Ciprofibrate

Ciprofibrate (48), a more potent lipid-lowering agent clofibrate, is prepared from Simmons-Smith product by Sandmeyer replacement of the amino group by a hydroxyl via the diazonium salt. Phenol undergoes the Reimer-Thiemann like process common to these agents upon alkaline treatment with acetone and chloroform to complete the synthesis of ci profib-rate (48). 

Alprenolol HCl Bromelain Ciprofibrate Clortermine HCl Desonide Fenofibrate Flucloronide Flunisolide Fluocinonide Flurandrenolide Glucagon Gramicidin Hetacillin potassium I proniazid Kebuzone Methyltestosterone Niaprazine Probucol Relaxin Somatotropin Triamcinolone acetonide Acetonitrile... 

Linfolysin - Chlorambucil Linosal - Betamethasone Linostil -Dimetacrine tartrate Linton Haloperidol Linyl - Phentermine HCI Lioresal Baclofen Lipanor - Ciprofibrate Lipenthyl - Fenofibrate Lipentyl - Fenofibrate Lipavil - Clofibrate Lipavlon - Clofibrate Lipenan - Clofibride Lipidax - Fenofibrate Lipidicon - Clofibrate Lipidil - Fenofibrate Lipo - Folic acid Lipo-BC - Inositol... 

Giometti CS et al. A comparative study of the effects of clofibrate, ciprofibrate, WY14.643, and di-[2-ethylhexyl)-phthalate on liver protein expression in mice. Appl. Theoret Electrophoresis 1991 2 101-107. 

Fibrates, such as fenofibrate (1), gemfibrozil (2), bezafibrate (3), clofibrate (4) and ciprofibrate (5) moderately enhance HDL levels by 10-15% [17], Fibrates are... 

Ciprofibrate 131 is a potent, long-acting hypolipidemic agent. It is effective in type Ila, Ilb, III and IV hyperlipoproteinemias and produces a beneficial elevation of the anti-atherogenic high density lipoprotein, Eq. (52) [182]. 

However, peroxisomal-proliferating chemicals do not appear to cause the phenomenon in all species, and humans are believed to be a nonresponsive species. Thus, guinea pigs are refractory, and with humans given ciprofibrate, only limited peroxisomal proliferation was seen, and there was no increase in acyl CoA oxidase. 

A number of chemicals, including some therapeutically important antihyperlipdemic drugs (e.g., clofibrate, ciprofibrate, bezafibrate, nafenopin, and Wy-14643) and plasticizers (e.g., diethylhexylphthalate), cause a phenomenon known as peroxisome proliferation. This phenomenon was discovered in 1960, and the importance of this became more apparent when in 1980 it was found that in rodents the same chemicals caused hepatic carcinomas. 

Various chemicals, such as the fibrate (e.g., clofibrate, bezafibrate, and ciprofibrate) and other lipid-lowering drugs (e.g., Wy-14643) and phthalate plasticizers (e.g., diethylhexyl phthalate), bind to and activate PPARa and are also hepa to carcinogenic in rodents. However, different compounds bind with different affinities, from strong (e.g., Wy-14643) to weak (e.g., phthalates). Thus, it is believed that peroxisomal proliferators act via the receptor (PPARa) to cause some of the effects seen. 

Refractory species such as guinea pig seem to have fewer PPARa receptors in the liver, and observations suggest there are significant differences between rodents and humans in a number of aspects of the response. Recent studies in cynomologous monkeys treated with ciprofibrate have detected peroxisomal proliferation but only found slight changes in certain parameters [e.g., messenger RNA (mRNA) induction for acyl CoA oxidase] of minimal oxidative stress, and despite hypertrophy, cell proliferation was not detected. 

The fibrates include beclobrate, bezafibrate, biclofi-brate, binifibrate, ciprofibrate, clinofibrate, clofibrate, dulofibrate, etofibrate, fenirofibrate, fenofibrate, gemfibrozil, lifibrate, nicofibrate, picafibrate, pirifibrate, ponfi-brate, ronifibrate, salafibrate, serfibrate, simfibrate, sitofibrate, tiafibrate, timofibrate, tocofibrate, urefibrate, and xantifibrate (all rINNs). 

Chronic radiodermatitis after cardiac catheterization has been observed in a 62-year-old woman taking ciprofibrate. A second catheterization performed when she had stopped taking it did not provoke new lesions (37). 

Acute renal insufficiency occurred in one patient taking ciprofibrate 100 mg/day and ibuprofen 400 mg/day (84). Both drugs are highly protein-bound and contain propionic acid groups. Thus, ibuprofen may displace ciprofibrate. 

Giro net N, Jan V, Machet MC, Machet L, Lorette G, Vaillant L. Radiodermite chronique post catheterisme car-diaque role favorisant du ciprofibrate (Lipanor) . [Chronic radiodermatitis after heart catheterization the contributing role of ciprofibrate (Lipanor) .] Ann Dermatol Venereol 1998 125(9) 598-600. 

Harvengt C. Drugs recently released in Belgium. Mefloquine—ciprofibrate. Acta Clin Belg 1991 46(2) 117-9. 

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