Note: Olmesartan medoxomil is known by several different names (see below). Throughout this site, for convenience, it is referred to by the brand name Benicar, the registered name used by its manufacturer Sankyo in the U.S.
Benicar® is a brand name prescription drug marketed by the Japanese pharmaceutical company Daiichi Sankyo. The patent will expire on April 25, 2016. It was approved in 2002 by the FDA to treat high blood pressure. The active ingredient in Benicar is olmesartan medoximil which is an Angiotensin Receptor Blocker (ARB). This class of drugs blocks off the receptors for angiotensin II (a hormone) which exist in inflamed tissues and elsewhere throughout the body. See this article for details about ARBs.
ARBs are commonly used to treat high blood pressure, heart failure, and kidney disease from diabetes because ARBs block the effect of angiotensin II, that can exacerbate these conditions.
Other medications in this class include:
Basic pharmacology studies tell us that they are not the same. Although all bind the receptor for angiotensin II, and block the effect of the hormone but they vary in their fit with the receptor, how long they last in the body, how they are handled by the body and what doses should be taken. Thus, they may have differing effects in the body.
"...the medoxomil-ester prodrug is rapidly and completely converted to its pharmacologically active form in the gastrointestinal mucosa, portal blood, and liver before it comes into systemic circulation."
Benicar is a unique ARB
Benicar plays a key role in the recovery process. Benicar is the only ARB we have noted to effectively result in Herxheimer reactions when taken according to Inflammation Therapy guidelines. We don't recommend using any other ARB for this purpose.
Other applications for Benicar besides hypertension
Studies have found that ARBs have many applications beyond hypertension including anti-inflammatory, arthritis, liver fibrosis, neurological, oxidative stress, preventing organ damage, Raynaud's syndrome, retinopathy, migraines, kidney disease, diabetes, insulin resistance, vascular remodeling, heart failure, C-reactive protein reduction, arrhythmias, myocarditis, atherosclerosis, and antibacterial agent. A list of studies can be found in our Physicians' Reference Library.
ARBs treat inflammatory diseases
A wide variety of illnesses has been successfully treated with Inflammation Therapy. See Diseases Believed to be Caused by Th1/Th17 Inflammation.
This study from Stanford University concluded, "Modulation of the renin-angiotensin-aldosterone system (RAAS) with inexpensive, safe pharmaceuticals used by millions worldwide is an attractive therapeutic strategy for application to human autoimmune diseases."
FDA approval and off-label use of Benicar
Although the Food and Drug Administration (FDA) approved Benicar at the 40mg dosage once a day for hypertension. It studied 80mg/day and found it safe. Benicar has not been submitted for approval at higher doses because the prospective clinical trials that are required for FDA approval need to be funded at the cost of tens of millions of dollars. In the absence of such a current scientific clinical trial, medical journals tend not to be interested in "anecdotal" reports of therapeutic successes. Medical Practitioners, however, are free to prescribe Benicar for 'off-label' uses.
Benicar's actions are extremely complex and the five actions that have been identified as probable have two opposite effects; a temporary increase in inflammatory symptoms and the reduction of some symptoms.
We believe Benicar's primary action is to activate the vitamin D receptor (VDR) so the immune system can manufacture the proteins (antimicrobial peptides or AMPs) it needs to fight intracellular bacterial pathogens. The VDR (in the nucleus of cells) is the key to effective operation of the innate immune system; that part of the immune system which attacks intracellular organisms.
Computer modeling (uncorroborated) by one independent researcher has shown that Benicar, at higher than anti-hypertensive doses, acts as a VDR agonist - a drug that binds to a receptor of a cell and triggers a response by the cell. An agonist often mimics the action of a naturally occurring substance (e.g., 1,25-dihydroxyvitamin-D). See PMID: 16403216
Theoretically, Benicar (putatively similar to 1,25-D) is also able to compete with, and dislodge, bacterial proteins from the VDR to up-regulate the VDR with these agonist effects:
Anecdotally, an activated VDR, and enhanced immune system function, is evidenced by the presence of a waxing and waning increase of inflammatory symptoms (herxing). See Herxheimer reaction.
Activating the VDR appears to occur at relatively low Benicar doses in some patients.
Benicar modulates the immune system
Second, Benicar has a modulatory effect on the immune system by slowing down cytokine production via the inflammatory pathway Nuclear Factor kappa-B which leads to fewer inflammatory symptoms.
"Olmesartan effectively suppressed the 4-hydroxy-2-nonenal protein expression and NF-kappaB..."
