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OLMESAVA 40

Quick Overview

Our aim is to reach out to the globe within shortest possible time frame


To promote this objective, not only we distribute and market our  Cardiovascular range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as Olmesava 40 which  contains Olmesartan Medoxomil 40 mg .


This Olmisava 40 contains same active ingredient as Benicar from Daiichi Sankyo

OLMESAVA 40

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Details

 OLMESAVA 40

Each filnn-coated tablet contains:

Olmesartan Medoxomil ....40 mg

Excipients          q.s

Colour: Titanium Dioxide BP

CHEMICAL NAME: 2,3-dihydroxy-2-butenyl 4(1-hydroxy-1- methylethyl)- 2 - p ro p yl - 1-[p- (o-1 H-tetrazol-5 - ylphenyl)benzyl]imidazole5-carboxylate, cyclic 2,3- carbonate

CATEGORY: Antihypertensive

DESCRIPTION:

OLMESAVA 40: White to off white round biconvex film coated tablet plain on both side.

CLINICAL PHARMACOLOGY

Pharmacokinetic Actions

Absorption

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

Distribution

The reported 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. Olmesartan passed across the placental barrier in rats and was distributed to the fetus. Olmesartan was distributed to milk at low levels in rats.

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 LA. Approximately 35% to 50% of the absorbed dose is recovered in urine while the remainder is eliminated in feces via the bile. 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 upto 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.

Geriatric

The pharmacokinetics of olmesartan was studied in the elderly ( 65 years). Overall, maximum plasma concentrations of olmesartan were similar in young adults and the elderly. Modest accumulation of olmesartan was observed in the elderly with repeated dosing; AUCs, t1/2 was 33% higher in elderly patients.

Pediatric

The pharmacokinetics of olmesartan was reported in pediatric hypertensive patients aged 1 to16 years. The

clearance of olnnesartan in pediatric patients was similar to that in adult patients when adjusted by the body weight.

Gender

Minor differences were observed in the pharmacokinetics of olmesartan in women compared to men. AUC and Cmax were 10-15% higher in women than in men.

MECHANISM OF ACTION:

Angiotensin ll is formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II). Angiotensin ll 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 ll by selectively blocking the binding of angiotensin ll to the AT1 receptor in vascular smooth muscle. Its action is, therefore, independent of the pathways for angiotensin ll 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 receptorthan for the AT2 receptor.

Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin ll from angiotensin I, is a mechanism of many drugs used to treat hypertension. Blockade of the angiotensin ll receptor inhibits the negative regulatory feedback of angiotensin ll on renin secretion, but the resulting increased plasma renin activity and circulating angiotensin ll levels do not overcome the effect of olmesartan on blood pressure.

INDICATIONS

Olmesartan medoxomil is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

CONTRAINDICATIONS None.

WARNING:

AVOID USE IN PREGNANCY

Fetal/Neonatal Morbidity and Mortality: When pregnancy is detected, discontinue olnnesartan medoxomil as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. Drugs that act directly on the renin-angiotensin system can cause fetal and neonatal morbidity and death when administered to pregnant women. Several dozen cases have been reported in the world literature of patients who were taking angiotensin converting enzyme inhibitors. When pregnancy is detected, discontinue olmesartan medoxomil as soon as possible.

The use of drugs that act directly on the renin-angiotensin system during the second and third trimesters of pregnancy has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure and death. Oligohydramnios has also been reported, presumably resulting from decreased fetal function; oligohydramnios in this setting has been associated with fetal limb contractures, craniofacial deformation and hypoplastic lung development.

Mothers whose embryos and fetuses are exposed to an angiotensin ll receptor antagonist only during the first trimester should be so informed. Nonetheless, when patients become pregnant, physicians should ask the patient to discontinue the use of olmesartan medoxomil as soon as possible.

Hypotension in Volume- or Salt-Depleted Patients

In patients with an activated renin-angiotensin aldosterone system, such as volume- and/or salt-depleted patients (e.g., those being treated with high doses of diuretics), symptomatic hypotension may be anticipated after initiation of treatment with olmesartan medoxomil. Initiate treatment under close medical supervision. If hypotension does occur, place the patient in the supine position and, if necessary, give an intravenous infusion of normal saline.

