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CAS NO.138402-11-6
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| Irbesartan Basic information |
| Product Name: | Irbesartan |
| Synonyms: | 3-butyl-2-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-2,4-diazaspiro[4.4]non-3-en-1-one;2-BUTYL-3-[[2'-(1H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1,3-DIAZASPIRO[4.4]NON-1-EN-4-ONE;IRBESARTAN;BMS-186295;AVAPRO;APROVEL;SR-47436;Lrbesartan |
| CAS: | 138402-11-6 |
| MF: | C25H28N6O |
| MW: | 428.53 |
| EINECS: | |
| Product Categories: | Active Pharmaceutical Ingredients;Antihypertensive;Hypertension;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;API's;Aromatics;Heterocycles;Isotopically Labeled Pharmaceutical Reference Standard;LITAREX |
| Mol File: | 138402-11-6.mol |
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| Irbesartan Chemical Properties |
| mp | 180-181°C |
| storage temp. | -20°C Freezer |
| CAS DataBase Reference | 138402-11-6(CAS DataBase Reference) |
| MSDS Information |
| Provider | Language |
|---|---|
| 3-Butyl-2-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-2,4-diazaspiro[4.4]non-3-en-1-one | English |
| Irbesartan Usage And Synthesis |
| Antihypertensives |
Irbesartan is an angiotensin Ⅱreceptor inhibitor, angiotensin Ⅱ receptors are divided into AT1, AT2, irbesartan can inhibit AngⅠtransform into AngⅡby selectively blocking the AT1 receptor of AngⅡ, specifically antagonize angiotensin converting enzyme 1 receptor (AT1), the antagonism of AT1 is 8500 times than that of AT2, it can inhibit vasoconstriction and aldosterone release by selectively blocking the binding AngⅡ with AT1 receptor and result in the antihypertensive effect. This product does not inhibit angiotensin converting enzyme (ACE), renin, and other hormone receptors, neither suppress the blood pressure regulation and the balance of sodium ion channels. Irbesartan can also reduce electrical remodeling of the myocardium, thereby reduce the mortality rate of patients with hypertension, it is the most effective drug for treatment of hypertension and cardiovascular disease. Angiotensin antagonists (ARB) is applied to the clinical treatment of hypertension and diabetic nephropathy. At present, domestic drugs for treating high blood pressure are divided into angiotensin converting enzyme inhibitors (ACEI), calcium channel blockers, beta blockers and so on according to different working parts. By contrast, ARB has better antihypertensive effect, while Irbesartan is a new type of angiotensin antagonist which has clear antihypertensive effect, and has an important role in inhibiting left ventricular hypertrophy and protecting the kidneys. According to foreign reports, it can quickly absorb by oral and the bioavailability is 60-80%, not affected by food. Plasma tmax is 1-1.5 hours, plasma protein combined rate is 90%, elimination half-life is 11 - 15 hours, reaching steady state in three days. By aldehyde oxidation acidification or glucose metabolism, vitro studies have shown that mainly oxidation by cytochrome enzymes of P450 and 2C9. This product and its metabolites excrete by biliary tract and kidney. Irbesartan (Emberd) produced by Sanofi-aventis hangzhou minsheng pharmaceutical co., LTD won the approval of the SFDA used in the treatment of hypertension in type 2 diabetic nephropathy on March 8, 2007, and becomes China's first effective antihypertensive drug. |
| Telmisartan |
Telmisartan is a new type of blood pressure drug, is a kind of specific angiotensin Ⅱ receptor (AT Ⅰ) antagonist, used in the treatment of essential hypertension. To instead of high affinity of angiotensin receptor Ⅱwith AT Ⅰ receptor subtypes (known angiotensin Ⅱ loci). Telmisartan has no effects in the AT Ⅰ receptor agonist sites, selectively combined with ATⅠ receptor and the combined effect is durable. Has no affinity with other receptor (including AT2 and other characteristics of less AT receptors). The other receptor function remains to be seen, excessive receptor stimulation effect due to telmisartan angiotensin Ⅱ level is also not known. Telmisartan is not inhibit human plasma renin, and also don't block the ion channel. Don't inhibit angiotensin converting enzymeⅡ, the enzyme can degrade and enhance adverse reactions caused by the excitation peptide inhibition. 