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/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 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 experiments on mice and rats.

The main ingredient of this product is telmisartan, and its chemical name is: 4-[(1,4-dimethyl-2-propyl[2,6-di-1H-benzimidazole]-1-yl)-methyl]-[1,1-diphenyl]-2-carboxylic acid.

This product is white or off-white tablets.

Treat essential hypertension.

Adults: Dosing should be individualized. The usual initial dose is one tablet (40 mg) once a day. Within the dose range of 20 to 80 mg, the antihypertensive effect of telmisartan is dose-related. If the ideal blood pressure is not achieved after medication, the dose can be increased, and the maximum dose is 80 mg (i.e. two tablets of 40 mg or one tablet of 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. 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. Patients with hepatic insufficiency: Patients with mild or moderate hepatic insufficiency should not use more than 40 mg per day. Elderly: No dose adjustment is required for this product. Children and adolescents: The safety and efficacy data of this product have not been established for children and adolescents under 18 years of age.

Placebo-controlled clinical trials showed that the total incidence of adverse events for telmisartan was 41.4% and for placebo was 43.9%. These adverse reactions were dose-independent and unrelated to the patient's gender, age and race. The adverse reactions listed below are cumulatively obtained from 5788 hypertensive patients treated with telmisartan in clinical trials. The incidence of adverse reactions is graded as follows: very common (ge; 1/10); common (ge; 1/100, 1/10); uncommon (ge; 1/1000, 1/100); rare (ge; 1/10000, 111000); very rare (1/10000) Within each frequency group, adverse reactions are listed in descending order of severity. Infections: Common: symptoms of infection (e.g. urinary tract infections, including cystitis), upper respiratory tract infections including pharyngitis and sinusitis Psychiatric system: Uncommon: anxiety Eyes: Uncommon: abnormal vision Ears and vestibular function: Uncommon: vertigo Gastrointestinal tract: Common: abdominal pain, diarrhea, indigestion Uncommon: dry mouth, flatulence Rare: stomach discomfort Skin and subcutaneous tissue: Common: eczematous skin lesions Uncommon: hyperhidrosis Musculoskeletal system: Common: arthritis, back pain (e.g., sciatica), leg cramps or leg pain, myalgia Uncommon: tendonitis Systemic reactions and application site: Common: chest pain, flu-like symptoms. In addition, since telmisartan has been marketed, there have been very few reports of cases of erythema, itching, syncope, insomnia, depression, stomach discomfort, vomiting, hypotension (including postural hypotension), bradycardia, tachycardia, abnormal liver function, liver disease, impaired renal function including acute renal failure (see [Precautions]), hyperkalemia, dyspnea, anemia, eosinophilia, thrombocytopenia, asthenia and lack of efficacy. The frequency of these events is unknown. As events independent of other angiotensin II receptor antagonists, angioedema, urticaria and other related cases have been reported. Laboratory examination findings: Occasionally, a decrease in hemoglobin or an increase in uric acid in the blood was observed, which occurred more frequently during treatment with telmisartan than with placebo. An increase in creatinine or an increase in liver enzymes was observed during treatment with telmisartan, but the probability of these changes in laboratory results was similar to or slightly lower than that of placebo. In addition, since telmisartan was marketed, there have been reports of an increase in blood creatine phosphokinase (CPK). Placebo-controlled clinical trials showed that the total incidence of adverse events for telmisartan was 41.4% and for placebo was 43.9%. These adverse reactions were dose-independent and unrelated to the patient's gender, age and race. The adverse reactions listed below are cumulatively obtained from 5788 hypertensive patients treated with telmisartan in clinical trials. The incidence of adverse reactions is graded as follows: very common (ge; 1/10); common (ge; 1/100, 1/10); uncommon (ge; 1/1000, 1/100); rare (ge; 1/10000, 111000); very rare (1/10000) Within each frequency group, adverse reactions are listed in descending order of severity. Infections: Common: symptoms of infection (e.g. urinary tract infections, including cystitis), upper respiratory tract infections including pharyngitis and sinusitis Psychiatric system: Uncommon: anxiety Eyes: Uncommon: abnormal vision Ears and vestibular function: Uncommon: vertigo Gastrointestinal tract: Common: abdominal pain, diarrhea, indigestion Uncommon: dry mouth, flatulence Rare: stomach discomfort Skin and subcutaneous tissue: Common: eczematous skin lesions Uncommon: hyperhidrosis Musculoskeletal system: Common: arthritis, back pain (e.g., sciatica), leg cramps or leg pain, myalgia Uncommon: tendonitis Systemic reactions and application site: Common: chest pain, flu-like symptoms. In addition, since telmisartan has been marketed, there have been very few reports of cases of erythema, itching, syncope, insomnia, depression, stomach discomfort, vomiting, hypotension (including postural hypotension), bradycardia, tachycardia, abnormal liver function, liver disease, impaired renal function including acute renal failure (see [Precautions]), hyperkalemia, dyspnea, anemia, eosinophilia, thrombocytopenia, asthenia and lack of efficacy. The frequency of these events is unknown. As events independent of other angiotensin II receptor antagonists, angioedema, urticaria and other related cases have been reported. Laboratory examination findings: Occasionally, a decrease in hemoglobin or an increase in uric acid in the blood was observed, which occurred more frequently during treatment with telmisartan than with placebo. An increase in creatinine or an increase in liver enzymes was observed during treatment with telmisartan, but the probability of these changes in laboratory results was similar to or slightly lower than that of placebo. In addition, since telmisartan was launched on the market, there have been reports of increased blood creatine phosphokinase (CPK).

