candesartan cilexetil indications/contra

Stem definitionDrug idCAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic) 475 145040-37-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • candesartan cilexetil
  • TCV-116
  • TCV 116
a nonpeptide angiotensin II receptor antagonist
  • Molecular weight: 610.67
  • Formula: C33H34N6O6
  • CLOGP: 7.08
  • LIPINSKI: 3
  • HAC: 12
  • HDO: 1
  • TPSA: 143.34
  • ALOGS: -5.48
  • ROTB: 13

Drug dosage:

DoseUnitRoute
8 mg O

Approvals:

DateAgencyCompanyOrphan
June 4, 1998 FDA ASTRAZENECA

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
Acute kidney injury 1258.02 33.81 392 2508 49291 3333668
Hyperkalaemia 735.32 33.81 188 2712 11106 3371853
Hypotension 597.29 33.81 226 2674 49288 3333671
Hyponatraemia 421.81 33.81 136 2764 18223 3364736
Oligohydramnios 377.84 33.81 71 2829 943 3382016
Drug interaction 266.66 33.81 126 2774 46686 3336273
Renal failure 251.97 33.81 109 2791 32831 3350128
Bradycardia 250.53 33.81 90 2810 16579 3366380
Blood creatinine increased 248.18 33.81 96 2804 21722 3361237
Orthostatic hypotension 241.09 33.81 66 2834 4970 3377989
Fall 205.51 33.81 114 2786 58769 3324190
Dizziness 200.63 33.81 123 2777 76389 3306570
Syncope 199.62 33.81 86 2814 25547 3357412
Dehydration 165.21 33.81 82 2818 33567 3349392
Renal impairment 157.72 33.81 66 2834 18195 3364764
Dyspnoea 151.67 33.81 116 2784 102818 3280141
Malaise 150.96 33.81 97 2803 65080 3317879
Hypertension 149.17 33.81 80 2820 38386 3344573
Blood pressure increased 138.93 33.81 64 2836 22166 3360793
Rhabdomyolysis 136.27 33.81 57 2843 15672 3367287
Exposure during pregnancy 131.71 33.81 66 2834 27497 3355462
Angioedema 124.92 33.81 53 2847 15082 3367877
Confusional state 119.78 33.81 69 2831 37929 3345030
Loss of consciousness 115.93 33.81 61 2839 28086 3354873
Lactic acidosis 114.29 33.81 41 2859 7459 3375500
Interstitial lung disease 112.07 33.81 48 2852 13968 3368991
Circulatory collapse 107.18 33.81 37 2863 6012 3376947
Pulmonary hypoplasia 103.51 33.81 19 2881 218 3382741
Blood pressure inadequately controlled 103.42 33.81 26 2874 1394 3381565
Skull malformation 95.28 33.81 18 2882 244 3382715

Pharmacologic Action:

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SourceCodeDescription
ATC C09CA06 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, PLAIN
Angiotensin II antagonists, plain
ATC C09DA06 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and diuretics
ATC C09DB07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
FDA MoA N0000000070 Angiotensin 2 Receptor Antagonists
FDA EPC N0000175561 Angiotensin 2 Receptor Blocker
MeSH PA D047228 Angiotensin II Type 1 Receptor Blockers
MeSH PA D057911 Angiotensin Receptor Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Chronic heart failure indication 48447003
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Oliguria contraindication 83128009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Surgical procedure contraindication 387713003
Azotemia contraindication 445009001
Atrial fibrillation off-label use 49436004 DOID:0060224
Diabetic renal disease off-label use 127013003
Diastolic heart failure off-label use 418304008 DOID:9775
Nondiabetic Proteinuric Nephropathy off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.25 acidic
pKa2 3.2 Basic

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
Type-1 angiotensin II receptor GPCR ANTAGONIST UNKNOWN CHEMBL
Adenosine receptor A3 GPCR Ki 6.16 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 5.76 CHEMBL
Cytochrome P450 2C9 Enzyme IC50 5.52 CHEMBL
Sodium-dependent noradrenaline transporter Transporter Ki 5.52 CHEMBL
Thromboxane-A synthase Enzyme IC50 5.51 CHEMBL
Beta-3 adrenergic receptor GPCR Ki 5.49 CHEMBL
Epidermal growth factor receptor Kinase IC50 5.48 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase IC50 5.23 CHEMBL
Cytochrome P450 3A4 Enzyme IC50 5.05 CHEMBL
Cruzipain Enzyme IC50 4.38 CHEMBL
Type-1 angiotensin II receptor GPCR IC50 6.96 CHEMBL
Type-1 angiotensin II receptor GPCR Ki 9.19 CHEMBL

