Product Overview
[Drug Name]
Generic Name: Telmisartan Tablets
Trade Name: AnNeiQiang Telmisartan Tablets 40mg*14 Tablets
Pinyin Code: AnNeiQiang TiMiShaTanPian 40mg*14 Tablets/He
[Main Ingredient]
Active ingredient: Telmisartan. Chemical name: 4′-[(1,4′-dimethyl-2′propyl[2,6′-di-1H-benzimidazole]-1′-yl)methyl]-[1,1′-biphenyl]-2-carboxylic acid. Molecular formula:
C₃₃H₃₀N₄O₂ Molecular weight: 514.63
[Properties]
This product is a white tablet.
[Indications/Main Functions]
For the treatment of essential hypertension.
[Specifications]
40mg*14 tablets
[Dosage and Administration]
1. Adults: Dosing should be individualized. The usual initial dose is one tablet. This product can be used in combination with thiazide diuretics, such as hydrochlorothiazide, as these diuretics have a synergistic antihypertensive effect. Because telmisartan takes 4 to 8 weeks to achieve its maximum effect, this consideration should be taken when increasing the dose. 2. Patients with Renal Impairment: No dose adjustment is required for patients with mild or moderate renal impairment. Telmisartan is not eliminated by hemodialysis.
3. Patients with Hepatic Impairment: For patients with mild or moderate hepatic impairment, the daily dose should not exceed one tablet. 4. Elderly: No dose adjustment is required. 5. Children and Adolescents: Safety and efficacy data for this product have not been established in children and adolescents under 18 years of age. Adverse Reactions:
In placebo-controlled trials, the overall incidence of adverse events with telmisartan (41.4%) was similar to that with placebo (43.9%). The incidence of adverse events was not dose-related or related to patient gender, age, or race. The following adverse reactions are cumulatively reported in 5,788 hypertensive patients treated with telmisartan in clinical trials. Adverse reactions are categorized by frequency as follows: Very Common (>1/10); Common (>1/100, <1/10); Uncommon (>1/1000, >1/100); Rare (>1/10,000, >1/1000); and Very Rare (>1/10,000). 1. Systemic Reactions: Common: Back pain (e.g., sciatica), chest pain, flu-like symptoms, and infectious symptoms (e.g., urinary tract infections including cystitis). Rare: Visual disturbances, hyperhidrosis. 2. Central and Peripheral Nervous System: Common: Dizziness. 3. Gastrointestinal System: Common: Abdominal pain, diarrhea, indigestion, gastrointestinal dysfunction. Rare: Visual disturbances, hyperhidrosis. 4. Musculoskeletal System: Common: Arthralgia, leg cramps or leg pain, muscle aches. 5. Nervous System: Rare: Anxiety. 6. Respiratory System: Common: Upper respiratory tract infections including pharyngitis and rhinitis. 7. Skin and Appendages: Common: Skin abnormalities such as eczema. 8. In addition, since the marketing of telmisartan, individual case reports have included erythema, pruritus, syncope, insomnia, depression, stomach discomfort, vomiting, hypotension, bradycardia, tachycardia, dyspnea, eosinophilia, thrombocytopenia, asthenia, and decreased work efficiency. Similar to other angiotensin II antagonists, rare cases have reported angioedema, urticaria, and other related adverse reactions. Laboratory Findings: Compared with placebo, decreased hemoglobin or increased uric acid were occasionally observed in the telmisartan treatment group. Telmisartan and placebo resulted in similar or lower increases in serum creatinine and liver enzymes.
[Contraindications]
1. Hypersensitivity to the active ingredient or any of the excipients of this product. 2. Pregnant women in their second or third trimester or breastfeeding women. 3. Patients with biliary obstructive disease. 4. Patients with severe hepatic impairment. 5. Patients with severe renal impairment (creatinine clearance <30 ml/min).
