Olmesartan Medoxomil 20 Mg

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Olmesartan Medoxomil Prescribing Information

Medically reviewed by Drugs.com. Last updated on Apr 1, 2022.

On This Page

• Boxed Warning
• Indications and Usage
• Dosage and Administration
• Dosage Forms and Strengths
• Contraindications
• Warnings and Precautions
• Adverse Reactions/Side Effects
• Drug Interactions
• Use In Specific Populations
• Overdosage
• Description
• Clinical Pharmacology
• Nonclinical Toxicology
• Clinical Studies
• How Supplied/Storage and Handling
• Patient Counseling Information

• When pregnancy is detected, discontinue Olmesartan Medoxomil tablets as soon as possible (5.1, 8.1).
• Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus (5.1, 8.1).

Indications and Usage for Olmesartan Medoxomil

Olmesartan Medoxomil tablets, USP are indicated for the treatment of hypertension in adults and children six years of age and older, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including the class to which this drug principally belongs. There are no controlled trials demonstrating risk reduction with Olmesartan Medoxomil tablets, USP.

Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC).

Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly.

Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal.

Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy.

It may be used alone or in combination with other antihypertensive agents.

Olmesartan Medoxomil Dosage and Administration

Adult Hypertension

Dosage must be individualized. The usual recommended starting dose of Olmesartan Medoxomil tablets is 20 mg once daily when used as monotherapy in patients who are not volume-contracted. For patients requiring further reduction in blood pressure after 2 weeks of therapy, the dose of Olmesartan Medoxomil tablets may be increased to 40 mg. Doses above 40 mg do not appear to have greater effect. Twice-daily dosing offers no advantage over the same total dose given once daily.

For patients with possible depletion of intravascular volume (e.g., patients treated with diuretics, particularly those with impaired renal function), initiate Olmesartan Medoxomil tablets under close medical supervision and give consideration to use of a lower starting dose [see Warnings and Precautions (5.3)] .

Pediatric Hypertension (6 Years of Age and Older)

For children who cannot swallow tablets, the same dose can be given using an extemporaneous suspension as described below [see Clinical Pharmacology (12.3)] .

Follow the suspension preparation instructions below to administer Olmesartan Medoxomil tablets as a suspension.

Preparation of Suspension (for 200 mL of a 2 mg/mL suspension)

Add 50 mL of Purified Water to an amber polyethylene terephthalate (PET) bottle containing twenty Olmesartan Medoxomil tablets 20 mg tablets and allow to stand for a minimum of 5 minutes. Shake the container for at least 1 minute and allow the suspension to stand for at least 1 minute. Repeat 1-minute shaking and 1-minute standing for four additional times. Add 100 mL of ORA-Sweet ® and 50 mL of ORA-Plus ® 1 to the suspension and shake well for at least 1 minute. The suspension should be refrigerated at 2-8°C (36-46°F) and can be stored for up to 4 weeks. Shake the suspension well before each use and return promptly to the refrigerator.

1 ORA-Sweet ® and ORA-Plus ® are registered trademarks of Paddock Laboratories, Inc.

Dosage Forms and Strengths

• 5 mg white or almost white round film-coated tablets, debossed “L20” on one side while blank on the other side.
• 20 mg white or almost white round film-coated tablets, debossed “L18” on one side while blank on the other side.
• 40 mg white or almost white round film-coated tablets, debossed “L17” on one side while blank on the other side.

Contraindications

Do not co-administer aliskiren with Olmesartan Medoxomil tablets in patients with diabetes [see Drug Interactions (7.3)].

Warnings and Precautions

Fetal Toxicity

Olmesartan Medoxomil tablets can cause fetal harm when administered to a pregnant woman. Use of drugs that act on the renin-angiotensin system (RAS) during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue Olmesartan Medoxomil as soon as possible [see Use in Specific Populations (8.1)].

Morbidity in Infants

Hypotension in Volume- or Salt-Depleted Patients

In patients with an activated renin-angiotensin-aldosterone system, such as volume- and/or salt-depleted patients (e.g., those being treated with high doses of diuretics), symptomatic hypotension may be anticipated after initiation of treatment with Olmesartan Medoxomil. Initiate treatment under close medical supervision and consider starting at a lower dose. If hypotension does occur, place the patient in the supine position and, if necessary, give an intravenous infusion of normal saline [see Dosage and Administration (2.1)] . A transient hypotensive response is not a contraindication to further treatment, which usually can be continued without difficulty once the blood pressure has stabilized.

