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Telmisartan / Amlodipine

Pronunciation: TEL-mi-SAR-tan/am-LOE-di-peen
Class: Antihypertensive combination

Trade Names

Twynsta
- Tablets, oral telmisartan 40 mg/amlodipine 5 mg
- Tablets, oral telmisartan 40 mg/amlodipine 10 mg
- Tablets, oral telmisartan 80 mg/amlodipine 5 mg
- Tablets, oral telmisartan 80 mg/amlodipine 10 mg

Pharmacology

Amlodipine

Inhibits movement of calcium ions across cell membranes in systemic and coronary vascular smooth muscle.

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Telmisartan

Antagonizes the effect of angiotensin II (vasoconstriction and aldosterone secretion) by blocking the angiotensin II receptor (AT 1 receptor) in vascular smooth muscle and the adrenal gland, producing decreased BP.

Indications and Usage

For the treatment of hypertension.

Contraindications

Known hypersensitivity (eg, anaphylaxis, angioedema) to telmisartan, amlodipine, or any other component of this product.

Dosage and Administration

Hypertension
Adults

PO Initially, telmisartan 40 mg/amlodipine 5 mg once daily. Patients requiring larger reductions in BP may be started on telmisartan 80 mg/amlodipine 5 mg once daily. After at least 2 wk, dosage may be increased (max, telmisartan 80 mg/amlodipine 10 mg). Switch patients who experience dose-limiting adverse reactions (eg, edema) on amlodipine 10 mg to telmisartan 40 mg/amlodipine 5 mg once daily.

Elderly

PO Titrate slowly. Because patients 75 y and older should initiate amlodipine at 2.5 mg once daily and the lowest dose of this combination is telmisartan 40 mg/amlodipine 5 mg, initial therapy with telmisartan/amlodipine is not recommended in these patients.

Renal Function Impairment

Titrate slowly in patients with severe renal impairment.

Hepatic Function Impairment

Titrate slowly. Because patients with hepatic impairment should initiate amlodipine at 2.5 mg once daily and the lowest dose of this combination is telmisartan 40 mg/amlodipine 5 mg, initial therapy with telmisartan/amlodipine is not recommended in these patients.

General Advice

  • May be taken with or without food.
  • May be substituted for the individually titrated components. When substituting for individual components, increase the dose of telmisartan/amlodipine if BP control has not been satisfactory.
  • Correct imbalances of intravascular volume or salt depletion before initiating therapy.

Storage/Stability

Store between 59° and 86°F. Protect from moisture and light.

Drug Interactions

No drug interaction studies have been conducted with telmisartan/amlodipine and other drugs, although studies have been conducted with the individual amlodipine and telmisartan components.

ACE inhibitors (eg, captopril, ramipril)

The risk of renal dysfunction and hyperkalemia may be increased. Consider monotherapy. If coadministration cannot be avoided, closely monitor renal function and serum potassium. Coadministration of telmisartan and ramipril is not recommended.

Aliskiren

The risk of hyperkalemia may be increased, especially in diabetic patients. In addition, coadministration may increase the risk of nonfatal stroke, renal complications, and hypotension in diabetic patients. Coadministration is not recommended in diabetic patients.

Azole antifungal agents (eg, itraconazole, ketoconazole)

Amlodipine plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions. Use with caution and monitor cardiac and hemodynamic status during coadministration.

Conivaptan

Plasma concentrations of amlodipine may be increased. Monitor for signs of extended pharmacologic effects of amlodipine.

Cyclooxygenase 2 inhibitors (eg, celecoxib), NSAIDs (eg, ibuprofen, indomethacin)

Coadministration may result in reversible deterioration of renal function, including acute renal failure, especially in patients who have renal impairment or are volume-depleted, and in elderly patients. Also, the antihypertensive effect of telmisartan may be reduced. Monitor renal function and BP.

Cyclosporine

Cyclosporine plasma concentrations may be elevated, increasing its pharmacologic effects.

Digoxin

Plasma concentrations of digoxin may be elevated, increasing the risk of toxicity. Monitor digoxin levels when initiating, adjusting, or discontinuing telmisartan/amlodipine.

Diltiazem

Amlodipine plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions. Closely monitor BP and adjust the amlodipine dose as needed.

