 | |
| Combination of | |
|---|---|
| Carbidopa | DOPA decarboxylase inhibitor |
| Levodopa | dopamineprecursor |
| Entacapone | catechol-O-methyltransferase inhibitor |
| Clinical data | |
| Trade names | Carlevent, Corbilta, L.C.E. Sandoz, Lecigon, Lecteva, Stalevo |
| AHFS/Drugs.com | Professional Drug Facts |
| MedlinePlus | a601068 |
| License data | |
| Pregnancy category | |
| Routes of administration | oral,subcutaneous,intravenous, intrajejunal infusion[2] |
| ATC code | |
| Legal status | |
| Legal status | |
| Identifiers | |
| CAS Number | |
| PubChemCID | |
| ChemSpider |
|
| KEGG | |
Carbidopa/levodopa/entacapone, sold under the brand nameStalevo among others, is adopaminergicfixed-dose combination medication that containscarbidopa,levodopa, andentacapone for the treatment ofParkinson's disease.[6]
Carbidopa/levodopa/entacapone is indicated for the treatment ofParkinson's disease.[6]
In the European Union it isindicated for the treatment of adults with Parkinson's disease and end-of-dose motor fluctuations not stabilized on levodopa/dopa decarboxylase inhibitor treatment.[7]
Sometimes a wearing off effect may occur at the end of the dosing interval, where a patient may feel Parkinson's symptoms. Urine, saliva, or sweat may be discolored (dark color such as red, brown, or black) after taking carbidopa/levodopa/entacapone.[9]
Carbidopa/levodopa/entacapone is contraindicated in patients taking a class ofantidepressant drugs known asnon-selective monoamine oxidase (MAO) inhibitors such asphenelzine andtranylcypromine.[10]
Carbidopa/levodopa/entacapone may be combined with the drugsrasagiline orselegiline. These drugs are a different type of MAO inhibitor known asselective MAO inhibitors that are often prescribed for Parkinson's disease.[9] Many drug interactions involving selegiline are theoretical, primarily based on interactions with non-selective MAO inhibitors; at oral doses the risk of these interactions may be very low. However,transdermal selegiline, known by its trade nameEmsam, is stillcontraindicated.[10] Transdermal selegiline results inhigher plasma levels at which it behaves like a non-selective MAO inhibitor.Concominant use of entacapone, a component of carbidopa/levodopa/entacapone, with MAO inhibitors may increase toxicity of MAO inhibitors. Levodopa, also a component of carbidopa/levodopa/entacapone, in combination with MAO inhibitors may result inhypertensive reactions.[11]
Levodopa is the immediateprecursor to dopamine. Entacapone is a selective, reversiblecatechol-O-methyltransferase (COMT) inhibitor that prevents the degradation of levodopa. Entacapone does not cross theblood–brain barrier. Carbidopa is aperipheralaromatic L-amino acid decarboxylase (AADC) inhibitor. It does not cross the blood–brain barrier, either, and therefore does not interfere with levodopa metabolism in the CNS. By inhibiting dopa decarboxylase, carbidopa prevents the conversion of levodopa to dopamine in the PNS, increasing the amount of levodopa delivered to the CNS.[12]
Carbidopa/levodopa/entacapone oral drug was approved for medical use in the United States in June 2003.[13][14] Levodopa-entacapone-carbidopa intestinal gel (LECIG) was first approved in Sweden in 2018,[15] followed by Denmark, Finland, and Norway in 2019, Austria, Belgium, Germany, the Netherlands, Romania, and Slovenia in 2020.[16]
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