Nakom
Active material: Levodopa, Carbidopa
When ATH: N04BA02
CCF: Of anti-drug – a combination of a dopamine precursor and an inhibitor of peripheral dopa decarboxylase
ICD-10 codes (testimony): G20, G21
When CSF: 02.06.01.01.01
Manufacturer: LEK d.d. (Slovenia)
Pharmaceutical form, composition and packaging
Pills Blue with white inclusions and individual splashes of dark blue color, Oval, lenticular, with a notch on one side.
| 1 tab. | |
| levodopa | 250 mg |
| carbidopa | 25 mg |
Excipients: microcrystalline cellulose, pre-gelatinized starch, corn starch, blue dye (indigotin E132), magnesium stearate.
10 PC. – blisters (10) – packs cardboard.
Pharmacological action
Of anti-drug. Levodopa reduces the symptoms of Parkinson's disease by enhancing the content of dopamine in the brain. Carbidopa, which is not to cross the Geb, lets èkstracerebral′nomu decarboxylation of levodopa, thereby increasing its number of, within the brain and preobrazuûŝeesâ in dopamine.
Naftohaz Ukrainy® has a more pronounced therapeutic effects compared with levodopa, provides long-lasting maintenance of therapeutic concentrations of levodopa in the plasma at doses, that approximately 80% below those, required if you apply one of levodopa.
The action of the drug is during the first day since the beginning of the reception, sometimes – after the first dose. The maximum effect is achieved within 7 days.
Pharmacokinetics
Carbidopa
Absorption
After intake of carbidopa in one dose in patients with Parkinson's disease tmax It is between 1.5 h to 5 no.
Metabolism and excretion
It is metabolized in the liver.
Among the metabolites, excreted in the urine, the main ones are alpha-methyl-3-methoxy-4-gidroksifenilpropionovaâ acid, as well as alpha-methyl-3.4-digidroksifenilpropionovaâ acid, that accounted for about 14% and 10% èkskretiruemyh metabolites, respectively. In smaller amounts are found two other metabolita. One of them identified as 3.4-digidroksifenil-acetone, other – previously as N-methyl-carbidopa. The content of each of these substances is no more 5% of the total number of metabolites. In the urine also reveals an unmodified carbidopa. Conjugates not identified.
Deduction
Excretion of unchanged drug in the urine is mostly complete within 7 h and is 35%.
Levodopa
Absorption
Levodopa is rapidly absorbed from the digestive tract and actively metabolized. Despite, that produces more 30 various metabolites, mostly levodopa is converted to dopamine, epinephrine, norepinephrine.
After intake of levodopa in one dose in patients with Parkinson's disease tmax is 1.5-2 h and is held on the therapeutic level for 4-6 no.
Deduction
Metabolites excretiruyutza with urine quickly – during 2 h displayed about 1/3 dose.
T1/2 levodopa is about 50 m.
When taking a combination of carbidopa and levodopa T1/2 levodopa increases to approximately 1.5 no.
Effect of carbidopa on the metabolism of levodopa
Carbidopa levodopa increases concentration in the blood plasma. Under the previous reception of carbidopa levodopa concentration in plasma is increased approximately 5 time, while maintaining therapeutic concentrations in the plasma increases from 4 to 8 no. While admission carbidopa and levodopa were obtained similar results.
In patients with Parkinson's disease, that previously took karbidopu, When taking levodopa in a single dose of T1/2 levodopa grew from 3 to 15 no. Concentrations of levodopa increases at the expense of carbidopa, at least, in 3 times. The concentration of dopamine and gomovanil′noj acid in plasma and urine is reduced with prior admission of carbidopa.
Testimony
is treatment of Parkinson's disease and Parkinsonism syndrome.
Dosage regimen
The optimal daily dose is determined by a careful individual selection. Tablet form allows you to divide it into two parts with minimum effort.
