On whom

Nakom is a medicine with dopaminergic and antiparkinsonian action.

[1], [2], [3]

Indications of the nakoma

It is shown with trembling paralysis, as well as Parkinson's syndrome.

[4]

Release form

Produced in tablets, 10 pieces inside the first blister. One package contains 10 blister plates.

Pharmacodynamics

Levodopa can reduce the manifestation of trembling paralysis by increasing dopamine levels within the brain. Not passing through GEB carbidopa prevents the process of extracerebral decarboxylation of the substance of levodopa, due to which the amount of this element penetrating into the brain increases and turns into a component of dopamine.

The drug has a powerful drug effect that exceeds the effectiveness of levodopa. It helps for a long time to maintain the drug plasma concentration of this element at dosages that are much lower than those used exclusively for levodopa (approximately 80%).

The effect of the drug on the body begins already on the first day after the start of the course (in some cases - after the use of the first dose). The peak of its effectiveness is reached after 1 week.

Pharmacokinetics

Absorption of levodopa from the gastrointestinal tract occurs quickly enough, after which an active metabolism of this substance is carried out. Although as a result of this process 30+ various degradation products are formed, often levodopa is converted into epinephrine with dopamine and norepinephrine.

With the internal use of drugs in a single dose in patients with tremor paralysis, the peak value occurs 1.5-2 hours later, and the drug-effective level of the substance is held for about 4-6 hours. Decay products are rapidly excreted together with urine: in about 2 hours, about a third of the entire dose is excreted.

The half-life of levodopa within the plasma is approximately 50 minutes. In the case of combined use of carbidopa with levodopa, the half-life of the latter is prolonged to about 1.5 hours.

With oral use of a single dose of carbidopa, the peak time is 1.5-5 hours in people with tremor paralysis. The metabolism of the substance is carried out in the liver.

Unchanged substance is excreted together by urine. Usually this process ends after 7 hours and equals 35%.

The main decay products that are excreted in the urine are α-methyl-tri-methoxy-4-hydroxyphenyl propionic acid, and in addition α-methyl-3,4-dihydroxyphenyl propionic acid. These substances account for approximately 14%, as well as 10% (respectively) of the deduced decay products. Lower concentrations are represented by two more decay products, one of which is 3,4-dihydroxyphenyl-acetone, and the other (according to preliminary data) is an element of N-methyl-carbidopa. The indices of each of these components constitute a maximum of 5% of the total level of the decay products. Inside the urine, carbidopa is also determined in unchanged form, but conjugates are not detected.

The effect of carbidopa on the process of metabolism of levodopa: the plasma indices of the latter increase under the influence of carbidopa. In the case of prior use of carbidopa, the plasma level of levodopa is increased 5-fold (approximately), and the period of maintenance of medicinal values inside the plasma is prolonged from 4 to 8 hours. In the case of a combination of these two substances, the results of treatment are approximately the same.

In the case of a single use of levodopa in people with a tremor paralysis who previously used carbidopa, the half-life of levodopa rises from 3 to 15 hours. As a result of carbidopa, the level of levodopa increases (approximately 3 times). It should also be noted that the preliminary drug use of carbidopa reduces the content of HVC and dopamine inside urine and plasma.

[5]

Dosing and administration

The medication is taken orally, with the necessary daily dose being detected after careful individual selection for each patient. Thanks to the shape of the tablet, it can be divided without any problems in half.

General requirements - because the dose is selected separately for each patient, it can be individually adjusted not only regarding the size, but also the frequency of use. Tests revealed that peripheral-type dofa-decarboxylase receives the required saturation with carbidopa in the case of the latter being used in the amount of about 70-100 mg per day. People who take carbidopa in smaller doses may develop vomiting with nausea.

When Nakom means is prescribed, the use of standard drugs used to eliminate parkinsonism (except those containing only levodopa) is allowed to continue, but it is necessary to re-select their dosages.

The standard dosage at the initial stages is selected by the treating doctor, taking into account the disease being eliminated, as well as the patient's response to the medication. Usually the initial dosage consists of 0.5 tablets taken 1-2 times per day. But this amount of medication may not be sufficient to provide the size of carbidopa required by the patient, so that, if necessary, another 0.5 tablets of medicines can be added (if taken daily or every other day) if it is necessary to achieve the desired effect.

The effect of the medication manifests itself on the first day, in some cases even immediately after the first dosage is used. Full-scale drug efficiency reaches a maximum for the period of the first week.

