Telmisartan
FDA Drug Information • Also known as: Micardis, Telmisartan
- Brand Names
- Micardis, Telmisartan
- Dosage Form
- POWDER
- Product Type
- BULK INGREDIENT
⚠ Boxed Warning (Black Box)
WARNING: FETAL TOXICITY
When pregnancy is detected, discontinue telmisartan tablets as soon as possible [ see Warnings and Precautions (5.1) and Use in Specific Populations ( 8.1) ]. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus [ see Warnings and Precautions (5.1) and Use in Specific Populations ( 8.1 ) ]. WARNING: FETAL TOXICITY See full prescribing information for complete boxed warning. When pregnancy is detected, discontinue telmisartan tablets as soon as possible ( 5.1 , 8.1 ) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus ( 5.1 , 8.1 )Description
11 DESCRIPTION Telmisartan is a non-peptide angiotensin II receptor (type AT 1 ) antagonist. Telmisartan is chemically described as 4'-[(1, 4'-dimethyl-2'-propyl [2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1’-biphenyl]-2-carboxylic acid. Its empirical formula is C 33 H 30 N 4 O 2 , its molecular weight is 514.63, and its structural formula is: Telmisartan,USP is a white to slightly yellowish solid. It is practically insoluble in water and in the pH range of 3 to 9, sparingly soluble in strong acid (except insoluble in hydrochloric acid), and soluble in strong base. Telmisartan is available as tablets for oral administration, containing 20 mg, 40 mg or 80 mg of telmisartan,USP. The tablets contain the following inactive ingredients: sodium hydroxide, meglumine, povidone, mannitol, and magnesium stearate. telmisartan tablets are hygroscopic and require protection from moisture. telmisartan-fig1
What Is Telmisartan Used For?
1 INDICATIONS AND USAGE Telmisartan is an angiotensin II receptor blocker (ARB) indicated for:
Treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.( 1.1 ) Cardiovascular (CV) risk reduction in patients unable to take ACE inhibitors (1.2) 1.1 Hypertension Telmisartan tablets,USP are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including the class to which this drug principally belongs. Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC). Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly. Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal. Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy. Telmisartan may be used alone or in combination with other antihypertensive agents [ see Clinical Studies (14.1) ]. 1.2...Dosage and Administration
2 DOSAGE & ADMINISTRATION
May be administered with or without food ( 2.1 ) When used for cardiovascular risk reduction, monitoring of blood pressure is recommended, and if appropriate, adjustment of medications that lower blood pressure may be necessary ( 2.2 ) Indication Starting Dose Dose Range Hypertension ( 2.1 ) 40 mg once daily 40 to 80 mg once daily Cardiovascular Risk Reduction ( 2.2 ) 80 mg once daily 80 mg once daily 2.1 Hypertension Dosage must be individualized. The usual starting dose of telmisartan tablets is 40 mg orally once a day. Blood pressure response is dose-related over the range of 20 to 80 mg [ see Clinical Studies (14.1) ]. Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks. No initial dosage adjustment is necessary for elderly patients or patients with renal impairment, including those on hemodialysis. Patients on dialysis may develop orthostatic hypotension; their blood pressure should be closely monitored. Telmisartan tablets may be administered with other antihypertensive agents. Telmisartan tablets may be administered with or without food. 2.2 Cardiovascular Risk Reduction The recommended dose of telmisartan tablets is 80 mg once a day and can be administered with or without food. It is not known whether doses lower than 80 mg of telmisartan are effective in reducing the risk of cardiovascular morbidity and mortality. When initiating telmisartan therapy for cardiovascular risk reduction, monitoring of blood pressure is recommended, and if appropriate, adjustment of medications that lower blood pressure may be necessary.Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS The following adverse reaction is described elsewhere in labeling: Renal dysfunction upon use with ramipril [ see Warnings and Precautions (5.6) ]
