Levodopa + Benserazide: Uses, Dosage, Side Effects...

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Hong Kong prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Parkinson's disease

Adult: Levodopa 50 mg and benserazide 12.5 mg conventional cap
Levodopa 100 mg and benserazide 25 mg conventional cap
Levodopa 200 mg and benserazide 50 mg conventional cap
Levodopa 100 mg and benserazide 25 mg conventional tab
Levodopa 200 mg and benserazide 50 mg conventional tab
≥25 years Patients not previously treated with levodopa: Initially, 50 mg/12.5 mg 3-4 times daily; gradually increased in increments of 100 mg/25 mg daily once or twice weekly according to response and tolerability. In advanced disease, may start the dose with 100 mg/25 mg tid. Maintenance: 400-800 mg levodopa/100-200 mg benserazide daily in 3-6 divided doses. Doses >1,000 mg levodopa daily are rarely given. Patients who experience response fluctuations may consider dividing the dose into smaller, more frequent doses (without changing the total daily dose) or switching to modified-release preparations.

Levodopa 50 mg and benserazide 12.5 mg dispersible tab
Levodopa 100 mg and benserazide 25 mg dispersible tab
≥25 years For patients not previously treated with levodopa who have dysphagia or requiring rapid symptom control, such as in those exhibiting early morning and afternoon akinesia, or "delayed on" or "wearing off" phenomena: Initially, 50 mg/12.5 mg 3-4 times daily; gradually increased in increments of 100 mg/25 mg daily once or twice weekly according to response and tolerability. In advanced disease, may start the dose with 100 mg/25 mg tid. Maintenance: 400-800 mg levodopa/100-200 mg benserazide daily in 3-6 divided doses. Doses >1,000 mg levodopa daily are rarely given. Patients who experience response fluctuations may consider dividing the dose into smaller, more frequent doses (without changing the total daily dose) or switching to modified-release preparations.

Levodopa 100 mg and benserazide 25 mg modified-release cap
≥25 years For patients with fluctuations in response or poorly controlled nocturnal symptoms: Patients not currently taking levodopa: Initially, 100 mg/25 mg tid; gradually adjusted every 2-3 days according to response and tolerability. Max initial dose: 600 mg levodopa daily. Supplementary immediate-release preparations may be needed with the 1st morning dose of modified-release preparations to compensate for the gradual onset. Max combined dose (immediate-release and modified-release): 1,200 mg levodopa daily. Patients switching from immediate-release to modified-release preparation: Substitute one 100 mg/25 mg modified-release cap for each 100 mg levodopa given at the same frequency; gradually increase in increments of 100 mg/25 mg every 2-3 days as needed. Average of 50% increase in daily levodopa dose may be required compared to previous immediate-release dosing; titration may take up to 4 weeks. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Elderly: Levodopa 50 mg and benserazide 12.5 mg conventional cap
Levodopa 100 mg and benserazide 25 mg conventional cap
Levodopa 200 mg and benserazide 50 mg conventional cap
Levodopa 50 mg and benserazide 12.5 mg dispersible tab
Levodopa 100 mg and benserazide 25 mg dispersible tab
Patients not previously treated with levodopa: Initially, 50 mg/12.5 mg once daily or bid; gradually increase in increments of 50 mg/12.5 mg daily every 3-4 days according to response and tolerability. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).

What are the brands available for Levodopa + Benserazide in Hong Kong?

Madopar/Madopar Dispersible/Madopar HBS

Administration

Benserazide + Levodopa IR formulations: May be taken with or without food. May take w/ or immediately after a non-protein or low-protein snack to control GI side effects. Dispersible tab: May be dispersed in approx 25 mL of water or diluted orange squash. Do not use orange juice. Administer within 30 minutes of preparation.
Benserazide + Levodopa ER cap: Should be taken on an empty stomach. Swallow whole & do not open.

