Description
release form
tablets.
Packing
Per pack 100 pcs.
Pharmacological action
Antiparkinsonian combination drug – a combination of carbidopa (an aromatic 1-amino acid decarboxylase inhibitor) and levodopa (a dopamine precursor). It weakens and eliminates the symptoms of Parkinson’s disease, including hypokinesia, stiffness, tremors, dysphagia, and salivation.
The antiparkinsonian effect of levodopa is due to its conversion to dopamine directly in the central nervous system, leading to the replenishment of dopamine deficiency in the central nervous system (CNS). Dopamine formed in peripheral tissues is not involved in the implementation of the anti-Parkinsonian effect of levodopa (does not penetrate the central nervous system) and is responsible for most of the side effects of levodopa.
Carbidopa, an aromatic L-amino acid decarboxylase inhibitor, reduces the formation of dopamine in peripheral tissues, which indirectly leads to an increase in the amount of levodopa entering the central nervous system.
Nakom ® provides an adequate reduction in symptoms of Parkinson’s disease in more patients. The effect of the drug manifests itself during the first day from the start of administration, sometimes after the first dose. The maximum effect is achieved within 7 days.
Indications
Treatment of Parkinson’s disease and Parkinson’s syndrome.
Contraindications
² Ñ hypersensitivity to the components of the
preparation ² Ñ simultaneous administration of non-selective
monoamine oxidase inhibitors (MAOs) ² Ñ less than two weeks after the end of taking
MAO inhibitors ² Ñ closed-angle glaucoma
malignant ² Ñ malignant skin disease
² Ñ unknown up to 18 years of age (the safety of the drug in young and middle children has not been established)
² Ñ lactation period.
With caution
² Ñ myocardial infarction with a rhythm disorder (history)
² Ñ chronic heart failure and other serious diseases of the cardiovascular system
² Ñ severe lung diseases, including bronchial asthma
² Ñ epileptic and other seizures (history of history) ulcerative lesions of the gastrointestinal tract (risk of bleeding from the upper gastrointestinal tract)
² Ñ diabetes mellitus and other decompensated endocrine diseases
² Ñ severe renal and / or liver failure
² Ñ open-angle glaucoma
² Ñ extrapyramidal reactions caused by the use of
² Ñ pregnancy.
Use during pregnancy and lactation
Safety of the drug during pregnancy has not been studied. The use of the drug is only possible if the expected benefit of the 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 harmful effect of the drug on the newborn and taking into account the importance of conducting therapy for the mother, if necessary, the use of the drug during lactation should decide whether to stop breastfeeding or cancel the drug Nakom.
In experimental studies revealed, that the combination of levodopa and carbidopa causes visceral and skeletal changes in laboratory animals.
Special instructions
Nakom ® can be prescribed to patients who are already taking levodopa in monotherapy. However, the administration of levodopa in a single-component form must be stopped at least 12 hours before the appointment of the drug Nakom ®.
Patients who previously took levodopa alone may experience dyskinesia because carbidopa allows levodopa to enter the brain more efficiently and therefore produces more dopamine. If dyskinesia occurs, a dose reduction may be required.
Like levodopa, levodopa / carbidopa can cause involuntary movements and mental disturbances. It is believed that these reactions are associated with an increase in dopamine levels in the brain after the administration of levodopa, and the use of levodopa / carbidopa can cause relapse. Dose reduction may be required.
All patients should be closely monitored for the development of depression with concomitant suicidal tendencies.
Precautions should be taken when treating patients who have previously had or are currently showing signs of psychosis.
Caution should be exercised with concomitant administration of psychoactive drugs and levodopa / carbidopa). In some patients, blepharospasm may be an early sign of an overdose.
As with levodopa, when prescribing Nakom ® to patients who have had a myocardial infarction and have a history of atrial, nodular, or ventricular arrhythmias, a thorough preliminary examination is necessary.
