Stalevo

Antiparkinsonian Drug

Drug class: Dopaminergic Antiparkinsonian Agent and is categorized as a combination of decarboxylase inhibitors and Catechol-O-methyltransferase Inhibitor, COMT Inhibitor

Carbidopa, Etacapon and Levodopa (STALEVO)（中文：美金剛）

Pronunciation

Stalevo 100mg

Common Strengths of Stalevo

Stalevo is available in six strengths, each containing a specific ratio of its components:

• Stalevo 50: 12.5 mg carbidopa, 50 mg levodopa, 200 mg entacapone
• Stalevo 75: 18.75 mg carbidopa, 75 mg levodopa, 200 mg entacapone
• Stalevo 100: 25 mg carbidopa, 100 mg levodopa, 200 mg entacapone
• Stalevo 125: 31.25 mg carbidopa, 125 mg levodopa, 200 mg entacapone
• Stalevo 150: 37.5 mg carbidopa, 150 mg levodopa, 200 mg entacapone
• Stalevo 200: 50 mg carbidopa, 200 mg levodopa, 200 mg entacapone

Drug Trade Name

The primary trade name for this medication is Stalevo.

Drug Usage

Stalevo is used to treat symptoms of Parkinson's disease, including tremors, stiffness, and difficulty with movement. It dose not cure the disease but helps manage its symptoms.

Mechanism of Action

Stalevo consists of three active ingredients: carbidopa, levodopa, and entacapone.

The mechanism involves:

• Levodopa converting to dopamine in the brain.
• Carbidopa prevents the premature conversion of levodopa to dopamine outside the brain.
• Entacpone inhibits the COMT enzyme to prolong the effect of levodopa by preventing its breakdown.

Route of Administration

Stalevo is administered orally, typically as a film-coated tablet.

Dosages

Dosage adjustments depend on individual patient needs and conditions.

Side Effects

Frequency	Adverse reactions
Common Side Effects	Nausea
	Dizziness
	Dyskinesia
Serious Side Effects	Neuroleptic Malignant Syndrome (NMS)
	Severe allergic reactions
	Dark discoloration of urine or sweat

Pharmacokinetics

The pharmacokinetics of Stalevo show:

• Peak concentrations for carbidopa at approximately 2.5 to 3.4 hours, while entacapone peaks at about 0.8 to 1.2 hours post-administration.
• The duration of action can vary but generally lasts several hours depending on individual metabolism and dosage.

Drug Precautions

Pregnancy

Stalevo falls under Category C; risks versus benefits should be evaluated before use during pregnancy.

Breastfeeding

Caution is advised; consult a healthcare provider regarding risk to the infant.

Drug Monitoring Items

Regular monitoring includes:

• Blood pressure checks
• Renal function tests (eGFR)
• Monitoring for dyskinesias or other movement disorders, may occur or worsen with Stalevo. Regular assessments are necessary to determine if dosage adjustments are needed.
• Mental Health Monitoring: Patients should be closely observed for mental changes, including depression and suicidal tendencies.
• Impulse Control Disorders: Patients and caregivers should be informed about the risk of impulse control disorders, which can manifest as compulsive behaviors such as gambling or eating.
• INR Monitoring: For patients on warfarin, monitoring of INR levels is recommended when initiating Stalevo therapy due to potential interaction

Drug Interactions

Notable interaction include:

• Contraindications with MAO Inhibitors: Concurrent use with non-selective MAO inhibitors (like phenelzine) can lead to severe hypertension.
• Dopamine Antagonists: Medications such as antipsychotics and antiemetics may reduce the effectiveness of Stalevo.
• Tricyclic Antidepressants: These can increase the risk of hypertension and dyskinesia when used alongside Stalevo.
• Phenytoin and Papaverine: These drugs may diminish the therqpeutic efects of levodopa.

Food interactions:

• High-protein meals can impair the absorption of levodopa.
• Alcohol may exacerbate side effects like dizziness or drowsiness.

FAQ

How Should I Take the Tablet?

Usually with food to minimize gastrointestinal upset.

What Should I Avoid While Taking?

Avoid consuming high-protein meals close to dosing time as they may interfere with the absorption of levodopa.

What Happens if I Miss a Dose?

If you miss a dose, take it as soon as you remember unless it is close to the time for your next dose; do not double up on doses.