Eprosartan (Teveten) - Uses, Dose, Side effects, MOA, Brands

Eprosartan (Teveten) is an angiotensin-converting-enzyme inhibitor that is used as monotherapy or in combination with other antihypertensive medications to reduce the blood pressure in hypertensive patients.

Eprosartan Uses:

  • Hypertension:

    • It is used for treating hypertension
  • Off Label Use of Eprosartan in Adults:

    • Acute coronary syndrome for secondary prevention
    • Stable coronary artery disease

Eprosartan (Teveten) Dose in Adults

Eprosartan (Teveten) Dose in the treatment of Hypertension:

Note: For initial treatment:

    • ≥20/10 mm Hg above goal, may be used in conjunction with other medicines in combination treatment (eg, a long-acting dihydropyridine calcium channel blocker or thiazide diuretic).
    • <20/10 mm Hg above the target, however many people eventually require combo medications.
  • Oral:
    • Initial: 600 mg once a day
    • Every 4 to 6 weeks, assess response and modify dosage.
    • One or two divided dosages of up to 800 mg/day may be administered.

Dose in Children:

Not indicated.

Pregnancy Risk Factor D

  • [Warning for US Boxes] Drugs that interfere with the renin-angiotensin system can damage or even kill a developing foetus.
  • It's crucial to stop taking the medication as soon as you find out you're pregnant.
  • Drugs that affect the RAAS system have the potential to cause oligohydramnios, which can result in skeletal or foetal lung abnormalities or hypoplasia.
  • Exchange transfusions may be required for infants who are exposed in utero. The second and third trimesters are when most complications occur in neonates.
  • Monitoring the exposed fetus for growth, amniotic fluid volume and formation of organs is important.
  • These complications are caused by maternal use during the second and third trimesters.

Eprosartan use during breastfeeding:

  • It is unknown if breast milk contains eprosartan.
  • The benefits of valsartan for the mother and the benefits of breastfeeding the infant should be considered by the clinician.

Eprosartan (Teveten) Dose in Kidney disease:

  • Mild impairment:

    • No dose adjustment required.
  • Moderate to severe impairment:

    • The manufacturer has not recommended any dosage adjustment in severe renal disease
    • maximum dose: 600 mg daily.
  • Hemodialysis:

    • The manufacturer has not recommended any dosage adjustment in severe renal disease; eprosartan is poorly removed by hemodialysis (Cl <1 L/hour)

Dose in Liver disease:

No dosage adjustment required.

Less Common Side Effects of Eprosartan (Teveten):

  • Cardiovascular:

    • Chest Pain
  • Central Nervous System:

    • Fatigue
    • Dizziness
    • Headache
    • Depression
  • Endocrine & Metabolic:

    • Dependent Edema
    • Hypertriglyceridemia
  • Gastrointestinal:

    • Abdominal Pain
    • Diarrhea
    • Dyspepsia
  • Genitourinary:

    • Urinary Tract Infection
  • Infection:

    • Viral Infection
  • Neuromuscular & Skeletal:

    • Arthralgia
    • Myalgia
  • Renal:

    • Increased Blood Urea Nitrogen
  • Respiratory:

    • Upper Respiratory Tract Infection
    • Pharyngitis
    • Rhinitis
    • Cough
    • Bronchitis
    • Sinusitis
  • Miscellaneous:

    • Accidental Injury

Contraindications to Eprosartan (Teveten):

  • Hypersensitivity
  • Use of a direct renin inhibitor in conjunction

Because of the similarities in structure/function, it is impossible to rule out the possibility of cross-sensitivity between angiotensin receptor blockers and angiotensin 2, but this cannot be excluded.

Canadian labeling: Additional contraindications not in US labeling

  • Renovascular disease on both sides, or severe stenosis in one functioning kidney
  • Galactose intolerance or glucose-galactose malabsorption, also known as Lapp lactase deficiencies, or Galactose intolerance
  • Combination use of aliskiren for severe renal impairment (GFR 60mL/minute/1.73m2)
  • Combination with ACEi for patients with diabetic nephropathy
  • Pregnancy
  • Breastfeeding

Warnings and precautions

  • Angioedema

    • Angioedema can occur (rarely) during any treatment.
    • Patients who have angioedema that is associated with ACE inhibitors, idiopathic or hereditary may be at greater risk.
    • It is possible to have abdominal pain due to involvement of the head, neck, or intestine.
    • If patients experience swelling in the larynx, glottis or face, it is important to monitor them.
    • If angioedema develops, stop taking medication immediately. Do not restart therapy for future uses
    • It is important to treat the patient immediately and aggressively. Intramuscular (IM), administration of epinephrine might be necessary.
  • Hyperkalemia:

    • Hyperkalemia is a more common risk. Risk factors include:
      • Renal dysfunction
      • DM
      • Concomitant use ACEi, aliskiren and potassium-sparing uriters
      • Potassium supplementation, potassium-containing Salts
  • Hypotension

