drug metabolism for dummies




Common Crazy Med Crap Index
Pharmacodynamics Basics | Pharmacology Index | Metabolism & Elimination

Pharmacokinetics (PK)1 is what your body does to a drug, as well as what a drug does to your body in specific ways that usually don’t have much to do with most of the effects of most crazy meds. Unless you count side effects. Pharmacokinetics is a geek’s paradise filled with hardcore, detailed, technical information about a medication. Pharmacists will often know more about a medication’s PK than doctors, because they spent more time in school learning about it. They also deal with PK on a daily basis, as they’re the people who answer the questions, often preemptively, most people don’t think of asking their doctors until after they drop off the prescription2. Questions such as:

  • What time of day should I take it?
  • Should I take this med with food, on an empty stomach, or does it matter?
  • When will it start to work?
  • Will it affect, or be affected by, other drugs I’m taking?
  • What sort of side effects can I expect?
  • If I need to stop taking it, how should I go about doing that?
  • How long will the side effects last after I stop taking it?

Most of those answers are based on:

  • The half-life, which is a key factor in how often you need to take a med and how long it takes to clear your system.
    • How long it takes a drug to clear your system is one of the main factors in determining how to stop taking a medication.
  • How your body clears the med from your system.
    • How you metabolize drugs is also how you convert some otherwise inert pills that you take into the substances called active metabolites that actually do something. Some working drugs also have active metabolites.
    • The vast majority of drug-drug and drug-food interactions involve how drugs are metabolized.
  • Bioavailability factors. These measure how well a medication is absorbed and distributed, and determine such things such as if it’s better to take a medication with meals, on an empty stomach, or whichever works better for you. They are the other factors involved in how often you need to take a medication.
    • Bioavailability factors are also used to determine if a generic medication is 80–125% bioequivalent of the brand name drug3.
  • A drug’s journey through your body is responsible for many side effects. Sometimes PK-related adverse reactions - as they technically wouldn’t be side effects - are worse than those caused by what a drug is actually doing. Most of these adverse reactions are what you’d expect: nausea, diarrhea, excessive gas, and assorted other GI problems. Some are actually due to how a med works, just working in the wrong place, such as an antipsychotic causing metabolic syndrome, which is an example of a true side effect.

Here are the basics of PK dumbed down as I understand them. I’m starting with how drugs are cleared from your system because

  1. It’s easier
  2. It’s what 80% of the people who read this site are interested in as far as PK is concerned

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Common Crazy Med Crap Index
Pharmacodynamics Basics | Pharmacology Index | Metabolism & Elimination


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1 Pharmacokinetics literally means how a drug moves through your body, (from the Greek pharmakon - medicine, and kinetikos - to set in motion) and that is exactly what it's about. From the time you swallow (or however it's delivered) a med until you piss it out (which is how most of the remnants of most meds finally leave).

2 And, as I write all over the place, doctors often can't address themselves in this world of 30-minute intake appointments and 15-minute medication-check follow-ups.

3 However, the FDA requires only a single, frequently sub-therapeutic dose taken by healthy volunteers - who are mostly, sometimes entirely white males between the ages of 20 and 50 willing to take recently developed drugs because they need the money - to determine pharmacokinetic data, including bioavailability and bioequivalence factors that determine the standard used to meet that 80-125% confidence range for bioequivalence.


Pharmacokinetics 101 by Jerod Poore is copyright © 2012 Jerod Poore

Last modified on Sunday, 01 June, 2014 at 11:20:18 by JerodPoorePage Author: Jerod PooreDate created: 14 December 2012

All drug names are the trademarks of someone else. Look on the appropriate PI sheets or ask Google who the owners are. The way pharmaceutical companies buy each other and swap products like Monopoly™ real estate, the ownership of any trademarks may have changed without my noticing.





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1 While there are plenty of books to help you with hypochondria, for some reason there’s not much in the way of websites. Then again, staying off of the Internet is a large part of curing/managing the disorder.

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3 Have I mentioned how open source operating systems for commercial applications is one of the dumbest ideas in the history of dumb ideas? I don’t even need my big-ass rant any more. Heartbleed has made my case for me. And that’s just the one that got all the media attention. The very nature of an open source operating system makes security as much of an illusion of anonymity. Before you flip out too much: the domain Crazymeds is hosted on uses a version of SSL that is not affected by the Heartbleed bug. That’s one of the many reasons why I pay a lot of money and keep this site on Lunarpages.

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