Impaired Renal Function

As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function may be anticipated in susceptible individuals treated with Olmesartan Medoxomil. In patients whose renal function may depend upon the activity of the renin-angiotensin-aldosterone system (e.g., patients with severe congestive heart failure), treatment with angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor antagonists has been associated with oliguria and/or progressive azotemia and rarely with acute renal failure and/or death. Similar results may be anticipated in patients treated with Olmesartan Medoxomil [see Dosage and Administration (2.1), Drug Interactions (7.3), Use in Specific Populations (8.7) and Clinical Pharmacology (12.3)] .

In studies of ACE inhibitors in patients with unilateral or bilateral renal artery stenosis, increases in serum creatinine or blood urea nitrogen (BUN) have been reported. There has been no long-term use of Olmesartan Medoxomil in patients with unilateral or bilateral renal artery stenosis, but similar results may be expected.

Sprue-like Enteropathy

Severe, chronic diarrhea with substantial weight loss has been reported in patients taking olmesartan months to years after drug initiation. Intestinal biopsies of patients often demonstrated villous atrophy. If a patient develops these symptoms during treatment with olmesartan, exclude other etiologies. Consider alternative antihypertensive therapy in cases where no other etiology is identified.

Hyperkalemia

Serum potassium should be monitored in patients receiving Olmesartan Medoxomil tablets. Drugs that inhibit the renin angiotensin system can cause hyperkalemia. Risk factors for the development of hyperkalemia include renal insufficiency, diabetes mellitus, and the concomitant use of potassium-sparing diuretics, potassium supplements and/or potassium-containing salt substitutes [see Drug Interactions (7.3)] .

Adverse Reactions

Clinical Trials Experience

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.

Olmesartan Medoxomil has been evaluated for safety in more than 3825 patients/subjects, including more than 3275 patients treated for hypertension in controlled trials. This experience included about 900 patients treated for at least 6 months and more than 525 for at least 1 year. Events generally were mild, transient and had no relationship to the dose of Olmesartan Medoxomil.

Analysis of gender, age and race groups demonstrated no differences between Olmesartan Medoxomil and placebo-treated patients. The rate of withdrawals due to adverse reactions in all trials of hypertensive patients was 2.4% (i.e., 79/3278) of patients treated with Olmesartan Medoxomil and 2.7% (i.e., 32/1179) of control patients. In placebo-controlled trials, the only adverse reaction that occurred in more than 1% of patients treated with Olmesartan Medoxomil and at a higher incidence versus placebo was dizziness (3% vs. 1%).

Facial edema was reported in five patients receiving Olmesartan Medoxomil. Angioedema has been reported with angiotensin II antagonists.

No relevant differences were identified between the adverse experience profile for pediatric patients aged 1 to 16 years and that previously reported for adult patients.

Post-Marketing Experience

The following adverse reactions have been reported in post-marketing experience. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Body as a Whole: Asthenia, angioedema, anaphylactic reactions

Gastrointestinal: Vomiting, sprue-like enteropathy [see Warnings and Precautions (5.5)]

Metabolic and Nutritional Disorders: Hyperkalemia

Urogenital System: Acute renal failure, increased blood creatinine levels

Skin and Appendages: Alopecia, pruritus, urticaria

Data from one controlled trial and an epidemiologic study have suggested that high-dose olmesartan may increase cardiovascular (CV) risk in diabetic patients, but the overall data are not conclusive. The randomized, placebo-controlled, double-blind ROADMAP trial (Randomized Olmesartan And Diabetes MicroAlbuminuria Prevention trial, n=4447) examined the use of olmesartan, 40 mg daily, vs. placebo in patients with type 2 diabetes mellitus, normoalbuminuria, and at least one additional risk factor for CV disease. The trial met its primary endpoint, delayed onset of microalbuminuria, but olmesartan had no beneficial effect on decline in glomerular filtration rate (GFR). There was a finding of increased CV mortality (adjudicated sudden cardiac death, fatal myocardial infarction, fatal stroke, revascularization death) in the olmesartan group compared to the placebo group (15 olmesartan vs. 3 placebo, HR 4.9, 95% confidence interval [CI], 1.4, 17), but the risk of non-fatal myocardial infarction was lower with olmesartan (HR 0.64, 95% CI 0.35, 1.18).

