Olmesartan, sold under the brand name Benicar among others, is a

medication Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to medical diagnosis, diagnose, cure, treat, or preventive medicine, prevent disease. Drug therapy (pharmaco ...

used to treat high blood pressure (

hypertension Hypertension, also known as high blood pressure, is a Chronic condition, long-term Disease, medical condition in which the blood pressure in the artery, arteries is persistently elevated. High blood pressure usually does not cause symptoms i ...

). It is taken

orally The word oral may refer to: Relating to the mouth * Relating to the mouth, the first portion of the alimentary canal that primarily receives food and liquid **Oral administration of medicines ** Oral examination (also known as an oral exam or oral ...

(swallowed by mouth). Versions are available as the combination

olmesartan/hydrochlorothiazide Olmesartan/hydrochlorothiazide, sold under the brand name Benicar HCT among others, is a fixed-dose combination medication used to treat high blood pressure. It is a combination of olmesartan medoxomil, an angiotensin II receptor blocker and h ...

and

olmesartan/amlodipine Amlodipine/olmesartan, sold under the brand name Azor, among others is a fixed-dose combination medication used to treat high blood pressure. It contains amlodipine, as the besilate, a dihydropyridine calcium channel blocker Calcium channel ...

. It is available as a prodrug, olmesartan medoxomil. Common side effects include dizziness,

headaches A headache, also known as cephalalgia, is the symptom of pain in the face, head, or neck. It can occur as a migraine, tension-type headache, or cluster headache. There is an increased risk of depression in those with severe headaches. Head ...

diarrhea Diarrhea (American English), also spelled diarrhoea or diarrhœa (British English), is the condition of having at least three loose, liquid, or watery bowel movements in a day. It often lasts for a few days and can result in dehydration d ...

, and back pain. Serious side effects may include

kidney problems Kidney failure, also known as renal failure or end-stage renal disease (ESRD), is a medical condition in which the kidneys can no longer adequately filter waste products from the blood, functioning at less than 15% of normal levels. Kidney fa ...

low blood pressure Hypotension, also known as low blood pressure, is a cardiovascular condition characterized by abnormally reduced blood pressure. Blood pressure is the force of blood pushing against the walls of the arteries as the heart pumps out blood and is ...

, and

angioedema Angioedema is an area of swelling (edema) of the lower layer of skin and tissue just under the skin or mucous membranes. The swelling may occur in the face, tongue, larynx, abdomen, or arms and legs. Often it is associated with hives, which are ...

. Use in

pregnancy Pregnancy is the time during which one or more offspring gestation, gestates inside a woman's uterus. A multiple birth, multiple pregnancy involves more than one offspring, such as with twins. Conception (biology), Conception usually occurs ...

may harm the fetus and use when

breastfeeding Breastfeeding, also known as nursing, is the process where breast milk is fed to a child. Infants may suck the milk directly from the breast, or milk may be extracted with a Breast pump, pump and then fed to the infant. The World Health Orga ...

is not recommended. It is an

angiotensin II receptor antagonist Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin II receptor antagonists, or AT1 receptor antagonists, are a group of pharmaceuticals tha ...

and works by blocking the effects of

angiotensin II Angiotensin is a peptide hormone that causes vasoconstriction and an increase in blood pressure. It is part of the renin–angiotensin system, which regulates blood pressure. Angiotensin also stimulates the release of aldosterone from the ...

. It was patented in 1991 and came into medical use in 2002. It is available as a

generic medication A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active ch ...

. In 2022, it was the 97th most commonly prescribed medication in the United States, with more than 6million prescriptions.

Medical uses

In the United States, olmesartan is

indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ...

for the treatment of hypertension in people aged six years of age and older to lower blood pressure. Olmesartan is used for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Contraindications

Contraindication In medicine, a contraindication is a condition (a situation or factor) that serves as a reason not to take a certain medical treatment due to the harm that it would cause the patient. Contraindication is the opposite of indication, which is a rea ...

s for treatment with olmesartan include

biliary obstruction A bile duct is any of a number of long tube-like structures that carry bile, and is present in most vertebrates. The bile duct is separated into three main parts: the fundus (superior), the body (middle), and the neck (inferior). Bile is requ ...

. Another major contraindication is pregnancy; reports in the scientific literature reveal fetal malformations for pregnant women taking sartan-derived drugs.

Adverse effects

The US

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respo ...

(FDA) has determined that the benefits of olmesartan continue to outweigh its potential risks when used for the treatment of people with high blood pressure according to the drug label. The incidence of adverse effects with olmesartan is reported as similar to placebo; the only adverse effect that occurred in >1% of patients treated with it and more frequently than placebo was

dizziness Dizziness is an imprecise term that can refer to a sense of disorientation in space, vertigo, or lightheadedness. It can also refer to Balance disorder, disequilibrium or a non-specific feeling, such as giddiness or foolishness. Dizziness is a ...

