Entacapone

Entacapone Brand Name– Comtan

What is Entacapone

Entacapone is a reversible inhibitor of peripheral catechol-O-methyltransferase (COMT) and is used as an adjunct to levodopa/carbidopa therapy in the treatment of Parkinson’s disease.

Clinically, COMT inhibitors improve levodopa availability in the CNS, thereby prolonging the motor response to levodopa treatment. Entacapone allows the patient’s dosage of levodopa to be lowered, and results in a decrease in the incidence or severity of levodopa dose-related side effects (e.g., dyskinesia, nausea, etc.).

With initial entacapone therapy, an increase in levodopa-induced side effects may be seen until the dosage of levodopa is adjusted downward.

Entacapone treatment of Parkinson’s disease patients has been associated with significant increases in daily “on” time and decreases in “off” time. In addition, entacapone has been shown to improve total activities of daily living and motor function scores, but it has no effect on cognitive function.

Entacapone may be given with regular or controlled-release formulations of levodopa/carbidopa with or without the concurrent use of selegiline.

As compared to another available COMT inhibitor, tolcapone, entacapone has a shorter duration of COMT inhibition but appears to have an improved side effect profile and does not require additional laboratory monitoring.

The FDA approved entacapone in October 1999.

Indications

  • Parkinson’s disease

For use as an adjunct to levodopa and carbidopa to treat end-of-dose ‘wearing-off’ in patients with Parkinson’s disease

Side Effects

  1. abdominal pain
  2. agitation
  3. anxiety
  4. asthenia
  5. back pain
  6. colitis
  7. confusion
  8. constipation
  9. diarrhea
  10. dizziness
  11. drowsiness
  12. dysgeusia
  13. dyskinesia
  14. dyspepsia
  15. dyspnea
  16. fatigue
  17. flatulence
  18. gastritis
  19. hallucinations
  20. hyperhidrosis
  21. hyperkinesis
  22. hypotension
  23. impulse control symptoms
  24. infection
  25. myalgia
  26. nausea
  27. neuroleptic malignant syndrome-like symptoms
  28. orthostatic hypotension
  29. psychosis
  30. pulmonary fibrosis
  31. purpura
  32. rhabdomyolysis
  33. skin discoloration
  34. sudden sleep onset
  35. syncope
  36. tongue discoloration
  37. urine discoloration
  38. ventricular tachycardia
  39. vomiting
  40. withdrawal
  41. xerostomia

Monitoring Parameters

  • LFTs
  • neurologic function

Contraindications

  • abrupt discontinuation
  • behavioral changes
  • biliary obstruction
  • breast-feeding
  • children
  • coadministration with other CNS depressants
  • colitis
  • diarrhea
  • driving or operating machinery
  • dyskinesia
  • ethanol ingestion
  • geriatric
  • hepatic disease
  • hyperthermia
  • hypotension
  • impulse control symptoms
  • infants
  • jaundice
  • MAOI therapy
  • melanoma
  • orthostatic hypotension
  • pregnancy
  • psychosis
  • pulmonary fibrosis
  • retroperitoneal fibrosis
  • rhabdomyolysis
  • surgery
  • syncope

