Olmesartan medoxomil (Benicar) - Drug Information

Olmesartan medoxomil is a selective and competitive reversible Angiotensin receptor blocker. It inhibits angiotensin receptors and has little effect on the angiotensin-converting enzyme. It is used to treat the following conditions:

  • Especially in patients with high-risk atherosclerotic cardiovascular disease, for the treatment of hypertension as a monotherapy or in combination with other drugs.

  • Off Label Uses of Olmesartan include:

    • In patients with acute coronary syndrome as a secondary prevention of cardiovascular events.

    • Patients with stable coronary artery Disease

Olmesartan Dose in Adults

Dose in the treatment of Hypertension in adults:

  • 20 mg orally once a day.
  • The dose should be titrated up to 40 mg once a day after 2 weeks.

Olmesartan Dose in Children

Dose for the treatment of Hypertension:

  • Children 6 - 16 years:
    • 20 kg to less than 35 kg:

      • 10 mg once daily by mouth
      • After two weeks, if the first reaction is still insufficient, the dose may be increased to a maximum of 20 mg once daily.
    • More than 35 kg:

      • One daily oral dose of 20 mg.
      • After two weeks, if the first reaction is still insufficient, the dose may be increased to a maximum of 40 mg once daily.

Pregnancy Risk Factor D/ X

  • [US Boxed Warning]
    • Olmesartan, along with other medications that affect the RAAS, has the potential to harm or kill a growing foetus.
    • Once pregnancy has been identified, it needs to end right away.
    • Olmesartan is used during pregnancy and can penetrate the placental barrier. It may result in oligohydramnios, which may induce skeletal or foetal lung hypoplasia.
    • Furthermore, oligohydramnios might not show up until severe foetal harm has been done.
    • It can also lead to hypotension, anuria and skull hypoplasia in infants and neonates.
    • Hypertensive patients who are pregnant should avoid ARBs and ACE-Inhibitors.
    • Alternative therapies should be considered if necessary.

Olmesartan use during breastfeeding:

  • Breastmilk does not contain candesartan.
  • Manufacturers recommend that you stop using the drug, or breastfeed, after weighing the benefits and risks 

Olmesartan dose in patients with Kidney disease:

  • CrCl of more than 40 mL/minute:

    • Adjustment in the dose is not necessary.
  • CrCl of less  than 40 mL/minute:

    • Adjustment in the initial dose is not necessary.
    • Patients with a CrCl of less than 20 mL/minute have an AUC that is three times higher.
    • For these patients, a maximum dose of 20 mg/day has been suggested.

Olmesartan Dose in Liver Disease:

  • Mild hepatic impairment:

    • Adjustment in the dose is not necessary.
  • Moderate to severe hepatic impairment:

    • Initial dosage adjustment is not necessary.
    • In moderate hepatic impairment, the total drug exposure is increased by about 60%.

Common Side Effects of Olmesartan Include:

  • Central nervous system:

    • Dizziness
    • Headache
  • Endocrine & metabolic:

    • Hyperglycemia
    • Hypertriglyceridemia
  • Gastrointestinal:

    • Diarrhea
  • Genitourinary:

    • Hematuria
  • Neuromuscular & skeletal:

    • Back pain
    • Increased Creatine Phosphokinase
  • Respiratory:

    • Bronchitis
    • Flu-Like Symptoms
    • Pharyngitis
    • Rhinitis
    • Sinusitis

Rare side effects of olmesartan:

  • Hematologic & oncologic:

    • Decreased hematocrit
    • Decreased hemoglobin

Contraindication to Olmesartan medoxomil Include:

Warnings and Precautions

  • Angioedema
    • Angioedema can occur at any stage of treatment.
    • Patients who have angioedema that is associated with ACE inhibitors, idiopathic or hereditary may be at greater risk.
    • If patients experience swelling in the larynx, glottis or face, it is important to monitor them.
    • The drug should be stopped immediately and not restarted. Aggressive management of the airway and Intramuscular epinephrine should be part of the resuscitation.
  • Gastrointestinal effects:
    • Olmesartan-treated patients may experience severe, persistent diarrhea and significant weight loss.
    • It is possible for symptoms to develop over several years. Intestinal biopsy may be necessary in order to detect villous atrophy.
    • Patients should be referred to antihypertensive medication alternatives once all other causes are ruled out.
    • There has been an improvement in symptoms and biopsies after stopping the drug.
  • Hyperkalemia:
    • Hyperkalemia is a risk for the following:
      • Patients with impaired renal function
      • Diabetes mellitus
      • Use potassium-sparing diuretics in conjunction
      • Patients ingesting potassium supplements or sodium 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 suffering from low renal blood flow (e.g. Acute renal impairment may occur in patients with heart disease and renal artery narrowing.
    • If there is a marked decline in renal function, therapy should be stopped.
  • Mitral and aortic stenosis:
    • Patients with significant mitral or aortic valve stenosis or aortic stenosis need to be cautious about taking the drug.
  • Ascites:
    • Patients with cirrhosis should not be given olmesartan.
    • Rapid deterioration of renal function can occur after treatment.
  • Renal artery stenosis
    • Patients with bilateral renal arterial stenosis should not be used.
    • Patients with unilateral renal arterial stenosis may need to be cautious.

