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Levodopa dosage. Levodopa and dopamine deficiency in Parkinson's disease

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Latin name: Levodopa/Benserazide-Teva

ATX code: N04BA

Active substance: Levodopa + Benserazide

Manufacturer: Pharmaceutical plant Teva Private Co. Ltd., Hungary

Description is valid on: 14.12.17

Levodopa benserazide is an antiparkinsonian drug.

Active substance

Levodopa + Benserazide.

Release form and composition

Levodopa benserazide is sold in tablet form. The medication is available in polyethylene bottles (20, 30, 50, 60 or 100 tablets), placed in cardboard packages of 1 pc.

Indications for use

The indication for prescribing the drug is Parkinson's disease.

Contraindications

Contraindications to the use of the drug are:

Severe functional disorders of the liver and/or kidneys.
Exogenous and endogenous psychoses.
Severe functional disorder of the endocrine system.
Glaucoma.
Women of childbearing age who are not using reliable methods of contraception.
Severe functional impairment of the cardiovascular system.
The period of pregnancy and breastfeeding.
Combined use with non-selective MAO inhibitors.
The patient's age is up to 25 years.
Hypersensitivity to benserazide, levodopa or other auxiliary components.

Instructions for use Levodopa Benserazide (method and dosage)

The drug is intended for oral use. The tablets should be taken half an hour before or an hour after meals with a small amount of liquid.

Treatment should begin with a minimum dose, gradually increasing until the desired therapeutic effect is achieved. It is not recommended to take large doses of the drug.

For patients who have not previously taken levodopa, the drug is prescribed 50 mg levodopa/12.5 mg benserazide 2-4 times a day. If the patient responds normally to the therapy, it is possible to increase the dosage of the drug to 100 mg levodopa/25 mg benserazide, which are taken every three days until the desired effect is achieved.

The maximum permissible dosage per day is 800 mg for levodopa and 200 mg for benserazide.

If an adverse reaction develops, it is necessary to reduce the dosage of the drug or completely discontinue this drug.

For patients who have previously taken levodopa, this drug should be started 12 hours after stopping levodopa. The dosage should be approximately 20% of the previously taken dose of levodopa.

Patients with Parkinson's disease who have previously taken levodopa in combination with an aromatic L-amino acid decarboxylase inhibitor should begin taking it 12 hours after stopping previous therapy. To prevent a decrease in the effectiveness of treatment, treatment should be stopped at night and Levodopa Benserazide should be started the next morning.

Dosage regimens in special cases

Patients experiencing severe motor fluctuations should take the drug more than 4 times a day, following the daily dosage.

Elderly people should increase their dosage very slowly.

Patients with mild to moderate renal and hepatic impairment do not require dose adjustment.

In case of spontaneous movements (athetosis or chorea) or a negative reaction from the cardiovascular system, it is recommended to reduce the daily dosage.

Side effects

Using the drug may cause the following side effects:

Central nervous system: often - episodes of “freezing”, headache, “on-off” phenomenon, dizziness, weakening of the effect towards the end of the dose, convulsions, increased symptoms of restless legs syndrome, spontaneous movement disorders (such as athetosis and chorea) ; sometimes – episodes of sudden drowsiness, severe drowsiness.
Cardiovascular system: sometimes - increased blood pressure, orthostatic hypotension (weakens after reducing the dose of the drug), arrhythmias; frequency unknown – “tides”.
Hematopoietic system: sometimes – thrombocytopenia, transient leukopenia, hemolytic anemia.
Digestive system: sometimes - attacks of nausea, diarrhea, vomiting, dryness of the oral mucosa, isolated cases of changes or loss of taste; frequency unknown - bleeding in the gastrointestinal tract.
Subcutaneous tissues and skin: rarely - skin rashes, itching.
Mental disorders: rarely - insomnia, agitation, increased libido, anxiety, anorexia, depressed mood, hypersexuality, delirium, pathological addiction to gambling, moderate delight, depression, aggression; sometimes – temporary disorientation, hallucinations.
Laboratory indicators: uncommon - increased concentrations of bilirubin, alkaline phosphatase, creatinine and urea in the blood, transient increase in the activity of liver enzymes, change in urine color to red (may darken when standing).
Other: frequency unknown - excessive sweating, febrile fever.

