Pentoxifylline


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Peripheral vascular disease
Adult: As extended-release tab: 400 mg tid, may be reduced to 400 mg bid according to toxicity.
Renal Impairment
CrCl (mL/min) Dosage
<30 Reduce dose by approx 30-50%, according to tolerability.
Hepatic Impairment
Severe: Dose reduction may be necessary.
Cách dùng
Should be taken with food.
Chống chỉ định
Hypersensitivity to pentoxifylline, other methyl xanthines. Cerebral and extensive retinal haemorrhage, acute MI, severe cardiac arrhythmias.
Thận trọng
Patient w/ risk factors complicated by haemorrhage (e.g. recent surgery, peptic ulceration, cerebral and/or retinal bleeding), cerebrovascular disease, hypotension, severe coronary artery disease. Renal and severe hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
Significant: Anaphylactic reaction, angina, transient hypotension, reduction in coronary artery perfusion, arrhythmia.
Nervous: Headache, dizziness, tremor, nervousness, drowsiness, insomnia, agitation, sleep disorder.
CV: Tachycardia, flushing.
GI: Nausea, vomiting, epigastric discomfort, abdominal distention, constipation, diarrhoea, dyspepsia, hypersalivation.
Resp: Bronchospasm.
Hepatic: Increased transaminases, cholestasis.
Haematologic: Thrombocytopenia, leukopenia/neutropenia, haemorrhage.
Ophthalmologic: Blurred vision.
Dermatologic: Rash, erythema, pruritus, urticaria.
MonitoringParameters
Monitor prothrombin time, Hb, haematocrit. Monitor renal function.
Quá liều
Symptoms: Somnolence, loss of consciousness, convulsions, agitation, flushing, hypotension and fever. Management: Symptomatic and supportive treatment. Perform gastric lavage and/or give activated charcoal. Maintain BP and support respiration and control convulsions.
Tương tác
Increased exposure and toxicity w/ cimetidine, ciprofloxacin. Increased risk of bleeding and prolonged prothrombin time w/ anticoagulants (e.g. warfarin), platelet aggregation inhibitors (e.g. clopidogrel), and ketorolac. May increase theophylline levels and toxicity. Increased pharmacological effects of antihypertensive agents, insulin and oral hypoglycaemic agents.
Tác dụng
Description: Pentoxifylline is a xanthine derivative. The exact mechanism of action has not been fully elucidated. But it is thought to decrease blood viscosity, increase leukocyte deformability and erythrocyte flexibility, and decrease neutrophil adhesion/activation. It also improves microcirculation and peripheral tissue oxygenation by increasing blood flow.
Onset: W/in 2-4 wk.
Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the GI tract. Time to peak plasma concentration: W/in 2-4 hr.
Distribution: Enters breast milk.
Metabolism: Undergoes extensive first pass metabolism in the liver. Metabolised in the erythrocyte membrane and liver via reduction and oxidation into active metabolite I [1-(5-hydroxyhexyl)-3,7-dimethylxanthine] and metabolite V [1-(3-carboxypropyl)-3,7-dimethylxanthine] respectively.
Excretion: Mainly via urine (95%; 50-80%, as metabolite V, 20%, as other metabolites); faeces (<4%). Plasma elimination half-life: 24-48 min (pentoxifylline); 60-96 min (metabolites).
Đặc tính

Chemical Structure Image
Pentoxifylline

Source: National Center for Biotechnology Information. PubChem Database. Pentoxifylline, CID=4740, https://pubchem.ncbi.nlm.nih.gov/compound/Pentoxifylline (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C. Protect from light.
Phân loại ATC
C04AD03 - pentoxifylline ; Belongs to the class of purine derivative agents. Used as peripheral vasodilators.
References
Anon. Pentoxifylline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/10/2017.

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

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

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

Pentoxifylline Tablet, Extended Release (PD-Rx Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 10/10/2017.

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