    • Hypotension is a risk factor for patients who are salt- and volume-depleted (e.g. Patients taking high-dose diuretics. The patient must be well hydrated before initiating treatment.
  • Renal function deterioration:

    • Patients with decreased renal blood flow, such as Patients with renal artery stenosis and heart disease may experience acute renal impairment.
    • Small increases in serum creatinine may occur once treatment begins; however, stopping treatment will cause a severe or gradual decline in renal function.
  • Aortic/mitral stenosis:

    • Patients with severe aortic/mitralstenosis should be cautious.
  • Ascites:

    • Patients with cirrhosis should not use it as there is a risk of rapid decline in renal function.
  • Renal artery stenosis

    • It should not be used by individuals who have unilateral or bilateral renal arterial stenosis.
    • High risk of renal dysfunction deterioration
  • Renal impairment

    • Prevent severe renal impairment and renal insufficiency.

Eprosartan: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy)

Alfuzosin The hypotensive effects of blood pressure-lowering medications may be strengthened.
Amphetamines May lessen the effectiveness of antihypertensive agents.
Angiotensin II The therapeutic benefit of angiotensin II may be reduced by receptor blockers.
Antipsychotic Agents (Second Generation [Atypical]) Antipsychotic drugs' hypotensive effects may be enhanced by blood pressure-lowering medications (Second Generation [Atypical]).
Barbiturates The hypotensive effects of blood pressure-lowering medications may be strengthened.
Benperidol The hypotensive effects of blood pressure-lowering medications may be strengthened.
Brigatinib May lessen the effectiveness of antihypertensive agents. Antihypertensive Agents' bradycardic action may be strengthened by brutinib.
Brimonidine (Topical) The hypotensive effects of blood pressure-lowering medications may be strengthened.
CycloSPORINE (Systemic) CycloSPORINE's hyperkalemic impact may be enhanced by angiotensin II receptor blockers (Systemic).
Dapoxetine Angiotensin II Receptor Blockers' orthostatic hypotensive action might be improved.
Dexmethylphenidate May lessen the effectiveness of antihypertensive agents.
Diazoxide The hypotensive effects of blood pressure-lowering medications may be strengthened.
Drospirenone Drospirenone's hyperkalemic impact may be enhanced by angiotensin II receptor blockers.
DULoxetine Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine.
Eplerenone Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened.
Heparin Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened.
Heparins (Low Molecular Weight) Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened.
Herbs (Hypertensive Properties) May lessen the effectiveness of antihypertensive agents.
Herbs (Hypotensive Properties) The hypotensive effects of blood pressure-lowering medications may be strengthened.
Hypotension-Associated Agents The hypotensive action of hypotension-associated agents may be strengthened by blood pressure lowering medications.
Levodopa-Containing Products Levodopa-Containing Products' hypotensive effects may be strengthened by blood pressure-lowering medications.
Lormetazepam The hypotensive effects of blood pressure-lowering medications may be strengthened.
Methylphenidate May lessen the effectiveness of antihypertensive agents.
Molsidomine The hypotensive effects of blood pressure-lowering medications may be strengthened.
Naftopidil The hypotensive effects of blood pressure-lowering medications may be strengthened.
Nicergoline The hypotensive effects of blood pressure-lowering medications may be strengthened.
Nicorandil Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened.
Nicorandil The hypotensive effects of blood pressure-lowering medications may be strengthened.
Nitroprusside Nitroprusside's hypotensive impact may be strengthened by blood pressure-lowering medications.
Nonsteroidal Anti-Inflammatory Agents Nonsteroidal Anti-Inflammatory Agents' negative/toxic effects may be amplified by angiotensin II receptor blockers. In particular, the combination may cause a marked decline in renal function. Angiotensin II Receptor Blockers' therapeutic impact may be lessened by non-steroidal anti-inflammatory drugs. Both glomerular filtration rate and renal function may be considerably reduced by the combination of these two drugs.
Pentoxifylline The hypotensive effects of blood pressure-lowering medications may be strengthened.
Pholcodine Pholcodine's hypotensive impact may be strengthened by blood pressure lowering medications.
Phosphodiesterase 5 Inhibitors The hypotensive effects of blood pressure-lowering medications may be strengthened.
Potassium Salts Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened.
Potassium-Sparing Diuretics Potassium-Sparing Diuretics may have a stronger hyperkalemic impact when used with Angiotensin II Receptor Blockers.
Prostacyclin Analogues The hypotensive effects of blood pressure-lowering medications may be strengthened.
Quinagolide The hypotensive effects of blood pressure-lowering medications may be strengthened.
Ranolazine Angiotensin II Receptor Blockers' hazardous or harmful effects might be exacerbated.
Tacrolimus (Systemic) Tacrolimus's hyperkalemic impact may be enhanced by angiotensin II receptor blockers (Systemic).
Tolvaptan Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened.
Trimethoprim Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened.
Yohimbine May lessen the effectiveness of antihypertensive agents.

