Eprosartan

(ep roe sar' tan)

PCI  : Contraindicated in pregnancy

LCaution when used during lactation : Caution when used during lactation

Molecule Info

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WARNING

FETAL TOXICITY 

  • When pregnancy is detected, discontinue Eprosartan as soon as possible.
  • Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus.

Indication(s) & Dosage

Eprosartan is indicated for the treatment of essential hypertension.

The recommended dose is 600 mg eprosartan once daily.

Achievement of maximal blood pressure reduction in most patients may take 2 to 3 weeks of treatment.

Eprosartan may be used alone or in combination with other anti-hypertensives. In particular, addition of a thiazide-type diuretic such as hydrochlorothiazide or a calcium channel blocker such as sustained release nifedipine has been shown to have an additive effect with Eprosartan.

Eprosartan may be taken with or without food.

Geriatric patients

No dose adjustment is required in the elderly.

Dosage in Hepatically Impaired Patients:

There is limited experience in patients with hepatic insufficiency.

Dosage in Renally Impaired Patients:

In patients with moderate or severe renal impairment (creatinine clearance <60 ml/min), the daily dose should not exceed 600 mg.

Paediatric patients

Teveten is not recommended for use in children and adolescents due to lack of data on safety and efficacy.

Administration

May be taken with or without food.

Contraindications

  • Hypersensitivity to the active substance or to any of the excipients.
  • Second and third trimester of pregnancy.
  • Severe hepatic impairment.
  • Haemodynamically significant bilateral renovascular disease or severe stenosis of a solitary functioning kidney.

Special Precautions

Hepatic impairment

When Eprosartan is used in patients with mild to moderate hepatic impairment, special care should be exercised due to the fact that there is limited experience in this patient population

Renal impairment

No dose adjustment is required in patients with mild to moderate renal insufficiency (creatinine clearance ≥ 30 ml/min). Caution is recommended for use in patients with creatinine clearance < 30 ml/min or in patients undergoing dialysis

Patients at risk of renal impairment

Some patients whose renal function is dependent on the continued inherent activity of the renin-angiotensin-aldosterone system (e.g., patients with severe cardiac insufficiency [NYHA-classification: class IV], bilateral renal artery stenosis, or renal artery stenosis of a solitary kidney), have risks of developing oliguria and/or progressive azotaemia and rarely acute renal failure during therapy with an angiotensin converting enzyme (ACE) inhibitor. These events are more likely to occur in patients treated concomitantly with a diuretic. Angiotensin II receptor blockers such as eprosartan have not had adequate therapeutic experience to determine if there is a similar risk of developing renal function compromise in these susceptible patients. When eprosartan is to be used in patients with renal impairment, renal function should be assessed before starting treatment with eprosartan and at intervals during the course of therapy. If worsening of renal function is observed during therapy, treatment with eprosartan should be reassessed.

The following precautions have been included based on experience with other agents in this class and also ACE inhibitors:

Hypotension

Symptomatic hypotension may occur in patients with severe sodium depletion and/or volume depletion (e.g. high dose diuretic therapy). These conditions should be corrected before commencing therapy.

Coronary Heart Disease

There is limited experience in patients with coronary heart disease at this time.

Aortic and Mitral Valve Stenosis / Hypertrophic Cardiomyopathy.

As with all vasodilators, eprosartan should be used with caution in patients with aortic and mitral valve stenosis or hypertrophic cardiomyopathy.

Primary hyperaldosteronism

Patients with primary hyperaldosteronism are not recommended to be treated with eprosartan.

Renal Transplantation

There is no experience in patients with recent kidney transplantation.

Hyperkalaemia

During treatment with other medicinal products which affect the renin-angiotensin-aldosterone system hyperkalaemia may occur, especially in the presence of renal impairment and/or heart failure. Adequate monitoring of serum potassium in patients at risk is recommended.

Based on experience with the use of other medicinal products which affect the renin-angiotensinaldosterone system, concomitant use of potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium or other medicinal products which may increase the potassium level (e.g. heparin) may lead to an increase in serum potassium and should therefore be co-administered cautiously with Teveten.

Pregnancy

Eprosartan should not be initiated during pregnancy. Unless continued Eprosartan therapy is considered essential, patients planning pregnancy should be changed to alternative anti-hypertensive treatments which have an established safety profile for use in pregnancy. When pregnancy is diagnosed, treatment with Eprosartan should be stopped immediately, and, if appropriate, alternative therapy should be started.

Other warnings and precautions

As observed for angiotensin converting enzyme inhibitors, eprosartan and the other angiotensin antagonists are apparently less effective in lowering blood pressure in black people than in non-blacks, possibly because of higher prevalence of low-renin states in the black hypertensive population.

Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take Eprosartan.

Adverse Drug Reaction(s)

Fatigue, depression, hypertriglyceridaemia, abdominal pain, flatulence, urinary tract infection, upper resp tract infection, rhinitis, pharyngitis, cough, viral infection, injury, angina, asthma, arthritis, ataxia, increased BUN, increased creatinine, eczema, oedema, esophagitis, gingivitis, gout, influenza-like symptoms, leg cramps, migraine, somnolence, tendonitis, tinnitus, tremor, urinary incontinence, leukopaenia, maculopapular rash, neuritis, neutropaenia, paraesthesia, peripheral ischaemia, purpura, renal calculus, thrombocytopaenia, vertigo.

Drug Interactions

No effect on the pharmacokinetics of digoxin and the pharmacodynamics of warfarin or glyburide (glibenclamide) has been shown with eprosartan. Similarly no effect on eprosartan pharmacokinetics has been shown with ranitidine, ketoconazole or fluconazole.

Eprosartan can be used concomitantly with thiazide diuretics (e.g. hydrochlorothiazide) and calcium channel blockers (e.g. sustained-release nifedipine) without evidence of clinically significant adverse interactions.

Since in placebo-controlled clinical studies significantly elevated serum potassium concentration were observed, and based on experience with the use of other drugs that affect the renin-angiotensinaldosterone system, concomitant use of K-sparing diuretics, K-supplements, salt substitutes containing potassium or other drugs that may increase serum potassium levels (e.g. heparin) may lead to increase in serum potassium.

The antihypertensive effect may be potentiated by other antihypertensives.

Toxicity and areversible increase in serum lithium concentrations have been reported during concomitant administration of lithium with ACE inhibitors. The possibility of a similar effect cannot be excluded and careful monitoring of serum lithium levels is recommended during concomitant use.

Eprosartan has been shown not to inhibit human cytochrome P450 enzymes CYP1A, 2A6, 2C9/8, 2C19, 2D6, 2E and 3A in vitro.

As with ACE inhibitors, concomitant use of Angiotensin II antagonists and NSAIDs may lead to an increased risk of worsening of renal function, including possible acute renal failure, and an increase in serum potassium, especially in patients with poor pre-existing renal function. The combination should be administered with caution, especially in the elderly. Patients should be adequately hydrated and consideration should be given to monitoring renal function after initiation of concomitant therapy, and periodically thereafter. Concomitant use of losartan with the NSAID indometacin led to a decrease in efficacy of the angiotensin II antagonist; a class effect can not be excluded.

Food Interaction

Garlic may increase antihypertensive effect.

Pregnancy Category (FDA)

Pregnancy

Pregnancy Category D. The use of Eprosartan is not recommended during the first trimester of pregnancy and is contraindicated during second and third trimester of pregnancy.

Epidemiological evidence regarding the risk of teratogenicity following exposure to ACE inhibitors during the first trimester of pregnancy has not been conclusive; however, a small increase in risk cannot be excluded. Whilst there is no controlled epidemiological data on the risk with angiotensin II receptor blockers, similar risks may exist for this class of drugs. Unless continued Eprosartan therapy is considered essential, patients planning pregnancy should be changed to alternative anti-hypertensive treatments which have an established safety profile for use in pregnancy. When pregnancy is diagnosed, treatment with Eprosartan should be stopped immediately and, if appropriate, alternative therapy should be started.

Exposure to Eprosartan therapy during the second and third trimesters is known to induce human foetotoxicity (decreased renal function, oligohydramnios, skull ossification retardation) and neonatal toxicity (renal failure, hypotension, hyperkalaemia).

Should exposure to Eprosartan have occurred from the second trimester of pregnancy, ultrasound check of renal function and skull is recommended.

Infants whose mothers have taken Eprosartan should be closely observed for hypotension.

Lactation

Because no information is available regarding the use of Eprosartan during breast-feeding, Eprosartan is not recommended and alternative treatments with better established safety profiles during breast-feeding are preferable, especially while nursing a newborn or preterm infant.

Pharmacology

Pharmacodynamics:

Eprosartan is a potent, synthetic, orally active non-biphenyl non-tetrazole angiotensin II receptor antagonist, which binds selectively to the AT1 receptor. Angiotensin II is a potent vasoconstrictor and the primary active hormone of the renin-angiotensin-aldosterone system, playing a major part in the pathophysiology of hypertension. Angiotensin II binds to the AT1 receptor in many tissues (e.g. smooth vascular musculature, suprarenals, kidney, heart) and produces important biological effects such as vasoconstriction, sodium retention and release of aldosterone. More recently, angiotensin II has been implicated in the genesis of cardiac and vascular hypertrophy through its effect on cardiac and smooth muscle cell growth.

