Drug Action

Drug Receptors

Drugs of C.N.S
 Elmhurst College
Enzyme Inhibition Sulfa Drugs Cancer Drugs I  Chemistry Department
Penicillin Other Antibiotics Cancer Drugs II  Virtual ChemBook

Drug Classification:

Drugs can be classified according to various criteria including chemical structure or pharmacological action. The preferred classification is the latter one which may be divided into main groups as follows:

a) Chemotherapeutic agents - used to cure infectious diseases and cancer. (Sulfa drugs, Antibiotics)
b) Pharmacodynamic agents - used in non-infectious diseases (Cholinergic, Adrenergic, Hallucinogenic, Sedatives)
c) Miscellaneous agents (Narcotic Analgesics, Local Anesthetics)

Drug Names:

Drugs have three or more names including a: chemical name, brand or trade name, and generic or common name. The chemical name is assigned according to rules of nomenclature of chemical compounds. The brand name is always capitalized and is selected by the manufacturer. The generic name refers to a common established name irrespective of its manufacturer.

In most cases, a drug bearing a generic name is equivalent to the same drug with a brand name. However, this equivalency is not always true. Although drugs are chemically equivalent, different manufacturing processes may cause differences in pharmacological action. Several differences may be crystal size or form, isomers, crystal hydration, purity-(type and number of impurities), vehicles, binders, coatings, dissolution rate, and storage stability.

Introduction to Drug Action


A very broad definition of a drug would include "all chemicals other than food that affect living processes." If the affect helps the body, the drug is a medicine. However, if a drug causes a harmful effect on the body, the drug is a poison. The same chemical can be a medicine and a poison depending on conditions of use and the person using it.

Another definition would be "medicinal agents used for diagnosis, prevention, treatment of symptoms, and cure of diseases." Contraceptives would be outside of this definition unless pregnancy were considered a disease.

Disease Classification:

A disease is a condition of impaired health resulting from a disturbance in the structure or function of the body. Diseases may be classified into the following major categories:

1) Infections caused by viruses, ricketsia, bacteria, fungi, protozoa and worms
2) Allergic diseases caused by antigens and foreign substances
3) Metabolic disorders caused by defects in the body's ability to carry out normal reactions - these may be hereditary, deficiency, and congenital defects
4) Cancer
5) Toxic diseases caused by poisons
6) Psychosomatic and mental diseases

Chemotherapy, broadly defined, means the treatment of any disease by chemicals including infectious and non-infectious diseases. The original definition applied only to drugs which were used in the treatment of infectious diseases. The proper term for the treatment of non-infectious diseases is pharmacodynamics.

 Sites of Drug Action:

l. Enzyme Inhibition:

Drugs act within the cell by modifying normal biochemical reactions. Enzyme inhibition may be reversible or non reversible; competitive or non-competitive. Antimetabolites may be used which mimic natural metabolites. Gene functions may be suppressed.

2. Drug-Receptor Interaction:

Drugs act on the cell membrane by physical and/or chemical interactions. This is usually through specific drug receptor sites known to be located on the membrane. A receptor is the specific chemical constituents of the cell with which a drug interacts to produce its pharmacological effects. Some receptor sites have been identified with specific parts of proteins and nucleic acids. In most cases, the chemical nature of the receptor site remains obscure.

3. Non-specific Interactions:

Drugs act exclusively by physical means outside of cells. These sites include external surfaces of skin and gastrointestinal tract. Drugs also act outside of cell membranes by chemical interactions. Neutralization ofstomach acid by antacids is a good example.


Mode of Drug Action:

It is important to distinguish between actions of drugs and their effects. Actions of drugs are the biochemical physiological mechanisms by which the chemical produces a response in living organisms. The effect is the observable consequence of a drug action. For example, the action of penicillin is to interfere with cell wall synthesis in bacteria and the effect is the death of the bacteria.

One major problem of pharmacology is that no drug produces a single effect. The primary effect is the desired therapeutic effect. Secondary effects are all other effects beside the desired effect which may be either beneficial or harmful. Drugs are chosen to exploit differences between normal metabolic processes and any abnormalities which may be present. Since the differences may not be very great, drugs may be nonspecific in action and alter normal functions as well as the undesirable ones. This leads to undesirable side effects.

The biological effects observed after a drug has been administered are the result of an interaction between that chemical and some part of the organism. Mechanisms of drug action can be viewed from different perspectives, namely, the site of action and the general nature of the drug-cell interaction.

l. Killing Foreign Organisms:

Chemotherapeutic agents act by killing or weakening foreign organisms such as bacteria, worms, viruses. The main principle of action is selective toxicity, i.e. the drug must be more toxic to the parasite than to the host.

2. Stimulation and Depression:

Drugs act by stimulating or depressing normal physiological functions. Stimulation increases the rate of activity while depression reduces the rate of activity.