You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameTelmisartan
Accession NumberDB00966  (APRD01247)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. Recent studies suggest that telmisartan may also have PPAR-gamma agonistic properties that could potentially confer beneficial metabolic effects.

Structure
Thumb
Synonyms
4'-((1,4'-Dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid
4'-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid
4'-[(1,4'-Dimethyl-2'propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid
4'-[(1,7'-Dimethyl-2'-propyl-1H,3'h-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid
BIBR 277
Micardis
Telmisartan
External Identifiers
  • BIBR 277
  • BIBR 277SE
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Telmisartantablet80 mgoralActavis Pharma Company2012-10-19Not applicableCanada
Act Telmisartantablet40 mgoralActavis Pharma Company2012-10-19Not applicableCanada
Auro-telmisartantablet80 mgoralAuro Pharma Inc2016-04-08Not applicableCanada
Auro-telmisartantablet40 mgoralAuro Pharma Inc2016-04-08Not applicableCanada
Mar-telmisartantablet80 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mar-telmisartantablet40 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Micardistablet80 mg/1oralPhysicians Total Care, Inc.2002-03-25Not applicableUs
Micardistablet40 mg/1oralPhysicians Total Care, Inc.2005-01-19Not applicableUs
Micardistablet80 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-15Not applicableUs
Micardistablet80 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2000-12-01Not applicableUs
Micardistablet40 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2000-12-01Not applicableUs
Micardistablet20 mg/1oralBoehringer Ingelheim Pharmaceuticals, Inc.2000-12-01Not applicableUs
Micardistablet20 mg/1oralPhysicians Total Care, Inc.2010-11-02Not applicableUs
Micardis 40mg Tabtablet40 mgoralBoehringer Ingelheim (Canada) Ltd Ltee1999-09-01Not applicableCanada
Micardis 80mg Tabtablet80 mgoralBoehringer Ingelheim (Canada) Ltd Ltee1999-09-01Not applicableCanada
Mylan-telmisartantablet40 mgoralMylan Pharmaceuticals Ulc2012-01-10Not applicableCanada
Mylan-telmisartantablet80 mgoralMylan Pharmaceuticals Ulc2012-01-10Not applicableCanada
Ntp-telmisartantablet40 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-telmisartantablet80 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Pendo-telmisartantablet80 mgoralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
Pendo-telmisartantablet40 mgoralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
PMS-telmisartantablet80 mgoralPharmascience Inc2012-08-28Not applicableCanada
PMS-telmisartantablet40 mgoralPharmascience Inc2012-08-28Not applicableCanada
Ran-telmisartantablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.2013-06-14Not applicableCanada
Ran-telmisartantablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.2013-06-14Not applicableCanada
Sandoz Telmisartantablet80 mgoralSandoz Canada Incorporated2012-01-04Not applicableCanada
Sandoz Telmisartantablet40 mgoralSandoz Canada Incorporated2012-01-04Not applicableCanada
Septa-telmisartantablet40 mgoralSepta Pharmaceuticals IncNot applicableNot applicableCanada
Septa-telmisartantablet80 mgoralSepta Pharmaceuticals IncNot applicableNot applicableCanada
Telmisartantablet20 mg/1oralRoxane Laboratories, Inc.2014-01-08Not applicableUs
Telmisartantablet80 mgoralPharmascience Inc2015-02-12Not applicableCanada
Telmisartantablet40 mgoralPharmascience Inc2015-02-12Not applicableCanada
Telmisartantablet80 mgoralSivem Pharmaceuticals Ulc2012-07-26Not applicableCanada
Telmisartantablet40 mgoralSivem Pharmaceuticals Ulc2012-07-26Not applicableCanada
Telmisartantablet80 mg/1oralRoxane Laboratories, Inc.2014-01-08Not applicableUs
Telmisartantablet80 mgoralPro Doc Limitee2012-11-22Not applicableCanada
Telmisartantablet80 mgoralSanis Health Inc2012-07-20Not applicableCanada
Telmisartantablet40 mg/1oralRoxane Laboratories, Inc.2014-01-08Not applicableUs
Telmisartantablet40 mgoralPro Doc Limitee2012-11-22Not applicableCanada
Telmisartantablet40 mgoralSanis Health Inc2012-07-20Not applicableCanada
Telmisartan Tabletstablet80 mgoralAccord Healthcare Inc2014-03-12Not applicableCanada
Telmisartan Tabletstablet40 mgoralAccord Healthcare Inc2014-03-12Not applicableCanada
Teva-telmisartantablet80 mgoralTeva Canada Limited2012-01-09Not applicableCanada
Teva-telmisartantablet40 mgoralTeva Canada Limited2012-01-09Not applicableCanada
Torrent-telmisartantablet80 mgoralTorrent Pharmaceuticals LimitedNot applicableNot applicableCanada
Torrent-telmisartantablet40 mgoralTorrent Pharmaceuticals LimitedNot applicableNot applicableCanada
Van-telmisartantablet80 mgoralVanc Pharmaceuticals Inc2015-07-10Not applicableCanada
Van-telmisartantablet40 mgoralVanc Pharmaceuticals Inc2015-07-10Not applicableCanada
Zinda-telmisartantablet80 mgoralZinda Pharma LimitedNot applicableNot applicableCanada
Zinda-telmisartantablet40 mgoralZinda Pharma LimitedNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-telmisartantablet80 mgoralApotex Inc2014-07-18Not applicableCanada
Apo-telmisartantablet40 mgoralApotex Inc2014-07-18Not applicableCanada
Telmisartantablet20 mg/1oralGlenmark Pharmaceuticals Inc., Usa2014-07-07Not applicableUs
Telmisartantablet40 mg/1oralCadila Healthcare Limited2014-08-27Not applicableUs
Telmisartantablet20 mg/1oralCadila Healthcare Limited2014-08-27Not applicableUs
Telmisartantablet80 mg/1oralQualitest Pharmaceuticals2013-03-06Not applicableUs
Telmisartantablet20 mg/1oralMylan Pharmaceuticals Inc.2014-07-07Not applicableUs
Telmisartantablet80 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-08-27Not applicableUs
Telmisartantablet20 mg/1oralMedsource Pharmaceuticals2014-08-27Not applicableUs
Telmisartantablet40 mg/1oralQualitest Pharmaceuticals2013-03-06Not applicableUs
Telmisartantablet80 mg/1oralTorrent Pharmaceuticals Limited2014-07-07Not applicableUs
Telmisartantablet20 mg/1oralQualitest Pharmaceuticals2013-03-06Not applicableUs
Telmisartantablet40 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-08-27Not applicableUs
Telmisartantablet40 mg/1oralTorrent Pharmaceuticals Limited2014-07-07Not applicableUs
Telmisartantablet80 mg/1oralActavis Pharma, Inc.2014-01-08Not applicableUs
Telmisartantablet20 mg/1oralZydus Pharmaceuticals (USA) Inc.2014-08-27Not applicableUs
Telmisartantablet20 mg/1oralTorrent Pharmaceuticals Limited2014-07-07Not applicableUs
Telmisartantablet40 mg/1oralActavis Pharma, Inc.2014-01-08Not applicableUs
Telmisartantablet80 mg/1oralAurobindo Pharma Limited2015-09-03Not applicableUs
Telmisartantablet80 mg/1oralSandoz Inc2015-02-06Not applicableUs
Telmisartantablet20 mg/1oralActavis Pharma, Inc.2014-01-08Not applicableUs
Telmisartantablet40 mg/1oralAvera Mc Kennan Hospital2015-04-15Not applicableUs
Telmisartantablet40 mg/1oralAurobindo Pharma Limited2015-09-03Not applicableUs
Telmisartantablet80 mg/1oralGlenmark Pharmaceuticals Inc., Usa2014-07-07Not applicableUs
Telmisartantablet20 mg/1oralAurobindo Pharma Limited2015-09-03Not applicableUs
Telmisartantablet40 mg/1oralSandoz Inc2015-02-06Not applicableUs
Telmisartantablet80 mg/1oralMylan Pharmaceuticals Inc.2014-07-07Not applicableUs
Telmisartantablet40 mg/1oralGlenmark Pharmaceuticals Inc., Usa2014-07-07Not applicableUs
Telmisartantablet80 mg/1oralCadila Healthcare Limited2014-08-27Not applicableUs
Telmisartantablet20 mg/1oralSandoz Inc2015-02-06Not applicableUs
Telmisartantablet40 mg/1oralMylan Pharmaceuticals Inc.2014-07-07Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PritorNot Available
Brand mixtures
NameLabellerIngredients
Ach-telmisartan HctzAccord Healthcare Inc
Act Telmisartan/hctActavis Pharma Company
Apo-telmisartan/hctzApotex Inc
Micardis HctBoehringer Ingelheim Pharmaceuticals, Inc.
Micardis PlusBoehringer Ingelheim (Canada) Ltd Ltee
Mylan-telmisartan HctzMylan Pharmaceuticals Ulc
Ntp-telmisartan HctzTeva Canada Limited
Pendo-telmisartan-hctzPendopharm Division Of De Pharmascience Inc
PMS-telmisartan-hctzPharmascience Inc
Ran-telmisartan HctzRanbaxy Pharmaceuticals Canada Inc.
Sandoz Telmisartan HctSandoz Canada Incorporated
Telmisartan and AmlodipineMylan Pharmaceuticals Inc.
Telmisartan and HydrochlorothiazideRoxane Laboratories, Inc.
Telmisartan and Hydrochlorothiazide 40 Mg/12.5 mgAlembic Pharmaceuticals Limited
Telmisartan and Hydrochlorothiazide 80 Mg/12.5 mgAlembic Pharmaceuticals Limited
Telmisartan and Hydrochlorothiazide 80 Mg/25 mgAlembic Pharmaceuticals Limited
Telmisartan and HydrochlorthiazideTorrent Pharmaceuticals Limited
Telmisartan HctzSivem Pharmaceuticals Ulc
Telmisartan-hctzPro Doc Limitee
Telmisartan/hctzSanis Health Inc
Teva-telmisartan HctzTeva Canada Limited
Torrent-telmisartan and HydrochlorothiazideTorrent Pharmaceuticals Limited
TwynstaBoehringer Ingelheim Pharmaceuticals, Inc.
Van-telmisartan-hctzVanc Pharmaceuticals Inc
Zinda-telmisartan/ HctzZinda Pharma Limited
SaltsNot Available
Categories
UNIIU5SYW473RQ
CAS number144701-48-4
WeightAverage: 514.6169
Monoisotopic: 514.236876224
Chemical FormulaC33H30N4O2
InChI KeyInChIKey=RMMXLENWKUUMAY-UHFFFAOYSA-N
InChI
InChI=1S/C33H30N4O2/c1-4-9-30-35-31-21(2)18-24(32-34-27-12-7-8-13-28(27)36(32)3)19-29(31)37(30)20-22-14-16-23(17-15-22)25-10-5-6-11-26(25)33(38)39/h5-8,10-19H,4,9,20H2,1-3H3,(H,38,39)
IUPAC Name
2-(4-{[4-methyl-6-(1-methyl-1H-1,3-benzodiazol-2-yl)-2-propyl-1H-1,3-benzodiazol-1-yl]methyl}phenyl)benzoic acid
SMILES
CCCC1=NC2=C(C=C(C=C2C)C2=NC3=CC=CC=C3N2C)N1CC1=CC=C(C=C1)C1=CC=CC=C1C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBiphenyls and derivatives
Direct ParentBiphenyls and derivatives
Alternative Parents
Substituents
  • Biphenyl
  • Benzoic acid
  • Benzoic acid or derivatives
  • Benzimidazole
  • Phenylmethylamine
  • Benzoyl
  • N-substituted imidazole
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed alone or in combination with other classes of antihypertensives for the treatment of hypertension. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart failure (only in patients who cannot tolerate ACE inhibitors).
PharmacodynamicsTelmisartan is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. It has the highest affinity for the AT1 receptor among commercially available ARBS and has minimal affinity for the AT2 receptor. New studies suggest that telmisartan may also have PPARγ agonistic properties that could potentially confer beneficial metabolic effects, as PPARγ is a nuclear receptor that regulates specific gene transcription, and whose target genes are involved in the regulation of glucose and lipid metabolism, as well as anti-inflammatory responses. This observation is currently being explored in clinical trials. Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Telmisartan works by blocking the vasoconstrictor and aldosterone secretory effects of angiotensin II.
Mechanism of actionTelmisartan interferes with the binding of angiotensin II to the angiotensin II AT1-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Telmisartan does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels. Studies also suggest that telmisartan is a partial agonist of PPARγ, which is an established target for antidiabetic drugs. This suggests that telmisartan can improve carbohydrate and lipid metabolism, as well as control insulin resistance without causing the side effects that are associated with full PPARγ activators.
Related Articles
AbsorptionAbsolute bioavailability depends on dosage. Food slightly decreases the bioavailability (a decrease of about 6% is seen when the 40-mg dose is administered with food).
Volume of distribution
  • 500 L
Protein bindingHighly bound to plasma proteins (>99.5%), mainly albumin and a1-acid glycoprotein. Binding is not dose-dependent.
Metabolism

Minimally metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.

Route of eliminationFollowing either intravenous or oral administration of 14C-labeled telmisartan, most of the administered dose (>97%) was eliminated unchanged in feces via biliary excretion; only minute amounts were found in the urine (0.91% and 0.49% of total radioactivity, respectively).
Half lifeBi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.
Clearance
  • >800 mL/min
ToxicityIntravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Telmisartan Action PathwayDrug actionSMP00164
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8794
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.6061
P-glycoprotein inhibitor INon-inhibitor0.5261
P-glycoprotein inhibitor IIInhibitor0.8653
Renal organic cation transporterNon-inhibitor0.6047
CYP450 2C9 substrateNon-substrate0.7876
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5255
CYP450 1A2 substrateInhibitor0.5699
CYP450 2C9 inhibitorNon-inhibitor0.5481
CYP450 2D6 inhibitorNon-inhibitor0.7796
CYP450 2C19 inhibitorNon-inhibitor0.5509
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.601
Ames testNon AMES toxic0.6432
CarcinogenicityNon-carcinogens0.9094
BiodegradationNot ready biodegradable0.9862
Rat acute toxicity2.8075 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9166
hERG inhibition (predictor II)Non-inhibitor0.7114
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Boehringer ingelheim
Packagers
Dosage forms
FormRouteStrength
Tabletoral40 mg
Tabletoral80 mg
Tabletoral20 mg/1
Tabletoral40 mg/1
Tabletoral80 mg/1
Tabletoral
Tablet, multilayeroral
Prices
Unit descriptionCostUnit
Micardis 30 40 mg tablet Box110.11USD box
Micardis HCT 30 40-12.5 mg tablet Box106.34USD box
Micardis HCT 30 80-12.5 mg tablet Box106.18USD box
Micardis 30 80 mg tablet Box103.92USD box
Micardis HCT 30 80-25 mg tablet Box100.48USD box
Micardis 30 20 mg tablet Box99.7USD box
Micardis 20 mg tablet3.29USD tablet
Micardis hct 40-12.5 mg tablet3.29USD tablet
Micardis hct 80-12.5 mg tablet3.29USD tablet
Micardis hct 80-25 mg tablet3.29USD tablet
Micardis 40 mg tablet2.24USD tablet
Micardis 80 mg tablet2.24USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2060624 No1999-12-212012-02-04Canada
US5591762 No1994-01-072014-01-07Us
US6358986 No2000-01-102020-01-10Us
US7998953 No2000-06-062020-06-06Us
US8003679 No2002-10-062022-10-06Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point261-263 °CNot Available
water solubilityPractically insolubleNot Available
logP7.7Not Available
Caco2 permeability-4.82ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0035 mg/mLALOGPS
logP6.66ALOGPS
logP6.04ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)3.65ChemAxon
pKa (Strongest Basic)6.13ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area72.94 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity164.49 m3·mol-1ChemAxon
Polarizability58.61 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference
  1. Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. Pubmed
General References
  1. Sharpe M, Jarvis B, Goa KL: Telmisartan: a review of its use in hypertension. Drugs. 2001;61(10):1501-29. [PubMed:11558835 ]
  2. Smith DH: Treatment of hypertension with an angiotensin II-receptor antagonist compared with an angiotensin-converting enzyme inhibitor: a review of clinical studies of telmisartan and enalapril. Clin Ther. 2002 Oct;24(10):1484-501. [PubMed:12462282 ]
  3. Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. doi: 10.3762/bjoc.6.25. [PubMed:20502601 ]
  4. Galzerano D, Capogrosso C, Di Michele S, Galzerano A, Paparello P, Lama D, Gaudio C: New standards in hypertension and cardiovascular risk management: focus on telmisartan. Vasc Health Risk Manag. 2010 Mar 24;6:113-33. [PubMed:20448797 ]
External Links
ATC CodesC09CA07C09DA07C09DB04
AHFS Codes
  • 24:32.08
PDB EntriesNot Available
FDA labelDownload (47.4 KB)
MSDSDownload (101 KB)
Interactions
Drug Interactions
Drug
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Telmisartan.
AlfuzosinAlfuzosin may increase the hypotensive activities of Telmisartan.
AliskirenAliskiren may increase the hyperkalemic activities of Telmisartan.
AmifostineTelmisartan may increase the hypotensive activities of Amifostine.
ArdeparinArdeparin may increase the hyperkalemic activities of Telmisartan.
BrimonidineBrimonidine may increase the antihypertensive activities of Telmisartan.
ButabarbitalButabarbital may increase the hypotensive activities of Telmisartan.
ButethalButethal may increase the hypotensive activities of Telmisartan.
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Telmisartan.
CiprofloxacinTelmisartan may increase the arrhythmogenic activities of Ciprofloxacin.
CyclosporineTelmisartan may increase the hyperkalemic activities of Cyclosporine.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Telmisartan.
DiazoxideDiazoxide may increase the hypotensive activities of Telmisartan.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Telmisartan.
DrospirenoneTelmisartan may increase the hyperkalemic activities of Drospirenone.
DuloxetineTelmisartan may increase the orthostatic hypotensive activities of Duloxetine.
EplerenoneEplerenone may increase the hyperkalemic activities of Telmisartan.
HeparinHeparin may increase the hyperkalemic activities of Telmisartan.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Telmisartan.
HexobarbitalHexobarbital may increase the hypotensive activities of Telmisartan.
InfliximabThe risk or severity of adverse effects can be increased when Telmisartan is combined with Infliximab.
LevodopaTelmisartan may increase the orthostatic hypotensive activities of Levodopa.
LithiumThe serum concentration of Lithium can be increased when it is combined with Telmisartan.
MethohexitalMethohexital may increase the hypotensive activities of Telmisartan.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Telmisartan.
MolsidomineMolsidomine may increase the hypotensive activities of Telmisartan.
MoxonidineMoxonidine may increase the hypotensive activities of Telmisartan.
NicorandilNicorandil may increase the hypotensive activities of Telmisartan.
ObinutuzumabTelmisartan may increase the hypotensive activities of Obinutuzumab.
PentobarbitalPentobarbital may increase the hypotensive activities of Telmisartan.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Telmisartan.
PerindoprilThe risk or severity of adverse effects can be increased when Telmisartan is combined with Perindopril.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Telmisartan.
PrimidonePrimidone may increase the hypotensive activities of Telmisartan.
QuinineQuinine may increase the hypotensive activities of Telmisartan.
RamiprilThe risk or severity of adverse effects can be increased when Telmisartan is combined with Ramipril.
RisperidoneTelmisartan may increase the hypotensive activities of Risperidone.
RituximabTelmisartan may increase the hypotensive activities of Rituximab.
SecobarbitalSecobarbital may increase the hypotensive activities of Telmisartan.
TadalafilTadalafil may increase the antihypertensive activities of Telmisartan.
TolvaptanTolvaptan may increase the hyperkalemic activities of Telmisartan.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Telmisartan.
TreprostinilTreprostinil may increase the hypotensive activities of Telmisartan.
TriamtereneTelmisartan may increase the hyperkalemic activities of Triamterene.
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Telmisartan.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Telmisartan.
VardenafilVardenafil may increase the antihypertensive activities of Telmisartan.
YohimbineYohimbine may decrease the antihypertensive activities of Telmisartan.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name:
AGTR1
Uniprot ID:
P30556
Molecular Weight:
41060.53 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Karlberg BE, Lins LE, Hermansson K: Efficacy and safety of telmisartan, a selective AT1 receptor antagonist, compared with enalapril in elderly patients with primary hypertension. TEES Study Group. J Hypertens. 1999 Feb;17(2):293-302. [PubMed:10067800 ]
  3. Balt JC, Mathy MJ, Nap A, Pfaffendorf M, van Zwieten PA: Effect of the AT1-receptor antagonists losartan, irbesartan, and telmisartan on angiotensin II-induced facilitation of sympathetic neurotransmission in the rat mesenteric artery. J Cardiovasc Pharmacol. 2001 Jul;38(1):141-8. [PubMed:11444497 ]
  4. Gohlke P, Weiss S, Jansen A, Wienen W, Stangier J, Rascher W, Culman J, Unger T: AT1 receptor antagonist telmisartan administered peripherally inhibits central responses to angiotensin II in conscious rats. J Pharmacol Exp Ther. 2001 Jul;298(1):62-70. [PubMed:11408526 ]
  5. Strohmenger HU, Lindner KH, Wienen W, Vogt J: Effects of the AT1-selective angiotensin II antagonist, telmisartan, on hemodynamics and ventricular function after cardiopulmonary resuscitation in pigs. Resuscitation. 1997 Aug;35(1):61-8. [PubMed:9259062 ]
  6. Fujimoto M, Masuzaki H, Tanaka T, Yasue S, Tomita T, Okazawa K, Fujikura J, Chusho H, Ebihara K, Hayashi T, Hosoda K, Nakao K: An angiotensin II AT1 receptor antagonist, telmisartan augments glucose uptake and GLUT4 protein expression in 3T3-L1 adipocytes. FEBS Lett. 2004 Oct 22;576(3):492-7. [PubMed:15498586 ]
  7. Sharpe M, Jarvis B, Goa KL: Telmisartan: a review of its use in hypertension. Drugs. 2001;61(10):1501-29. [PubMed:11558835 ]
  8. McClellan KJ, Markham A: Telmisartan. Drugs. 1998 Dec;56(6):1039-44; discussion 1045-6. [PubMed:9878991 ]
  9. Galzerano D, Capogrosso C, Di Michele S, Galzerano A, Paparello P, Lama D, Gaudio C: New standards in hypertension and cardiovascular risk management: focus on telmisartan. Vasc Health Risk Manag. 2010 Mar 24;6:113-33. [PubMed:20448797 ]
  10. Tagami T, Yamamoto H, Moriyama K, Sawai K, Usui T, Shimatsu A, Naruse M: A selective peroxisome proliferator-activated receptor-gamma modulator, telmisartan, binds to the receptor in a different fashion from thiazolidinediones. Endocrinology. 2009 Feb;150(2):862-70. doi: 10.1210/en.2008-0502. Epub 2009 Jan 15. [PubMed:19147680 ]
  11. Imayama I, Ichiki T, Inanaga K, Ohtsubo H, Fukuyama K, Ono H, Hashiguchi Y, Sunagawa K: Telmisartan downregulates angiotensin II type 1 receptor through activation of peroxisome proliferator-activated receptor gamma. Cardiovasc Res. 2006 Oct 1;72(1):184-90. Epub 2006 Jul 21. [PubMed:16938288 ]
  12. Kurtz TW: Beyond the classic angiotensin-receptor-blocker profile. Nat Clin Pract Cardiovasc Med. 2008 Jul;5 Suppl 1:S19-26. doi: 10.1038/ncpcardio0805. [PubMed:18580862 ]
  13. Yamagishi S, Takeuchi M: Telmisartan is a promising cardiometabolic sartan due to its unique PPAR-gamma-inducing property. Med Hypotheses. 2005;64(3):476-8. [PubMed:15617852 ]
  14. Yamagishi S, Nakamura K, Matsui T: Potential utility of telmisartan, an angiotensin II type 1 receptor blocker with peroxisome proliferator-activated receptor-gamma (PPAR-gamma)-modulating activity for the treatment of cardiometabolic disorders. Curr Mol Med. 2007 Aug;7(5):463-9. [PubMed:17691961 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
partial agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the nuclear receptor binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation...
Gene Name:
PPARG
Uniprot ID:
P37231
Molecular Weight:
57619.58 Da
References
  1. Tagami T, Yamamoto H, Moriyama K, Sawai K, Usui T, Shimatsu A, Naruse M: A selective peroxisome proliferator-activated receptor-gamma modulator, telmisartan, binds to the receptor in a different fashion from thiazolidinediones. Endocrinology. 2009 Feb;150(2):862-70. doi: 10.1210/en.2008-0502. Epub 2009 Jan 15. [PubMed:19147680 ]
  2. Imayama I, Ichiki T, Inanaga K, Ohtsubo H, Fukuyama K, Ono H, Hashiguchi Y, Sunagawa K: Telmisartan downregulates angiotensin II type 1 receptor through activation of peroxisome proliferator-activated receptor gamma. Cardiovasc Res. 2006 Oct 1;72(1):184-90. Epub 2006 Jul 21. [PubMed:16938288 ]
  3. Kurtz TW: Beyond the classic angiotensin-receptor-blocker profile. Nat Clin Pract Cardiovasc Med. 2008 Jul;5 Suppl 1:S19-26. doi: 10.1038/ncpcardio0805. [PubMed:18580862 ]
  4. Yamagishi S, Takeuchi M: Telmisartan is a promising cardiometabolic sartan due to its unique PPAR-gamma-inducing property. Med Hypotheses. 2005;64(3):476-8. [PubMed:15617852 ]
  5. Kurtz TW: Treating the metabolic syndrome: telmisartan as a peroxisome proliferator-activated receptor-gamma activator. Acta Diabetol. 2005 Apr;42 Suppl 1:S9-16. [PubMed:15868121 ]
  6. Yamagishi S, Nakamura K, Matsui T: Potential utility of telmisartan, an angiotensin II type 1 receptor blocker with peroxisome proliferator-activated receptor-gamma (PPAR-gamma)-modulating activity for the treatment of cardiometabolic disorders. Curr Mol Med. 2007 Aug;7(5):463-9. [PubMed:17691961 ]
  7. Yamagishi S, Takenaka K, Inoue H: Role of insulin-sensitizing property of telmisartan, a commercially available angiotensin II type 1 receptor blocker in preventing the development of atrial fibrillation. Med Hypotheses. 2006;66(1):118-20. Epub 2005 Sep 12. [PubMed:16154710 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Weiss J, Sauer A, Divac N, Herzog M, Schwedhelm E, Boger RH, Haefeli WE, Benndorf RA: Interaction of angiotensin receptor type 1 blockers with ATP-binding cassette transporters. Biopharm Drug Dispos. 2010 Mar;31(2-3):150-61. doi: 10.1002/bdd.699. [PubMed:20222053 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Weiss J, Sauer A, Divac N, Herzog M, Schwedhelm E, Boger RH, Haefeli WE, Benndorf RA: Interaction of angiotensin receptor type 1 blockers with ATP-binding cassette transporters. Biopharm Drug Dispos. 2010 Mar;31(2-3):150-61. doi: 10.1002/bdd.699. [PubMed:20222053 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Weiss J, Sauer A, Divac N, Herzog M, Schwedhelm E, Boger RH, Haefeli WE, Benndorf RA: Interaction of angiotensin receptor type 1 blockers with ATP-binding cassette transporters. Biopharm Drug Dispos. 2010 Mar;31(2-3):150-61. doi: 10.1002/bdd.699. [PubMed:20222053 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on May 28, 2016 02:11