SINEMET ® is a medicinal product based on Melevodopa hydrochloride and Carbidopa hydrate
THERAPEUTIC GROUP: Dopaminergic substances
IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects
Indications SINEMET ® - Melevodopa + Carbidopa
SINEMET ® is a drug indicated for the treatment of Parkinson's disease and Parkinson's syndrome, characterized by motor disorders such as bradykinesia, rigidity, tremor, dysphagia, postural instability and sialorrhea.
Mechanism of action SINEMET ® - Melevodopa + Carbidopa
SINEMET ® is a medicinal specialty that combines two very important active ingredients, with different biological functionalities, necessary to restore the correct dopaminergic balance lost in Parkinson's disease.
More precisely, Levodopa, once taken orally and absorbed by the gastrointestinal tract, also reaches the central nervous system, being decarboxylated by dopa-decaboxylases of the presynaptic endings of dopamine neurons in dopamine, and making up for the typical deficiency of Parkinson's and Parkinson's syndromes.
The aforementioned mechanism allows to rebalance the local balance between dopamine and aceticoline, thus controlling some of the classic symptoms such as bradykinesia, stiffness and tremor, related to the altered activity of the base nuclei.
The Carbidopa instead, not being able to overcome the blood-brain barrier, remains at the peripheral level engaging the peripheral decarboxylases and avoiding the formation of peripheral Dopamine, responsible both for a reduction in the clinical efficacy of the therapy and for an enhancement of the side effects of the same ..
After their activity, both active ingredients are excreted mainly via the kidneys.
Studies carried out and clinical efficacy
LEVODOPA / CARBIDOPA AND PSYCHIATRIC DISORDERS
Mov Disord. 2012 Apr; 27 (4): 588-90. doi: 10.1002 / mds.24898. Epub 2012 Jan 27.
Study that denounces some of the potential side effects of Levodopa therapy, and in particular those of a psychiatric or psychotic type such as the trichophagia observed in this patient after administration of levodopa and carbidopa-based gels.
CARBIDOPA / LEVODOPA IN POST-OPERATIVE PHASES
Am J Phys Med Rehabil. 2013 Apr; 92 (4): 307-11. doi: 10.1097 / PHM.0b013e318278dc20.
Study demonstrating that the association between Levodopa and Carbidopa may have a beneficial effect on normal nerve function, in particular on the neuromotor function, after excision of a brain tumor.
LEVODOPA AND HIGH-DOSE CARBIDOPA
BMJ Open. 2012 Dec 11; 2 (6). pii: e001971. doi: 10.1136 / bmjopen-2012-001971. Print 2012.
Interesting study that tests the usefulness of the various dosages of Carbidopa and Levodopa, evaluating among other things the possible possibility of identifying an attack dosage necessary to guarantee a prompt regression of the symptomatology.
Method of use and dosage
SINEMET ®
Carbidopa hydrated 27 mg tablets (equal to 25 of Carbidopa anhydrous) and 250 mg of Levodopa;
Modified release tablets from 50 mg of Carbidopa and 200 mg of Levodopa;
Carbidopa hydrated 27 mg modified-release tablets (equal to 25 of Carbidopa anhydrous) and 250 mg of Levodopa;
Carbidopa hydrated effervescent tablets of 27 mg (equal to 25 of Carbidopa anhydrous) 100 mg of Levodopa.
The dosage of SINEMET ® must necessarily be defined by a doctor experienced in the treatment of neurological diseases, taking care to modulate doses and methods of intake based on the patient's general health conditions, the severity of his / her clinical picture and the therapeutic response .
Dose adjustment may be necessary both during treatment following the appearance of side effects.
Warnings SINEMET ® - Melevodopa + Carbidopa
A careful neurological examination must necessarily precede the administration of SINEMET ®, in order to assess its prescriptive appropriateness and consider all the potential contraindications related to the establishment of a dopaminergic therapy.
Cardiovascular, pulmonary, hepatic, renal, psychotic and psychiatric disorders are just some of the main conditions for which it would be appropriate to be particularly careful when using dopaminergics.
The patient on SINEMET ® therapy should also avoid the use of machinery or vehicle driving given the documented sleep attacks and the reduction of perceptive abilities widely documented following the use of Levodopa.
During the entire treatment the main blood chemistry parameters should also be monitored, given Levodopa's ability to alter its values.
It is recommended to keep the medicine out of the reach of children.
PREGNANCY AND BREASTFEEDING
The absence of clinical trials able to fully characterize the safety profile for Levodopa for the health of the fetus and infant, extend the aforementioned contraindications to the use of SINEMET ® also to pregnancy and the subsequent breastfeeding period.
Interactions
The patient on treatment with SINEMET ® ® should avoid the simultaneous intake of antihypertensive drugs due to the risk of postural hypotension, antidepressants, due to the potential side effects linked to the simultaneous intake of Levodopa, and other active ingredients capable of altering the normal pharmacokinetic properties of Levodopa like iron, phenytoin and papaverine ..
Contraindications SINEMET ® - Melevodopa + Carbidopa
The use of SINEMET ® is contraindicated in patients who are hypersensitive to the active substance or to one of its excipients and in patients suffering from severe liver and kidney diseases, in patients with narrow-angle glaucoma, myocardial infarction, suspected melanoma lesions, in patients under the age of 18, during pregnancy and lactation.
Undesirable effects - Side effects
Treatment with SINEMET ®, especially if continued for a long time, could lead to the appearance of nausea, vomiting, dizziness, psychiatric disorders, tachycardia, drowsiness and fatigue.
Fortunately, the incidence of clinically relevant side effects among the various organs and systems is rarer, for which it is often necessary to adjust the dosage or suspend therapy.
Continuous medical supervision therefore becomes necessary even in the face of the high incidence of the aforementioned adverse reactions.
Note
SINEMET ® is a prescription-only drug.