Third, Benicar can also cause a shift in immune cell subsets to usually reduce inflammation overall.
"Treatment with olmesartan attenuated the myocardial mRNA expressions of proinflammatory cytokines, [Interleukin (IL)-1β, monocyte chemoattractant protein-1, tumor necrosis factor-α and interferon-γ)] and the protein expression of tumor necrosis factor-α..."
Fourth, at higher doses, Benicar may dock into several different cellular receptors besides the VDR to provide a degree of palliation and symptom reduction.
"However, a variety of evidence has revealed that olmesartan could also be involved in other biological activities, such as anti-inflammation, anti-oxidation and anti-apoptosis independently of anti-hypertension."
Fifth, Benicar reduces angiotensin II, that is significantly inflammatory in numerous disease states. 1,25-D has a similar effect by repressing renin genetic expression to down-regulate the RAS.
Individualizing the dose
Benicar apears to be a somewhat unusual drug in being both immune-stimulating and immune-suppressing at the same time to varying degrees based upon individual biochemistry. There appears to be a delicate balance of VDR activation and NF-kappa-B down-regulation.
Therefore, the dose of Benicar must be individualized based upon patient response.
Treatment balance can shift, so it's important not to get lulled into exploring only one set of dosing options. Chronic Illness Recovery endeavors to determine what works best for each patient because exploring individual variations in medication response is essential for developing accurate advice based upon the experiences of previous patients.
The FDA has set no toxic level for Benicar. See Benicar Safety.
Benicar has the least effect on blood pressure of all the antihypertensive drugs and only causes a very mild depression in blood pressure. This graph from the Benicar drug insert pamphlet illustrates that Benicar's direct effect on blood pressure is minimal beyond a 40mg dose. At this dose, there were no significant side effects listed beyond dizziness which occurred in 3% (the only side effect that occurred in more than 1% of the study cohort). It should be noted that reported 'side effects' were likely due to Herxheimer reactions.
When Benicar is taken per Inflammation Therapy recommendation, it appears to activate the VDR and the immune system appears to be eliminating intracellular bacteria because inflammatory symptoms worsen. These inflammatory consequences are sometimes labeled "side effects" but we believe these varied symptoms are evidence of systemic intracellular infection.
Benicar and potassium
Benicar may decrease urine potassium excretion and increase serum potassium. Other medications that may also have this effect should be avoided or used with caution (monitor potassium regularly) while taking Benicar. These include ACE inhibitors, other ARBs, NSAIDs, potassium-sparing diuretics such as spironolactone (Aldactone), triamterene (Dyrenium), and also trimethoprim-sulfamethoxazole (Bactrim).
Impact of Benicar on symptoms
Benicar lowers the level of cytokines (proteins that are released by the immune system) and this effect sometimes makes patients feel better initially.
However, some patients find that their immune system immediately recognizes and attacks the intracellular bacteria when they start taking Benicar and they experience an increase in symptoms.
Benicar does not directly cause symptoms; it merely makes Th1/Th17 inflammation evident. The cause of symptom exacerbation is the inflammatory process.
An illness that stays below the surface of clinical detection is referred to as subclinical. A subclinical disease has no recognizable clinical findings. It's distinct from a clinical disease, which has signs and symptoms that can be recognized. Many diseases can be subclinical before surfacing as clinical diseases. Symptoms that are subclinical without treatment will remain, get worse and become evident unless Th1/Th17 inflammation is resolved.
At higher doses Benicar may have an anti-inflammatory, palliative effect due to a partial suppression of the immune system Nuclear Factor kappa-B pathway. A higher dose can provide temporary symptomatic relief but is not recommended for the long-term .This is sometimes called the Benicar 'blockade'.
There has been a tendency to believe that Benicar can "fix anything" but often palliative medications are also needed to treat certain conditions and symptoms until inflammation is resolved.
Concern has been expressed about the importance of taking enough Benicar to prevent “organ damage” during Inflammation Therapy. See Benicar Dosing to Prevent Organ Damage.
Metabolism and Excretion
Neither the liver nor kidneys break down Benicar. The drug will eventually go to the liver unchanged, about 50% to the liver and about the same to kidney elimination. The liver portion will be excreted via the bile into to the small intestine where some of it will no doubt be absorbed and recirculated again via the portal system.
According to the FDA Olmesartan Drug Information:
Patients with impaired kidney function may do better with a smaller dose of Benicar. Studies show that in patients with renal insufficiency, serum concentrations of olmesartan were elevated compared with subjects with normal renal function.
According to the FDA Olmesartan Drug Information:
Long-term use of Benicar (as used on IT) appears to be safe and may provide continued protection from inflammation even after overt symptoms have resolved. The long term effect of higher dose Benicar, in regards to partially blocking the NF kappa-B cytokine pathway which is essential for immune system function, is not known.
Therapeutic probe with Benicar
When a patient with obvious Th1/Th17 inflammatory symptoms doesn't test strongly for Th1/Th17 inflammation via the D-metabolites tests, or doesn't test at all, it's possible to determine if Inflammation Therapy will be an effective treatment by doing a therapeutic probe. This is accomplished by avoiding foods high in vitamin D, avoiding sunlight and beginning Benicar to see how the patient reacts.
Persons without Th1/Th17 inflammation usually note only a mild reduction in blood pressure. Most patients with Th1/Th17 inflammation will experience a reduction in elevated 1,25-D with an accompanying reduction in symptoms or an exacerbation of symptoms due to the Herxheimer reaction. This response would then indicate that continued treatment is warranted. Patients who do not respond to Benicar should add 25mg Minocycline every other day to continue the therapeutic probe See Therapeutic Probe.
The right kind of Benicar
It's important to take the form of Benicar that doesn't contain any other ingredients.
Benicar manufactured by Sankyo Pharmaceuticals is a white tablet with these markings:
Another form of Benicar also contains Hydrochlorothiazide (HCTZ), a diuretic, and should NOT be used. HCTZ is too hard on the kidneys and liver, and these are organs in which patients with chronic illnesses may have undetected problems. These tablets are orange.
Benicar (Votum) tablets from Germany may not have the Sankyo name on them.
Olmesartan medoxomil) is available in both generic and brand name forms worldwide in more than 50 in countries, including:
Olmesartan is not available in: Cambodia, New Zealand, or South Africa.
Benicar may be purchased from another country if necessary.
Generic olmesartan medoxomil is available by mail order and is reported to work as well as the brand name Benicar. It's called Olmezest or Olmecip and is made by a pharmaceutical company in India.
Some patients have reported that the Olmecip tablets don't smell like the Sankyo formulation which is an issue for some patients. Olmecip has a different binder formulation from Sankyo's Benicar, has a thinner coating and dissolves more quickly.
Use care to order the correct tablets with no extra ingredients.
Plan ahead because shipping usually takes 3 weeks or longer.
It’s best not to order too many tablets at once, as there is always the chance that Customs will seize or delay the shipment.
Online mail-order sources
http://www.planetdrugsdirect.com 90/$55.00 $0.61/per tablet (free shipping)
Prices were checked 2/11/14.
You can find reputable online pharmacies and compare costs of medications at Pharmacy Checker.
In Australia, Olmesartan is an unrestricted benefit on the PBS (i.e., its cost is subsidized by the Australian Government) and its use is not restricted to a particular condition. The price of PBS scripts is capped at around $30, or around $4.95 for concession card holders. Unrestricted benefit means that patients do not have to have hypertension to qualify for the PBS subsidy.
Ask your doctor to call for an Authority script. The Authority Approvals process can provide one months supply of a drug, for the PBS cost of one pack (i.e., an Authority script will provide 120 tabs for the minimum cost). If you are taking 5 x 40mg tabs/day, your doctor can prescribe 150 tabs per month (or more if needed).
Olmesartan medoxomil is also available in capsules in Australia at:
Fax or mail a copy of the prescription to:
According to the Active Pharmaceutical Index from India (available online), olmesartan medoxomil is available there. There is an email address at the bottom of that list.
Olmesartan was approved for use in Canada on Oct. 28, 2008. It is called Olmetec and the drug identification numbers are 40mg (DIN = 02318679) and 20mg (DIN = 02318660).
Olmetic is now covered by the Ontario Drug Benefit Program and a claim can be made to the Ministry of Health.
This pharmacy is in Quebec but can fill prescriptions for all Canadians. Fax the prescription (indicate timed-release or regular), credit card number and mailing address to:
If more than three months’ supply is ordered @ 40 mg per day, customs will return the package to sender without informing the recipient. There are three options to get around this:
Financial help to purchase Benicar
Many insurers will pay for Benicar 40mg two times a day. If a prescription's coverage is denied through an administrative decision, insurers have an appeals process. Check benefits coverage information to find out the appeals process for the plan to obtain your rightful insurance benefit. During the appeal process, emphasis should be on the fact that the doctor is in charge and s/he has determined this patient should take Benicar at this dosage.
Updated February 11, 2014