Grapefruit juice

May increase the bioavailability of amlodipine. Avoid coadministration.

Lithium

Lithium plasma concentrations may be elevated, increasing its pharmacologic effects and the risk of toxicity. Monitor lithium levels and adjust the lithium dose as needed.

Potassium preparations (eg, potassium supplements), potassium-sparing diuretics (eg, amiloride)

The risk of hyperkalemia, possibly with cardiac arrhythmias or cardiac arrest, may be increased. Closely monitor serum potassium and renal function. Adjust therapy as needed.

Protease inhibitors (eg, indinavir, ritonavir)

The antihypertensive effects of amlodipine may be increased. Use with caution and closely monitor clinical response.

Simvastatin

Plasma concentrations and pharmacologic effects of simvastatin may be increased. The dosage of simvastatin should not exceed 20 mg/day when amlodipine is coadministered.

Trimethoprim

The risk of hyperkalemia is increased, especially in elderly patients. An alternative antibiotic may be preferred in elderly patients. If coadministration cannot be avoided, monitor serum potassium concentrations and clinical response. Adjust the antihypertensive dose as needed.

Adverse Reactions

Cardiovascular

Hypotension, syncope (less than 2%).

CNS

Dizziness (3%).

Metabolic

Peripheral edema (5%); edema (less than 2%).

Musculoskeletal

Back pain (2%).

Precautions

Warnings

When used in pregnancy, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.


Monitor

Monitor BP and assess renal function at regular intervals during therapy. Periodically monitor serum electrolytes. Closely monitor patients with heart failure, hepatic insufficiency, or biliary obstructive disorders.


Pregnancy

Category D . 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. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue telmisartan/amlodipine as soon as possible. These adverse outcomes are usually associated with use of these drugs in the second and third trimesters of pregnancy.

Lactation

Undetermined. Breast-feeding is not recommended.

Children

Safety and efficacy not established.

Elderly

Use with caution reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Use as initial therapy is not recommended in these patients.

Renal Function

Use with caution in patients with severe renal impairment. In studies of ACE inhibitors in patients with unilateral or bilateral renal artery stenosis, increases in serum creatinine or BUN were observed; anticipate a similar effect with telmisartan.

Hepatic Function

Use with caution in patients with biliary obstructive disorders or hepatic insufficiency; not recommended as initial therapy in patients with hepatic impairment.

Cardiovascular effects

Increased frequency, duration, or severity of angina or acute MI may occur. Use with caution in patients with heart failure or severe aortic stenosis.

Hyperkalemia

May occur in patients on angiotensin II receptor blockers, especially in patients with advanced renal impairment or heart failure, on renal replacement therapy, or on potassium supplements, potassium-sparing diuretics, potassium-containing salt substitutes, or other drugs that increase potassium levels.

Hypotension

Symptomatic hypotension may occur after initiation of therapy in patients who have an activated renin-angiotensin system, such as volume- or salt-depleted patients (eg, those treated with diuretics). Correct this condition prior to administration or start treatment under close medical supervision with a reduced dose.

Renal effects

Treatment with angiotensin-receptor antagonists has been associated with oliguria and/or progressive azotemia, and (rarely) with acute renal failure and/or death in patients whose renal function depends on the activity of the renin-angiotensin-aldosterone system (eg, patients with CHF).

Overdosage

Symptoms

Bradycardia, dizziness, hypotension, peripheral vasodilation, tachycardia.

Patient Information

  • Inform women of childbearing age about the consequences of exposure to telmisartan/amlodipine during pregnancy. Discuss treatment options with women planning to become pregnant. Ask patients to report pregnancies to their health care provider as soon as possible.
  • Caution patients that light-headedness can occur, especially during the first few days of therapy, and to report it to the prescribing health care provider. Inform patients that, if syncope occurs, they should discontinue telmisartan/hydrochlorothiazide until the health care provider has been consulted.
  • Caution patients that inadequate fluid intake, excessive perspiration, diarrhea, or vomiting can lead to an excessive fall in BP, with the same consequences of light-headedness and possible syncope.
  • Advise patients not to use potassium supplements or salt substitutes containing potassium without consulting their health care provider.

Copyright © 2009 Wolters Kluwer Health.

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