In the course of treatment may require correction as individually tailored dose, and the frequency of dose. As research, peripheral decarboxylase-track saturated with karbidopoj when receiving the last dose about 70-100 mg / day. Patients, receiving karbidopu in lower dose, possible nausea and vomiting.
In the case of the appointment of Nakoma® reception of standard drugs for the treatment of Parkinson's disease, with the exception of those, that contain one l-dopa, may be continued, the dose should be selected again.
Initial dose filled, in accordance with the indications and the reaction of the patient. The initial dose of the drug to Naftohaz Ukrainy® is 1/2 tab. 1-2 times / day. However, this dose might not provide the optimal amount of carbidopa, It takes patient. Therefore, in case of need, add 1/2 tab. Nakoma® every day or every other day to achieve an optimal effect. Therapeutic effect is observed on the first day, sometimes – after the first dose. The full effect of the drug is achieved within 7 days.
When switching from drugs levodopa reception last should stop, at least, for 12 hours before the start of treatment with Naftohaz Ukrainy® (for 24 no – in the case of the use of drugs levodopa prolonged action). The daily dose of Naftohaz Ukrainy® should provide approximately 20% previous daily doses of levodopa.
Patient, taking more 1.5 Mr. levodopa, the initial dose of Nakoma® is 1 tab. 3-4 times / day.
In the maintenance therapy if necessary dose Nakoma® You can raise 1/2-1 tab. every day or every other day until the maximum dose – 8 tab. / day. Experience the reception in a dose of carbidopa 200 mg/day limited.
The maximum recommended dosage of Naftohaz Ukrainy® is 8 tab. / day (200 mg and carbidopa 2 Mr. levodopa). It is approximately 3 mg and carbidopa 30 mg levodopa on 1 kg body weight (in the body weight of the patient 70 kg).
Side effect
Frequently – dyskinesias, including involuntary movements (incl. horeepodobnye, dystonic), as well as nausea.
Early signs of, on the basis of which a decision may be taken to abolish drug are muscle twitching and Blepharospasm.
From the central and peripheral nervous system: neuroleptic malignant syndrome, episodes bradikinezii (“on-off”-syndrome), dizziness, drowsiness, paraesthesia, episodes of psychotic conditions, including illusions, hallucinations and paranoid thinking, depression with the development of suicidal intentions or no, dementia, sleep disorders, excitation, confusion, increased libido.
In rare cases, – convulsions, However, a causal link with the admission of the drug Naftohaz Ukrainy® not installed.
From the digestive system: possible anorexia, vomiting, bleeding from the gastrointestinal tract, worsening ulcers duodenal ulcer, diarrhea, darkening of saliva.
From the body as a whole: possible fainting, chest pain.
Cardio-vascular system: arrhythmia and/or palpitations, Orthostatic effects (incl. increase or decrease the episodes of HELL), phlebitis.
From the hematopoietic system: leukopenia, anemia (incl. hemolytic), thrombocytopenia, agranulocytosis.
The respiratory system: Perhaps Dyspnea.
Dermatological reactions: possible alopecia, skin rash, darkening of the secretion of the sweat glands.
With the genitourinary system: dark urine.
Allergic reactions: angioedema, hives, itching, disease Šenlejn-Genoha.
Other side effects, that may occur as a result of taking levodopa
From the digestive system: dyspepsia, dry mouth, bitterness in the mouth, sialoreâ, dysphagia, bruxism, bouts of hiccups, pain and discomfort in the abdomen, constipation, flatulence, stinging tongue.
Metabolism: decrease or increase in body weight, swelling.
CNS: weakness, swoon, fatiguability, headache, asthenia, reducing mental activity, disorientation, ataxia, stupor, increased tremor of hands, muscle cramps, Trizm, Activating a latent Syndrome Bernard-Horner, insomnia, anxiety, euphoria, psychomotor agitation, unsteady gait.
From the senses: diplopia, blurred vision, mydriasis, oculogyric crises.
