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Entacapone

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Molecule Summary

Uses
Parkinson's disease
Therapy
Anti-Parkinsonian
Side Effects
Nausea, diarrhoea, abdominal pain, dry mouth, constipation, vomiting
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Molecule Description

Entacapone is a medicine used in adults with Parkinson's disease as an add-on to standard levodopa therapy. It helps manage "end-of-dose" motor fluctuations, which are periods during which symptoms such as stiffness, slowness, or tremors recur before the next scheduled levodopa dose. By improving the consistency of levodopa's effect, Entacapone helps patients maintain better control over their movements and daily activities. The medication works by blocking the enzyme catechol-O-methyltransferase (COMT). This enzyme normally breaks down levodopa in the body. By inhibiting COMT, Entacapone increases the amount and duration of levodopa in the bloodstream, which helps reduce the "off" periods when Parkinson's symptoms reappear and improves the overall effectiveness of levodopa therapy. Entacapone is usually administered with each levodopa dose, and it is important to follow the physician's instructions regarding timing and dosage. It should be taken with water and can be taken with or after food to reduce stomach upset. Consistent dosing helps maintain stable levodopa levels, reducing symptom fluctuations and improving patients' sense of control over their movements throughout the day. Some patients may experience side effects such as nausea, diarrhoea, abdominal pain, dry mouth, or constipation. Dizziness, sleepiness, or sudden sleep episodes can also occur, particularly when standing up quickly. Patients should be cautious about driving or operating machines until they know how the medicine affects them. Any unusual muscle pain, weakness, or dark urine should be reported to a doctor immediately. Entacapone interacts with certain other medications, including some antidepressants, iron supplements, and catechol-based medicines. It may slightly affect warfarin, a blood-thinning medicine, so monitoring is recommended. Maintaining hydration, a balanced diet, and avoiding abrupt changes in dose can help improve tolerance and effectiveness. Overall, Entacapone provides a valuable addition to levodopa therapy, helping patients with Parkinson's disease manage their symptoms more reliably.

Uses

Entacapone is used in adults with Parkinson's disease as an add-on to standard levodopa therapy (levodopa/carbidopa or levodopa/benserazide). It helps manage "end-of-dose" motor fluctuations, improving symptom control in patients who cannot achieve stable responses with levodopa combinations alone.

Contraindications

When should one not use Entacapone

  • If you are allergic to entacapone or any of the other ingredients of this medicine.
  • If you have liver problems or severe hepatic impairment.
  • If you have a tumour called pheochromocytoma.
  • If you are taking non-selective MAO inhibitors (e.g., phenelzine, tranylcypromine) at the same time as Entacapone.
  • If you are taking a combination of selective MAO-A and MAO-B inhibitors with Entacapone.
  • If you have a history of neuroleptic malignant syndrome (NMS) or unexplained muscle breakdown (rhabdomyolysis).

Side effects

Common side effects of this drug are:

  • Nausea
  • Diarrhoea
  • Abdominal pain
  • Dry mouth
  • Constipation
  • Vomiting

Precautions and Warnings

Pregnancy

Pregnancy

No, Entacapone should not be used during pregnancy. Always consult your doctor before using it.

Breast Feeding

Breast Feeding

No, Entacapone should not be used while breastfeeding, as it can pass into breast milk and its safety for infants is unknown. Always consult your doctor before using it.

Driving

Driving

Entacapone, when taken with levodopa, may cause dizziness, sleepiness, or sudden sleep episodes. Avoid driving or operating machines until you know how the medicine affects you and any symptoms have resolved.

Alcohol

Alcohol

Drinking alcohol while taking Entacapone may increase side effects such as dizziness, drowsiness, or sudden sleep episodes. It is best to avoid or limit alcohol while on this medicine.

Other General Warnings

Other General Warnings

Talk to your doctor if
  • You have a history of muscle breakdown (rhabdomyolysis) or neuroleptic malignant syndrome (NMS).
  • You have heart problems, including ischaemic heart disease or low blood pressure when standing (orthostatic hypotension).
  • You are taking medicines that affect catecholamines (e.g., adrenaline, dopamine, dobutamine, alpha-methyldopa, apomorphine).
  • You are on levodopa or other Parkinson's medicines, as dose adjustments may be needed to reduce side effects.
  • You experience severe or persistent diarrhoea, as this may indicate colitis or lead to excessive weight loss.
  • You develop impulse control problems, such as compulsive gambling, increased sexual drive, binge eating, or compulsive shopping.
  • You experience rapid weight loss, loss of appetite, or general weakness, liver function and overall health should be assessed.
  • You have a rare sugar-metabolism disorder (e.g., fructose intolerance, glucose-galactose malabsorption, sucrase-isomaltase deficiency), as this medicine contains sucrose.
  • You feel very sleepy or suddenly fall asleep during the day, you should avoid driving or operating machinery.

Mode of Action

How Does It Work?

Entacapone works by inhibiting the enzyme catechol-O-methyltransferase (COMT). This enzyme normally breaks down levodopa in the body. By inhibiting COMT, entacapone increases the amount and duration of levodopa available in the bloodstream, thereby improving control of Parkinson's disease symptoms, reducing "off" periods, and enhancing the effectiveness of levodopa therapy.

Interactions

Interactions with other medicines

  • No interactions have been observed between Entacapone and carbidopa at the recommended doses. Interaction with benserazide has not been studied.
  • No significant interactions were seen in studies with imipramine, moclobemide, or selegiline, though caution is advised when combining Entacapone with MAO-A inhibitors, tricyclic antidepressants, noradrenaline reuptake inhibitors (e.g., desipramine, maprotiline, venlafaxine), or catechol-based medicines (e.g., rimiterol, isoprenaline, adrenaline, noradrenaline, dopamine, dobutamine, alpha-methyldopa, apomorphine, paroxetine).
  • Entacapone can be used with selegiline (a selective MAO-B inhibitor) if the daily dose of selegiline does not exceed 10 mg.
  • Entacapone may bind to iron in the gut; take iron supplements at least 2–3 hours apart from this medicine.
  • Entacapone may bind to the same protein sites as medicines like diazepam or ibuprofen, but no significant interactions are expected at normal doses.
  • Entacapone may slightly affect medicines metabolized by CYP2C9, such as warfarin; blood clotting tests (INR) should be monitored when starting Entacapone.

Interactions with food items

  • Avoid taking Entacapone concurrently with iron supplements, as it can reduce absorption; leave at least 2–3 hours between them.
  • There are no significant interactions with other foods, but maintaining a balanced diet supports overall treatment effectiveness.
  • Drink adequate water while taking Entacapone to help absorption and reduce digestive discomfort.
  • Grapefruit or grapefruit juice is not expected to significantly affect Entacapone, but it's generally better to avoid large amounts of grapefruit with any Parkinson's medications.

Dosage

Overdose

If you think you have taken too much of this medicine, contact your doctor immediately or visit the nearest hospital.

Missed a Dose

If you miss any dose of Entacapone, take it as soon as you remember with food. However, if it is time for the next dose, then skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Frequently Asked Questions (FAQs)

Entacapone is used in adults with Parkinson's disease as an add-on to levodopa therapy. It helps reduce "end-of-dose" symptom fluctuations, improving control over movements, stiffness, and tremors.

Common side effects include nausea, diarrhoea, abdominal pain, dry mouth, constipation, dizziness, and drowsiness. Some people may experience sudden sleep episodes, especially when standing up quickly.

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