Tolcapone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Parkinson's disease
Adult: As adjunct to levodopa combination therapy in patient w/ "end of dose" motor fluctuations: 100 mg tid. 1st daily dose given at the same time w/ levodopa preparation, succeeding doses at 6 and 12 hr later. Max: 200 mg tid as tolerated, discontinue if no clinical benefit is obtained w/in 3 wk. Dose reduction of levodopa may be necessary.
Hepatic Impairment
Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Elevated liver enzyme, severe dyskinesia, history of neuroleptic malignant syndrome (NMS), symptom complex (e.g. non-traumatic rhabdomyolysis, hyperthermia), phaeochromocytoma. Hepatic impairment. Concomitant use w/ non-selective MAOI(s).
Thận trọng
Patients w/ pre-existing dyskinesia or dystonia, major psychotic disorder. Severe renal impairment. Pregnancy and lactation. Avoid abrupt withdrawal or dose reduction.
Phản ứng phụ
Significant: Abnormal thinking/behavioural changes (e.g. paranoid ideation, delusions, confusion, psychotic-like behavior, disorientation, aggressive behavior, agitation, delirium); diarrhoea, hallucinations, impulse control disorders (e.g. restless-leg syndrome, pathological gambling, increased libido, binge eating); melanoma, orthostatic hypotension, pleural/retroperitoneal fibrosis, somnolence, dyskinesia and psychosis exacerbation, NMS associated w/ withdrawal.
Nervous: Drowsiness, sleep disorders, dystonia, increased dream activity, dizziness, confusion, fatigue, loss of balance, paraesthesia, headache.
CV: Syncope, chest pain, hypotension, palpitations.
GI: Nausea, vomiting, anorexia, constipation, abdominal pain, dry mouth, dyspepsia, flatulence.
Resp: Upper resp tract infection, influenza, dyspnoea, sinus congestion.
Hepatic: Jaundice.
Genitourinary: Urine discolouration, UTI, haematuria, urination disorder.
Endocrine: Increased serum transaminases.
Musculoskeletal: Muscle cramps, hyperkinesia, hypokinesia, muscle rigidity, neck pain, arthritis.
Ophthalmologic: Cataract, inflammation.
Dermatologic: Increased sweating, pruritus.
Potentially Fatal: Severe hepatotoxicity (e.g. acute fulminant liver failure).
Thông tin tư vấn bệnh nhân
This drug may cause dizziness and/or sudden sleep disorder, if affected, do not drive or operate machinery.
MonitoringParameters
Perform LFT upon initiation of treatment and monitor every 2 wk for 1st yr; every 4 wk for next 6 mth; every 8 wk thereafter. Discontinue if liver enzyme levels exceed 2 times the upper limit of normal values. Monitor BP, signs and symptoms of mental status.
Quá liều
Symptoms: Nausea, vomiting, dizziness. Management: Symptomatic and supportive treatment. Hospitalization is advised.
Tương tác
May increase the bioavailability of levodopa.
Potentially Fatal: May cause severe hypertension w/ non-selective MAOI(s) (e.g. phenelzine, tranylcypromine).
Food Interaction
Food delays and decreases the absorption. May enhance CNS depressant effect of alcohol.
Tác dụng
Description: Tolcapone is a selective, reversible peripheral inhibitor of catechol-O-methyltransferase (COMT), an enzyme responsible for the breakdown of levodopa and dopamine. Its inhibition allows more levodopa to reach the brain, leading to enhanced dopaminergic activity.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Food delays and decreases the absorption. Absolute bioavailability: Approx 65%. Time to peak plasma concentration: W/in 2 hr.
Distribution: Volume of distribution: 9 L. Plasma protein binding: >99%, mainly to albumin.
Metabolism: Extensively metabolised in the liver, mainly via conjugation into inactive glucuronide; methylation by COMT into 3-O-methyltolcapone; and by CYP450 isoenzymes CYP3A4 and CYP2A6.
Excretion: Mainly via urine (approx 60% as metabolites; 0.5% as unchanged drug); faeces (40%). Elimination half-life: Approx 2-3 hr.
Đặc tính

Chemical Structure Image
Tolcapone

Source: National Center for Biotechnology Information. PubChem Database. Tolcapone, CID=4659569, https://pubchem.ncbi.nlm.nih.gov/compound/Tolcapone (accessed on Jan. 23, 2020)

Bảo quản
Store between 20-25°C.
Phân loại MIMS
Phân loại ATC
N04BX01 - tolcapone ; Belongs to the class of other dopaminergic agents used in the management of Parkinson's disease.
References
Anon. Tolcapone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/10/2017.

Bausch & Lomb (NZ) Ltd. Tasmar 100 mg Film-Coated Tablets data sheet 19 September 2016. Medsafe. http://www.medsafe.govt.nz/. Accessed 23/10/2017.

Buckingham R (ed). Tolcapone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com/. Accessed 23/10/2017.

Joint Formulary Committee. Tolcapone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/10/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Tolcapone. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 23/10/2017.

Preston CL (ed). Tolcapone + Phenelzine. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/11/2017.

Preston CL (ed). Tolcapone + Tranylcypromine. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/11/2017.

Tolcapone Tablets (Oceanside Pharmaceuticals). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/10/2017.

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