Madopar Levodopopa and Benserazide 250 Roche treats innocent Parkinson's disease (30 tablets)
Dosage form Box of 30 tablets
Specifications Levodopa, benserazide
Ingredient
| Composition information | Content |
| Levodopa | 200mg |
| Benserazide | 50mg |
Uses
indications
Madopar drugs are indicated in the following cases:
Madopar is a suitable preparation for patients with difficulty swallowing or patients who need a product that has a faster onset effect.
For example, patients with dysentine loss in the early morning or afternoon, or patients with the phenomenon of delaying time "turning on" or prolonging the "turning" time.
Madopar HBS is indicated for patients with all forms of oscillation (eg, dysligane disorder at the dose or worsening at the end of the dose - such as immobile at night).
Mechanism of action
Parkinson's disease:
dopamine , the substance acts as a neurotransmitter in the brain, does not have enough concentrations in the central gray core of Parkinson patients.
Levodopa (INN) or L - Dopa (3,4 - Dihydroxy L - Phenylalanin) is an intermediate substance during the biosynthesis of dopamine.
levodopa (precursor of dopamine) is used as a precursor to increase dopamine concentration because it can penetrate the blood -brain barrier while freedom can not pass.
When Levodopa entered the central nervous system, it was converted into dopamine by L - Amino acid decarboxylase.
After use, Levodopa has been reduced to the carboxyl group quickly to become dopamine, both in the brain as well as the area outside the brain.
As a result, most of the levodopa taken in is not in the central gray cores, and dopamine is produced in the peripheral region often causing many side effects.
Therefore, it is necessary to pay special attention to preventing Levodopa's carboxyl reduction process in the brain, which can be achieved by simultaneous use of Levodopa with Benserazide, inhibitors of peripheral decarboxylase.
Madopar is a combination of these two substances with a 4: 1 ratio, this ratio has been proven to be optimized in clinical trials and used in treatment and has the same effect as when using high -dose Levodopa.
Yen Nguyen Phat's vacuum syndrome:
It is unknown the exact mechanism of action, but there is evidence that the dopaminergic system plays an important role in the pathology of uneasy vacuum syndrome.
pharmacokinetic
absorption
Common form:
Levodopa is absorbed mainly at the upper segment of the small intestine, and the absorption does not depend on the location. Levodopa's maximum plasma concentration is about an hour after taking the standard Madopar.
Puppies and tablets of ordinary Madopar are equivalent to bioavailability.
Maximum concentration in Levodopa's plasma and Levodopa's absorption level (AUC) increases proportional to the dose (50 - 200mg Levodopa).
Food eats in reducing the speed and level of absorption of Levodopa. Levodopa's peak concentration in plasma decreased by 30% and appeared later when the standard Madopar was used after the main meal. Levodopa's absorption level decreased by 15%.
soluble form:
Levodopa's pharmacokinetics parameters after using Madopar in a healthy volunteer and Parkinson's patient similar to this group of people using standard Madopar, but the time of reaching peak concentration is shorter when using Madopar in tan.
There is less variation between individuals for the absorption parameters when the masopar -tinted Madopar is taken in the form of a mixture.
Controlled release:
Madopar HBS pharmacokinetics properties are different from the pharmacokinetics of the usual Madopar (tablets and capsules) and soluble.
The active ingredient is slowly released in the stomach.
Maximum concentration in plasma, 20-30% compared to the maximum concentration in plasma of conventional drugs, reaching 3 hours after drinking.
The plasma concentration curve shows that "the period of half of the value is longer (the time in which the concentration of the drug in plasma is equivalent or higher than the maximum concentration), this shows that the drug has controlled release properties as announced.
Madopar HBS's bioavailability is about 50-70% of the usual tablet form and is not affected by food. Levodopa's maximum plasma concentrations are not affected by food but achieved later (5 hours) after taking Madopar HBS after eating.
Distribution
Levodopa passes through the bloody barrier through the saturated transportation system. It does not bind to plasma proteins and the distribution volume is 57 liters. Levodopa's AUC in cerebrospinal fluid is 12% in plasma.
In contrast to Levodopa, Benserazide cannot penetrate through the brain barrier at the dose of treatment. The drug is mainly concentrated in the kidneys, lungs, small intestine and liver.
Metabolism
Levodopa is metabolized through two main paths (reduction of carboxyl and o - methylation) and two other small paths (transaminization and oxidation).
Aromatic amino acid decarboxylase transforms levodopa into dopamine.
