Carbidopa/levodopa/entacapone

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Carbidopa/levodopa/entacapone
Stalevo.jpg
Combination of
Carbidopa DOPA decarboxylase inhibitor
Levodopa dopamine precursor
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
PubChem CID
ChemSpider
  • none
KEGG

Carbidopa/levodopa/entacapone, sold under the brand name Stalevo among others, is a dopaminergic fixed-dose combination medication that contains carbidopa, levodopa, and entacapone for the treatment of Parkinson's disease. [6]

Contents

Medical uses

Carbidopa/levodopa/entacapone is indicated for the treatment of Parkinson's disease. [6]

In the European Union it is indicated for the treatment of adults with Parkinson's disease and end-of-dose motor fluctuations not stabilized on levodopa/dopa decarboxylase inhibitor treatment. [7]

Side effects

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]

Drug interactions

Carbidopa/levodopa/entacapone is contraindicated in patients taking a class of antidepressant drugs known as non-selective monoamine oxidase (MAO) inhibitors such as phenelzine and tranylcypromine. [10]

Carbidopa/levodopa/entacapone may be combined with the drugs rasagiline or selegiline. These drugs are a different type of MAO inhibitor known as selective 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 name Emsam, is still contraindicated. [10] Transdermal selegiline results in higher 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 in hypertensive reactions. [11]

Mechanism of action

Carbidopa/levodopa/entercapone's pathway Levodopa metabolism 2.png
Carbidopa/levodopa/entercapone's pathway

Levodopa is the immediate precursor to dopamine. Entacapone is a selective, reversible catechol-O-methyltransferase (COMT) inhibitor that prevents the degradation of levodopa. Entacapone does not cross the blood–brain barrier. Carbidopa is a peripheral aromatic 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]

Society and culture

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]

References

  1. ↑ "Carbidopa / entacapone / levodopa Use During Pregnancy". Drugs.com. 14 October 2019. Archived from the original on 28 November 2020. Retrieved 19 May 2020.
  2. ↑ "The device-aided intrajejunal delivery of levodopa–entacapone–carbidopa intestinal gel the treatment of Parkinson's disease: overview of efficacy and safety". Expert Review of Medical Devices. 9 September 2019. Retrieved 14 November 2025.
  3. ↑ "Stalevo 75/18.75/200 levodopa/carbidopa (as monohydrate)/entacapone tablet bottle (160686)". Therapeutic Goods Administration (TGA). 27 May 2022. Retrieved 30 April 2023.
  4. ↑ "Carlevent levodopa/carbidopa/entacapone 100/25/200 mg tablet bottle (195747)". Therapeutic Goods Administration (TGA). 26 May 2022. Retrieved 1 May 2023.
  5. ↑ "Stalevo 100 mg/25 mg/200 mg Film-coated Tablets - Summary of Product Characteristics (SmPC)". (emc). 9 September 2019. Archived from the original on 2 December 2021. Retrieved 19 May 2020.
  6. 1 2 3 "Stalevo- carbidopa, levodopa, and entacapone tablet, film coated". DailyMed. 30 July 2021. Archived from the original on 6 December 2021. Retrieved 1 May 2023.
  7. 1 2 "Stalevo EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 31 October 2020. Retrieved 25 May 2020.
  8. ↑ "Corbilta". European Medicines Agency (EMA). 16 January 2023. Archived from the original on 3 February 2023. Retrieved 1 May 2023.
  9. 1 2 "Carbidopa, entacapone, and levodopa Advanced Patient Information". Drugs.com. 9 December 2022. Archived from the original on 5 July 2022. Retrieved 1 May 2023.
  10. 1 2 "Stalevo: Dosing, contraindications, side effects, and pill pictures". Epocrates Online. Archived from the original on 5 February 2022. Retrieved 30 April 2023.
  11. ↑ Leikin JB, Paloucek FP (2007). Poisoning and toxicology handbook (4th ed.). Informa Health Care. p. 610. ISBN   978-1-4200-4479-9. Archived from the original on 1 May 2023. Retrieved 6 December 2020.
  12. ↑ Miyaue N, Nagai M. "Sex differences in the pharmacokinetics of levodopa and carbidopa in patients with Parkinson's disease". Parkinsonism & Related Disorders. 139 108006. doi:10.1016/j.parkreldis.2025.108006.
  13. ↑ "Drug Approval Package: Stalevo 50, 100 & 150 (carbidopa/ levodopa/ entacapone) Tablets NDA #021485". U.S. Food and Drug Administration (FDA). Archived from the original on 7 April 2021. Retrieved 1 May 2023.
  14. ↑ "Carbidopa, entacapone, and levodopa Uses, Side Effects & Warnings". Drugs.com. 4 October 2022. Archived from the original on 13 January 2023. Retrieved 1 May 2023.
  15. ↑ Öthman M, Widman E, Nygren I, Nyholm D (March 2021). "Initial Experience of the Levodopa-Entacapone-Carbidopa Intestinal Gel in Clinical Practice". Journal of Personalized Medicine. 11 (4): 254. doi: 10.3390/jpm11040254 . PMC   8067183 . PMID   33807308.
  16. ↑ Auffret M, Weiss D, Stocchi F, Vérin M, Jost WH (November 2023) [2023-07-12]. "Access to device-aided therapies in advanced Parkinson's disease: navigating clinician biases, patient preference, and prognostic uncertainty". Journal of Neural Transmission. 130 (11): 1411–1432. doi:10.1007/s00702-023-02668-9. PMC   10645670 . PMID   37436446.
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