Overdose

Symptoms of overdose: increased manifestation of negative reactions - pathological involuntary movements, insomnia, arrhythmia, nausea and vomiting, confusion. The development of signs of overdose may be delayed as a result of delayed absorption of the drug from the gastrointestinal tract.

Symptomatic therapy is used as treatment, which consists of taking antipsychotics, antiarrhythmic drugs and respiratory analeptics.

Analogues

Analogs by ATC code: Levodopa + Benserazide, Madopar.

Do not decide to change the drug on your own; consult your doctor.

pharmachologic effect

Levodopa Benserazide is a combination drug that has an antiparkinsonian effect. It contains a dopamine precursor and a peripheral aromatic L-amino acid decarboxylase inhibitor.

In Parkinson's disease, dopamine is synthesized in insufficient quantities and this drug is used as replacement therapy. The main part of levodopa is transformed into dopamine in peripheral tissues, which does not have an antiparkinsonian effect. To increase the effect of this substance, the drug is supplemented with benserazide.

special instructions

Undesirable manifestations from the gastrointestinal tract (occur at the initial stage of therapy) are largely eliminated with a slower dose increase, as well as if the tablets are taken with a small amount of liquid or taken with meals. The use of the drug for the treatment of Huntington's chorea and iatrogenic extrapyramidal syndrome is not advisable.

People with a history of osteomalacia, gastrointestinal ulcers and seizures need to regularly analyze the relevant indicators. During therapy, it is necessary to monitor the functional parameters of the kidneys, liver, and blood count. Patients with a history of heart rhythm disturbances, myocardial infarction, or coronary heart disease should undergo regular electrocardiogram monitoring.

Patients with a history of orthostatic hypotension should be closely monitored by a specialist, especially at the beginning of treatment.

Patients with diabetes need frequent dosage adjustments of oral hypoglycemic agents and monitoring of blood glucose levels. Cases of sudden onset of sleep have been reported with the use of Levodopa Benserazide. Patients should be informed about this.

When using the drug, the risk of malignant melanoma increases. In this regard, taking pills in people with this disease (including a history of it) is not advisable. Use of this drug, especially in high doses, increases the likelihood of developing compulsive disorders.

Taking Levodopa Benserazide should not be stopped abruptly. This can provoke a “withdrawal syndrome” (muscle stiffness, increased body temperature, as well as a possible increase in the activity of creatinine phosphokinase in the blood and mental changes) or an akinetic crisis, which can take a life-threatening form. If such signs appear, the patient should be under close supervision of a specialist (hospitalization if necessary) and receive appropriate treatment. Sometimes repeated use of Levodopa Benserazide is advisable.

Before general anesthesia, the medication should be taken for as long as possible. An exception is halothane anesthesia. Since a patient receiving Levodopa Benserazide may develop arrhythmias and blood pressure fluctuations during halothane anesthesia, the drug should be discontinued 12-24 hours before surgery. After surgery, therapy is resumed, gradually increasing the dose.

Some people with Parkinson's disease have developed cognitive and behavioral disorders due to uncontrolled use of increasing doses of the drug (despite a significant increase in therapeutic doses and doctor's recommendations).

Depression may occur during treatment with Levodopa Benserazide. It can also be a clinical symptom of an underlying disease (parkinsonism). Such people should be under the supervision of a physician for timely detection of psychiatric adverse reactions.

Experience with the drug in people under 25 years of age is limited.

Patients who experience sudden sleep episodes or excessive daytime sleepiness should avoid driving or operating complex machinery. If these signs occur during therapy, it is advisable to consider discontinuing treatment or reducing the dose.

During pregnancy and breastfeeding

The drug is contraindicated during pregnancy and breastfeeding.

In childhood

The drug is not prescribed to persons under 25 years of age.

In old age

It is prescribed with special caution to elderly people. A slow increase in dosage is required.

For impaired renal function

The drug is not prescribed to patients with severe renal failure.

