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Carbidopa and Levodopa Teva
Last reviewed: 23.04.2024
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Carbidopa and levodopa-teva is a complex anti-parkinsonian drug, which contains a dopamine metabolic precursor (levodopa), as well as a substance that slows down peripheral dopa-decarboxylase (carbidopa).
Signs of trembling paralysis are believed to be caused by dopamine deficiency. With normal dopamine levels, it acts as a neurotransmitter and is produced by some brain cells that control muscle activity. Therefore, it is believed that motor disorders occur due to a lack of dopamine inside the body.
Indications Carbidopa and Levodopa Teva
It is used during trembling paralysis.
Release form
The release of the drug substance is made in tablets - 10 pieces inside a blister pack. In a pack - 5 or 10 such packages.
Pharmacodynamics
The anti-parkinsonian activity of levodopa is associated with its transformation into dopamine (due to decarboxylation occurring directly inside the central nervous system), as a result of which dopamine deficiency within the nerve cells is replenished.
Carbidopa can not overcome the BBB; prevents the processes of extracerebral decarboxylation of levodopa, because of which it increases its entry into the brain with subsequent transformation into dopamine inside the central nervous system. These processes cause the weakening of the signs of trembling paralysis in a large number of patients.
Pharmacokinetics
Both active components of drugs are well absorbed; Plasma Cmax values are noted after 1-3 hours. The term half-life of levodopa (with carbidopa exposure) is approximately 2 hours. Under the influence of carbidopa, plasma excretion of levodopa is reduced by 50%. When exposed to carbidopa, levodopa is usually transformed into amino acids (a small part is converted into catecholamine derivatives). All the metabolic components of levodopa with carbidopa are excreted in the urine.
Dosing and administration
Selection of the optimal daily dosage of the drug is implemented through careful titration of each patient individually.
Taking into account the intensity of the pathology, it may take about six months to obtain an optimal medication effect.
Persons who have not used levodopa.
For people starting the use of drugs, you must first take half a table 1-2 times a day. If necessary, add another half a table daily or with daily interruptions until the required amount of carbidopa is obtained.
The drug effect develops immediately on the day of intake (sometimes even after the 1st portion). It reaches full effectiveness after 7 days (using only levodopa, it takes weeks or months).
People using levodopa.
The introduction of levodopa must be canceled at least 12 hours (or 24 hours if drugs were used with a slow release type) before starting treatment with the medication. You can take levodopa in the morning, and then do not use it at night. A serving should be approximately 20% of the previous daily dosage of levodopa.
Initial portion.
Persons consuming less than 1.5 g of levodopa per day must first use 0.075-0.1 g of carbidopa and 0.3-0.4 g of levodopa (use medication with a dosage of 1k4 carbidopa / levodopa), 3 -4 use.
For people who consume more than 1.5 g of levodopa per day, first take the first pill of the medication 3-4 times per day.
The supporting portion.
It is necessary to use the medicine taking into account the personal characteristics of the person, changing the portion gradually (taking into account the medication effect).
If it is necessary to take a larger amount of levodopa, the dosage is allowed to be increased to the 1st tablet 3-4 times a day. If needed, the portion can be increased by 0.5-1-well pill per day (at the same time, no more than 8 tablets can be taken per day).
In cases when during the transfer of a patient from Levodopa to Carbidopa and Levodopa-Teva, the use of other agents that slow down decarboxylase is carried out, the administration of drugs must be stopped at least 12 hours before using the medication. Drug administration should be started with a portion similar to the amount of levodopa and a substance that slows down decarboxylase, in previous medications.
Persons using other anti-parkinsonic substances.
The combination of drugs and MAOI-B can enhance the drug activity of the first with controlled manifestations of dyskinesia or akinesia.
It is allowed to continue taking other standard anti-parkinsonian substances other than levodopa, with the introduction of carbidopa with levodopa, although the injected portions may require adjustment.
