Gemfibrozil


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Hyperlipidaemias
Adult: 1.2 g daily in 2 divided doses. Alternatively, 900 mg as a single dose in the evening.
Renal Impairment
Mild to moderate (GFR 30-80 mL/min/1.73m2): Initially, 900 mg daily. Severe: Contraindicated.
Hepatic Impairment
Contraindicated.
Cách dùng
Should be taken on an empty stomach. Take 30 min before meals.
Chống chỉ định
History of photosensitivity or phototoxic reaction w/ fibrates. History of or pre-existing gall bladder or biliary tract disease (e.g. gallstones). Severe Hepatic (including primary biliary cirrhosis) and severe renal impairment. Lactation. Concomitant use w/ repaglinide, dasabuvir, or statins.
Thận trọng
Pregnancy. Mild to moderate renal impairment.
Phản ứng phụ
Significant: Myopathy, myositis, rhabdomyolysis, elevated hepatic transaminases and CPK, decreased Hb, haematocrit, WBC; increased risk of cholelithiasis, malignancy. Rarely, bone marrow hypoplasia, anaemia, eosinophilia, leucopenia, thrombocytopenia.
Nervous: Dizziness, drowsiness, headache, fatigue, paraesthesia, depression, peripheral neuritis/neuropathy, vertigo, headache.
CV: AF.
GI: Dry mouth, taste disturbance, appendicitis, diarrhoea, constipation, nausea, vomiting, abdominal pain, flatulence.
Resp: Laryngeal oedema.
Hepatic: Cholecystitis, cholestatic jaundice.
Genitourinary: Impotence, reduced libido.
Musculoskeletal: Myasthenia, muscle pain, myalgia, synovitis.
Ophthalmologic: Blurred vision.
Dermatologic: Exfoliative dermatitis, circumscribed exanthema, pruritus, urticaria, angioedema, dermatomyositis, eczema, rash. Rarely, photosensitivity.
Others: Hypokalaemia.
Thông tin tư vấn bệnh nhân
Avoid exposure to sunlight.
MonitoringParameters
Monitor lipid, blood sugar, blood count, and LFT.
Quá liều
Symptoms: Abdominal pain, cramps, abnormal LFT, diarrhoea, increased creatine phosphokinase (CPK), joint and muscle pain, nausea and vomiting. Management: Symptomatic and supportive treatment. In acute overdosage, perform gastric lavage immediately.
Tương tác
Increases the plasma concentration of rosiglitazone, pioglitazone, bexarotene. May potentiate the effect of coumarin type vit K antagonist anticoagulants (e.g. warfarin). Reduced bioavailability when given w/ resin-granule drugs (e.g. colestipol).
Potentially Fatal: Risk of severe hypoglycaemia w/ repaglinide. Increases dasabuvir exposure which may result in increased risk of QT prolongation. Increased risk of muscle related adverse effects (e.g. myopathy, rhabdomyolysis) w/ statins (e.g. simvastatin).
Tác dụng
Description: Gemfibrozil is a fibric acid derivative which decreases serum triglycerides and VLDL, and increases HDL cholesterol. The exact mechanism of its action has not been fully established but it has been shown to inhibit lipolysis of fat in adipose tissue and decrease hepatic fatty acid reuptake. It also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule of VLDL.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the GI tract. Bioavailability: Approx 100%. Time to peak plasma concentration: W/in 1-2 hr.
Distribution: Plasma protein binding: Approx 98%.
Metabolism: Metabolised in the liver via oxidation into hydroxymethyl and carboxyl metabolites; undergoes enterohepatic recirculation.
Excretion: Mainly via urine (approx 70%, mainly as glucuronide conjugates and metabolites); faeces (6%). Elimination half-life: Approx 1.5 hr.
Đặc tính

Chemical Structure Image
Gemfibrozil

Source: National Center for Biotechnology Information. PubChem Database. Gemfibrozil, CID=3463, https://pubchem.ncbi.nlm.nih.gov/compound/Gemfibrozil (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C. Protect from light and moisture.
Phân loại MIMS
Phân loại ATC
C10AB04 - gemfibrozil ; Belongs to the class of fibrates. Used in the treatment of hyperlipidemia.
References
Anon. Gemfibrozil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/05/2017.

Buckingham R (ed). Gemfibrozil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/05/2017.

Gemfibrozil Tablet, Film Coated (Apotex Corp.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/05/2017.

Joint Formulary Committee. Gemfibrozil. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/05/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Gemfibrozil. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 23/05/2017.

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