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.
Acute coronary syndrome:
Note: May be used as an alternative in patients who cannot tolerate an ACE inhibitor (eg, due to cough) (Ref). In patients with prior angiotensin-converting enzyme (ACE) inhibitor-associated angioedema (ie, without urticaria or other signs of hypersensitivity), an angiotensin II receptor blocker (ARB) may also be an alternative. ARBs do not appear to elevate the risk of angioedema (Ref); however, patients must be educated that angioedema due to an ACE inhibitor can sometimes reoccur within months following discontinuation (Ref); referral to an allergist may be appropriate.
Non-ST-elevation acute coronary syndrome (alternative agent) (off-label use):
Note: Patients should be hemodynamically stable before initiation. Use as a component of an appropriate medical regimen, which may also include antiplatelet agent(s), a beta-blocker, and a statin. Continue ARB therapy indefinitely for patients with concurrent diabetes, left ventricular ejection fraction ≤40%, hypertension, or stable chronic kidney disease (CKD) (Ref). Dosing is based on general dosing range in the manufacturer's labeling.
Oral: Initial: 20 mg once daily; increase dose as tolerated up to 40 mg/day under close monitoring to avoid hypotension.
ST-elevation myocardial infarction (alternative agent) (off-label use):
Note: Patients should be hemodynamically stable before initiation. Use as a component of an appropriate medical regimen, which may also include antiplatelet agent(s), a beta-blocker, and a statin. Continue ARB therapy indefinitely (Ref). Dosing is based on general dosing range in the manufacturer's labeling.
Oral: Initial: 20 mg once daily; increase dose as tolerated up to 40 mg/day under close monitoring to avoid hypotension.
Hypertension, chronic:
Note: For patients who warrant combination therapy (BP >20/10 mm Hg above goal or suboptimal response to initial monotherapy), may use with another appropriate agent (eg, long-acting dihydropyridine calcium channel blocker or thiazide diuretic) (Ref).
Oral: 20 mg once daily; evaluate response after ~2 to 4 weeks and titrate dose (eg, increase the daily dose by doubling) as needed up to 40 mg once daily; if additional blood pressure control is needed, consider combination therapy. Patients with severe asymptomatic hypertension and no signs of acute end organ damage should be evaluated for medication titration within 1 week (Ref).
Proteinuric chronic kidney disease, diabetic or nondiabetic (off-label use):
Oral: Initial: 20 mg once daily; titrate gradually (eg, by doubling the dose every 2 to 4 weeks) to the maximally tolerated dose, not to exceed 40 mg/day. If proteinuria target is not met despite optimized dosage, consider additional therapies (eg, sodium-glucose cotransporter-2 inhibitor) (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥40 mL/minute: No dosage adjustment necessary.
CrCl <40 mL/minute: No initial dosage adjustment necessary. AUC is increased 3-fold in patients with CrCl <20 mL/minute and a maximum dose of 20 mg/day has been recommended for these patients (Ref).
Mild impairment: No dosage adjustment necessary.
Moderate to severe: No initial dosage adjustment necessary. Total drug exposure increased ~60% in moderate impairment. Should be used with caution in patients with ascites due to cirrhosis (Ref).
Refer to adult dosing.
(For additional information see "Olmesartan: Pediatric drug information")
Note: Consider lower starting dose in patients with possible depletion of intravascular volume (eg, patients receiving diuretics).
Hypertension: Oral:
Children 1 to 5 years and ≥5 kg: Limited data available; efficacy results variable: Initial: 0.3 mg/kg/dose once daily; if initial response inadequate after 2 weeks, dose may be increased to 0.6 mg/kg/dose once daily. Dosing was evaluated in a double-blind, placebo-controlled study of 59 patients and some efficacy was demonstrated; however, results were not statistically significant.
Children and Adolescents 6 to 16 years:
20 to <35 kg: 10 mg once daily; if initial response inadequate after 2 weeks, dose may be increased; maximum daily dose: 20 mg/day
≥35 kg: 20 mg once daily; if initial response inadequate after 2 weeks, dose may be increased; maximum daily dose: 40 mg/day
Adolescents >16 years: Initial: 20 mg once daily; if initial response is inadequate, may be increased to 40 mg once daily after 2 weeks
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no pediatric-specific recommendations; based on experience in adult patients, no initial dosage adjustment necessary; however, AUC is increased 3-fold in adult patients with CrCl <20 mL/minute; dosing adjustment may be necessary, use with caution.
Hemodialysis: There are no dosing recommendations provided in the manufacturer's labeling; has not been studied.