The main metabolites of this metabolic line are homovanillic acid and dihydroxyphenylacetic acid. Men Catechol - O - Methyltransferase Methylation Levodopa into 3 - O - Methyldopa.
Main metabolites in plasma have a half -life of 15 hours, and it is accumulated in patients treated with Madopar.Levodopa's peripheral carboxy reduction is reduced when oral with Benserazide is reflected in the higher plasma concentration of Levodopa and 3 - O - Methyidopa and lower plasma concentrations of cathecholines (dopamine, noradrenaline) and phenolcarboxylic acid (homovanillic acid, dihydroxyylacetic acid).
Benserazide is hydroxyl turned into trihydroxybenzylhydrazine in the intestinal and liver mucosa. This metabolic is the main inhibitor of the decarboxylase amino enzyme.
Elimination
When there is a inhibition of Levodopa's carboxyl reduction process in the periphery, Levodopa's half -life is about 1.5 hours.
Sales time is longer (25%) in older patients (65 - 78 years old) suffering from Parkinson's disease (see pharmacokinetic section in special subjects).
Levodopa's clearance in plasma is about 430ml/min.
Benserazide is almost completely eliminated the metabolic process. The metabolites are mainly eliminated through the urine (64%) and a small part of the stool (24%).
Pharmacokinetics in special subjects
There is no pharmacokinetic data in patients with hyper urea or liver disease.
The effect of age of pharmacokinetics of levodopa
In patients with Parkinson's disease (65 - 78 years old) both the half -life and the AUC of Levodopa are higher in young patients (34 - 64 years old) about 25%. The statistical effect of age is insignificant and less important in the dose mode at any specified.
Before taking Madopar Levodopopa and Benserazide 250 Roche treats innocent Parkinson's disease (30 tablets)
How to use
Take oral use.
Medication method:
When using a normal Madopar in the form of capsules or Madopar HBS, the patient must always ensure swallowing capsules without the need for medicine.
Madopar of regular tablets can be broken for easy swallowing. Madopar tablets can be mixed in a quarter of water glass (about 25 - 50ml). The tablet disintegrates completely in the water, forming a white milk diffusion solution for a few minutes.
Because the solution settles quickly, stirring before drinking.
Madopar tablets should be taken for half an hour after preparing the solution.
Parkinson's disease:
Madopar treatment should be used slowly, moreover, the dose should be evaluated for each patient and adjusted to achieve the dose for optimal efficiency.
The following dose guidelines should only be considered as general instructions.
Starting treatment
In the early stages of Parkinson's disease, it should start treatment with a Madopar 62.5 "or 1/2 Madopar 125 ° tablets, three or four times a day.
Immediately after seeing a good tolerance with the initial treatment regimen, the dose should be gradually increased by the patient's response.
The optimal effect is usually achieved when Madopar's daily dose corresponds to 300 - 800mg Levodopa + 75 - 200mg Benserazide, divided into 3 or more.It takes a period of 4 to 6 weeks to achieve optimal effect. If you find it necessary to increase the dose 2 more daily, should increase by month.
Maintain treatment
Average maintenance dose is a Madopan 125 capsule or tablet, use 3 to 6 times daily.
The number of drugs for each individual (not less than three) and the daily use of drug use time must be adjusted for optimal efficiency.
Madopar HBS or soluble Madopar can be used to replace the usual formar for optimal efficiency.
Special dose guidelines
Dosage must be carefully adjusted in all patients (see the indication of treatment).
Patients who are using other Parkinson treatments can still use Madopar.
However, while the Madopar treatment is conducted and the treatment effect becomes clear, the dose of those drugs may decrease or slowly stop.
Madopar tablet tablets are especially suitable for patients with difficulty swallowing or in a situation where it needs a quick onset effect.
For example: Patients with loss of exercise in the early morning or afternoon, or patients with the phenomenon of delaying the time of 'turning' or prolonging the 'turning' time.
For patients who know there is a great oscillation for the treatment effect of the drug during the day of treatment (on -off phenomenon), it is advisable to use the drug in many times with smaller doses, or should use Madopar HBS.
When switching from normal Madopar to Madopar HBS should be done from this date to the next day starting with the dose in the morning.
Dosage and the number of times used for the day should start like the dose of the usual Madopar.
After two to three days, the dose must be increased by about 50%. Patients must be informed that their condition may be affected for a while.
Due to the pharmacological characteristics of Madopar HBS, the drug time has the effect of being delayed.
