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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
- abdominal pain
- agitation
- alopecia
- amnesia
- anemia
- angina
- anorexia
- apnea
- arthropathy
- atopic dermatitis
- atrial fibrillation
- bleeding
- bradycardia
- bronchospasm
- cardiac arrest
- cataracts
- chest pain (unspecified)
- chills
- cholecystitis
- cholelithiasis
- cholestasis
- choreoathetosis
- colitis
- confusion
- constipation
- cough
- dehydration
- delirium
- depression
- diabetes mellitus
- diarrhea
- diplopia
- dizziness
- drowsiness
- dysarthria
- dyskinesia
- dyspepsia
- dysphagia
- dyspnea
- dystonic reaction
- dysuria
- edema
- elevated hepatic enzymes
- emotional lability
- encephalopathy
- epistaxis
- erythema multiforme
- esophagitis
- euphoria
- fatigue
- fever
- flank pain
- flatulence
- furunculosis
- GI bleeding
- hallucinations
- headache
- heart failure
- hematuria
- hepatic failure
- hepatotoxicity
- hiccups
- hostility
- hypercholesterolemia
- hyperesthesia
- hyperglycemia
- hyperhidrosis
- hyperkinesis
- hypersalivation
- hypertension
- hypertonia
- hyperventilation
- hypotension
- hypoxia
- impotence (erectile dysfunction)
- impulse control symptoms
- influenza
- insomnia
- irritability
- jaundice
- laryngitis
- libido decrease
- libido increase
- malaise
- mania
- meningitis
- migraine
- muscle cramps
- myalgia
- myocardial infarction
- myoclonia
- nasal congestion
- nausea
- neuropathic pain
- nocturia
- ocular hemorrhage
- ocular inflammation
- ocular pain
- oliguria
- oral ulceration
- orthostatic hypotension
- otalgia
- palpitations
- paranoia
- paresthesias
- parosmia
- peptic ulcer
- pericardial effusion
- pharyngitis
- pleural effusion
- polyuria
- pruritus
- psychosis
- pulmonary embolism
- pulmonary fibrosis
- rash
- rhabdomyolysis
- rhinitis
- seborrhea
- sinus tachycardia
- skin discoloration
- stroke
- sudden sleep onset
- syncope
- thrombocytopenia
- thrombosis
- tinnitus
- tremor
- urinary incontinence
- urinary retention
- urine discoloration
- urticaria
- vaginitis
- vertigo
- vomiting
- withdrawal
- 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