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Definition - What does prodrug mean?

A prodrug is a pharmaceutical compound that remains inactive in its biochemical form until it reaches its target site, such as an organ or tissue, and then undergoes an immediate metabolic decomposition (breakdown). A prodrug contains molecular compounds of the parent drug, or active ingredients, released at the point of delivery to generate optimal results. The main purpose for prodrugs is to enhance the absorption, distribution, metabolism, and elimination (ADME) rate at which the body can benefit from the substance without losing potency during the digestion or transport process within the body.

SureHire explains prodrug

Manufacturing new pharmaceuticals is expensive and requires years of research before being marketed to the public. Prodrugs are cheaper derivatives of active drugs that are designed to limit or prevent negative side effects and/or overcome physiological deficiencies associated with active drugs. The problem with active drugs is that they can become biochemically inactive or ineffective during digestion from acidic enzymes that dissolve the active ingredients into waste.

The advantages of using prodrugs includes chemical stability during metabolism, faster delivery to a target site (organ or tissue), diminished toxicity to secondary organs, slowed metabolic disintegration, and patient convenience. Unlike active drugs, prodrugs are capable of penetrating through membrane tissue such as the blood-brain barrier to deliver the parent drug dopamine, for example, essential to patients suffering from Parkinson?s disease.

With drug abuse escalating, prodrug-abuse-deterrents are also being introduced as a viable option to curb mass addiction, in particular, to opioid prescription medication. This alternative would prevent individuals from deliberately tampering with the active ingredient by injecting, smoking, or snorting its powdery contents to receive their usual rush. The prodrug formation of opioid would remain inactive until it enters the digestive system and begins to metabolize accordingly. This method avoids traditional means of abuse via mucous membrane tissue (nose) or circulatory system channels (intravenous injection) preferred by many users.

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