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Carbidopa

Carbidopa (MK-486) is a drug given to people with Parkinson's disease in order to inhibit peripheral metabolism of levodopa. more...

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Carbidopa inhibits aromatic-L-amino-acid decarboxylase (DDC), an enzyme important in the biosynthesis of L-tryptamine to 5-HT and in the biosynthesis of L-DOPA to Dopamine (DA). Along with carbidopa, other DDC inhibitors are benserazide (Ro-4-4602), difluromethyldopa, and a-methyldopa.

Used in tandem with levodopa (l-dopa, a dopamine precurser converted in the body to dopamine), it increases the plasma half-life of levodopa from 50 minutes to 1 1/2 hours.

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New formulation: Parcopa®, Schwarz Pharma: Carbidopa-levodopa
From Geriatrics, 11/1/04

Parkinson's tablet approved

The orally-disintegrating tablet formulation of carbidopa-levodopa was approved for the treatment of symptoms of idiopathic Parkinson's disease (paralysis agitans), postencephalitic parkinsonism, and symptomatic parkinsonism. Dosage. Optimum daily dosing of carbidopa-levodopa must be carefully titrated. This formulation is available in a 1:4 ratio of carbidopa to levodopa (25/100 mg) and a 1:10 ratio (25/250 and 10/100 mg). Tablets of the 2 ratios may be given separately or combined to provide optimum dosage and should be taken at regular intervals. Ingredients will begin release within 30 minutes of placing on tongue.

Standard drugs for Parkinson's disease, other than levodopa without a decarboxylase inhibitor, may be used concomitantly, although dosage adjustments may be required.

Geriatric dosage adjustments. None recommended.

Pharmacokinetics. Carbidopa reduces the amount of levodopa required to produce a given response by about 75% and when administered with levodopa, increases plasma levels and the plasma half-life of levodopa, and decreases plasma and urinary dopamine and homovanillic acid. The plasma half-life of levodopa is about 1.5 hours when taken with carbidopa.

Abnormalities in laboratory tests may include elevations of liver function tests, such as alkaline phosphatase, SGOT (AST), SGPT (ALT), lactic dehydrogenase, and bilirubin. Commonly, levels of blood urea nitrogen, creatinine, and uric acid are lower during administration of carbidopa-levodopa than with levodopa alone.

Safety. Nonselective MAOIs are contraindicated for use with carbidopa-levodopa tablets and must be discontinued at least 2 weeks prior to initiating therapy. Levodopa must be discontinued at least 12 hours prior to initiation of therapy with carbidopa-levodopa tablets.

CNS adverse events (eg, dyskinesias) may occur at lower dosages and sooner with carbidopa-levodopa tablets than with levodopa alone.

Cardiac function should be monitored in patients with a history of MI who have residual atrial, nodal, or ventricular arrhythmias.

A symptom complex resembling neuroleptic malignant syndrome has been reported sporadically in association with dose reductions or withdrawal of carbidopa-levodopa.

Carbidopa-levodopa tablets contain phenylalanine.

Avoid carbidopa-levodopa orally-disintegrating tablets in patients with narrow-angle glaucoma.

Rare reports exist of hypertension and dyskinesia resulting from concomitant use of tricyclic antidepressants and carbidopa-levodopa.

Symptomatic postural hypotension has occurred with carbidopa-levodopa treatment for patients already receiving antihypertensive drugs.

Adverse events. Commonly observed adverse events associated with carbidopa-levodopa therapy include nausea and dyskinesias, such as choreiform, dystonic, and other involuntary movements.

COPYRIGHT 2004 Advanstar Communications, Inc.
COPYRIGHT 2005 Gale Group

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