Peringatan Keamanan

The oral TDLO of gemfibrozil in humans is 18gm/kg/3Y.L8576 The oral LD50 in mice is 2218mg/kg and in rats is 1414mg/kg.L8576 The intraperitoneal LD50 in rats is 445mg/kg.L8576

Patients experiencing an overdose may present with abdominal cramps, adnormal liver function tests, diarrhea, increased CPK, joint and muscle pain, nausea, and vomiting.L8525 Patients should be treated with symptomatic and supportive measures.L8525

Gemfibrozil

DB01241

small molecule approved

Deskripsi

Gemfibrozil is a fibric acid agent, similar to clofibrate, used to treat Type IIb, IV, and V hyperlipidemias.A185777,L8525 Gemfibrozil is not a first line treatment and is prescribed to patients who have not responded adequately to weight loss, diet, exercise, and other medications.L8525

Gemfibrozil was granted FDA approval on 21 December 1981.L8525

Struktur Molekul 2D

Berat 250.3334
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Gemfibrozil has a plasma half-life of 1.5 hours.[L8525] In patients with renal failure the half life is 2.4h and in patients with liver disease the half life is 2.1h.[A185813]
Volume Distribusi The volume of distribution of gemfibrozil is estimated to be 0.8L/kg.[A185807]
Klirens (Clearance) The clearance of gemfibrozil is estimated to be 6.0L/h.[A185807]

Absorpsi

Gemfibrozil is absorbed from the gastrointestinal tract.L8525 In healthy volunteers, a 900mg oral dose of gemfibrozil has a Cmax of 46±16µg/mL with a Tmax of 2.2±1.1h.A185813 In patients with chronic renal failure, gemfibrozil has a Cmax of 13.8±11.1µg/mL with a Tmax of 2.3±1.0h.A185813 In patients with liver disease, gemfibrozil has a Cmax of 23.0±10.3µg/mL with a Tmax of 2.6±1.7h.A185813

Metabolisme

Gemfibrozil undergoes hydroxylation at the 5'-methyl and 4' positions to form the M1 and M2 metaolites respectivelyA185792. Gemfibrozil also undergoes O-glucuronidation to form gemfibrozil 1-beta glucuronide, an inhibitor of CYP2C8.A185783 This O-glucuronidation is primarily mediated by UGT2B7, but also by UGT1A1, UGT1A3, UGT1A9, UGT2B4, UGT2B17.A185783

Rute Eliminasi

Approximately 70% of a dose of gemfibrozil is eliminated in the urine.L8525 The majority of a dose is eliminated as a glucuronide conjugate and <2% is elimiinated as the unmetabolized drug.L8525 6% of a dose is eliminated in the feces.L8525 In healthy volunteers, 0.02-0.15% of a dose was detected in the urine as unmetabolized gemfibrozil, with 7-14% detected as conjugated metabolites.A185813 In patients with renal failure, trace amounts of unmetabolized gemfibrozil is present in the urine, with 0.5-9.8% detected as conjugated metabolites.A185813 In patients with liver disease, 0.1-0.2% of a dose was detected in the urine as unmetabolized gemfibrozil, with 25-50% detected as conjugated metabolites.A185813

