamine formed in the peripheral tissues does not participate in the implementation of the anti-parkinsonic effect of Levodopa, because It does not penetrate the CNS, in addition, it causes most of the peripheral side effects of Leveodopa. In connection with this, the levodopa is advisable to combine with peripheral dopa-decarboxylase (carbide, benserazide) inhibitors, which makes it possible to significantly reduce the dose of Levodopa and the severity of side effects.

Pharmacokinetics of the drug.

When taking inside, it is quickly absorbed from the gastrointestinal tract. Suction depends on the speed of evacuation of the contents of the stomach and from the pH in it. The presence of food in the stomach slows down suction. Some food amino acids can compete with the levodopa for absorption from the intestine and transport through the BC. Cmax in blood plasma is achieved after 1-2 hours after intake.

Only 1-3% of the active substance penetrates the brain, the remaining part is metabolized by extracerebral, mainly by decarboxylation with the formation of dopamine, which does not penetrate the BGB.

About 75% is derived from the urine in the form of metabolites for 8 hours.

Indications for use:

Parkinson's disease, Parkinsonism syndrome (with the exception of Parkinsonism caused by neuroleptics).

Dosage and method of use of the drug.

Individual. Treatment starts with a low dose, gradually increasing it to optimal for each patient. At the beginning of the treatment, the dose is 0.5-1 g / day, the average therapeutic doses - 4-5 g / day. In the treatment with drugs containing levodopop with peripheral dopa-decarboxylase inhibitors, in terms of Levodopa, significantly smaller daily doses are used.

Maximum daily dose: when taking inside - 8 g

Side effect of levodopa / Levodopa:

From the side of the cardiovascular system: often - orthostatic hypotension, arrhythmia.

From side digestive system: often - nausea, vomiting, anorexia, epigastric pain, dysphagia, ulcerogenic effect (in predisposed patients).

From the CNS: often - spontaneous movements, sleep disorders, assessment, dizziness; Rarely depressed.

From the system of blood formation: rarely leukopenia, thrombocytopenia.

In the treatment with drugs containing levodopop with peripheral dopa-decarboxylase inhibitors indicated side effects Come less often.

Contraindications for the drug:

Pronounced violations of the liver, kidney function, cardiovascular and / or endocrine systems, heavy psychosis, closedian glaucoma, melanoma, increased sensitivity to Levodopa, children's age.

Application during pregnancy and lactation.

If necessary, the use of levodopa during the lactation period should be resolved by the issue of cessation of breastfeeding.

Special guidelines for the use of levodopa / levodopa.

Caution to apply in patients with kidney diseases, lungs, endocrine system, cardiovascular system, especially when instructed by a history of myocardial infarction, violations heart Rhythm; in mental disorders, liver diseases, peptic ulcers, osteomalysis; In patients with diseases in which the use of sympathomimetic means may be required (including bronchial asthma), antihypertensive means.

Avoid sudden cessation of levodopa.

When translating the patient with the treatment of levodopa for the treatment of levodopa with peripheral dopa-decarboxylase inhibitors, levodopa reception should be stopped 12 hours before the combined drug is appointed.

The simultaneous use of levodopes with Mao inhibitors (with the exception of Mao Type B inhibitors) is not recommended, since blood circulation disorders are possible, incl. arterial hypertension, excitation, heartbeat, face redness, dizziness.

Impact on the ability to driving vehicles and control mechanisms

During the application period, levodopa should avoid activities at which a high concentration of attention and the speed of psychomotor reactions is required.

The interaction of levodopa / levodopa with other drugs.

With simultaneous use with antacids, the risk of side effects of the side effects increases.

With simultaneous use with antipsychotic means (neuroleptics), butthirofenone derivatives, diphenylbutyzine, thioxantine, phenothiazine, pyridoxine is possible oppression of anti-parkinsonic action.

With simultaneous use with beta adrenomimetics, heart rate disorders are possible.

With simultaneous use with Mao inhibitors (with the exception of Inhibitors of Mao Type B), circulatory disorders are possible. This is due to the accumulation under the influence of dopamine and norepine levels, the inactivation of which slows down under the influence of Mao inhibitors.

