SIRIO ® - Melevodopa + Carbidopa

SIRIO ® 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 SIRIO ® - Melevodopa + Carbidopa

SIRIO ® is indicated in the treatment of Parkinson's disease especially when characterized by motor fluctuations such as akinesia on waking, afternoon or at the end of the dose.

Mechanism of action SIRIO ® - Melevodopa + Carbidopa

SIRIO ® is a drug used in the treatment of Parkinson's disease, consisting of a methyl ester of Levodopa such as melevodopa and an inhibitor of peripheral decarbosilase such as Carbidopa.

This association makes the drug particularly active in the treatment of the disease and above all in the control of the akinesias; allowing melevodopa to reach the system of nuclei of the base, to be converted into Dopamine by decarboxylases present in the presynaptic endings of dopaminergic neurons at striatal level and in controlling the classical motor symptomatology associated with dopamiminergic deficiency present in Parkinson's disease.

The presence of Carbidopa instead allows to control the classic side effects of Levodopa, associated with the conversion into dopamine exerted by peripheral dopa-decarboxylases, not permeating the blood-brain barrier and concentrating therefore at the peripheral level

The aforementioned activities are also aided by advantageous pharmacokinetic properties, which allow Melevodopa to more effectively solubilize in an aqueous environment, making absorption faster and therefore therapeutic activity at a faster onset.

The metabolites derived from the absorption of both active ingredients are mainly excreted via the kidneys.

Studies carried out and clinical efficacy

LEVODOPA / CARBIDOPA AND QUALITY OF SLEEP

Acta Neurol Scand. 2013 May; 127 (5): e28-32. doi: 10.1111 / ane.12075. Epub 2013 Jan 11.

Interesting Italian study that demonstrates how treatment with Levodopa and Carbidopa in gel for intestinal infusion can significantly improve sleep quality in patients with Parkinson's disease.

EXTENDED RELEASE CARBIDOPA / LEVODOPA

Parkinsonism Relat Disord. 2013 Sep 5.

Work demonstrating how the administration of Carbidopa / prolonged release Levodpa can significantly improve clinical conditions in patients with Parkinson's disease in the initial phase, compared to the same combination in the normal formulation.

THE EFFECTIVENESS OF COMBINED THERAPIES IN THE PRECODED PARKINSON STATES

J Neural Transm. 2013 Nov 20. [Epub ahead of print]

The most recent study that combined with Levodopa / Carbidopa combination therapy also entacapone shows clearer improvements in patients in the early phase of Parkinson's, without registering any relevant side effects.

Method of use and dosage

SIRIO ®

Effervescent tablets of 27 mg Carbidopa idrata (equal to 25 of Carbidopa anhydrous) and 314 mg of Melevodopa hydrochloride (equal to 250 mg of Levodopa);

Effervescent tablets of 13.5 mg of Carbidopa idrata (equivalent to 12.5 of Carbidopa anhydrous) and 157 mg of Melevodopa hydrochloride (equivalent to 125 mg of Levodopa);

Effervescent tablets of 27 mg of Carbidopa hydrata (equal to 25 of Carbidopa anhydrous) and 125.6 mg of Melevodopa hydrochloride (equivalent to 100 mg of Levodopa).

The choice of the therapeutic scheme, the dosages and the timing of the assumption is up to the doctor expert in the treatment of neurological pathologies after having carefully evaluated the patient's overall health status and the severity of the relative clinical picture.

An adaptation of the doses normally used should evidently be considered in elderly patients or in patients suffering from renal diseases, for which the excretory capacities would be partially compromised.

Warnings SIRIO ® - Melevodopa + Carbidopa

SIRIO ® therapy must necessarily be preceded by a careful neurological examination aimed at clarifying both the origin of the symptomatology and the prescriptive appropriateness of Levodopa.

Treatment must also be supervised by experienced medical personnel, in order to promptly identify signs and symptoms attributable to potential side effects of the therapy and reassess the adequacy of the doses and the therapy chosen.

Particular caution in the use of SIRIO ® should also be maintained in patients suffering from psychiatric disorders, psychotic disorders, cardiovascular, pulmonary, hepatic and renal diseases.

The patient receiving SIRIO ® should avoid the use of machinery or vehicle driving given the documented sleep attacks and the reduction of perceptive abilities that are widely documented following the use of Levodopa.

SIRIO ® contains lactose among its excipients, making it therefore contraindicated in patients with lactase enzyme deficiency, glucose-galactose malabsorption syndrome and galactosemia.

It is recommended to keep the medicine out of the reach of children.

PREGNANCY AND BREASTFEEDING

The aforementioned contraindications to the use of SIRIO ® also extend to pregnancy and the subsequent breastfeeding period given the absence of studies able to fully characterize the safety profile of its active ingredients for fetal and infant health .

Interactions

The patient receiving SIRIO ® should avoid the simultaneous intake of:

antihypertensive drugs for the risk of postural hypotension;
antidepressants, due to the potential side effects associated with the simultaneous intake of Levodopa;
Phenotiazines, phenytoin, papaverine and other active ingredients capable of altering the normal pharmacokinetic properties of Levodopa.

Contraindications SIRIO ® - Melevodopa + Carbidopa

The use of SIRIO ® is contraindicated in patients hypersensitive to the active ingredient 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

Despite the association with Carbidopa, it allows to significantly contain the potential side effects related to the intake of Levodopa, the use of SIRIO ® could determine the appearance of side effects such as nausea, vomiting, dizziness, psychiatric disorders, tachycardia, drowsiness and fatigue .

Fortunately, the incidence of clinically relevant side effects spread among the various organs and systems is rare, for which it is often necessary to adjust the dosage.

Continuous medical supervision therefore becomes necessary even in the face of the high incidence of the aforementioned adverse reactions.