Properties
- Form
- tableti
- Dosage mg
- 40
- Pack
- 30
What is it?
Instructions for use Telmisartan Tablets 40mg Telzisarti Trade name: Telzisarti 40 International Nonproprietary Name: Telmisartan Pharmaceutical form Tablets Composition Each uncoated tablet contains: Telmisartan USP 40mg Pharmacotherapeutic group: Angiotensin II antagonists Pharmacological characteristics Pharmacodynamics Mechanism of action: Telmisartan is an orally effective and specific angiotensin II receptor subtype 1 (AT1) antagonist. Telmisartan displaces angiotensin II from its binding site with very high affinity to the AT1 receptor subtype, which is responsible for the effects of angiotensin II. Telmisartan does not exhibit partial agonist activity at the AT1 receptor. The binding is long-lasting. Telmisartan does not exhibit affinity for other receptors, including AT2 and other less characterized AT receptors. The functional role of these receptors is unknown, nor is the effect of their potential overstimulation by angiotensin II, the levels of which are increased by telmisartan. Plasma aldosterone levels are reduced by telmisartan. Telmisartan does not inhibit plasma renin levels and does not block ionic channels. Telmisartan does not inhibit angiotensin-converting enzyme (kininase II), an enzyme that also inactivates bradykinin. Therefore, potentiation of bradykinin-induced side effects is not expected. Pharmacokinetics Absorption: Absorption of telmisartan is rapid, although the amount absorbed varies. The mean absolute bioavailability of telmisartan is 50%. Food slightly reduces the bioavailability of telmisartan by reducing the concentration-time curve (AUC) by approximately 6% when taking a 40mg tablet and by 19% when taking 160mg. 3 hours after administration, plasma telmisartan concentrations are similar whether taken fasting or with food. Distribution Telmisartan is highly bound to plasma proteins (>99.5%), primarily albumin and alpha-1-acid glycoprotein. The volume of distribution of telmisartan is approximately 500 liters. Biotransformation Telmisartan is metabolized by conjugation to form the glucuronide of the parent compound. The pharmacological activity of the conjugate has not been demonstrated. Elimination Telmisartan is characterized by bioexponential pharmacokinetics, with a terminal half-life of >20 hours. Peak plasma concentration (Cmax) and the concentration-time curve (AUC) increase disproportionately with dose. After oral and intravenous administration, telmisartan is almost completely excreted in feces, mainly unchanged. Cumulative excretion in urine is less than 1% of the dose. The total plasma clearance of telmisartan is high (approximately 1000 ml/min) compared to hepatic blood flow (approximately 1500 ml/min). Therapeutic indications Telmisartan is indicated for: Hypertension: Treatment of essential hypertension. In adults. Cardiovascular prevention: Reduction of cardiovascular morbidity in adults with: - Manifested atherothrombotic cardiovascular disease (history of ischemic heart disease, stroke, or peripheral artery disease) or - Type 2 diabetes mellitus with confirmed target organ damage. Dosage and method of administration Treatment of essential hypertension: The usual effective dose is 40mg once daily. In some patients, 20mg once daily may be beneficial. When the target blood pressure is not achieved, the dose may be increased up to 80mg once daily. Alternatively, telmisartan may be used in combination with thiazide-type diuretics, such as hydrochlorothiazide, which has an additive blood pressure-lowering effect. When considering dose increases, it should be noted that the maximum antihypertensive effect is usually achieved 4-8 weeks after the start of treatment. Cardiovascular prevention: The recommended dose is 80mg once daily. It is not known whether doses of telmisartan lower than 80mg are effective for reducing cardiovascular morbidity. When initiating treatment with telmisartan for the reduction of cardiovascular morbidity, blood pressure monitoring and appropriate adjustment of blood pressure-lowering medications are recommended. Special populations Patients with renal impairment: A lower starting dose of 20mg is recommended in such patients. Dose adjustment is not recommended in patients with mild to moderate renal insufficiency. Patients with hepatic impairment: Telmisartan is contraindicated in patients with severe hepatic insufficiency. In patients with mild to moderate hepatic insufficiency, the dose should not exceed 40mg once daily. Method of administration Telmisartan tablets are intended for once-daily oral administration, to be taken with fluid, with or without food. Contraindications • Hypersensitivity to any of the active ingredients • Second and third trimester of pregnancy • Biliary obstructive diseases • Severe hepatic insufficiency Concomitant use of telmisartan with products containing aliskiren is contraindicated in patients with diabetes mellitus or renal impairment (GFR <60 ml/min/1.73 m2). Special warnings and precautions for use Pregnancy The use of angiotensin II receptor antagonists should be discontinued immediately upon diagnosis of pregnancy, and alternative treatment should be initiated if possible. Hepatic impairment Telmisartan should be used with caution in patients with mild to moderate hepatic insufficiency. Renovascular hypertension There is an increased risk of acute hypotension and renal impairment in patients with bilateral renal artery stenosis or stenosis of a single functioning renal artery who are taking medical products acting on the renin-angiotensin-aldosterone system. Intravascular hypovolemia Symptomatic hypotension, especially after the first dose, may occur in patients with volume and/or sodium depletion due to aggressive diuretic therapy, dietary salt restriction, diarrhea, or