Nakom pills 250mg 25mg N100
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Active ingredients
Levodopa + Carbidopa
Release form
Pills
Composition
1 tab. contains levodopa 250 mg, carbidopa 25 mg. Excipients: pregelatinized starch - 45 mg; corn starch - 6.5 mg; blue dye (indigotin E132) - 0, -72 mg; magnesium stearate - 4.2 mg; MCC - up to 380 mg
Pharmacological effect
Levodopa relieves the symptoms of Parkinson's disease by increasing the dopamine content in the brain. Carbidopa, which does not penetrate the BBB, interferes with extracerebral decarboxylation of levodopa, thereby increasing its amount, which enters the brain and converts it into dopamine. which are about 80% lower than those required in the case of the use of one levodopa. The effect of the drug appears during the first days from the beginning of the reception, sometimes yes - after taking the first dose. The maximum effect is achieved within 7 days
Pharmacokinetics
Levodopa. Levodopa is rapidly absorbed from the gastrointestinal tract and is actively metabolized. Despite the fact that more than 30 different metabolites are formed, mainly levodopa is converted to dopamine, epinephrine, norepinephrine. After oral administration by patients with Parkinson's disease, a single dose of levodopa Tmax is 1.5-2 h and is maintained at a therapeutic level for 4-6 h. Metabolites are rapidly excreted in the urine: within 1 h about 1/3 of the dose is excreted. The T1 / 2 of levodopa in the blood plasma is about 50 minutes. When combined with carbidopa and levodopa T1 / 2, levodopa increases to approximately 1.5 hours. Carbidopa. After oral administration of a single dose of carbidopa, Tmax ranges from 1.5 to 5 hours in patients with Parkinson's disease. Metabolized in the liver. Excretion in the urine of the unchanged drug is mostly completed within 7 hours and is 35%. Among the metabolites excreted in the urine, the main are alpha-methyl-3-methoxy-4-hydroxyphenylpropionic acid, as well as alpha-methyl-3,4-dihydroxyphenylpropionic acid. They constitute about 14 and 10% of excreted metabolites, respectively. In smaller quantities, two other metabolites are found.One of them was identified as 3,4-dihydroxyphenyl-acetone, the other - previously as N-methyl-carbidopa. The content of each of these substances is not more than 5% of the total number of metabolites. Unchanged carbidopa is also found in the urine. Conjugates have not been identified. The effect of carbidopa on the metabolism of levodopa. Carbidopa increases the concentration of levodopa in the blood plasma. In the case of previous carbidopa, the concentration of levodopa in plasma increases about 5 times, and the time to maintain therapeutic plasma concentrations increases from 4 to 8 hours. Simultaneous intake of carbidopa and levodopa gave similar results. When a single dose of levodopa was taken by patients with Parkinson's disease, who previously took carbidopa, T1 / 2 for levodopa increases from 3 to 15 h. The concentration of levodopa is increased by at least 3 times carbidopa. The concentration of dopamine and homovanillic acid in the blood plasma and urine decreases with the preliminary intake of carbidopa
Indications
Treatment of Parkinson's Disease and Parkinson's Syndrome
Contraindications
Angle-closure glaucoma; - established or suspected melanoma; - skin diseases of unknown etiology; - simultaneous use with non-selective MAO inhibitors (taking MAO inhibitors should be stopped 2 weeks before starting to receive levodopa); - hypersensitivity to the drug components. severe diseases of the cardiovascular system, including with myocardial infarction with heart rhythm disorders (in history), heart failure, severe respiratory system diseases, including bronchial asthma, convulsive seizures (in history), including epileptic, erosive and ulcerative lesions of the gastrointestinal tract (due to the possibility of bleeding from the upper GI tract ), decompensated diseases of the endocrine system, including diabetes mellitus, severe renal failure, severe liver failure, open-angle glaucoma
Precautionary measures
With caution (requires more careful selection of doses and monitoring the safety of treatment) should be prescribed the drug for myocardial infarction with a rhythm disturbance (in history),heart failure and other serious diseases of the cardiovascular system; in severe lung diseases, including bronchial asthma; epileptic and other convulsive seizures (in history); erosive and ulcerative lesions of the gastrointestinal tract (due to the possibility of bleeding from the upper gastrointestinal tract), diabetes mellitus and other decompensated endocrine diseases, severe renal and / or liver failure, open-angle glaucoma