Eprosartan antagonised the effect of angiotensin II on blood pressure, renal blood flow and aldosterone secretion in normal volunteers. In hypertensive patients, comparable blood pressure control is achieved when eprosartan is administered as a single dose or in two divided doses. In placebo-controlled studies, in 299 patients treated receiving 600-800 mg once daily, there was no evidence of first dose postural hypotension. Discontinuation of treatment with eprosartan does not lead to a rapid rebound increase in blood pressure.

Eprosartan was evaluated in mild to moderate hypertensive patients (sitting DBP ≥95 mmHg and <115 mmHg) and severe hypertensive patients (sitting DBP ≥115 mmHg and ≤125 mmHg).

A dose of 1200 mg once daily, for 8 weeks, has been shown in 72 patients in clinical trials to be effective. In placebo-controlled studies using doses up to 1200 mg once daily, there is no apparent dose relationship in the incidence of adverse experiences reported.

In patients with hypertension, blood pressure reduction did not produce a change in heart rate.

In hypertensive patients eprosartan does not affect fasting triglycerides, total cholesterol, or LDL (low density lipoprotein) cholesterol levels. In addition, eprosartan has no effect on fasting blood sugar levels.

Eprosartan does not compromise renal autoregulatory mechanisms. In normal adult males eprosartan has been shown to increase mean effective renal plasma flow. Effective renal plasma flow is not altered in patients with essential hypertension and patients with renal insufficiency treated with eprosartan. Eprosartan does not reduce glomerular filtration rate in normal males, in patients with hypertension or in patients with varying degrees of renal insufficiency. Eprosartan has a natriuretic effect in normal subjects on a salt restricted diet.

Eprosartan does not significantly affect the excretion of urinary uric acid.

Pharmacokinetics:

Eprosartan does not potentiate effects relating to bradykinin (ACE-mediated), e.g. cough. In a study specifically designed to compare the incidence of cough in patients treated with eprosartan and an angiotensin converting enzyme inhibitor, the incidence of dry persistent cough in patients treated with eprosartan (1.5%) was significantly lower (p<0.05) than that observed in patients treated with an angiotensin converting enzyme inhibitor (5.4%). In a further study investigating the incidence of cough in patients who had previously coughed while taking an angiotensin converting enzyme inhibitor, the incidence of dry, persistent cough was 2.6% on eprosartan, 2.7% on placebo, and 25.0% on an angiotensin converting enzyme inhibitor (p<0.01, eprosartan versus angiotensin converting enzyme inhibitor).

Absolute bioavailability following a single 300 mg oral dose of eprosartan is about 13%, due to limited oral absorption. Eprosartan plasma concentrations peak at one to two hours after an oral dose in the fasted state. Plasma concentrations are dose proportional from 100 to 200 mg, but less than proportional for 400 and 800 mg doses. The terminal elimination half-life of eprosartan following oral administration is typically five to nine hours. A slight accumulation (14%) is seen with chronic use of eprosartan. Administration of eprosartan with food delays absorption with minor increases (<25%) observed in Cmax and AUC.

Plasma protein binding of eprosartan is high (approximately 98%) and constant over the concentration range achieved with therapeutic doses. The extent of plasma protein binding is not influenced by gender, age, hepatic dysfunction or mild-moderate renal impairment but has shown to be decreased in a small number of patients with severe renal impairment.

Following oral and intravenous dosing with [14C] eprosartan in human subjects, eprosartan was the only drug-related compound found in the plasma and faeces. In the urine, approximately 20% of the radioactivity excreted was an acyl glucuronide of eprosartan with the remaining 80% being unchanged eprosartan.

The volume of distribution of eprosartan is about 13 litres. Total plasma clearance is about 130 ml/min. Biliary and renal excretion contribute to the elimination of eprosartan. Following intravenous [14C] eprosartan, about 61% of radioactivity is recovered in the faeces and about 37% in the urine. Following an oral dose of [14C] eprosartan, about 90% of radioactivity is recovered in the faeces and about 7% in the urine.

Both AUC and Cmax values of eprosartan are increased in the elderly (on average, approximately two-fold).

Following administration of a single 100 mg dose of eprosartan, AUC values of eprosartan (but not Cmax) are increased, on average, by approximately 40% in patients with hepatic impairment. Since an intravenous dose of eprosartan was not administered to patients with hepatic impairment, the plasma clearance of eprosartan could not be measured.

Compared to subjects with normal renal function (n=7), mean AUC and Cmax values were approximately 30% higher in patients with creatinine clearance 30-59 ml/min (n=11) and approximately 50% higher in patients with creatinine clearance 5-29 ml/min (n=3).