[7]
Use Carbidopa and Levodopa Teva during pregnancy
There is no information on the effects of carbidopa and levodopa-teva on the course of pregnancy, but levodopa, as well as its combination with carbidopa, led to the appearance of anomalies in the development of the skeleton with internal organs during animal tests. Do not use the drug during breastfeeding and pregnancy. Women of reproductive age who use drugs should use reliable contraception.
There is no information as to whether the drug is excreted in breast milk. To prevent the occurrence of negative symptoms in infants, it is necessary to make a decision about the cancellation of drugs or the termination of breastfeeding (taking into account the need for its reception for a woman).
Contraindications
Among the contraindications:
- strong sensitivity associated with the active elements of the drug or its other ingredients;
- glaucoma;
- failure of the heart to work hard;
- arrhythmia of the heart, having a severe character;
- severe psychosis;
- combined use with selective MAOI-A, as well as non-selective MAOI (except for small portions of some MAOI-B). These medicines need to be canceled at least 14 days before starting to use the drug;
- suspicious, as well as undiagnosed epidermal diseases, or melanoma, available in history.
The drug is not prescribed to persons who can not take sympathomimetics.
Side effects Carbidopa and Levodopa Teva
Negative symptoms that occur when taking drugs are usually associated with the neuropharmacological activity of dopamine. Basically, they pass or weaken after reducing the portion.
Often, when using the medication, dyskinesia appears (dystonic, choreiform, and other movements that have an involuntary nature). If blepharospasms and muscle cramps occur, reduce dosage.
Other serious side effects include mental changes (psychosis with paranoid thoughts, as well as depression with suicidal tendencies or not) and dementia. There are reports of the development of hypersexuality or the excitement that has a pathological character, and besides this, of increased libido (especially when using large portions of the medicine). Such symptoms disappear after dosage reduction or drug discontinuation.
Among the negative manifestations associated with levodopa and its combinations:
- lymph and hematopoietic lesions: anemia (also hemolytic), platelet or leukopenia and agranulocytosis;
- immune disorders: manifestations of intolerance, including urticaria and angioedema;
- disorders of the function of the cardiovascular system: fainting, palpitation, phlebitis, heartbeat rhythm disorders, increased blood pressure values, tendency to loss of consciousness and orthostatic signs, including a decrease in blood pressure indicators
- problems with the work of NA: ataxia, chorea, bradykinesia or dyskinesia, dizziness and the phenomenon of the so-called "on-off" (sometimes occurs several months later or years after the start of therapy with the introduction of levodopa; most likely, develops due to the progression of the disease (with such violations may require changing the size of portions and the intervals between their injections)). In addition, trismism, dystonia, increased tremor, affecting the hands, muscle spasms, motor and extrapyramidal manifestations, paresthesias, muscular twitching, CSN, loss of consciousness and a tendency to faint, and also gait disorder, convulsions and activation of latent oculosympathetic syndrome;
- mental disorders: mania, depression, confusion, exhaustion, nightmares and suicide attempts. In addition, insomnia, dizziness, dementia, delirium, euphoria, great anxiety and hallucinations. Also on the list are changes in mental state (this includes temporary psychosis and paranoid thinking), agitation, fear, convulsions, thinking or walking disorder, headaches, disorientation and torpor, as well as sudden severe sleepiness;
- lesions associated with the gastrointestinal tract: dysphagia, diarrhea, dry oral mucous membranes, dyspepsia, hypersalivation, bruxism and nausea, as well as the appearance of a bitter taste, hiccups, vomiting and bloating, obstruction, pain in the abdominal zone, glossary, pain, having gastrointestinal nature, bleeding inside the digestive tract, burning of the tongue, dark color of saliva and an ulcer affecting the duodenum;
- problems with metabolic processes: swelling, weight gain or anorexia;
- disorders associated with the subcutaneous layers and the epidermis: hyperhidrosis, alopecia, pruritus, activation of melanoma of a malignant nature, hyperemia, rash, dark sweat and rheumatic purpura;
- problems with the work of the respiratory system: hoarse voice, dyspnea, pain in the sternum and respiratory distress;
- lesions of the musculoskeletal structure: muscular spasms;
- impaired urinary function: incontinence or urinary retention, priapism and dark urine;
- visual disorders: diplopia, visual impairment, eye cramps, mydriasis, blepharospasm, oculomotor crisis. Blepharospasm may be an early sign of poisoning;
- changes in test results: increased values of liver activity (ALT, along with alkaline phosphatase and AST, bilirubin, creatinine, LDH, uric acid and blood urea nitrogen), a positive response from Coombs' test, an increase in serum sugar levels, a decrease in hematocrit with hemoglobin, bacteriuria and leukocytosis with hematuria;
- other: fatigue, general feeling of weakness, a sharp exacerbation of existing diseases, deterioration of health, hyperemia, flushing of blood in the area of the skin of the face and melanoma, which is malignant;
- impulsive decision disorders: overeating and impulsive need for making purchases when dopamine agonists or other drugs containing dopamine are injected (among them, and levodopa with carbidopa).
