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Deconstructing a Full Prescribing Information : Part V Monday 1/30/12

Posted by smcgamer in Deconstucting The.
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If by tomorrow, I meant 382 days, then yeah, I meant tomorrow.  At any rate, we’re back for more Lunesta!

Pharmacokinetics Continued


Following oral administration, eszopiclone is extensively metabolized by oxidation and demethylation.

Ribbon diagram of human cytochrome P450 isozym...

Image via Wikipedia

Once Lunesta is consumed, it’s metabolized (used) through oxidation and demethylation (which is removing methyl groups from a molecule).

The primary plasma metabolites are (S)-zopiclone-N-oxide and (S)-N-desmethyl zopiclone; the latter binds to GABA receptors with substantially lower potency than eszopiclone, and the former compound shows no significant binding to this receptor.

A metabolite is the intermediate or product of a metabolism (usage, so to speak).  Zopiclone is, to put it simply, a different type of eszopiclone that’s sold in Canada and the UK, and serves similar purposes to eszopiclone, zopiclone’s active stereoisomer.  A GABA receptor responds to gamma-aminobutyric acid, a neurotransmitter.  As we recall from an earlier post, a GABA receptor also helps with sleep, and blocking it hinders sleep (perhaps so Lunesta can do its job without the body getting in the way).

In vitro studies have shown that CYP3A4 and CYP2E1enzymes are involved in the metabolism of eszopiclone.

An in vitro study is a study with organic chemicals done outside of said chemical’s natural environment (like in a test tube).  Cytochrome P450 3A4 is one of the most important enzymes in xenobiotics, and Cytochrome P450 2E1 is also helpful in xenobiotics.  These studies have shown that these two enzymes help out in metabolizing Lunesta.

Eszopiclone did not show any inhibitory potential on CYP450, 1A2, 2A6, 2C9, 2C19, 2D6, 2E1, and 3A4 in cryopreserved human hepatocytes.

So Lunesta doesn’t harm or affect negatively any of those eight cytochrome enyzmes, which is probably a good thing.  Cryopreservation is keeping organic tissue really, really cold so it doesn’t spoil or rot.  A hepatocyte is a liver cell.  They create and store proteins, process waste, transforms carbohydrates and produces bile, cholesterol, and phosopholipids.

And We’re Back: My Plans for this Blog Sunday 1/29/12

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My hiatus is over, so I’m back to bring some new posts into this world.  Let’s go over what I’ll be doing over this next year or so:

  • Minecraft: I got Minecraft some time ago, and I’ve been doing some great exploring and building.  Now, as reading about Minecraft isn’t nearly as fun as watching it (for both of us), I’ll also do some Minecraft stuff over on my YouTube channel (seems everyone has one these days).
  • Programming: I’m a C# programmer, and I’m currently working on a open-source Mario clone entitled Super Mario Limitless.  We’re still very early in development, though.
  • Deconstructing: Yes, I’ll continue that.  I’ll restart “Deconstructing a Full Prescribing Information” for starters.
  • And lots more!

So, I’ll plan to post something roughly every other day for now.  Once I get enough separate things going, posts can become more varied and regular.

Sit back, relax, and enjoy!

Chronolapse – Useful Time-Lapse Software Sunday 5/29/11

Posted by smcgamer in Archive, Uncategorized.
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Chronolapse – Timelapse Maker by Keeyai

Chronolapse is a time-lapse maker featured on Lifehacker today, and I figured I’d share it with you.  It takes pictures of your desktop or a webcam every so often and saves them to a specified folder.  You can also register a hotkey to force a capture.  It has a scheduling feature, annotations, even picture-in-picture.  But the main attraction is that you can compile your captures into a video, built-in to the software (uses MEncoder), as well as adding audio to videos, it appears.

Chronolapse is freeware for Windows.






Update Thursday 4/21/11

Posted by smcgamer in Archive, Uncategorized.
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Hi, everyone.  I’m sorry I haven’t checked in for a while.  I’ve been putting myself though some stress over the projects I have, so I’m going to take a break from all of them, including my blog (yes, I was here).  I’ll be back in a few weeks, ready to blog!

Also, thank you for over 1,300 views.  The most popular posts are the SMBX review and how to insert custom graphics.

See you soon!


Deconstructing a Full Prescribing Information: Part VII Monday 2/28/11

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My blogging habits have been abysmal as of late.  With two bloggers writing here instead of one, however, posts should start coming faster.

Let us continue with part seven.


Two Announcements Wednesday 2/23/11

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The logo of the blogging software WordPress.

Image via Wikipedia

Today, I have two new announcements for my blog, as well as a few news items.

Firstly, my brother, who goes by the screen name justanotherperlhacker, has joined WordPress and is now an editor on my blog.  He is interested in math, computers, and Linux.

Secondly, I’m having some trouble with algebra in school, so I’m going to start blogging about it.  Basically, I’m going to explain how to do each operation so I (and, hopefully, your) can get a better grasp of what I’m studying.  I’m up to Exponents and Radical Functions, which isn’t nearly as hard as what I’ve almost finished, polynomials.

Oh, and the Deconstructing a Full Prescribing Information will continue shortly.

Thanks for reading!

What are the odds of randomly generating a video? Monday 2/7/11

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I like to figure out the odds for things that are so long that they will never happen – like the monkey and the typewriter – that is, the odds of a monkey randomly banging a typewriter to perfectly reproduce the complete works of Shakespeare.


Aside #3 Monday 1/24/11

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Please, readers, plan out your days.  It’ll save you from days like I had today.

Deconstructing a Full Prescribing Information – Part VI Sunday 1/23/11

Posted by smcgamer in Archive, Deconstucting The, Post-A-Week 2011.
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This is my first post of Post-A-Week 2011, and today, I’m continuing with the deconstruction of Lunesta’s full prescribing information.  We continue with the pharmacokinetics of eszopiclone, specifically the elimination, and we will continue with the effect of food, and special populations.


Aside #2 Thursday 1/20/11

Posted by smcgamer in Archive, Uncategorized.
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Rule of Advertising #119,216: All brand names sound cooler with “3D” or “HD” somewhere in them, regardless of whether or not they are relevant.