In a separate investigation, mean AUC was approximately 60% higher in patients undergoing dialysis (n=9) compared to subjects with normal renal function (n=10).

There is no difference in the pharmacokinetics of eprosartan between males and females.

ATC Classification

C09CA02 - eprosartan; Belongs to the class of angiotensin II antagonists.  Used in the treatment of cardiovascular disease.

 

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IMPORTANT WARNING:

Tell your doctor if you are pregnant or plan to become pregnant.  Do not take eprosartan if you are pregnant.  If you become pregnant while you are taking eprosartan, stop taking eprosartan and Consult your doctor immediately.  Eprosartan may cause death or serious injury to the fetus when taken in the last 6 months of pregnancy.

 

Why Eprosartan is prescribed?

Eprosartan is used alone or in combination with other medications to treat high blood pressure.  Eprosartan is in a class of medications called angiotensin II receptor antagonists.  It works by blocking the action of certain natural substances that tighten the blood vessels, allowing the blood to flow more smoothly and the heart to pump more efficiently.

How should Eprosartan be used?

Eprosartan comes as a tablet to take by mouth.  It is usually taken once or twice a day with or without food.  To help you remember to take eprosartan, take it at around the same time every day.  Follow the directions on your prescription label carefully, and ask your Doctor to explain any part you do not understand.  Take eprosartan exactly as directed.  Do not take more or less of it or take it more often than prescribed by your doctor.

Eprosartan controls high blood pressure but does not cure it.  Your blood pressure may decrease during the first 2 weeks of your treatment, but it may take 2 to 3 weeks for you to notice the full benefit of eprosartan. Continue to take eprosartan even if you feel well.  Do not stop taking eprosartan without talking to your doctor. 

Other uses for Eprosartan 

Eprosartan is also used sometimes to treat congestive heart failure and diabetic nephropathy.  Talk to your doctor about the possible risks of using this medication for your condition.

This medication may be prescribed for other uses; ask your Doctor for more information.

What special precautions to follow?

Before taking eprosartan,

  • tell your Doctor if you are allergic to eprosartan, any other medications, or any of the ingredients in eprosartan tablets.  Ask your Doctor for a list of the ingredients.
  • tell your doctor if you have diabetes and you are taking aliskiren.  Your doctor will probably tell you not to take eprosartan if you have diabetes and you are also taking aliskiren.
  • tell your Doctor what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.  Be sure to mention the following: aspirin and other nonsteroidal anti-inflammatory medications such as ibuprofen and naproxen and selective COX-2 inhibitors such as celecoxib; diuretics; and potassium supplements.  Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had heart failure or kidney disease.
  • tell your doctor if you are breast-feeding.
  • you should know that eprosartan may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position.  This is more common when you first start taking eprosartan.  To help avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.
  • you should know that diarrhea, vomiting, not drinking enough fluids, and sweating a lot can cause a drop in blood pressure, which may cause lightheadedness and fainting.  Tell your doctor if you have any of these problems or develop them during your treatment.

What special dietary instructions to follow?

Do not use salt substitutes containing potassium without talking to your doctor.  If your doctor prescribes a low-salt or low-sodium diet, follow these directions carefully.

What to do if I forget a dose?

Take the missed dose as soon as you remember it.  However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule.  Do not take a double dose to make up for a missed one.

What side effects can this medication cause?

Eprosartan may cause side effects.  Tell your doctor if any of these symptoms are severe or do not go away: 

  • excessive tiredness
  • stomach pain
  • joint pain
  • swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
  • hoarseness
  • difficulty breathing or swallowing

Some side effects can be serious.  If you experience any of these symptoms, or those listed in the SPECIAL PRECAUTIONS section, consult your doctor immediately:

Eprosartan may cause other side effects.  Consult your doctor if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your doctor may send a report to the Office of Directorate General, Drugs Administration.

What storage conditions are needed for Eprosartan? 

Keep this medication in the container it came in, tightly closed, and out of reach of children.  Store it at room temperature and away from excess heat and moisture.  Throw away any medication that is outdated or no longer needed.  Talk to your Doctor about the proper disposal of your medication.

In case of emergency/overdose

In case of overdose, consult your Doctor.  If the victim has collapsed or is not breathing, consult local medical emergency services. 

What other information to know? 

Keep all appointments with your doctor and the laboratory. Your blood pressure should be checked regularly to determine your response to eprosartan.

Do not let anyone else take your medication.  

It is important for you to keep a written list of all of the prescription and nonprescription medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital.  It is also important information to carry with you in case of emergencies. 

Ref: U.S. Natl. Library of Medicine

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