With the genitourinary system: urinary retention, urinary incontinence, priapism.
Other: hoarseness, malaise, rush of blood to the face, neck and chest, dyspnoea, zlokachestvennaya melanoma.
From the laboratory parameters: increased activity of alkaline phosphatase, IS, GOLD, LDH, the increase of bilirubin, urea nitrogen plasma, elevation of serum creatinine, hyperuricemia, Positive Coombs, decrease in hemoglobin and hematocrit, giperglikemiâ, leukocytosis, bacteriuria, eritrotsiturii.
Preparations, containing karbidopu and l-dopa, may cause lozhnopolaugitionuyu reactions to the ketone bodies in urine, If ketonurii used test strips. This reaction does not change after boiling samples of urine. False negative results may be obtained from the use of the glûkozooksidaznogo method to determine glucosuria.
Contraindications
- Zakrыtougolynaya glaucoma;
is melanoma established or suspected;
-skin disease of unknown etiology;
- Concomitant use of non-selective MAO inhibitors;
- Hypersensitivity to the drug.
FROM caution the drug should be used in patients with severe cardiovascular diseases, incl. myocardial infarct violations heart rhythm (history), Heart Failure, serious diseases of the respiratory system, including bronchial asthma, pripadkah convulsions (history), including epileptic, erosive and ulcerative lesions of the gastrointestinal tract (due to the possibility of bleeding from the upper gastrointestinal divisions), dekompensirovannyh diseases of the endocrine system, including diabetes, severe renal insufficiency, severe hepatic insufficiency, open-angle glaucoma.
Pregnancy and lactation
Influence Of Nakoma® on the course of pregnancy in women is unknown. IN experimental studies revealed, that combination of levodopa and carbidopa causes visceral and skeletal changes in animals. Therefore, the use of the drug is possible only in case of, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.
Unknown, whether with breast milk levodopa and carbidopa.
There 1 a message about the excretion of levodopa in breast milk from a nursing mother with Parkinson's disease. Therefore, because of possible serious harmful effects of the drug on the newborn and, given the importance of the therapy to the mother, If necessary, the use of the drug during lactation should decide either to cease breastfeeding, or withdrawal Naftohaz Ukrainy®.
Cautions
As in the cases of levodopa, When assigning Nakoma® patients, survivors of myocardial infarction and atrial, an anchor or ventricular arrhythmias, careful preliminary examination. In these patients it is necessary to monitor cardiac activity, especially in the appointment of the first dose and dose selection period.
Patients with open-angle glaucoma Naftohaz Ukrainy® It should be administered with caution and subject to permanent monitoring of intraocular pressure during treatment.
Because the side effects tend to occur when applying the combination of carbidopa and levodopa, than one levodopa, between dose selection for patients should be closely monitored. In particular, Naftohaz Ukrainy® more, than levodopa, causes involuntary movement. The appearance of involuntary movements may require lower doses. An early sign of excessive doses of some patients may serve as Blepharospasm. If the therapeutic response to the drug levodopa are fickle, and signs and symptoms of Parkinson's disease are not monitored during the whole day, moving to Naftohaz Ukrainy® typically reduces fluctuations in reaction to medication.
Naftohaz Ukrainy® provides adequate patients reduce symptoms of Parkinson's disease.
Naftohaz Ukrainy® also see patients with Parkinsonism, receiving vitamin preparations, containing pyridoxine hydrochloride (vitamin B6).
Naftohaz Ukrainy® not recommended for eliminating extrapiramidale disorders, caused by drugs.
Naftohaz Ukrainy® can be prescribed to patients, already receiving drugs, containing only l-dopa, However, receiving levodopa should be discontinued, at least 12 hours before the start of treatment with Naftohaz Ukrainy®. Naftohaz Ukrainy® should be appointed in doses, that provide approximately 20% from the previous dose of levodopa.
