Levodopa (levodopum)

LEVODOPA (Levodopum). (--)- 3-(3, 4-Dioksifenil) -1 - Alanine, or 3-oksi-1- Tyrosine.
     Synonyms : Kaldopa, Levopa, Avodopa, Bendopa, Biodopa, Brocadopa, Caldopa, Cicandopa, Dalutrin, Deadopa, Dopacin, Dopaflex, Dopal, Dopar, Doparkin, Dopastral, Doprin, Eldopar, Eurodopa, Larodopa, Levodopa, Levopa, Levopar, Madopan, Medidopa, Oridopa, Pardopa, Parkidopa, Parmidin, Speciadopa, Tonodopa, Veldopa and others.
     The white crystalline powder, little is soluble in water, alcohol in nerastvorim.
     Dioksifenilalanin (abbreviated subs, or Dov) is a nutrient substance in the body of obrazuyuscheesya tirozina and the predecessor of release, which in turn is the precursor noradrenalina (see Adrenaline).
     Because that parkinsonizme lowered maintenance release bazalnyh nerve in the brain to treat the disease to the use of substances that increase the content of the amine in the central nervous system. Sam release could not be used for that purpose, as it does through the blood-brain barrier penetrating. It turned out that instead of showing can be used by its predecessor, dioksifenilalanin (Dov), which absorbed oral introduction, into the central nervous system, is decarboxylation, and turns into something, adding to its holdings in bazalnyh nerve stimulates receptors dofamine and ensures parkinsonizme curative effect .
     As a medicine, synthetic isomer levovraschayuschy dioksifenilalanina-L-Dov, which is much more active than pravovraschayuschy isomer.
     Levodopa well absorbed by ingestion. The maximum concentration in plasma is 1 to 2 h after administration. There were significantly (over 75%), kidney, part of faeces.
     Most of levodopa becomes by decarboxylation of tissues (liver, kidney, intestines) in something that does not penetrate through the blood-brain barrier. To reduce the decarboxylation of levodopa apply inhibitors dofa- dekarboksilazy (see Naka, Madopar).
     The use of L-Dov in parkinsonizme reduces primarily rigidity and hypokinesia, to a lesser extent, and later reduced tremor, disfagiya, salivation. It was found that treatment involves a 50-60% of patients. The rest expressed little effect dose of the drug could not be increased because of the side effects.
     Assign product in Parkinson's disease and symptoms (postentsefaliticheskom, ateroskleroticheskom, toxic) parkinsonizme. There are indications of the effectiveness of the drug in extrapiramidale hereditary diseases characterized akinetorigidnym syndrome. To find the effectiveness of L-distorting Dov in treating muscular dystonia. While the treatment L-Dov jet stuporoznyh conditions (especially in patients with decreased excretion release).
     As proof, with events parkinsonizma caused Neuroleptics, L-Dov is not appointed.
     In order to obtain the best therapeutic effect with the least adverse events dose of the drug should be tailored individually, starting with relatively small doses with a gradual increase it.
     Careful monitoring of the patient, particularly at the beginning of treatment.
     Assign L-Dov inside during or after eating.
     Initial dose is usually 0.25 grams a day, every 2 - 3 days to increase the dose of 0.25 g of a daily dose of 3 to the city if necessary dose and then increase to 0.25 - 0.5 g every 10 to 14 days up to a total daily dose of 4 to 5 grams (daily dose divided into 3 - 4 admission). In the rare cases when good endurance daily intake of 6 g. The development of side effects reduce the dose or stop receiving the drug in the event of renewed reception designate smaller doses, increasing gradually with caution.
     L-Dov may be nominated along with holinoliticheskimi drugs. Combined with the use of L-holinolitikov Dov effectively with rigidnobradikineticheskoy and vascular parkinsonizma drozhatelnoy forms. You can also combine the use of L-Dov and midantana.
     The beneficial effects of the application of L-Dov develops slowly; Improvement is usually in the first month. Diluted take long. It should be borne in mind that in a long continuous treatment may diminish the effect.
     When a reception L-Dov phenomenon parkinsonizma usually renewed, but with a rapid lifting of the drug after long-term therapy can dramatically worsen symptoms.
     The application offers different drug side effects : diarrhoeal events (nausea, vomiting, loss of appetite), Orthostatic hypotension, arrhythmia, chronic and horeoatetoidnye giperkinezy, headache, rash, etc. These phenomena are reduced with the lower dose. To avoid diarrhoeal events and for more equitable drug intake after taking food.
     In highly expressed side events should stop receiving the drug.
     Contraindications to express atherosclerosis, hypertension with a significant increase in blood pressure in uncompensated endocrine, kidney, liver, cardiovascular, pulmonary diseases, glaucoma uzkougolnoy (with wide glaucoma treatment is conducted under the close supervision of inner pressure and continuing antiglaukomatoznoy therapy), with the disease blood melanoma, as well as individual sensitivity to the drug. L-Dov and containing L-Dov drugs are not encouraged to nominate pregnant, nursing mothers and children under the age of 12 years.
     During the treatment the patient should not take vitamin B (pyridoxine), which blocks the effects of L-Dov.
     There are also indications that the L-Dov weakened by papaverina (apparently in connection with the blocking effect on brain receptors dofamine).
     Previously stated that the use of L-Dov contraindicated while appointing inhibitors mono aminoksidazy (MAO). Currently, it specifies. The drug should not be used in conjunction with irreversible MAO inhibitor type A (see Nialamid). In the case before the appointment of irreversible MAO inhibitors their admission should be discontinued at least 14 days prior to the admission of L-Dov. However, the recently proposed for strengthening of the L-Dov MAO inhibitors type B (see Deprenil).
     With caution should be appointed levodopa patients with bronchial asthma, emphysema, patients with active stomach ulcer, with psychosis and psihonevrozah, sick survivors of myocardial infarction in the past.
     If necessary, conduct general anastezii be 24 hour deadline for L-Dov.
     In the treatment process to be carried out periodically blood tests to verify the function of liver and kidneys.
     Method of issuance : capsules and tablets of 0.25 and 0.5 g in packs of 100 and 1000.
     Storage : List B.

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