External reference:

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IDSource
4021148 VUID
N0000179517 NUI
C0527379 UMLSCUI
D00522 KEGG_DRUG
DB00796 DRUGBANK_ID
CHEMBL1014 ChEMBL_ID
CHEMBL1016 ChEMBL_ID
4021148 VANDF
N0000148601 NDFRT
N0000179517 NDFRT
007276 NDDF
7490 MMSL
188909 MMSL
108589006 SNOMEDCT_US
135481 RXNORM
386878000 SNOMEDCT_US
C081643 MESH_SUPPLEMENTAL_RECORD_UI
2540 PUBCHEM_CID
R85M2X0D68 UNII
7239 INN_ID
139481-59-7 SECONDARY_CAS_RN
C077793 MESH_SUPPLEMENTAL_RECORD_UI
DB13919 DRUGBANK_ID
CHEBI:3348 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
ATACAND HUMAN PRESCRIPTION DRUG LABEL 1 0186-0004 TABLET 4 mg ORAL NDA 19 sections
ATACAND HUMAN PRESCRIPTION DRUG LABEL 1 0186-0008 TABLET 8 mg ORAL NDA 19 sections
ATACAND HUMAN PRESCRIPTION DRUG LABEL 1 0186-0016 TABLET 16 mg ORAL NDA 19 sections
ATACAND HUMAN PRESCRIPTION DRUG LABEL 1 0186-0032 TABLET 32 mg ORAL NDA 19 sections
ATACAND HCT HUMAN PRESCRIPTION DRUG LABEL 2 0186-0162 TABLET 16 mg ORAL NDA 12 sections
ATACAND HCT HUMAN PRESCRIPTION DRUG LABEL 2 0186-0322 TABLET 32 mg ORAL NDA 12 sections
ATACAND HCT HUMAN PRESCRIPTION DRUG LABEL 2 0186-0324 TABLET 32 mg ORAL NDA 12 sections
Candesartan Cilexetil and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-3001 TABLET 16 mg ORAL ANDA 12 sections
Candesartan Cilexetil and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-3002 TABLET 32 mg ORAL ANDA 12 sections
Candesartan Cilexetil and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0378-3003 TABLET 32 mg ORAL ANDA 12 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 0781-5936 TABLET 4 mg ORAL ANDA 19 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 0781-5937 TABLET 8 mg ORAL ANDA 19 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 0781-5938 TABLET 16 mg ORAL ANDA 19 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 0781-5939 TABLET 32 mg ORAL ANDA 19 sections
Candesartan HUMAN PRESCRIPTION DRUG LABEL 1 33342-114 TABLET 4 mg ORAL ANDA 20 sections
Candesartan HUMAN PRESCRIPTION DRUG LABEL 1 33342-115 TABLET 8 mg ORAL ANDA 20 sections
Candesartan HUMAN PRESCRIPTION DRUG LABEL 1 33342-116 TABLET 16 mg ORAL ANDA 20 sections
Candesartan HUMAN PRESCRIPTION DRUG LABEL 1 33342-117 TABLET 32 mg ORAL ANDA 20 sections
Candesartan Cilexetil and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33342-131 TABLET 16 mg ORAL ANDA 13 sections
Candesartan Cilexetil and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33342-132 TABLET 32 mg ORAL ANDA 13 sections
Candesartan Cilexetil and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 33342-133 TABLET 32 mg ORAL ANDA 13 sections
CANDESARTAN CILEXETIL HUMAN PRESCRIPTION DRUG LABEL 1 46708-060 TABLET 32 mg ORAL ANDA 18 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 49884-658 TABLET 4 mg ORAL NDA authorized generic 19 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 49884-659 TABLET 8 mg ORAL NDA authorized generic 19 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 49884-660 TABLET 16 mg ORAL NDA authorized generic 19 sections
Candesartan cilexetil HUMAN PRESCRIPTION DRUG LABEL 1 49884-661 TABLET 32 mg ORAL NDA authorized generic 19 sections
ATACAND HUMAN PRESCRIPTION DRUG LABEL 1 54868-4413 TABLET 16 mg ORAL NDA 18 sections
ATACAND HUMAN PRESCRIPTION DRUG LABEL 1 54868-4612 TABLET 32 mg ORAL NDA 18 sections
ATACAND HCT HUMAN PRESCRIPTION DRUG LABEL 2 54868-4729 TABLET 16 mg ORAL NDA 12 sections
ATACAND HCT HUMAN PRESCRIPTION DRUG LABEL 2 54868-4869 TABLET 32 mg ORAL NDA 12 sections