vomiting. These conditions should be corrected before taking telmisartan tablets. Dual blockade of the renin-angiotensin-aldosterone system (RAAS). ACE inhibitors and angiotensin II receptor blockers should not be used concomitantly in patients with diabetic nephropathy. Primary aldosteronism Patients with primary aldosteronism usually do not respond to antihypertensive medical products acting on the renin-angiotensin-aldosterone system. Therefore, the use of telmisartan tablets is not recommended. Aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy As with other vasodilators, particular caution is required in patients with aortic or mitral stenosis or obstructive hypertrophic cardiomyopathy. Diabetic patients treated with insulin or antidiabetic agents Hypoglycemia may occur in these patients when telmisartan is used. Therefore, monitoring of glucose levels is necessary in such patients. The dose of insulin and antidiabetic agents may need to be adjusted if indicated. - Hyperkalemia The use of medicinal products acting on the renin-angiotensin-aldosterone system may cause hyperkalemia. Intensive monitoring of serum potassium levels is necessary in patients at risk. - Hypokalemia Other As with any antihypertensive agent, excessive reduction in blood pressure in individuals with ischemic cardiomyopathy or ischemic cardiovascular disease may lead to myocardial infarction or stroke. Interactions with other medicinal products and other forms of interaction Digoxin: Concomitant administration of telmisartan with digoxin has been associated with a mean increase in peak plasma digoxin concentration (49%) and an increase in concentration (20%). Monitoring of digoxin levels is required when initiating, changing, or discontinuing telmisartan to maintain therapeutic range. Potassium-sparing diuretics or potassium supplements: If concomitant use is necessary due to confirmed hypokalemia, it should be administered with caution and with frequent monitoring of serum potassium levels. Lithium If this combination is necessary, intensive monitoring of serum lithium levels is required. Non-steroidal anti-inflammatory medicinal products Adequate hydration of patients is required, and renal function should be monitored when initiating and periodically thereafter for concomitant therapy. Other antihypertensive agents: The blood pressure-lowering effect of telmisartan may be enhanced by the use of other antihypertensive agents. Fertility, pregnancy and lactation: Pregnancy: The use of angiotensin II receptor antagonists is not recommended in the first trimester of pregnancy. The use of angiotensin II receptor antagonists is contraindicated in the second and third trimesters of pregnancy. Breastfeeding: The use of telmisartan during breastfeeding is not recommended, and alternative therapy with a better-established safety profile during lactation should be initiated, especially when breastfeeding a newborn or premature infant. Effects on ability to drive and use machines When driving or operating machinery, it should be noted that dizziness and drowsiness may occasionally occur when taking telmisartan. Undesirable effects The following side effects have been reported with the use of telmisartan. Adverse reactions are classified by frequency as follows: very common (>1/10), common (>1/100 to <1/10), uncommon (>1/1000 to <1/100), rare (>1/10,000 to <1/1000), very rare (<1/10,000), unknown (cannot be estimated from available data). Telmisartan Uncommon: Urinary tract infections including cystitis, upper respiratory tract infections including pharyngitis and sinusitis, anemia, hyperkalemia, insomnia, depression, syncope, vertigo, bradycardia, hypotension, orthostatic hypotension, dyspnea, cough, abdominal pain, diarrhea, dyspepsia, flatulence, vomiting, pruritus, hyperhidrosis, rash, back pain (e.g., sciatica), muscle spasms, myalgia, renal impairment (including acute renal failure), chest pain, asthenia (weakness), increased blood creatinine. Rare: Sepsis including fatal outcome, eosinophilia, thrombocytopenia, anaphylactic reactions, hypersensitivity, hypoglycemia (in diabetic patients), anxiety, somnolence, visual disturbances, tachycardia, dry mouth, gastric discomfort, dysgeusia, angioedema (including fatal outcome), eczema, erythema, urticaria, drug eruption, toxic skin eruption, arthralgia, limb pain, tendon pain (symptoms of tendinitis), flu-like illness, decreased hemoglobin, increased uric acid in blood, increased liver enzymes, increased serum creatine phosphokinase. Arthrosis, tendon pain, decreased hemoglobin. Very rare: Interstitial lung disease. Overdose The most prominent manifestations of telmisartan overdose were hypotension and tachycardia, bradycardia, dizziness, vomiting, increased serum creatinine, acute renal failure. Treatment Telmisartan is not removed by hemodialysis. Intensive monitoring of the patient is required; treatment should be symptomatic and supportive. Management depends on the time elapsed since ingestion and the severity of symptoms. Suggested measures include induction of vomiting and/or gastric lavage. Activated charcoal may be effective for treating overdose. Intensive monitoring of serum electrolytes and creatinine levels is required. In case of hypotension, the patient should be placed in a supine position and rapidly administered salt and fluids. Pre-clinical safety data No particular hazards to humans have been observed in terms of safety pharmacology, genotoxicity, and carcinogenicity potential. Incompatibility Unknown. Form of release and packaging 3X10 tablets in Alu-AAlu blister pack. Shelf life 3 years. Special storage precautions Store at a temperature not exceeding 25°C, in a place protected from moisture. Keep out of reach of children. Dispensing category: Pharmaceutical product group II, dispensed with prescription form N#3.
