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Olmesartan

Pronunciation

Pronunciation

(ole me SAR tan)

Index Terms

  • Olmesartan Medoxomil

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as medoxomil:

Benicar: 5 mg, 20 mg, 40 mg

Brand Names: U.S.

  • Benicar

Pharmacologic Category

  • Angiotensin II Receptor Blocker
  • Antihypertensive

Pharmacology

As a selective and competitive, nonpeptide angiotensin II receptor antagonist, olmesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II; olmesartan interacts reversibly at the AT1 and AT2 receptors of many tissues and has slow dissociation kinetics; its affinity for the AT1 receptor is 12,500 times greater than the AT2 receptor. Angiotensin II receptor antagonists may induce a more complete inhibition of the renin-angiotensin system than ACE inhibitors, they do not affect the response to bradykinin, and are less likely to be associated with nonrenin-angiotensin effects (eg, cough and angioedema). Olmesartan increases urinary flow rate and, in addition to being natriuretic and kaliuretic, increases excretion of chloride, magnesium, uric acid, calcium, and phosphate.

Distribution

17 L; does not cross the blood-brain barrier (animal studies)

Metabolism

Olmesartan medoxomil is hydrolyzed in the GI tract to active olmesartan. No further metabolism occurs.

Excretion

All as unchanged drug: Feces (50% to 65%); urine (35% to 50%); Clearance: 1.3 L/hour; similar data reported in children (1 to 16 years) when adjusted by body weight

Time to Peak

1 to 2 hours

Half-Life Elimination

Terminal: 13 hours

Protein Binding

99%

Special Populations: Renal Function Impairment

AUC is approximately tripled when CrCl is less than 20 mL/min.

Special Populations: Hepatic Function Impairment

In patients with moderate hepatic impairment, AUC increased by approximately 60%; Cmax was also increased.

Special Populations: Elderly

AUC increased by 33%, and there is a 30% reduction in renal Cl.

Special Populations: Gender

AUC and Cmax increased 10% to 15% in women.

Special Populations: Race

Antihypertensive effect was smaller in black patients.

Use: Labeled Indications

Hypertension: Treatment of hypertension with or without concurrent use of other antihypertensive agents

Guideline recommendations:

Hypertension: The 2014 guideline for the management of high blood pressure in adults (Eighth Joint National Committee [JNC 8; James 2013]) recommends initiation of pharmacologic treatment to lower blood pressure for the following patients:

• Patients ≥60 years of age with systolic blood pressure (SBP) ≥150 mm Hg or diastolic blood pressure (DBP) ≥90 mm Hg. Goal of therapy is SBP <150 mm Hg and DBP <90 mm Hg.

• Patients <60 years of age with SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

• Patients ≥18 years of age with diabetes and SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

• Patients ≥18 years of age with chronic kidney disease (CKD) and SBP ≥140 mm Hg or DBP ≥90 mm Hg. Goal of therapy is SBP <140 mm Hg and DBP <90 mm Hg.

Chronic kidney disease (CKD) and hypertension: Regardless of race or diabetes status, the use of an ACE inhibitor (ACEI) or angiotensin receptor blocker (ARB) as initial therapy is recommended to improve kidney outcomes. In the general nonblack population (without CKD), including those with diabetes, initial antihypertensive treatment should consist of a thiazide-type diuretic, calcium channel blocker, ACEI, or ARB. In the general black population (without CKD), including those with diabetes, initial antihypertensive treatment should consist of a thiazide-type diuretic or a calcium channel blocker instead of an ACEI or ARB.

Coronary artery disease (CAD) and hypertension: The American Heart Association, American College of Cardiology, and American Society of Hypertension (AHA/ACC/ASH) 2015 scientific statement for the treatment of hypertension in patients with CAD recommends the use of an ARB (or ACE inhibitor) as part of a regimen in patients with hypertension and chronic stable angina if there is prior MI, LV systolic dysfunction, diabetes mellitus, or CKD. A BP target of <140/90 mm Hg is reasonable for the secondary prevention of cardiovascular events. A lower target BP (<130/80 mm Hg) may be appropriate in some individuals with CAD, previous MI, stroke or transient ischemic attack, or CAD risk equivalents (AHA/ACC/ASH [Rosendorff 2015]).

