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Buflomedil, sold under the brand name Loftyl, is a
vasoactive A vasoactive substance is an endogenous agent or pharmaceutical drug that has the effect of either increasing or decreasing blood pressure and/or heart rate through its vasoactivity, that is, vascular activity (effect on blood vessels). By adju ...
drug used to treat claudication or the symptoms of
peripheral arterial disease Peripheral artery disease (PAD) is an abnormal narrowing of arteries other than those that supply the heart or brain. When narrowing occurs in the heart, it is called coronary artery disease, and in the brain, it is called cerebrovascular diseas ...
. It is currently not approved by the
Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...
(FDA) for use in the United States.


Toxicity

This drug has been suspended from marketing in the European Union, because of concerns about severe
neurological Neurology (from el, νεῦρον (neûron), "string, nerve" and the suffix -logia, "study of") is the branch of medicine dealing with the diagnosis and treatment of all categories of conditions and disease involving the brain, the spinal ...
and
cardiac toxicity Cardiotoxicity is the occurrence of heart dysfunction as electric or muscle damage, resulting in heart toxicity. The heart becomes weaker and is not as efficient in pumping blood. Cardiotoxicity may be caused by chemotherapy (a usual example is th ...
. In its press release dated 17 November 2011 EMA suggested that doctors "should stop using buflomedil and consider alternative treatment options". The European Commission advised all member states to revoke marketing authorisation. Various
adverse effect An adverse effect is an undesired harmful effect resulting from a medication or other intervention, such as surgery. An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. The term complica ...
s have been reported to the FDA.http://www.drugcite.com/?q=BUFLOMEDIL&s=&a=


Synthesis

] Acylation between 1,3,5-trimethoxybenzene 21-23-8(1) and 4-pyrrolidinobutyronitrile 5543-25-0(2) occurs in chlorobenzene solvent in the presence of gaseous hydrochloric acid to give ''Bufomedil'' (3). This is a demonstration of the Hoesch reaction.


References

Alpha-1 blockers Alpha-2 blockers Piceol ethers Pyrrolidines Resorcinol ethers Vasodilators {{Cardiovascular-drug-stub