For liver dysfunction

The drug is contraindicated in severe liver dysfunction.

Drug interactions

Trihexyphenidyl and Metoclopramide reduce the rate of absorption of levodopa, and antacids reduce the degree of absorption.

Antipsychotics, opioids, and antihypertensive drugs containing reserpine help suppress the effect of the drug. Pyridoxine reduces the antiparkinsonian effect of the drug.

Combining the drug with non-selective MAO inhibitors is contraindicated.

Combined use of the drug with antihypertensive drugs can lead to the development of orthostatic hypotension.

Combining levodopa/benserazide with other antiparkinsonian drugs is acceptable.

High-protein foods reduce the therapeutic effect of the drug.

Levodopa/benserazide may affect laboratory test results for creatinine, bilirubin, alkaline phase, uric acid, and catecholamines.

Conditions for dispensing from pharmacies

Dispensed by prescription.

4.42 out of 5 (6 Votes)

pharmachologic effect

Antiparkinsonian drug. The active substance is a precursor of dopamine, into which it is converted as a result of decarboxylation.
The drug reduces rigidity and hypokinesia, tremor, dysphagia and salivation, increases range of motion, and restores the ability to concentrate.

Mode of application

Method of administration and dosage of Levodopa
Inside, with a small amount of food or after a meal, with water and without chewing. Since there is competition between aromatic amino acids and levodopa for absorption, large amounts of protein should be avoided while using the drug.
The average daily dose of carbidopa required to suppress the peripheral conversion of levodopa is 70-100 mg. Exceeding 200 mg of carbidopa does not entail a further increase in the therapeutic effect. The daily dose of levodopa should not exceed 2000 mg.
The initial dose is 1/2 tablet 2 times a day, if necessary, it can be increased by 1/2 tablet per day. As a rule, at the beginning of replacement therapy, the daily dose should not exceed 3 tablets per day (1 tablet 3 times a day).
Use at this dosage is recommended at the beginning of treatment of severe cases of parkinsonism.
As an exception, the daily dose of the drug can be increased during monotherapy, but should not exceed 8 tablets (1 tablet 8 times a day). Use of more than 6 tablets per day should be done with great caution.

Indications

Parkinson's disease, parkinsonism syndrome (except for parkinsonism caused by antipsychotics).

Contraindications

Hypersensitivity, simultaneous use of MAO inhibitors, pregnancy, lactation, children (up to 12 years). With caution.
Diseases of the kidneys and liver, lungs, endocrine system, cardiovascular system, psychosis, closed-angle (including predisposition) and open-angle (chronic course) glaucoma, liver and/or renal failure, melanoma (including history), central nervous system depression, seizures , bronchial asthma, emphysema, peptic ulcer of the stomach and duodenum, myocardial infarction (including a history, as well as in combination with atrial, nodal or ventricular arrhythmias), heart rhythm disturbances (history).

Side effects

Nausea, anorexia, vomiting, epigastric pain, constipation, dysphagia, gastrointestinal bleeding (in patients with a history of peptic ulcer), hypotension, weakness, dizziness, agitation, insomnia, tachycardia, polyuria. Rarely - cardiac arrhythmias, diplopia.
Special instructions. The drug is not combined with MAO inhibitors, pyridoxine, reserpine, phenothiazine, amphetamine

Release form

Tablets 25 mg, 250 mg, 500
10 tablets in a blister made of PVC film and aluminum foil. 10 blisters along with instructions for use are placed in a cardboard box.

ATTENTION!

The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to provide healthcare workers with additional information about certain medications, thereby increasing their level of professionalism. The use of the drug "" necessarily requires consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.

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ANTIPARKINSONIC DRUGS

This group of drugs is used to treat parkinsonism, the occurrence of which is associated with damage to the extrapyramidal system (basal ganglia and substantia nigra), where metabolic processes are disrupted (as a result of sclerosis of cerebral vessels, inflammatory reactionstions, etc.) and the content of dopamine decreases. This leads to a decrease in the inhibitory effect of dopamine on certain brain structures (in particular, the striatum) that regulate the activity of motor neurons. As a result, choliner begins to predominateical influence (excitation of cholinergic neurons of the caudate nucleus), which, inultimately leads to an increase in skeletal muscle tone. Characteristic symptoms of parkinsonism are stiffness of movement, tremors, mincing gait, mask-like face, and muscle rigidity.