Hypertension: The most common adverse events (≥1%) reported in hypertension trials are back pain, sinusitis, and diarrhea ( 6.1 ) Cardiovascular risk reduction: The serious adverse events (≥1%) reported in cardiovascular risk reduction trials were intermittent claudication and skin ulcer ( 6.1) To report SUSPECTED ADVERSE REACTIONS, contact Modavar Pharmaceuticals LLC At 800-688-4697, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reactions rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. Hypertension Telmisartan has been evaluated for safety in more than 3700 patients, including 1900 treated for over 6 months and more than 1300 for over one year. Adverse experiences have generally been mild and transient in nature and have infrequently required discontinuation of therapy. In placebo-controlled trials involving 1041 patients treated with various doses of telmisartan (20 to 160 mg) monotherapy for up to 12 weeks, the overall incidence of adverse events was similar to that in patients treated with placebo. Adverse events occurring at an incidence of ≥1% in patients treated with telmisartan and at a greater rate than in patients treated with placebo, irrespective of their causal association, are presented in Table 1. Table 1 Adverse Events Occurring at an Incidence of ≥1% in Patients Treated with telmisartan and at a Greater Rate Than Patients Treated with Placebo Telmisartan n=1455 % Placebo n=380 % Upper respiratory tract infection 7 6 Back pain 3 1 Sinusitis 3 2 Diarrhea 3 2 Pharyngitis 1 0 In addition to the adverse events in the table, the following events occurred at a rate of ≥1% but were at least as frequent in the placebo group: influenza-like symptoms, dyspepsia, myalgia, urinary tract infection, abdominal pain, headache, dizziness, pain, fatigue, coughing, hypertension, chest pain, nausea, and peripheral edema. Discontinuation of therapy because of adverse events was required in 2.8% of 1455 patients treated with telmisartan tablets and 6.1% of 380 placebo patients in placebo-controlled clinical trials. The incidence of adverse events was not dose-related and did not correlate with gender, age, or race of patients. The incidence of cough occurring with telmisartan in 6 placebo-controlled trials was identical to that noted for placebo-treated patients (1.6%). In addition to those listed above, adverse events that occurred in more than 0.3% of 3500 patients treated with telmisartan monotherapy in controlled or open trials are listed below. It cannot be determined whether these events were causally related to telmisartan tablets: Autonomic Nervous System : impotence, increased sweating, flushing; Body as a Whole : allergy, fever, leg pain, malaise; Cardiovascular : palpitation, dependent edema, angina pectoris, tachycardia, leg edema, abnormal ECG; CNS : insomnia, somnolence, migraine, vertigo, paresthesia, involuntary muscle contractions, hypoesthesia; Gastrointestinal : flatulence, constipation, gastritis, vomiting, dry mouth, hemorrhoids, gastroenteritis, enteritis, gastroesophageal reflux, toothache, non-specific gastrointestinal disorders; Metabolic : gout, hypercholesterolemia, diabetes mellitus; Musculoskeletal : arthritis, arthralgia, leg cramps; Psychiatric : anxiety, depression, nervousness; Resistance Mechanism : infection, fungal infection, abscess, otitis media; Respiratory : asthma, bronchitis, rhinitis, dyspnea, epistaxis; Skin : dermatitis, rash, eczema, pruritus; Urinary : micturition frequency, cystitis; Vascular : cerebrovascular disorder; and Special Senses : abnormal vision, conjunctivitis,...Drug Interactions
7 DRUG INTERACTIONS Aliskiren: Do not co-administer aliskiren with telmisartan in patients with diabetes. Avoid use of aliskiren with telmisartan in patients with renal impairment (GFR <60 mL/min). Digoxin: When telmisartan was co-administered with digoxin, median increases in digoxin peak plasma concentration (49%) and in trough concentration (20%) were observed. Therefore, monitor digoxin levels when initiating, adjusting, and discontinuing telmisartan for the purpose of keeping the digoxin level within the therapeutic range. Lithium : Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium with angiotensin II receptor antagonists including telmisartan. Therefore, monitor serum lithium levels during concomitant use. Non-Steroidal Anti-Inflammatory Agents including Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors) : In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, co-administration of NSAIDs, including selective COX-2 inhibitors, with angiotensin II receptor antagonists, including telmisartan, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving telmisartan and NSAID therapy. The antihypertensive effect of angiotensin II receptor antagonists, including telmisartan may be attenuated by NSAIDs including selective COX-2 inhibitors.
