What is a pro drug pharmacology?
A prodrug can be defined as a drug substance that is inactive in the intended pharmacological actions and is must to be converted into the pharmacologically active agent by metabolic or physico-chemical transformation.
How does a pro drug work?
A prodrug is a medication or compound 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 the drug is absorbed, distributed, metabolized, and excreted (ADME).
What are the examples of mutual prodrug?
Mutual prodrugs of aspirin and paracetamol. Ibuprofen guiacol ester. Acetylsalicylic acid and paracetamol prodrug. Indomethacin ester prodrug.
What are the advantages of prodrugs?
Prodrugs can improve how an active drug molecule is absorbed, distributed, metabolized and eliminated. Designed to maximize the amount of active drug that reaches its site of action, prodrugs contain a carrier that will be removed by either enzymatic cleavage or chemical reaction.
What is a pro drug give an example?
Prodrug: A precursor (forerunner) of a drug. For example, sulfasalazine is a prodrug. It is not active in its ingested form. It has to be broken down by bacteria in the colon into two products — 5-aminosalicylic acid (5ASA) and sulfapyridine — before becoming active as a drug.
What is drug bioavailability?
Bioavailability refers to the extent a substance or drug becomes completely available to its intended biological destination(s).
Why aspirin is given as a pro drug?
Aspirin was originally considered a prodrug to salicylic acid since it was at that time thought to have the same pharmacodynamic effects as salicylic acid and is rapidly transformed to it in vivo. Later aspirin was also found to be effective in its own right.
Is Benorylate a prodrug?
Benorylate is a bipartite mutual prodrug of aspirin and paracetamol, linked by an ester bond.
Is aspirin a prodrug?
Why are pro drugs developed?
Prodrugs are inactive precursors of therapeutic agents converted to the biologically active parent drug by enzymatic and/or chemical transformations in vivo (Ettmayer et al., 2003). They are commonly developed to resolve formulation, toxicity and drug delivery limitations of problematic agents.
Which drug has highest bioavailability?
Bioavailability of Drugs
- Drugs having low therapeutic index include:
- Therapeutic window is the range between the high therapeutic index and low therapeutic index.
- Drugs having 100% bioavailability include chlordiazepoxide, diazepam, lithium, metronidazole, phenobarbitol, salicylic acid, trimethoprin and valproic acid.