Telmisartan Tablets

Telmisartan is an orally effective, specific angiotensin II receptor (AT1 type) antagonist that binds to the AT1 subtype of angiotensin II receptor (known angiotensin II action site) with high affinity. The binding effect is long-lasting, but there is no partial agonist effect. The receptor overstimulation effect that may be caused by the increase in angiotensin II levels caused by telmisartan is also unknown. Telmisartan can cause a decrease in blood aldosterone levels. Telmisartan does not inhibit human plasma renin or block ion channels. Angiotensin converting enzyme (kinase II) can also degrade bradykinin. Since telmisartan does not inhibit angiotensin converting enzyme, there will be no adverse reactions caused by enhanced bradykinin action. Telmisartan has no affinity for other receptors (including AT2 and other less characterized AT receptors whose functions are still unclear). In humans, administration of 80 mg of telmisartan can almost completely inhibit the increase in blood pressure caused by angiotensin II. The inhibitory effect lasts for 24 hours and can still be measured at 48 hours. The antihypertensive effect gradually becomes apparent within 3 hours after the first dose of telmisartan. The maximum antihypertensive effect can be obtained 4 weeks after the start of treatment and can be maintained in long-term treatment. Ambulatory blood pressure monitoring shows that the antihypertensive effect lasts for more than 24 hours after taking the medicine, including the 4 hours before the next dose. This result was confirmed in a placebo-controlled clinical trial study: after taking 40mg and 80mg of telmisartan, the ratio of trough to peak was continuously above 80%. There is a significant dose-time dependence in returning to baseline SBP. The data on DBP in this regard are inconsistent. For patients with hypertension, telmisartan can reduce systolic and diastolic blood pressure without affecting heart rate. The antihypertensive effect of telmisartan is comparable to other types of representative antihypertensive drugs. (Clinical trials have compared telmisartan with amlodipine, atenolol, enalapril, hydrochlorothiazide, losartan, and lisinopril.) If telmisartan treatment is suddenly discontinued, blood pressure gradually returns to pre-treatment levels after a few days, and rebound hypertension does not occur. In clinical trials directly comparing two antihypertensive drugs, the incidence of dry cough in patients treated with telmisartan was significantly lower than that in patients treated with angiotensin-converting enzyme inhibitors. The effect of telmisartan on improving mortality and cardiovascular disease morbidity is currently unknown. Toxicology The doses used in preclinical safety studies, which are equivalent to clinical treatment doses, can cause a decrease in red blood cell indices (erythrocytes, hemoglobin, hematocrit) and changes in renal hemodynamics (increased blood urea nitrogen and creatinine) and an increase in serum potassium in normotensive animals. Renal tubular dilatation and atrophy can be seen in dogs. Digestive mucosal damage (erosion, ulceration, or inflammation) can also be seen in rats and dogs. These pharmacological adverse reactions are known from preclinical studies to be common reactions of angiotensin-converting enzyme inhibitors and angiotensin II antagonists, and can be prevented by oral salt supplements. Increased plasma renin activity and hypertrophy/hyperplasia of glomerular juxtaglomerular cells can be seen in both species. The above changes are also common reactions of angiotensin-converting enzyme inhibitors and other angiotensin II antagonists and are not clinically specific. Animal experiments have shown that telmisartan has some potential adverse effects on the postnatal development of the fetus, including weight loss, delayed eye opening, and increased mortality. No mutagenicity and related mutagenic activity were found in in vitro experiments. No carcinogenicity was found in mouse and rat experiments.

Telmisartan (pregnancy classification: C; D-if used in the second or third trimester of pregnancy)

This product is white or off-white tablets.

Used for the treatment of essential hypertension.

1 Adults should be given individualized medication. The usual initial dose is one tablet (40 mg) each time, once a day. Within the dose range of 20 to 80 mg, the antihypertensive effect of telmisartan is related to the dose. If the ideal blood pressure is not achieved after medication, the dose can be increased, with the maximum dose being 80 mg once a day. This product can be used in combination with thiazide diuretics such as hydrochlorothiazide, which have a synergistic antihypertensive effect with this product. Because telmisartan can only exert its maximum efficacy four to eight weeks after the start of the treatment, this should be considered if the drug dose is to be increased. 2 Patients with renal insufficiency Patients with mild or moderate renal insufficiency do not need to adjust the dose of this product. Telmisartan is not eliminated through blood filtration. 3 Patients with hepatic insufficiency Patients with mild or moderate hepatic insufficiency should not take more than 40 mg per day. 4 Elderly people do not need to adjust the dose of this product. 5 Children and adolescents For children and adolescents under 18 years old, the safety and efficacy data of this product have not yet been established.

In placebo-controlled trials, the overall incidence of adverse events was similar for telmisartan (41.4%) and placebo (43.9%). The incidence of adverse events was not dose-related and was not related to the patient's gender, age, or race.

Patients who are allergic to the active ingredients and any of the excipients of this product; those in the second or third trimester of pregnancy or breastfeeding; patients with biliary obstructive diseases; patients with severe liver dysfunction; patients with severe renal impairment (creatinine clearance 30 ml/min).

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 women in the middle and late stages of pregnancy and breastfeeding; Precautions for the elderly: No dosage adjustment is required when taking this product.

1 Lithium Lithium combined with angiotensin converting enzyme inhibitors can cause reversible increases in blood lithium levels and toxic reactions. There are also individual cases caused by the combination of lithium and angiotensin II receptor antagonists. Therefore, lithium and this product should be used with caution. If combined use is necessary, blood lithium levels should be monitored during the combined use. 2 Some drugs can affect blood potassium levels or cause hyperkalemia (such as ACE inhibitors, potassium-sparing diuretics, potassium ion supplements, potassium-containing salt substitutes, cyclosporine A or other drugs such as heparin sodium); if this product needs to be used in combination with these drugs, it is recommended to monitor blood potassium levels. Based on the experience of using other drugs that affect the renin-angiotensin system, this product combined with the above drugs can cause an increase in blood potassium levels (see Precautions). 3 Pharmacokinetic studies have studied the interaction of this product with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, amlodipine and other drugs. It can increase the mean trough blood concentration of digoxin by 20% (in some cases by 39%), so digoxin plasma concentration must be monitored. 4 This product can enhance the antihypertensive effect of other antihypertensive drugs. Other clinically significant interactions have not yet been confirmed. 5 Based on their pharmacological properties, the following drugs can enhance the antihypertensive effect of antihypertensive drugs including telmisartan: baclofen, amifostine. In addition, alcohol, barbiturates, sedatives, hypnotics or antidepressants can enhance the orthostatic hypotensive effect. 6 When used in combination with telmisartan, the Cmax of simvastatin metabolites (simvastatin acid) is slightly increased (1.34 times) and its elimination is accelerated.

Seal and store in a cool place.

40mg

48 months.

Tianjin Kangrui Pharmaceutical Co., Ltd.

• Founded in:

  1996-10-10

• Address:

  No. 18, West 7th Road, Tianjin Pilot Free Trade Zone (Airport Economic Zone)

• Tax NO.:

  911201162396623808

• Registered Funds:

  49 million yuan

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