Clinical efficiency can be achieved faster by using Madopar HBS together with conventional Madopar or soluble Madopar.
This is really useful for the first dose in the morning, which should be taken a bit higher than the next dose of the day.
The dose for each individual using Madopar HBS must be done slowly and carefully, with at least two to three days between each dose change.
In patients with motionless at night, the positive effect has been reported when the final dose of the last to 250mg of Madopar HBS before bed.
Excessive response with Madopar HBS (motor disorder) can be controlled by increasing the distance between use rather than by reducing the dosage alone.
In case of poor response to Madopar HBS, it is advisable to return to previous treatment with standard Madopar or dispersed Madopar.
Patients should be carefully monitored about unwanted mental side effects.
What to do when overdose?
Symptoms and signs
Symptoms and overdose of nature are similar to the side effects of Madopar at the treatment but the severity is more serious.
Overdose can lead to:
Treatment
Monitor the patient's survival signs and establish supportive measures specified according to the patient's clinical condition.
In special cases may need symptomatic treatment as consequences on the cardiovascular system (for example, anti -arrhythmia) or consequences on the central nervous system (for example, respiratory stimulants, sedatives).
In addition, for slow release, it is necessary to prevent additional absorption later by appropriate measures.
What to do when forgetting the dose?
If you forget a dose, drink as soon as possible. However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Do not drink twice as prescribed.
Side Effects
Notify the doctor any side effects related to the medication.
Unwanted effects have been reported after using Levopoda - Benserazide (unknown frequency, not estimated from existing data):
Classification by the following frequency:
Very popular:> 1/10;
Popular:> 1/100 to
Uncommon:> 1/1,000 to
Rare: (21/10,000 to
Very rare: (
Unknown (not estimated from existing data).
mental disorders
kidney and urinary tract disorders
Gambling pathology, increasing libido, crazy.
neurological disorders
Depression can be part of the common clinical disease in patients with Parkinson's patient and unpredictable vacuum syndrome and can occur in patients treated with Madopar. Mental disorders occur commonly in Parkinson's patient, including patients treated with Levodopa, including anxiety, agitation, insomnia, depression, illusion, hallucinations, loss of time.
The later stage of treatment, movement disorders (dance or dance) may occur. This condition may be lost or tolerated after the dose reduction. There may be oscillations in response to long -term treatment.
This oscillation includes an inert, heavy stage at the end of the dose and the phenomenon of "on - off".
These phenomena are lost or can be used when adjusting the dose or splitting the dose many times more.
Then can find a way to increase the dose again to increase the effectiveness of treatment. Levodopa - Benserazide is related to drowsiness and is rarely related to excessive sleepiness during the day or there are sudden sleep stages.
Gastrointestinal disorders
Unwanted effects on the gastrointestinal tract can occur mainly at the beginning of the treatment, mostly can be controlled by using Madopar with food or liquid or increasing the dose slowly.
Gastrointestinal bleeding has been reported when treated with Levodopa. Some cases of loss or change of taste.
vascular disorders
Pose disorder is mostly improved after decreased Madopar.
Disorders of musculoskeletal and connective tissue.
Peaceful vacuum syndrome
The severe progression of the disease (the time of symptoms from the evening/night to the beginning of the afternoon and evening before taking the next night dose) is the most common adverse reaction when long -term treatment with dopaminergic drugs.
Flush and sweat has been reported when using Levodopa.
Testing
Testing: Urine may be changed in color, usually red and then dark to settle. This change is due to metabolic substances and no need to worry.
other types of body or tissue fluid may also be discolored or dyed, including saliva, tongue, teeth or oral mucosa.
Warnings
Contraindicated
Madopar is not used for patients who are clearly hypersensitive to Levodopa or Benserazide or any ingredients of the drug.
Madopar is not coordinated with non -selective inhibitors Monoamine Oxidase (MA). However, there is no indications if combined with selective inhibitors on Mao -B yeast as Selegiline or Rasagiline or selective inhibitor on Mao - A yeast as Moclobemide. The combination of Mao - A and Mao inhibitors inhibitors is similar to the inhibition of non -selective Mao yeast, so it should not be used simultaneously with this combination with Madopar (see interactive items with other drugs and drug interactions).
Madopar is not used for patients with hormonal disease, liver or kidney disease (except for patients with dialysis), cardiovascular disorders, mental illnesses with psychotic manifestations, or closed angle glaucoma.
Madopar is not used for patients under 25 years old (because the development of the skeletal system must be completed).
