Olmesartan medoxomil is an ester prodrug for olmesartan. It is hydrolysed to olmesartan during absorption from the GI tract. Olmesartan is a selective and competitive angiotensin II Type 1 (AT1) receptor antagonist and hence it blocks the vasocontrictor and aldosterone-secreting effects of angiotensin II.

Absorption: Bioavailability: About 26%. Tmax: Reached within 1-2 hr.
Distribution: Distribution: Vd: 17 L; protein binding: 99%.
Metabolism: Olmesartan medoxomil is hydrolysed in the GI tract to Olmesartan during absorption.
Excretion: Excreted as Olmesartan in faeces via the bile (50-65%) and in urine (35-50%). Terminal elimination half-life: About 13 hr.

Used to treat hypertension.

Dizziness, headache, abdominal pain, dyspepsia, diarrhoea, gastroenteritis, nausea, chest pain, bronchitis, cough, pharyngitis, rhinitis, arthritis, back pain, fatigue, flu-like symptoms, hypotension, peripheral oedema, haematuria, UTI, hyperkalaemia, hypertriglyceridemia, hyperuricaemia, elevated liver enzymes, facial edema, angioedema, and rhabdomyolysis.
Potentially Fatal: Acute renal failure.

Overdosage: Symptoms: Hypotension and tachycardia; bradycardia may occur if there is vagal stimulation. Treatment: Dialysability of Olmesartan Medoxomil is unknown; provide symptomatic and supportive therapy.

Drugs that act on renin-angiotensin system can cause fetal injury and death when used in 2nd and 3rd trimesters of pregnancy. Olmesartan medoxomil should be discontinued as soon as possible once pregnancy is detected. Symptomatic hypotension may occur in patients who are volume- and/or salt-depleted. May be associated with oliguria, progressive azotaemia, and acute renal failure (rare). Patients with bilateral or unilateral renal artery stenosis may have increased risk of severe hypotension and renal insufficiency. Caution in renal impairment; monitor serum creatinine and potassium levels periodically. Avoid use in severe renal impairment (CrCl< 20 mL/min) and severe hepatic impairment. Caution in patients with aortic or mitral valve stenosis, obstructive hypertrophic cardiomyopathy. Patients with primary aldosteronism may not respond to angiotensin receptor antagonist. Not recommended in lactation.

Concurrent use with ACE inhibitors, potassium-sparing diuretics, potassium salts, and drugs that may increase serum potassium (e.g. ciclosporin, eplerenone) may increase the risk of hyperkalaemia. Concomitant use with NSAIDs may decrease glomerular filtration synergistically; acute renal failure may occur. Increased serum concentrations of lithium  and toxicity when used with angiotensin receptor antagonist have been reported; avoid concomitant use of lithium and Olmesartan medoxomil.

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Adult: Initial: 10-20 mg once daily. Antihypertensive effect is substantially present within 2 wk of therapy initiation. Dose may be increased up to 40 mg once daily if needed. May consider a lower starting dose in patients with possible depletion of intravascular volume (e.g. patients receiving concomitant diuretics, especially those with renal impairment).
Child: 6 to 16 yr: 20-35 kg: 10 mg once daily, may increase to maximum of 20 mg once daily. ≥35 kg: 20 mg once daily, may increase to maximum of 40 mg once daily.
Elderly: May consider lower starting dose of 5-10 mg daily.

May be taken with or without food

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Pregnancy (2nd and 3rd trimesters); biliary obstruction

Oral: Store at 20-25°C

Increased creatine phosphokinase