Tolcapone

What is Tolcapone

Tolcapone is an oral peripherally and centrally-acting catechol-O-methyltransferase (COMT) inhibitor 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.

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

Tolcapone increases daily “on” time and decreases in “off” time. As compared to the other COMT inhibitor, entacapone, tolcapone is more potent and longer acting. Further, entacapone acts only peripherally.

However, tolcapone has been associated with a less favorable side effect profile, including life-threatening severe hepatocellular injury; the labeling carries a boxed warning regarding hepatotoxicity.

The clinician must monitor the patient for the presence of hepatic injury at baseline and at recommended intervals throughout treatment. FDA approval for tolcapone was granted in 1998

Brand Name

Tasmar

Indications

  • Parkinson’s disease

For use as adjunctive treatment to levodopa and carbidopa for the treatment of signs and symptoms of idiopathic Parkinson’s disease

Side Effects

  1. abdominal pain
  2. agitation
  3. alopecia
  4. amnesia
  5. anemia
  6. angina
  7. anorexia
  8. apnea
  9. arthropathy
  10. atopic dermatitis
  11. atrial fibrillation
  12. bleeding
  13. bradycardia
  14. bronchospasm
  15. cardiac arrest
  16. cataracts
  17. chest pain (unspecified)
  18. chills
  19. cholecystitis
  20. cholelithiasis
  21. cholestasis
  22. choreoathetosis
  23. colitis
  24. confusion
  25. constipation
  26. cough
  27. dehydration
  28. delirium
  29. depression
  30. diabetes mellitus
  31. diarrhea
  32. diplopia
  33. dizziness
  34. drowsiness
  35. dysarthria
  36. dyskinesia
  37. dyspepsia
  38. dysphagia
  39. dyspnea
  40. dystonic reaction
  41. dysuria
  42. edema
  43. elevated hepatic enzymes
  44. emotional lability
  45. encephalopathy
  46. epistaxis
  47. erythema multiforme
  48. esophagitis
  49. euphoria
  50. fatigue
  51. fever
  52. flank pain
  53. flatulence
  54. furunculosis
  55. GI bleeding
  56. hallucinations
  57. headache
  58. heart failure
  59. hematuria
  60. hepatic failure
  61. hepatotoxicity
  62. hiccups
  63. hostility
  64. hypercholesterolemia
  65. hyperesthesia
  66. hyperglycemia
  67. hyperhidrosis
  68. hyperkinesis
  69. hypersalivation
  70. hypertension
  71. hypertonia
  72. hyperventilation
  73. hypotension
  74. hypoxia
  75. impotence (erectile dysfunction)
  76. impulse control symptoms
  77. influenza
  78. insomnia
  79. irritability
  80. jaundice
  81. laryngitis
  82. libido decrease
  83. libido increase
  84. malaise
  85. mania
  86. meningitis
  87. migraine
  88. muscle cramps
  89. myalgia
  90. myocardial infarction
  91. myoclonia
  92. nasal congestion
  93. nausea
  94. neuropathic pain
  95. nocturia
  96. ocular hemorrhage
  97. ocular inflammation
  98. ocular pain
  99. oliguria
  100. oral ulceration
  101. orthostatic hypotension
  102. otalgia
  103. palpitations
  104. paranoia
  105. paresthesias
  106. parosmia
  107. peptic ulcer
  108. pericardial effusion
  109. pharyngitis
  110. pleural effusion
  111. polyuria
  112. pruritus
  113. psychosis
  114. pulmonary embolism
  115. pulmonary fibrosis
  116. rash
  117. rhabdomyolysis
  118. rhinitis
  119. seborrhea
  120. sinus tachycardia
  121. skin discoloration
  122. stroke
  123. sudden sleep onset
  124. syncope
  125. thrombocytopenia
  126. thrombosis
  127. tinnitus
  128. tremor
  129. urinary incontinence
  130. urinary retention
  131. urine discoloration
  132. urticaria
  133. vaginitis
  134. vertigo
  135. vomiting
  136. withdrawal
  137. xerostomia

Monitoring Parameters

  • LFTs
  • neurologic function

Contraindications

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

Interactions

  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Alfentanil
  • Alprazolam
  • Amitriptyline; Chlordiazepoxide
  • Amoxapine
  • 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
  • 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
  • Clobazam
  • Clonazepam
  • Clonidine
  • Clorazepate
  • Codeine
  • Codeine; Guaifenesin
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Deutetrabenazine
  • Dexmedetomidine
  • Dexmethylphenidate
  • Dextromethorphan; Promethazine
  • Diazepam
  • Dihydrocodeine; Guaifenesin; Pseudoephedrine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Dobutamine
  • Dopamine
  • Dronabinol
  • Droperidol
  • Enflurane
  • Epinephrine
  • Esketamine
  • Estazolam
  • Eszopiclone
  • Ethanol
  • Etomidate
  • 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
  • Nefazodone
  • Norepinephrine
  • Opiate Agonists-Antagonists
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Perampanel
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenelzine
  • Phenothiazines
  • Phenylephrine; Promethazine
  • Pimozide
  • Pramipexole
  • Pregabalin
  • Prilocaine; Epinephrine
  • Procarbazine
  • Prochlorperazine
  • Promethazine
  • Propofol
  • Quazepam
  • Racepinephrine
  • Ramelteon
  • Remifentanil
  • 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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