Treatment of the disease can be aimed at either enhancing dopaminergic effects or reducing cholinergic ones.

DRUGS THAT ACTIVATE THE DOPAMINERGIC MECHANISM

LEVODOPA (pharmacological analogues: levopa, dopaflex, etc.) - penetrates the blood-brain barrier and is converted into dopamine in the basal ganglia, thus enhancing the dopaminergic effect. Levdopa is prescribed orally at a dose of 0.25 g and gradually (over 1-2 months) the dose is increased to 3-5 g per day (prescribed in 3-4 doses). Side effects of levdopa: a sharp decrease in blood pressure when changing body position (orthostatic hypotension), nausea, vomiting, increased excitability of the nervous system. Levdopa is contraindicated in cases of dysfunction of the liver and kidneys, endocrine glands in childhood, and in women during lactation. Release form of levdopa: tablets and capsules containing 0.25 g and 0.5 g of the drug. List B.

Recipe example l eudopa in Latin:

Rp.: Levodopa 0.5 (Levopa)

D.t. d. N. 500 in caps, gelat.

S. 1 capsule 4 times a day.

There are drugs containing levodopa: nacom (sinemet) and madopar

ON WHOM (pharmacological analogues: sinemet) - contains 0.25 g of levodopa and 0.025 g of carbidopa monohydrate in 1 tablet. Nakom produces tablets with a different ratio of active ingredients. Prescribed orally (during or after meals) 1/2 tablet 1-2 times a day, the dose is increased by "/ 2 tablets every 2-3 days. The optimal dose of nacoma is usually 3-6 tablets per day (but not more than 8 tablets Side effects the effects when using nacom and contraindications are the same as for levodopa.Currently, a long-acting drug “Nakom SP” (Sinemet-Plus) has been developed in the USA, more effective and less toxic than nacom.

MADOPAR- a drug containing levodopa and benserazide hydrochloride. Treatment begins with madopar-125 by taking 1 capsule 3 times a day, gradually increasing the dose (usually 4-8 capsules per day). When increasingdaily dose of madopar (more than 5 capsules), it is advisable to switch to treatment with madopar-250. Side effects of madopar and contraindications are the same as for levodopa. Release form of levdopa: capsules containing 100 mg of levodopa and 25 mg of benserazide (madopar-125) and 200 mg of levodopa and 50 mg of benserazide (madopar-250).

In recent years, a new dosage form “Madopar - HBS” has been created in special capsules that provide prolonged action.

N04BA03 (Levodopa in combination with a decarboxylase inhibitor and a COMT inhibitor)
N04BA02 (Levodopa in combination with a decarboxylase inhibitor)

Analogues of the drug according to ATC codes:

Clinical and pharmacological groups

02.017 (Antiparkinsonian drug - a combination of a precursor with a peripheral dopa decarboxylase inhibitor and a COMT inhibitor)
02.016 (Antiparkinsonian drug - a combination of a dopamine precursor and a peripheral dopa decarboxylase inhibitor)

pharmachologic effect

Antiparkinsonian drug. It is a levorotatory isomer of dioxyphenylalanine, a precursor of dopamine, into which levodopa is converted under the influence of the enzyme dopa decarboxylase. The antiparkinsonian effect of levodopa is due to its conversion to dopamine directly in the central nervous system, which leads to replenishment of dopamine deficiency in the central nervous system. However, most of the levodopa that enters the body is converted to dopamine in peripheral tissues. Dopamine formed in peripheral tissues is not involved in the implementation of the antiparkinsonian effect of levodopa, because does not penetrate the central nervous system, in addition, it causes most of the peripheral side effects of levodopa. In this regard, it is advisable to combine levodopa with peripheral dopa decarboxylase inhibitors (carbidopa), which can significantly reduce the dose of levodopa and the severity of side effects.

