Carbidopa/levodopa/entacapone

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.[5]

Carbidopa/levodopa/entacapone
Combination of
CarbidopaDOPA decarboxylase inhibitor
Levodopadopamine precursor
Entacaponecatechol-O-methyltransferase inhibitor
Clinical data
Trade namesStalevo, Corbilta, Carlevent
AHFS/Drugs.comProfessional Drug Facts
MedlinePlusa601068
License data
Pregnancy
category
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
ChemSpider
  • none
KEGG
  (verify)

Medical uses

Carbidopa/levodopa/entacapone is indicated for the treatment of Parkinson's disease.[5]

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 (DDC) inhibitor treatment.[6]

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.[8]

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.[9]

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.[8] 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.[9] 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.[10]

Mechanism of action
Main articles: Levodopa, Carbidopa, and Entacapone

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. Carbidopa, which also does not cross the blood–brain barrier, is combined with levodopa to prevent its conversion to dopamine in the periphery.[11]

Society and culture

Carbidopa/levodopa/entacapone was approved by the US Food and Drug Administration (FDA) in June 2003.[12][13]

Research

It may help decrease a change of response to Parkinson's medications.[14]

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. "Stalevo 75/18.75/200 levodopa/carbidopa (as monohydrate)/entacapone tablet bottle (160686)". Therapeutic Goods Administration (TGA). 27 May 2022. Retrieved 30 April 2023.
  3. "Carlevent levodopa/carbidopa/entacapone 100/25/200 mg tablet bottle (195747)". Therapeutic Goods Administration (TGA). 26 May 2022. Retrieved 1 May 2023.
  4. "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.
  5. "Stalevo- carbidopa, levodopa, and entacapone tablet, film coated". DailyMed. 30 July 2021. Archived from the original on 6 December 2021. Retrieved 1 May 2023.
  6. "Stalevo EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 31 October 2020. Retrieved 25 May 2020.
  7. "Corbilta". European Medicines Agency (EMA). 16 January 2023. Archived from the original on 3 February 2023. Retrieved 1 May 2023.
  8. "Carbidopa, entacapone, and levodopa Advanced Patient Information". Drugs.com. 9 December 2022. Archived from the original on 5 July 2022. Retrieved 1 May 2023.
  9. "Stalevo: Dosing, contraindications, side effects, and pill pictures". Epocrates Online. Archived from the original on 5 February 2022. Retrieved 30 April 2023.
  10. 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 2023-05-01. Retrieved 2020-12-06.
  11. "Drug Reference for FDA Approved Parkinson's Disease Drugs". Redirecting. Archived from the original on 7 December 2022. Retrieved 1 May 2023.
  12. "Drug Approval Package: talevo 50, 100 & 150 (carbidopa/ levodopa/ entacapone) NDA #021485". U.S. Food and Drug Administration (FDA). Archived from the original on 7 April 2021. Retrieved 1 May 2023.
  13. "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.
  14. Salat D, Tolosa E (January 2013). "Levodopa in the treatment of Parkinson's disease: current status and new developments". Journal of Parkinson's Disease. 3 (3): 255–69. doi:10.3233/JPD-130186. PMID 23948989.
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