Generic
Levodopa + Benserazide
10 brands available in the market
At a glance
Levodopa + Benserazide is used in the treatment of Parkinson's disease. Levodopa is a dopamine precursor that crosses the blood-brain barrier and is converted to dopamine in the brain. Benserazide is a peripheral decarboxylase inhibitor that reduces peripheral metabolism of levodopa, allowing more levodopa to reach the brain.
Description
Levodopa + Benserazide capsule is an anti-Parkinson's agent. Levodopa dopamine precursor is used as a prodrug because it can cross the blood-brain barrier whereas dopamine itself cannot. Once levodopa enters the CNS, it is metabolized to dopamine by aromatic L-amino acid decarboxylase. After administration, levodopa is rapidly decarboxylated to dopamine in extra-cerebral as well as cerebral tissues. Most of the levodopa administered is not available to the basal ganglia and peripherally produced dopamine frequently causes unwanted side effects. Therefore, inhibiting extra-cerebral decarboxylation of levodopa is desirable. This can be achieved by simultaneous administration of levodopa-benserazide capsule, a peripheral decarboxylase inhibitor. Levodopa-benserazide capsule is a combination of these two substances in a 4:1 ratio - optimal in clinical trials - and is as effective as large doses of levodopa alone.
Indications
- Parkinson's disease - Immediate Release capsule: all forms except drug-induced Parkinsonism
- Parkinson's disease - Controlled Release capsule: patients with motor fluctuations, especially peak dose dyskinesia and end of dose deterioration and for better control of nocturnal symptoms
Therapeutic class
Antiparkinson Drugs
Pharmacological class
Dopamine Precursor + Decarboxylase Inhibitor
Pharmacology
Levodopa is a prodrug that crosses the blood-brain barrier and is converted to dopamine in the CNS by aromatic L-amino acid decarboxylase. Benserazide is a peripheral decarboxylase inhibitor that reduces peripheral decarboxylation of levodopa, increasing its availability to the brain and reducing side effects.
Mechanism of action
Increases dopamine levels in the brain and inhibits peripheral decarboxylation to control Parkinson's disease symptoms.
Dosage
Immediate Release IR Capsule:
- Patients not receiving levodopa: Early stage: 50+12.5 62.5 mg, 1-2 times/day; gradually increase by 62.5 mg every 3-4 days
- Adult: 50+12.5 62.5 mg, 3-4 times/day OR Advanced stage: 100+25 125 mg, 3 times/day
- Maintenance: 100+25 125 mg, up to 3-6 times/day
- Previous levodopa monotherapy: Initiate with 10-15% of previous dose
- Previous other levodopa/dopa decarboxylase combination: Withdraw previous therapy for 12 hours, start 50+12.5 62.5 mg, 3-4 times/day
Controlled Release CR Capsule:
- Patients not receiving levodopa: 100+25 125 mg, 3 times/day; maximum 6 capsules/day
- Previous levodopa-benserazide IR: Substitute every 100 mg levodopa with 1 CR capsule; increase every 2-3 days
Administration
- Swallow capsule whole; do not chew, crush or break
- May be taken with or without food
- Discontinue 12-48 hours before surgery with halothane anesthesia
Missed dose
If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.
Side effects
Common Side Effects:
- Anxiety, decreased appetite
- Arrhythmia
- Depression
- Diarrhea
- Hallucinations
- Movement disorders dyskinesia
- Nausea
- Postural hypotension
- Sleep disorders
- Altered taste
- Vomiting
- Leucopenia
Precautions & warnings
- Reduce dose if dyskinesia occurs early
- Caution with orthostatic hypotension
- Caution in psychiatric illness, diabetes, cardiovascular disease, peptic ulcer, glaucoma, pheochromocytoma
- Caution in Cushing's syndrome, endocrine disorders, hyperthyroidism, osteomalacia
- May activate malignant melanoma - do not use in suspicious lesions or history of melanoma
Contraindications
- Hypersensitivity to levodopa-benserazide or excipients
- Non-selective MAO inhibitors risk of hypertensive crisis
- Decompensated endocrine, renal or hepatic function
- Cardiac disorders
- Psychiatric diseases with psychotic component
- Closed-angle glaucoma
- Intention tremor and Huntington's chorea
- History of melanoma or suspicious lesions
- Patients less than 30 years old skeletal development must be complete
- Pregnancy
Drug interactions
- Neuroleptics, opioids, and reserpine-containing antihypertensives inhibit levodopa action
- Do not co-administer with sympathomimetics adrenaline, noradrenaline, isoproterenol, amphetamine - levodopa may potentiate their effects
- Dopamine-receptor blocking antipsychotics especially D2-receptor antagonists may antagonize antiparkinsonian effects
- Discontinue 12-48 hours before halothane anesthesia - blood pressure fluctuations and/or arrhythmias may occur
Food interactions
Safety with alcohol is not known; consult your doctor.
Use in pregnancy
Use in Pregnancy: Levodopa + Benserazide is contraindicated during pregnancy Category B3 and in women of childbearing potential without adequate contraception. Discontinue if pregnancy occurs.
Pregnancy Category: B3 — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Safe use of Levodopa + Benserazide during lactation has not been established. Should not be used.
Pediatric use
Contraindicated in patients less than 30 years of age - skeletal development must be complete.
Geriatric use
No dose adjustment may be needed in elderly; may be adjusted based on renal function.
Renal / hepatic impairment
Renal Impairment: No dose reduction necessary in mild to moderate renal insufficiency.
Hepatic Impairment: Safety and efficacy not established in hepatic impairment.
Overdose effects
Overdose requires symptomatic treatment for cardiovascular effects anti-arrhythmics or CNS effects respiratory stimulants, neuroleptics; for CR formulation, prevent further absorption.
Storage conditions
Store below 30°C, away from light and moisture; keep out of reach of children.
Chemical structure
Levodopa + Benserazide