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Chỉ định và Liều dùng
Oral
Multiple sclerosis Adult: To improve walking disability: 10 mg 12 hrly, discontinue therapy if no improvement. Max: 20 mg daily.
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Suy thận
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Chống chỉ định
Hypersensitivity. History of seizures. Moderate to severe renal impairment (CrCl ≤50 mL/min).
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Thận trọng
Patient w/ arrhythmia, SA/AV conduction disorder. Mild renal impairment (CrCl 51-80 mL/min).
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Tác dụng không mong muốn
Significant: Anaphylaxis or severe allergic reactions (e.g. resp compromise, urticaria, tongue/throat angioedema), seizures, UTI.
Nervous: Insomia, dizziness, headache, anxiety, asthenia, paraesthesia, balance disorder, fatigue, risk of fall, tremor, exacerbation of multiple sclerosis. CV: Palpitations, tachycardia, peripheral oedema. GI: Constipation, dyspepsia, nausea, vomiting. Resp: Nasopharangytis, dyspnoea, pharyngolaryngeal pain. Musculoskeletal: Back pain, weakness, muscle spasm. |
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Thông tin tư vấn bệnh nhân
This drug may cause dizziness, if affected, do not drive or operate machinery.
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Chỉ số theo dõi
Assess risk of seizures, walking ability. Monitor EEG, renal function before initiation of therapy and monitor thereafter.
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Quá liều
Symptoms: Confusion, tremulousness, diaphoresis, seizures, status epilepticus, amnesia, involuntary and choreoathetoid movements, cardiac arrhythmias (e.g. supraventricular tachycardia/bradycardia), ventricular tachycardia, hypotension. Management: Supportive treatment. Repeated seizure activity may be treated w/ benzodiazepines, phenytoin or other anti-seizure therapy.
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Tương tác
Increased risk of seizures w/ drugs that lower seizure threshold (e.g. TCA, SSRI(s), phenothiazines, butyrophenones, tramadol). Increased serum concentration w/ organic cation transporter-2 (OCT2) inhibitor (e.g. cimetidine) or substrate (e.g. metformin, carvedilol, propranolol).
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Tác dụng
Description:
Mechanism of Action: Fampridine is a potassium channel blocker. The exact mechanism of action has not been fully elucidated, but it is thought that the inhibition of potassium channel reduces leakage of ionic current, thereby delaying repolarization and increasing conduction of action potentials in demyelinated axons. This results in improved peripheral motor neurologic function and strengthening of muscle fibre twitch activity. Pharmacokinetics: Absorption: Rapidly and extensively absorbed from the GI tract. Bioavailability: 96%. Time to peak plasma concentration: 3-4 hr. Distribution: Crosses blood-brain barrier. Volume of distribution: 2.6 L/kg. Plasma protein binding: 1-3%. Metabolism: Small portion (<10%) is metabolised in the liver via oxidation by CYP2E1 into 3-hydroxy-4-aminopyridine and conjugated 3-hydroxy-4-aminopyridine sulfate. Excretion: Mainly via urine (96%, 90% as unchanged drug; 4.3% as 3-hydroxy-4-aminopyridine, 2.6% as 3-hydroxy-4-aminopyridine sulfate); faeces (0.5%). Elimination half-life: 5.2-6.5 hr. |
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Đặc tính
 Source: National Center for Biotechnology Information. PubChem Database. 4-Aminopyridine, CID=1727, https://pubchem.ncbi.nlm.nih.gov/compound/4-Aminopyridine (accessed on Jan. 20, 2020) |
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Bảo quản
Store below 25°C. Protect from light and moisture.
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Phân loại MIMS
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Phân loại ATC
N07XX07 - fampridine ; Belongs to the class of other nervous system drugs.
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Tài liệu tham khảo
Ampyra Tab, Film Coated, Extended Release (Acroda Therapeutics, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/09/2017. Anon. Dalfampridine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/09/2017. Buckingham R (ed). Fampridine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2017. Joint Formulary Committee. Fampridine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2017. McEvoy GK, Snow EK, Miller J et al (eds). Dalfampridine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 08/09/2017. Preston CL (ed). Fampridine (Dalfampridine) + Miscellaneous. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/09/2017.
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