Olmesartan medoxomil

Olmesartan medoxomil
ATC Code C09CA08
Formula C24H26N6O3
Molar Mass (g·mol−1) 446,50
Physical State solid
Melting Point (°C) 180–182
PKS Value 4.3
CAS Number 144689-24-7
PUB Number 158781
Drugbank ID DB00275
Solubility practically insoluble in water, slightly soluble in methanol

Basics

Olmesartan is a drug in the group of antihypertensives (drugs against high blood pressure). Within this group, it belongs to the AT1 antagonists, which are also called sartans. It is used to treat high blood pressure. In its pure form it cannot be absorbed by the body, which is why it is administered in the form of its resorption ester olmesartan medoxomil. The most common dosage form is the tablet. Olmesartan is available only on prescription.

Pharmacology

Pharmacodynamics

The effect is due to the blockade of the AT1 receptor. The hormone angiotensin II normally binds to this receptor, increasing blood pressure. Olmesartan competitively inhibits the receptor, reducing the frequency with which angiotensin II binds to AT1, resulting in a decrease in blood pressure. In addition, olmesartan also shows beneficial effects on renal function and also possesses antisclerotic properties, which has additional beneficial effects on blood pressure and the cardiovascular system.

Pharmacokinetics

Olmesartan is administered in the form of its prodrug olmesartan medoxomil, which in its pure form is not absorbed by the body. It is converted to the active form during the first liver passage. Thus, the bioavailability is about 26%. The maximum plasma concentration is reached after 1-3 hours and plasma protein binding is about 99%. The degradation of olmesartan is not catalyzed by the enzymes of the CYP450 system, which significantly reduces the likelihood of interactions with other drugs. A large proportion of the given dose is excreted unchanged in the faeces. The plasma half-life is 10-15 hours.

Drug Interactions

Drug interactions occur mainly in association with other antihypertensive drugs. As a result, the antihypertensive effect may be too strong, which may have life-threatening consequences. Acetylsalicylic acid may damage the kidneys when used together. Antacids can lower the serum concentration of olmesartan and thus weaken its effect. In rare cases, olmesartan may increase the concentration of lithium to toxic levels.

Toxicity

Side effects

Typical side effects include:

  • Hypertriglyceridemia
  • Dizziness
  • Headache
  • Fatigue
  • Gastrointestinal complaints
  • Arthritis, back and skeletal pain
  • Chest pain and others
  • Respiratory infections and flu-like symptoms
  • Hematuria
  • Peripheral edema
  • Elevation of liver enzymes, urea, and creatine phosphokinase in the blood

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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