Carbidopa/levodopa/entacapone explained

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.[1]

Medical uses

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

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.[2]

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.

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.[3]

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.[4] 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. 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.[5]

Mechanism of action

See main article: 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.[6]

Society and culture

Legal status

Carbidopa/levodopa/entacapone was approved by the US Food and Drug Administration (FDA) in June 2003.[7] [8]

Research

It may help decrease a change of response to Parkinson's medications.[9]

External links

Notes and References

  1. Web site: Stalevo- carbidopa, levodopa, and entacapone tablet, film coated . DailyMed . 30 July 2021 . 1 May 2023 . 6 December 2021 . https://web.archive.org/web/20211206095857/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=53c488d8-4146-7563-8021-d90c931d1a95 . live .
  2. Web site: Stalevo EPAR . European Medicines Agency (EMA) . 17 September 2018 . 25 May 2020 . 31 October 2020 . https://web.archive.org/web/20201031022927/https://www.ema.europa.eu/en/medicines/human/EPAR/stalevo . live .
  3. Web site: Stalevo: Dosing, contraindications, side effects, and pill pictures . Epocrates Online . 30 April 2023 . 5 February 2022 . https://web.archive.org/web/20220205031541/https://online.epocrates.com/noFrame/showPage.do?method=drugs&MonographId=3518&ActiveSectionId=4 . live .
  4. Web site: Carbidopa, entacapone, and levodopa Advanced Patient Information . Drugs.com . 9 December 2022 . 1 May 2023 . 5 July 2022 . https://web.archive.org/web/20220705134423/https://www.drugs.com/cons/carbidopa-entacapone-and-levodopa.html . live .
  5. Book: Leikin JB, Paloucek FP . 2007 . Poisoning and toxicology handbook . 4th . Informa Health Care . 610 . 978-1-4200-4479-9 . 2020-12-06 . 2023-05-01 . https://web.archive.org/web/20230501030554/https://books.google.com/books?id=0Bw2UJTC_uMC&pg=PP1 . live .
  6. Web site: Drug Reference for FDA Approved Parkinson's Disease Drugs . Redirecting . 1 May 2023 . 7 December 2022 . https://web.archive.org/web/20221207133304/https://www.neurotransmitter.net/parkinsons_drug_reference.html . live .
  7. Web site: Drug Approval Package: talevo 50, 100 & 150 (carbidopa/ levodopa/ entacapone) NDA #021485 . U.S. Food and Drug Administration (FDA) . 1 May 2023 . 7 April 2021 . https://web.archive.org/web/20210407091242/https://www.accessdata.fda.gov/drugsatfda_docs/nda/2003/21-485_Stalevo.cfm . live .
  8. Web site: Carbidopa, entacapone, and levodopa Uses, Side Effects & Warnings . Drugs.com . 4 October 2022 . 1 May 2023 . 13 January 2023 . https://web.archive.org/web/20230113160358/https://www.drugs.com/mtm/carbidopa-entacapone-and-levodopa.html . live .
  9. Salat D, Tolosa E . Levodopa in the treatment of Parkinson's disease: current status and new developments . Journal of Parkinson's Disease . 3 . 3 . 255–269 . January 2013 . 23948989 . 10.3233/JPD-130186 . free .