Aparkin Capsule

Introduction

Levodopa and benserazide are combined in a medication used primarily to treat Parkinson's disease and Parkinsonism. Levodopa is a precursor to dopamine, which is deficient in patients with Parkinson's disease. Benserazide is a peripheral decarboxylase inhibitor that enhances the effectiveness of levodopa by preventing its conversion to dopamine outside the brain, thereby increasing its availability to the central nervous system.

Uses

The combination of levodopa and benserazide is used to:

• Treat the symptoms of Parkinson's disease, including tremor, rigidity, and bradykinesia (slowness of movement)
• Manage Parkinsonism, a condition with similar symptoms to Parkinson's disease
• Improve motor function and quality of life in patients with these neurological disorders

Brand Name	Aparkin
Type	Capsule
Weight	200 mg+50 mg
Generic	Levodopa + Benserazide
Manufacturer	Ziska Pharmaceuticals Ltd.
Available in	English বাংলা

Mechanism of Action

Levodopa is a precursor to dopamine, which is converted to dopamine in the brain. This helps replenish the depleted levels of dopamine in Parkinson's disease. Benserazide inhibits the enzyme aromatic L-amino acid decarboxylase (AADC) in peripheral tissues, which prevents the conversion of levodopa to dopamine outside the brain. This ensures that more levodopa reaches the brain, where it can be converted to dopamine.

How Long Does It Take to Work?

The effects of levodopa and benserazide generally begin within 30-60 minutes of administration. Peak effects are typically observed within 1-2 hours. The duration of action can vary based on individual response and dosage.

Absorption

Levodopa is well absorbed from the gastrointestinal tract, with peak plasma levels occurring approximately 1-2 hours after oral administration. Benserazide enhances the absorption of levodopa by preventing its premature conversion to dopamine outside the brain.

Route of Elimination

Levodopa and benserazide are primarily eliminated through the urine. Levodopa is metabolized to dopamine in the brain and to various metabolites in peripheral tissues. Benserazide is metabolized in the liver and excreted in the urine.

Dosage

For Immediate Release capsule (IR):


For Controlled Release capsule (CR):


Patients with renal impairment: No dose reduction of Levodopa-Benserazide is considered necessary in case of mild or moderate renal insufficiency.
Patients with hepatic impairment: The safety and efficacy of Levodopa-Benserazide have not been established in patients with hepatic impairment.

The dosage of levodopa and benserazide is individualized based on the severity of Parkinson's disease and the patient's response to therapy. Typical starting doses are:

• Levodopa 100 mg and benserazide 25 mg, taken orally 2-3 times daily

Dosage may be adjusted based on efficacy and tolerability, with the goal of minimizing symptoms while reducing side effects.

Administration

This combination medication is administered orally in the form of tablets. It is usually taken with or without food. Consistent dosing times and adherence to the prescribed regimen are important for optimal management of symptoms.

Side Effects

Common side effects include:

• Nausea and vomiting
• Dizziness
• Dry mouth
• Orthostatic hypotension (drop in blood pressure when standing)

Serious side effects may include:

• Extrapyramidal symptoms (e.g., involuntary movements, muscle rigidity)
• Hallucinations or confusion
• Severe dyskinesias (involuntary movements)

Toxicity

Toxicity can manifest as:

• Severe gastrointestinal symptoms (e.g., persistent vomiting, severe nausea)
• Cardiovascular symptoms (e.g., severe hypotension)
• Neurological symptoms (e.g., severe dyskinesia or psychosis)

In case of suspected toxicity, discontinue use and seek immediate medical attention. Treatment may involve supportive care and adjustment of dosage.

Precautions

Precautions should be taken in individuals with:

• Severe cardiovascular disease
• Severe renal or hepatic impairment
• History of psychotic disorders
• History of peptic ulcer disease

Regular monitoring and dose adjustments may be required based on individual response and tolerability.

Interaction

Interactions may include:

• Other medications affecting dopamine levels (e.g., antipsychotics)
• Medications affecting gastrointestinal motility (e.g., antacids)
• Antihypertensive medications: May require dose adjustment due to potential blood pressure effects

Monitor for potential interactions and adjust therapy as needed.

Disease Interaction

The combination should be used with caution in patients with:

• Severe cardiovascular disease
• Severe renal or hepatic impairment
• Active peptic ulcer disease
• Psychiatric disorders

Drug Interaction

Drug interactions may include:

• Antipsychotic medications: May counteract the effects of levodopa
• Iron supplements: May reduce the absorption of levodopa
• Other antihypertensives: May enhance the hypotensive effects

Food Interactions

Food interactions are minimal, but it is generally advised to take the medication with food to minimize gastrointestinal discomfort. Avoid high-protein meals close to dosing times as they may interfere with levodopa absorption.

Pregnancy Use

Levodopa and benserazide are classified as Category C drugs for pregnancy. There are no well-controlled studies in pregnant women, and their use during pregnancy should be limited to situations where the benefits outweigh potential risks. Consult a healthcare provider for advice if pregnancy is suspected or confirmed.

Lactation Use

Levodopa and benserazide are excreted in breast milk. Caution is advised as the effects on a nursing infant are not well studied. The medication should be used during lactation only if the benefits justify the potential risks. Consult a healthcare provider for guidance on breastfeeding while using this medication.

Acute Overdose

Acute overdose may result in:

• Severe gastrointestinal symptoms (e.g., persistent vomiting)
• Severe cardiovascular effects (e.g., hypotension)
• Neurological symptoms (e.g., severe dyskinesia, hallucinations)

In case of overdose, discontinue use and seek immediate medical attention. Treatment may involve supportive care and symptom management.

Contraindication

The combination is contraindicated in individuals with:

• Hypersensitivity to levodopa, benserazide, or any component of the formulation
• History of melanoma or suspicious skin lesions (due to potential for increased risk of melanoma with long-term use)
• Severe cardiovascular or renal disease
• Active peptic ulcer disease

Use Direction

Follow the specific instructions provided by your healthcare provider or product label. The medication should be taken consistently at the prescribed times. Adhere to the recommended dosage and report any adverse effects or issues to a healthcare provider.

Storage Conditions

Store levodopa and benserazide tablets at room temperature, between 15°C and 30°C (59°F and 86°F). Keep in a dry place, away from light and moisture. Ensure the medication is kept out of reach of children and not used beyond its expiration date.

Volume of Distribution

The volume of distribution for levodopa is approximately 1.5 L/kg, indicating extensive distribution in body tissues. Benserazide's volume of distribution is not well documented but is distributed throughout the body.

Half Life

The half-life of levodopa is approximately 1-3 hours, while benserazide has a half-life of about 1-2 hours. The effects of levodopa can persist longer due to its central action and the inhibition of peripheral decarboxylation by benserazide.

Clearance

Levodopa is primarily cleared through renal excretion and hepatic metabolism. Benserazide is also cleared through the urine, with metabolic processing in the liver.

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