Telmisartan raw material Telmisartan Powder 144701-48-4

CAS:144701-48-4

MF:C33H30N4O2

MW:514.62

EINECS:620-494-7

Specification: 99% min Telmisartan Powder

Sample:Telmisartan Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Telmisartan Powder Usage and Synthesis.

Telmisartan is a new blood pressure-lowering drug, a specific angiotensin II receptor (AT I type) antagonist, used in the treatment of essential hypertension.

The alternative angiotensin II receptor binds with high affinity to the ATⅠreceptor subtype (a known site of angiotensin II action).

Telmisartan has no site agonist effect at the ATⅠreceptor site and selectively binds to the ATⅠreceptor, a binding effect that is long-lasting.

There is no affinity for other receptors, including AT2 and other less well characterised AT receptors.

The function of the other receptors mentioned above is not known, nor are the possible receptor overstimulation effects due to the increase in angiotensin II levels caused by telmisartan.

Telmisartan does not inhibit plasma renin or block ion channels in humans.

It does not inhibit angiotensin-converting enzyme II, which may also degrade bradykinin resulting in adverse effects due to increased bradykinin action.

Uses and functions of Telmisartan.

Timosartan Tablets: for the treatment of hypertension.

Timosartan Capsules: for essential hypertension.

Timosartan Dispersible Tablets:

Used for hypertension, for the treatment of essential hypertension in adults, to reduce cardiovascular risk, age 55 years and older, in patients with a high risk of serious cardiovascular events who cannot be treated with angiotensin-converting (ACE) inhibitors to reduce the risk of myocardial infarction, stroke, or death due to cardiovascular disease.

High risk of cardiovascular events includes coronary artery disease, peripheral arterial disease, ischaemic attack or a history of high-risk type 2 diabetes mellitus or non-insulin-dependent disease with evidence of end-organ damage.

Telmisartan may also be used concomitantly with other necessary therapy (e.g., antihypertensive agents, antiplatelet agents, or lipid-lowering agents); concomitant use of telmisartan with ACE inhibitors is not recommended.

Pharmacological Effect of Telmisartan.

1. Telmisartan is an orally active, specific angiotensin I receptor (AT1-type) antagonist that binds with high affinity to the AT, subtype of the angiotensin I receptor (the known site of action of angiotensin I), which is persistent without any partial agonist effect.

The possible receptor overstimulation effect due to the increase in angiotensin II levels caused by telmisartan is also unknown.

2. Timosartan may cause a decrease in blood aldosterone levels. Timosartan does not inhibit plasma renin or block ion channels in humans.

Angiotensin-converting enzyme (kinase) can also degrade bradykinin, because temesartan does not inhibit angiotensin-converting enzyme, so there will be no bradykinin effect caused by the enhancement of adverse reactions.

Telmisartan has no affinity for other receptors (including AT1 and other less well characterised AT receptors, the function of which is unknown).

3, In humans, administration of 80 mg of temesartan almost completely inhibits angiotensin I-induced increases in blood pressure; the inhibitory effect lasts for 24 hours and remains measurable at 48 hours. The antihypertensive effect becomes progressively more pronounced within 3 hours after the first dose of timosartan.

Maximum antihypertensive effect is obtained 4 weeks after the start of treatment and can be maintained during long-term therapy. Ambulatory blood pressure monitoring showed that the antihypertensive effect persisted for more than 24 hours after dosing, including 4 hours before the next dose.

This result was confirmed in placebo-controlled clinical pilot studies The trough-to-peak ratio was consistently above 80% after taking temesartan 40 mg and 80 mg.

There was a clear dose-time dependence of return to baseline SBP. Data on DBP in this area are inconsistent.

4, In patients with hypertension, telmisartan reduces systolic and diastolic blood pressure without affecting heart rate. The antihypertensive effect of telmisartan is comparable to other types of antihypertensive representative drugs.

(Clinical trial studies were conducted comparing temesartan with amlodipine, atenolol, enalapril, dihydrochlorothiazide, cloxartan and lenopril.) Timosartan therapy. If abruptly interrupted, blood pressure gradually returns to pre-treatment levels after several days without rebound hypertension.

5, In a clinical trial study directly comparing two antihypertensive drugs, the incidence of dry cough was significantly lower in the temesartan-treated group than in the blood, tubulin-converting enzyme inhibitor-treated group.

The role of telmisartan in improving mortality and the prevalence of cardiovascular disease is not yet known.

Contraindication of Bulk Telmisartan Powder.

1, allergic to the active ingredient of this product and any kind of excipient components.

2、Expectant eyes and breastfeeding.

3、Biliary tract obstructive disease loyalists.

4、Patients with severe hepatic insufficiency.

5、Patients with severe renal dysfunction (creatinine clearance <30ml/min).