The epidemiologic study included patients 65 years and older with overall exposure of > 300,000 patient-years. In the sub-group of diabetic patients receiving high-dose olmesartan (40 mg/d) for > 6 months, there appeared to be an increased risk of death (HR 2.0, 95% CI 1.1, 3.8) compared to similar patients taking other angiotensin receptor blockers. In contrast, high-dose olmesartan use in non-diabetic patients appeared to be associated with a decreased risk of death (HR 0.46, 95% CI 0.24, 0.86) compared to similar patients taking other angiotensin receptor blockers. No differences were observed between the groups receiving lower doses of olmesartan compared to other angiotensin blockers or those receiving therapy for < 6 months.

Overall, these data raise a concern of a possible increased CV risk associated with the use of high-dose olmesartan in diabetic patients. There are, however, concerns with the credibility of the finding of increased CV risk, notably the observation in the large epidemiologic study for a survival benefit in non-diabetics of a magnitude similar to the adverse finding in diabetics.

Drug Interactions

Agents Increasing Serum Potassium

Concomitant use of olmesartan with other agents that block the renin-angiotensin system, potassium-sparing diuretics (e.g., spironolactone, triamterene, amiloride), potassium supplements, salt substitutes containing potassium or other drugs that may increase potassium levels (e.g., heparin) may lead to increases in serum potassium. If co-medication is considered necessary, monitoring of serum potassium is advisable.

Non-Steroidal Anti-Inflammatory Agents Including Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors)

In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, co-administration of NSAIDs, including selective COX-2 inhibitors, with angiotensin II receptor antagonists, including Olmesartan Medoxomil, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving Olmesartan Medoxomil and NSAID therapy.

The antihypertensive effect of angiotensin II receptor antagonists, including Olmesartan Medoxomil, may be attenuated by NSAIDs including selective COX-2 inhibitors.

Dual Blockade of the Renin-Angiotensin System (RAS)

Dual blockade of the RAS with angiotensin receptor blockers, ACE inhibitors, or aliskiren is associated with increased risks of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. Most patients receiving the combination of two RAS inhibitors do not obtain any additional benefit compared to monotherapy. In general, avoid combined use of RAS inhibitors. Closely monitor blood pressure, renal function and electrolytes in patients on Olmesartan Medoxomil and other agents that affect the RAS.

Do not co-administer aliskiren with Olmesartan Medoxomil in patients with diabetes [see Contraindications (4)]. Avoid use of aliskiren with Olmesartan Medoxomil in patients with renal impairment (GFR

Lithium

Increases in serum lithium concentrations and lithium toxicity have been reported during concomitant administration of lithium with angiotensin II receptor antagonists, including Olmesartan Medoxomil tablets. Monitor serum lithium levels during concomitant use.

Colesevelam Hydrochloride

Concurrent administration of bile acid sequestering agent colesevelam hydrochloride reduces the systemic exposure and peak plasma concentration of olmesartan. Administration of olmesartan at least 4 hours prior to colesevelam hydrochloride decreased the drug interaction effect. Consider administering olmesartan at least 4 hours before the colesevelam hydrochloride dose [see Clinical Pharmacology (12.3)] .

USE IN SPECIFIC POPULATIONS

Pregnancy

Olmesartan Medoxomil tablets can cause fetal harm when administered to a pregnant woman. Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Most epidemiologic studies examining fetal abnormalities after exposure to antihypertensive use in the first trimester have not distinguished drugs affecting the renin-angiotensin system from other antihypertensive agents. In animal reproduction studies, Olmesartan Medoxomil tablets treatment during organogenesis resulted in increased embryofetal toxicity in rats at doses lower than maternally toxic doses.

