Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H25NO4.ClH |
| Molecular Weight | 343.846 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=CC(OC)=C(C(=O)CCCN2CCCC2)C(OC)=C1
InChI
InChIKey=ZDPACSAHMZADFZ-UHFFFAOYSA-N
InChI=1S/C17H25NO4.ClH/c1-20-13-11-15(21-2)17(16(12-13)22-3)14(19)7-6-10-18-8-4-5-9-18;/h11-12H,4-10H2,1-3H3;1H
DescriptionCurator's Comment: description was created based on several sources, including
https://www.drugs.com/international/buflomedil.html | https://www.ncbi.nlm.nih.gov/pubmed/3784966 | https://www.ncbi.nlm.nih.gov/pubmed/26193704 | http://www.medscape.com/viewarticle/753768
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/buflomedil.html | https://www.ncbi.nlm.nih.gov/pubmed/3784966 | https://www.ncbi.nlm.nih.gov/pubmed/26193704 | http://www.medscape.com/viewarticle/753768
Buflomedil (trade name Loftyl) is a vasoactive drug used to treat claudication or the symptoms of peripheral arterial disease. Buflomedil has been used for people with diseases of the leg arteries and has shown some benefits for people with a previous stroke. The most common type of stroke is due to narrowing or blockage of an artery in the brain (i.e. ischaemic stroke). Buflomedil is a drug that can dilate brain blood vessels, which may have benefit for people with ischaemic stroke. However, it has not been approved to treat stroke in clinical practice. In 2012 the European Medicines Agency has completed a review of the safety and effectiveness of buflomedil-containing medicines, both oral and injectable, due to severe neurological and cardiac side effects seen with buflomedil. The Agency’s Committee for Medicinal Products for Human Use (CHMP) concluded that the benefits of buflomedil do not outweigh its risks, and has recommended that all marketing authorisations for medicines containing buflomedil should be suspended throughout the European Union (EU).
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| [Emetic and catalepsy-inducing actions of buflomedil]. | 1988 Dec |
|
| Ticlopidine-pentoxifylline combination in the treatment of atherosclerosis and the prevention of cerebrovascular accidents. | 1989 Jan-Feb |
|
| Clinical and hemorheological effects of buflomedil in diabetic subjects with intermittent claudication. | 2001 Dec |
|
| Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate. | 2001 Feb 23 |
|
| Effects of buflomedil on early carotid atherosclerosis in Type 2 diabetic patients. | 2001 Jun |
|
| [Myoclonic coma and severe cardiac insufficiency in a patient with arteritis]. | 2001 Jun |
|
| [Clinical study of the effect of buflomedil on peripheral neuropathy in diabetic patients]. | 2001 Jun 28 |
|
| [Retrograde venous perfusion (RVP in ulcero-mutilating neuropathy]. | 2001 Oct |
|
| [Sudden hearing loss. Clinical case]. | 2002 |
|
| Rheological and biochemical examination of red blood cells after treatment with different pharmacological and toxic substances. | 2002 |
|
| Highlights of the 22nd French pharmacovigilance meeting. | 2002 Feb |
|
| [Bullous pemphigoid induced by spironolactone]. | 2002 Jan |
|
| Rapid HPLC measurement of buflomedil in plasma in poisoning cases. | 2002 Oct |
|
| Drug treatment of intermittent claudication. | 2004 |
|
| Suicide by buflomedil HCl: a case report. | 2004 Feb |
|
| Development of pulsatile release tablets with swelling and rupturable layers. | 2004 Mar 5 |
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| [Suicidal buflomedil intoxication]. | 2004 Mar-Apr |
|
| [Secondary prevention and conservative therapy of obliterative arteriosclerosis]. | 2004 May 16 |
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| Rapid and sensitive liquid chromatography-electrospray ionization-mass spectrometry method for the determination of eperisone in human plasma: method and clinical applications. | 2004 May-Jun |
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| Inhibitory effect of buflomedil on prostate alpha1A adrenoceptor in the Wistar rat. | 2004 Sep 2 |
|
| Therapy of hearing disorders - conservative procedures. | 2005 |
|
| [Pharmaceutical analysis and validation of hospital prescriptions, a 5-year study]. | 2005 Aug 27 |
|
| Does Danshen improve disability after acute ischaemic stroke? | 2005 Feb |
|
| Effect of loading on a swelling-controlled drug delivery system studied by optical techniques. | 2005 Jan 3 |
|
| Buflomedil and pentoxifylline in the viability of dorsal cutaneous flaps of rats treated with nicotine. | 2006 |
|
| Facilitated column selection in pharmaceutical analyses using a simple column classification system. | 2006 Jan 6 |
|
| [Severe peripheral ischemia of rare origin]. | 2006 Jan-Mar |
|
| Comparison between intravenous iloprost and vasoactive drugs in limb ischemia IIB severe. A retrospective analysis. | 2006 Jun |
|
| Assemblage of novel release modules for the development of adaptable drug delivery systems. | 2006 Mar 10 |
|
| Preclinical and clinical examinations of Salvia miltiorrhiza and its tanshinones in ischemic conditions. | 2006 Nov 23 |
|
| Buflomedil: still seizures and cardiac disorders. Too many patients are exposed to an unjustified risk of serious adverse effects. | 2007 Feb |
|
| [Adenosine for treatment of ischemic pain in thromboangiitis obliterans. A case report]. | 2007 Jun |
|
| Detailed documentation of one lipolysis treatment: blood values, histology, and ultrasound findings. | 2007 Mar-Apr |
|
| Effectiveness of mesotherapy on body contouring. | 2008 Apr |
|
| Buflomedil in peripheral arterial disease: trials and tribulations. | 2008 Feb 12 |
|
| Oral buflomedil in the prevention of cardiovascular events in patients with peripheral arterial obstructive disease: a randomized, placebo-controlled, 4-year study. | 2008 Feb 12 |
|
| Buflomedil for intermittent claudication. | 2008 Jan 23 |
|
| Cutaneous granulomatous reaction from mesotherapy. | 2009 Feb |
|
| Buflomedil: potential new indications for an old agent. | 2009 Jun |
|
| Naftidrofuryl for intermittent claudication: meta-analysis based on individual patient data. | 2009 Mar 10 |
|
| Surgical management of a diabetic calcaneal ulceration and osteomyelitis with a partial calcanectomy and a sural neurofasciocutaneous flap. | 2010 |
|
| Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
Patents
Sample Use Guides
The effect of buflomedil (Fonzylane; Laboratoire Lafon, Maisons-Alfort, France) on platelet function, a drug used clinically for the treatment of peripheral vascular diseases, was investigated in vitro. The compound significantly inhibits epinephrine-induced aggregation at the micromolar level. At higher doses (approximately 1 mM), a weak inhibition of ADP- and collagen-induced aggregation was observed; at these concentrations, buflomedil inhibits granular secretion and the interaction of fibrinogen with its receptor on platelet. Further investigations indicate that the drug affects calcium uptake at the membrane level and inhibits the binding of [3H]-yohimbine to the same extent as observed with phentolamine. The IC50 determined from competition binding assays was 1 +/- 0.5 microM.
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235934
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3J944AFS8S
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35543-24-9
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252-611-9
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759291
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100000090428
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m2750
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SUB00891MIG
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37170
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ACTIVE MOIETY
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