What is an Antimetabolite?

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  • Written By: Mary McMahon
  • Edited By: Kristen Osborne
  • Last Modified Date: 20 January 2020
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An antimetabolite is a drug that interferes with normal cell metabolism. These drugs can be used in a variety of ways in medical treatment, ranging from cancer therapy to treatment for bacterial infection, and pharmaceutical companies are consistently developing promising new drugs in this class. Antimetabolites work by mimicking the actions of a compound normally found in the body to participate in biochemical reactions inside a cell, thereby disrupting the cell's metabolism by blocking or changing the actions of a metabolic process.

Structurally, antimetabolites look like chemicals found in the body. They can compete at receptor sites and trick the body into thinking they are chemicals the body is producing and would normally use. One use for an antimetabolite is to block a process altogether by preventing a metabolite from working. These chemicals can also alter chemical reactions to change their outcome.

In treatment of infections, antimetabolites that shut down the metabolisms of infectious microorganisms without hurting the host can be used. These medications often work by interfering with DNA production, preventing infectious organisms from reproducing and exchanging genetic material. They can also interfere with the production of enzymes necessary for physical function, killing organisms by halting their normal metabolic processes.


With cancers, antimetabolites can be turned against the body itself. These drugs can be designed to target cancer cells and block their division and reproduction, causing tumors to stop growing. This can provide an opening for other treatments to shrink the tumor. Some examples of antimetabolite drugs used in medical treatment include folic acid antagonists, pyrimidine antagonists, and purine antagonists.

These medications can be dangerous if they are not administered properly, especially in the case of cancer drugs, as cancer drugs are hazardous to human cells. It is important to calculate dosages appropriately and to deliver the medication to the right area of the body. Doctors are also concerned with correctly identifying the origins of a cancer so that they use the right drug in the first place, choosing an antimetabolite that will target the rogue cells while causing minimal damage to neighboring healthy cells.

Antimetabolites are usually available by prescription only and some are offered only in clinical environments. This is designed to ensure that the drugs are used correctly and to reduce the risks of developing drug resistance in organisms sensitized to these drugs. It is important to follow dosage and administration instructions carefully and to avoid sharing antimetabolite medications with other people.


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Post 3

I'm on a antimetabolite drug called Methotrexate for my rheumatoid arthritis. The drug actually works really well, it provides pain relief and helps a lot with the inflammation. It has some side effects as well, but I guess that's expected with any medication.

The only side-effect that's really bothering me is the fatigue. I am mostly pain-free when I take the drug, but I feel so tired all the time that I can't do most of what I want to do. If I run a few errands or do the laundry, I'm exhausted and need to lay down for some time.

Is anyone else having this side effect with antimetabolites?

Post 2

@burcinc-- I'm not a doctor so don't take this to be an expert opinion or anything like that. But as far as I know, some antimetabolites do weaken the immune system. This means that the drug affects healthy cells to some degree that there are less white or red blood cells while it is being used.

So in terms of disrupting functions of healthy cells, yes, it does do that to some degree. But it really depends on the type of antimetabolite, how your body processes the medication and the dose.

That's why cancer patients who are generally on higher doses of antimetabolites go to the hospital often to get their blood cell counts checked to make sure that everything is okay.

Post 1

How do antimetabolites differentiate between a dangerous microorganism/cancer cell from a healthy cell? Are different antimetabolites made specifically for certain tumor cells or for certain bacteria?

I'm curious because it sounds like antimetabolites can also disrupt functions of healthy and vital cells along with diseased cells or along with bacteria. If that happens, I'm sure it would be very dangerous.

I'm guessing that there must be many different kinds of antimetabolites available for different purposes right? For example, are there separate antimetabolites made to target separate types of bacteria? And how in the world does the antimetabolite recognize them?

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