With simultaneous use with M-cholinoblockers, a decrease in anti-parkinsonic action is possible; With the means for anesthesia - the risk of developing arrhythmia.

There are data on the reduction of levodop bioavailability while simultaneously use of tricyclic antidepressants.

With simultaneous use with diazepam, cloop, methionine, clonidine, phenytio is possible to reduce anti-parkinsonic action.

With simultaneous use with lithium salts, it is possible to raise the risk of dyskinesium and hallucinations.

With simultaneous use with papaverine hydrochloride, a significant reduction in anti-parkinsonic action is possible; with suucamenim - the arrhythmias are possible; With tubararian - raising the risk of the development of the arterial hypotension.

Description of the active component

pharmachologic effect

Anti-parkinsonic. It is a left-handing isomer of dioxiphenylalanine - a dopamine precursor, in which the levodopa turns under the influence of the enzyme dopa-decarboxylase. The anti-parkinsonic effect of Leveodopa is due to its transformation into dopamine directly into the central nervous system, which leads to replenishing dopamine deficiency in the CNS. However, most of the levodopa entered the body turns into dopamine in peripheral tissues. The dopamine formed in the peripheral tissues does not participate in the implementation of the anti-parkinsonic effect of Levodopa, because It does not penetrate the CNS, in addition, it causes most of the peripheral side effects of Leveodopa. In connection with this, the levodopa is advisable to combine with peripheral dopa-decarboxylase (carbide, benserazide) inhibitors, which makes it possible to significantly reduce the dose of Levodopa and the severity of side effects.

Indications

Parkinson's disease, Parkinsonism syndrome (with the exception of Parkinsonism caused by neuroleptics).

Dosing mode

Individual. Treatment starts with a low dose, gradually increasing it to optimal for each patient. At the beginning of the treatment, the dose is 0.5-1 g / day, the average therapeutic doses - 4-5 g / day. In the treatment with drugs containing levodopop with peripheral dopa-decarboxylase inhibitors, in terms of Levodopa, significantly smaller daily doses are used.

Maximum daily dosewhen taking inside is 8 g.

Side effect

From the side of the cardiovascular system: Often - orthostatic hypotension, arrhythmia.

From the digestive system: Often - nausea, vomiting, anorexia, epigastric pain, dysphagia, ulcerogenic effect (in predisposed patients).

From the CNS: Often - spontaneous movements, sleep disorders, assessment, dizziness; Rarely depressed.

From the hematopopitation system: Rarely leukopenia, thrombocytopenia.

In the treatment with drugs containing levodopop with peripheral dopa-decarboxylase inhibitors, the specified side effects are less common.

Contraindications

Pronounced violations of the liver, kidney function, cardiovascular and / or endocrine systems, heavy psychosis, closedian glaucoma, melanoma, increased sensitivity to Levodopa, children's age.

Pregnancy and lactation

If necessary, the use of levodopa during the lactation period should be resolved by the issue of cessation of breastfeeding.

Application with violations of liver function

The lesodopa is contraindicated with pronounced liver function. With caution to apply with liver diseases.

Application with violations of the kidney function

Legodopa is contraindicated with pronounced renal impairments. With caution to apply in patients with kidney disease.

Application for children

Legodopa is contraindicated in childhood.

special instructions

With caution to apply in patients with diseases of the kidneys, lungs, endocrine system, cardiovascular system, especially when instructed by the myocardial infarction, heart rate disorders; in mental disorders, liver diseases, peptic ulcers, osteomalysis; In patients with diseases in which the use of sympathomimetic means may be required (including with bronchial asthma), antihypertensive agents.

Avoid sudden cessation of levodopa.

When translating the patient with the treatment of levodopa for the treatment of levodopa with peripheral dopa-decarboxylase inhibitors, levodopa reception should be stopped 12 hours before the combined drug is appointed.

The simultaneous use of levodopes with Mao inhibitors (with the exception of Mao Type B inhibitors) is not recommended, since blood circulation disorders are possible, incl. Arterial hypertension, excitation, heartbeat, redness of the face, dizziness.

