Stalevo is an oral drug formulation developed by Novartis that contains a combination of three different drugs — carbidopa, levodopa and entacapone — to treat Parkinson’s disease. The three work together to boost the amount of dopamine in the brain, thereby relieving the symptoms of Parkinson’s.

How Stalevo works

Levodopa in Stalevo is a precursor of dopamine, which can cross the blood-brain barrier and be converted into dopamine in the brain.

When levodopa is administered orally, it is rapidly broken down by a biological process called decarboxylation that limits the amount reaching the brain. This is prevented by carbidopa, a dopa decarboxylase inhibitor, which inhibits the decarboxylation of levodopa, making more levodopa available for the brain.

Levodopa is also broken down by another process called methylation. This is prevented by entacapone, a selective inhibitor of the methylating enzyme called catechol-O-methyltransferase (COMT), which methylates and causes levodopa to break down.

When entacapone is given in conjunction with levodopa and carbidopa, levels of levodopa in the blood are greater and more sustained than after the administration of levodopa and carbidopa alone.

Indications and usage

Stalevo can be substituted for carbidopa/levodopa and entacapone, which are administered as individual drugs. It can also replace carbidopa/levodopa therapy (without entacapone) when patients experience the signs and symptoms of end-of-dose “wearing off.” This is only for patients taking a total daily dose of levodopa of 600 mg or less, and not experiencing dyskinesia or involuntary movements.

The tablets should not be split, crushed or chewed. Only one tablet should be given at each dosing interval.

Dosage and administration

The optimum daily dosage must be determined by careful titration in each patient.

Each tablet contains a fixed ratio of carbidopa to levodopa (1:4) in combination with a fixed amount of 200 mg of entacapone. Stalevo tablets are available in six strengths:

  • Stalevo 50 containing 12.5 mg of carbidopa, 50 mg of levodopa, and 200 mg of entacapone.
  • Stalevo 75 containing 18.75 mg of carbidopa, 75 mg of levodopa, and 200 mg of entacapone.
  • Stalevo 100 containing 25 mg of carbidopa, 100 mg of levodopa, and 200 mg of entacapone.
  • Stalevo 125 containing 31.25 mg of carbidopa, 125 mg of levodopa, and 200 mg of entacapone.
  • Stalevo 150 containing 37.5 mg of carbidopa, 150 mg of levodopa, and 200 mg of entacapone.
  • Stalevo 200 containing 50 mg of carbidopa, 200 mg of levodopa, and 200 mg of entacapone.

Contraindications

It is contraindicated for patients who have demonstrated hypersensitivity to any component (carbidopa, levodopa, or entacapone) of the drug or its excipients. Other nonselective monoamine oxidase (MAO) inhibitors should not be used together with Stalevo. The drug should also not be used in patients with suspicious, undiagnosed skin lesions or a history of melanoma.

Warnings and precautions

The components in Stalevo may cause adverse reactions such as daytime drowsiness, low blood pressure, involuntary movements, hallucinations, confusion, diarrhea, colitis, melanoma or depression with concomitant suicidal tendencies, among other conditions. The most common adverse reactions are involuntary movements, urine discoloration, diarrhea, nausea, abdominal pain, vomiting and dry mouth.

Stalevo should be administered cautiously to patients with severe cardiovascular or pulmonary disease, bronchial asthma, and kidney, liver or hormonal diseases.

Based on data from animal research, Stalevo may harm the fetus, so women should be careful using this drug during pregnancy, or while nursing.

Drug interactions

Some drugs may interact with Stalevo such as anti-hypertensive agents or antidepressants. Follow a doctor’s advice regarding drug interactions.

 

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