FDA Approves Livalo (pitavastatin)
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Jeez...
This one have the grapefruit problem?
This one have the grapefruit problem?
It isn't extensively metabolized by 3A4, according to Clinical Pharmacology. Looks like it goes through 2C9.
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Yippy for the 2C9 polymorph.
Seriously, Another statin? What advantage does this one have over the others?
Grapefruit doesn't neutralize it (among a whole bunch of other things)? That'd be a huge benefit, wouldn't it? Young Padawan thinks it sounds great.
or... for the 200 dollars extra you save a month, you can drink champagne or whatever the crap oldies drink.
I don't see how grapefruit juice can be compared to an alcoholic bev. of any sort.
You're probably just being facetious so... okay! I like champagne, though 😡
Well, fewer drug interactions (metabolized more extensively by CYP2C9 as opposed to 3A4) and perhaps increased tolerance to grapefruit juice would certainly enable this member of the statins to stand out.
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We need a comparative trial against Crestor or this thread is useless....
It's approved based off five trials and has been used in Japan for a while. I haven't seen any comparative trials against rosuvastatin, but there's an ongoing one against simvastatin and atorvastatin.
Alright gimme percentages of LDL reduction then. Any dose will do thanks to that whole "rule of 6s" thing with doubling doses of statins. If it's less than Crestor, it's useless. And even if it isn't, it's still probably useless pharmacoeconomically...
especially once atorv goes generic in 2011
Sweet. All the people still on pravastatin or simvastatin who have some how managed to not be switched to Lipitor or Crestor have another opportunity to be switched to a horribly expensive drug that will do the exact same thing as the one they are on. Awesome! Go big pharma!
Of course once Lipitor goes generic those patients will have to be switched to the latest greatest brand only drug just like the Zocor patients were switced to Lipitor or Crestor. Once the big boobed blond drug reps stop coming around the once block buster drug works no more.
Of course once Lipitor goes generic those patients will have to be switched to the latest greatest brand only drug just like the Zocor patients were switced to Lipitor or Crestor. Once the big boobed blond drug reps stop coming around the once block buster drug works no more.
In "Chemical and pharmacological properties of statins," (Fundamental and Clinical Pharmacology 2004; 19: 117-125), pitavastatin sort of around rosovastatin/atorvastatin level of potency, at least wrt LDL:
Atorvastatin 40mg: lowers LDL-C 50%, raises HDL 6%, lowers TG 29%;
Rosuvastatin 40mg: lowers LDL-C 63%, raises HDL 10%, lowers TG 28%;
Pitavastatin 4 mg: lowers LDL-C 48%, lowers TG 23%, NO SIGNIFICANT EFFECT observed on HDL.
Let's see, other properties: its half life is 11 h, so longer than the older statins (except ator and rosu); bioavailability is 80%, so highest of all the statins. It's a lipophilic statin...
Nothing groundbreaking here.
*yawn*
Drug introductions, particularly the "me toos" like this one, make me glad I don't work in retail any more. Soon after the reps make the rounds, we'd be getting all these scripts for it, and we'd have to call the drs and get it changed it to something that's covered because it'll be months before it's on the provincial formulary.
Atorvastatin 40mg: lowers LDL-C 50%, raises HDL 6%, lowers TG 29%;
Rosuvastatin 40mg: lowers LDL-C 63%, raises HDL 10%, lowers TG 28%;
Pitavastatin 4 mg: lowers LDL-C 48%, lowers TG 23%, NO SIGNIFICANT EFFECT observed on HDL.
Let's see, other properties: its half life is 11 h, so longer than the older statins (except ator and rosu); bioavailability is 80%, so highest of all the statins. It's a lipophilic statin...
Nothing groundbreaking here.
*yawn*
Drug introductions, particularly the "me toos" like this one, make me glad I don't work in retail any more. Soon after the reps make the rounds, we'd be getting all these scripts for it, and we'd have to call the drs and get it changed it to something that's covered because it'll be months before it's on the provincial formulary.
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Yup. Useless. Crestor is still king in the purely pharmacodynamic sense...Zocor's the king in the practical sense until generic Lipitor comes out.
Baycol was also a lipophilic statin with a pretty high bioavailability. I guess post-marketing studies in Japan would rule out excessive rates of rhabdomyolysis, but I think it's worth taking some pause and thinking about.
If it has no effect on HDL, I can't see it being nearly as popular as Lipitor or Crestor.
Good point; other statins have a low bioavailability (Lipitor 12%, Crestor 20%, Lescol 24%). Baycol's was 60%. The article I quoted also said that Baycol was the most extremely lipophilic of all statins. The hydrophilic statins (Crestor, Pravachol) are taken up by the liver through an active process of carrier-mediated uptake, while the lipophilic statins (the rest of them) can passively diffuse into hepatocytes. But this lipophilicity also means that it can passively diffuse through, say, muscle cells. So the authors postulate its lipophilicity may have been a contributing factor to the high rates of rhabdo seen with Baycol.
yup.