When pregnancy is detected, discontinue Olmesartan Medoxomil tablets as soon as possible. Consider alternative antihypertensive therapy during pregnancy.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%–4% and 15%–20%, respectively.

Disease-Associated Maternal and/or Embryo/Fetal Risk

Hypertension in pregnancy increases the maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section and post-partum hemorrhage). Hypertension increases the fetal risk for intrauterine growth restriction and intrauterine death. Pregnant women with hypertension should be carefully monitored and managed accordingly.

Fetal/Neonatal Adverse Reactions

Oligohydramnios in pregnant women who use drugs affecting the renin-angiotensin system in the second and third trimesters of pregnancy can result in the following: reduced fetal renal function leading to anuria and renal failure, fetal lung hypoplasia, skeletal deformations, including skull hypoplasia, hypotension and death.

In patients taking Olmesartan Medoxomil tablets during pregnancy, perform serial ultrasound examinations to assess the intra-amniotic environment. Fetal testing may be appropriate, based on the week of gestation. Patients and physicians should be aware, however, that oligohydramnios may not appear until after the fetus has sustained irreversible injury.

Closely observe infants with histories of in utero exposure to Olmesartan Medoxomil tablets for hypotension, oliguria, and hyperkalemia. In neonates with a history of in utero exposure to Olmesartan Medoxomil tablets, if oliguria or hypotension occurs, utilize measures to maintain adequate blood pressure and renal perfusion. Exchange transfusions or dialysis may be required as a means of reversing hypotension and supporting renal function.

No teratogenic effects were observed when Olmesartan Medoxomil was administered to pregnant rats at oral doses up to 1000 mg/kg/day (240 times the maximum recommended human dose (MRHD) on a mg/m 2 basis) or pregnant rabbits at oral doses up to 1 mg/kg/day (half the MRHD on a mg/m 2 basis; higher doses could not be evaluated for effects on fetal development as they were lethal to the does). In rats, significant decreases in pup birth weight and weight gain were observed at doses ≥1.6 mg/kg/day, and delays in developmental milestones (delayed separation of ear auricula, eruption of lower incisors, appearance of abdominal hair, descent of testes, and separation of eyelids) and dose-dependent increases in the incidence of dilation of the renal pelvis were observed at doses ≥ 8 mg/kg/day. The no observed effect dose for developmental toxicity in rats is 0.3 mg/kg/day, about one-tenth the MRHD of 40 mg/day.

Lactation

There is no information regarding the presence of olmesartan in human milk, the effects on the breastfed infant, or the effects on milk production. Olmesartan is secreted at low concentration in the milk of lactating rats (see Data) . Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.

Presence of olmesartan in milk was observed after a single oral administration of 5 mg/kg [ 14 C] Olmesartan Medoxomil to lactating rats.

Pediatric Use

The antihypertensive effects of Olmesartan Medoxomil were evaluated in one randomized, double-blind clinical study in pediatric patients 1 to 16 years of age [see Clinical Studies (14.2)] . The pharmacokinetics of Olmesartan Medoxomil were evaluated in pediatric patients 1 to 16 years of age [see Clinical Pharmacology (12.3)] . Olmesartan Medoxomil was generally well tolerated in pediatric patients, and the adverse experience profile was similar to that described for adults.

Olmesartan Medoxomil has not been shown to be effective for hypertension in children

Geriatric Use

Of the total number of hypertensive patients receiving Olmesartan Medoxomil in clinical studies, more than 20% were 65 years of age and over, while more than 5% were 75 years of age and older. No overall differences in effectiveness or safety were observed between elderly patients and younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out [see Clinical Pharmacology (12.3)] .

Hepatic Impairment

Increases in AUC 0-∞ and C max were observed in patients with moderate hepatic impairment compared to those in matched controls, with an increase in AUC of about 60%. No initial dosage adjustment is recommended for patients with moderate to marked hepatic dysfunction [see Clinical Pharmacology (12.3)] .

Renal Impairment

Patients with renal insufficiency have elevated serum concentrations of olmesartan compared to subjects with normal renal function. After repeated dosing, the AUC was approximately tripled in patients with severe renal impairment (creatinine clearance

Black Patients

The antihypertensive effect of Olmesartan Medoxomil was smaller in black patients (usually a low-renin population), as has been seen with ACE inhibitors, beta-blockers and other angiotensin receptor blockers.

