entacapone/levodopa/carbidopa

Action and Spectrum

Actions and Spectrum:

Actions:

• Increasing dopamine levels: Levodopa is converted into dopamine in the brain, which helps to improve motor function and reduce tremors and stiffness.
• Enhancing the effectiveness of levodopa: Carbidopa is included in the combination to prevent the breakdown of levodopa in the bloodstream, which enhances its effectiveness in reaching the brain and improving symptoms.

Spectrum of benefits:

• Improving motor function: The combination of entacapone, levodopa, and carbidopa can help to improve motor function, reducing tremors, stiffness, and difficulty with coordination and balance.
• Reducing the risk of “on-off” episodes: The combination of entacapone, levodopa, and carbidopa can help to reduce the risk of “on-off” episodes, which are periods of time when the medication is not effective in controlling symptoms.

Drug Interaction

Adverse Reaction

Frequency Defined

>10% 

Entacapone 

• Dyskinesia (25%)
• Diarrhea (10%)
• Nausea (14%)
• Urine discoloration (10%)
• Hyperkinesia (10%)

1-10% 

Entacapone 

• Increased sweating (2%)
• Abdominal pain (8%)
• Back pain (4%)
• Hypokinesia (9%)
• Purpura (2%)
• Bacterial infection (1%)
• Dyspnea (3%)

Frequency Not Defined 

Levodopa/Carbodopa 

• Agitation
• insouciance
• Alopecia
• Edema
• Abdominal pain
• Muscular spasms
• Urinary incontinence
• oculogyric problems

Entacapone 

• Confusion
• Insomnia
• Postural hypotension

Black Box Warning

Black Box Warning

The black box warning for entacapone/levodopa/carbidopa (also known as Stalevo) is related to the risk of developing melanoma (skin cancer).

Contraindication / Caution

Contraindication/Caution:

Contraindications: 

• Hypersensitivity to any of the ingredients in the medication
• Severe liver problems
• Pregnancy or breastfeeding

Cautions: 

• Patients with a history of depression, mental illness, or suicidal thoughts should use this medication with caution.
• Patients with uncontrolled narrow-angle glaucoma should not use this medication.
• Patients with high blood pressure, heart problems, or a history of stroke should use this medication with caution.

Patients with a history of skin or eye pigmentation changes should use this medication with caution. 

Pregnancy / Lactation

Pregnancy warnings:   

Pregnancy category: N/A

Lactation: Excreted into human milk is known

Pregnancy Categories:     

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

entacapone/levodopa/carbidopa is a combination medication used in the treatment of Parkinson’s disease.

Pharmacodynamics:

The pharmacology of this medication is based on the action of its three active ingredients:

• Entacapone: Entacapone is a catechol-O-methyltransferase (COMT) inhibitor. It works by preventing the breakdown of dopamine, a neurotransmitter that is important for controlling movement. By increasing the amount of dopamine available in the brain, entacapone can help to improve motor symptoms in Parkinson’s disease.
• Levodopa: Levodopa is converted into dopamine in the brain and is used to replace the dopamine that is lost in Parkinson’s disease. Levodopa is the most effective medication for treating the symptoms of Parkinson’s disease, but it can become less effective over time.
• Carbidopa: Carbidopa is a peripheral decarboxylase inhibitor. It works by preventing the breakdown of levodopa in the peripheral tissues, which can increase the amount of levodopa that reaches the brain and improve its effectiveness.

Pharmacokinetics:

Absorption 

entacapone/levodopa/carbidopa is usually taken orally, in tablet form. The medication is absorbed into the bloodstream through the digestive system. 

Distribution 

Once absorbed, the medication is distributed throughout the body, including the brain where it is needed to treat Parkinson’s disease. 

Metabolism 

entacapone is metabolized by the liver, while levodopa and carbidopa are metabolized in the bloodstream. 

Elimination and Excretion 

entacapone and its metabolites are excreted primarily through the kidneys, while Levodopa and Carbidopa are excreted through the urine.

Adminstartion

Administration:

Orally administration

entacapone/levodopa/carbidopa is a combination medication used to treat the symptoms of Parkinson’s disease. It is usually taken orally, in tablet or capsule form. The administration of Entacapone/Levodopa/Carbidopa involves the following steps:

• Determining the dosage: The dosage of Entacapone/Levodopa/Carbidopa is usually determined by a healthcare provider and may vary depending on the severity of symptoms and the patient’s response to the medication.
• Taking the medication: The patient should take the medication as directed by their healthcare provider, usually with or without food. They should not crush or chew the tablets or capsules, as this may affect the effectiveness of the medication.
• Monitoring symptoms: The patient should monitor their symptoms and report any changes to their healthcare provider. If the medication is not effective in reducing symptoms, the dosage may need to be adjusted.

Patient Information Leaflet

Patient information leaflet

Generic Name: entacapone/levodopa/carbidopa

Why do we use entacapone/levodopa/carbidopa?

entacapone/levodopa/carbidopa is a combination medication used to treat the symptoms of Parkinson’s disease. Parkinson’s disease is a progressive disorder that affects movement, causing symptoms such as tremors, stiffness, and difficulty with coordination and balance.