There are no pediatric-specific recommendations; based on experience in adult patients, no initial dosage adjustment may be necessary; however, in adult patients with moderate hepatic impairment, an increase in AUC of ~60% was observed; use with caution.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Central nervous system: Dizziness (3%), headache (>1%)
Endocrine & metabolic: Hyperglycemia (>1%), hypertriglyceridemia (>1%)
Gastrointestinal: Diarrhea (>1%; may be severe and chronic)
Genitourinary: Hematuria (>1%)
Neuromuscular & skeletal: Back pain (>1%), increased creatine phosphokinase (>1%)
Respiratory: Bronchitis (>1%), flu-like symptoms (>1%), pharyngitis (>1%), rhinitis (>1%), sinusitis (>1%)
Frequency not defined: Hematologic & oncologic: Decreased hematocrit, decreased hemoglobin
<1%, postmarketing, and/or case reports: Abdominal pain, acute renal failure, alopecia, anaphylaxis, angioedema, arthralgia, arthritis, asthenia, chest pain, dyspepsia, facial edema, gastroenteritis, hypercholesterolemia, hyperkalemia, hyperlipidemia, hyperuricemia, increased liver enzymes, increased serum bilirubin, increased serum creatinine, myalgia, nausea, peripheral edema, pruritus, rhabdomyolysis, skin rash, sprue-like symptoms, tachycardia, urticaria, vertigo, vomiting
Concomitant use with aliskiren in patients with diabetes mellitus.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US 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); pregnancy; breastfeeding.
Concerns related to adverse effects:
• Angioedema: Angiotensin II receptor antagonists (ARBs) do not appear to elevate the risk of angioedema (Rasmussen 2019; Toh 2012). Patients with a history of angioedema due to an angiotensin-converting enzyme (ACE) inhibitor must be educated that sometimes there can be recurrence within months following discontinuation (Beltrami 2011). No matter the cause of angioedema, prolonged frequent monitoring is required, especially if tongue, glottis, or larynx are involved, as they are associated with airway obstruction. Discontinue therapy immediately if angioedema occurs. Aggressive early management is critical. IM administration of epinephrine may be necessary. Do not readminister the ARB to patients who experience angioedema from this medication.
• 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; dose reduction may be considered. 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 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.
• Ascites: Generally, avoid use in patients with ascites due to cirrhosis or refractory ascites; if use cannot be avoided in patients with ascites due to cirrhosis, monitor BP and renal function carefully to avoid rapid development of renal failure (AASLD [Runyon 2013]).
• 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 preexisting renal insufficiency.
Special populations:
• Pediatric: Olmesartan has not been shown to be effective for hypertension in children <6 years of age. Children <1 year of age 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: [US 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.
• Race/Ethnicity: In Black patients, the BP-lowering effects of ARBs may be less pronounced. The exact mechanism is not known; differences in the renin-angiotensin-aldosterone system, low renin levels, and salt sensitivity more commonly found in Black patients may contribute (Brewster 2013; Helmer 2018; manufacturer's labeling).
• 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). Based on current research and clinical guidelines in patients undergoing noncardiac surgery, continuing ARBs is reasonable in the perioperative period. If ARBs are held before surgery, it is reasonable to restart postoperatively as soon as clinically feasible (ACC/AHA [Fleisher 2014]).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral, as medoxomil:
Benicar: 5 mg, 20 mg, 40 mg
Generic: 5 mg, 20 mg, 40 mg
Yes
Tablets (Benicar Oral)
5 mg (per each): $9.55
20 mg (per each): $11.67
40 mg (per each): $16.22
Tablets (Olmesartan Medoxomil Oral)
5 mg (per each): $5.13 - $5.65
20 mg (per each): $6.28 - $6.91
40 mg (per each): $8.73 - $9.61
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral, as medoxomil:
Olmetec: 20 mg, 40 mg
Generic: 20 mg, 40 mg
Oral: Administer with or without food.
Oral: May be administered with or without food.
Hypertension, chronic: Management of hypertension in adults and pediatric patients ≥6 years of age.
Non-ST-elevation acute coronary syndrome; Proteinuric chronic kidney disease, diabetic or nondiabetic; ST-elevation myocardial infarction
Benicar may be confused with Mevacor
Substrate of OATP1B1/1B3 (SLCO1B1/1B3)
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: 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. Risk D: Consider therapy modification
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification
Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Angiotensin II: Receptor Blockers may diminish the therapeutic effect of Angiotensin II. Risk C: Monitor therapy
Angiotensin-Converting Enzyme Inhibitors: Angiotensin II Receptor Blockers may enhance the adverse/toxic effect of Angiotensin-Converting Enzyme Inhibitors. Angiotensin II Receptor Blockers may increase the serum concentration of Angiotensin-Converting Enzyme Inhibitors. Management: 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 when possible. Monitor blood pressure, renal function, and potassium if combined. Risk D: Consider therapy modification
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy
Arginine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination
Colesevelam: May decrease the serum concentration of Olmesartan. Management: Administer olmesartan at least 4 hours prior to colesevelam. Risk D: Consider therapy modification
Dapoxetine: May enhance the orthostatic hypotensive effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Drospirenone-Containing Products: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy
Eplerenone: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Finerenone: Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of Finerenone. Risk C: Monitor therapy
