Drug absorption summary, Mitschriften von Biologie

The study of drug absorption, distribution, metabolism, excretion, and how the body affects the drug falls under the term pharmacokinetics. The application of pharmacokinetic methods to ensure patients are treated safely and effectively is known as clinical pharmacokinetics. The introduction of pharmacokinetics as a discipline has facilitated the development of rational drug therapy, understanding drug action and metabolism, understanding of concentration-effect relationship, and the establishment of dosage regimens.

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2023/2024

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Essay Pharmacology
Luca Chiara Jacobs Group 6!
Drug Absorption
The study of drug absorption, distribution, metabolism, excretion, and how the body
affects the drug falls under the term pharmacokinetics. The application of
pharmacokinetic methods to ensure patients are treated safely and effectively is
known as clinical pharmacokinetics. The introduction of pharmacokinetics as a
discipline has facilitated the development of rational drug therapy, understanding
drug action and metabolism, understanding of concentration-effect relationship, and
the establishment of dosage regimens.
The most important principle in pharmacokinetics theory is drug absorption which is
defined as the transportation of the unmetabolized drug from the site of
administration to the body circulation system. Several mechanisms of drug absorption
have been identified, including passive diffusion, carrier-mediated membrane
transport such as active and facilitated diffusion, and other nonspecific drug
transporters, such as P-glycoprotein. Different factors can affect drug absorption;
these factors can be classified as drug-specific and patient-specific factors. Therefore,
the percentage of drug absorption is varied among different routes of administration,
such as oral, subcutaneous (SQ), transdermal, intravenous (IV), and intramuscular
(IM). Since the oral route is the major route of administration, the major emphasis of
this article will be on gastrointestinal (GI) drug absorption. The bioavailability of a
drug product is known as the rate and extent of its absorption. A better understanding
of the drug absorption process and affecting factors play an important role in
achieving better bioavailability and thus better therapeutic effect.
For drug absorption to occur, a drug must cross biologic barriers
(e.g. epithelial/endothelial cells ). Only a few drugs move across cellular barriers in
an “active” way; that is, a way that requires energy (ATP) and moves the drug from
an area of low concentration to an area of higher concentration.
On the other hand, most drugs cross cellular barriers via passive diffusion; that is,
drugs simply move from an area of higher concentration to an area of lower
concentration by diffusing through cell membranes.
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Essay Pharmacology

Luca Chiara Jacobs Group 6

Drug Absorption

The study of drug absorption, distribution, metabolism, excretion, and how the body affects the drug falls under the term pharmacokinetics. The application of pharmacokinetic methods to ensure patients are treated safely and effectively is known as clinical pharmacokinetics. The introduction of pharmacokinetics as a discipline has facilitated the development of rational drug therapy, understanding drug action and metabolism, understanding of concentration-effect relationship, and the establishment of dosage regimens. The most important principle in pharmacokinetics theory is drug absorption which is defined as the transportation of the unmetabolized drug from the site of administration to the body circulation system. Several mechanisms of drug absorption have been identified, including passive diffusion, carrier-mediated membrane transport such as active and facilitated diffusion, and other nonspecific drug transporters, such as P-glycoprotein. Different factors can affect drug absorption; these factors can be classified as drug-specific and patient-specific factors. Therefore, the percentage of drug absorption is varied among different routes of administration, such as oral, subcutaneous (SQ), transdermal, intravenous (IV), and intramuscular (IM). Since the oral route is the major route of administration, the major emphasis of this article will be on gastrointestinal (GI) drug absorption. The bioavailability of a drug product is known as the rate and extent of its absorption. A better understanding of the drug absorption process and affecting factors play an important role in achieving better bioavailability and thus better therapeutic effect. For drug absorption to occur, a drug must cross biologic barriers (e.g. epithelial/endothelial cells ). Only a few drugs move across cellular barriers in an “active” way; that is, a way that requires energy (ATP) and moves the drug from an area of low concentration to an area of higher concentration. On the other hand, most drugs cross cellular barriers via passive diffusion; that is, drugs simply move from an area of higher concentration to an area of lower concentration by diffusing through cell membranes.

This type of drug movement does not require any energy expenditure, but will be influenced by the size of the drug and the solubility of the drug. For drug absorption to be most efficient, the properties of the drug itself and the pH of the environment where the drug is located must be considered. Most drugs are either weak acids or weak bases. Drugs that are weak acids will pick up a proton when placed in an acidic environment and will, thus, be un-ionized. H+^ + A-^ <-> HA In the above example, when the weak acid, A-, is placed into an acidic environment, H+; the drug picks up a proton and is no longer ionized (it becomes protonated as HA). If the same acid, A-, is placed into an alkaline environment, - OH, the drug will remain ionized, as A-. Drugs that are un-ionized will be better able to diffuse through a lipid cellular membrane, cross a biologic barrier, and enter the bloodstream (e.g. be absorbed) compared to drugs that are ionized. Thus, a drug that is a weak acidic will be best absorbed in an acidic environment (because it gains a proton and becomes un- ionized). The opposite is true for drugs that are weak bases. Consider, a weak base, NH 3. In an acidic environment, H+, the drug gains a proton and becomes ionized. H+^ + NH 3 <-> NH 4 + On the other hand, in an alkaline environment, a drug that is a weak base would remain un-ionized. Thus, weakly basic drugs are more likely to absorbed in alkaline environments where they remain un-ionized compared to acidic environments where they gain a proton and pick up a charge. Ionized (or charged) drugs are not absorbed as efficiently as un-ionized drugs are. Practically speaking, this means that if taken orally, a drug that is a weak acid will be absorbed primarily in the acidic environment; whereas, a drug that is a weak base will be absorbed in the alkaline environment small intestines. Physiogically speaking, even though the stomach is acidic, it is not well-suited for drug absorption, even for drugs that are weak acids due to its thick mucus layer and relatively small surface area. The stomach is more of a “storage” organ than an absorptive one. In contrast, the small intestines have a large surface area available for absorption owing to extensive villi and microvilli.

Other situations where IV drugs are required include unconscious patients, those who have a non-functional GI tract, when there is an unavailability of an oral dosage form, or when there is a need for tissue penetration that is not achievable by oral therapy. Drug absorption and bioavailability are essential aspects of pharmacokinetics. They influence drug effectiveness and safety. They can also affect the onset, intensity, and sometimes the duration of action. Many factors can affect the absorption and bioavailability of drugs; some are drug-specific while the others are patient-specific. Bioavailability and pharmacokinetic studies aim to optimize drug use by maintaining the drug concentration within the therapeutic range.

References https://www.ncbi.nlm.nih.gov/books/NBK557405/ https://www.pharmacologyeducation.org/pharmacology/drug-absorption https://www.msdmanuals.com/home/drugs/administration-and-kinetics-of-drugs/ drug-absorption https://pharmacylibrary.com/doi/10.21019/9781582121260.ch