Entacapone

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Generic Name of Entacapone - Learn More

Entacapone

Entacapone Precaution - What You Need to Know

Entacapone is a medication primarily used in the treatment of Parkinson’s disease, often as an adjunct to levodopa/carbidopa therapy. Several precautions should be considered when prescribing entacapone:

- Pregnancy and Breastfeeding: Entacapone is classified as a category C drug during pregnancy, meaning that there are no well-controlled studies in humans, but potential benefits may outweigh risks in certain situations. It should only be used during pregnancy if absolutely necessary, and the risks versus benefits should be evaluated. As for breastfeeding, entacapone is excreted into human milk, and its use should be avoided unless the benefit justifies the potential risk to the infant.

- Hepatic Impairment: Entacapone is metabolized in the liver, so it should be used with caution in patients with liver disease. In particular, patients with severe hepatic impairment should avoid entacapone due to potential accumulation and increased side effects. Dose adjustments are recommended in patients with mild to moderate liver dysfunction.

- Monitoring Parameters: Regular monitoring of liver function tests, including ALT and AST, should be done during entacapone therapy. Additionally, patients should be monitored for any signs of dyskinesia (excessive involuntary movements), which can occur due to the increased levodopa bioavailability.

- Potential Misuse or Dependency: There is no significant risk of misuse or dependency with entacapone. However, improper use, especially with levodopa, could lead to a higher-than-normal concentration of levodopa, which may cause excessive side effects like nausea, confusion, or dyskinesia.

Entacapone Indication - Uses and Benefits

Entacapone is primarily indicated as an adjunct therapy in the treatment of Parkinson’s disease, particularly for patients who experience the wearing-off effect with levodopa therapy.

- Parkinson’s Disease: Entacapone is used to increase the effectiveness of levodopa by inhibiting the COMT (catechol-O-methyltransferase) enzyme, which normally breaks down levodopa before it can exert its full therapeutic effect. By inhibiting this enzyme, entacapone prolongs the action of levodopa, reducing the "off" times in patients and improving motor symptoms.

- Wearing-Off Effect: It is particularly beneficial in patients who experience motor fluctuations where the effects of levodopa wear off before the next dose is due. Entacapone helps smooth these fluctuations and extend the "on" time where the patient experiences improved motor control.

- Off-label Uses: While the primary use is for Parkinson’s disease, entacapone has also been studied in various other neurodegenerative conditions, but it has not been officially approved for these uses. There is some evidence suggesting its potential role in managing symptoms in conditions like progressive supranuclear palsy, though it is not a standard treatment.

Entacapone Contraindications - Important Warnings

There are specific conditions where entacapone should not be used due to safety concerns.

- Hypersensitivity to Entacapone or Related Compounds: Patients who have a known allergy to entacapone or other drugs in the COMT inhibitor class should avoid using this medication.

- Severe Liver Disease: Entacapone should not be used in patients with severe hepatic impairment, as the drug is metabolized by the liver, and in these patients, the risk of toxicity due to reduced clearance is higher.

- Narrow-Angle Glaucoma: Although not a direct contraindication, caution should be taken in patients with narrow-angle glaucoma due to the potential for exacerbation of the condition.

- Melanoma: As with other dopaminergic treatments, entacapone may be associated with a risk of melanoma. Thus, it should be used with caution in patients with a history of melanoma or those at high risk for skin cancer.

Entacapone Side Effects - What to Expect

Like all medications, entacapone can cause side effects, although not everyone will experience them.

- Common Side Effects:
- Dyskinesia: Involuntary movements, particularly in the limbs and face, are a known side effect of entacapone due to its enhancement of levodopa effects.
- Nausea and Vomiting: These are common side effects when levodopa doses are adjusted, especially in combination with entacapone.

- Serious Side Effects:
- Hepatotoxicity: In rare cases, entacapone can lead to liver injury. Symptoms like jaundice, dark urine, or unexplained fatigue should prompt immediate discontinuation of the medication and evaluation of liver function.
- Orthostatic Hypotension: Some patients may experience a drop in blood pressure when standing, leading to dizziness or fainting. This can be managed with dose adjustments and monitoring.

- Long-term Effects: Long-term use of entacapone, particularly with levodopa, may increase the risk of developing melanin-related conditions like melanoma. Regular dermatological checkups are recommended.

Entacapone Pregnancy Category ID - Safety Information

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Entacapone Mode of Action - How It Works

Entacapone exerts its therapeutic effects by inhibiting catechol-O-methyltransferase (COMT), an enzyme responsible for the breakdown of levodopa in the peripheral circulation.

- Pharmacodynamics: By inhibiting COMT, entacapone prevents the methylation of levodopa into its inactive metabolite 3-O-methyldopa, thereby increasing the amount of levodopa available to cross the blood-brain barrier. This results in prolonged and enhanced effects of levodopa on the central nervous system, improving motor symptoms in patients with Parkinson’s disease.

- Pharmacokinetics: Entacapone is rapidly absorbed and reaches peak plasma concentration within 1 hour of administration. It has a half-life of about 1.5 hours, which supports its dosing schedule alongside levodopa/carbidopa. Entacapone is extensively metabolized by the liver, and its metabolites are excreted primarily in the urine.

Entacapone’s mechanism of action is particularly beneficial in the management of Parkinson’s disease as it enhances levodopa’s therapeutic effect while mitigating the "wearing-off" phenomenon seen with levodopa therapy alone.

Entacapone Drug Interactions - What to Avoid

Entacapone can interact with several other drugs, particularly those that affect dopamine metabolism or have central nervous system (CNS) effects.

- Levodopa: The most significant interaction is with levodopa, as entacapone enhances the bioavailability of levodopa by inhibiting its breakdown. While this is a desired effect, it can increase the risk of levodopa-induced side effects, such as nausea, dizziness, and dyskinesia. Close monitoring is needed to adjust levodopa doses accordingly.

- Other Antihypertensive Medications: Entacapone may lower blood pressure in some patients, especially when used with other antihypertensive medications. This can result in orthostatic hypotension or dizziness.

- MAO Inhibitors: Entacapone should not be taken with monoamine oxidase inhibitors (MAOIs), as this combination may increase the risk of hypertensive crises due to excess catecholamines.

- Iron Supplements: Iron may reduce the absorption of entacapone, so it is advised to take iron supplements and entacapone at different times of the day, if possible.

- Food and Alcohol: There are no major food interactions with entacapone, but alcohol may increase the risk of CNS side effects like dizziness or drowsiness. Caution should be exercised with alcohol consumption.

Entacapone Adult Dose - Recommended Dosage

The typical adult dose of entacapone is 200 mg taken with each dose of levodopa/carbidopa, up to a maximum of 8 doses (1600 mg) per day.

- For Parkinson’s Disease: Entacapone is administered orally with levodopa and carbidopa, typically as 200 mg with each dose of levodopa. If needed, the dose can be adjusted based on the clinical response.

- Dosing Adjustments: The dose of entacapone should be adjusted based on the response to levodopa, and the total daily dose of levodopa should be considered when adjusting entacapone.

Entacapone Child Dose - Dosage for Children

Entacapone is not recommended for use in pediatric patients due to a lack of safety and efficacy data in this population. There is insufficient evidence to support its use in children under 18 years of age, and it is not approved for pediatric indications.

Entacapone Renal Dose - Dosage for Kidney Conditions

Renal impairment does not significantly affect the pharmacokinetics of entacapone, so no dose adjustment is necessary in patients with mild to moderate renal impairment. However, it is still important to monitor renal function periodically.

- Severe Renal Impairment: In patients with severe renal impairment (creatinine clearance less than 30 mL/min), entacapone should be used with caution, as there may be an increased risk of drug accumulation.