Foscarbidopa/foslevodopa

Combination drug for Parkinson's disease

Foscarbidopa/foslevodopa is a combination medication used in the treatment of Parkinson's disease. It consists of two components: foscarbidopa and foslevodopa. This combination is designed to improve the delivery and effectiveness of levodopa, a precursor to the neurotransmitter dopamine, which is deficient in patients with Parkinson's disease.

Components

Foscarbidopa

Foscarbidopa chemical structure

Foscarbidopa is a prodrug of carbidopa, which is a peripheral decarboxylase inhibitor. Carbidopa works by inhibiting the enzyme aromatic L-amino acid decarboxylase (AADC) outside the central nervous system (CNS). This inhibition prevents the conversion of levodopa to dopamine in the periphery, allowing more levodopa to reach the brain where it can be converted to dopamine. Foscarbidopa is designed to enhance the bioavailability of carbidopa, improving its ability to inhibit peripheral decarboxylation.

Foslevodopa

Foslevodopa chemical structure

Foslevodopa is a prodrug of levodopa, the direct precursor to dopamine. Levodopa is the most effective treatment for the motor symptoms of Parkinson's disease. By converting to dopamine in the brain, it helps replenish the depleted levels of this neurotransmitter, thereby alleviating symptoms such as bradykinesia, rigidity, and tremor. Foslevodopa is designed to improve the pharmacokinetic profile of levodopa, enhancing its absorption and reducing fluctuations in plasma levels.

Mechanism of Action

The combination of foscarbidopa and foslevodopa is intended to optimize the delivery of levodopa to the brain. By using prodrugs, the formulation aims to improve the stability and absorption of the active compounds. Foscarbidopa ensures that more levodopa reaches the CNS by inhibiting peripheral metabolism, while foslevodopa provides a more consistent supply of levodopa for conversion to dopamine in the brain.

Clinical Use

Foscarbidopa/foslevodopa is used in the management of Parkinson's disease, particularly in patients who experience "off" periods or fluctuations in their response to traditional levodopa/carbidopa therapy. The prodrug formulation is designed to provide a more stable and sustained delivery of levodopa, potentially reducing the frequency and severity of motor fluctuations.

Administration

The medication is typically administered orally. The dosing regimen is tailored to the individual patient's needs, based on the severity of symptoms and response to treatment. As with all Parkinson's disease treatments, careful titration and monitoring are essential to optimize therapeutic outcomes and minimize side effects.

Side Effects

Common side effects of foscarbidopa/foslevodopa may include nausea, dizziness, headache, and dyskinesia. As with other levodopa formulations, patients may experience "on-off" phenomena, where the effectiveness of the medication fluctuates. Long-term use can also lead to the development of motor complications.

Related pages

• Parkinson's disease
• Levodopa
• Carbidopa
• Dopamine