Contraindications

Concomitant use with aliskiren in patients with diabetes mellitus

Canadian labeling: Additional contraindications (not in U.S. labeling): Hypersensitivity to olmesartan or any component of the formulation; concomitant use with aliskiren in patients with moderate to severe renal impairment (GFR <60 mL/minute/1.73 m2)

Documentation of allergenic cross-reactivity for angiotensin II receptor blockers is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Dosing: Adult

Hypertension: Oral: Initial: 20 mg once daily; if initial response is inadequate, may be increased to 40 mg once daily after 2 weeks. Usual dosage range (ASH/ISH [Weber, 2014]): 20 to 40 mg daily. May administer with other antihypertensive agents if blood pressure inadequately controlled with olmesartan. Consider lower starting dose in patients with possible depletion of intravascular volume (eg, patients receiving diuretics).

Dosing: Geriatric

Hypertension: Oral: No initial dosage adjustment is necessary per labeling; however, may consider starting at 5 to 10 mg once daily (due to concomitant disease or age changes).

Dosing: Pediatric

Hypertension: Children 6 to 16 years: Oral:

20 kg to <35 kg: Initial: 10 mg once daily; if initial response inadequate after 2 weeks, dose may be increased (maximum: 20 mg once daily)

≥35 kg: Initial: 20 mg once daily; if initial response inadequate after 2 weeks, dose may be increased (maximum: 40 mg once daily)

Dosing: Renal Impairment

U.S. labeling: Initial: No dosage adjustment is necessary for patients with moderate to severe renal impairment (creatinine clearance <40 mL/minute). However, AUC increased 3-fold in patients with CrCl <20 mL/minute; use with caution.

Canadian labeling:

Mild to moderate impairment: Maximum dose: 20 mg once daily

Severe impairment: There are no dosage adjustments provided in the manufacturer’s labeling; use is not recommended.

Dosing: Hepatic Impairment

U.S. labeling: Initial: No dosage adjustment is necessary for patients with moderate to severe hepatic dysfunction. Total drug exposure increased 60% in patients with moderate impairment.

Canadian labeling:

Mild impairment: No dosage adjustment is necessary.

Moderate impairment: Initial: Lower starting dose is recommended (maximum: 20 mg once daily)

Severe impairment: There is no dosage adjustment provided in the manufacturer’s labeling; use is not recommended.

Extemporaneously Prepared

A 2 mg/mL oral suspension may be made with olmesartan tablets. Combine 50 mL purified water and twenty 20 mg tablets in an 8-ounce amber bottle and allow to stand for ≥5 minutes. Shake well for ≥1 minute, then allow to stand for ≥1 minute. Repeat shaking and standing process four additional times. Add 100 mL Ora-Sweet® and 50 mL Ora-Plus® to the suspension and shake well for ≥1 minute. Label "shake well" and "refrigerate". Stable for 28 days refrigerated.

Benicar® prescribing information, Daiichi Sankyo, Inc, Parsippany, NJ, 2010.

Administration

May be administered with or without food.

Dietary Considerations

May be taken with or without food.

Storage

Store at 20°C to 25°C (68°F to 77°F).

Drug Interactions

ACE Inhibitors: Angiotensin II Receptor Blockers may enhance the adverse/toxic effect of ACE Inhibitors. Angiotensin II Receptor Blockers may increase the serum concentration of ACE Inhibitors. Management: In US labeling, use of telmisartan and ramipril is not recommended. It is not clear if any other combination of an ACE inhibitor and an ARB would be any safer. Consider alternatives to the combination when possible. Consider therapy modification

Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Aliskiren: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Aliskiren may enhance the hypotensive effect of Angiotensin II Receptor Blockers. Aliskiren may enhance the nephrotoxic effect of Angiotensin II Receptor Blockers. Management: Aliskiren use with ACEIs or ARBs in patients with diabetes is contraindicated. Combined use in other patients should be avoided, particularly when CrCl is less than 60 mL/min. If combined, monitor potassium, creatinine, and blood pressure closely. Consider therapy modification

Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification

Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Monitor therapy

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Canagliflozin: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Canagliflozin may enhance the hypotensive effect of Angiotensin II Receptor Blockers. Monitor therapy

Ciprofloxacin (Systemic): Angiotensin II Receptor Blockers may enhance the arrhythmogenic effect of Ciprofloxacin (Systemic). Monitor therapy

Colesevelam: May decrease the serum concentration of Olmesartan. Management: Administer olmesartan at least 4 hours prior to colesevelam. Consider therapy modification

CycloSPORINE (Systemic): Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of CycloSPORINE (Systemic). Monitor therapy

Dapoxetine: May enhance the orthostatic hypotensive effect of Angiotensin II Receptor Blockers. Monitor therapy

Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Drospirenone: Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of Drospirenone. Monitor therapy

DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Monitor therapy

Eltrombopag: May increase the serum concentration of OATP1B1/SLCO1B1 Substrates. Monitor therapy

Eplerenone: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Monitor therapy

Gemfibrozil: May increase the serum concentration of OATP1B1/SLCO1B1 Substrates. See separate drug interaction monographs for agents listed as exceptions. Monitor therapy

Heparin: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Monitor therapy

Heparin (Low Molecular Weight): May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Monitor therapy

Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy

Levodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa. Monitor therapy

Lithium: Angiotensin II Receptor Blockers may increase the serum concentration of Lithium. Management: Lithium dosage reductions will likely be needed following the addition of an angiotensin II receptor antagonist. Consider therapy modification

Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicorandil: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Monitor therapy

Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: Angiotensin II Receptor Blockers may enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents. Specifically, the combination may result in a significant decrease in renal function. Nonsteroidal Anti-Inflammatory Agents may diminish the therapeutic effect of Angiotensin II Receptor Blockers. The combination of these two agents may also significantly decrease glomerular filtration and renal function. Monitor therapy

Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Consider therapy modification

Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Potassium Salts: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Monitor therapy

Potassium-Sparing Diuretics: Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Monitor therapy

Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Sodium Phosphates: Angiotensin II Receptor Blockers may enhance the nephrotoxic effect of Sodium Phosphates. Specifically, the risk of acute phosphate nephropathy may be enhanced. Management: Consider avoiding this combination by temporarily suspending treatment with ARBs, or seeking alternatives to oral sodium phosphate bowel preparation. If the combination cannot be avoided, maintain adequate hydration and monitor renal function closely. Consider therapy modification

Teriflunomide: May increase the serum concentration of OATP1B1/SLCO1B1 Substrates. Monitor therapy

Tolvaptan: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Monitor therapy

Trimethoprim: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Monitor therapy

Yohimbine: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Adverse Reactions

1% to 10%:

Central nervous system: Dizziness (3%), headache

Endocrine & metabolic: Hyperglycemia, hypertriglyceridemia

Gastrointestinal: Diarrhea

Neuromuscular & skeletal: Back pain, CPK increased

Renal: Hematuria

Respiratory: Bronchitis, pharyngitis, rhinitis, sinusitis

Miscellaneous: Flu-like syndrome

<1% (Limited to important or life-threatening): Acute renal failure, alopecia, anaphylaxis, angioedema, arthritis, gastroenteritis, hypercholesterolemia, hyperkalemia, hyperlipidemia, hyperuricemia, liver enzymes increased, peripheral edema, rhabdomyolysis, serum creatinine increased, sprue-like symptoms, tachycardia

ALERT: U.S. Boxed Warning

Fetal toxicity:

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

Warnings/Precautions

Concerns related to adverse effects:

• Angioedema: Angioedema has been reported rarely with some angiotensin II receptor antagonists (ARBs) and may occur at any time during treatment (especially following first dose). It may involve the head and neck (potentially compromising airway) or the intestine (presenting with abdominal pain). Patients with idiopathic or hereditary angioedema or previous angioedema associated with ACE-inhibitor therapy may be at an increased risk. Prolonged frequent monitoring may be required, especially if tongue, glottis, or larynx are involved, as they are associated with airway obstruction. Patients with a history of airway surgery may have a higher risk of airway obstruction. Discontinue therapy immediately if angioedema occurs. Aggressive early management is critical. Intramuscular (IM) administration of epinephrine may be necessary. Do not readminister to patients who have had angioedema with ARBs.