Madopar is not used for pregnant women or pregnant women but does not apply adequate contraception (see the section of pregnant women and nursing women). Must stop the drug immediately if pregnant during the time of using Madopar (according to the doctor's instructions for the prescription).
There is a doubt that Levodopa can activate malignant color.
Therefore, Madopar should not be used for patients with a history or a risk of malignant pigmentation. Madopar should not be used simultaneously with neuroleptics that have anti -vomiting effects (see interactive items with other drugs and interactive forms).
Precautions when taking drugs
General
When other drugs must be used simultaneously with Madopar, the patient must be carefully monitored with abnormal side effects or increasing the impact of the drug.
There may be hypersensitivity reactions in sensitive patients.
Need to regularly measure glaucoma for patients with open-angle glaucoma, because in theory, Levodopa can increase glaucoma.
Caution to use Madopar for patients with a history of dynamic - coronary disease, arrhythmia or heart failure.
Heart function should be monitored and specially cared for in these patients during the beginning of treatment and periodically during treatment.
closely monitor patients with risk factors (such as high age, simultaneous use with anti -hypertension drugs or drugs that are likely to cause other standing posture hypotension) or a history of standing posture, especially the first stage of treatment or when increasing the dose.
Madopar has been reported to reduce the number of blood cells (such as hemolytic anemia, thrombocytopenia and leukopenia). A few cases of grain leukemia and reducing all the blood cells have been reported, in which Madopar is not confirmed nor can not completely exclude. Therefore, periodically checking blood counts should be conducted during treatment.
Depression can be part of clinical disease in Parkinson patients and uneasy vacuum syndrome, and can also appear in patients being treated with Madopar.
All patients should be carefully monitored with mental and depression changes whether or not to commit suicide.
If the patient is using Levodopa, the body anesthesia is needed, the dosage should continue to reach as close to the surgery date as possible, except in the case of anesthesia with Halothane.
When anesthesia with Halothane, Madopar should be stopped before surgery intervention 12 - 48 hours because of the vibration of blood pressure and/or arrhythmia in patients using Madopar. Madopar may be used after surgery; Need to increase the dose gradually until the dose is applied before surgery.
Do not stop Madopar suddenly because it can cause sedative syndrome similar to the properties (high fever and muscle spasm, mental changes and increased creatinine phosphokinase in serum, some other signs in serious cases may include myoglobinuria, muscle pattern and acute kidney failure), this syndrome can be life -threatening.
If such a collection of symptoms appears, the patient needs to be closely monitored, if necessary, must be hospitalized and treat symptoms quickly and properly.
This treatment includes re -treatment with Madopar after fully evaluated.
Levodopa is related to a chicken sleep condition or suddenly sleeping space.
Sleeping suddenly during daily activity, some cases of unknown or without warning signs, have been reported though very dangerous.
Patients must be informed about this and be advised to note when driving or operating machinery while being treated with Levodopa.
Patients who have been sleeping or sleeping intervals have to stop driving or operating machinery.
Moreover, it is possible to consider reducing the dose or stopping treatment (see item 2.4.3 Driving capabilities or using machines).
Pulse control disorders
Patients should be monitored periodically to detect impulse control disorders.
Patients and patients care for patients should be told the symptoms of the act of pulse control disorders including pathological gambling, increased libido, lewd, uncontrolled shopping, uncontrolled and controlled eating tea that may occur for patients being treated with dopamine and/or other dopaminergic drugs containing Levodopa, including Madopar.
Review the treatment if these symptoms appear.
Malignant pigment
Epidemic research has shown that Parkison's patient is at higher risk of developing pigment tumors (about 26 times). It is not clear whether the increased risk is recorded in Parkinson's treatment.
Therefore, patients and prescriptions are recommended regularly monitoring to detect pigment tumors when using Madopar in any indications. Ideally, periodic skin examination should be done by an appropriate professional (such as a dermatologist).
Dopaminergic medicine
Pathological cards, enhancement of libido and excessive sexual activity have been reported in some patients treated with Dopamine Agonist in Parkinson's disease.
There is no connection set between Madopar and the above events, nor the dopamine bronze medicine. However, it should be noted because Madopar is a dopaminergic group.
The ability to drive and operate machinery
Patients treated with levodopa and have symptoms of sleeping or sudden sleep intervals must be notified so as not to drive or participate in activities where the ability to reduce their vigilance can make them or others suffer from serious damage or death (for example, operating machinery) until the symptoms of sleep or sleep are relieved Determination.
