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Chỉ định và Liều dùng
Oral
Idiopathic parkinsonism Adult: 1 mg once daily as monotherapy or as adjunctive therapy to levodopa.
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Suy gan
Mild: 0.5 mg once daily.
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Cách dùng
May be taken with or without food. Avoid tyramine-rich foods, beverages or dietary supplements & amines (from cough/cold prep).
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Chống chỉ định
Severe hepatic impairment. Concomitant use w/ other MAOIs and pethidine w/in 14 days after discontinuation of therapy; St John's wort.
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Thận trọng
Mild to moderate hepatic impairment. Pregnancy and lactation
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Tác dụng không mong muốn
Headache, flu-like syndrome, malaise, neck pain, angina pectoris, dyspepsia, anorexia, leucopenia, arthralgia, arthritis, depression, vertigo, rhinitis, conjunctivitis, skin rashes, melanoma, and urinary urgency. Rarely, CVA and MI.
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Thông tin tư vấn bệnh nhân
Avoid tobacco smoking.
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Chỉ số theo dõi
Monitor BP, symptoms of parkinsonism, new or worsening mental status and behavioural changes, somnolence and falling asleep during daily activities and skin examination for presence of melanoma.
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Quá liều
Symptoms: Dysphoria, hypomania, hypertensive crisis and serotonin syndrome. Management: Symptomatic and supportive therapy.
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Tương tác
Increased plasma levels w/ potent CYP1A2 inhibitors (e.g. ciprofloxacin). Increased clearance w/ entacapone.
Potentially Fatal: Increased risk of non-selective MAO inhibition w/ other MAOIs and pethidine that may lead to hypertensive crises. |
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Tương tác với thức ăn
Increased risk of hypertensive crises w/ St John's wort. May reduce plasma concentration w/ tobacco smoking.
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Tác dụng
Description:
Mechanism of Action: Rasagiline is a potent, irreversible monoamine oxidase (MAO)-B selective inhibitor which may cause an increase in extracellular levels of dopamine in the striatum, leading to reduced symptomatic motor deficits of Parkinson's disease. Duration: Approx 1 wk (irreversible inhibition). Pharmacokinetics: Absorption: Rapidly absorbed from the GI tract. Absolute bioavailability: Approx 36%. Time to peak plasma concentration: Approx 30-60 min. Distribution: Plasma protein binding: Approx 60-70%. Metabolism: Undergoes extensive hepatic metabolism via N-dealkylation and/or hydroxylation to yield 1-aminoindan (major metabolite), 3-hydroxy-N-propargyl-1 aminoindan and 3-hydroxy-1-aminoindan by CYP1A2 isoenzyme, and conjugation to yield glucuronides. Excretion: Mainly in the urine (<1% as unchanged drug) and partly in the faeces. Terminal half-life: 0.6-2 hr. |
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Đặc tính
 Source: National Center for Biotechnology Information. PubChem Database. Rasagiline, CID=3052776, https://pubchem.ncbi.nlm.nih.gov/compound/Rasagiline (accessed on Jan. 22, 2020) |
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Bảo quản
Store below 25°C.
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Phân loại MIMS
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Phân loại ATC
N04BD02 - rasagiline ; Belongs to the class of dopaminergic agents, monoamine oxidase B inhibitors. Used in the management of Parkinson's disease.
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Tài liệu tham khảo
Anon. Rasagiline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/04/2016. Buckingham R (ed). Rasagiline Mesilate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2016. Joint Formulary Committee. Rasagiline. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/04/2016. McEvoy GK, Snow EK, Miller J et al (eds). Rasagiline Mesylate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/04/2016.
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