Impact on the ability to driving vehicles and control mechanisms

During the application period, levodopa should avoid activities at which a high concentration of attention and the speed of psychomotor reactions is required.

Medicinal interaction

With simultaneous use with antacids, the risk of side effects of the side effects increases.

With simultaneous use with antipsychotic means (neuroleptics), butthirofenone derivatives, diphenylbutyzine, thioxantine, phenothiazine, pyridoxine is possible oppression of anti-parkinsonic action.

With simultaneous use with beta adrenomimetics, heart rate disorders are possible.

With simultaneous use with Mao inhibitors (with the exception of Inhibitors of Mao Type B), circulatory disorders are possible. This is due to the accumulation under the influence of dopamine and norepine levels, the inactivation of which slows down under the influence of Mao inhibitors.

With simultaneous use with M-cholinoblockers, a decrease in anti-parkinsonic action is possible; With the means for anesthesia - the risk of developing arrhythmia.

There are data on the reduction of levodop bioavailability while simultaneously use of tricyclic antidepressants.

With simultaneous use with diazepam, cloop, methionine, clonidine, phenytio is possible to reduce anti-parkinsonic action.

With simultaneous use with lithium salts, it is possible to raise the risk of dyskinesium and hallucinations.

With simultaneous use with papaverine hydrochloride, a significant reduction in anti-parkinsonic action is possible; with suucamenim - the arrhythmias are possible; With tubararian - raising the risk of the development of the arterial hypotension.

Recipe (international)

RP: Levodopa 0.5 (Levopa)
D. T. d. N. 500 IN CAPS, GELAT.
S. 1 capsule 4 times a day.

Recipe (Russia)

Recipentar Blank - 107-1 /

Active substance

Levodopa, Benserazide (Levodopa, Benserazide)

pharmachologic effect

Anti-parkinsonic. The active substance is a predecessor of dopamine, which turns into a decarboxylation.
The drug reduces the rigidity and hypokinesia, tremor, dysphagia and salivation, contributes to an increase in the volume of movements, restores the ability to concentrate attention.

Mode of application

For adults: The use and dose of levodopa
Inside, with a little food or after eating, drinking water and not chewing. Since there is a competition between aromatic amino acids and levodopa during suction, during the use of the drug should avoid consumption of a large number of proteins.
The average daily dose of carbide, necessary to suppress the peripheral transformation of Levodopa, is 70-100 mg. Exceeding 200 mg carbide does not entail further strengthening the therapeutic effect. Daily dose Levodopa should not exceed 2000 mg.
Initial dose - 1/2 tablets 2 times a day, if necessary, can be increased by 1/2 tablets per day. As a rule, at the beginning of substitution therapy, the daily dose should not exceed 3 tablets per day (on the 1st tablet 3 times a day).
Application in this dosage is recommended at the beginning of the treatment of severe cases of Parkinsonism.
The daily dose of the drug in the form of exception can be increased during monotherapy, but should not exceed 8 tablets (according to the 1st tablet 8 times a day). Application in the amount of more than 6 tablets per day should be carried out with great caution.

Indications

Parkinson's disease, Parkinsonism syndrome (with the exception of Parkinsonism caused by neuroleptics).

Contraindications

- increased sensitivity to levodopa, benserazide or any other component of the drug;

- severe violation of the functions of the organs of the endocrine system;

- glaucoma;

- severe liver function;

- severe breach of the kidney function;

- severe violation of the function of the CSS;

- endogenous and exogenous psychosis;

- simultaneous reception with non-selective MAO inhibitors, a combination of Inhibitors of Mao Type A and Mao type B (which is equivalent to non-selective inhibition of MAO);

- women of childbearing age that do not apply reliable methods of contraception;

- pregnancy;

- period of breastfeeding;

Side effects

From the side of the blood formation system: very rarely hemolytic anemia, transient leukopenia, thrombocytopenia.

