Olmesartan medoxomil is a selective angiotensin II receptor antagonist (AT1 subtype). It is a prodrug, which is hydrolyzed to olmesartan during absorption from the gastrointestinal tract. 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 AT1 receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis.  Pharmacokinetics: Absorption: Olmesartan medoxomil is rapidly and completely bioactivated by ester hydrolysis to olmesartan during absorption from the gastrointestinal tract. The absolute bioavailability of olmesartan is approximately 26%. After oral administration, the peak plasma concentration (Cmax) of olmesartan is reached after 1 to 2 hour. Distribution: The volume of distribution is approximately 17 L. Olmesartan is highly bound to plasma proteins (99%). 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. Its terminal elimination half-life is approximately 13 hours.



    Presulock 20 tablet: Each film coated tablet contains Olmesartan Medoxomil BP 20 mg.


    Presulock is an angiotensin II receptor blocker (ARB) indicated for the treatment of hypertension, alone or with other antihypertensive agents, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarction.

Dosage & Administration

    Adult Hypertension:

    Starting dose: 20 mg Presulock once daily.
    Dose range: 20-40 mg Presulock once daily.

    Pediatric Hypertension(6-16 years):

    Starting dose:
    20 to <35 kg: 10 mg Presulock once daily
    >=35 kg: 20 mg Presulock once daily
    Dose range:
    20 to <35 kg: 10-20 mg Presulock once daily
    >=35 kg : 20-40 mg Presulock once daily


    Olmesartan is contraindicated in patients who are hypersensitive to any component of this product. Co-administration of aliskiren with olmesartan is contraindicated.

Warning & Precautions

Side effects

    Treatment with olmesartan was well tolerated, with an incidence of adverse events similar to placebo. The following adverse events occurred in placebo-controlled clinical trials at an incidence of more than 1% of patients treated with olmesartan, but also occurred at about the same or greater incidence in patients receiving placebo: back pain, bronchitis, creatine phosphokinase increased, diarrhea, headache, hematuria, hyperglycemia, hypertriglyceridemia, influenza-like symptoms, pharyngitis, rhinitis and sinusitis.
    Other potentially important adverse reactions that have been reported with an incidence of greater than 0.5% are: chest pain, peripheral edema, vertigo, abdominal pain, dyspepsia, gastroenteritis, nausea, tachycardia, hypercholesterolemia, anthralgia, arthritis, myalgia, rash. Facial edema can rarely occur.

Drug interaction

    No significant drug interactions were reported in studies in which olmesartan 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.
    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-admininstration 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.
    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.
    Colesevelam hydrochloride: Concurrent administration of bile acid sequestering agent colesevelam hydrochloride reduces the systemic exposure and peak plasma concentration of olmesartan.
    Lithium: Increases in serum lithium concentrations and lithium toxicity have been reported during concomitant administration of lithium with angiotensin II receptor antagonists, including olmesartan.

Use in special groups

    Pregnancy & Lactation: Pregnancy catagory D. 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.
    Pediatric Use: Generally well tolerated in pediatric patients (6-16 years of age) and the adverse events are similar to that described for adult patients.
    Elderly: No initial dosage adjustment is required.
    Renal Impairment: No initial dosage adjustment is recommended for patients with moderate to marked renal impairment (creatinine clearance <40 mL/min).
    Hepatic Impairment: No initial dosage adjustment is recommended for patients with moderate to marked hepatic dysfunction.


    Presulock 20 tablet: Each box contains 30 tablets in alu-alu blister pack.