Patients, taking l-dopa previously, dyskinesia may occur, tk. carbidopa allows more levodopa to reach brain, and, thus, produces greater amounts of dopamine. The appearance of psoriasis may require lower doses.
Like levodopa, Naftohaz Ukrainy® can cause involuntary movements or mental disorders. Expected, that these reactions are due to the increased content of dopamine in the brain. These phenomena may require lower doses of. All patients, host Naftohaz Ukrainy®, should be supervised with regard to the possibility of developing depression with suicidal tendencies. Patients, who have experienced psychosis, requires a cautious approach when selecting therapies.
Should be cautious appoint Naftohaz Ukrainy® and psychotropic drugs. With the sudden lifting of protivoparkinsoničeskih drugs was described by symptom, reminiscent neirolepticeski Malignant Syndrome, including muscle rigidity, fever, mental disorders and an increase in the concentration of serum CPK. It is therefore necessary to a thorough examination of patients in a period of sharp decline dose Nakoma® or its cancellation, especially if the patient receives antipsychotics. As is the case with levodopa, during the lengthy treatment Nakomom® It is recommended that periodic monitoring of liver function, blood, cardiovascular systems and kidneys.
If you require general anesthesia, the drug Naftohaz Ukrainy® can be taken until the patient allowed to oral administration of fluids and medications.
If the treatment temporarily interrupted, the reception of Nakoma® may be renewed in the usual dose, Once the patient is able to take the drug inside.
Use in Pediatrics
The safety of the drug in children younger and middle age is not installed.
Not recommended to appoint Naftohaz Ukrainy® children and adolescents under the age of 18 years.
Overdose
Symptoms: increased side effects.
Treatment: should ensure a thorough monitoring and ECG monitoring with a view to identifying possible arrhythmias, If necessary, adequate therapy should be antiaritmičeskuû. It is necessary to take into account the possibility that, that, along with the drug Naftohaz Ukrainy® the patient was taking other medications.
Drug Interactions
When applying the Nakoma® patients, receiving antihypertensive therapy, was observed symptomatic ortostatical gipotenzia (at the beginning of treatment with Naftohaz Ukrainy® in such cases, you might need to dose adjustment antigipertenzivnogo drug).
While the use of levodopa with MAO inhibitors (except MAO-B inhibitor) possible circulatory disorders (MAO inhibitors should stop for 2 the week before you start taking levodopa). This is due to the accumulation under the influence of dopamine and norepinephrine levodopa, inactivation inhibited MAO inhibitors. As a result, the probability of excitation development, increase blood pressure, tachycardia, facial flushing and dizziness.
There are anecdotal reports of adverse reactions, including raising HELL and hypertension diskineziu in the case of combined use of tricyclic antidepressants and Nakoma®.
Bioavailability of carbidopa and levodopa and/or dropping while applying iron sulfate or iron glukonata.
With simultaneous use of levodopa with beta-agonists, ditilinom and means for inhalation anesthesia may increase the risk of heart rhythm disorders.
Dopaminovykh antagonists (D)2-receptors (eg, fenotiazinы, butyrophenones and risperidone), as well as isoniazid can reduce the therapeutic effect levodopa.
There have been reports of blocking the positive therapeutic effects of levodopa in Parkinson's disease by fenitoina and papaverina. For patients, receiving these drugs simultaneously with preparation Naftohaz Ukrainy®, requires careful monitoring to detect reducing therapeutic action.
Drugs lithium increases the risk of development of dyskinesias and hallucinations.
Together with the use of methyldopa strengthens side effects Nakoma®.
The simultaneous use of tubokurarina increases the risk of arterial hypotension.
Absorption of levodopa can be compromised in some patients, located on the high-protein diet, because the levodopa competes with some amino acids.
Carbidopa inhibits the action of pyridoxine hydrochloride (vitamin B6), that speeds up biotransformatia levodopa into dopamine in peripheral tissues.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year. Do not use after the expiry date, on the package.