NSAIDs: Increased risk of renal impairment and loss of anti-hypertensive effect (7) Do not co-administer aliskiren with telmisartan in patients with diabetes (7)Contraindications
4 CONTRAINDICATIONS Telmisartan tablets are contraindicated in patients with known hypersensitivity (e.g., anaphylaxis or angioedema) to telmisartan or any other component of this product [ see Adverse Reactions (6.2) ]. Do not co-administer aliskiren with telmisartan tablets in patients with diabetes [ see Drug Interactions (7) ].
Known hypersensitivity (e.g., anaphylaxis or angioedema) to telmisartan or any other component of this product ( 4 ) Do not co-administer aliskiren with telmisartan in patients with diabetes ( 4 )Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary Telmisartan can cause fetal harm when administered to a pregnant woman. Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death (see Clinical Considerations). Most epidemiologic studies examining fetal abnormalities after exposure to antihypertensive use in the first trimester have not distinguished drugs affecting the renin-angiotensin system from other antihypertensive agents. Studies in rats and rabbits with telmisartan showed fetotoxicity only at maternally toxic doses (see Data). When pregnancy is detected, discontinue telmisartan as soon as possible. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Hypertension in pregnancy increases the maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section, and post-partum hemorrhage). Hypertension increases the fetal risk for intrauterine growth restriction and intrauterine death. Pregnant women with hypertension should be carefully monitored and managed accordingly. Fetal/Neonatal adverse reactions Use of drugs that act on the RAS in the second and third trimesters of pregnancy can result in the following: oligohydramnios, reduced fetal renal function leading to anuria and renal failure, fetal lung hypoplasia, skeletal deformations, including skull hypoplasia, hypotension, and death. In the unusual case that there is no appropriate alternative to therapy with drugs affecting the...
Overdosage
10 OVERDOSAGE Limited data are available with regard to overdosage in humans. The most likely manifestation of overdosage with telmisartan tablets would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Telmisartan is not removed by hemofiltration and is not dialyzable.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Telmisartan tablets USP, 20 mg are white to off-white, round shaped, uncoated tablet, debossed with "C44" on one side and plain on other side and are supplied as follows: NDC 72241-015-16, in blister pack of 30 tablets (3 x 10 Unit-Dose) NDC 72241-015-18, in child resistant blister pack of 30 tablets (3 x 10 Unit-Dose) NDC 72241-015-22 Bottles of 30 NDC 72241-015-04 Bottles of 90 NDC 72241-015-05 Bottles of 100 NDC 72241-015-10 Bottles of 500 NDC 72241-015-11 Bottles of 1000 Telmisartan tablets USP, 40 mg are white to off-white, oblong, biconvex, uncoated tablet, debossed with "C141" on one side and plain on other side and are supplied as follows: NDC 72241-016-16, in blister pack of 30 tablets (3 x 10 Unit-Dose) NDC 72241-016-18, in child resistant blister pack of 30 tablets (3 x 10 Unit-Dose) NDC 72241-016-22 Bottles of 30 NDC 72241-016-04 Bottles of 90 NDC 72241-016-05 Bottles of 100 NDC 72241-016-10 Bottles of 500 NDC 72241-016-11 Bottles of 1000 Telmisartan tablets USP, 80 mg are white to off-white, oval, biconvex, uncoated tablet, debossed with "C144" on one side and plain on other side and are supplied as follows: NDC 72241-017-16, in blister pack of 30 tablets (3 x 10 Unit-Dose) NDC 72241-017-18, in child resistant blister pack of 30 tablets (3 x 10 Unit-Dose) NDC 72241-017-22 Bottles of 30 NDC 72241-017-04 Bottles of 90 NDC 72241-017-05 Bottles of 100 NDC 72241-017-10 Bottles of 500 NDC 72241-017-11 Bottles of 1000 Storage Store at 25°C (77°F); excursions permitted between 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Tablets should not be removed from blisters or bottles until immediately before administration.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.