Telmisartan Capsules

1. Pharmacological properties Telmisartan is an orally effective, specific angiotensin II receptor (AT1 type) antagonist. Telmisartan binds with high affinity to the AT1 subtype of angiotensin II receptor (known angiotensin II action site). Telmisartan has no partial agonist effect at the AT1 receptor site. Telmisartan selectively binds to the AT1 receptor, and the binding effect is long-lasting. Telmisartan has no affinity for other receptors (including AT2 and other AT receptors with fewer characteristics). The functions of the above other receptors are not yet known, and 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. Telmisartan does not inhibit angiotensin converting enzyme (kinase II), which can also degrade bradykinin, so there will be no adverse reactions caused by the enhanced effect of bradykinin. Administration of 80 mg of telmisartan to humans can almost completely inhibit the increase in blood pressure caused by angiotensin II, and the inhibitory effect lasts for 24 hours and can still be measured after 48 hours. The antihypertensive effect gradually becomes obvious 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. Dynamic blood pressure monitoring shows that the antihypertensive effect lasts for more than 24 hours after taking the medicine, including 4 hours before the next dose. This result was confirmed in a placebo-controlled clinical trial study: after taking 40 mg and 80 mg of telmisartan, the ratio of trough to peak was continuously above 80%. There is a significant dose-time dependence in the return to baseline SBP. The data on DBP in this regard are inconsistent. For hypertensive patients, telmisartan can reduce systolic and diastolic blood pressure without affecting the pulse. The antihypertensive effect of telmisartan is comparable to other types of representative antihypertensive drugs. (Clinical experimental studies have compared telmisartan with amlodipine, atenolol, enalapril, hydrochlorothiazide, losartan and lisinopril) If telmisartan treatment is suddenly discontinued, blood pressure will gradually return to the pre-treatment level after a few days, and rebound hypertension will not occur. In a clinical experimental study directly comparing two antihypertensive drugs, the incidence of dry cough in the telmisartan treatment group was significantly lower than that in the angiotensin converting enzyme inhibitor treatment group. The effect of telmisartan on improving mortality and cardiovascular disease morbidity is currently unknown. 2. Toxicology The doses used in preclinical safety studies are equivalent to clinical treatment doses, which can cause a decrease in red blood cell indices (erythrocytes, hemoglobin, hematocrit) and changes in renal hemodynamics (increased blood urea nitrogen and creatinine) as well as increased blood potassium in animals with normal blood pressure. Renal tubular dilatation and atrophy can be seen in dogs. Digestive tract mucosal damage (erosion, ulcer 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 supplementation. Increased plasma renin activity and hypertrophy/proliferation of 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 newborns, including weight loss, delayed eye opening, and increased mortality. No mutagenicity and related mutagenic activity were found in in vitro experiments, and no carcinogenicity was found in mouse and rat experiments.

4'-[(2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)methyl]diphenyl-2-carboxylic acid = Telmisartan

This product is a capsule, and the contents are white or off-white granules.

Used for the treatment of essential hypertension.

1. Adults: Individualized medication should be used. The usual initial dose is one tablet (40 mg) once a day. Within the dose range of 20-80 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, and the maximum dose is 80 mg (two tablets) 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, if you want to increase the drug dose, this should be considered. 2. Patients with renal insufficiency, patients with mild or moderate renal dysfunction, do not need to adjust the dose of this product. Telmisartan cannot be eliminated by hemodialysis. 3. Patients with hepatic insufficiency, patients with mild or moderate hepatic insufficiency, the daily dosage of this product should not exceed 40 mg. 4. Elderly: No dose adjustment is required for taking this product. 5. Children: The safety and efficacy data of this product have not been established for children and adolescents under 18 years of age.

Diarrhea is a possible adverse reaction after taking this product, which is similar to other angiotensin II antagonists. Angioedema, itching, rash, and urticaria have been reported in very rare cases.

1. Those who are allergic to the active ingredients and any of the excipients of this product. 2. Those in the second or third trimester of pregnancy and breastfeeding. 3. Patients with biliary obstructive diseases. 4. Patients with severe liver dysfunction. 5. Patients with severe renal dysfunction (creatinine clearance 30ml/min).

Precautions for children: For children and adolescents under 18 years old, the safety and efficacy data of this product have not been established. Precautions for pregnancy and lactation: 1. Use during pregnancy: There is not enough data to show whether this product can be used in pregnant women. Animal experiments did not show teratogenicity, but showed embryotoxicity. Therefore, for the sake of caution, do not use telmisartan in the first two months of pregnancy. Before planning pregnancy, appropriate alternative therapies should be taken. In the middle and late stages of pregnancy (during the second and third trimesters), drugs that directly act on the renin-angiotensin system can cause damage to the fetus or even death, so telmisartan is contraindicated in the middle and late stages of pregnancy. Once pregnancy is confirmed, this product should be discontinued as soon as possible. 2. Use during lactation: Since it is unknown whether this product is excreted through breast milk, this product is contraindicated during lactation. Precautions for the elderly: No dosage adjustment is required when taking this product.

1. Lithium punishment: The combination of lithium and 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 test 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 average trough blood concentration of digoxin by 20% (in some cases by 39%), so the digoxin plasma concentration must be clinically measured. 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 hypotension effect. 6. When used in combination with telmisartan, the Cmax of simvastatin metabolites (simvastatin acid) is slightly increased (1.34 times) and the elimination is accelerated.

Store at room temperature in a dry place.

40mg

24 months

Beijing SL Pharmaceutical Co., Ltd.

• Founded in:

  1994-12-24

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  4th Floor, Building 1, Bitongyuan, No. 69, Fushi Road, Haidian District, Beijing

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  91110000102299779W

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