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:

• Severe adverse reactions to olmesartan or any other formulation component, including
• Concomitant use of direct renin inhibitors - Aliskiren
• Pregnancy
• Breastfeeding

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: