gemfibrozil indications/contra

Stem definitionDrug idCAS RN
1285 25812-30-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gemfibrosil
  • gemfibrozil
  • decrelip
  • lopizid
A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol.
  • Molecular weight: 250.34
  • Formula: C15H22O3
  • CLOGP: 3.94
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 46.53
  • ALOGS: -3.95
  • ROTB: 6

Drug dosage:

DoseUnitRoute
1.20 g O

Approvals:

DateAgencyCompanyOrphan
Dec. 21, 1981 FDA PFIZER PHARMS

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Rhabdomyolysis 1627.85 42.38 312 749 15417 3369381
Acute kidney injury 518.95 42.38 157 904 49526 3335272
Drug hypersensitivity 459.71 42.38 133 928 35547 3349251
Blood creatine phosphokinase increased 389.90 42.38 95 966 12918 3371880
Myalgia 361.10 42.38 108 953 31967 3352831
Drug interaction 269.72 42.38 95 966 46717 3338081
Completed suicide 204.98 42.38 70 991 31044 3353754
Asthenia 151.02 42.38 69 992 65596 3319202
Myopathy 127.58 42.38 29 1032 2830 3381968
Muscular weakness 118.91 42.38 42 1019 20299 3364499
Myositis 104.36 42.38 24 1037 2461 3382337
Haemodialysis 90.24 42.38 24 1037 4468 3380330
Aspartate aminotransferase increased 87.89 42.38 34 1027 21079 3363719
Alanine aminotransferase increased 84.16 42.38 34 1027 23606 3361192
Blood creatinine increased 83.28 42.38 33 1028 21785 3363013
Polymyositis 73.69 42.38 14 1047 562 3384236
Chromaturia 66.56 42.38 19 1042 4579 3380219
Blood triglycerides increased 62.27 42.38 18 1043 4532 3380266
Liver function test abnormal 61.62 42.38 23 1038 12878 3371920
Hepatic enzyme increased 56.81 42.38 22 1039 13603 3371195
Blood cholesterol increased 54.21 42.38 18 1043 7151 3377647
Renal tubular necrosis 50.21 42.38 14 1047 3094 3381704
Gait disturbance 47.40 42.38 24 1037 27968 3356830
Fall 47.23 42.38 31 1030 58852 3325946
Abdominal pain 46.24 42.38 28 1033 46197 3338601
Hyperkalaemia 46.22 42.38 18 1043 11276 3373522
Dialysis 46.01 42.38 14 1047 4195 3380603
Blood urea increased 45.49 42.38 16 1045 7544 3377254
Chronic kidney disease 44.16 42.38 15 1046 6377 3378421
Renal failure 43.72 42.38 24 1037 32916 3351882

Pharmacologic Action:

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SourceCodeDescription
ATC C10AB04 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, PLAIN
Fibrates
FDA EPC N0000175596 Peroxisome Proliferator Receptor alpha Agonist
FDA MoA N0000175375 Peroxisome Proliferator-activated Receptor alpha Agonists
FDA Chemical/Ingredient N0000170118 PPAR alpha
CHEBI has role CHEBI:35679 antilipemic drug
MeSH PA D000963 Antimetabolites
MeSH PA D065687 Cytochrome P-450 CYP2C8 Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D000960 Hypolipidemic Agents
MeSH PA D057847 Lipid Regulating Agents
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertriglyceridemia indication 302870006
Primary Prevention of Coronary Heart Disease indication
Primary biliary cirrhosis contraindication 31712002 DOID:12236
Disorder of gallbladder contraindication 39621005 DOID:0060262
Acute nephropathy contraindication 58574008
Leukopenia contraindication 84828003 DOID:615
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Calculus in biliary tract contraindication 266474003
Anemia contraindication 271737000 DOID:2355
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Breastfeeding (mother) contraindication 413712001
Hypoalphalipoproteinemia off-label use 190785000

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.13 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Peroxisome proliferator-activated receptor alpha Nuclear hormone receptor AGONIST EC50 4.23 IUPHAR CHEMBL
Cytochrome P450 2C8 Enzyme Ki 5.74 WOMBAT-PK
Lipoprotein lipase Enzyme WOMBAT-PK
Cytochrome P450 2C9 Enzyme Ki 4.52 WOMBAT-PK
Transthyretin Secreted Kd 7 CHEMBL
Fatty acid-binding protein, liver Unclassified Ki 5.73 CHEMBL

External reference:

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IDSource
3439 IUPHAR_LIGAND_ID
4018639 VUID
N0000146952 NUI
C0017245 UMLSCUI
D00334 KEGG_DRUG
CHEMBL457 ChEMBL_ID
3463 PUBCHEM_CID
523 MMSL
4719 RXNORM
35282000 SNOMEDCT_US
387189002 SNOMEDCT_US
4778 MMSL
d00245 MMSL
4018639 VANDF
N0000146952 NDFRT
N0000007039 NDFRT
002050 NDDF
CHEBI:5296 CHEBI
DB01241 DRUGBANK_ID
Q8X02027X3 UNII
3899 INN_ID
D015248 MESH_DESCRIPTOR_UI
4TX PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Lopid HUMAN PRESCRIPTION DRUG LABEL 1 0071-0737 TABLET, FILM COATED 600 mg ORAL NDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0093-0670 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9130 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0143-9707 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0179-0037 TABLET, COATED 600 mg ORAL ANDA 13 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0179-0048 TABLET, COATED 600 mg ORAL ANDA 13 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0179-0221 TABLET 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0615-3559 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 0904-5988 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 10544-569 TABLET, FILM COATED 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 16714-101 TABLET 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 21695-732 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 24658-260 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 31722-225 TABLET 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 33261-146 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
GEMFIBROZIL HUMAN PRESCRIPTION DRUG LABEL 1 42806-260 TABLET 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 43063-745 TABLET 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 43353-090 TABLET, FILM COATED 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 43353-772 TABLET, FILM COATED 600 mg ORAL ANDA 13 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 50090-0458 TABLET 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 50268-350 TABLET 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 50436-6540 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 51138-588 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 51655-142 TABLET 600 mg ORAL ANDA 9 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 53002-1068 TABLET 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 53217-251 TABLET 600 mg ORAL ANDA 12 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 53808-0251 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 53808-0368 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 53808-0673 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections
Gemfibrozil HUMAN PRESCRIPTION DRUG LABEL 1 53808-0838 TABLET, FILM COATED 600 mg ORAL ANDA 11 sections