First-Pass Metabolism: Difference between revisions
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First-pass metabolism (also known as presystemic [[Metabolism|metabolism]]) refers to the action of metabolic [[Enzyme|enzymes]], in the [[Liver|liver]] and gut wall, on drugs <ref>Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. These enzymes metabolise drugs before they enter the [[Systemic Circulation|systemic circulation]], often rendering a fraction of the drug inactive <ref name="null">Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. This lowers the proportion of an ingested drug that is acquired by the systemic circulation in its active form (its [[Bioavailability|bioavailability]]).<ref>Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc</ref> | First-pass metabolism (also known as presystemic [[Metabolism|metabolism]]) refers to the action of metabolic [[Enzyme|enzymes]], in the [[Liver|liver]] and gut wall, on drugs <ref name="null">Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. These enzymes metabolise drugs before they enter the [[Systemic Circulation|systemic circulation]], often rendering a fraction of the drug inactive <ref name="null">Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. This lowers the proportion of an ingested drug that is acquired by the systemic circulation in its active form (its [[Bioavailability|bioavailability]]).<ref name="null">Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref> | ||
This form of metabolism is therapeutically relevant as... | This form of metabolism is therapeutically relevant as... | ||
#It implies that the [[Drug Efficacy|efficacy]] of a drug is lower when its route of administration is oral rather than intravenous. <ref name="null">Grahame-Smith D, Aronson J. (2002) Oxford Textbook of Clinical Pharmacology and Drug Therapy, 3rd Edition, Hong Kong: Oxford University Press.</ref>This frequently means that a higher dose is used when a drug is administered orally <ref name="null">Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. First-pass metabolism can reduce the bioavailability of some drugs to the extent that it renders them completely ineffective and makes oral administration unsuitable ([[Insulin|insulin]] is an example of this) <ref>Grahame-Smith D, Aronson J. (2002) Oxford Textbook of Clinical Pharmacology and Drug Therapy, 3rd Edition, Hong Kong: Oxford University Press.</ref>. | #It implies that the [[Drug Efficacy|efficacy]] of a drug is lower when its route of administration is oral rather than intravenous. <ref name="null">Grahame-Smith D, Aronson J. (2002) Oxford Textbook of Clinical Pharmacology and Drug Therapy, 3rd Edition, Hong Kong: Oxford University Press.</ref>This frequently means that a higher dose is used when a drug is administered orally <ref name="null">Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. First-pass metabolism can reduce the bioavailability of some drugs to the extent that it renders them completely ineffective and makes oral administration unsuitable ([[Insulin|insulin]] is an example of this) <ref>Grahame-Smith D, Aronson J. (2002) Oxford Textbook of Clinical Pharmacology and Drug Therapy, 3rd Edition, Hong Kong: Oxford University Press.</ref>. | ||
#First-Pass Metabolism differs between people <ref>Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. | #First-Pass Metabolism differs between people <ref name="null">Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc.</ref>. | ||
=== References === | === References === | ||
Revision as of 18:01, 14 November 2011
First-pass metabolism (also known as presystemic metabolism) refers to the action of metabolic enzymes, in the liver and gut wall, on drugs [1]. These enzymes metabolise drugs before they enter the systemic circulation, often rendering a fraction of the drug inactive [1]. This lowers the proportion of an ingested drug that is acquired by the systemic circulation in its active form (its bioavailability).[1]
This form of metabolism is therapeutically relevant as...
- It implies that the efficacy of a drug is lower when its route of administration is oral rather than intravenous. [1]This frequently means that a higher dose is used when a drug is administered orally [1]. First-pass metabolism can reduce the bioavailability of some drugs to the extent that it renders them completely ineffective and makes oral administration unsuitable (insulin is an example of this) [2].
- First-Pass Metabolism differs between people [1].
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 Rang H, Dale M, Ritter J, Flower R and Henderson G. (2012) Rang and Dale's Pharmacology, 7th Edition, Spain: Elsevier Inc. Cite error: Invalid
<ref>tag; name "null" defined multiple times with different content - ↑ Grahame-Smith D, Aronson J. (2002) Oxford Textbook of Clinical Pharmacology and Drug Therapy, 3rd Edition, Hong Kong: Oxford University Press.