Risk Factor D (Consider therapy modification)

Aliskiren Angiotensin II Receptor Blockers' hyperkalemic impact might be strengthened. The hypotensive effects of angiotensin II receptor blockers may be strengthened by aliskiren. Angiotensin II Receptor Blockers' nephrotoxic effects may be made worse by aliskiren. Treatment: It is not advised for diabetic patients to take aliskiren along with ACEIs or ARBs. Combination therapy should be avoided in other patients, especially when CrCl is less than 60 mL/min. If combined, keep a close eye on your blood pressure, potassium, and creatinine levels.
Amifostine Amifostine's hypotensive impact may be strengthened by blood pressure lowering medications. Treatment: Blood pressure-lowering drugs need to be avoided for 24 hours before amifostine is administered when used at chemotherapeutic doses. Amifostine should not be given if blood pressure lowering treatment cannot be stopped.
Angiotensin-Converting Enzyme Inhibitors Angiotensin II Receptor Blockers may make angiotensin-converting enzyme inhibitors more harmful or toxic. Angiotensin-Converting Enzyme Inhibitors' serum levels may rise in response to angiotensin II receptor blockers. Management: According to US labelling, it is not advisable to take telmisartan and ramipril. It is unclear whether another ACE inhibitor and ARB combo would be any safer. When possible, take into account alternatives to the mix.
Lithium It's possible that angiotensin II receptor blockers will raise the level of lithium in the blood. Management: After adding an angiotensin II receptor antagonist, it will probably be necessary to lower the dosage of lithium.
Obinutuzumab The hypotensive effects of blood pressure-lowering medications may be strengthened. Management: Take into account temporarily stopping blood pressure-lowering drugs starting 12 hours before the start of the obinutuzumab infusion and lasting until 1 hour after it.
Sodium Phosphates Angiotensin II Receptor Blockers may make sodium phosphates more nephrotoxic. In particular, there may be an increased risk of acute phosphate nephropathy. Treatment: You might want to temporarily stop taking ARBs or look into alternatives to the oral sodium phosphate bowel preparation in order to prevent this combo. Maintaining appropriate hydration and properly monitoring renal function should be done if the combination cannot be avoided.

Risk Factor X (Avoid combination)

Bromperidol May lessen blood pressure lowering agents' hypotensive effects. The hypotensive impact of bromperidol may be enhanced by blood pressure lowering medications.

Monitoring parameters:

  • Blood pressure
  • serum potassium
  • serum creatinine
  • BUN
  • eGFR 

Hypertension: The 2017 guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults.

  • Less than 130/80 mmHg in hypertensive patients with known cardiovascular disease or a 10-year ASCVD risk of more than 10%.
  • Less than 130/80 mmHg may be reasonable in hypertensive patients without markers of ASCVD risk.

Blood pressure targets in Diabetic patients: (ADA 2019):

  • Less than 140/90 in patients with co-morbid diabetes and hypertension and age less than 65 years

  • Less than 130/80 among diabetic patients under 65 who are also at high risk for cardiovascular disease.

  • Less than 140/90 mmHg in diabetic patients above the age of 65.

  • Less than 150/90 mmHg in patients with diabetes and a poor health status who are older than 65.

How to administer Eprosartan (Teveten)?

Oral: May be taken with or without food.

Mechanism of action of Eprosartan (Teveten):

  • Eprosartan is an inhibitor of angiotensin II. 
  • It preferentially prevents angiotensin II from binding to the AT1 receptor.

The following mechanisms can be used to lower blood pressure:

  • Vasodilation
  • Inhibition of aldosterone production
  • Catecholamine inhibition
  • Blocking the release arginine vasopressin
  • Hypertrophic and water intake can be inhibited.

ACEi blocks the biosynthesis angiotensin II (angiotensin 1) and causes bradykinin to be degraded. Eprosartan is not an inhibitor of ACE and does not alter the bradykinin response. It also has fewer side effect than ACEi.

Protein binding:

  • 98%

Metabolism:

  • Minimally hepatic

Bioavailability:

  • 300 mg dose: 13%

Half-life elimination:

  • Terminal: 5 - 9 hours

Time to peak, serum:

  • Fasting: 1 - 2 hours

Excretion: mainly through feces

  • Feces (90%)
  • Urine (7%, mostly as unchanged drug)

International Brand Names of Eprosartan:

  • Teveten
  • Cosarnomid
  • Epratenz
  • Futuran
  • Tangio
  • Tensrelive
  • Teveten
  • Tevetens
  • Tevetenz

Eprosartan Brand Names in Pakistan:

Eprosartan Tablets 400 mg in Pakistan

Level Wilsons Pharmaceuticals

 

Eprosartan Tablets 600 mg in Pakistan

Teveten Abbott Laboratories (Pakistan) Limited.