[6]
Overdose
Among the early manifestations of intoxication: having an involuntary form of movement, muscle twitching, heart rhythm disorder, an increase in blood pressure, blepharospasm, having a tonic form, loss of appetite, and with it an increase in heart rate, insomnia, anxious form of arousal, confusion and anxiety.
Immediate gastric lavage is required along with induction of vomiting.
Symptomatic actions: infusions are carefully applied; must take into account the degree of patency of the respiratory tract. In the case of arrhythmias, therapy is performed with observation on an ECG. No data regarding the use of dialysis in case of poisoning. Using pyridoxine will be ineffective.
Interactions with other drugs
Caution is required when used with the following medications.
Antihypertensive drugs.
In individuals who used some antihypertensive drugs, the use of combinations of levodopa and a means of slowing down the action of decarboxylase, led to the appearance of symptomatic orthostatic collapse. Because of this, at the initial stage of therapy, it is necessary to adjust the dosage of the hypotensive substance.
Antidepressants.
There are separate reports regarding the occurrence of negative symptoms (among them dyskinesia and an increase in blood pressure) associated with the combination of drugs and tricyclics.
The drug is allowed to use only with selective IMAO-B, in the recommended portions (for example, with selegilinom).
Anesthetics.
When administered together with anesthetics, arrhythmia may appear.
Cholinolytic drugs.
They can demonstrate synergy with levodopa while tremor is weakened, therefore this feature is often used to increase medication influence. But it must be borne in mind that such a combination may lead to an aggravation of movements that have an uncontrollable character.
Large portions of these substances can weaken the positive effect of levodopa, because it reduces the rate of its absorption, thereby increasing intragastric metabolic processes of drugs.
The remaining medicines.
Benzodiazepines, phenytoin with phenothiazines, butyrophenones, papaverine and isoniazid can weaken the medicinal activity of levodopa.
Levodopa exchange processes are enhanced with the introduction of anticonvulsants.
Because Levodopa competes with individual amino acids, in individuals who follow a high-protein diet, it is possible that the absorption of the drug is reduced.
The use of carbidopa prevents the strengthening of metabolic processes with the transformation of levodopa into dopamine, which occur under the influence of pyridoxine. The drug is allowed to be prescribed to people with parkinsonism who use substances containing pyridoxine hydrochloride.
Introduction in combination with selegilin can cause severe orthostatic collapse.
Fe medicines can inhibit the absorption of levodopa.
Sympathomimetics potentiate the negative symptoms of levodopa associated with cardiovascular disease.
Amantadine and dopamine antagonists can be combined with medication. When sharing them, dosage adjustment may be necessary.
Plasma levodopa values increase when using metoclopramide.
Introduction together with elements that slow catecholomethyltransferase (enacapapone with tolcapone) may increase the level of bioavailability of levodopa.
Combination with other anti-parkinsonic substances, which do not contain levodopa, is allowed.
[10]
Shelf life
Carbidopa and levodopa-teva can be used within a 36-month term from the time a drug is sold.
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Attention!
To simplify the perception of information, this instruction for use of the drug "Carbidopa and Levodopa Teva" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.