Transition to a drug with drugs containing levodopa: Levodopa should be consumed at least 12 hours before using Nakoma (or 24 hours if levodopa with prolonged effect is used). The daily dose of Nakoma should provide approximately 20% of the previously used daily dosage of levodopa.

People taking levodopa in the amount of 1500+ mg, at the initial stage should take Nakom in the amount of 250/25 mg 3-4 times a day.

With maintenance treatment, the size of the drug dose, if necessary, can be increased by 0.5-1 tablet daily (or every other day) until the maximum allowed daily dose (8 tablets) is reached. There is only limited information on the use of carbidopa in a daily dose of more than 200 mg.

The maximum size of the recommended dosage is equal to 8 tablets of medicine per day (2 g of levodopa substance, as well as 0.2 g of carbidopa substance). Approximately it is 3 mg of carbidopa substance and 30 mg of levodopa substance per 1 kg (at a weight of 70 kg patient).

[7]

Use of the nakoma during pregnancy

There is no information on the effects of the drug when used by pregnant women. It should be taken into account that the combination of carbidopa with levodopa leads to skeletal as well as visceral changes in the body of animals. Therefore, it is recommended to use the medicine only when the possible benefit for the woman will exceed the possibility of developing a negative reaction in the fetus.

There is no information on excretion of active ingredients in breast milk. There is a single report on the isolation of levodopa along with milk from a lactating woman with a trembling paralysis. Because of this, since the drug can adversely affect the baby, it is required to decide whether to abort feeding or using Nakoma, taking into account also the importance of using medicines for women's health.

Contraindications

Among the contraindications of the medicine:

• intolerance to any of the constituent elements of the drug;
• combined use with indiscriminate MAO inhibitors (drug use should be discontinued at least 2 weeks before the start of treatment with Nakoma);
• glaucoma of the closed type;
• existing melanoma or suspicion of its presence;
• having an unknown origin of the skin disease.

Caution with the selection of dosages, as well as control over the safety of the treatment course, are necessary in such cases:

• presence in the anamnesis of myocardial infarction with rhythm disorders;
• heart failure and other severe pathologies in the CCC;
• severe forms of pulmonary pathologies (among them bronchial asthma);
• seizures of epilepsy and other forms of convulsive seizures (presence in the anamnesis);
• presence in the gastrointestinal tract of erosive and ulcerative lesions (since in the upper part of the gastrointestinal tract may begin bleeding);
• presence of diabetes mellitus and other decompensated forms of endocrine pathologies;
• severe degree of liver or kidney failure;
• open type glaucoma.

Since there is no information on the safety of use of the drug in children and adolescents under the age of 18, it is prohibited to use a medicine for the described category of patients.

[6]

Side effects of the nakoma

The use of the drug often leads to the development of dyskinesias (among which are dystonic or choreiform), and besides other involuntary movements and nausea. Earlier symptoms that may contribute to the decision to reduce dosage are considered blepharospasm and muscle twitching. Among other side effects:

• general: pain in the sternum, the development of anorexia and syncope;
• organs CAS: the development of heartbeat or arrhythmia, and in addition the occurrence of orthostatic actions, including a decrease or increase in blood pressure, as well as phlebitis;
• organs of the digestive system: the appearance of bleeding in the gastrointestinal tract, vomiting and diarrhea, and in addition to darkening the color of saliva and exacerbation of the ulcer in the area of the 12-colon;
• organs of the hematopoietic system: development of thrombocyto- or leukopenia, and in addition to agranulocytosis or anemia (also hemolytic form);
• manifestations of allergy: the emergence of urticaria, edema Quincke, as well as skin itching and hemorrhagic vasculitis;
• mental disorders and organs of the National Assembly: development of the NSA, paresthesias, drowsiness and dizziness. In addition to this, the manifestations of bradykinesia (the development of on-off syndrome), the manifestation of individual psychotic states (among which hallucinations with illusions, as well as paranoid thoughts), the state of depression (with the appearance of thoughts about suicide, or without them), problems with sleep, , dementia, increased libido and development of confusion. Occasionally, convulsive seizures appeared, but in this case it was not possible to establish a causal relationship using the drug;
• respiratory organs: development of dyspnea;
• skin: rashes, baldness, darkening of the color of secretions of sweat glands;
• organs of the urogenital system: darkening of the color of urine.

Also, side effects caused by the use of levodopa should be considered, since they can also occur with the use of Nakoma:

• Gastrointestinal organs: development of dysphagia, pentavism, bruxism, and besides this hiccups and bloating with constipation. There may also be a feeling of bitterness in the mouth or dry mouth mucous, a feeling of discomfort in the abdomen or abdominal pain, a burning sensation in the area of the tongue, and in addition there may be diarrheal phenomena;
• metabolic processes: the appearance of swelling, increase or decrease in weight;
• organs of the central nervous system: the appearance of a sense of anxiety, fatigue, weakness, disorientation, and numbness. In addition, the occurrence of headaches, fainting, muscle cramps, asthenia and ataxia. Insomnia, euphoria, trismus, a sensation of psychomotor agitation can develop, and in addition to tremors in the arms area, mental activity worsen, gait instability and latent oculosympathetic syndrome appear;
• sensory organs: development of diplopia, mydriasis, tonic convulsions of vision and visual fuzziness;
• urogenital system: delay or vice versa urinary incontinence and development of priapism;
• other manifestations of disturbances: development of malaise, malignant tumors on the skin, dyspnea, vocal hoarseness, and besides, the flow of blood to individual areas of the skin - to the sternum, neck or face;
• laboratory analysis data: an increase in the active activity of ALT with AST, as well as APF and LDH, and in addition to this indices of bilirubin and urea nitrogen inside the plasma, the development of hyperuricemia or hypercreatininaemia and the positive result of the Coombs test. There were also reports of a decrease in hematocrit with hemoglobin, and in addition to the development of bacteriuria, leukocytosis and erythrocyturia.

Drugs that contain both levodopa and carbidopa at the same time can provoke a false positive response to the presence of ketone bodies inside the urine (in cases where special test strips are used to detect ketonuria). This result will remain unchanged after the procedure of boiling the sampled samples is completed. To get a false negative answer, you need to apply a glucose oxidase method to detect glucosuria.

Overdose

In case of an overdose, the severity of side reactions increases.

To get rid of the disorders, careful monitoring of the patient, as well as ECG monitoring, will be necessary to be able to detect the development of arrhythmia. If necessary, the required antiarrhythmic treatment should be performed. It is also necessary to take into account the fact that together with Nakom the patient could use other drugs.

Interactions with other drugs

It is necessary with precautions to combine Nakom with the following medicines:

Antihypertensives - in people taking such drugs, adding to the combination of Nakoma became the cause of postural hypotension (symptomatic). Because of this, at an early stage of Nakoma's use, correction of the dosage of antihypertensive drugs may be necessary.

Antidepressants - a combination of levodopa and MAO inhibitors (except for drugs such as MAO B) can lead to a disorder of the circulatory system, and therefore it is required to complete the use of inhibitors 2 weeks before the onset of Nakoma. This disorder arises from the cumulation of dopamine with norepinephrine under the influence of levodopa - their inactivation is slowed by MAO inhibitors. As a consequence, the risk of tachycardia and feelings of excitement increases, and in addition to dizziness, redness of the face and increased blood pressure.

There is some information about the development of side effects, including dyskinesia and an increase in blood pressure, when combining drugs with tricyclics.

Iron medications - the level of bioavailability of levodopa or carbidopa decreases in the case of combined use with gluconate / ferrous sulphate.

Other medications - when levodopa is combined with dithilin, β-adrenostimulants, and in addition with drugs used in inhalation anesthesia, the likelihood of heart rhythm disturbances may increase.

Antagonists of dopamine D2 receptors (among them risperidone with phenothiazines, as well as butyrophenones), and besides isoniazid - are able to weaken the medicinal action of levodopa.

There is evidence of a blocking of the positive drug effect of levodopa in the case of a tremor paralysis due to a combination with papaverine and phenytoin. It is necessary to closely monitor the condition of persons who use these drugs in combination - in time to detect a weakening of the medicinal effect.

Lithium drugs increase the likelihood of hallucinations or dyskinesias. Enhancement of adverse reactions is observed when combined with methyldopa, and a combination with tubocurarine increases the possibility of lowering blood pressure.

There may be a violation of absorption of levodopa in people who use a high-protein diet, since levodopa is a competitor to individual amino acids.

The effect of pyridoxine (the acceleration of the metabolism of levodopa in dopamine inside the peripheral tissues) may be impaired by carbidopa.

[8]

Storage conditions

The medicine should be kept in a place that is closed from light and moisture, and also inaccessible to children. Temperature conditions - no more than 25 ° C.

Shelf life

Nakom is allowed to take in the period of 3 years from the date of manufacture of the medicinal product.