Such patients are advised to regularly conduct cardiological examinations, especially when prescribing the first dose and during the dose selection period.
Levodopa / carbidopa should be used with caution in patients with severe cardiovascular or pulmonary diseases, bronchial asthma, kidney, liver, endocrine diseases or with indications of peptic ulcer (due to the possibility of gastrointestinal bleeding from the upper digestive tract ) or a history of seizures.
Patients with open-angle glaucoma while taking Nakom ® need regular monitoring of intraocular pressure.
MAO inhibitors should be discontinued at least two weeks before starting treatment with Nakom ®.
With the sudden cancellation of antiparkinsonian drugs, a symptom complex resembling a malignant antipsychotic syndrome (muscle rigidity, fever, mental disorders and an increase in the concentration of serum creatinine phosphokinase) is possible. It is necessary to carefully examine patients during a period of a sharp decrease in the dose of Nakom ® or its withdrawal, especially if the patient receives antipsychotic drugs.
Levodopa was accompanied by drowsiness and episodes of sudden falling asleep.
Extremely rarely reported cases of sudden falling asleep during daily activities, in some cases without awareness or warning signs.
If these symptoms appear, consider reducing the dose.
It is necessary to periodically conduct a blood test, with prolonged therapy, it is recommended to periodically monitor the functions of the cardiovascular system, liver and kidneys.
If general anesthesia is required, Nakom ® can be taken as long as the patient is allowed to take the drug by mouth. If treatment is interrupted temporarily, then the usual dose may be prescribed again as soon as the patient is able to take the drug again orally.
Studies have shown that patients with Parkinson’s disease have an increased risk of developing melanoma, therefore, patients taking Nakom ® need to undergo regular examinations by a dermatologist.
It is not clear whether the increased risk is associated with Parkinson’s disease or other factors, such as drugs used to treat Parkinson’s disease.
Patients receiving dopamine antagonists exhibit pathological gambling addiction, hypersexuality, compulsive embezzlement (craving for purchases), gluttony and overeating, increased libido. With the development of the above symptoms, a dose / treatment adjustment is recommended.
Nakom ® is not recommended for the treatment of extrapyramidal disorders caused by drugs.
High protein foods may interfere with the absorption of the drug.
Effect on ability to drive vehicles,
mechanisms In very rare cases, levodopa can cause drowsiness and cases of sudden onset of sleep. During treatment with Nakom ®, patients should be informed of the possibility of sudden falling asleep. Patients with drowsiness and experiencing sudden falling asleep (cases of sudden falling asleep) should refrain from driving vehicles and engaging in potentially dangerous activities, requiring increased concentration of attention and speed of psychomotor reactions.
Composition
1 tab. contains:
active substances:
levodopa – 250 mg,
carbidopa – 25 mg
excipients:
pregelatinized starch – 45 mg
corn starch – 6.5 mg
blue dye (indigotine E132) srdk Magnesium-0, -72, -72 stearate – 4.2 mg
MCC – up to 380 mg.
Dosage and Administration
Inside.
The dose should be selected individually for each patient, which may require both correction of the individual dose and frequency of administration of the drug. The shape of the tablet allows you to divide it into two parts with minimal effort.
The initial daily dose is 1/2 (half) tablets 1 or 2 times a day. However, the optimal amount of carbidopa required by many patients may not be provided. If necessary, 1/2 tablet should be added every day or every other day until the optimal effect is achieved. The effect is observed already in the first day, sometimes after a single dose. The full effect of the drug is achieved in up to seven days.
Studies have shown that saturation of peripheral decarboxylases of aromatic 1-amino acids is achieved by the administration of 70-100 mg of carbidopa per day.
If a patient receives a lower dose of carbidopa, the likelihood of nausea and vomiting is higher.
When prescribing Nakom ®, you can continue to take standard antiparkinsonian drugs (with the exception of levodopa as monotherapy), and dose adjustment is required.