(3% vs 1%). Rarely, olmesartan can cause severe

gastrointestinal issues The gastrointestinal tract (GI tract, digestive tract, alimentary canal) is the tract or passageway of the digestive system that leads from the mouth to the anus. The tract is the largest of the body's systems, after the cardiovascular system. T ...

. The symptoms, which include nausea, vomiting, diarrhea, weight loss, and

electrolyte abnormalities Electrolyte imbalance, or water-electrolyte imbalance, is an abnormality in the concentration of electrolytes in the body. Electrolytes play a vital role in maintaining homeostasis in the body. They help to regulate heart and neurological function ...

, are common among those who have

celiac disease Coeliac disease (British English) or celiac disease (American English) is a long-term autoimmune disorder, primarily affecting the small intestine. Patients develop intolerance to gluten, which is present in foods such as wheat, rye, spel ...

. Recent studies suggested this form of sprue-like

enteropathy Enteropathy refers to any pathology of the intestine. Although enteritis specifically refers to an inflammation of the intestine, and is thus a more specific term than "enteropathy", the two terms are sometimes used interchangeably. __TOC__ Types ...

could be caused by the inhibition of

TGF-β Transforming growth factor beta (TGF-β) is a multifunctional cytokine belonging to the transforming growth factor superfamily that includes three different mammalian isoforms (TGF-β 1 to 3, HGNC symbols TGFB1, TGFB2, TGFB3) and many other ...

, a polypeptide cytokine that maintains intestinal

homeostasis In biology, homeostasis (British English, British also homoeostasis; ) is the state of steady internal physics, physical and chemistry, chemical conditions maintained by organism, living systems. This is the condition of optimal functioning fo ...

. However, it is still unclear why this action was never observed with other ARBs. In studies of angiotensin II receptor antagonists such as olmesartan, patients with unilateral or bilateral

renal artery stenosis Renal artery stenosis (RAS) is the narrowing of one or both of the renal arteries, most often caused by atherosclerosis or fibromuscular dysplasia. This narrowing of the renal artery can impede blood flow to the target kidney, resulting in r ...

, increases in

serum creatinine Creatinine (; ) is a breakdown product of creatine phosphate from muscle and protein metabolism. It is released at a constant rate by the body (depending on muscle mass). Biological relevance Serum creatinine (a blood measurement) is an impor ...

or blood urea nitrogen 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.

Chemistry

Olmesartan medoxomil, an ester

prodrug A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be ...

, is completely and rapidly

hydrolyzed Hydrolysis (; ) is any chemical reaction in which a molecule of water breaks one or more chemical bonds. The term is used broadly for substitution, elimination, and solvation reactions in which water is the nucleophile. Biological hydrolysi ...

to its active acid form, olmesartan. Olmesartan medoxomil metabolism

History

It was patented in 1991 and came into medical use in 2002.

Society and culture

Brand names

Olmesartan and Sevikar HCT combined is marketed worldwide by

Daiichi Sankyo is a global pharmaceutical company and the second-largest pharmaceutical company in Japan. It achieved JPY 1,278 billion in revenue in 2022. The company owns the American pharmaceutical company American Regent. Daiichi Sankyo, Inc. (DSI) began ...

, in India by Abbott Healthcare Pvt. Ltd. under the trade name WinBP, by Zydus Cadila under the trade name Olmy, by Ranbaxy Laboratories Ltd. under the trade name Olvance, Olsar by Unichem Laboratories and in Canada by Schering-Plough as Olmetec. The marketing rights to the brand names Benicar, Benicar HCT, Azor, and Tribenzor in the United States were transferred from Daiichi Sankyo to Cosette in January 2022. Several preparations containing olmesartan and other antihypertensives are available. Teva Pharmaceuticals produces a formulation containing olmesartan,

amlodipine Amlodipine, sold under the brand name Norvasc among others, is a calcium channel blocker medication used to treat hypertension, high blood pressure, coronary artery disease (CAD) and variant angina (also called Prinzmetal angina or coronary ar ...

, and

hydrochlorothiazide Hydrochlorothiazide, sold under the brand name Hydrodiuril among others, is a diuretic medication used to treat hypertension and swelling due to fluid build-up. Other uses include treating diabetes insipidus and renal tubular acidosis and t ...

. Benicar HCT is the brand name of a medication containing olmesartan medoxomil with hydrochlorothiazide. Benitec H, another medication containing olmesartan medoxomil and hydrochlorothiazide, is marketed by GlaxoSmithKline in India.

Research

Olmesartan has demonstrated potential benefits in reducing the progression of atherosclerotic buildup in arteries. In large randomized placebo-controlled or active drug-controlled studies conducted in participants with hypertension, stable angina, or type 2 diabetes, long-term treatment with olmesartan has been shown to reduce the levels of markers of vascular inflammation. This effect was also observed in a high-cholesterol primate test model.

References

{{Authority control Angiotensin II receptor antagonists Imidazoles Tetrazoles Carboxylate esters Tertiary alcohols Biphenyls 1995 in biotechnology Daiichi Sankyo Drugs developed by Merck & Co. Wikipedia medicine articles ready to translate