80 mg of telmisartan in the human body is almost completely inhibit angiotensin Ⅱ causing increased blood pressure. Inhibition effect is last for a full of 24 hours and can still be detectable in 48 hours. Antihypertensive effect is obvious in 3 hours after the first dose. At 4 weeks after treatment began to gain maximum antihypertensive effect, and can be maintained in the long-term treatment. If the treatment was interrupted suddenly, the blood pressure returns to the treatment level in just a few days, rather than a resilient high blood pressure. In direct comparison of two kinds of high blood pressure drugs in clinical trials, treatment group was significantly lower than that of patients with dry cough angiotensin converting enzyme inhibitors in treatment group. The above information is edited by the Chemicalbook of Duan Yalan. |
| Usage and Dosage |
Oral: recommended starting dose of 0.15 g, 1 time a day. It can be increased to 0.3 g according to the condition, 1 time a day. Can be used alone, also can be shared with other anti-hypertensive drugs. Severe hypertension and not satisfied with drop in blood pressure after the drug increment, can add with small dose of diuretic (such as thiazide) or other antihypertensive drugs. |
| Drug interaction |
It has no obvious interactions with hydrochlorothiazide, digoxin, warfarin, nitrate benzene, pyridine. It should be paid attention to when shared with diuretics due to insufficient blood volume and low sodium which can cause low blood pressure (hypotension). When shared with potassium diuretics (such as ammonia, benzene with organism), should avoid potassium increasing. Do not affect each other pharmacokinetics when shared with digitalis drugs such as digoxin, beta blockers such as atenolol, calcium antagonists such as benzene, pyridine nitrate. |
| Overdose | After an overdose of this product can occur hypotension, tachycardia or bradycardia, vomiting, gastric lavage and support therapy should be adopted. |
| Adverse reactions |
Common adverse reactions: headache, dizziness, palpitation, etc., I have a cough, general degree is slight, the majority of patients continue to drugs are tolerated. Rare urticaria and angioneurotic oedema. Literature on this product is: the incidence of adverse reactions to more than 1% of indigestion, stomach burning, diarrhea, skeletal muscle pain, fatigue, and upper respiratory tract infection, but with the blank control group no significant difference. Greater than 1% but less than control group in the incidence of abdominal pain, anxiety, nervousness, nausea, vomiting, chest pain, pharyngitis, skin rashes, tachycardia, etc. Low blood pressure and incidence of orthostatic hypotension is about 0.4%. |
| Chemical property | Crystallization from 96% ethanol, melting point is 180-181 ℃. |
| Application | Antihypertensive drugs. Angiotensin Ⅱ - l (Ⅱ 1 A) receptor antagonist. Used to treat high blood pressure. |
| Production Method |
Methods 1: 1 - (fluorene methoxy carbonyl amino) ring e carboxylic acid (I) benzylamine reaction with 4 - (2 - phenyl cyano) amidation, product (Ⅲ) and water release N to produce compound (Ⅳ). (Ⅳ) and Triethyl orthobutyrate condensation, cyclization to compound (V), then azide to formation tetrazolium with sodium reaction to obtain Telmisartan. Methods 2: 1 - (fluorene methoxyl carbonyl amino) ring e carboxylic acid (I) condensation with compound(Ⅳ), the product remove N protection based to compound (Ⅷ), reacts with Triethyl orthobutyrate, obtain the product. |
| Chemical Properties | Crystalline Solid |
| Usage | An angiotensin II type 1 (AII1)-receptor antagonist |
| Usage | antidepressant |
| Usage | For the treatment of hypertension, as well as diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension. Irbesartan is also used as a second line agent in the treatment of conges |
| Irbesartan Preparation Products And Raw materials |
| Raw materials | Sodium azide-->Benzylamine-->Fluorene-->3-METHOXYPROPIONIC ACID-->Tetrazole-->ORTHO-N-VALERIC ACID TRIETHYL ESTER-->Triethyl orthobutyrate |