Indications

This immediate release capsule is indicated for the treatment of all forms of Parkinson's syndrome with the exception of medicine-induced Parkinsonism. On the other hand, controlled release capsule indicated for patients presenting with all types of motor fluctuations in response, especially those related to fluctuations in plasma levels (i.e. "peak dose dyskinesia" and "end of dose deterioration") and for better control of nocturnal symptoms.

Composition

Pharmacology

This capsule is an anti-Parkinson’s agent. Levodopa (dopamine precursor) is used as a prodrug to increase dopamine levels since it is able to cross the blood brain barrier whereas dopamine itself cannot. Once levodopa has entered the central nervous system, it is metabolized to dopamine by aromatic L-amino acid decarboxylase. After administration, levodopa is rapidly decarboxylases to dopamine in extra-cerebral as well as cerebral tissues. As a result, most of the levodopa administered is not available to the basal ganglia and the dopamine produced peripherally frequently causes unwanted side effects. It is therefore particularly desirable to inhibit extra-cerebral decarboxylation of levodopa. 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 ratio of 4:1- this ratio having proved optimal in clinical trials and therapeutic use - and is just as effective as large doses of levodopa given alone.

Dosage & Administration

For Immediate Release capsule (IR): Parkinson's disease Initial dose Maintenance Patients not presently receiving levodopa Early Stage Elderly (50+12.5) 62.5 mg, 1-2 times/day Gradually increase by Levodopa Benserazide (50+12.5) 62.5 mg daily, in every 3-4 dauys according to response. Adult (50+12.5) 62.5 mg, 3-4 times/day 1 capsule of Levodopa-Benserazide (100+25) 125 mg 3 to 6 times/day Advance stage (100+25) 125 mg, 3 times/day Patients previously on levodopa monotherapy Initiate with 10-15% of the usual dose previously taken Patients previously on other levodopa/dopadecarbixylase combination therapy Withdraw previous therapy for 12 hours before initiating therapy at Levodopa-Benserazide (50+12.5) 62.5 mg, 3 or 4 times daily For Controlled Release capsule (CR): Parkinson's disease with motor fluctuation Initial dose Maximum dose Patients not presently receiving levodopa 1 capsule of Levodopa-Benserazide (100+25) 125 mg controlled release capsule, 3 times/day 6 capsules/day Patients previously on levodopa-Benserazide immediate release preperation Initially dose should substitute every 100 mg of Levodopa with 1 controlled-release cap, given at same dosage frequency as before. Increase every 2-3 days according to response. 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.

Contraindications

This combination is contraindicated in patients with -known hypersensitivity to levodopa-benserazide or any of the excipients, patients receiving non-selective monoamine oxidase (MAO) Inhibitors due to the risk of hypertensive crisis. However, selective MAO-B inhibitors, such as selegiline and rasagiline, or selective MAO-A inhibitors, such as moclobemide, are not contraindicated. Patients with decompensated endocrine, renal or hepatic function, cardiac disorders, psychiatric diseases with a psychotic component or dosed angle glaucoma. Because levodopa may activate a malignant melanoma, this combination should not be used in patients with suspicious, undiagnosed lesions or a history of melanoma. The management of patients with intention tremor and Huntington's chorea. Patients less than 30 years old (skeletal development must be complete).

Side Effects

Anxiety, appetite decreased, arrhythmia, depression, diarrhea, hallucination, movement disorders, nausea, postural hypotension, sleep disorders, altered taste, vomiting, leucopenia etc.

Pregnancy & Lactation

Pregnancy Category B3. This capsule is contraindicated during pregnancy and in women of childbearing potential in the absence of adequate contraception. If pregnancy occurs in a woman taking this capsule, the medicine must be discontinued. The safe use of This capsule during lactation has not been established. Use in Children: This capsule is contraindicated in patients less than 30 years old.

Precautions & Warnings

Cushing's syndrome, diabetes mellitus, endocrine disorders, history of convulsions, history of myocardial infarction with residual arrhythmia, history of peptic ulcer, hyperthyroidism, osteomalacia, pheochromocytoma, psychiatric illness, severe cardiovascular disease, severe pulmonary disease, susceptibility to angle-closure glaucoma.

Therapeutic Class

Antiparkinson drugs

Storage Conditions

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.