Drug Interaction:
Drug Interactions- summary-
MAO inhibitors + Entacapone-
Combination of MAO inhibitor (eg phenelzine, tranylcypromine ) would result in inhibition of
majority of the path ways responsible for normal catecholamine metabolism.
patients should ordinarily not be treated concomittantly with entacapone and a non selective
MAO inhibitor.
Probenecid, cholestyramine, eryhromycin , rifampin, ampicillin, chloramphenicol + Entacapone-
excecise caution when drugs known to interfere with biliary excretion, glcuroidation and
intestinal glucoronidase are given concurrently with entacapone
Entacapone + Isoproterenol , epinephrine, dopamine, dobutamine, methyldopa, apormorphine,
isoetherine, biolterol-
administer drugs known to be metabolized by COMT ( catechol -O- methyltranferase )
eg isopreterenol, epinephrine, noepinephrine, dopamine, dobutamine, methyldopa,
apomorphine, isoetherine, biolterol ) with caution in patients receiving entacapone .
This may result in increased heart rate, arrhythmias and excessive changes in blood pressure
Indication:
Parkinsonism
LIST OF DRUGS DURING 2004
Sr.No- 265
Name of the Drug- Entacapone (200mg) tablet Pharmacological Classification- For parkinsons disease
Date of Approval- 30-12-2004
Approved by U.S.FDA on 30-12-2004 (Ref- FDA approved List- 2004)
Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
Entacapone 200mg For Parkinson Disease 30-12-2004
tablet
Adverse Reaction:
Adverse reactions-
Dermatologic- sweating increased 2%
Musculoskeletal - back pain 2%
CNS- dyskinesia 24% hyperkinesia 9% hypokinesia 8% dizziness 7%
Psychiatric disorders - anxiety 2% somnolence 1%
GI- nausea 12% diarrhea 9% abdominal pain 7% constipation 5% vomiting 4%
dry mouth 2%
Respiratory - dyspnea 2%
GU - urine discoloration 9%
Miscellaneous- fatigue 5%
Contra-Indications:
Hypesensitivity to the drug
Special Precautions-
Diarrhea- diarrhea presents itself within 4 to 12 weeks after entacapone is started but may appear
as early as thevfirst week after initiation of treatment
Hallucination - reported in patients treated with 200mg entacapone andrarely in some cases
required hospitalisation
Dyskinesia- entacapone may potentiate the dopaminergic side effects of levodopa and may
exacerbate preexisting dyskinesia
Rhabdomylosis - cases of severe rhabdomyoluysis have been reported with entacapone use
Hyperpyrexia and confusion- cases of symptom complex resembling theneuroleptic malignant
syndrome characterised by elevated temperature, muscular rigidity, and altered consciousness
and elevated creatinine phosphokinase have been reported with rapid dosage reduction or
withdrawal of dopaminergic drugs.
Pregnancy - entacaponeshould be used during pregnancy only if the potential benefit justifies
the potential risk to the fetus.
Lacation- caution should be excercised whenn entacapone is administered to a nursing woman
Children- no identified potential use of entacapone in pediatric patients
Dosages/ Overdosage Etc:
Indication-
Parkinsonism
Dosage-
one 200mg tablet administred concomittantly with each levodopa/carbidopa dose to
a mximum of 8 times daily ( 200mg * 8 = 1600mg per day.
Clinical experience daily dose above 1600mg is limited.
Patient Information:
1. Patients should be informed that hallucinations can occur
2. Patients should be adviced that they may develop postural ( orthostatic ) hypotension with
or without symptoms such as dizziness, nausea, syncope, and sweating.
3. Patients should be cautioned against rising rapidly after sitting or lying down especially
if they have been doing so for prolonged periods
4. Patients should be adviced that they neither drive a car or operate complex machinery unless
they have gained sufficient experience to gauge whether or not it affects their mental or motor
performance adversely
5. Patients should be adviced that entacapone may cause a change in the color of their urine to
brownish orange
6. Patients should be adviced to inform their doctor if they are pregnant or plan to become pregnant
7,Patients should inform their doctor if they intent to breast feed or breast feeding an infant.
Pregnancy and lactation:
Pregnancy -
Entacapone should be used during pregnancy only if the potential benefit justifies
the potential risk to the fetus.
Lacation-
Caution should be excercised whenn entacapone is administered to a nursing woman
Children-
No identified potential use of entacapone in pediatric patients