DRUG ABSORPTION

 

Introduction: Absorption is a process involving the movement of a substance from its site of administration, across body membranes, to circulating fluids. Drugs may be absorbed across the skin and associated mucous membranes, or they may move across membranes that line the gastrointestinal (GI) or respiratory tract. Most drugs, with the exception of a few topical medications, intestinal anti-infectives, and some radiologic contrast agents, must be absorbed to produce an effect. Absorption is the primary pharmacokinetic factor determining the length of time it takes a drug to produce its effect. Pharmacokinetics

In order for a drug to be absorbed it must dissolve. The rate of dissolution determines how quickly the drug disintegrates and disperses into simpler forms; therefore, drug formulation is an important factor of bioavailability. Bioavailability

In general, the more rapid the dissolution, the faster the drug absorption and the faster the onset of drug action. For example, famotidine administered as an orally disintegrating tablet dissolves within seconds and after being swallowed is delivered to the stomach where it blocks acid secretion from the stomach, thereby treating conditions of excessive acid secretion. Pepticulcer disease: Histamine H2 receptor blockers

At the other extreme some drugs have shown good clinical response as slowly dissolving drugs such as liothyronine sodium (T3) and thyroxine (T4) administered for resolution of hypothyroid symptoms. In some instances it is advantageous for a drug to disperse rapidly. In other cases, it is better for the drug to be released slowly where the effects are more prolonged for positive therapeutic benefit. Absorption is conditional on many factors. Drugs in elixir or syrup formulations are absorbed faster than tablets or capsules. Drugs administered in high doses are generally absorbed more quickly and have a more rapid onset of action than those given in low concentrations. The speed of digestive motility, surface area, pH, lipid solubility, exposure to enzymes in the digestive tract, and blood flow to the site of drug administration also affect absorption. Because drugs administered IV directly enter the bloodstream, absorption to the tissues after the infusion is very rapid. IM medications take longer to absorb. Drug distribution

Other factors that influence the absorption of medications include the following: Drug formulation and dose, Size of the drug molecule, Surface area of the absorptive site, Digestive motility or blood flow, Lipid solubility, Degree of ionization, Acidity or alkalinity (pH), Interactions with food and other medications. The degree of ionization of a drug also affects its absorption. A drug’s ability to become ionized depends on the surrounding pH. Aspirin provides an excellent example of the effects of ionization on absorption. In the acid environment of the stomach, aspirin is in its non-ionized form and thus readily absorbed and distributed by the bloodstream. As aspirin enters the alkaline environment of the small intestine, however, it becomes ionized. In its ionized form, aspirin is not as likely to be absorbed and distributed to target cells.

Unlike acidic drugs, medications that are weakly basic are in their nonionized form in an alkaline environment; therefore, basic drugs are absorbed and distributed better in alkaline environments such as in the small intestine. The pH of the local environment directly influences drug absorption through its ability to ionize the drug.

Drug–drug or food–drug interactions may influence absorption. Many examples of these interactions have been discovered. For example, administering tetracyclines with food or drugs containing calcium, iron, or magnesium can significantly delay absorption of the antibiotic.  High-fat meals can slow stomach motility significantly and delay the absorption of oral medications taken with the meal. Dietary supplements may also affect absorption.

RELATED;

1.  DRUG DISTRIBUTION  

2.  PHARMACOKINETICS

3.  PHARMACOLOGY AND THERAPEUTICS

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