Use during pregnancy and lactation
The effect of Nakoma on the course of pregnancy in women is unknown. In experimental studies revealed that the combination of levodopa and carbidopa causes visceral and skeletal changes in animals. Therefore, the use of the drug is possible only when the expected benefit of therapy for the mother outweighs the potential risk to the fetus. It is not known whether levodopa and carbidopa are excreted in breast milk. There is one report on the excretion of levodopa with breast milk in a nursing mother with Parkinson's disease. Therefore, due to the possible serious adverse effects of the drug on the newborn and taking into account the importance of therapy for the mother, if necessary, use of the drug during lactation should decide whether to stop breastfeeding or cancel the drug Nacom
Dosage and administration
The optimal daily dose is determined by careful individual selection. The form of the tablet allows you to divide it into two parts with minimal effort. During the treatment process, it may be necessary to adjust both the individually selected dose and the frequency of taking the drug. Studies have shown that peripheral dopa decarboxylase is saturated with carbidopa when it is taken at a dose of about 70-100 mg / day. Nausea and vomiting are possible in patients receiving carbidopa at a lower dose. If Nakoma is prescribed, standard drugs for the treatment of parkinsonism, except for those containing one levodopa, can be continued, and their dose should be adjusted anew. according to the indications and patient response to treatment. The initial dose of Nakom is 1/2 tab. 1-2 times / day.However, such a dose may not provide the optimal amount of carbidopa the patient will need. Therefore, if necessary, add 1/2 tab. Nakoma every day or every other day to achieve the optimal effect. The therapeutic effect is observed on the first day, and sometimes after taking the first dose. The full effect of the drug is achieved within 7 days. When switching from levodopa preparations, the latter should be stopped for at least 12 hours before the start of treatment with Nacom (24 hours if you use levodopa with prolonged action). The daily dose of Nacom should provide about 20% of the previous daily dose of levodopa. For patients who took more than 1.5 g of levodopa, the initial dose of Nakoma is 1 tab. 3-4 times / day. With maintenance therapy, if necessary, the dose of Nakoma can be increased by 1 / 2-1 tab. every day or every other day before reaching the maximum dose - 8 pills / day. The experience of taking carbidopa in a dose of more than 200 mg / day is limited. The maximum recommended dose of Nakom is 8 pills / day (200 mg of carbidopa and 2 g of levodopa). This is about 3 mg of carbidopa and 30 mg of levodopa per 1 kg of body weight (with a patient's body weight of 70 kg).
Side effects
The most common are dyskinesias, including involuntary movements (including choreiform, dystonic), as well as nausea. Early signs that may lead to the decision to discontinue the drug are muscle twitching and blepharospasm. From the CNS and peripheral nervous system: ZNS, episodes of bradykinesia (on-off syndrome), dizziness, drowsiness, paresthesia, episodes of psychotic states, including illusions, hallucinations and paranoid thinking, depression with the development of suicidal intentions or without them, dementia, sleep disorders, agitation, confusion, increased libido. In rare cases, convulsions, but a causal connection with taking Nakom has not been established. On the digestive system: anorexia, vomiting, bleeding from the gastrointestinal tract, exacerbation of duodenal ulcer, diarrhea, browning are possible saliva. On the whole body: possible fainting, chest pain. Since the cardiovascular system: arrhythmias and / or heartbeat, orthostatic effects (includingepisodes of increase or decrease in blood pressure), phlebitis. From the hematopoietic system: leukopenia, anemia (including hemolytic), thrombocytopenia, agranulocytosis. From the respiratory system: possible dyspnea. Dermatological reactions: alopecia, rash, darkening of the sweat glands . From the urogenital system: darkening of the urine. Allergic reactions: angioedema, urticaria, pruritus, Shenlein-Genoch