Interaksi Makanan

1 Data
  • 1. Take before a meal. Take 30 minutes before meals.

Interaksi Obat

1273 Data
Pravastatin The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Pravastatin.
Lovastatin The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Lovastatin.
Cerivastatin The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Cerivastatin.
Simvastatin The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Simvastatin.
Atorvastatin The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Atorvastatin.
Fluvastatin The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Fluvastatin.
Mevastatin The risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Mevastatin.
Pitavastatin The risk or severity of myopathy and rhabdomyolysis can be increased when Gemfibrozil is combined with Pitavastatin.
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Gemfibrozil.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Gemfibrozil.
Flibanserin The serum concentration of Flibanserin can be increased when it is combined with Gemfibrozil.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Gemfibrozil resulting in a loss in efficacy.
Irinotecan The risk or severity of neutropenia can be increased when Gemfibrozil is combined with Irinotecan.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Gemfibrozil.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Gemfibrozil.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Gemfibrozil.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Gemfibrozil.
Cefotiam The excretion of Cefotiam can be decreased when combined with Gemfibrozil.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Gemfibrozil.
Methotrexate The excretion of Methotrexate can be decreased when combined with Gemfibrozil.
Cephalexin The excretion of Cephalexin can be decreased when combined with Gemfibrozil.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Gemfibrozil.
Acyclovir The excretion of Acyclovir can be decreased when combined with Gemfibrozil.
Cefaclor The excretion of Cefaclor can be decreased when combined with Gemfibrozil.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Gemfibrozil.
Cefazolin The excretion of Cefazolin can be decreased when combined with Gemfibrozil.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Gemfibrozil.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Gemfibrozil.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Gemfibrozil.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Gemfibrozil.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Gemfibrozil.
Tenofovir The excretion of Tenofovir can be decreased when combined with Gemfibrozil.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Gemfibrozil.
Piperacillin The excretion of Piperacillin can be decreased when combined with Gemfibrozil.
Trifluridine The excretion of Trifluridine can be decreased when combined with Gemfibrozil.
Allopurinol The excretion of Allopurinol can be decreased when combined with Gemfibrozil.
Cefdinir The excretion of Cefdinir can be decreased when combined with Gemfibrozil.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Gemfibrozil.
Tetracycline The excretion of Tetracycline can be decreased when combined with Gemfibrozil.
Doripenem The excretion of Doripenem can be decreased when combined with Gemfibrozil.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Gemfibrozil.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Gemfibrozil.
Succinic acid The excretion of Succinic acid can be decreased when combined with Gemfibrozil.
Citrulline The excretion of Citrulline can be decreased when combined with Gemfibrozil.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Gemfibrozil.
Leucovorin The excretion of Leucovorin can be decreased when combined with Gemfibrozil.
Fluorescein The excretion of Fluorescein can be decreased when combined with Gemfibrozil.
Quinapril The excretion of Quinapril can be decreased when combined with Gemfibrozil.
Famotidine The excretion of Famotidine can be decreased when combined with Gemfibrozil.
Tazobactam The excretion of Tazobactam can be decreased when combined with Gemfibrozil.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Gemfibrozil.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Gemfibrozil.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Gemfibrozil.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Gemfibrozil.
Avibactam The excretion of Avibactam can be decreased when combined with Gemfibrozil.
Relebactam The excretion of Relebactam can be decreased when combined with Gemfibrozil.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Gemfibrozil.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Gemfibrozil.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Gemfibrozil.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Gemfibrozil.
Pioglitazone The serum concentration of Pioglitazone can be increased when it is combined with Gemfibrozil.
Treprostinil The serum concentration of Treprostinil can be increased when it is combined with Gemfibrozil.
Lamotrigine The metabolism of Gemfibrozil can be increased when combined with Lamotrigine.
Testosterone propionate The metabolism of Gemfibrozil can be increased when combined with Testosterone propionate.
Ezetimibe The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Ezetimibe.
Clofibrate The risk or severity of adverse effects can be increased when Clofibrate is combined with Gemfibrozil.
Fenofibrate The risk or severity of adverse effects can be increased when Fenofibrate is combined with Gemfibrozil.
Bezafibrate The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Bezafibrate.
Etofibrate The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Etofibrate.
Ciprofibrate The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Ciprofibrate.
Simfibrate The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Simfibrate.
Ronifibrate The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Ronifibrate.
Aluminium clofibrate The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Aluminium clofibrate.
Clofibride The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Clofibride.
Fenofibric acid The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Fenofibric acid.
Glycochenodeoxycholic Acid The therapeutic efficacy of Glycochenodeoxycholic Acid can be decreased when used in combination with Gemfibrozil.
Cholic Acid The therapeutic efficacy of Cholic Acid can be decreased when used in combination with Gemfibrozil.
Glycocholic acid The therapeutic efficacy of Glycocholic acid can be decreased when used in combination with Gemfibrozil.
Deoxycholic acid The therapeutic efficacy of Deoxycholic acid can be decreased when used in combination with Gemfibrozil.
Taurocholic acid The therapeutic efficacy of Taurocholic acid can be decreased when used in combination with Gemfibrozil.
Obeticholic acid The therapeutic efficacy of Obeticholic acid can be decreased when used in combination with Gemfibrozil.
Chenodeoxycholic acid The therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Gemfibrozil.
Taurochenodeoxycholic acid The therapeutic efficacy of Taurochenodeoxycholic acid can be decreased when used in combination with Gemfibrozil.
Tauroursodeoxycholic acid The therapeutic efficacy of Tauroursodeoxycholic acid can be decreased when used in combination with Gemfibrozil.
Bamet-UD2 The therapeutic efficacy of Bamet-UD2 can be decreased when used in combination with Gemfibrozil.
Dehydrocholic acid The therapeutic efficacy of Dehydrocholic acid can be decreased when used in combination with Gemfibrozil.
Hyodeoxycholic Acid The therapeutic efficacy of Hyodeoxycholic Acid can be decreased when used in combination with Gemfibrozil.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Gemfibrozil.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Gemfibrozil.
Cyclosporine The risk or severity of renal failure can be increased when Cyclosporine is combined with Gemfibrozil.
Colestipol Gemfibrozil can cause a decrease in the absorption of Colestipol resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Gemfibrozil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Gemfibrozil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Gemfibrozil resulting in a reduced serum concentration and potentially a decrease in efficacy.
Phenindione The risk or severity of bleeding can be increased when Gemfibrozil is combined with Phenindione.
Tioclomarol The risk or severity of bleeding can be increased when Gemfibrozil is combined with Tioclomarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Gemfibrozil is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Gemfibrozil is combined with Ethyl biscoumacetate.
Clorindione The risk or severity of bleeding can be increased when Gemfibrozil is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Gemfibrozil is combined with Diphenadione.