Impaired Renal Function

As a consequence of inhibiting the renin-angiotensin-aldosterone system, changes in renal function may be anticipated in susceptible individuals treated with olmesartan medoxomil. In patients whose renal function may depend upon the activity of the renin angiotensin-aldosterone system (e.g., patients with severe congestive heart failure), treatment with angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor antagonists has been associated with oliguria and/or progressive azotemia and rarely with acute renal failure and/or death. Similar results may be anticipated in patients treated with olmesartan medoxomil.

Use in Specific population

In reported studies of ACE inhibitors in patients with unilateral or bilateral renal artery stenosis, increases in serum creatinine or blood urea nitrogen (BUN) have been reported. There has been no long-term use of Olmesartan in patients with unilateral or bilateral renal artery stenosis, but similar results may be expected.

PREGNANCY AND LACTATION

Pregnancy

Pregnancy Categories C and D

Nursing Mothers

It is not known whether olmesartan is excreted in human milk, but olmesartan is secreted at low concentration in the milk of lactating rats. 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 accountthe importance of the drug to the mother.

Pediatric Use

Olmesartan medoxomil was generally well tolerated in pediatric patients, and the adverse experience profile was similarto that described for adults.

INTERACTIONS:

No significant drug interactions were reported in studies in which Olmesartan medoxomil was co-administered with digoxin or warfarin in healthy volunteers.

The bioavailability of olnnesartan medoxonnil was not significantly altered by the co-administration of antacids [Al(OH)3/Mg(OH)2].

Olmesartan medoxomil is not metabolized by the cytochronne 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 Cyclomgenase-2 Inhibitors (COX-2 Inhibitors).

In patients who are elderly, volume-depleted (including those on diuretic therapy) or with compromised renal function, coadministration 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. These effects are usually reversible.

Monitor renal function periodically in patients receiving olmesartan medoxomil and NSAID therapy.

The antihypertensive effect of angiotensin ll receptor antagonists, including olnnesartan medoxomil may be attenuated by NSAIDs including selective COX-2 inhibitors.

DOSAGE:

Adult Hypertension

Dosage must be individualized. The usual recommended starting dose of Olmesartan medoxomil 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 overthe 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 nnL/min) or with moderate to marked hepatic dysfunction.

 

Use in Specific Populations

For patients with possible depletion of intravascular volume (e.g., patients treated with diuretics, particularly those with impaired renal function), initiate Olnnesartan under close medical supervision and give consideration to use of a lower starting dose Olmesartan may be administered with or without food.

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

Pediatric Hypertension (610 16 years of age)

Dosage must be individualized. For children who can swallow tablets, the usual recommended starting dose of Olmesartan is 10 mg once daily for patients who weigh 20 to <35 kg (44 to 77 lb), or 20 mg once daily for patients who weigh 35 kg. For patients requiring further reduction in blood pressure after 2 weeks of therapy, the dose of Olmesartan may be increased to a maximum of 20 mg once daily for patients who weigh <35 kg or 40 mg once daily for patients who weigh 35 kg.

ADVERSE EFFECTS:

Reported events generally were mild, transient and had no relationship to the dose of Olnnesartan medoxomil.

Body as a Whole: chest pain, peripheral edema

Central and Peripheral Nervous System: Vertigo Gastrointestinal: Abdominal pain, dyspepsia, gastroenteritis, nausea

Heart Rate and Rhythm Disorders: Tachycardia

Metabolic and Nutritional Disorders: Hypercholesterolemia, hyperlipemia, hyperuricemia

Musculoskeletal: Arthralgia, arthritis, myalgia.

Skin and Appendages: Rash

Facial edema was reported in five patients receiving Olmesartan medoxomil. Angioedema has been reported with angiotensin II antagonists.

 

Reported Laboratory Test Findings

Hemoglobin and Hematocrit: Small decreases in hemoglobin and hematocrit (mean decreases of approximately 0.3 g/dL and 0.3 volume percent, respectively) were observed.

Liver Function Tests: Elevations of liver enzymes and/or serum bilirubin were observed infrequently.

OVERDOSAGE:

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.

Packing: Blister of 10 Tablets.

Storage: Store in a cool and dry place below 30°C.

Shelf Life: 24 months from the date of manufacturing.

 

 

 
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