telmisartan indications/contra

Stem definitionDrug idCAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic) 2583 144701-48-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • telmisartan
  • tolura
  • micardis
  • pritor
angiotensin II receptor antagonist and antihypertensive agent; structure given in first source
  • Molecular weight: 514.63
  • Formula: C33H30N4O2
  • CLOGP: 7.29
  • LIPINSKI: 2
  • HAC: 6
  • HDO: 1
  • TPSA: 72.94
  • ALOGS: -5.17
  • ROTB: 7

Drug dosage:

DoseUnitRoute
40 mg O

Approvals:

DateAgencyCompanyOrphan
Nov. 10, 1998 FDA BOEHRINGER INGELHEIM

FDA Adverse Event Reporting System

scroll-->
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 354.32 27.98 160 2983 49523 3333193
Hyponatraemia 320.41 27.98 113 3030 18246 3364470
Hyperkalaemia 314.86 27.98 99 3044 11195 3371521
Dizziness 232.22 27.98 139 3004 76373 3306343
Interstitial lung disease 231.82 27.98 83 3060 13933 3368783
Hypotension 212.45 27.98 113 3030 49401 3333315
Blood pressure increased 208.03 27.98 87 3056 22143 3360573
Loss of consciousness 172.78 27.98 82 3061 28065 3354651
Hypoglycaemia 143.77 27.98 59 3084 14259 3368457
Angioedema 133.92 27.98 57 3086 15078 3367638
Blood pressure inadequately controlled 131.35 27.98 32 3111 1388 3381328
Syncope 131.16 27.98 66 3077 25567 3357149
Nausea 121.97 27.98 117 3026 129528 3253188
Asthenia 121.94 27.98 88 3055 65577 3317139
Suicide attempt 121.65 27.98 54 3089 15793 3366923
Fall 121.09 27.98 84 3059 58799 3323917
Renal impairment 120.52 27.98 56 3087 18205 3364511
Renal failure 115.60 27.98 66 3077 32874 3349842
Dehydration 114.29 27.98 66 3077 33583 3349133
Hepatic function abnormal 104.98 27.98 44 3099 11183 3371533
Hypertensive crisis 101.83 27.98 31 3112 3116 3379600
Liver disorder 98.72 27.98 41 3102 10182 3372534
Rhabdomyolysis 96.85 27.98 46 3097 15683 3367033
Orthostatic hypotension 91.33 27.98 32 3111 5004 3377712
Blood creatinine increased 90.94 27.98 49 3094 21769 3360947
Oedema peripheral 89.80 27.98 57 3086 34304 3348412
Blood creatine phosphokinase increased 89.21 27.98 41 3102 12972 3369744
Hypertension 88.74 27.98 59 3084 38407 3344309
Blood pressure decreased 86.81 27.98 41 3102 13795 3368921
Rash 84.07 27.98 73 3070 70748 3311968

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC C09CA07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, PLAIN
Angiotensin II antagonists, plain
ATC C09DA07 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and diuretics
ATC C09DB04 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
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
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35457 EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
CHEBI has role CHEBI:61016 angiotensin receptor antagonist
FDA MoA N0000000070 Angiotensin 2 Receptor Antagonists
FDA EPC N0000175561 Angiotensin 2 Receptor Blocker

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Cerebrovascular accident indication 230690007 DOID:6713
Myocardial Infarction Prevention indication
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Obstruction of bile duct contraindication 30144000 DOID:13580
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
Hepatic failure contraindication 59927004
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
Chronic idiopathic constipation contraindication 82934008
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:2527
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Azotemia contraindication 445009001
Severe Aortic Valve Stenosis contraindication
Chronic heart failure off-label use 48447003
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

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.65 acidic
pKa2 5.79 Basic
pKa3 5.13 Basic

Orange Book patent data (new drug applications)

scroll-->
Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
80MG MICARDIS BOEHRINGER INGELHEIM N020850 Nov. 10, 1998 RX TABLET ORAL 7998953 June 6, 2020 REDUCTION OF CARDIAC TISSUE DAMAGE ASSOCIATED WITH MYOCARDIAL INFARCTION
80MG MICARDIS BOEHRINGER INGELHEIM N020850 Nov. 10, 1998 RX TABLET ORAL 8003679 Oct. 6, 2022 TREATMENT OR PREVENTION OF STROKE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Type-1 angiotensin II receptor GPCR ANTAGONIST IC50 9.31 CHEMBL CHEMBL
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor EC50 5.82 CHEMBL
Multidrug and toxin extrusion protein 1 Transporter IC50 4.75 CHEMBL
Type-2 angiotensin II receptor GPCR IC50 9.48 CHEMBL
Angiotensin-converting enzyme Enzyme Ki 5.22 CHEMBL
Glycine receptor subunit alpha-1 Ion channel EC50 5.49 CHEMBL
Type-1B angiotensin II receptor GPCR IC50 8.52 CHEMBL
Type-1A angiotensin II receptor GPCR Ki 9.64 CHEMBL

External reference:

scroll-->
IDSource
592 IUPHAR_LIGAND_ID
4021146 VUID
N0000148599 NUI
C0248719 UMLSCUI
D00627 KEGG_DRUG
DB00966 DRUGBANK_ID
4021146 VANDF
N0000006703 NDFRT
N0000148599 NDFRT
007683 NDDF
53287 MMSL
d04364 MMSL
7789 MMSL
73494 RXNORM
129487008 SNOMEDCT_US
387069000 SNOMEDCT_US
CHEMBL1017 ChEMBL_ID
65999 PUBCHEM_CID
C084178 MESH_SUPPLEMENTAL_RECORD_UI
U5SYW473RQ UNII
7144 INN_ID
CHEBI:9434 CHEBI
TLS PDB_CHEM_ID

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0054-0542 TABLET 20 mg ORAL NDA authorized generic 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0054-0543 TABLET 40 mg ORAL NDA authorized generic 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0054-0544 TABLET 80 mg ORAL NDA authorized generic 19 sections
telmisartan and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0054-0545 TABLET 40 mg ORAL NDA authorized generic 18 sections
telmisartan and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0054-0546 TABLET 80 mg ORAL NDA authorized generic 18 sections
telmisartan and hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 2 0054-0547 TABLET 80 mg ORAL NDA authorized generic 18 sections
Telmisartan and Amlodipine HUMAN PRESCRIPTION DRUG LABEL 2 0378-1075 TABLET 40 mg ORAL ANDA 19 sections
Telmisartan and Amlodipine HUMAN PRESCRIPTION DRUG LABEL 2 0378-1076 TABLET 40 mg ORAL ANDA 19 sections
Telmisartan and Amlodipine HUMAN PRESCRIPTION DRUG LABEL 2 0378-1077 TABLET 80 mg ORAL ANDA 19 sections
Telmisartan and Amlodipine HUMAN PRESCRIPTION DRUG LABEL 2 0378-1078 TABLET 80 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0378-2920 TABLET 20 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0378-2921 TABLET 40 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0378-2922 TABLET 80 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0591-3292 TABLET 20 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0591-3293 TABLET 40 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0591-3294 TABLET 80 mg ORAL ANDA 19 sections
Micardis HUMAN PRESCRIPTION DRUG LABEL 1 0597-0039 TABLET 20 mg ORAL NDA 18 sections
Micardis HUMAN PRESCRIPTION DRUG LABEL 1 0597-0040 TABLET 40 mg ORAL NDA 18 sections
Micardis HUMAN PRESCRIPTION DRUG LABEL 1 0597-0041 TABLET 80 mg ORAL NDA 18 sections
Micardis HCT HUMAN PRESCRIPTION DRUG LABEL 2 0597-0042 TABLET 80 mg ORAL NDA 18 sections
Micardis HCT HUMAN PRESCRIPTION DRUG LABEL 2 0597-0043 TABLET 40 mg ORAL NDA 18 sections
Micardis HCT HUMAN PRESCRIPTION DRUG LABEL 2 0597-0044 TABLET 80 mg ORAL NDA 18 sections
Twynsta HUMAN PRESCRIPTION DRUG LABEL 2 0597-0124 TABLET, MULTILAYER 40 mg ORAL NDA 18 sections
Twynsta HUMAN PRESCRIPTION DRUG LABEL 2 0597-0125 TABLET, MULTILAYER 40 mg ORAL NDA 18 sections
Twynsta HUMAN PRESCRIPTION DRUG LABEL 2 0597-0126 TABLET, MULTILAYER 80 mg ORAL NDA 18 sections
Twynsta HUMAN PRESCRIPTION DRUG LABEL 2 0597-0127 TABLET, MULTILAYER 80 mg ORAL NDA 18 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0781-5372 TABLET 20 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0781-5374 TABLET 40 mg ORAL ANDA 19 sections
Telmisartan HUMAN PRESCRIPTION DRUG LABEL 1 0781-5378 TABLET 80 mg ORAL ANDA 19 sections
TELMISARTAN HUMAN PRESCRIPTION DRUG LABEL 1 13668-158 TABLET 80 mg ORAL ANDA 18 sections