olmesartan medoxomil

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Overview

What is olmesartan medoxomil?

Olmesartan medoxomil, a prodrug, is hydrolyzed to olmesartan during absorption from the gastrointestinal tract. Olmesartan is a selective AT subtype angiotensin II receptor antagonist.

Olmesartan medoxomil is described chemically as 2,3-dihydroxy-2-butenyl 4-(1 hydroxy-1-methylethyl)-2-propyl-1-[ -( - -tetrazol-5-ylphenyl)benzyl]imidazole-5 carboxylate, cyclic 2,3-carbonate.

Its empirical formula is C H N O and its structural formula is:

Olmesartan medoxomil is a white to light yellowish-white powder or crystalline powder with a molecular weight of 558.59. It is practically insoluble in water and sparingly soluble in methanol. Olmesartan medoxomil tablets are available for oral use as film-coated tablets containing 5 mg, 20 mg, or 40 mg of olmesartan medoxomil and the following inactive ingredients: hydroxypropyl cellulose, hypromellose, lactose monohydrate, low-substituted hydroxypropyl cellulose, magnesium stearate, microcrystalline cellulose, purified talc, titanium dioxide, and (5 mg only) iron oxide yellow.

What does olmesartan medoxomil look like?

What are the available doses of olmesartan medoxomil?

Tablets: 5 mg, 20 mg, and 40 mg .

What should I talk to my health care provider before I take olmesartan medoxomil?

How should I use olmesartan medoxomil?

Olmesartan medoxomil tablets are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including the class to which this drug principally belongs. There are no controlled trials demonstrating risk reduction with olmesartan medoxomil.

Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than one drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC).

Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly.

Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal.

Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (e.g., on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy.

It may be used alone or in combination with other antihypertensive agents.

Dosage must be individualized. The usual recommended starting dose of olmesartan medoxomil tablets is 20 mg once daily when used as monotherapy in patients who are not volume-contracted. For patients requiring further reduction in blood pressure after 2 weeks of therapy, the dose of olmesartan medoxomil may be increased to 40 mg. Doses above 40 mg do not appear to have greater effect. Twice-daily dosing offers no advantage over the same total dose given once daily.

No initial dosage adjustment is recommended for elderly patients, for patients with moderate to marked renal impairment (creatinine clearance <40 mL/min) or with moderate to marked hepatic dysfunction . For patients with possible depletion of intravascular volume (e.g., patients treated with diuretics, particularly those with impaired renal function), initiate olmesartan medoxomil under close medical supervision and give consideration to use of a lower starting dose .

Olmesartan medoxomil tablets may be administered with or without food.

If blood pressure is not controlled by olmesartan medoxomil alone, a diuretic may be added. Olmesartan medoxomil tablets may be administered with other antihypertensive agents.

What interacts with olmesartan medoxomil?

Sorry No Records found

What are the warnings of olmesartan medoxomil?

Sorry No Records found

What are the precautions of olmesartan medoxomil?

Sorry No Records found

What are the side effects of olmesartan medoxomil?

Sorry No records found

What should I look out for while using olmesartan medoxomil?

Do not co-administer aliskiren with olmesartan medoxomil tablets in patients with diabetes

What might happen if I take too much olmesartan medoxomil?

Limited data are available related to overdosage in humans. The most likely manifestations of overdosage would be hypotension and tachycardia; bradycardia could be encountered if parasympathetic (vagal) stimulation occurs. If symptomatic hypotension occurs, initiate supportive treatment. The dialyzability of olmesartan is unknown.

How should I store and handle olmesartan medoxomil?

