Drug

III

How Drugs Move through the Body

The effect of a drug on the body depends on a number of processes that the drug undergoes as it moves through the body. All these processes together are known as pharmacokinetics (literally, “motion of the drug”). First in these processes is the administration of the drug after which it must be absorbed into the bloodstream. From the bloodstream, the drug is distributed throughout the body to various tissues and organs. As the drug is metabolized, or broken down and used by the body, it goes through chemical changes that produce metabolites, or altered forms of the drug, most of which have no effect on the body. Finally, the drug and its metabolites are eliminated from the body.

A

Administration

Depending on the drug and its desired effect, there are a variety of administration methods. Most drugs are administered orally—that is, through the mouth. Only drugs that will not be destroyed by the digestive processes of the stomach or intestines can be given orally. Drugs can also be administered by injection into a vein (intravenously), which assures quick distribution through the bloodstream and a rapid effect; under the skin (subcutaneously) into the tissues, which results in localized action at a particular site as with local anesthetics; or into a muscle (intramuscularly), which enables rapid absorption through the many blood vessels found in muscles. An intramuscular injection may also be given as a depot preparation, in which the drug is combined with other substances so that it is slowly released into the blood.

Inhaled drugs are designed to act in the nose or lungs. General anesthetics may be given through inhalation. Some drugs are administered through drug-filled patches that stick to the skin. The drug is slowly released from the patch and enters the body through the skin. Drugs may be administered topically—that is, applied directly to the skin; or rectally—absorbed through an enema (an injection of liquid into the rectum) or a rectal suppository (a pellet of medication that melts when inserted in the rectum).

B

Absorption

Absorption is the transfer of a drug from its site of administration to the bloodstream. Drugs that are inhaled or injected enter the bloodstream more quickly than drugs taken orally. Oral drugs are absorbed by the stomach or small intestine and then passed through the liver before entering the bloodstream.

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C

Distribution

Distribution is the transport of a drug from the bloodstream to tissue sites where it will be effective, as well as to sites where the drug may be stored, metabolized, or eliminated from the body. Once a drug reaches its intended destination, the drug molecules move from blood through cellular barriers to various tissues. These barriers include the walls of blood vessels, the walls of the intestines, the walls of the kidneys, and the special barrier between the brain and the bloodstream that acts as a filtration system to protect the brain from exposure to potentially harmful substances.

The drug molecules move from an area of high drug concentration—the bloodstream—to an area of low drug concentration—the tissues—until a balance between the two areas is reached. This process is known as diffusion. When a drug reaches its highest concentration in the tissues, the body begins to eliminate the drug and its effect on the body begins to diminish. The time it takes for the level of a drug to fall by 50 percent is known as the drug’s half-life. Depending on the drug, this measurement can vary from a few minutes to hours or even days. For example, if a drug’s highest concentration level in the blood is 1 mg/ml and this level falls to 0.5 mg/ml after five hours, the half-life of the drug is five hours. A drug’s half-life is used to determine frequency of dosage and the amount of drug administered.

Distribution of a drug may be delayed by the binding of the drug to proteins in the blood. Because the proteins are too large to pass through blood vessel walls, the drug remains in the blood for a longer period until it is eventually released from the proteins. While this process may increase the amount of time the drug is active in the body, it may decrease the amount of the drug available to the tissues.

D

Metabolism and Elimination

While circulating through the body, a drug undergoes chemical changes as it is broken down in a process called metabolism, or biotransformation. Most of these changes occur in the liver, but they can take place in other tissues as well. Various enzymes oxidize (add oxygen to), reduce (remove oxygen from), or hydrolyze (add water to) the drug. These changes produce new chemicals or metabolites that may continue to be medically active in the body or may have no activity at all. A drug may be broken down into many different metabolites. Eventually, most drugs or their metabolites circulate through the kidney, where they are discharged, or eliminated, into the urine. Drugs can also be excreted in the body’s solid waste products, or evaporated through perspiration or the breath.

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