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Telmisartan Tablets

Function and Efficacy

Pharmacological action: Telmisartan is an oral specific non-peptide angiotensin II receptor (AT1 type) antagonist. Telmisartan selectively binds to the AT1 receptor site with high affinity, persistently antagonizes angiotensin II, and causes a decrease in blood aldosterone levels, thereby reducing blood pressure. Telmisartan does not inhibit human plasma renin, nor does it block ion channels, nor does it inhibit angiotensin converting enzyme (kinase II), nor does it affect the degradation of bradykinin by the enzyme, so there will be no adverse reactions caused by the enhanced effect of bradykinin. For patients with hypertension, telmisartan can reduce systolic and diastolic blood pressure without affecting heart rate. No rebound hypertension occurs after telmisartan is discontinued. The antihypertensive effect gradually becomes apparent within 3 hours after the first dose of telmisartan. Ambulatory blood pressure monitoring shows that the antihypertensive effect of telmisartan lasts for more than 24 hours after taking the drug. The trough/peak ratio of blood pressure reduction after taking 40mg or 80mg of telmisartan is always above 60%. The maximum antihypertensive effect can be obtained 4 weeks after the start of treatment and can be maintained in long-term treatment. Non-clinical toxicology studies: The use of telmisartan in a dose range equivalent to clinical treatment can cause a decrease in red blood cell indices (erythrocytes, hemoglobin, hematocrit) and an increase in blood urea nitrogen and creatinine, as well as an increase in blood potassium in animals with normal blood pressure. Renal tubular dilatation and atrophy can be seen in dogs. Gastric mucosal damage (erosion, ulcer, inflammation) can be seen in rats and dogs. Increased plasma renin activity and hypertrophy/hyperplasia of renal juxtaglomerular cells can be seen. These reactions, which are common to angiotensin-converting enzyme inhibitors and other angiotensin II antagonists, can be prevented by oral salt supplements. Animal experiments suggest that telmisartan has potential adverse effects on the postnatal development of offspring, including lower body weight, delayed eye opening, and higher mortality. In vitro experiments did not find mutagenicity and related mutagenic activity, and no carcinogenicity was found in rats and mice.

Ingredients

The main ingredient of this product is telmisartan, and its chemical name is: 4-[2-propyl-methyl-6-[methylbenzimidazole-2-yl]benzimidazole-1-methyl]biphenyl-2-carboxylic acid; molecular formula: C33H30N4O2 molecular weight: 514.63

Name Description Content CAS NO. Manufacturer
TelmisartanIngredients

Telmisartan is an oral specific non-peptide angiotensin II receptor (AT1 type) antagonist. Telmisartan selectively binds to the AT1 receptor site with high affinity, persistently antagonizes angiotensin II, and causes a decrease in blood aldosterone levels, thereby reducing blood pressure. Telmisartan does not inhibit human plasma renin, nor does it block ion channels, nor does it inhibit angiotensin converting enzyme (kinase II), nor does it affect the degradation of bradykinin by the enzyme, so there will be no adverse reactions caused by the enhanced effect of bradykinin. For patients with hypertension, telmisartan can reduce systolic and diastolic blood pressure without affecting heart rate. Rebound hypertension does not occur after discontinuation of telmisartan.

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144701-48-4 109

Appearance

This product is white or off-white tablets.

Indication

Used to treat essential hypertension.

Usage and Dosage

The recommended adult dose is 40 mg (1 tablet), once a day, orally. According to the antihypertensive effect, adjust the dose between 20 mg and 80 mg as prescribed by the doctor. The maximum dose is 80 mg (2 tablets), once a day. This product can be used in combination with thiazide diuretics such as hydrochlorothiazide, which has a synergistic antihypertensive effect. If you want to increase the drug dose, you must consider the time when telmisartan exerts its maximum antihypertensive effect, which is usually four to eight weeks after the start of treatment. Patients with renal insufficiency Patients with mild or moderate renal insufficiency do not need to adjust the dose of this product. Patients with hepatic insufficiency Patients with mild or moderate hepatic insufficiency should not use more than 40 mg per day. Elderly people do not need to adjust the dose of this product. Children The safety and efficacy data of this product for children have not yet been established.

Adverse Reactions

Adverse reactions that may occur after taking this product include dizziness, headache, back pain, nausea, loss of appetite, diarrhea, upper respiratory tract infection, etc. Most of them can be relieved within 72 hours or one week after taking the medicine. Angioedema, itching, rash, and urticaria have been reported in very few cases.

Precautions

People who are allergic to this product; pregnant women and breastfeeding women; patients with biliary obstructive diseases; patients with severe liver dysfunction; patients with severe renal dysfunction.

Special Population Medication

Precautions for children: The safety and efficacy data of this product have not been established for children and adolescents under the age of 18. Precautions for pregnancy and lactation: Pregnant and lactating women are prohibited. Precautions for the elderly: No dosage adjustment is required when taking this product.

Drug Interactions

This product can enhance the antihypertensive effect of other antihypertensive drugs. This product can increase the median blood trough concentration of digoxin by 20% (up to 39% in some cases), so the digoxin plasma concentration must be monitored. Continuous use of telmisartan can slightly reduce the mean plasma trough concentration of warfarin, but will not cause changes in the international standard ratio. There have been reports of reversible increases in blood lithium levels and toxic reactions caused by the combination of lithium agents and this product. The blood lithium level should be carefully monitored when the two are used in combination. The sympathomimetic activity of ephedrine and pseudoephedrine can weaken the activity of this drug.

Storage

Seal tightly and store in a cool, dark place.

Packaging Specification

40 mg

Validity Period

48 months.

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