tolcapone

Contraindicated in:

Hypersensitivity;
Concurrent MAO inhibitor therapy;
Clinical evidence of liver disease.

Use Cautiously in:

Severe renal impairment (safety not established if CCr <25 mL/min);
OB: Lactation: Safety not established.

Adv. Reactions/Side Effects ⬆ ⬇

CV: orthostatic hypotension

Derm: ↑sweating, melanoma

GI: constipation, diarrhea, ↑liver enzymes, anorexia, HEPATOTOXICITY, nausea, vomiting

GU: hematuria, yellow discoloration of urine

Neuro: dyskinesia, dystonia, headache, sleep disorder, hallucinations, syncope, urges (gambling, sexual)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use with MAO inhibitors is not recommended; both agents inhibit the metabolic pathways of catecholamines.
May ↑ the effects of apomorphine, dobutamine, or isoproterenol; dose reduction may be necessary.
↑the bioavailability of levodopa by two-fold; this is a desired effect.

Availability ⬆ ⬇

(Generic available)

Tablets: 100 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 100 mg 3 times daily; may cautiously ↑ to 200 mg 3 times daily if benefit is justified.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a selective and reversible inhibitor of the enzyme catechol-O-methyltransferase.
Inhibition of this enzyme prevents the breakdown of levodopa, greatly increasing its availability to the CNS.

Therapeutic effects:

Prolongs duration of response to levodopa without end-of-dose motor fluctuations.
Decreased signs and symptoms of Parkinson’s disease.

Classifications ⬆ ⬇

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: catechol o methyltransferase comt inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly absorbed following oral administration with 65% bioavailability.

Distribution: Unknown.

Protein Binding: >99% bound to plasma proteins.

Metabolism/Excretion: Mostly metabolized by the liver; <0.5% excreted unchanged in urine.

Half-Life: 2–3 hr.

Time/Action Profile ⬆ ⬇

(blood levels)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.7 hr	8 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed. Caution patient not to discontinue tolcapone without consulting health care professional. Abrupt discontinuation or rapid dose reduction may result in neuroleptic malignant syndrome (↑ temperature, muscular rigidity, altered consciousness).
Caution patient to make position changes slowly to minimize orthostatic hypotension, especially at the beginning of therapy.
May affect mental and/or motor performance. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to avoid taking alcohol or other CNS depressants concurrently with tolcapone.
Inform patient and caregiver that hallucinations, nausea, dyskinesia, or dystonia may occur during tolcapone therapy.
Instruct patient to notify health care professional if persistent diarrhea occurs.
Advise patient to notify health care professional if symptoms of liver failure (clay-colored stools, jaundice, fatigue, loss of appetite, lethargy), suspicious or unusual skin changes, hallucinations, or new or increased gambling, sexual, or other intense urges occur.
Advise patient to notify health care professional if pregnancy is planned or suspected.
Emphasize the importance of routine follow-up exams.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

0187- Valeant Pharmaceuticals North America LLC
- 0187-0938- Tasmar
  - 0187-0938-01- 90 TABLET, FILM COATED in 1 BOTTLE (0187-0938-01)

49884- Par Pharmaceutical, Inc.
- 49884-254- Tolcapone
  - 49884-254-09- 90 TABLET, COATED in 1 BOTTLE (49884-254-09)

50742- Ingenus Pharmaceuticals, LLC
- 50742-193- TOLCAPONE
  - 50742-193-90- 90 TABLET in 1 BOTTLE (50742-193-90)

68682- Oceanside Pharmaceuticals
- 68682-938- Tolcapone
  - 68682-938-90- 90 TABLET, FILM COATED in 1 BOTTLE (68682-938-90)

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Indications ⬇

Contraind./Precautions ⬆ ⬇