Pregnancy and lactation
Pregnancy
Madopar is contraindicated in pregnant women and women who are likely to become pregnant but do not apply adequate contraception (see the control item, the properties of teratogenic and other characteristics).
Breastfeeding period
Because it is unknown whether Benserazide is excreted in milk or not, mothers need Madopar treatment should not breastfeed because they do not exclude the possibility of bone deformation in children.
Other special subjects (elderly, children, allergies)
Patients with renal failure
Both Levodopa and Benserazide are broadly metabolized and less than 10% of Levodopa is excreted in the form of unchanged through the kidney. Therefore, there is no need to reduce the dose in cases where the renal function is mild or medium.
There is no levodopa pharmacokinetic data in patients with impaired renal function. Madopar well tolerated in patients with hyper urea is conducting dialysis.
Patients with liver failure
Levodopa is metabolized mainly by Aromatic Amino Acid Decarboxylase enzyme, which is also present in the gastrointestinal tract, kidney and liver heart.
There is no levodopa pharmacokinetic data in patients with liver failure.
Medicinal interaction
pharmacokinetic interaction
Concomitance of anti -cholinergic trahexyphenidyl with common formar that reduces the rate of levodopa absorption but does not reduce the absorption level. Simultaneous use of Trihexyphenidyl with Madopar HBS does not affect the pharmacokinetics of Levodopa.
Simultaneous use of acid resistance and Madopar HBS reduces the absorption level of Levodopa 32%. Iron sulphate reduces the maximum concentration in plasma and AUC of Levodopa by 30-50%.
Observed people see clinical pharmacokinetic changes during treatment with iron sulphate in some patients, not all. Metoclopramide increases the speed of Levodopa's absorption.
There is no pharmacokinetic interaction between Levodopa and the following active ingredients: Bromocriptin, Amantadine, Selegiline and Domperidone.
Pharmacological interaction
Sedative, opioids and hypertension drugs with reserpine both inhibit the effects of Madopar.
If Madopar is used for patients who are using non -recovery and non -selective enzyme inhibitors, it is necessary to stop this enamel inhibitors for at least 2 weeks before starting Madopar treatment. If not, side effects such as hypertension may occur (see the contraindication section).
Selective inhibitors on Mao - B, such as Selegiline and Rasagiline and selective inhibitors on Mao - A such as Moclobemide, can be indicated for patients being treated with Madopar.
As recommended, the Levodopa dose should be adjusted according to each patient based on efficiency and tolerance.
The combination of Mao -A and Mao inhibitors inhibitors is equivalent to the inhibitor of non -selective Mao inhibitors, so this combination is not used with Madopar (see the contraindication section).
Madopar is not used with sympathetic medications (such as epinephrin, norepinephrine , isoproterenol or amphetamine are sensitive nervous system stimulants) because Levodopa can increase the effect of these drugs.
If it is necessary to be used, close to the cardiovascular system and should reduce the dose of sympathetic stimulants.
Concomitance of anti -psychotic drugs with Dopamine receptor inhibitors, especially D2 receptor antagonists can fight against Parkinson's anti -Parkodopa - Benserazid.
.Levodopa can reduce the anti -psychotic effect of these drugs. Should be cautious when using these drugs.
Other interactions
It is possible to coordinate with other drugs such as anti -cholinergic, amantadine, Selegiline, Bromocriptine and dopamine, but both desired and unwanted effects can increase.
So it is necessary to reduce the dose of Madopar or other drugs. When starting treatment support with comt inhibitors, Madopar is required.
Do not stop the cholinergic antiviral drug when starting to use Madopar, because Levodopa needs some time to promote the effect. Levodopa can affect the results of some tests on catecholamine, creatinine, tumor acid and glucose. Urine test results can be fake positive for ceton.
Test Coom can give a fake positive result if done in patients using Madopar.
The effect of the drug is reduced when the drug is used in a protein -rich meal.
Body anesthesia with Halothane: Madopar should be discontinued 12 - 48 hours before the surgery requires a systemic anesthesia with Halothane because of blood pressure and arrhythmia may occur.
In case of body anesthesia with other anesthesia viewing general (warning and caution).
Storage
You should store at room temperature, avoid moisture and avoid light. No storage in the bathroom or in the freezer.
You should remember that each drug may have different storage methods. Therefore, you should read carefully storage instructions on the packaging or ask the pharmacist.
Keep pills out of reach of children and pets.
Expiry date: 48 months from the date of production.
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