Telmisartan-Amlodipine (telmisartan/amlodipine besylate)
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)).
Amlodipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent with an intrinsically long duration of action.
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.
Amlodipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent that is structurally related to felodipine, nifedipine, and nimodipine. Unlike other currently available agents in the dihydropyridine class, amlodipine has an intrinsically long duration of action. Amlodipine inhibits transmembrane influx of extracellular calcium ions across the membranes of myocardial cells and vascular smooth muscle cells, without changing serum calcium concentrations.
Amlodipine is a peripheral arterial vasodilator; it acts directly on vascular smooth muscle causing reduction in peripheral vascular resistance and blood pressure. In patients with exertional angina, amlodipine reduces total peripheral resistance (afterload) and rate pressure product, and thus myocardial oxygen demand, at any given level of exercise. In patients with vasospastic angina, amlodipine inhibits coronary spasm; the drug blocks constriction and restores blood flow in coronary arteries in response to calcium, potassium, epinephrine, serotonin, and thromboxane A2 analog in animal studies and human vessels in vitro.
Following oral administration of amlodipine besylate tablets and solution (Norliqva(R)), peak plasma concentrations of the drug are attained within 6-12 and 6.5 hours, respectively. With chronic once-daily administration, the antihypertensive effects of amlodipine persist for at least 24 hours. Steady-state amlodipine plasma levels are reached after 7-8 days.
Absolute bioavailability ranges from 64-90%; food does not affect bioavailability of amlodipine. The peak plasma concentration and AUC of amlodipine benzoate (Katerzia(R)) suspension are similar to amlodipine besylate (Norvasc(R)) tablets. A standard high-fat, high-calorie breakfast, compared to fasted state administration, did not have a significant effect on the absorption of amlodipine benzoate suspension.
Administration of amlodipine besylate (Norliqva(R)) solution with a high-fat, high-calorie meal did not have a significant effect on peak plasma concentration and AUC. Amlodipine is approximately 93% bound to plasma proteins. Amlodipine is present in human milk (4.2% estimated median relative infant dose) and in cord blood.
Amlodipine is extensively (approximately 90%) metabolized to inactive metabolites in the liver. Amlodipine is excreted in urine as metabolites (60%) and unchanged drug (10%). The terminal elimination half-life of amlodipine is 30-50 hours; in patients with impaired hepatic function, the plasma elimination half-life is 56 hours.
Geriatric patients and patients with hepatic insufficiency or moderate to severe heart failure have decreased amlodipine clearance resulting in an approximately 40-60% higher AUC. Amlodipine pharmacokinetics are not influenced by renal impairment. In pediatric patients 6-17 years of age, weight-adjusted clearance and volume of distribution were similar to values in adults.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. This product contains 2 medications, telmisartan and amlodipine.
Telmisartan belongs to a class of drugs known as angiotensin receptor blockers (ARBs). Amlodipine belongs to a class of drugs known as calcium channel blockers. They both work by relaxing blood vessels so blood can flow more easily.
Generic name: telmisartan/amlodipine besylate
Pronunciation: (TEL-mi-SAR-tan/am-LOE-di-peen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Telmisartan-Amlodipine
Indications
The following indications are listed for Telmisartan-Amlodipine:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
Dosage of amlodipine besylate and amlodipine benzoate is expressed in terms of amlodipine.
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.
Amlodipine is administered orally (as tablets, solution, or suspension) without regard to meals, preferably at the same time each day. Amlodipine is also commercially available in fixed combination with benazepril (e.g., Lotrel(R)), olmesartan medoxomil (e.g., Azor(R)), olmesartan medoxomil and hydrochlorothiazide (e.g., Tribenzor(R)), telmisartan, valsartan (e.g., Exforge(R)), valsartan and hydrochlorothiazide (e.g., Exforge(R) HCT), and atorvastatin (e.g., Caduet(R)). See the full prescribing information for additional administration instructions for each specific combination product.
If a dose of amlodipine is missed, the missed dose may be administered as soon as possible. If the dose is missed for more than 12 hours, do not take the dose and resume treatment with the next scheduled dose.
Amlodipine besylate tablets: Store the tablets at 15-30degreesC; dispense in a tight, light-resistant container.
