Telmisartan (telmisartan)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Telmisartan is a nonpeptide, benzimidazole-derivative angiotensin II type 1 (AT1) receptor antagonist (also referred to as an angiotensin II receptor blocker (ARB)).
Telmisartan is a nonpeptide, angiotensin II receptor (AT1) antagonist. Telmisartan blocks the vasoconstriction and aldosterone-secreting effects of angiotensin II by blocking the binding of angiotensin II to the AT1 receptor in many tissues. Angiotensin II is the primary pressor agent from the renin-angiotensin system that causes vasoconstriction, stimulation of the synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium.
Telmisartan does not inhibit the degradation of bradykinin like angiotensin converting enzyme (ACE) inhibitors.
Following oral administration, peak plasma concentrations of telmisartan occur after 0.5-1 hour. Administration of telmisartan with food slightly reduces the bioavailability of the drug. At 40 mg and 160 mg doses, the bioavailability of telmisartan is 42% and 58%, respectively.
Telmisartan has an accumulation index of 1.5-2.0 with repeated once daily dosing. Antihypertensive effects of telmisartan are evident within 2 weeks of initiation, with maximum blood pressure lowering observed after 4 weeks. Telmisartan is highly bound to plasma proteins (>99.5%), principally albumin and alpha1-acid glycoprotein.
Telmisartan is excreted mainly (>97%) as unchanged drug in feces via biliary elimination; only small amounts (less than 1% of an administered dose) are excreted in urine. The drug undergoes conjugation with glucuronic acid, forming pharmacologically inactive metabolites. Telmisartan is not metabolized by the cytochrome P-450 (CYP) microsomal enzyme system.
In addition, in vitro studies indicate that telmisartan does not appear to have an inhibitory effect on CYP isoenzymes except for CYP2C19. The elimination half-life of telmisartan is approximately 24 hours.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Telmisartan belongs to a class of drugs known as angiotensin receptor blockers (ARBs).
It works by relaxing blood vessels so blood can flow more easily.
Generic name: telmisartan
Pronunciation: (tel-mi-SAR-tan)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Telmisartan
Indications
The following indications are listed for Telmisartan:
- Hypertension
- Myocardial Infarction Prevention
- Prevention Of Cerebrovascular Accident
Also known as: Acute Mi Prophylaxis, Acute Myocardial Infarction Prophylaxis, Ami Prophylaxis, Cardiac Infarct Prophylaxis, Cardiac Infarction Prophylaxis, Cva Prophylaxis, Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Mi Prophylaxis, Myocardial Infarct Prophylaxis, Myocardial Infarction Prophylaxis, Stroke Prophylaxis, Systemic Arterial Hypertension.
Dosing
No dosing information is available for this tab.
Telmisartan is administered orally as tablets. Although food may reduce the bioavailability of telmisartan, the manufacturer states that the drug can be taken without regard to meals.
Telmisartan is also commercially available in fixed combination with hydrochlorothiazide and with amlodipine. See the prescribing information for these fixed-combination products for additional information on administration.
Store tablets at 20-25degreesC (may be exposed to 15-30degreesC). Tablets should not be removed from blisters until immediately before administration.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Telmisartan is not metabolized by cytochrome P-450 (CYP) isoenzymes and has no effect on CYP isoenzymes except for some inhibition of CYP2C19 in vitro.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity (e.g., anaphylaxis or angioedema) to telmisartan or any ingredient in the formulation.
*Concomitant use of telmisartan and aliskiren in patients with diabetes mellitus.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in >=1% of patients receiving telmisartan in clinical trials include back pain, sinusitis, diarrhea, intermittent claudication, and skin ulcer.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy have not been established in pediatric patients younger than 18 years of age.
If oliguria or hypotension occurs in infants with in utero exposure to telmisartan, blood pressure and renal function should be supported; exchange transfusions or dialysis may be required.
Telmisartan can cause fetal and neonatal morbidity and mortality when administered to a pregnant woman. Telmisartan should be discontinued as soon as possible when pregnancy is detected. Drugs that act on the renin-angiotensin system (e.g., ACE inhibitors, angiotensin II receptor antagonists) reduce fetal renal function and increase fetal and neonatal morbidity and mortality when used during the second and third trimesters of pregnancy. Oligohydramnios, reduced fetal renal function leading to anuria and renal failure, fetal lung hypoplasia, and skeletal deformations, including skull hypoplasia, hypotension, and death, have occurred.
In patients receiving telmisartan during pregnancy, perform serial ultrasound examinations to assess the intra-amniotic environment and perform fetal testing as appropriate, based on gestational age. If oligohydramnios is observed, telmisartan should be discontinued unless it is considered life-saving for the mother. Oligohydramnios may not appear until after the fetus has sustained irreversible injury.
Infants exposed in utero to telmisartan should be monitored for hypotension, oliguria, and hyperkalemia. If oliguria or hypotension occurs in infants with in utero exposure to telmisartan, blood pressure and renal function should be supported; exchange transfusions or dialysis may be required.
It is not known whether telmisartan is excreted into human milk. Telmisartan is present in the milk of lactating rats. The effects of telmisartan on the breast-fed infant and the effects on milk production are not known. Because of the potential for serious adverse reactions to telmisartan (including hypotension, hyperkalemia, and renal impairment) in nursing infants, discontinue nursing or the drug.
The manufacturer states that no adjustment in initial telmisartan dosage is necessary in geriatric patients.
No substantial differences in safety and efficacy of telmisartan in geriatric patients have been observed relative to younger adults, but increased sensitivity cannot be ruled out.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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