disease. Other Side effects that may occur as a result of taking levodopa: From the digestive system we: dyspepsia, dry mouth, bitterness in the mouth, sialorea, dysphagia, bruxism, attacks of hiccups, pain and discomfort in the stomach, constipation, flatulence, burning sensation of the tongue. On the side of metabolism: weight loss or increase, edema. CNS: weakness, fainting, fatigue, headache, asthenia, decreased mental activity, disorientation, ataxia, numbness, increased hand tremors, muscle cramps, trismism, activation of latent Bernard-Horner syndrome, insomnia, anxiety, euphoria, psychomotor agitation , n gait stability. On the part of the sense organs: diplopia, blurred vision, dilated pupils, ocular crises. On the urogenital system: urinary retention, urinary incontinence, priapism. Others: hoarseness, indisposition, flushing of blood to the skin of the face, neck and chest, dyspnea, malignant melanoma. From the laboratory indicators: increased activity of alkaline phosphatase, AST, ALT, LDH, increased bilirubin, urea nitrogen in plasma, increased serum creatinine, hyperuricemia, positive test Ku BSA, decrease in hemoglobin and hematocrit, hyperglycemia, leukocytosis, bacteriuria, eritrotsituriya.Preparaty containing carbidopa and levodopa, can cause false positive reactions to ketone bodies in urine, for the determination of ketonuria if used test strips. This reaction will not change after boiling urine samples. False negative results can be obtained using the glucose oxidase method of determining glucosuria.
Overdose
In case of overdose Nakoma increases the severity of side effects. Treatment: it is necessary to ensure careful monitoring and electrocardiographic monitoring of the patient in order to identify possible arrhythmias, if necessary, should be carried out adequate antiarrhythmic therapy.It is necessary to take into account the possibility that the patient took other medications along with Nacom.
Interaction with other drugs
Precautions should be taken if the drugs listed below are prescribed with Nakom. Antihypertensive drugs. In patients receiving some antihypertensive drugs, the addition of Nakoma caused orthostatic symptomatic hypotension. Therefore, it may be necessary to adjust the dose of the antihypertensive drug at the beginning of Nacoma treatment. Anti-depressants. With simultaneous use of levodopa with MAO inhibitors (with the exception of MAO-B inhibitors), circulatory disorders are possible (the intake of MAO inhibitors should be discontinued within 2 weeks). This is due to the accumulation of dopamine and norepinephrine under the influence of levodopa, the inactivation of which is inhibited by MAO inhibitors. As a result, the likelihood of developing excitement, increasing blood pressure, tachycardia, facial flushing and dizziness is high. There were separate reports of adverse reactions, including an increase in blood pressure and dyskinesia in the case of the combined use of tricyclic antidepressants in combination with Nacom. Preparations of iron. The bioavailability of carbidopa and / or levodopa decreases with the simultaneous use of iron sulfate or iron gluconate by the patient. Other preparations. With simultaneous use of levodopa with beta-adrenergic stimulants, ditilin and inhalation anesthesia agents, an increased risk of developing heart rhythm disturbances is possible. D2-receptor D2 receptor antagonists (for example, phenothiazines, butyrophenones and risperidone), as well as isoniazid, can reduce the therapeutic effect of levodoins. There are reports of blocking the positive therapeutic effects of levodopa in Parkinson's disease as a result of taking phenytoin and papaverine. Patients taking these medications at the same time as Nacom require careful monitoring to detect a decrease in the therapeutic effect in a timely manner. Lithium preparations increase the risk of dyskinesias and hallucinations; methyldopa enhances side effects, simultaneous use of tubocurarine increases the risk of arterial hypotension. Levodopa absorption may be impaired in some patients,are on a high-protein diet because levodopa competes with certain amino acids. Carbidopa interferes with the action of pyridoxine hydrochloride (vitamin B6), which accelerates the metabolism of levodopa to dopamine in peripheral tissues
special instructions
It should be used with caution in patients with severe hepatic impairment. It should be used with caution in patients with severe renal failure