Flunarizine: May enhance the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Heparin: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Heparins (Low Molecular Weight): May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Indoramin: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Levodopa-Foslevodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Foslevodopa. Risk C: Monitor therapy
Lithium: Angiotensin II Receptor Blockers may increase the serum concentration of Lithium. Management: Initiate lithium at lower doses in patients receiving an angiotensin II receptor blocker (ARB). Consider lithium dose reductions in patients stable on lithium therapy who are initiating an ARB. Monitor lithium concentrations closely when combined. Risk D: Consider therapy modification
Loop Diuretics: May enhance the hypotensive effect of Angiotensin II Receptor Blockers. Loop Diuretics may enhance the nephrotoxic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicorandil: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: 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. Risk C: Monitor therapy
Nonsteroidal Anti-Inflammatory Agents (Topical): May diminish the therapeutic effect of Angiotensin II Receptor Blockers. Risk C: 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. Risk D: Consider therapy modification
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Polyethylene Glycol-Electrolyte Solution: Angiotensin II Receptor Blockers may enhance the nephrotoxic effect of Polyethylene Glycol-Electrolyte Solution. Risk C: Monitor therapy
Potassium Salts: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Potassium-Sparing Diuretics: Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of Potassium-Sparing Diuretics. Risk C: Monitor therapy
Prazosin: Antihypertensive Agents may enhance the hypotensive effect of Prazosin. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Ranolazine: May enhance the adverse/toxic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Silodosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: 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. Risk C: Monitor therapy
Sparsentan: May enhance the adverse/toxic effect of Angiotensin II Receptor Blockers. Risk X: Avoid combination
Tacrolimus (Systemic): Angiotensin II Receptor Blockers may enhance the hyperkalemic effect of Tacrolimus (Systemic). Risk C: Monitor therapy
Terazosin: Antihypertensive Agents may enhance the hypotensive effect of Terazosin. Risk C: Monitor therapy
Tolvaptan: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Trimethoprim: May enhance the hyperkalemic effect of Angiotensin II Receptor Blockers. Risk C: Monitor therapy
Urapidil: Antihypertensive Agents may enhance the hypotensive effect of Urapidil. Risk C: Monitor therapy
Medications considered acceptable for the treatment of chronic hypertension during pregnancy may generally be used in patients trying to conceive. Angiotensin II receptor blockers (ARBs) are fetotoxic. Transition patients prior to conception to an agent preferred for use during pregnancy unless treatment with an ARB is absolutely necessary (ACC/AHA [Whelton 2018]; ACOG 2019; NICE 2019).
Drugs that act on the renin-angiotensin system can cause injury and death to the developing fetus. Exposure to an angiotensin II receptor blocker (ARB) during the first trimester of pregnancy may be associated with an increased risk of fetal malformations (ACOG 2019; ESC [Regitz-Zagrosek 2018]). Following exposure during the second or third trimesters, drugs that act on the renin-angiotensin system are associated with oligohydramnios. Oligohydramnios, due to decreased fetal kidney function, may lead to fetal lung hypoplasia and skeletal malformations. Oligohydramnios may not appear until after an irreversible fetal injury has occurred. ARB use during pregnancy is also associated with anuria, hypotension, kidney failure, skull hypoplasia, and death in the fetus/neonate. Monitor infants exposed to an ARB in utero for hyperkalemia, hypotension, and oliguria. Exchange transfusions or dialysis may be required to reverse hypotension or improve renal function.
Chronic maternal hypertension is also associated with adverse events in the fetus/infant. Chronic maternal hypertension may increase the risk of birth defects, low birth weight, premature delivery, stillbirth, and neonatal death. Actual fetal/neonatal risks may be related to the duration and severity of maternal hypertension. Untreated chronic hypertension may also increase the risks of adverse maternal outcomes, including gestational diabetes, preeclampsia, delivery complications, stroke, and myocardial infarction (ACOG 2019).
Discontinue ARBs as soon as possible once pregnancy is detected. Agents other than an ARB are recommended for the treatment of chronic hypertension during pregnancy (ACOG 2019; ESC [Cífková 2020]; ESC [Regitz-Zagrosek 2018]; SOGC [Magee 2022]). Closely monitor patients exposed to an ARB during pregnancy with serial ultrasounds.
It is not known if olmesartan is present in breast milk.
Due to the potential for serious adverse reactions in the breastfeeding infant, the manufacturer recommends a decision be made whether to discontinue breastfeeding or to discontinue the drug, considering the importance of treatment to the mother. When treatment for hypertension is needed in a breastfeeding patient, consider use of an agent other than an angiotensin II receptor blocker (ESC [Cífková 2020]; NICE 2019).
Blood pressure; serum electrolytes (eg, potassium [especially in patients on concomitant potassium-sparing diuretics, potassium supplements, and/or potassium-containing salts]); kidney function.
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 non-renin-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)
Protein binding: 99%
Metabolism: Olmesartan medoxomil is hydrolyzed in the GI tract to active olmesartan. No further metabolism occurs.
Bioavailability: 26%
Half-life elimination: Terminal: 13 hours
Time to peak: 1 to 2 hours
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
Altered kidney function: AUC is approximately tripled when CrCl is <20 mL/minute.
Hepatic function impairment: In patients with moderate hepatic impairment, AUC increased by ~60%; Cmax was also increased.
Older adult: AUC increased by 33%, and there is a 30% reduction in renal Cl.
Sex: AUC and Cmax increased 10% to 15% in women.
Race/ethnicity: Antihypertensive effect was smaller in black patients.
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