RISPERDAL Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and moisture.RISPERDAL 1 mg/mL Oral Solution should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and freezing.RISPERDAL M-TAB Orally Disintegrating Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F).Keep out of reach of children.RISPERDAL Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and moisture.RISPERDAL 1 mg/mL Oral Solution should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and freezing.RISPERDAL M-TAB Orally Disintegrating Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F).Keep out of reach of children.RISPERDAL Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and moisture.RISPERDAL 1 mg/mL Oral Solution should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and freezing.RISPERDAL M-TAB Orally Disintegrating Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F).Keep out of reach of children.RISPERDAL Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and moisture.RISPERDAL 1 mg/mL Oral Solution should be stored at controlled room temperature 15°–25°C (59°–77°F). Protect from light and freezing.RISPERDAL M-TAB Orally Disintegrating Tablets should be stored at controlled room temperature 15°–25°C (59°–77°F).Keep out of reach of children.Product: 71335-0775NDC: 71335-0775-1 30 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-2 60 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-3 90 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-4 180 TABLET, FILM COATED in a BOTTLEProduct: 71335-0775NDC: 71335-0775-1 30 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-2 60 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-3 90 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-4 180 TABLET, FILM COATED in a BOTTLEProduct: 71335-0775NDC: 71335-0775-1 30 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-2 60 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-3 90 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-4 180 TABLET, FILM COATED in a BOTTLEProduct: 71335-0775NDC: 71335-0775-1 30 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-2 60 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-3 90 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-4 180 TABLET, FILM COATED in a BOTTLEProduct: 71335-0775NDC: 71335-0775-1 30 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-2 60 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-3 90 TABLET, FILM COATED in a BOTTLENDC: 71335-0775-4 180 TABLET, FILM COATED in a BOTTLE

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Clinical Information

Chemical Structure

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Clinical Pharmacology

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 AT receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin II synthesis.

An AT 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 AT receptor than for the AT receptor.

Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is a mechanism of many drugs used to treat hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because olmesartan medoxomil does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known.

Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and circulating angiotensin II levels do not overcome the effect of olmesartan on blood pressure.

Non-Clinical Toxicology

Do not co-administer aliskiren with olmesartan medoxomil tablets in patients with diabetes

Disulfiram

Psychotic reactions have been reported in alcoholic patients who are using metronidazole and disulfiram concurrently. Metronidazole should not be given to patients who have taken disulfiram within the last two weeks (see .

Alcoholic Beverages

Abdominal cramps, nausea, vomiting, headaches, and flushing may occur if alcoholic beverages or products containing propylene glycol are consumed during or following metronidazole therapy (see ).

Warfarin and other Oral Anticoagulants

Metronidazole has been reported to potentiate the anticoagulant effect of warfarin and other oral coumarin anticoagulants, resulting in a prolongation of prothrombin time. When metronidazole is prescribed for patients on this type of anticoagulant therapy, prothrombin time and INR should be carefully monitored.

Lithium

In patients stabilized on relatively high doses of lithium, short-term metronidazole therapy has been associated with elevation of serum lithium and, in a few cases, signs of lithium toxicity. Serum lithium and serum creatinine levels should be obtained several days after beginning metronidazole to detect any increase that may precede clinical symptoms of lithium intoxication.

Busulfan

Metronidazole has been reported to increase plasma concentrations of busulfan, which can result in an increased risk for serious busulfan toxicity. Metronidazole should not be administered concomitantly with busulfan unless the benefit outweighs the risk. If no therapeutic alternatives to metronidazole are available, and concomitant administration with busulfan is medically needed, frequent monitoring of busulfan plasma concentration should be performed and the busulfan dose should be adjusted accordingly.

Drugs that Inhibit CYP450 Enzymes

The simultaneous administration of drugs that decrease microsomal liver enzyme activity, such as cimetidine, may prolong the half-life and decrease plasma clearance of metronidazole.

Drugs that Induce CYP450 Enzymes

The simultaneous administration of drugs that induce microsomal liver enzymes, such as phenytoin or phenobarbital, may accelerate the elimination of metronidazole, resulting in reduced plasma levels; impaired clearance of phenytoin has also been reported.

Drug/Laboratory Test Interactions

Metronidazole may interfere with certain types of determinations of serum chemistry values, such as aspartate aminotransferase (AST, SGOT), alanine aminotransferase (ALT, SGPT), lactate dehydrogenase (LDH), triglycerides, and glucose hexokinase. Values of zero may be observed. All of the assays in which interference has been reported involve enzymatic coupling of the assay to oxidation-reduction of nicotinamide adenine dinucleotide (NADNADH). Interference is due to the similarity in absorbance peaks of NADH (340 nm) and metronidazole (322 nm) at pH 7.

Pregnancy Category D

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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