Overdosage

Limited data are available related to overdosage in humans. The most likely manifestations of overdosage would be hypotension and tachycardia; bradycardia could be encountered if parasympathetic (vagal) stimulation occurs. If symptomatic hypotension occurs, initiate supportive treatment. The dialyzability of olmesartan is unknown.

Olmesartan Medoxomil Description

Olmesartan Medoxomil, a prodrug, is hydrolyzed to olmesartan during absorption from the gastrointestinal tract. Olmesartan is a selective AT 1 subtype angiotensin II receptor antagonist.

Olmesartan Medoxomil is described chemically as 2,3-dihydroxy-2-butenyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[ p -( o -1 H -tetrazol-5-ylphenyl)benzyl]imidazole-5-carboxylate, cyclic 2,3-carbonate.

Its empirical formula is C 29 H 30 N 6 O 6 and its structural formula is:

Olmesartan Medoxomil is a white to light yellowish-white powder or crystalline powder with a molecular weight of 558.59. It is practically insoluble in water and sparingly soluble in methanol. Olmesartan Medoxomil tablets, USP are available for oral use as film-coated tablets containing 5 mg, 20 mg, or 40 mg of Olmesartan Medoxomil and the following inactive ingredients: hydroxypropyl cellulose, hypromellose, lactose monohydrate, low-substituted hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose, titanium dioxide, polyethylene glycol.

FDA approved dissolution method differs from the USP dissolution method.

Olmesartan Medoxomil – Clinical Pharmacology

Mechanism of Action

Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation and renal reabsorption of sodium. Olmesartan blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT 1 receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis.

An AT 2 receptor is found also in many tissues, but this receptor is not known to be associated with cardiovascular homeostasis. Olmesartan has more than a 12,500-fold greater affinity for the AT 1 receptor than for the AT 2 receptor.

Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is a mechanism of many drugs used to treat hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because Olmesartan Medoxomil does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known.

Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and circulating angiotensin II levels do not overcome the effect of olmesartan on blood pressure.

Pharmacodynamics

Olmesartan Medoxomil doses of 2.5 mg to 40 mg inhibit the pressor effects of angiotensin I infusion. The duration of the inhibitory effect was related to dose, with doses of Olmesartan Medoxomil >40 mg giving >90% inhibition at 24 hours.

Plasma concentrations of angiotensin I and angiotensin II and plasma renin activity (PRA) increase after single and repeated administration of Olmesartan Medoxomil to healthy subjects and hypertensive patients. Repeated administration of up to 80 mg Olmesartan Medoxomil had minimal influence on aldosterone levels and no effect on serum potassium.

Pharmacokinetics

Olmesartan Medoxomil is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract.

Olmesartan Medoxomil tablets and the suspension formulation prepared from Olmesartan Medoxomil tablets are bioequivalent [see Dosage and Administration (2.2)] .

The absolute bioavailability of olmesartan is approximately 26%. After oral administration, the peak plasma concentration (C max ) of olmesartan is reached after 1 to 2 hours. Food does not affect the bioavailability of olmesartan. Olmesartan Medoxomil tablets may be administered with or without food.

The volume of distribution of olmesartan is approximately 17 L. Olmesartan is highly bound to plasma proteins (99%) and does not penetrate red blood cells. The protein binding is constant at plasma olmesartan concentrations well above the range achieved with recommended doses.

In rats, olmesartan crossed the blood-brain barrier poorly, if at all. Olmesartan passed across the placental barrier in rats and was distributed to the fetus. Olmesartan was distributed to milk at low levels in rats.

Metabolism and Excretion

Following the rapid and complete conversion of Olmesartan Medoxomil to olmesartan during absorption, there is virtually no further metabolism of olmesartan. Total plasma clearance of olmesartan is 1.3 L/h, with a renal clearance of 0.6 L/h. Approximately 35% to 50% of the absorbed dose is recovered in urine while the remainder is eliminated in feces via the bile.

