Active metabolite

Short description: Form of a substance after metabolism

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An active metabolite, or pharmacologically active metabolite is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental chemical. Active metabolites may produce therapeutic effects, as well as harmful effects.[1]

## Contents

* 1 Metabolites of drugs
* 2 Prodrugs
* 3 References
* 4 Further reading

## Metabolites of drugs

An active metabolite results when a drug is metabolized by the body into a modified form which produces effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide). Certain drugs such as codeine and tramadol have metabolites (morphine and O-desmethyltramadol respectively) that are stronger than the parent drug[2][3][4] and in these cases the metabolite may be responsible for much of the therapeutic action of the parent drug. Sometimes, however, metabolites may produce toxic effects and patients must be monitored carefully to ensure they do not build up in the body. This is an issue with some well-known drugs, such as pethidine (meperidine) and dextropropoxyphene.[4][5]

## Prodrugs

Main article: Chemistry:Prodrug

Sometimes drugs are formulated in an inactive form that is designed to break down inside the body to form the active drug. These are called prodrugs. The reasons for this type of formulation may be because the drug is more stable during manufacture and storage as the prodrug form, or because the prodrug is better absorbed by the body or has superior pharmacokinetics (e.g., lisdexamphetamine).[6]

## References

1. ↑ Fura, Aberra (February 2006). "Role of pharmacologically active metabolites in drug discovery and development". Drug Discovery Today 11 (3–4): 133–142. doi:10.1016/S1359-6446(05)03681-0. PMID 16533711.
2. ↑ "On the assessment of drug metabolism by assays of codeine and its main metabolites". Therapeutic Drug Monitoring 22 (3): 258–65. June 2000. doi:10.1097/00007691-200006000-00005. PMID 10850391.
3. ↑ Raffa RB (July 1996). "A novel approach to the pharmacology of analgesics". The American Journal of Medicine 101 (1A): 40S–46S. doi:10.1016/s0002-9343(96)00137-4. PMID 8764759.
4. ↑ 4.0 4.1 "Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development". Current Medicinal Chemistry 16 (27): 3480–675. 2009. doi:10.2174/092986709789057635. PMID 19515014.
5. ↑ "Role of active metabolites in the use of opioids". European Journal of Clinical Pharmacology 65 (2): 121–39. February 2009. doi:10.1007/s00228-008-0570-y. PMID 18958460.
6. ↑ Müller CE (November 2009). "Prodrug approaches for enhancing the bioavailability of drugs with low solubility". Chemistry & Biodiversity 6 (11): 2071–83. doi:10.1002/cbdv.200900114. PMID 19937841.

## Further reading

* Nedderman, Angus N.R.; Walker, Don K. (2011). "Metabolite testing in drug development". in Bonate, Peter L.. Pharmacokinetics in Drug Development: Advances and Applications, Volume 3. Springer. ISBN 9781441979360. https://books.google.com/books?id=MUYUeKb_rpIC&pg=PA131.

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Combined substance use and adulteration

Combined substance use|

* Active metabolite
* Codrug
* Combination drug
* Combined drug intoxication
* Drug interaction
* Poly drug use
* Polypharmacy
* Polysubstance dependence
* Prodrug
* Synergy

Adulteration|

* Contamination
* Clandestine chemistry
* Cutting agent
* Diluent
* Impurity
* Lacing
* Mickey Finn

Harm reduction|

* Pill testing
* Reagent testing

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