1. It is contraindicated for those who are allergic to any active ingredient or any excipient of this product. 2. It is contraindicated for women in the second and third trimesters of pregnancy and breastfeeding. 3. It is contraindicated for patients with biliary obstructive diseases. 4. It is contraindicated for patients with severe liver damage.

Precautions for children: The safety and efficacy data of this product have not been established for children and adolescents under 18 years old. Precautions for pregnancy and lactation: It is forbidden for women in the second and third trimesters of pregnancy and lactation. Precautions for the elderly: No dosage adjustment is required when taking this product.

Interaction studies have been conducted only in adults. Drugs or therapeutic classes that may cause hyperkalemia: salt substitutes containing potassium, potassium-sparing diuretics, angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, nonsteroidal anti-inflammatory drugs (including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporine or tacrolimus), trimethoprim. The occurrence of hyperkalemia depends on the relevant risk factors. In the case of the above-mentioned treatment combinations, the risk is increased. The risk is particularly high when angiotensin-converting enzyme inhibitors or nonsteroidal anti-inflammatory drugs are used in combination with potassium-sparing diuretics and salt substitutes containing potassium, but the risk is lower when used in combination with angiotensin-converting enzyme inhibitors when precautions are strictly observed. Concomitant use is not recommended: 1. Potassium-sparing diuretics or potassium supplements: Angiotensin II receptor antagonists reduce potassium losses caused by diuresis. Potassium-sparing diuretics such as spironolactone, eplerenone, triamterene or amiloride, potassium supplements or salt substitutes containing potassium may cause a significant increase in serum potassium. If concomitant use is due to well-documented hypokalemia, it should be used with caution and serum potassium levels should be monitored frequently. 2. Lithium: When lithium and angiotensin-converting enzyme inhibitors are taken simultaneously, there have been reports of reversible increases in serum lithium concentrations and toxicity, but this situation rarely occurs during co-administration with angiotensin receptor antagonists. If co-administration is necessary, careful monitoring of blood lithium levels is recommended. Concomitant medications that require caution: 1. Nonsteroidal anti-inflammatory drugs: Nonsteroidal anti-inflammatory drugs (acetylsalicylic acid, COX-2 inhibitors, and non-selective nonsteroidal anti-inflammatory drugs given at anti-inflammatory doses) may reduce the antihypertensive effect of angiotensin II receptor antagonists. In some patients with renal impairment (such as dehydrated patients or elderly patients with renal impairment), the combined use of angiotensin II receptor antagonists and drugs that inhibit cyclooxygenase may lead to further deterioration of renal function, including possible acute renal failure, which is usually reversible. Therefore, co-administration should be cautious, especially in the elderly. Patients should have blood volume supplementation, and regular monitoring of renal function should be considered after the start of concurrent treatment. 2. Diuretics (thiazide or loop diuretics): Previous high-dose diuretic therapy may lead to decreased blood volume and the risk of hypotension when starting treatment with telmisartan. Concomitant medications that must be considered: 1. Other antihypertensive drugs: The blood pressure-lowering effect of telmisartan may be increased by the concomitant use of other antihypertensive drugs. Based on their pharmacological properties, it can be expected that the following drugs may enhance the antihypertensive effect of all antihypertensive drugs, including telmisartan: baclofen, amisartan. In addition, alcohol, barbiturates, anesthetics or antidepressants may exacerbate orthostatic hypotension. 2. Corticosteroids (systemic route): Reduce the antihypertensive effect.

Keep tightly closed.

20mg

24 months.

Zhejiang Kinglyuan Pharmaceutical Co., Ltd.

• Founded in:

  2002-12-18

• Address:

  No. 3, Weijiu Road, Shangyu Economic and Technological Development Zone, Hangzhou Bay, Shangyu District, Shaoxing City, Zhejiang Province

• Tax NO.:

  91330604746318437J

• Registered Funds:

  68.2 million yuan

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