In controlled clinical trials, clinically important changes in standard laboratory parameters were rarely associated with administration of Benicar. Small decreases in hemoglobin and hematocrit mean decreases of approximately 0. Of the five Benicar patients, three had elevated transaminases, which were attributed to alcohol use, and one had a single elevated bilirubin value, which normalized while treatment continued.
Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Asthenia, angioedema, anaphylactic reactions Gastrointestinal: Vomiting, sprue-like enteropathy [see Warnings and Precautions 5. Acute renal failure, increased blood creatinine levels Skin and Appendages: Alopecia, pruritus, urticaria Data from one controlled trial and an epidemiologic study have suggested that high-dose olmesartan may increase cardiovascular CV risk in diabetic patients, but the overall data are not conclusive.
The trial met its primary endpoint, delayed onset of microalbuminuria, but olmesartan had no beneficial effect on decline in glomerular filtration rate GFR. There was a finding of increased CV mortality adjudicated sudden cardiac death, fatal myocardial infarction, fatal stroke, revascularization death in the olmesartan group compared to the placebo group 15 olmesartan vs.
In contrast, high-dose olmesartan use in non-diabetic patients appeared to be associated with a decreased risk of death HR 0. Overall, these data raise a concern of a possible increased CV risk associated with the use of high-dose olmesartan in diabetic patients.
There are, however, concerns with the credibility of the finding of increased CV risk, notably the observation in the large epidemiologic study for a survival benefit in non-diabetics of a magnitude similar to the adverse finding in diabetics. Olmesartan medoxomil is not metabolized by the cytochrome P system and has no effects on P 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-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. 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.
Most patients receiving the combination of two RAS inhibitors do not obtain any additional benefit compared to monotherapy. In general, avoid combined use of RAS inhibitors. Do not co-administer aliskiren with Benicar in patients with diabetes [see Contraindications 4 ]. Lithium Increases in serum lithium concentrations and lithium toxicity have been reported during concomitant administration of lithium with angiotensin II receptor antagonists, including Benicar.
Monitor serum lithium levels during concomitant use. When pregnancy is detected, discontinue Benicar as soon as possible. These adverse outcomes are usually associated with use of these drugs in the second and third trimester of pregnancy. Appropriate management of maternal hypertension during pregnancy is important to optimize outcomes for both mother and fetus. In the unusual case that there is no appropriate alternative to therapy with drugs affecting the renin-angiotensin system for a particular patient, apprise the mother of the potential risk to the fetus.
Perform serial ultrasound examinations to assess the intra-amniotic environment. If oligohydramnios is observed, discontinue Benicar, unless it is considered lifesaving for the mother. Fetal testing may be appropriate, based on the week of pregnancy.
Patients and physicians should be aware, however, that oligohydramnios may not appear until after the fetus has sustained irreversible injury. Closely observe infants with histories of in utero exposure to Benicar for hypotension, oliguria, and hyperkalemia [see Use in Specific Populations 8. 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.
If oliguria or hypotension occurs, direct attention toward support of blood pressure and renal perfusion. The renin-angiotensin aldosterone system RAAS plays a critical role in kidney development. RAAS blockade has been shown to lead to abnormal kidney development in very young mice. Administering drugs that act directly on the renin- angiotensin aldosterone system RAAS can alter normal renal development.
No overall differences in effectiveness or safety were observed between elderly patients and younger patients. 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. Olmesartan is a selective AT1 subtype angiotensin II receptor antagonist. Olmesartan medoxomil is described chemically as 2,3-dihydroxybutenyl 4- 1-hydroxymethylethyl propyl[p- o-1H-tetrazolylphenyl benzyl]imidazolecarboxylate, cyclic 2,3-carbonate.
Its empirical formula is C29H30N6O6 and its structural formula is: Olmesartan medoxomil is a white to light yellowish-white powder or crystalline powder with a molecular weight of It is practically insoluble in water and sparingly soluble in methanol. Benicar is available for oral use as film-coated tablets containing 5 mg, 20 mg, or 40 mg of olmesartan medoxomil and the following inactive ingredients: 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.
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,fold greater affinity for the AT1 receptor than for the AT2 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. 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.
Plasma concentrations of angiotensin I and angiotensin II and plasma renin activity PRA increase after single and repeated administration of Benicar to healthy subjects and hypertensive patients. Repeated administration of up to 80 mg Benicar had minimal influence on aldosterone levels and no effect on serum potassium. Food does not affect the bioavailability of olmesartan. Distribution The volume of distribution of olmesartan is approximately 17 L.
The protein binding is constant at plasma olmesartan concentrations well above the range achieved with recommended doses.
In rats, olmesartan crossed the blood-brain barrier poorly, if at all. 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. Olmesartan shows linear pharmacokinetics following single oral doses of up to 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. Overall, maximum plasma concentrations of olmesartan were similar in young adults and the elderly. Angiotensin is used by the human body as a blood pressure elevator.
Angiotensin acts as a powerful vasoconstrictor it causes your blood vessels to tighten up thereby reducing their inner diameter. When your body needs to ratchet up blood pressure, such as during periods of exercise or stress your body releases a tiny amount of angiotensin.
Think of it this way: What would happen if all of a sudden, the hose's diameter shrunk down to the width of a drinking straw?
The pressure would increase! Angiotensin receptor blockers form a protective shield on the blood vessels so that angiotensin's ability to tighten up your blood vessels is reduced.
If the angiotensin can't do it's job the blood vessels remain in a relaxed state and blood pressure remains low. How can you make angiotensin receptor blocking agents stronger? Combination with diuretics In and of themselves, ARB's are not terribly potent.
However, when you add a water-pill into the mix, the blood-pressure lowing effect of the ARB is greatly enhanced. For this reason, all of the ARB's are available as a combination pill that contains the ARB plus a small dose of water pill usually hydrochlorthiazide. Sometimes doctors do this anyway if they feel that a patient's blood pressure needs to be managed rapidly and the benefits outweigh the risks.
Because Atacand is an expensive and popular drug, some internet pharmacies discount it to get you in the door:
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