From side nervous system: often - headache, dizziness, convulsions, spontaneous motor disorders (such as chore and athetosis), episodes of frozen, weakening the effect by the end of the dose period, the inclusion phenomenon, enhancing the manifestations of restless leg syndrome; Very rarely expressed drowsiness, episodes of sudden drowsiness.

Violations of psyche: rarely - assessment, anxiety, depressed mood, insomnia, nonsense, aggression, depression, anorexia, moderate delight, pathological tendency to gambling, hypersexuality, elevated libido; Very rarely hallucinations, temporary disorientation.

From the SCC: very rare arrhythmias, orthostatic hypotension (weakens after a reduction in the dose of the drug), an increase in blood pressure; The frequency is unknown - tides.

From the digestive system: very rarely - nausea, vomiting, diarrhea, individual cases of loss or change of taste sensations, dry oral mucosa; The frequency is unknown - gastrointestinal bleeding.

From the side of the skin and subcutaneous fabrics: rarely - itching the skin, rash.

From the side of the laboratory indicators: infrequently - transient increase in the activity of hepatic transaminases, the urea, increasing the concentration of bilirubin, the increase in urea and creatinine in the blood, the change in urine color to the red, darkening when standing.

Others: The frequency is unknown - febrile fever, high sweating.

Form release

Tablets 100 mg + 25 mg: 20, 30, 50, 60 or 100 pcs.
Tablets 200 mg + 50 mg: 20, 30, 50, 60 or 100 pcs.

ATTENTION!

Information on the page you will be viewed exclusively for informational purposes and does not promote self-treatment. The resource is intended to familiarize health officers with additional information about certain medicines, thereby increasing their level of professionalism. The use of the drug "" necessarily provides for advice with a specialist, as well as its recommendations for the method of application and dosage of the medicine you have chosen.

Parkinson's patients doctors may discharge different medicines. But one of the best, of course, is "levodopa". This truly unique medical drug helps to alleviate almost all the symptoms of the disease. In addition to Parkinson's disease« Levodopa, instructions for usewhich will be considered by us in the article can be used And in some other cases.

Composition and form of release

Supplied in the pharmacy pharmacological companies is a medicine in the form of ordinary tablets (0.25 and 0.5 mg). The main active substance of the drug ise.because of the levodopa itself. In addition, the medicine contains several auxiliary components. Sometimes in the pharmacy you can also purchase capsules of this drug. They contain white crystalline powder, poorly soluble in water.

For the first time, this composition was applied in the 60s of the last century. Then he was considered hardly a magical means. It was the first medicine that helps with neuralgic diseases. Previously, the missing substances, the pharmacological industry not been produced in the patient's brain of the patient.

What action is rendered

Pharmacologically, this medicine is a predecessor of dopamine. Penetrated through the BC, the drug accumulates in basal ganglia. Here he turns into dopamine. The benefits of this drug, among other things, belong to the fact that it is very well absorbed inside the body. The maximum effect of its reception occurs in about 1-2 hours. The drug from the body of the kidneys is derived.

Indications for use

Disposable "Leodopopia" medicine, the instruction on the use of which is not particularly difficult, most often it is when Parkinson's disease. It is also used to treat:

symptomatic parkinsonism;

hereditary extrapyramidal diseases;

deforming muscle dystonia.

There are also data on the successful use of this medication in spoiling states. In Parkinsonism caused by degenerative generalized brain diseases, this tool is not used. In this case, it is considered ineffective.

"Leveodopa": instructions for the use of the drug

The dosage of this medication is calculated by a doctor for each patient individually. The patient's condition when using this fund should be carefully tracked. We begin treatment with the drug "Levodopa" with small doses. Subsequently, they gradually increase.

Take medicine "Legodopa"Leans 30 minutes before meals. You can also give patients with these tablets and an hour after meals. The initial dose of the drug is most often 0.25 g per day(twice half a tablet). Every two-three days, the amount of the received medicine is raised by 0.25 g. In the end, the dose is adjusted to 3 grams per day. In some cases, the patient may be given the reception of this drug in the amount and 5 g per day. Increase the dosage from 3 g in this case also gradually - by 0.25 g every 10 days.