Interactions

  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Alfentanil
  • Alprazolam
  • Amitriptyline; Chlordiazepoxide
  • Amoxapine
  • Ampicillin
  • Ampicillin; Sulbactam
  • Articaine; Epinephrine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
  • Atropine
  • Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
  • Atropine; Difenoxin
  • Atropine; Diphenoxylate
  • Atropine; Edrophonium
  • Atropine; Hyoscyamine; Phenobarbital; Scopolamine
  • atypical antipsychotic
  • Azelastine
  • Azelastine; Fluticasone
  • Barbiturates
  • Belladonna; Opium
  • Benzhydrocodone; Acetaminophen
  • Benzodiazepines
  • Brompheniramine; Carbetapentane; Phenylephrine
  • Brompheniramine; Guaifenesin; Hydrocodone
  • Brompheniramine; Hydrocodone; Pseudoephedrine
  • Cannabidiol
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbetapentane; Guaifenesin
  • Carbetapentane; Guaifenesin; Phenylephrine
  • Carbetapentane; Phenylephrine
  • Carbetapentane; Phenylephrine; Pyrilamine
  • Carbetapentane; Pseudoephedrine
  • Carbetapentane; Pyrilamine
  • Carbinoxamine; Hydrocodone; Phenylephrine
  • Carbinoxamine; Hydrocodone; Pseudoephedrine
  • Cenobamate
  • Cetirizine
  • Cetirizine; Pseudoephedrine
  • Chloral Hydrate
  • Chloramphenicol
  • Chlordiazepoxide
  • Chlordiazepoxide; Clidinium
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpromazine
  • Chlorthalidone; Clonidine
  • Cholestyramine
  • Clobazam
  • Clonazepam
  • Clonidine
  • Clorazepate
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Colchicine; Probenecid
  • Deutetrabenazine
  • Dexmedetomidine
  • Dexmethylphenidate
  • Dextromethorphan; Promethazine
  • Diazepam
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Dobutamine
  • Dopamine
  • Dronabinol
  • Droperidol
  • Enflurane
  • Ephedrine
  • Epinephrine
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Esketamine
  • Estazolam
  • Eszopiclone
  • Ethanol
  • Etomidate
  • Fenfluramine
  • Fentanyl
  • Flibanserin
  • Fluphenazine
  • Flurazepam
  • Fospropofol
  • Gabapentin
  • General anesthetics
  • Guaifenesin; Hydrocodone
  • Guaifenesin; Hydrocodone; Pseudoephedrine
  • Guanfacine
  • Haloperidol
  • Halothane
  • Heterocyclic antidepressants
  • Homatropine; Hydrocodone
  • Hydrochlorothiazide, HCTZ; Methyldopa
  • Hydrocodone
  • Hydrocodone; Ibuprofen
  • Hydrocodone; Phenylephrine
  • Hydrocodone; Potassium Guaiacolsulfonate
  • Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
  • Hydrocodone; Pseudoephedrine
  • Hydromorphone
  • Ibuprofen; Oxycodone
  • Isocarboxazid
  • Isoflurane
  • Isoniazid, INH
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Isoproterenol
  • Ketamine
  • Lasmiditan
  • Lemborexant
  • Levocetirizine
  • Levorphanol
  • Linezolid
  • Lofexidine
  • Lorazepam
  • Loxapine
  • Maprotiline
  • Melatonin
  • Meperidine
  • Meperidine; Promethazine
  • Meprobamate
  • Mesoridazine
  • Methadone
  • Methyldopa
  • Methylphenidate
  • Metoclopramide
  • Midazolam
  • Mirtazapine
  • Molindone
  • Morphine
  • Morphine; Naltrexone
  • Nabilone
  • Nefazodone
  • Norepinephrine
  • Opiate Agonists-Antagonists
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Perampanel
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenelzine
  • Phenothiazines
  • Phenylephrine; Promethazine
  • Pimozide
  • Pramipexole
  • Pregabalin
  • Prilocaine; Epinephrine
  • Probenecid
  • Procarbazine
  • Prochlorperazine
  • Promethazine
  • Propofol
  • Quazepam
  • Racepinephrine
  • Ramelteon
  • Remifentanil
  • Rifampin
  • Scopolamine
  • Sedating H1-blockers
  • Sevoflurane
  • Skeletal Muscle Relaxants
  • Sodium Oxybate
  • Solriamfetol
  • Sufentanil
  • Suvorexant
  • Tapentadol
  • Tasimelteon
  • Temazepam
  • Tetrabenazine
  • Thalidomide
  • Thiethylperazine
  • Thioridazine
  • Thiothixene
  • Tizanidine
  • Tramadol
  • Tranylcypromine
  • Trazodone
  • Triazolam
  • Tricyclic antidepressants
  • Trifluoperazine
  • Valerian, Valeriana officinalis
  • Valproic Acid, Divalproex Sodium
  • Warfarin
  • Zaleplon
  • Zolpidem
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