Transition from levodopa preparations. Levodopa should be discontinued at least 12 hours before the start of treatment with Nakom ® (24 hours in the case of prolonged action of levodopa drugs). The daily dose of Nakom ® should provide approximately 20% of the previous daily dose of levodopa.
For patients taking more than 1500 mg of levodopa, the initial dose of Nakom ® is 25/250 mg 3 or 4 times a day.
supportive care. If necessary, the dose of Nakom ® can be increased by 1 tablet every day or every other day until the maximum dose is reached – 8 tablets per day. Experience with a daily dose of carbidopa in excess of 200 mg is limited.
The maximum recommended dose is eight tablets of Nakom ® per day (200 mg of carbidopa and 2000 mg of levodopa), which corresponds to approximately 3 mg / kg of carbidopa and 30 mg / kg of levodopa per kilogram of body weight with a patient body weight of 70 kg.
Elderly patients: There is extensive experience with levodopa and carbidopa in elderly patients.
Dose adjustment not required.
Patients with renal / hepatic insufficiency: dose adjustment not required.
Side effects
According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very often (? 1/10), often (? 1/100, <1/10), infrequently (? 1/1000, <1/100), rarely (? 1/10000, <1/1000) and very rarely (<1/10000) the frequency is unknown - the frequency of occurrence of phenomena cannot be determined on the basis of available data. The most common side effects are dyskinesias, including choreic, dystonic, and other involuntary movements, as well as nausea. Muscle twitching and blepharospasm may be considered early signs on the basis of which a decision can be made to reduce the dose. Benign, malignant, and unspecified neoplasms, including cysts and polyps frequency unknown: malignant melanoma. From the hemopoietic organs: rarely: leukopenia, anemia (including hemolytic), thrombocytopenia, agranulocytosis. On the part of the immune system: rarely: angioedema. From the side of metabolism: often: anorexia frequency unknown: loss or weight gain, edema. From the psyche: often: sleep disturbance, including nightmares, hallucinations, depression (including with suicidal intentions), confusion, infrequent: rarely agitation: psychotic reactions, including delusions, and paranoid thinking, increased libido. Patients receiving dopamine antagonists exhibit pathological gambling addiction, hypersexuality, compulsive embezzlement (craving for shopping), gluttony and overeating, increased libido. The reactions listed above basically disappeared after a dose reduction or cessation of treatment. frequency unknown: anxiety, disorientation, euphoria, insomnia, bruxism. From the nervous system: very often: dyskinesia, including chorea, dystonia, and other involuntary movements of often: episodes of bradykinesia (on-off syndrome), dizziness, paresthesia, drowsiness, including less commonly drowsiness in the daytime, and episodes of sudden falling asleep infrequently: syncope rarely: dementia, unknown frequency: ataxia, hand tremor, extrapramidal disorders, malignant antipsychotic syndrome, muscle twitching, headache, decreased severity of intelligence, trismus, activation of the Bernard-Horner latent syndrome, insomnia, nervousness, euphoria, numbness eating, fainting, falling, gait disturbance, irritation, compulsions. Convulsions have been reported, but a causal relationship with Nakom ® has not been established. From the sensory organs: frequency unknown: blepharospasm, diplopia, visual impairment,s (tonic cramps of the external muscles of the eyeball). From the cardiovascular system: often: palpitations, orthostatic reactions, including episodes of low blood pressure rarely: arrhythmias, phlebitis, increased blood pressure frequency unknown: hot flashes, hyperemia. From the respiratory system: often: shortness of breath frequency unknown: hoarseness, abnormal nature of breathing. From the gastrointestinal tract: often: vomiting, diarrhea rarely: gastrointestinal bleeding, exacerbation of a duodenal ulcer, darkening of the saliva frequency unknown: dry mouth, salivation, dysphagia, abdominal pain, constipation, bloating, dyspepsia, burning sensation of the