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 Stalevo, Corbilta, Carlevent
AHFS/Drugs.com Professional Drug Facts
MedlinePlus a601068
License data
Pregnancy
category
Routes of
administration
By mouth
ATC code
Legal status
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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]

Contents

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

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] [ unreliable medical source? ]

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]

See also

Related Research Articles

<span class="mw-page-title-main">Carbidopa</span> Chemical compound

Carbidopa (Lodosyn) is a drug given to people with Parkinson's disease in order to inhibit peripheral metabolism of levodopa. This property is significant in that it allows a greater proportion of administered levodopa to cross the blood–brain barrier for central nervous system effect, instead of being peripherally metabolised into substances unable to cross said barrier.

<span class="mw-page-title-main">Selegiline</span> Monoamine oxidase inhibitor

Selegiline, also known as L-deprenyl and sold under the brand names Eldepryl, Zelapar, and Emsam among others, is a medication which is used in the treatment of Parkinson's disease and major depressive disorder. It has also been studied for a variety of other indications, but has not been formally approved for any other use. The medication in the form licensed for depression has modest effectiveness for this condition that is similar to that of other antidepressants. Selegiline is provided as a swallowed tablet or capsule or an orally disintegrating tablet (ODT) for Parkinson's disease and as a patch applied to skin for depression.

<span class="mw-page-title-main">Tetrabenazine</span> Medication for hyperkinetic movement disorders

Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorders. It is sold under the brand names Nitoman and Xenazine among others. On August 15, 2008, the U.S. Food and Drug Administration approved the use of tetrabenazine to treat chorea associated with Huntington's disease. Although other drugs had been used "off label," tetrabenazine was the first approved treatment for Huntington's disease in the U.S. The compound has been known since the 1950s.

Carbidopa/levodopa, also known as levocarb and co-careldopa, is the combination of the two medications carbidopa and levodopa. It is primarily used to manage the symptoms of Parkinson's disease, but it does not slow down the disease or stop it from getting worse. It is taken by mouth. It can take two to three weeks of treatment before benefits are seen. Each dose then begins working in about ten minutes to two hours with a duration of effect of about five hours.

<span class="mw-page-title-main">Dopaminergic</span> Substance related to dopamine functions

Dopaminergic means "related to dopamine", a common neurotransmitter. Dopaminergic substances or actions increase dopamine-related activity in the brain.

<span class="mw-page-title-main">Entacapone</span> Chemical compound

Entacapone, sold under the brand name Comtan among others, is a medication commonly used in combination with other medications for the treatment of Parkinson's disease. Entacapone together with levodopa and carbidopa allows levodopa to have a longer effect in the brain and reduces Parkinson's disease signs and symptoms for a greater length of time than levodopa and carbidopa therapy alone.

<span class="mw-page-title-main">Tolcapone</span> Chemical compound

Tolcapone, sold under the brand name Tasmar, is a medication used to treat Parkinson's disease (PD). It is a selective, potent and reversible nitrocatechol-type inhibitor of the enzyme catechol-O-methyltransferase (COMT). It has demonstrated significant liver toxicity, which has led to suspension of marketing authorisations in a number of countries.

<span class="mw-page-title-main">Rasagiline</span> Chemical compound

Rasagiline, sold under the brand name Azilect among others, is a medication which is used in the treatment of Parkinson's disease. It is used as a monotherapy to treat symptoms in early Parkinson's disease or as an adjunct therapy in more advanced cases. The drug is taken by mouth.

In the management of Parkinson's disease, due to the chronic nature of Parkinson's disease (PD), a broad-based program is needed that includes patient and family education, support-group services, general wellness maintenance, exercise, and nutrition. At present, no cure for the disease is known, but medications or surgery can provide relief from the symptoms.