• Gastrointestinal effects: Symptoms of sprue-like enteropathy (ie, severe, chronic diarrhea with significant weight loss) has been reported; may develop months to years after treatment initiation with villous atrophy commonly found on intestinal biopsy. Once other etiologies have been excluded, discontinue treatment and consider other antihypertensive treatment. Clinical and histologic improvement was noted after treatment was discontinued in a case series of 22 patients (Ianiro, 2014; Rubio-Tapia, 2012).

• Hyperkalemia: May occur; risk factors include renal dysfunction, diabetes mellitus, concomitant use of potassium-sparing diuretics, potassium supplements and/or potassium containing salts. Use cautiously, if at all, with these agents and monitor potassium closely.

• Hypotension: Symptomatic hypotension may occur upon initiation in patients who are salt- or volume-depleted (eg, those treated with high-dose diuretics); correct volume depletion prior to administration. This transient hypotensive response is not a contraindication to further treatment with olmesartan.

• Renal function deterioration: May be associated with deterioration of renal function and/or increases in serum creatinine, particularly in patients with low renal blood flow (eg, renal artery stenosis, heart failure) whose glomerular filtration rate (GFR) is dependent on efferent arteriolar vasoconstriction by angiotensin II; deterioration may result in oliguria, acute renal failure, and progressive azotemia. Small increases in serum creatinine may occur following initiation; consider discontinuation only in patients with progressive and/or significant deterioration in renal function.

Disease-related concerns:

• Aortic/mitral stenosis: Use caution in patients with significant aortic/mitral stenosis.

• Renal artery stenosis: Use olmesartan with caution in patients with unstented unilateral/bilateral renal artery stenosis. When unstented bilateral renal artery stenosis is present, use is generally avoided due to the elevated risk of deterioration in renal function unless possible benefits outweigh risks.

• Renal impairment: Use with caution with pre-existing renal insufficiency.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Pediatric: Olmesartan has not been shown to be effective for hypertension in children younger than 6 years. Children younger than 1 year must not receive olmesartan for hypertension. The renin-angiotensin-aldosterone system plays a critical role in kidney development. Administering drugs that act directly on the renin-angiotensin-aldosterone system can have effects on the development of immature kidneys and alter normal renal development.

• Pregnancy: [U.S. Boxed Warning]: Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible once pregnancy is detected.

• Surgical patients: In patients on chronic ARB therapy, intraoperative hypotension may occur with induction and maintenance of general anesthesia; however, discontinuation of therapy prior to surgery is controversial. If continued preoperatively, avoidance of hypotensive agents during surgery is prudent (Hillis, 2011).

Monitoring Parameters

Blood pressure, electrolytes, serum creatinine, BUN, urinalysis

Pregnancy Risk Factor

D

Pregnancy Considerations

[U.S. Boxed Warning]: Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible once pregnancy is detected. The use of drugs which act on the renin-angiotensin system are associated with oligohydramnios. Oligohydramnios, due to decreased fetal renal function, may lead to fetal lung hypoplasia and skeletal malformations. Use is also associated with anuria, hypotension, renal failure, skull hypoplasia, and death in the fetus/neonate. The exposed fetus should be monitored for fetal growth, amniotic fluid volume, and organ formation. Infants exposed in utero should be monitored for hyperkalemia, hypotension, and oliguria (exchange transfusions or dialysis may be needed). These adverse events are generally associated with maternal use in the second and third trimesters.

Untreated chronic maternal hypertension is also associated with adverse events in the fetus, infant, and mother. The use of angiotensin II receptor blockers is not recommended to treat chronic uncomplicated hypertension in pregnant women and should generally be avoided in women of reproductive potential (ACOG, 2013).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Have patient report immediately to prescriber signs of kidney problems (urinary retention, blood in urine, change in amount of urine passed, or weight gain), signs of high potassium (abnormal heartbeat, confusion, dizziness, passing out, weakness, shortness of breath, numbness or tingling feeling), severe dizziness, passing out, severe diarrhea, or excessive weight loss (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patients should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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