[Drug Interactions]
1. Lithium. Concomitant use of lithium with angiotensin-converting enzyme inhibitors can cause reversible increases in blood lithium levels and toxic reactions. Isolated cases have also been reported when lithium is used with angiotensin I receptor antagonists. Therefore, caution should be exercised when lithium is used concomitantly with this product. If concomitant use is necessary, serum potassium levels should be monitored during this period. 2. Some drugs can affect serum potassium levels or cause hyperkalemia (such as ACE inhibitors, potassium-sparing diuretics, potassium ion diuretics, potassium ion supplements, potassium-containing salt substitutes, cyclosporine A, or other drugs such as heparin sodium). If this product is used concomitantly with these drugs, monitoring of serum potassium levels is recommended. Based on experience with other drugs that affect the renin-angiotensin system, concomitant use of this product with these drugs may result in increases in serum potassium levels (see Precautions). 3. Pharmacokinetic studies have investigated the interaction of this product with digoxin, warfarin, hydrochlorothiazide, glyburide, ibuprofen, acetaminophen, and amlodipine. This medication may increase the mean trough blood concentration of digoxin by 20% (in some cases by 39%), so peak digoxin plasma concentrations should be monitored. 4. This medication may enhance the antihypertensive effect of other antihypertensive drugs. Other clinical interactions have not yet been confirmed. 5. Based on their pharmacological properties, the following medications may enhance the antihypertensive effect of antihypertensive drugs, including telmisartan: baclofen and amifostine. Additionally, alcohol, barbiturates, sedatives, hypnotics, or antidepressants may potentiate the orthostatic hypotensive effect. 6. When coadministered with telmisartan, the Cmax of simvastatin metabolites (simvastatin acid) was slightly increased (1.34-fold) and their elimination was accelerated.
[Precautions]
1. Hepatic Impairment: This medication should not be used in patients with cholestasis, biliary obstructive disease, or severe hepatic impairment, as telmisartan is primarily excreted in the bile, and the clearance of this medication may be reduced in these patients. This medication should be used with caution in patients with mild to moderate hepatic impairment. 2. Renovascular Hypertension: In patients with bilateral renal artery stenosis or stenosis of a single functioning kidney, the use of drugs that affect the renin-angiotensin-aldosterone system increases the risk of severe hypotension and renal insufficiency. 3. Renal Insufficiency and Renal Transplant Patients: This product should not be used in patients with severe renal insufficiency (creatinine clearance <30 ml/min, see Contraindications). For patients with renal insufficiency, serum potassium and creatinine levels should be monitored regularly during use of this product. There are no data on the use of this product in patients shortly after a recent renal transplant. 4. Patients with Volume Depletion: In patients with volume depletion or low serum sodium levels due to strong diuretic therapy, salt restriction, nausea, or vomiting, the use of this product, especially after the first dose, may cause symptomatic hypotension. Therefore, serum sodium and volume levels should be corrected before using this product. 5. Other Conditions Related to Stimulation of the Renin-Angiotensin-Aldosterone System: For patients whose vascular tone and renal function are primarily dependent on the activity of the renin-angiotensin-aldosterone system (such as patients with severe congestive heart failure or renal disease including renal artery stenosis), use of this drug may affect this system. 6. Primary Aldosteronism: Antihypertensive drugs that inhibit the renin-angiotensin-aldosterone system are generally ineffective in patients with primary aldosteronism. Therefore, this drug is not recommended for use in such patients. 7. Aortic or Mitral Stenosis, Obstructive Hypertrophic Cardiomyopathy: As with other vasodilators, patients with aortic or mitral stenosis or obstructive hypertrophic cardiomyopathy should exercise caution when using this drug. 8. Electrolyte Imbalance: Hyperkalemia: Use of drugs that affect the renin-angiotensin-aldosterone system may cause hyperkalemia, particularly in patients with renal impairment and/or heart failure, as well as in patients with diabetes. However, for patients at risk, serum potassium levels should be closely monitored while taking this drug. Based on experience with other drugs that affect the renin-angiotensin system, this drug may increase serum potassium levels when used concomitantly with potassium-sparing diuretics, potassium supplements, potassium-containing salt substitutes, or other drugs that increase serum potassium levels (such as heparin). Therefore, caution should be exercised when using this drug (see Drug Interactions). 9. Other: Similar to angiotensin-converting enzyme inhibitors, the antihypertensive effect of this drug and other angiotensin antagonists is less in blacks than in other ethnic groups. This may be related to the higher prevalence of low renin status in hypertensive populations in blacks. As with other antihypertensive drugs, excessive blood pressure reduction can cause myocardial infarction or stroke in patients with ischemic heart disease or ischemic cardiovascular disease. 10. Effects on Driving and Operating Machinery: The effects of this drug on driving and operating machinery have not been studied. However, caution should be exercised when driving or operating machinery, as antihypertensive treatment can sometimes cause dizziness and drowsiness.
[Pediatric Use]
Safety and efficacy data for this drug have not been established in children and adolescents under 18 years of age. [Use in Elderly Patients]
No dosage adjustment is required for this product.
[Overdose]
No case reports of overdose have been reported. The most likely manifestations of a telmisartan overdose are hypotension and tachycardia, although bradycardia may also occur. Telmisartan cannot be removed by hemodialysis. In the event of an overdose, the patient should be closely observed and symptomatic and supportive care should be provided. Treatment should be tailored to the timing of ingestion and the severity of symptoms. Recommended measures include inducing vomiting and/or gastric lavage. Activated charcoal may be effective in treating overdose. Serum electrolytes and creatinine should be closely monitored. If hypotension occurs, the patient should be placed supine and salt and fluid intake should be promptly replaced.
[Pharmacology and Toxicology]
Pharmacological Action: Telmisartan is a specific angiotensin II receptor (ATI) antagonist. Telmisartan binds with high affinity to the ATI receptor subtype (known angiotensin II action site) by displacing the angiotensin II receptor. Telmisartan has no agonist effect at any site within the ATI receptor site and binds selectively and persistently to the ATI receptor. Telmisartan has no affinity for other receptors, including AT2 and other less characterized AT receptors. The functions of these other receptors are unknown, as is the potential for receptor overstimulation due to telmisartan-induced increases in angiotensin II levels. Telmisartan does not inhibit plasma renin in humans or block ion channels. It does not inhibit angiotensin-converting enzyme (ACE), which can also lead to adverse reactions by enhancing bradykinin degradation. Telmisartan has no affinity for other receptors, including AT2 and other less characterized AT receptors whose functions are still unknown. In humans, administration of 80 mg of telmisartan almost completely inhibits the angiotensin II-induced blood pressure increase. This inhibitory effect persists for 24 hours and is still measurable after 48 hours. The antihypertensive effect becomes apparent within 3 hours after the first dose of telmisartan. Maximum antihypertensive effect is achieved 4 weeks after the start of treatment and is maintained with long-term treatment. Ambulatory blood pressure monitoring demonstrates that the antihypertensive effect persists for more than 24 hours after dosing, including the 4 hours before the next dose. This finding was confirmed in placebo-controlled clinical trials: after taking 40 mg and 80 mg of telmisartan, the trough-to-peak ratio remained consistently above 80%. There was a clear dose-time dependence for return to baseline SBP. Data regarding DPB are conflicting. In patients with hypertension, telmisartan lowers both systolic and diastolic blood pressure without affecting heart rate. Telmisartan's antihypertensive effects are comparable to those of other representative antihypertensive drugs. (Clinical trials have compared telmisartan with amlodipine, atenolol, enalapril, hydrochlorothiazide, losartan, and lisinopril.) If telmisartan treatment is abruptly discontinued, blood pressure gradually returns to pre-treatment levels over several days, without rebound hypertension. In clinical trials directly comparing two antihypertensive drugs, the incidence of dry cough was significantly lower in patients treated with telmisartan than in those treated with angiotensin-converting enzyme inhibitors. The effectiveness of telmisartan in improving mortality and cardiovascular morbidity remains unknown. Toxicology: Preclinical safety studies, at doses comparable to clinically effective doses, resulted in decreased erythrocyte indices (erythrocytes, hemoglobin, and hematocrit), altered renal hemodynamics (increased blood urea nitrogen and creatinine), and elevated serum potassium in normotensive animals. Renal tubular dilation and atrophy were observed in dogs. Gastrointestinal mucosal damage (erosions, ulcers, or inflammation) was also observed in rats and dogs. These adverse pharmacological reactions, known from preclinical studies to be common to both angiotensin-converting enzyme inhibitors and angiotensin II antagonists, can be prevented with oral salt supplementation. Increased plasma renin activity and juxtaglomerular cell hypertrophy/proliferation were also observed in both species. These changes, common to both angiotensin-converting enzyme inhibitors and other angiotensin II antagonists, are not clinically specific. Animal studies have shown potential adverse effects on fetal and postnatal development, including weight loss, delayed eye opening, and increased mortality. No mutagenicity or related mutagenic activity was observed in vitro, and no carcinogenicity was observed in mice or rats.