What symptoms takes off

This is as provided for the drug.and "Levodopa" instructions for use. Follow the recommendations of the attending physician when taking this fund needed.Develops therapeutic effect usingthis medicinegradually. Pronounced improvements in patients are observed about a month after the start of reception. Take the "Levodop" usually long - For 2-5 years. With prolonged use, its effect may decrease a little. It is impossible to abruptly cancel this drug to patients. Otherwisemanifestations Parkinsonism they can jump abandoned.

Good reviews of doctors This medicine has earned primarily for making symptoms:

hypokinesia and muscle rigidity;

tremor;

dysphagia and salivament.

It also restores the patient's ability to concentrate attention and increases the volume of movements.

Compatibility with other medicines

If necessarya drug"Legodop.but», instructionon the use of which was considered by us above can be used in the complex with suchactorlike "Midtan".It is not allowed to apply it simultaneously with drugs containing:

phenothiazine;

reserpine;

pyridoxine;

amphetamine.

Do not write to the means "levodopbut»Patients and simultaneously with Mao inhibitors,since it is able to strengthen the effect of the latter. The effect of receiving the vitamins of the group to this medication, on the contrary, is able to weaken.

ABOUTchen often "levodopw.»Used together with Eldepril preparation. This medicine slows down the process of burning brain cells. And this, in turn, reduces the dosage "Levodops" According to some data, Vitamin E. is different similar effect.

Contraindications

It helps, according to many patients, in Parkinson's disease, a very good medicine "Levodopa" is very good. Instructions for use, however, prescribes it far from all cases. Contraindications to the use of this drug are:

clotted glaucoma;

melanoma;

severe psychosis;

essential tremor;

huntington's disease;

neurosis;

skin diseases of unknown origin.

Also do not prescribe this medicinechildren under 12 years old. It is contraindicated in pregnancy.Otherwise, the fetal may have pathologies for the development of the spine. It is impossible to use it during the lactation period.For peptic disease Stomach, heavy pathologies of the cardiovascular system, with problems with lightweight drugs are prescribed with caution.

Which patient can develop side effects

Sometimes this medicine can have on patients and negative effects. For example, this:

dystonia and dyskinesia;

malignant neuroleptic symptom;

transient psychosis;

convulsions and involuntary movements;

drowsiness, dizziness;

anxiety and insomnia;

hallucinations and confusion of consciousness.

Sometimes patients may also have nausea and vomiting, darling saliva.

Overdose

Thus, prescribes to take up to 3-5 grams in dosages to the drug "Levodopa" instruction. And the composition of each tablet, and even the form of the release of the medicine (there is a fault line) allow you to take it with convenience. Accidentally, drinking too much this drug is impossible. However, overdose of such a medicine, unfortunately, sometimes occur. In this case, the patient may have the following symptoms:

raising blood pressure;

arrhythmia;

confusion of consciousness and anxiety;

ortostatic hypotension.

Prescribing to make a patient to wash the stomach during overdose of the drug "Leveodopa" instructions for use. While all the symptoms disappear, careful control should be carried out for the patient. In addition to washing the stomach, an ECG is assigned to the patient with overdose (to detect arrhythmia). After that, if necessary, appropriate therapy is performed.

What analogues are available

Large doses R.assessable drug Often cause patients with nausea and vomiting.This can occur even if it is accurately complied with the means"Leodopopa" instructions for use. Analogsthis medicine has numerous. But the best is considered yet"Carbidop". This medication Assign to those patients who cannot drink "Levodop" due to nausea.The active substance of this drug is exactly the same. That is, essentially "Carbide " is synonymous "Levodopa ". The difference of this medication is that it controls the receiptactive substance in the brain.

There is a market and another very popular analogue of "Levodopa". It is called "cinema". It is a means of essentially a combination of levodopa / carbide substances. Instructions for use is about the same as the "Levodopa". It is usually prescribed at a dose of 1-2 tablets (250 mg + 25 mg) per day.

Another analogue "Levodopa" is Madopar. The action on the body of patients is the medicine is practically the same. Its active substances are levodopia and benserazide.