Periodic monitoring of hepatic, renal, haematopoietic and CV functions in patients on prolonged therapy. Monitor for changes in IOP in patients with chronic wide-angle glaucoma. Caution when used in patients with biliary obstruction. Caution when interpreting plasma and urine levels of catecholamines and their metabolites. Withdrawal should be gradual.
Lactation: not known if excreted in breast milk; use caution
Indication
Parkinson's disease and 'end of dose' motor fluctuations
Contra Indication
Hypersensitivity. Narrow angle glaucoma. Should not be used in patients with suspicious, undiagnosed skin lesions or a history ot melanoma.
Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks
Mode of Action
Levodopa is the metabolic precurosor of dopamine, it crosses the blood-brain barrier and is converted to dopamine in the brain. Carbidopa increases the amount of levodopa that is transported into the CNS by inhibiting the decarboxylation of peripheral levodopa. Entacapone is a selective inhibitor of catechol-o-methyltransferase. Given concurrently, entacapone results in greater and more substained plasma levels of levodopa, leading to greater control of parkinsonism symptoms.
Interaction
Increased risk of postural hypotension when used concurrently with hypotensive drugs. Severe orthostatic hypotension may result from concurrent usage with MAOIs. Dopamine D2 receptor antagonists, phenytoin or papaverine may reduce the efficacy of levodopa. Iron salts may reduce the bioavailability. Concurrent usage with drugs that interfere with biliary excretion may lead to increased plasma levels of entacapone. May depress prolactin secretion and increase growth hormone levels.
Pregnancy Category Note
Pregnancy Category: C
Lactation: not known if excreted in breast milk; use caution
Adult Dose
Parkinson's disease
Adult: PO: Each tab contains levodopa and carbidopa in a ratio of 4:1 and entacapone 200 mg: Initial: 1 tab/day. Titrate dose according to patient's response. Recommended to take only 1 tab per dose administration. Max: 8 tabs/day.
Hepatic impairment: Severe: Contraindicated.
Child Dose
Safety & efficacy not established
Renal Dose
N/A
Administration
May be taken with or without food. Keep a consistent diet. A change in diet to foods high in protein may delay levodopa absorption & reduce amount taken up in circulation. Excessive acidity also delays stomach emptying & thus delays levodopa absorption. Fe salts (eg in multivit prep) may also reduce amount of levodopa available to the body. Swallow whole.
Disclaimer
The information provided herein are for informational purposes only and not intended to be a substitute for professional medical advice, diagnosis, or treatment. Please note that this information should not be treated as a replacement for physical medical consultation or advice. Great effort has been placed to provide accurate and comprehensive data. However, Medicart along with its authors and editors make no representations or warranties and specifically disclaim all liability for any medical information provided on the site. The absence of any information and/or warning to any drug shall not be considered and assumed as an implied assurance of the Company.