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Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase01:27

Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase

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Phase II biotransformation reactions are essential for detoxifying and eliminating xenobiotics, including many pharmaceutical compounds. These reactions typically involve conjugation, the covalent attachment of polar endogenous groups such as glucuronic acid, sulfate, methyl, or acetyl moieties to functional groups introduced during Phase I metabolism. The resulting conjugates are more water-soluble, enabling efficient renal or biliary excretion.The major classes of Phase II enzymes include...
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Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

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α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
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Therapeutic Drug Monitoring: Affecting Factors01:29

Therapeutic Drug Monitoring: Affecting Factors

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Therapeutic Drug Monitoring (TDM) is the clinical practice of measuring specific drug levels in a patient's blood or body tissues to manage and optimize therapy. TDM is crucial for drugs with narrow therapeutic windows, like warfarin and phenytoin, where incorrect doses can lead to treatment failure or severe side effects. This monitoring ensures the dosage administered is within a safe and effective range. The factors affecting therapeutic drug monitoring include:Patient-Specific Factors:a.
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Crohn's disease is an inflammatory bowel disorder marked by chronic inflammation of the GI tract. Various treatment strategies for Crohn's disease are employed, such as immunomodulatory agents, glucocorticoids, and biologics or anti-TNF therapy. Azathioprine (Imuran), a commonly used immunomodulatory drug for Crohn's disease, is converted in the body to mercaptopurine, which inhibits purine biosynthesis and cell proliferation. Both are utilized in severe cases of Inflammatory Bowel...
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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
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Related Experiment Video

Updated: May 1, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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Glucarpidase Intervention for Delayed Methotrexate Clearance.

Jennifer L Cavone1, Daisy Yang2, Alice Wang1

  • 1The University of Texas MD Anderson Cancer Center, Houston, TX, USA.

The Annals of Pharmacotherapy
|April 19, 2014
PubMed
Summary
This summary is machine-generated.

Glucarpidase effectively reduces high serum methotrexate levels in patients with delayed clearance or kidney issues. This drug should be reserved for cases unresponsive to standard care due to its cost.

Keywords:
carboxypeptidaseglucarpidasemethotrexate

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Area of Science:

  • Pharmacology
  • Oncology
  • Clinical Practice

Background:

  • High-dose methotrexate (HD-MTX) is a critical chemotherapy agent.
  • Delayed methotrexate clearance and renal dysfunction can lead to severe toxicity.
  • Effective rescue strategies are essential for managing HD-MTX therapy.

Conclusions:

  • Glucarpidase is effective in lowering sMTX in patients with delayed clearance and renal dysfunction.
  • Due to its cost, glucarpidase should be reserved for specific patients.
  • It is recommended for patients unresponsive to standard supportive care measures.