Monitoring Parameters:

  • Blood pressure
  • Serum electrolytes
  • BUN and serum creatinine
  • Urinalysis

The dose should be adjusted to achieve the target blood pressure of:

  • Hypertensive patients with known heart disease, or those at greater risk for ASCVD in the next 10 years will have blood pressures of less than 130/80 mmHg
  • In hypertensive patients, a lower than 130/80mmHg is possible without ASCVD risk markers.

Blood Pressure Targets in Diabetes patients (ADA 2018 recommendations):

  • Patients with co-morbid hypertension and diabetes, and patients who are less than 65 years old, have less than 140/90
  • Patients less than 65 years old with diabetes or at high risk for cardiovascular disease have a lower rate of 130/80.
  • Patients over 65 years old with Diabetes have a lower blood pressure of less than 140/90 mmHg.
  • Patients over 65 years old with Diabetes or poor health have a lower reading of 150/90 mmHg.

How to take Olmesartan?

  • It may be administered orally with or without food.

Mechanism of action of Olmesartan:

  • Olmesartan is a selective and aggressive nonpeptide Angiotensin II receptor inhibitor. It prevents angiotensin II's vasoconstrictor and aldosterone-secreting actions.
  • It responds reversibly with Angiotensin I and Angiotensin II receptors in numerous organs.
  • It has a 12,500x higher affinity for angiotensin I receptors than angiotensin II does.
  • The RAAS is more inhibited by angiotensin II receptor blockade than by ACE medications.
  • Since they don't interfere with the bradykinin systems, they are less likely to result in angioedema or coughing.
  • Olmesartan can increase the rate of urinary flow. It can cause natriuresis and kaliuresis.
  • It also increases the excretion of calcium, magnesium, uric acids, calcium, as well as phosphate.

It doesn't cross the blood-brain boundary and is 99 percent safe protein-bound.It is then hydrolyzed in your gastrointestinal tract to make the active compound. It has been abioavailability26% with a 13-hour half-life. When plasma concentration reaches its peakIt takes between 1 and 2 hours. 50% of the drug isexcretedIn the feces, as an unchanged drug, while 35-45% isexcretedIn the urine.

International Brands of Olmesartan:

  • Abetis
  • Almetec
  • Alteis
  • Alzor
  • Angiosartan
  • Ao Tan
  • Arb-S
  • Belsar
  • Benetor
  • Benicar
  • Cardioplus
  • Cresart
  • Dolezine
  • Erastapex
  • Esatec
  • Eukene
  • Ixia
  • Kaportan
  • Lezberg
  • Macolme
  • Mesar
  • Normesar
  • Olartan
  • Oldesar
  • Olesta
  • Olimestra
  • Olme
  • Olmec
  • Olmecor
  • Olmepas
  • Olmes
  • Olmesan
  • Olmesta
  • Olmetec
  • Olmetel
  • Olmezar
  • Olsart
  • Omecor
  • Openvas
  • Orion
  • Osaver
  • Presulock
  • Tenzar
  • Vivactra
  • Votum

Olmesartan Brands in Pakistan:

Olmesartan Medoxomil [Tabs 5 Mg]

Bensar Pharmevo (Pvt) Ltd.
Negatin Wilsons Pharmaceuticals
Oscord Hilton Pharma (Pvt) Limited

Olmesartan Medoxomil [Tabs 10 Mg]

Malisartan Alied Medical
Omsana Hilton Pharma (Pvt) Limited
Orion Ferozsons Laboratoies Ltd.
Oscord Hilton Pharma (Pvt) Limited

Olmesartan Medoxomil [Tabs 20 Mg]

Baritec Barrett Hodgson Pakistan (Pvt) Ltd.
Bensar Pharmevo (Pvt) Ltd.
Malisartan Alied Medical
Negatin Wilsons Pharmaceuticals
Olesta Searle Pakistan (Pvt.) Ltd.
Olmicar Rasco Pharma
Olmipress Remington Pharmaceutical Industries (Pvt) Ltd.
Omsana Hilton Pharma (Pvt) Limited
Orion Ferozsons Laboratoies Ltd.
Oscord Hilton Pharma (Pvt) Limited

Olmesartan Medoxomil [Tabs 40 Mg]

Baritec Barrett Hodgson Pakistan (Pvt) Ltd.
Bensar Pharmevo (Pvt) Ltd.
Bensar Pharmevo (Pvt) Ltd.
Malisartan Allied Medical
Negatin Wilsons Pharmaceuticals
Negatin Wilsons Pharmaceuticals
Olesta Searle Pakistan (Pvt.) Ltd.
Olmicar Rasco Pharma
Olmipress Remington Pharmaceutical Industries (Pvt) Ltd.
Omsana Hilton Pharma (Pvt) Limited
Orion Ferozsons Laboratoies Ltd.
Oscord Hilton Pharma (Pvt) Limited