Prodrug

Prodrug is a type of drug that, after administration, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how a drug is absorbed, distributed, metabolized, and excreted (ADME).

Overview

Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects.

Mechanism of action

Prodrugs are typically designed to be safer or more effective than their active forms. The active compounds are often poorly absorbed, have a high first-pass metabolism rate, are quickly eliminated, or might be toxic. The prodrug form can be a way to overcome these problems.

Examples

Some examples of prodrugs and their active forms include:

• Codeine (prodrug), which is metabolized into morphine (active drug)
• Psilocybin (prodrug), which is metabolized into psilocin (active drug)
• Aspirin (prodrug), which is metabolized into salicylic acid (active drug)

See also

• Drug design
• Pharmacokinetics
• Pharmacodynamics

References

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