Overview

Olmesartan Medoxomil belongs to a group of medicines called angiotensin-II receptor antagonists. They lower blood pressure by relaxing the blood vessels. Olmesartan Medoxomil are used for the treatment of high blood pressure (also known as ‘hypertension’) in adults and in children and adolescents aged 6 to less than 18 years. High blood pressure can damage blood vessels in organs such as the heart, kidneys, brain and eyes. In some cases this may lead to a heart attack, heart or kidney failure, stroke or blindness. Usually high blood pressure has no symptoms. It is important to have your blood pressure checked to prevent damage occurring.High blood pressure can be controlled with medicines such as Olmesartan Medoxomil.

Indication:

Treatment of hypertension in children and adolescents from 6 to less than 18 years of age.

Side Effects

Back pain

Bronchitis

Diarrhea

Headache

Blood in your urine

High blood sugar

High triglycerides

flu-like symptoms, such as fever and body aches

Pharmacology :

Mechanism of Action

Olmesartan medoxomil, a prodrug, is hydrolyzed to olmesartan during absorption from the gastrointestinal tract. Olmesartan is a selective AT1 subtype angiotensin II receptor antagonist. Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II). Angiotensin II is the principal press or 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 AT1 receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis. An AT2 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 AT1 receptor than for the AT2 receptor.
Olmesartan medoxomil inhibits the pressor effect of an angiotensin II infusion in a dosedependent manner at doses of 2.5 to 40 mg. The inhibition was 90% at doses of olmesartan medoxomil > 40 mg 24 hours post dose. Plasma concentrations of angiotensin I and angiotensin II and plasma renin activity (PRA) increased 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.

Pharmacodynamics

Pharmacokinetics Properties:

Absorption: Olmesartan medoxomil is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. 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 absolute bioavailability of olmesartan is approximately 26%. After oral administration, the peak plasma concentration (Cmax) of olmesartan is reached after 1 to 2 hours. Food does not affect the bioavailability of olmesartan.

Distribution: 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.

Metabolism & Excretion: 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.

Pregnancy & breast-feeding Olmesartan Medomoxil Tablets is not recommended in early pregnancy, and must not be taken when more than 3 months pregnant, as it may cause serious harm to your baby if used after the third month of pregnancy.
Breast-feeding if you are breast-feeding or about to start breast-feeding. Olmesartan Medomoxil tablets is not recommended for mothers who are breast-feeding, and your doctor may choose another treatment for you if you wish to breast-feed, especially if your baby is newborn, or was born prematurely. Ask your doctor or pharmacist for advice before taking any medicine.