tongue, a feeling of bitterness in the mouth, nausea, belching. From the skin: infrequently: urticaria rarely: itching, hemorrhagic vasculitis (Shenplein-Genoch’s purpura), alopecia, rash, darkening of sweat frequency unknown: increased sweating. From the urinary system: rarely: dark urine frequency unknown: urinary incontinence, urinary retention. From the side of musculoskeletal and connective tissue: infrequently: muscle cramps frequency unknown: muscle twitching. From the reproductive system: frequency unknown: priapism. General disorders and disorders at the injection site: often: chest pain frequency unknown: asthenia, swelling, weakness, malaise, fatigue, malignant antipsychotic syndrome. Laboratory parameters: frequency unknown: increased activity of alkaline phosphatase, aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase, an increase in the content of bilirubin, urea nitrogen in blood plasma, urea in blood plasma, hypercreatininemia, hyperuricemia, a positive Coombs test. A decrease in hemoglobin and hematocrit, hyperglycemia, leukocytosis, bacteriuria, and hematuria has been reported. Preparations containing carbidopa and levodopa can cause a false positive reaction to ketone bodies in the urine if test strips are used to determine ketonuria. This reaction will not change after boiling urine samples. False negative results can be obtained using the glucose oxidase method for determining glucosuria. Drug interaction When used simultaneously with antihypertensive drugs, it is necessary to adjust the dose of the latter due to the risk of orthostatic hypotension. With the simultaneous use of levodopa with monoamine oxidase inhibitors (MAOs) (with the exception of MAO-B inhibitors), circulatory disorders are possible (taking MAO inhibitors should be stopped at least 2 weeks before taking the drug). This is due to the accumulation of dopamine and norepinephrine under the influence of levodopa, inactivation of which is inhibited by MAO inhibitors, and a high likelihood of developing excitement, increased blood pressure (BP), tachycardia, facial redness and dizziness. Iron salts may decrease the bioavailability of levodopa and carbidopa. The clinical significance of this interaction is unknown. With the simultaneous use of levodopa with -adrenomimetics, ditilin and drugs for inhalation anesthesia, an increased risk of developing heart rhythm disturbances is possible. D2 dopamine receptor antagonists (e.g. derivatives of butyrophenone, diphenylbutylpiperidine, thioxanthene, phenothiazine, risperidone), as well as isoniazid, reduce the therapeutic effect of levodopa. There are reports of blocking the positive therapeutic effects of levodopa as a result of taking phenytoin and papaverine. Lithium preparations increase the risk of dyskinesia and hallucinations. Methyldopa enhances side effects. The simultaneous use of tubocurarine increases the risk of hypotension. Levodopa absorption may be impaired in patients high-protein diets because levodopa competes with certain amino acids. Carbidopa inhibits the action of pyridoxine hydrochloride (vitamin B6), which accelerates the metabolism of levodopa to dopamine in peripheral tissues. Overdose The overdose increases the severity of the symptoms in the “side effect” section. Treatment: gastric lavage, activated charcoal intake should be carefully monitored and electrocardiographically monitored for timely detection of arrhythmias, and appropriate antiarrhythmic therapy should be performed if necessary. Measures for an acute overdose of the drug Nakom ® are basically the same as for an acute overdose of levodopa. It should be noted that pyridoxine is not effective for removing the action of the drug Nakom ®. The concomitant therapy that the patient receives along with Nakom ® should also be considered. Storage conditions Keep out of the reach and sight of children at temperatures not exceeding 25 ° C. Shelf life 3 years. Conditions of release from pharmacies Prescription dosage form tablets Possible product names Nakom 250mg + 25mg Tab. X100 (R) NAKOM N100 TABLE Nakom tab 250mg + 25mg N100 (pack contact N10x10) Nakom tab 250mg + 25mg x 100 Nakom tab N100 Sandoz, Switzerland