Catechol-<i>O</i>-methyltransferase inhibitor Medication

A catechol-O-methyltransferase inhibitor is a drug that inhibits the enzyme catechol-O-methyltransferase. This enzyme methylates catecholamines such as dopamine, norepinephrine and epinephrine. It also methylates levodopa. COMT inhibitors are indicated for the treatment of Parkinson's disease in combination with levodopa and an aromatic L-amino acid decarboxylase inhibitor. The therapeutic benefit of using a COMT inhibitor is based on its ability to prevent the methylation of levodopa to 3-O-methyldopa, thus increasing the bioavailability of levodopa. COMT inhibitors significantly decrease off time in people with Parkinson's disease also taking carbidopa/levodopa.

<span class="mw-page-title-main">Droxidopa</span> Synthetic amino acid/norepinephrine prodrug

Droxidopa, also known as L-threo-dihydroxyphenylserine (L-DOPS) and sold under the brand names Northera and Dops among others, is sympathomimetic medication which is used in the treatment of hypotension and for other indications. It is taken by mouth.

<span class="mw-page-title-main">Levodopa</span>

Levodopa, also known as L-DOPA and sold under many brand names, is a dopaminergic medication which is used in the treatment of Parkinson's disease and certain other conditions. The drug is usually used and formulated in combination with carbidopa or benserazide. It is taken by mouth and certain other routes such as inhalation.

Aromatic <small>L</small>-amino acid decarboxylase inhibitor

An aromatic L-amino acid decarboxylase inhibitor (synonyms: DOPA decarboxylase inhibitor, extracerebral decarboxylase inhibitor, DDCI and AAADI) is a medication of type enzyme inhibitor which inhibits the synthesis of dopamine by the enzyme aromatic L-amino acid decarboxylase (AADC, AAAD, or DOPA decarboxylase). It is used to inhibit the decarboxylation of L-DOPA to dopamine outside the brain, i.e. in the blood. This is primarily co-administered with L-DOPA to combat Parkinson's disease. Administration can prevent common side-effects, such as nausea and vomiting, as a result of interaction with D2 receptors in the vomiting center (or cheomoreceptor trigger zone) located outside the blood–brain barrier.

<span class="mw-page-title-main">Safinamide</span> Reversible monoamine oxidase B inhibitor

Safinamide, sold under the brand name Xadago, is a medication used as treatment for Parkinson's disease with "off" episodes; it has multiple modes of action, including the inhibition of monoamine oxidase B.

Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less likely to cause sedation. These peripherally selective opioids can be used as antidiarrheals, for instance loperamide (Imodium).

<span class="mw-page-title-main">Opicapone</span> Chemical compound

Opicapone, sold under the brand name Ongentys, is a medication which is administered together with levodopa in people with Parkinson's disease. Opicapone is a catechol-O-methyltransferase (COMT) inhibitor.

Levodopa/benserazide, sold under the brand name Prolopa among others, is a fixed-dose combination medication used for the treatment of Parkinson's disease.

<span class="mw-page-title-main">Foscarbidopa/foslevodopa</span> Combination medication

Foscarbidopa/foslevodopa, sold under the brand name Vyalev, is a fixed-dose combination medication used for the treatment of Parkinson's disease. It is a combination of prodrugs for levodopa and carbidopa that was developed by AbbVie.

<span class="mw-page-title-main">Pharmacology of selegiline</span> Pharmacology of the antiparkinsonian and antidepressant selegiline

The pharmacology of selegiline pertains to the pharmacodynamic and pharmacokinetic properties of the antiparkinsonian and antidepressant selegiline (L-deprenyl). Selegiline is available in a few different forms, including oral tablets and capsules, orally disintegrating tablets (ODTs), and transdermal patches. These forms have differing pharmacological properties.

<span class="mw-page-title-main">Melevodopa/carbidopa</span> Combination dopaminergic medication

Melevodopa/carbidopa, sold under the brand name Sirio, is a combination of melevodopa, a prodrug of the dopamine precursor and hence non-selective dopamine receptor agonist levodopa (L-DOPA), and carbidopa, a peripherally selective aromatic L-amino acid decarboxylase (AAAD) inhibitor, which is used in the treatment of Parkinson's disease in Italy. It is taken orally in the form of tablets.

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. 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.
  6. 1 2 "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. 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.
  9. 1 2 "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): 255–269. doi: 10.3233/JPD-130186 . PMID   23948989.