Olmesartan appears to be eliminated in a biphasic manner with a terminal elimination half-life of approximately 13 hours. Olmesartan shows linear pharmacokinetics following single oral doses of up to 320 mg and multiple oral doses of up to 80 mg. Steady-state levels of olmesartan are achieved within 3 to 5 days and no accumulation in plasma occurs with once-daily dosing.

The pharmacokinetics of olmesartan were studied in the elderly (≥65 years). Overall, maximum plasma concentrations of olmesartan were similar in young adults and the elderly. Modest accumulation of olmesartan was observed in the elderly with repeated dosing; AUC ss , τ was 33% higher in elderly patients, corresponding to an approximate 30% reduction in CL R [see Dosage and Administration (2.1) and Use in Specific Populations (8.5)] .

The pharmacokinetics of olmesartan were studied in pediatric hypertensive patients aged 1 to 16 years. The clearance of olmesartan in pediatric patients was similar to that in adult patients when adjusted by the body weight [see Use in Specific Populations (8.4)] .

Olmesartan pharmacokinetics have not been investigated in pediatric patients less than 1 year of age [see Warnings and Precautions (5.2) and Use in Specific Populations (8.4)].

Male and Female Patients

Minor differences were observed in the pharmacokinetics of olmesartan in women compared to men. AUC and C max were 10-15% higher in women than in men.

Patients with Hepatic Impairment

Increases in AUC 0-∞ and C max were observed in patients with moderate hepatic impairment compared to those in matched controls, with an increase in AUC of about 60% [see Dosage and Administration (2.1) and Use in Specific Populations (8.6)] .

Patients with Renal Impairment

In patients with renal insufficiency, serum concentrations of olmesartan were elevated compared to subjects with normal renal function. After repeated dosing, the AUC was approximately tripled in patients with severe renal impairment (creatinine clearance

Drug Interaction Studies

Bile Acid Sequestering Agent Colesevelam

Concomitant administration of 40 mg Olmesartan Medoxomil and 3750 mg colesevelam hydrochloride in healthy subjects resulted in 28% reduction in C max and 39% reduction in AUC of olmesartan. Lesser effects, 4% and 15% reduction in C max and AUC respectively, were observed when Olmesartan Medoxomil was administered 4 hours prior to colesevelam hydrochloride [see Drug Interactions (7.5)] .

No significant drug interactions were reported in studies in which Olmesartan Medoxomil was co-administered with digoxin or warfarin in healthy volunteers.

The bioavailability of olmesartan was not significantly altered by the co-administration of antacids [Al(OH) 3 /Mg(OH) 2 ].

Olmesartan Medoxomil is not metabolized by the cytochrome P450 system and has no effects on P450 enzymes; thus, interactions with drugs that inhibit, induce, or are metabolized by those enzymes are not expected.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Olmesartan Medoxomil was not carcinogenic when administered by dietary administration to rats for up to 2 years. The highest dose tested (2000 mg/kg/day) was, on a mg/m 2 basis, about 480 times the maximum recommended human dose (MRHD) of 40 mg/day. Two carcinogenicity studies conducted in mice, a 6-month gavage study in the p53 knockout mouse and a 6-month dietary administration study in the Hras2 transgenic mouse, at doses of up to 1000 mg/kg/day (about 120 times the MRHD), revealed no evidence of a carcinogenic effect of Olmesartan Medoxomil.

Both Olmesartan Medoxomil and olmesartan tested negative in the in vitro Syrian hamster embryo cell transformation assay and showed no evidence of genetic toxicity in the Ames (bacterial mutagenicity) test. However, both were shown to induce chromosomal aberrations in cultured cells in vitro (Chinese hamster lung) and tested positive for thymidine kinase mutations in the in vitro mouse lymphoma assay. Olmesartan Medoxomil tested negative in vivo for mutations in the MutaMouse intestine and kidney and for clastogenicity in mouse bone marrow (micronucleus test) at oral doses of up to 2000 mg/kg (olmesartan not tested).

Fertility of rats was unaffected by administration of Olmesartan Medoxomil at dose levels as high as 1000 mg/kg/day (240 times the MRHD) in a study in which dosing was begun 2 (female) or 9 (male) weeks prior to mating.

Clinical Studies

Adult Hypertension

The antihypertensive effects of Olmesartan Medoxomil have been demonstrated in seven placebo-controlled studies at doses ranging from 2.5 mg to 80 mg for 6 to 12 weeks, each showing statistically significant reductions in peak and trough blood pressure. A total of 2693 patients (2145 Olmesartan Medoxomil; 548 placebo) with essential hypertension were studied. Olmesartan Medoxomil once daily lowered diastolic and systolic blood pressure. The response was dose related, as shown in the following graph. An Olmesartan Medoxomil dose of 20 mg daily produces a trough sitting blood pressure (BP) reduction over placebo of about 10/6 mmHg and a dose of 40 mg daily produces a trough sitting BP reduction over placebo of about 12/7 mmHg. Olmesartan Medoxomil doses greater than 40 mg had little additional effect. The onset of the antihypertensive effect occurred within 1 week and was largely manifest after 2 weeks.

Data above are from seven placebo-controlled studies (2145 Olmesartan Medoxomil patients, 548 placebo patients). The blood pressure lowering effect was maintained throughout the 24-hour period with Olmesartan Medoxomil once daily, with trough-to-peak ratios for systolic and diastolic response between 60 and 80%.

The blood pressure lowering effect of Olmesartan Medoxomil, with and without hydrochlorothiazide, was maintained in patients treated for up to 1 year. There was no evidence of tachyphylaxis during long-term treatment with Olmesartan Medoxomil or rebound effect following abrupt withdrawal of Olmesartan Medoxomil after 1 year of treatment.

The antihypertensive effect of Olmesartan Medoxomil was similar in men and women and in patients older and younger than 65 years. The effect was smaller in black patients (usually a low-renin population), as has been seen with ACE inhibitors, beta-blockers and other angiotensin receptor blockers. Olmesartan Medoxomil had an additional blood pressure lowering effect when added to hydrochlorothiazide.

There are no trials of Olmesartan Medoxomil demonstrating reductions in cardiovascular risk in patients with hypertension, but at least one pharmacologically similar drug has demonstrated such benefits.

Pediatric Hypertension

In the same study, 59 patients aged 1 to 5 years who weighed ≥5 kg received 0.3 mg/kg of Olmesartan Medoxomil once daily for three weeks in an open-label phase and then were randomized to receiving Olmesartan Medoxomil or placebo in a double-blind phase. At the end of the second week of withdrawal, the mean systolic/diastolic blood pressure at trough was 3/3 mmHg lower in the group randomized to Olmesartan Medoxomil; this difference in blood pressure was not statistically significant (95% C.I. -2 to 7/-1 to 7).

How Supplied/Storage and Handling

Olmesartan Medoxomil tablets, USP are supplied as white or almost white round film-coated tablets, debossed “L17”, “L18” and “L20” on one side for 40mg, 20mg and 5mg strengths, respectively, while blank on the other side.

Tablets are supplied as follows:

Store at 20-25°C (68-77°F); excursions permitted to 15°C and 30°C (59°F-86°F) [see USP Controlled Room Temperature] .

Patient Counseling Information

Pregnancy: Advise female patients of childbearing age about the consequences of exposure to Olmesartan Medoxomil tablets during pregnancy. Discuss treatment options with women planning to become pregnant. Tell patients to report pregnancies to their physicians as soon as possible [see Warnings and Precautions (5.1) and Use in Specific Populations (8.1)] .

Lactation : Advise nursing women not to breastfeed during treatment with Olmesartan Medoxomil tablets [see Use in Specific Populations (8.2)] .

Hyperkalemia: Advise patients not to use potassium supplements or salt substitutes that contain potassium without consulting their healthcare provider [see Drug Interactions (7.1)] .

* All trademark names are the property of their respective owners.

Sunshine Lake Pharma Co., Ltd.

Northern Industry Road 1#,

Song Shan Lake, DongGuan,

GuangDong Province, 523808,

Lannett Company, Inc.

13200 Townsend Road,

Philadelphia, PA 19154

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Lannett Company, Inc.

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Olmesartan

Medically reviewed by Drugs.com on Apr 18, 2023. Written by Cerner Multum.

What is olmesartan?