Pharmacokinetics

When taken orally, it is quickly absorbed from the gastrointestinal tract. Absorption depends on the rate of gastric emptying and the pH in the stomach. The presence of food in the stomach slows down absorption. Some dietary amino acids may compete with levodopa for absorption from the intestine and transport across the BBB. Cmax in blood plasma is achieved 1-2 hours after oral administration.

Only 1-3% of the active substance penetrates the brain, the rest is metabolized extracerebrally, mainly by decarboxylation to form dopamine, which does not penetrate the BBB.

About 75% is excreted in the urine in the form of metabolites within 8 hours.

LEVODOPA: DOSAGE

Individual. Treatment begins with a small dose, gradually increasing it to the optimal dose for each patient. At the beginning of treatment, the dose is 0.5-1 g/day, the average therapeutic dose is 4-5 g/day. When treating with drugs containing levodopa with peripheral dopa decarboxylase inhibitors, significantly lower daily doses are used in terms of levodopa.

The maximum daily dose when taken orally is 8 g.

Drug interactions

When used simultaneously with antacids, the risk of side effects increases.

When used simultaneously with antipsychotics (neuroleptics) derivatives of butyrophenone, diphenylbutylpiperidine, thioxanthene, phenothiazine, pyridoxine, the antiparkinsonian effect may be inhibited.

When used simultaneously with beta-agonists, heart rhythm disturbances are possible.

When used simultaneously with MAO inhibitors (except for MAO type B inhibitors), circulatory disorders are possible. This is due to the accumulation of dopamine and norepinephrine under the influence of levodopa, the inactivation of which is slowed down by the influence of MAO inhibitors.

When used simultaneously with m-anticholinergics, the antiparkinsonian effect may be reduced; with anesthesia - the risk of developing arrhythmia.

There is evidence of a decrease in the bioavailability of levodopa with simultaneous use of tricyclic antidepressants.

When used simultaneously with diazepam, clozepine, methionine, clonidine, phenytoin, the antiparkinsonian effect may be reduced.

When used simultaneously with lithium salts, the risk of developing dyskinesias and hallucinations may increase.

When used simultaneously with papaverine hydrochloride and reserpine, a significant decrease in the antiparkinsonian effect is possible; with suxamethonium - arrhythmias are possible; with tubocurarine - increased risk of developing arterial hypotension.

Pregnancy and lactation

If it is necessary to use levodopa during lactation, the issue of stopping breastfeeding should be decided.

LEVODOPA: SIDE EFFECTS

From the cardiovascular system: often - orthostatic hypotension, arrhythmias.

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

From the side of the central nervous system: often - spontaneous movements, sleep disturbances, agitation, dizziness; rarely - depression.

From the hematopoietic system: rarely - leukopenia, thrombocytopenia.

When treated with drugs containing levodopa with peripheral dopa decarboxylase inhibitors, these side effects are less common.

Indications

Parkinson's disease, parkinsonism syndrome (except for parkinsonism caused by antipsychotics).

Contraindications

Severe dysfunction of the liver, kidneys, cardiovascular and/or endocrine systems, severe psychoses, angle-closure glaucoma, melanoma, hypersensitivity to levodopa, childhood.

special instructions

Use with caution in patients with diseases of the kidneys, lungs, endocrine system, cardiovascular system, especially if there is a history of myocardial infarction or heart rhythm disturbances; for mental disorders, liver diseases, peptic ulcers, osteomalacia; in patients with diseases that may require the use of sympathomimetic drugs (including bronchial asthma), antihypertensive drugs.

Abrupt discontinuation of levodopa should be avoided.

When transferring a patient from treatment with levodopa to treatment with levodopa with peripheral dopa decarboxylase inhibitors, levodopa should be discontinued 12 hours before prescribing the combination drug.

The simultaneous use of levodopa with MAO inhibitors (with the exception of MAO type B inhibitors) is not recommended, as circulatory disorders are possible, incl. arterial hypertension, agitation, palpitations, facial flushing, dizziness.

Impact on the ability to drive vehicles and operate machinery

During the period of use of levodopa, you should avoid activities that require a high concentration of attention and speed of psychomotor reactions.