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Introduction To Pharmacokinetics

The document discusses the four phases of pharmacokinetics: absorption, distribution, metabolism, and excretion. It describes how drugs move through the body and are broken down and removed from the system. Many factors can influence how quickly or slowly a drug passes through these phases, including a person's genetics, age, diseases, and other drug interactions.

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11 views

Introduction To Pharmacokinetics

The document discusses the four phases of pharmacokinetics: absorption, distribution, metabolism, and excretion. It describes how drugs move through the body and are broken down and removed from the system. Many factors can influence how quickly or slowly a drug passes through these phases, including a person's genetics, age, diseases, and other drug interactions.

Uploaded by

stephanienwafor18
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
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INTRODUCTION TO PHARMACOKINETICS

Pharmacokinetics (PK) is the study of how the body interacts with administered
substances for the entire duration of exposure (medications for the sake of this article).
This is closely related to but distinctly different from pharmacodynamics, which
examines the drug's effect on the body more closely.

Many factors can influence the therapeutic efficacy of a drug,


including pharmacokinetics, which refers to the passage of drugs into the body, through
it, and out of the body.

Think of pharmacokinetics as a drug’s journey through the body, during which it passes
through four different phases: absorption, distribution, metabolism, and excretion
(ADME). The four steps are:

 Absorption: Describes how the drug moves from the site of administration to the
site of action.
 Distribution: Describes the journey of the drug through the bloodstream to
various tissues of the body.
 Metabolism: Describes the process that breaks down the drug.
 Excretion: Describes the removal of the drug from the body.

Let’s look at these phases in more detail:


Absorption

Absorption is the movement of a drug from its site of administration to the bloodstream.
The rate and extent of drug absorption depend on multiple factors, such as:

 Route of administration
 The formulation and chemical properties of a drug
 Drug-food interactions

The administration (e.g., oral, intravenous, inhalation) of a drug influences


bioavailability, the fraction of the active form of a drug that enters the bloodstream and
successfully reaches its target site.

When a drug is given intravenously, absorption is not required, and bioavailability is


100% because the active form of the medicine is delivered immediately to the systemic
circulation. However, orally administered medications have incomplete absorption and
result in less drug delivery to the site of action. For example, many orally administered
drugs are metabolized within the gut wall or the liver before reaching the systemic
circulation. This is referred to as first-pass metabolism, which reduces drug absorption.

Distribution

The process of drug distribution is important because it can affect how much drug ends
up in the active sites, and thus drug efficacy and toxicity. A drug will move from the
absorption site to tissues around the body, such as brain tissue, fat, and muscle. Many
factors could influence this, such as blood flow, lipophilicity, molecular size, and how the
drug interacts with the components of blood, like plasma proteins.

For example, a drug like warfarin is highly protein-bound, which means only a small
percentage of the drug is free in the bloodstream to exert its therapeutic effects. If a
highly protein-bound drug is given in combination with warfarin, it could displace
warfarin from the protein-binding site and increase the amount that enters the
bloodstream.

Additionally, there are anatomical barriers found in certain organs like the blood-brain
barrier, preventing certain drugs from going into brain tissue. Drugs with certain
characteristics, like high lipophilicity, small size, and molecular weight will be better able
to cross the blood brain barrier.

Metabolism

Cytochrome P450 (CYP450) enzymes are responsible for the biotransformation or


metabolism of about 70-80% of all drugs in clinical use.
What are some factors that affect drug metabolism?

 Genetics can impact whether someone metabolizes drugs more quickly or slowly.
 Age can impact liver function; the elderly have reduced liver function and may
metabolize drugs more slowly, increasing risk of intolerability, and newborns or
infants have immature liver function and may require special dosing
considerations.
 Drug interactions can lead to decreased drug metabolism by enzyme inhibition or
increased drug metabolism by enzyme induction.

Generally, when a drug is metabolized through CYP450 enzymes, it results in inactive


metabolites, which have none of the original drug’s pharmacologic activity. However,
certain medications, like codeine, are inactive and become converted in the body into a
pharmacologically active drug. These are commonly referred to as prodrugs.

As you can imagine, having genetic variations in CYP2D6, the metabolic pathway for
codeine, can have significant clinical consequences. Usually, CYP2D6 poor metabolizers
(PMs) have higher serum levels of active drugs. In codeine, PMs have higher serum
levels of the inactive drug, which could result in inefficacy. Conversely, ultra-rapid
metabolizers (UMs) will transform codeine to morphine extremely quickly, resulting in
toxic morphine levels.

The FDA added a black box warning to the codeine drug label, stating that respiratory
depression and death have occurred in children who received codeine following a
tonsillectomy and/or adenoidectomy and who have evidence of being a CYP2D6 UM.

Excretion

Elimination involves both the metabolism and the excretion of the drug through the
kidneys, and to a much smaller degree, into the bile.

Excretion into the urine through the kidneys is one of the most important mechanisms of
drug removal.

Many factors affect excretion, such as:


 Direct renal dysfunction, which could prolong the half-life of certain drugs and
necessitate dose adjustments.
 Age, which can contribute to differing rates of excretion and impact dosing of
medications.
 Pathologies that impact renal blood flow, such as congestive heart failure and
liver disease can make drug excretion less efficient

Whether it’s a patient who just had gastric bypass surgery, a CYP2D6 poor metabolizer,
or a patient with renal dysfunction, an individual’s characteristics affect these four
processes, which can ultimately influence medication selection.

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