Olmesartan is an angiotensin II receptor blocker (sometimes called an ARB).

Olmesartan is used to treat high blood pressure (hypertension) in adults and children at least 6 years old. It is sometimes given together with other blood pressure medications.

Olmesartan may also be used for purposes not listed in this medication guide.

Warnings

Do not use if you are pregnant. Stop using olmesartan and tell your doctor right away if you become pregnant.

If you have diabetes, do not take olmesartan with any medication that contains aliskiren (a blood pressure medicine).

Related/similar drugs

Before taking this medicine

You should not take olmesartan if you are allergic to it.

If you have diabetes, do not use olmesartan together with any medication that contains aliskiren (a blood pressure medicine).

You may also need to avoid taking olmesartan with aliskiren if you have kidney disease.

Tell your doctor if you have ever had:

• a heart condition other than one being treated with olmesartan;
• kidney disease; or
• if you are on a low salt diet.

Do not use if you are pregnant. Stop using the medicine and tell your doctor right away if you become pregnant. Olmesartan can cause injury or death to the unborn baby if you take the medicine during your second or third trimester.

If you plan to get pregnant, ask your doctor for a safer medicine to use before and during pregnancy. Having high blood pressure during pregnancy may cause complications in the mother and the baby.

You should not breastfeed while using olmesartan.

How should I take olmesartan?

Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose. Use the medicine exactly as directed.

You may take olmesartan with or without food.

For a child who cannot swallow a tablet whole, a pharmacist can mix the medicine into a liquid.

Shake the liquid before you measure a dose. Use the dosing syringe provided, or use a medicine dose-measuring device (not a kitchen spoon).

Olmesartan doses are based on weight in children and/or teenagers. Your child’s dose needs may change if the child gains or loses weight.

Call your doctor if you are sick with vomiting or diarrhea, or if you are sweating more than usual. You can easily become dehydrated while taking olmesartan.

It may take up to 2 weeks before your blood pressure is under control. Keep using this medicine as directed, even if you feel well. High blood pressure often has no symptoms.

You may need to use blood pressure medicine for the rest of your life. Treatment may also include diet, exercise, lowering cholesterol, not smoking, and controlling diabetes.

Your blood pressure will need to be checked often. Your kidney function may also need to be checked.

Store tablets at room temperature away from moisture and heat.

Store the liquid in a refrigerator. Throw away any liquid leftover after 4 weeks.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include fast heartbeats or fainting.

What should I avoid while taking olmesartan?

Do not use potassium supplements or salt substitutes, unless your doctor has told you to.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy.

Olmesartan side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Olmesartan may cause serious side effects. Call your doctor at once if you have:

• a light-headed feeling, like you might pass out;
• little or no urination;
• severe diarrhea and weight loss; or
• high potassium level–nausea, weakness, tingly feeling, chest pain, irregular heartbeats, loss of movement.

Common side effects of olmesartan may include:

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Olmesartan dosing information

Usual Adult Dose for Hypertension:

20 mg orally once a day; may increase dose to 40 mg in two weeks if further blood pressure reduction is needed.

Maximum dose: 40 mg orally once a day

Usual Pediatric Dose for Hypertension:

6 to 16 years:
-20 to less than 35 kg: 10 mg orally once a day; may increase dose to 20 mg in two weeks if further blood pressure reduction is needed
-35 kg or more: 20 mg orally once a day; may increase dose to 40 mg in two weeks if further blood pressure reduction is needed

What other drugs will affect olmesartan?

If you take colesevelam, take your olmesartan dose 4 hours before you take colesevelam.

Tell your doctor about all your other medicines, especially:

• lithium;
• a diuretic (water pill) or other medicines that lower blood pressure; or
• NSAIDs (nonsteroidal anti-inflammatory drugs)–aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve), celecoxib, diclofenac, indomethacin, meloxicam, and others.

This list is not complete. Other drugs may affect olmesartan, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

More about olmesartan

• Check interactions
• Compare alternatives
• Pricing & coupons
• Reviews (191)
• Drug images
• Side effects
• Dosage information
• During pregnancy
• Drug class: angiotensin receptor blockers
• Breastfeeding
• En español

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