Lipid regulating drugs

The lipid regulator drugs bezafibrate and fenofibrate at initial concentrations of 4.5 and 4.2 ng g-1 in sterile sludge were completely removed after the fungal treatment. The fate of fenofibrate, also present in non-sterile sludge, was the same. Meanwhile, the most abundant atorvastatin, a cholesterol lowering statin, decreased its concentration in 80% and 65% in sterile and non-sterile conditions, respectively. 

Questran contains colestyramine, a lipid-regulating drug that acts as a bile acid sequestrant it is also used in pruritus associated with partial biliary obstruction and primary biliary cirrhosis. 

Rhabdomyolysis is the destruction of skeletal muscle tissues and may be associated with lipid-regulating drugs such as the fibrates and the statins. The risk of this side-effect is increased in patients with renal impairment and with hypothyroidism. Rhabdomyolysis may also occur with nicotinic acid, the antipsychotic aripiprazole, and the anaesthetic propofol. 

Choice of lipid-regulating drugs. Med Lett 2001 43 (Issue 1105) 43 8. 

D. J. Hauss, S. Mehta, G. W. Radebaugh, Targeted lymphatic transport and modified systemic distribution of CI-976, a lipophilic lipid-regulator drug, via a formulation approach, hit. J. Pharmaceut. 108 85-93 (1994). 

The Committee on Safety of Medicines (CSM) has advised that rhabdomyolysis with lipid-regulating drugs is rare (1 case in every 100 000 treatment years) but may be increased in those with renal impairment and/or hypothyroidism. 

Synthetic statins are important lipid regulating drugs for the treatment of atherosclerosis and other diseases related to hyperlipidaemia, especially coronary heart disease. As the pharmacophore, all synthetic statins contain a saturated or partially unsaturated syn-3,5-dihydroxy C7-carboxylate. An important building block for the synthesis of the side chain is represented by 4-chloro-3-hydroxybutanoate esters (CHBE). Both enantiomers can be obtained by enzyme-catalyzed reduction of the (1-keto ester. The group of Kataoka and Shimizu found that an aldehyde reductase of Sporobolomyces salmonicolor [161] and a carbonyl reductase of Candida... 

In vitro studies found quinupristin/dalfopristin inhibited the cytochrome P450 isoenzyme CYP3A4-mediated metabolism of docetaxel, tamoxifen, and terfenadine. Quinupristin/dalfopristin is predicted to raise the levels of other drugs ineluding antiarrhythmics (disopyramide, lidocaine, quinidine), antiretrovirals (such as delavirdine, indinavir, nevirapine, ritonavir), astemizole, carbamazepine, cisapride, methyl-prednisolone, paclitaxel, statins (but see Lipid regulating drugs , (p.l086)), and vinca alkaloids. More study is needed. 

Note that a number of the large-scale trials of the use of lipid-regulating drugs in primary or secondary prevention of cardiovascular events included patients with diabetes. A review of these subgroups concluded that statins were the drug of choice for lipid-lowering therapy in patients with type 2 diabetes and known coronary artery disease or other cardiovascular risk factors. There was no evidence to recommend one statin over another. ... 

The marked rises in statin levels and/or toxicity (rhabdomyolysis) probably occur because both the statin and eielosporin compete for the same metabolising enzyme, the cytochrome P450 isoenzyme CYP3A4. The extent of the interaction seems to depend on the relative affinities of the different statins for this isoenzyme, and also on whether they can be metabolised by alternative pathways. P-glycoprotein and other transporter proteins may also have a part to play, especially in the raised eielosporin levels seen with pravastatin. See Lipid regulating drugs , (p.l086) for more information about the metabolism of the statins. 

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