Fluvastatin excretion

Lactation Lovastatin and atorvastatin are excreted in the milk of rats atorvastatin is likely to be excreted in breast milk it is not known whether lovastatin, rosuvastatin, and simvastatin are excreted in breast milk a small amount of pravastatin is excreted in breast milk fluvastatin is present in breast milk in a 2 1 ratio (milk plasma). 

Pravastatin and fluvastatin are almost completely absorbed after oral administration oral doses of lovastatin and simvastatin are absorbed from 30 to 50%. Similarly, pravastatin and fluvastatin are active as such, whereas lovastatin and simvastatin must be hydrolyzed to the acid. Due to first-pass extraction, the primary action of these drugs is on the liver. All are biotransformed, with some of the products retaining activity. Excretion takes place principally through the bile and feces, but some urinary elimination also occurs. Their half-lives range from 1.5 to 2 hours. 

Most statins are highly plasma protein hound and highly lipophilic. The exceptions are pravastatin and rosuvastatin, but it is not known whether they distribute into ascitic fluid [19, 21]. The statins, except possibly rosuvastatin and fluvastatin, are substrates for P-glycoprotein, a pump which is responsible for the excretion of drugs back into the gut, from where they may be reabsorbed or excreted in the faeces [23, 24]. 

It has been suggested that the pharmacokinetics of fluvastatin, including extensive biliary excretion and absence of circulating active metabolites, might be associated with a low incidence of systemic adverse effects compared with other statins. In over 1800 patients treated for an average of 61 weeks, fluvastatin was safe and tolerable (SEDA-19, 408). Pooled data from clinical trials have shown that gastrointestinal symptoms occurred in 14% of fluvastatin recipients compared with 9% taking placebo other complaints occurred... 

Recently, the HMG-CoA reductase inhibitor fluvastatin was reported to reduce urinary protein excretion in moderately proteinuric (0.6 to 1.6 g/day) patients who had IgA nephropathy with normal renal function. Creatinine clearance remained stable during the 6-month study. Longer-term evaluation in a larger patient population will be needed to confirm the effect of this class of agents. 

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