FDA warns that Olmesartan may induce Sprue-like enteropathy, and approves the label changes on 3rd July 2013.

1. Olmesartan induced
Enteropathy
P.Naina Mohamed
Pharmacologist

2. Olmesartan
 Olmesartan is one of several angiotensin II receptor blocking
(ARB) agents.
 Olmesartan has been shown to have a longer half-life and a
greater effect on systolic blood pressure than other ARB
agents, making it widely prescribed for the management of
hypertension.
Olmesartan medoxomil (Inactive ester prodrug)
Hydrolysis (GIT)
Olmesartan (Active form)
Blockade of AT1 receptor
Reduction of Blood Pressure

3. FDA Warning
 FDA is warning on 3rd July 2013, that the blood pressure drug Olmesartan
Medoxomil (marketed as Benicar, Benicar HCT, Azor, Tribenzor, and
generics) can cause intestinal problems known as sprue-like enteropathy.
 Symptoms of sprue-like enteropathy include severe, chronic diarrhea with
substantial weight loss.
 FDA has approved changes to the labels of these drugs to include this
concern.
 Sprue-like enteropathy has not been detected with ARB drugs other than
olmesartan.
 FDA will continue to evaluate the safety of olmesartan-containing products
and will communicate again if additional information becomes available.
 Health care professionals should tell patients to contact them if they develop
severe, chronic diarrhea with substantial weight loss while taking an
olmesartan-containing product, even if it takes months to years for
symptoms to develop.
 Patients should contact their health care professional right away if they take
an olmesartan-containing product and experience severe diarrhea, diarrhea
that does not go away, or significant weight loss.

4. Possible Mechanism of
development of Enteropathy
Olmesartan medoxomil (Inactive ester prodrug)
Hydrolysis (GIT)
Olmesartan (Active form)
Cell-mediated immune response
Damage to the small intestinal brush border
Spruelike enteropathy
Severe, chronic diarrhea with substantial weight loss

5. References
 http://www.fda.gov/Safety/MedWatch/SafetyInformat
ion/SafetyAlertsforHumanMedicalProducts/ucm3595
28.htm?source=govdelivery
 Basic & Clinical Pharmacology, 12e
Bertram G. Katzung, Susan B. Masters, Anthony J.
Trevor
 Goodman & Gilman's The Pharmacological
Basis of Therapeutics, 12e
Laurence L. Brunton, Bruce A. Chabner, Björn C.
Knollmann

6. References
 http://www.ncbi.nlm.nih.gov/pubmed/22728033
 http://www.mayoclinicproceedings.org/article/S0025-
6196(12)00558-7/fulltext
 http://www.hindawi.com/crim/gm/2013/618071/
 http://www.iscpcardio.org/expert-opinion/iscp-
features/severe-spruelike-enteropathy-associated-
with-olmesartan/
 http://www.theheart.org/article/1419079.do