Contraindications

Decompensated CV, endocrine, haematologic, pulmonary, renal, or hepatic disease; severe metabolic or bone marrow disorders; severe cardiac disorders (e.g. severe tachycardia, severe arrhythmias or cardiac failure); psychiatric diseases with psychotic component; angle-closure glaucoma; suspicious undiagnosed skin lesions or history of melanoma. Patients <25 years old. Pregnancy; women of childbearing potential without adequate contraception. Concomitant use with or within 14 days of discontinuing non-selective MAOIs or a combination of monoamine oxidase A (MAO-A) and B (MAO-B) inhibitors.

Special Precautions

Patient with CV disease, including pre-existing coronary artery disorders, previous MI, cardiac arrhythmias or cardiac failure; history of orthostatic hypotension; gastrointestinal ulceration (e.g. peptic ulcer disease); history of seizure disorder or convulsions, history of psychotic disorders (e.g. depression); osteomalacia, diabetes mellitus, endocrine or pulmonary disease; open-angle glaucoma. Not indicated in the management of Huntington's chorea, intention tremors, or drug-induced extrapyramidal symptoms. Perioperative patients requiring general anaesthesia must continue therapy as close to the surgery as possible, except when using halothane; in case of general anaesthesia with halothane, discontinue treatment 12-48 hours before surgery. Avoid abrupt withdrawal. Renal and hepatic impairment. Elderly. Lactation. Concomitant use with sympathomimetic agents.

Adverse Reactions

Significant: CNS effects (e.g. daytime somnolence, sudden onset of sleep), impulse control disorders (e.g. pathological gambling, hypersexuality, binge eating, compulsive spending or buying), depression; fluctuations in therapeutic response, including "freezing" episodes, "end-of-dose" deterioration, "on-off" effect (particularly during prolonged use); dyskinesia (choreiform or athetotic); dopamine dysregulation syndrome; increased growth hormone levels; arrhythmia, orthostatic hypotension; haemolytic anaemia, thrombocytopenia, leucopenia, agranulocytosis, pancytopenia; gastrointestinal effects (e.g. dysgeusia, nausea, vomiting, diarrhoea); potential increase in IOP; hypersensitivity reactions.
Cardiac disorders: Angina pectoris.
Gastrointestinal disorders: Ageusia, dry mouth, constipation, discolouration of saliva, gastrointestinal haemorrhage, oral mucosa discolouration, sialorrhoea, tooth or tongue discolouration.
General disorders and administration site conditions: Lethargy, asthenia, oedema.
Investigations: Increased alkaline phosphatase, transaminases, GGT, and BUN.
Metabolism and nutrition disorders: Decreased appetite.
Musculoskeletal and connective tissue disorders: Muscle spasm or cramps.
Nervous system disorders: Dizziness, headache, somnolence, involuntary body movements.
Psychiatric disorders: Confusional state, agitation, insomnia, delusions, anxiety, hallucination, disorientation.
Renal and urinary disorders: Chromaturia.
Skin and subcutaneous tissue disorders: Pruritus, rash, diaphoresis, flushing.
Potentially Fatal: Neuroleptic malignant-like syndrome (particularly if abruptly withdrawn).

Patient Counseling Information

This drug may cause excessive daytime somnolence or sudden onset of sleep, if affected, do not drive or operate machinery. Women of childbearing potential must use effective birth control methods during treatment.

Monitoring Parameters

Monitor CV, hepatic, renal, and haematopoietic function regularly. Check blood glucose frequently in diabetic patients. Monitor blood pressure and for signs and symptoms of psychosis, depression, or impulse control disorders. Perform periodic skin exam to monitor for melanomas.

Overdosage

Symptoms: CV effects (e.g. cardiac arrhythmias), psychiatric disturbances (e.g. confusion, insomnia), gastrointestinal effects (e.g. nausea, vomiting) and abnormal involuntary movements.

Management: Symptomatic and supportive treatment.