Target Protein

Peroxisome proliferator-activated receptor alpha PPARA
Lipoprotein lipase LPL
Solute carrier organic anion transporter family member 1B1 SLCO1B1
Organic anion transporter 3 SLC22A8
Solute carrier organic anion transporter family member 2B1 SLCO2B1
Solute carrier organic anion transporter family member 1B3 SLCO1B3

Referensi & Sumber

Synthesis reference: Gianfranco Piccoli, Antonio Tarquini, Giovanni Frare, "Process for the preparation of gemfibrozil." U.S. Patent US5654476, issued May, 1980.
Artikel (PubMed)
  • PMID: 3923042
    Saku K, Gartside PS, Hynd BA, Kashyap ML: Mechanism of action of gemfibrozil on lipoprotein metabolism. J Clin Invest. 1985 May;75(5):1702-12. doi: 10.1172/JCI111879.
  • PMID: 828261
    Okerholm RA, Keeley FJ, Peterson FE, Glazko AJ: The metabolism of gemfibrozil. Proc R Soc Med. 1976;69 Suppl 2:11-4.
  • PMID: 31424850
    Quintanilla Rodriguez BS, Correa R: Gemfibrozil .
  • PMID: 17670842
    Mano Y, Usui T, Kamimura H: The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos. 2007 Nov;35(11):2040-4. doi: 10.1124/dmd.107.017269. Epub 2007 Aug 1.
  • PMID: 9010630
    Sallustio BC, Fairchild BA, Pannall PR: Interaction of human serum albumin with the electrophilic metabolite 1-O-gemfibrozil-beta-D-glucuronide. Drug Metab Dispos. 1997 Jan;25(1):55-60.
  • PMID: 3468088
    Hamberger C, Barre J, Zini R, Taiclet A, Houin G, Tillement JP: In vitro binding study of gemfibrozil to human serum proteins and erythrocytes: interactions with other drugs. Int J Clin Pharmacol Res. 1986;6(6):441-9.
  • PMID: 2381138
    Knauf H, Kolle EU, Mutschler E: Gemfibrozil absorption and elimination in kidney and liver disease. Klin Wochenschr. 1990 Jul 5;68(13):692-8. doi: 10.1007/bf01667018.
  • PMID: 18370512
    Fereshetian AG, Davidson M, Haber H, Black DM: Gemfibrozil treatment in patients with elevated lipoprotein a: a pilot study. Clin Drug Investig. 1998;16(1):1-7. doi: 10.2165/00044011-199816010-00001.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 160 • International brands: 5
Produk
  • Apo-gemfibrozil
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Apo-gemfibrozil Cap 300mg USP
    Capsule • 300 mg • Oral • Canada • Generic • Approved
  • Dom-gemfibrozil
    Tablet • 600 mg • Oral • Canada • Generic • Approved
  • Dom-gemfibrozil
    Capsule • 300 mg • Oral • Canada • Generic • Approved
  • Gemfibrozil
    Tablet • 600 mg/1 • Oral • US • Approved
  • Gemfibrozil
    Tablet, film coated • 600 mg/1 • Oral • US • Generic • Approved
  • Gemfibrozil
    Tablet, film coated • 600 mg/1 • Oral • US • Generic • Approved
  • Gemfibrozil
    Tablet, film coated • 600 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 160 produk.
International Brands
  • Gemlipid — Farmellas Enterprises
  • Gen-Fibro
  • Genlip — Teofarma
  • Jezil
  • Lipur — Pfizer

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul