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Telmisartan

Chemical Properties Mechanisms of Action Side Effects Patent

CAS No. 144701-48-4
Chemical Name: Telmisartan
Synonyms: TU-199;PRITOR;BIBR 277;MICARDIS;Telmisaran;TIMISHATAN;BIBR 277SE;TELMISARTAN;TIMETAZIDINE;TelMisartan API
CBNumber: CB4266172
Molecular Formula: C33H30N4O2
Formula Weight: 514.63
MOL File: 144701-48-4.mol
Telmisartan Property
Melting point : 261-263°C
density : 1.16
RTECS : DV2037500
storage temp. : Hygroscopic, -20°C Freezer, Under Inert Atmosphere
solubility : DMSO: >5 mg/mL at 60 °C
form : solid
color : white
Water Solubility : insoluble
CAS DataBase Reference: 144701-48-4(CAS DataBase Reference)
Safety
Hazard Codes : Xi
Risk Statements : 36/37/38
Safety Statements : 22-24/25-36-26
WGK Germany : 2
Hazardous Substances Data: 144701-48-4(Hazardous Substances Data)

Telmisartan Chemical Properties,Usage,Production

Chemical Properties
White or off-white crystalline powder, odorless and tasteless. Soluble in chloroform, slightly soluble in methanol, very slightly soluble in acetone, practically insoluble in water. Slightly soluble in 0.1mol/L hydrochloric acid, soluble in 0.1mol/L sodium hydroxide.
Absorption coefficient(E1%1cm):509~541
Mechanisms of Action
80mg of telmisartan for the human body will practically completely counter the high blood pressure caused by angiotension II. Effects will last for 24 and can still be detected within 48 hours. Blood pressure-lowering effects should gradually become apparent within 3 hours after the initial dose. If treatment is suddenly interrupted, blood pressure will return to the same level as before treatment in a matter of days, and there will be no rebound high blood pressure. In a clinical trial that compared two kinds of antihypertensive drugs, patients in the treatment group experienced lower rates of coughing than those in the group treated by angiotensin converting enzyme inhibitors.
Telmisartan has a half-life of 18~24 hours, and will take effect 1~4 hours after taken. Medicinal effects can last for as long as 35 hours, with a high (T/P) ratio and outstanding effects in controlling morning blood pressure. Thus, this medicine can effectively control blood pressure for 24 hours, and it meets the once-daily medicinal standard (40~80mg, qd).
Clinical effects and characteristics:
  • Pharmacokinetics show: Rapid effects (0.3h), long duration (35.4h), little effect on heart rate when lowering blood pressure.
  • Compared to Enalapril: Stronger antihypertensive effects than Enalapril; when both are used in combination with diuretics, Telmisartan still appears to be superior and results in a lower coughing rate.
  • Compared to Lisinopril: More apparent antihypertensive effects (for both systolic and diastolic blood pressure), coughing rate for Telmisartan (16%) is drastically lower than that of Lisinopril (60%).
  • Compared to Atenolol: Similar antihypertensive effects, lower rate of side effects (impotence and fatigue).
  • Compared to Amlodipine: The Telmisartan group experienced noticeably lower heart rates four hours after ingestion and from six a.m. to twelve p.m.
Overall, Telmisartan has the following characteristics in comparison with other antihypertensive medicine: specific receptor effects, noticeable hypertensive effects, good diuretic effects, improvement of myocardial stenosis, safe usage, good tolerance, and convenient daily dosage.
Side Effects
In the placebo control experiment, the incidence rate of negative events for the Telmisartan group (41.4%) was similar to that of the placebo group (43.9%). Negative events were unrelated to dosage, sex, age, or race.
The following lists negative reactions were accumulated via the 5788 hypertensive patients that were treated with Telmisartan in the clinical trial.
Negative effects are categorized by incident rate as:
Very common (>1/10); common (>1/100, <1/10=); uncommon (>1/1000, <1/100=); rare (>1/10000, <1/1000=); very rare (<1/100000=)
Bodily reaction: Common: Back pain (e.g. sciatica), chest pain, flu-like symptoms, infection symptoms (e.g. urinary tract infection including cystitis). Uncommon: sight abnormality, sweating.
Central and peripheral nervous system: Common: vertigo.
Digestive system: Common: stomach pain, diarrhea, indigestion, gastrointestinal disorders. Rare: dry mouth, bloating.
Muscle skeletal system: Common: joint pain, leg cramps or leg pain, muscle pain. Rare: Tenosensitis symptoms.
Nervous system: Rare: anxiety.
Respiratory system: Common: upper respiratory tract infection, including pharyngitis and rhinitis.
Skin and accessory system: Common: Skin abnormalities such as eczema.
Additionally, since Telmisartan entered the market, there have been individual cases of erythema, itching, syncope, insomnia, depression, stomach discomfort, vomiting, hypotension, bradycardia, tachycardia, dyspnea, eosinophilia, thrombocytopenia, weakness, and reduced work efficiency. Similar to other angiotensin II receptor blockers, very few cases have reported vascular edema, nettles, and other negative reactions.
The laboratory found: compared to the placebo, the Telmisartan group occasionally exhibited lowered hemoglobin or raised uric acid. Any increase in serum creatinine or liver enzymes in the Telmisartan group was similar or lower than that of the placebo group.
Patent
Telmisartan was originally formulated by the German pharmaceutical company Boehringer Ingelheim; it earned the German patent EP502,314 in 1991, was first approved to enter the American market in November 1998, and then entered German, Philippines, Australian, Belgium, British, and other markets.
Chemical Properties
White or off white crystalline powder
Uses
cardiotonic
Uses
Telmisartan is an angiotensin II receptor antagonist.
Uses
anti-cancer agent
Uses
Used 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
Definition
ChEBI: A member of the class of benzimidazoles used widely in the treatment of hypertension.
Telmisartan Preparation Products And Raw materials
Raw materials
N-Methyl-1,2-benzenediamine dihydrochloride
Preparation Products
Telmisartan Suppliers      Global( 394)Suppliers     
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd. +86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Shenzhen Sendi Biotechnology Co.Ltd. 0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3230 55
Hubei Xinyuanshun Pharmaceutical Chemical Co., Ltd. 027-50664929 / 13971561712
027-50664927 / QQ: 3452835437 hubxys2001@163.com China 2014 55
Zhuhai Beri Medical Technology Co., Ltd +86(0756)8699 456
+86(0756)8699 456 sales@zhberi.com China 141 58
Guangzhou Kafen Biotech Co.,Ltd 020-31121484 18027468163 QQ:2355327168
020-31121510 gy@yccreate.com China 4346 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
+86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96831 76
Meryer (Shanghai) Chemical Technology Co., Ltd. +86-(0)21-61259100(Shanghai) +86-(0)755-86170099(ShenZhen) +86-(0)10-62670440(Beijing)
+86-(0)21-61259102(Shanghai) +86-(0)755-86170066(ShenZhen) +86-(0)10-88580358(Beijing) sh@meryer.com China 40403 62
INTATRADE GmbH +49 3493/605464
+49 3493/605470 sales@intatrade.de Germany 3589 66
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15950 69
Arden pharmaceutical &chemical Co., Ltd +86-(0)533-3595900 13793319233
+86-(0)533-3595900 info@chems.com.cn China 670 61
 
144701-48-4(Telmisartan)Related Search:
Valsartan Telmisartan-d3 Acyl--D-glucuronide 4-Methyl Biphenyl-2-Carboxylate [Telmisartan Intermediates] Telmisartan acyl glucuronide 4-butanamide-3-methyl-5-nitrobenzene carboxylate acid cas:(intermediate of telmisartan) 3-methyl-4-n-butyramide-5-amino-benzoic acid methyl ester (intermediate of telmisartan) Telmisartan Methyl Ester TERT-BUTHYL 4'-(METHYL)BIPHENYL-2-CARBOXYLATE(FOR TELMISARTAN) N-METHYL-O-PHENLENEDIAMINE DIHYDROCHLORIDE/INTERMEDIATE OF TELMISARTAN METHYL4/-(BROMOMETHYL)-BIPHENYL2-CARBOXLATE/INTERMEDIATE OF TELMISARTAN Intermediate of Telmisartan A 2-N-PROPYL-4-METHYL-6-(1-METHYLBENZIMIDAZOLE-2-YL)BENZIMIDAZOLE(INTERMEDIATE OF TELMISARTAN) 2-N-PROPY1-4-METHYL-6-(1-METHYL BENZIMIDAZOLE-2-YL) BENZIMIDAZOLE/INTERMEDIATE OF TELMISARTAN TELMISARTAN-D3 ACYL-B-D-GLUCURONIDE TELMISARTAN SODIUM 4'-[[1,4'-Dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl]-methyl]-1,1'-biphenyl-2-carboxylic acid 1,1-dimethylethyl ester METHYL 4'-[[2-N-PROPYL-4-METHYL-6-(1-METHYLBENZIMIDAZOL-2-YL)-BENZIMIDAZOL-1-YL]METHYL]BIPHENYL-2-CARBOXYLATE Telmisartan Acyl--D-glucuronide
TU-199 TELMISARTAN PRITOR MICARDIS BIBR 277 144701-48-4 4'[(1,4'-DIMETHYL-2'-PROPYL[2,6'-BI-1H-BENZIMIDAZOL]-1'-YL)METHYL][1,1'-BIPHENYL]-2-CARBOXYLIC ACID 4'-[(1,4'-DIMETHYL-2'-PROPYL[2,6'-BI-H-BENZIMIDAZOL]-1'-YL)METHYL][1,1'-BIPHENYL]-2-CARBOXYLIC ACID 3-methoxy-8-[(4-methoxy-3,5-dimethyl-pyridin-2-yl)methyl sulfinyl]-2,7,9-triazabicyclo[4.3.0]nona-2,4,8,10-tetraene [1,1'-Biphenyl]-2-carboxylic acid, 4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]- 4'-[[1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl]-methyl]-1,1'-biphenyl-2carboxylic acid,dimethylethyl ester Telmisaran Telmisartan99.5% TelmisartanC33H30N402 C16H18N4O3S C33H30N4O2 Micardis, Pritor, 4[(1,4Dimethyl-2propyl[2,6bi-H-benzimidazol]-1yl)methyl][1,1biphenyl]-2-carboxylic Acid, TIMETAZIDINE TIMISHATAN 4′-((2-n-Propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)methyl)biphenyl-2-carbonsure 1447014-48-4 Pharmaceutical material and intermeidates Active Pharmaceutical Ingredients C37H38N4O2 4'-[{1,4'-Dimethyl-2'-Propyl[2,6'-Bi-1H-Benzimiaszol]-1'yl}-Methyl}-1,1'-Biphenyl-2-Caroxylic Acid INTERMEDIATESOF Antihypertensive 4'-[{1,4'-Dimethyl-2'-Propyl[2,6'-Bi-1H-Benzimiaszol]-1'yl}-Methyl}-1,1'-Biphenyl-2-Caroxylic Acid Dimethyl Ethyl Ester Imidazoles (intermediates of telmisartan) 4''-(1,7''-DIMETHYL-2''-PROPYL-1H-[2,5'']BIBENZOIMIDAZOLYL-3''-YLMETHYL)-BIPHENYL-2-CARBOXYLIC ACID 4-chloromethyl-5-methyl-1,3-dioxol-2-tone Telmisartan 4'-(1,7'-Dimethyl-2'-propyl-1H- Hypertension Intermediates & Fine Chemicals Pharmaceuticals API's BIBR 277, 4μ[(1,4μ-Dimethyl-2μ-propyl[2,6μ-bi-1H-benzimidazol]-1μ-yl)methyl][1,1μ-biphenyl]-2-carboxylic acid C20H24N2O5SD4 C33H27N4O2D3 4'-[[4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl]methyl]-2-biphenylcarboxylic acid Telmisartan,4′[(1,4′-Dimethyl-2′-propyl[2,6′-bi-1H-benzimidazol]-1′-yl)methyl][1,1′-biphenyl]-2-carboxylic acid, BIBR 277 4'-[[1,4'-Dimethyl-2 Other Products Telmisartan (150 mg) 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 TelMisartan (Micardis) BIBR 277SE TelMisartan API Hypertension. 4'-[[4-Methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-propyl-1H-benzimidazol-1-yl]methyl]biphenyl-2-carboxylic Acid 4'-((1,7'-DiMethyl-2'-propyl-1H,3'H-[2,5'-bibenzo[d]iMidazol]-3'-yl)Methyl)-[1,1'-biphenyl]-2-carboxylic acid 4'-((1,7'-Dimethyl-2'-propyl-1H,3'H-[2,5'-bibenzo[d]imidazol]-3'-yl)methyl)-[1,1'-biphenyl]-2-car CARADRIN Telmisartan Synonyms 4'[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid (1,1'-Biphenyl)-2-carboxylic acid, 4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-b 2-[4-[[4-methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl]methyl]phenyl]benzoic acid
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