Olmesartan Medoxomil

For the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Angiotensin Receptor Blocker

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 1 receptor in vascular smooth muscle. An AT 2 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 1 receptor than for the AT 2 receptor. Olmesartan medoxomil does not inhibit ACE (kininase II), it does not affect the response to bradykinin. 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.

Dosage must be individualized. The usual recommended starting dose of Olmesartan 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 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 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. 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 Drugs (NSAIDs) 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-administration 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 II receptor antagonists, including olmesartan medoxomil may be attenuated by NSAIDs including selective COX-2 inhibitors.

Olmesartan is contraindicated in patients who are hypersensitive to any component of this product.

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 & sinusitis.

Pregnancy Categories: 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 account the importance of the drug to the mother. Use in Children: Safety & Effectiveness in pediatric patients have not been established.

There is no experience of overdose with Olmesartan. The most likely effects of olmesartan medoxomil overdosage are hypotension and tachycardia; bradycardia could be encountered if parasympathetic (vagal) stimulation occurred. If intake is recent, gastric lavage or induction of emesis may be considered. Clinically significant hypotension due to an overdose of Olmesartan requires the active support of the cardiovascular system, including close monitoring of heart and lung function, the elevation of the extremities, and attention to circulating fluid volume and urine output.

Store in cool & dry place below 30ºC, protect from light & moisture. Keep out of the reach of children.