Drug Interactions

Increased risk of hypertensive crises with non-selective MAOIs or a combination of MAO-A and MAO-B inhibitors. May increase the anti-Parkinsonian effect with selective MAO-B inhibitors (e.g. selegiline, rasagiline). May result in increased hypotensive effects with antihypertensive agents. May cause blood pressure fluctuations or arrhythmias with halothane; discontinue levodopa + benserazide 12-48 hours before surgery. May potentiate the CV effects with other antiparkinsonian agents (e.g. anticholinergics, amantadine, dopamine agonists) and sympathomimetics (e.g. epinephrine, norepinephrine, isoproterenol). Effects may be inhibited by antipsychotics, opioids, reserpine-containing antihypertensives, and neuroleptics.
Levodopa: May reduce the rate of absorption with anticholinergic agents (e.g. trihexyphenidyl). Decreased peak plasma concentrations with ferrous sulfate. Increased rate of absorption with metoclopramide. May increase the bioavailability and risk of cardiac arrhythmia with domperidone.

Food Interaction

Levodopa: May decrease the absorption and therapeutic effect with a high-protein diet. Reduced extent of absorption by 15% and peak plasma concentration by 30% with food. Increased serum concentration with alcohol.

Lab Interference

Levodopa: May interfere with determinations of catecholamines, creatinine, uric acid, and glucose. May cause false-positive urine test results for ketone bodies, false-positive Coombs' test and false-negative results for urine glucose by glucose-oxidase method.

Action

Description:
Overview: Levodopa is the immediate precursor of dopamine, a neurotransmitter depleted in the brain of Parkinson's disease patients.
Benserazide is a peripheral decarboxylase inhibitor.
Mechanism of Action: Levodopa is converted to dopamine by striatal enzymes, thereby increasing the levels of dopamine in the striatum, pallidum and substantia nigra of patients with Parkinson's disease.
Benserazide inhibits peripheral decarboxylation of levodopa, thereby increasing levodopa availability in the brain without significantly affecting its metabolism.
Pharmacokinetics:
Absorption: Levodopa: Rapidly absorbed from the gastrointestinal tract, particularly in the proximal small intestine. Reduced extent of absorption by 15% and peak plasma concentration by 30% with food. Bioavailability: 98% (range: 74-112%). Time to peak plasma concentration: Approx 1 hour.
Distribution: Levodopa: Crosses the placenta and enters breast milk. Crosses the blood-brain barrier. Volume of distribution: 57 L.
Benserazide: Mainly concentrated in the kidneys, liver, lungs, and small intestine.
Metabolism: Levodopa: Metabolised mainly via decarboxylation by aromatic amino acid decarboxylase into dopamine, which is further metabolised to form homovanillic acid and dihydroxyphenylacetic acid; levodopa also undergoes O-methylation by COMT into 3-O-methyldopa. Minor pathways are via transamination and oxidation.
Benserazide: Metabolised in the intestine and liver via hydroxylation to form trihydroxybenzylhydrazine, the active aromatic amino acid decarboxylase inhibitor.
Excretion: Levodopa: Via urine (as metabolites). Elimination half-life: 1.5 hours (levodopa); 15 hours (3-O-methyldopa).
Benserazide: Via urine (64%); faeces (24%).

Chemical Structure

Storage

Store between 15-30°C. Protect from light.

MIMS Class

Antiparkinsonian Drugs

ATC Classification

N04BA02 - levodopa and decarboxylase inhibitor ; Belongs to the class of dopa and dopa derivative dopaminergic agents. Used in the management of Parkinson's disease.

References

Benserazide and Levodopa. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/11/2025.

Brayfield A, Cadart C (eds). Benserazide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/11/2025.

Brayfield A, Cadart C (eds). Levodopa. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/11/2025.

Joint Formulary Committee. Co-beneldopa. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/11/2025.

Levodopa/Benserazide 100 mg/25 mg Capsules (Teva UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 10/11/2025.

Levodopa/Benserazide 50 mg/12.5 mg Capsules (Teva UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 10/11/2025.

Madopar (Roche [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 10/11/2025.

Madopar 100 mg/25 mg Dispersible Tablets (Roche Products Limited). MHRA. https://products.mhra.gov.uk. Accessed 18/11/2025.

Madopar CR 100 mg/25 mg Prolonged Release Hard Capsules (Roche Products Limited). MHRA. https://products.mhra.gov.uk. Accessed 18/11/2025.

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