Amlodipine besylate oral solution (Norliqva(R)): Store the oral solution at 20-25degreesC (excursions permitted to 15-30degreesC). Store and dispense in the original packaging (amber glass bottle).
Amlodipine benzoate oral suspension (Katerzia(R)): Shake the suspension well and measure each dose with a calibrated measuring device; do not use a household teaspoon or tablespoon. Store the oral suspension at 2-8degreesC and protect from light. Avoid freezing and excessive heat.
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.
Amlodipine is a weak inhibitor of cytochrome P-450 (CYP) 3A isoenzymes.
When amlodipine is used in fixed combination with other drugs, interactions associated with the concomitant agent(s) must be considered in addition to those associated with amlodipine.
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.
Amlodipine is contraindicated in patients with known hypersensitivity to the drug.
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.
Adverse effects reported in 1% or more of patients receiving amlodipine include dose-related edema, dizziness, flushing, and palpitations; fatigue, nausea, abdominal pain, and somnolence also reported. Adverse effects reported in the clinical trial in pediatric patients with hypertension were similar to those that have been reported in adults.
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.
Safety and efficacy of amlodipine in children younger than 6 years of age have not been established. Safety and effectiveness of amlodipine (2.5-5 mg daily) for the treatment of pediatric patients 6-17 years of age with hypertension have been established in a trial of 8 weeks' duration.
Safety and efficacy of amlodipine in fixed combination with atorvastatin, benazepril, olmesartan (with or without hydrochlorothiazide), telmisartan, or valsartan (with or without hydrochlorothiazide) have not been established in pediatric patients.
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.
The manufacturers state that there are limited data on use of amlodipine in pregnant women to inform a drug-associated risk for major birth defects and miscarriage. There is some data indicating that amlodipine crosses the placenta in measurable quantities in the third trimester of pregnancy.
Hypertension in pregnancy is a major cause of maternal, fetal or neonatal morbidity and mortality. Maternal risks include pre-eclampsia, gestational diabetes, premature delivery, placental abruption, delivery complications (e.g., need for cesarean section, postpartum hemorrhage), stroke, pulmonary edema, thromboembolic events, multiple organ failure (liver, kidney) and disseminated intravascular coagulation. Fetal risks include intrauterine growth restriction, prematurity, and intrauterine death. Neonates may require prolonged high-level care and experience morbidity. Pregnant women with hypertension should be carefully monitored and managed accordingly.
Teratogenicity or other embryo-fetal toxicity was not observed when pregnant rats and rabbits were treated orally with a different salt form of amlodipine (amlodipine maleate) at doses up to 10 mg/kg per day (approximately 10 and 20 times the maximum recommended human dose (MRHD) based on body surface area, respectively) during their respective periods of major organogenesis. However, when amlodipine maleate at doses up to 10 mg amlodipine/kg per day was administered to rats for 14 days prior to mating and throughout gestation, litter size decreased approximately 50%, and a 5-fold increase in the number of intrauterine deaths was observed at this dose equivalent to 10 times the MDRD. Amlodipine maleate has also been shown to prolong both the gestation period and the duration of labor in rats at this dose.
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 limited available data from a published clinical lactation study reported that amlodipine is present in human milk at an estimated median relative infant dose of 4.2%. No adverse effects of amlodipine on the breastfed infant have been observed; there is no available information on the effects of amlodipine on milk production.
The manufacturer states that no adjustment in initial telmisartan dosage is necessary in geriatric patients.
The elimination of amlodipine may be impaired substantially in geriatric patients, resulting in increased exposure to the drug (AUC increases of 40-60%). For management of hypertension, some manufacturers recommend an initial amlodipine dosage of 2.5 mg once daily for geriatric patients. For management of vasospastic (Prinzmetal variant) angina or chronic stable angina in geriatric patients, an amlodipine dosage of 5 mg daily is recommended; adequate control of angina usually requires a maintenance dosage of 10 mg once daily.
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.
In geriatric patients, amlodipine clearance is decreased and AUC is increased by about 40-60%. Therefore, amlodipine dosage should be selected carefully, usually initiating therapy with dosages at the lower end of the recommended range (i.e., 2.5 mg daily). The greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly also should be considered.
Clinical studies of amlodipine did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients; however, other clinical experience has not revealed age-related differences in response or tolerance.
ICD codes
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Last reviewed · Source: First Databank (FDB) drug data
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