gardenmaniac, you have asked about Zetia (Ezetimebe) and I have reproduced a small passage from a PubMed paper for you. It is a technical quote that will reward careful and repeated reading. (in other words, you need to analyse the words used and then give them their common meanings)
The drug, Zetia, is supposedly not a statin (could the pharmaceutical industry be worried about some determined and sustained bad press about statins by clinicians and have they attempted to take our minds off the term?) but is reported as lowering cholesterol by interfering with the absorbtion of cholesterol from the intestine. The wording in the first paragraph strongly suggests that its effects are not widely understood (or even understood at all) which is a huge warning sign. AVOID THIS DRUG LIKE YOU WOULD AVOID THE PLAGUE!
It is not yet clear, after decades of dedicated research, that lowering cholesterol is a good or worthwhile aim. Lower cholesterol has been linked to increased risk of death (among many other effects) think about that. There are many ignorant doctors who practise medicine by repeating what their colleagues say. They don't think about how they do their job but just do as they have been told and frequently... they have suspended all critical analysis.
The substance, Ezitimibe, has a very long half-life of some 20 hours in the body... that is the duration it it takes for the drug to reach half of its original concentration strength. My take on this particular aspect of Zetia is that if nature thought that it was a good thing to have this substance in my body in the first place... it would already be there because we all would have been born with it. I personally trust evolution to do what is best for the survival of the species. Treat your body as your personal temple and keep this junk outside of your body, where it very firmly belongs. Interfere with your own body biochemistry, at your peril.
The third paragraph discusses what 'appears' to be the principle medical benefit, that is a reduction in LDLc and that is followed by the pure alchemy inherent in the statement "There is also a reduction in the cholesterol content of chylomicrons, which *may* provide *some* reduction in the atherogenic *potential* of the plasma lipoprotein pool." BEWARE! Your chylomicron count is too high and the cash registers of the pharmaceutical industry are already ringing as your doctor prescribes this chylomicron lowering medication to you.
To read this sort of nonsense in a journal that purports to be about medical science, is a shocking indictment of the state of education among medics. The editor should have been fired for permitting such psuedo-scientific claptrap to grace the pages of a scientific journal.
Note the use of the phrase "atherogenic potential" It is complete nonsense... there is a huge amount of suggestion (speculation) and no actual evidential proof that cholesterol is atherogenic, after all... it is required by every cell in your body... a fact that this small monograph about the wonders of Zetia has failed to acknowledge. The proof that cholesterol is harmful has had researchers (read as drug companies) searching and claiming that they have found the 'truth' for decades. It still has not been shown to be the case.
The bottom line is the drug, Zetia, is yet more smoke and mirrors from the pharmaceutical industry. The drug has been used in combination with Simvastatin (Zocor) and goes under the trade name Vytorin. Read all about it on this very site here...
http://www.spacedoc.net/vytorin_side_effects.htm
(you must remove the asterisk from the front of the following URL before pasting it into your web browser)
[quotation from PubMed 2003]
*http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=Retrieve&db=PubMed&list_uids=12743640&dopt=Abstract
"Ezetimibe is the first of a new class of drugs that specifically reduces the intestinal absorption of cholesterol. The drug is absorbed into the intestinal epithelial cell and remains associated in great part with the apical cell membrane where it is believed to interfere with the putative sterol transporter system. This apparently prevents both free cholesterol and plant sterols (phytosterols) from being transported into the cell from the intestinal lumen.
The mechanism is very different from the reduction produced by phytosterol esters and phytostanol esters that have been documented previously as interfering with the micellar presentation of sterols to the cell surface. The drug is rapidly absorbed and glucuronidated in the intestinal cell before secretion into the blood. Ezetimibe is avidly taken up by the liver from the portal blood and excreted into the bile, resulting in low peripheral blood concentrations. The glucuronide conjugate is hydrolyzed and absorbed and is equally effective in inhibiting sterol absorption.
This enterohepatic recycling is responsible for a half-life in the body of more than 20 h. The principle medical benefit appears to be a reduction in low-density lipoprotein cholesterol (LDLc). There is also a reduction in the cholesterol content of chylomicrons, which may provide some reduction in the atherogenic potential of the plasma lipoprotein pool. Triglycerides fall moderately and a modest rise in high-density lipoprotein cholesterol (HDLc) has been consistently observed in groups of treated patients.
The maximum mean reduction of LDL cholesterol is approximately 20-25% in small studies at the maximal dose tested of 40 mg/day and the reduction is usually in the 16-20% range at the dosage of 10 mg/day. Most subsequent studies have been completed with the 10 mg/day dose. The medication is effective as a single daily dose due to its long residence time in the body. Combinations of ezetimibe with all available statins have been completed and demonstrate LDLc reductions of approximately 25% as additive effects to any statin dose alone.
There are also small additional increases in HDL (2-3%) and reductions in triglycerides (10-15%). Additive effects to statin therapy have also been documented in patients with homozygous familial hypercholesterolemia. Reduction of plant sterols has been demonstrated in phytosterolemia, offering the first drug treatment for this rare inherited disease."
[PubMed abstract from Feb 2007] *http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=ShowDetailView&TermToSearch=17253923
The second abstract discusses the rapid development of myopathy 16 days after adding ezitimebe to the patient' statin and resolved 12 days after removing it.
gardenmaniac, this short introduction to Zetia carries one take home message only... Don't do drugs... you know it makes sense.
Kind regards,
xrn