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What is a pro-drug?

Updated: 4/28/2022
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5y ago

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A pro-drug is a pharmacological inactive compound which becomes active through metabolism.

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Q: What is a pro-drug?
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What are the benefits of a prodrug?

A prodrug actually has several biopharmaceutical benifits. First of all, it is important to understand the definition of a prodrug. A prodrug is a drug that is taken inactive, and through natural metabolic processes becomes active. One benifit is that a prodrug formulation actually increases the bioavailability of the drug. This means that if a drug is poorly absorbed by the body, a prodrug formulation of it can actually increase the amount of drug brought into the circulatory system (By making less polar/ionized). Next, this formulation can act as a vehicle to bring the drugs to specific areas of the body for usage. Drugs that need to pass the blood brain barrier for CNS affects can use a very lipid soluble vehicle bound to it to allow it to cross the barrier. Once the drugs gets to its target site, it is broken down by specific metabolic processes that present the active drug. Furthermore, a mutual prodrug is when both componants give pharmacotherapeutic affect. The Vigabatrin (GABA deaminase inhibitor), GABA (inhibbitory neurotransmitter), Fatty acyl ester (very lipid soluble) prodrug combination is a mutual prodrug in which the Vehicle takes the drug to the brain, the vigabatrin blocks the breakdown of GABA, and GABA is released. This prodrug is a treatment of Parkinsons disease as it increases the inhibition of the tremors and erratic movements associated with it. Finally, it also gives less side effects. Because of increased specificity (due to the fact only certain metabolic processes break down the prodrug, releasing its active componants at specific sites) their are a reduced amount of side effects. Hope this helps


Which drug is a prodrug that is activated by colonic bacteria when given orally?

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Will vyvance show up on a drug screen as an amphetamine?

Yes. It is a prodrug of an amphetamine.