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GP04 [Jul97] Rectal administration of drugs:

A. Gives predictable blood levels
B. From lower 1/3rd avoids first pass & upper 2/3rds doesn't C. None undergoes first pass metabolism
D. All of it undergoes first pass metabolism
E. ?

User Ironfist
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1 Answer

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Final answer:

Rectal drug administration can bypass first-pass metabolism when drugs are absorbed from the lower one-third of the rectum as they enter the systemic circulation directly. Absorption from the upper two-thirds, however, is subject to first-pass metabolism via the liver. This method's predictability and extent of metabolism depend on drug properties and formulation.

Step-by-step explanation:

The concept of rectal administration of drugs is relevant to the field of medicine, specifically pharmacokinetics. Rectal administration is a method of drug delivery that is used when drugs cannot be administered orally due to issues such as poor gastrointestinal absorption or the need to avoid the gastrointestinal tract because of vomiting or other issues. When rectal delivery is used, part of the administered dose can indeed avoid the first-pass metabolism, mainly if the drug is absorbed in the lower one-third of the rectum. This is because the lower rectum's venous blood supply is connected to the systemic circulation directly, bypassing the liver. In contrast, the upper two-thirds of the rectum drain into the portal circulation, which can then be subject to first-pass metabolism in the liver.

The degree to which rectal drug administration bypasses first-pass metabolism depends on the extent to which a drug is absorbed through the lower versus the upper parts of the rectum. Moreover, the pharmacokinetic profile of rectally administered drugs, including the predictability of blood levels, depends on various factors, such as drug formulation, the chemical properties of the drug, and the physiological conditions of the patient. The venous drainage from the lower part of the rectum is such that it avoids the liver initially, resulting in less first-pass metabolism, while the upper part drains into the portal system, meaning it would be subject to liver metabolism.

User Ralphje
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