Irinotecan and Doxorubicin Overview
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Irinotecan and Doxorubicin Overview

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Questions and Answers

What type of drug is irinotecan classified as?

  • Inhibitor of topoisomerase (correct)
  • Anticancerous targeted therapy
  • Immunotherapy
  • Antifolique

    • Which of the following drugs is NOT an alkylant?

  • Cyclophosphamide
  • Cisplatin
  • Bleomycin
  • Methotrexate (correct)

    • Which delivery method is mentioned for irinotecan?

  • Topical application
  • Intramuscular injection
  • Intravenous infusion (correct)
  • Oral administration

    • What is a common side effect of topoisomerase inhibitors such as irinotecan?

    <p>Nausea and vomiting</p> Signup and view all the answers

    Which drug is identified as an example of targeted anticancer therapy?

    <p>Imatinib</p> Signup and view all the answers

    Which of the following correctly describes the administration form of irinotecan?

    <p>Dilutable solution for infusion</p> Signup and view all the answers

    What type of agent is vincristine classified as?

    <p>Microtubule poison</p> Signup and view all the answers

    Which mechanism of action do antifoliques, like methotrexate, primarily target?

    <p>Folate metabolism</p> Signup and view all the answers

    What process involves the conversion of irinotecan to the active metabolite SN-38?

    <p>Hydrolysis</p> Signup and view all the answers

    Which enzyme is responsible for the oxidation of the terminal piperidine ring of irinotecan?

    <p>CYP3A4</p> Signup and view all the answers

    How is SN-38 eliminated from the body after glucuronidation?

    <p>Through both feces and urine</p> Signup and view all the answers

    What percentage of the intravenously administered dose of irinotecan is excreted unchanged?

    <p>More than 50%</p> Signup and view all the answers

    What effect do anticonvulsants such as carbamazepine have on irinotecan and its metabolites?

    <p>Decrease plasma concentrations</p> Signup and view all the answers

    Which of the following inhibitors may lead to increased systemic exposure to SN-38 when co-administered with irinotecan?

    <p>Erlotinib</p> Signup and view all the answers

    What is the terminal phase half-life of irinotecan?

    <p>10 hours</p> Signup and view all the answers

    What is the role of glucuronidation in the metabolism of SN-38?

    <p>Produces an inactive metabolite</p> Signup and view all the answers

    What is the primary route of administration for Doxorubicin?

    <p>Intravenous administration</p> Signup and view all the answers

    What is the typical dose of Doxorubicin for monotherapy in adults?

    <p>75 mg/m² every 3 weeks</p> Signup and view all the answers

    Which of the following cancers is NOT indicated for treatment with Doxorubicin?

    <p>Pancreatic cancer</p> Signup and view all the answers

    Which metabolite of Doxorubicin is considered to be active?

    <p>Doxorubicinol</p> Signup and view all the answers

    What is the plasma protein binding percentage range for Doxorubicin?

    <p>50-85%</p> Signup and view all the answers

    How long is the terminal half-life of Doxorubicin?

    <p>17 hours</p> Signup and view all the answers

    What is the clearance rate of Doxorubicin in ml/min/m²?

    <p>400-583 ml/min/m²</p> Signup and view all the answers

    Which statement about the distribution of Doxorubicin is correct?

    <p>It reaches higher concentrations in ascites than in plasma.</p> Signup and view all the answers

    What effect does verapamil have on doxorubicin?

    <p>It increases doxorubicin concentration and clinical effects.</p> Signup and view all the answers

    What is the mechanism of action of doxorubicin?

    <p>It forms free radicals causing strand breakage.</p> Signup and view all the answers

    Which of the following does NOT contraindicate the use of doxorubicin?

    <p>Mild liver impairment</p> Signup and view all the answers

    What are the side effects associated with bortezomib?

    <p>Prevention of protein degradation</p> Signup and view all the answers

    What is a potential risk when doxorubicin is used concurrently with trastuzumab?

    <p>Increased risk of cardiac dysfunction</p> Signup and view all the answers

    Which option correctly describes an effect of doxorubicin?

    <p>It commonly causes fever.</p> Signup and view all the answers

    Which of the following side effects occurs most frequently in patients receiving doxorubicin?

    <p>Vomiting</p> Signup and view all the answers

    What is the effect of using ciclosporin in combination with doxorubicin?

    <p>It increases the concentration of doxorubicin.</p> Signup and view all the answers

    What is a key characteristic of bortezomib?

    <p>It is a proteasome inhibitor.</p> Signup and view all the answers

    Doxorubicin dosage is typically administered how often?

    <p>Every 3 weeks at 75 mg/m²</p> Signup and view all the answers

    Which antineoplastic drug, when given before doxorubicin, is known to increase its plasma concentrations?

    <p>Paclitaxel</p> Signup and view all the answers

    What type of myelosuppression is associated with doxorubicin?

    <p>Leukopenia</p> Signup and view all the answers

    Which of the following is NOT an indication for the use of doxorubicin?

    <p>Chronic myeloid leukemia</p> Signup and view all the answers

    What class of drug does bortezomib belong to?

    <p>Proteasome inhibitors</p> Signup and view all the answers

    What may occur as a result of doxorubicin enhancing the effects of 6-mercaptopurine?

    <p>Increased risk of liver damage</p> Signup and view all the answers

    What is a significant interaction consideration for doxorubicin?

    <p>CYP3A4 inducers and inhibitors</p> Signup and view all the answers

    Study Notes

    Irinotecan

    • Irinotecan is a single-dose vial dilutable solution used for infusion.
    • Irinotecan's metabolism involves hydrolysis by carboxylesterases (CE) to its active metabolite SN-38, oxidation by CYP3A4, and glucuronidation by UGT1A1 to an inactive metabolite, SN-38 glucuronide (SN-38G).
    • Irinotecan is primarily eliminated unchanged, with 33% excreted in feces and 22% in urine.
    • Irinotecan's half-life is approximately 10 hours.
    • CYP3A4 and/or UGT1A1 inhibitors can increase systemic exposure to irinotecan or SN-38.
    • Anticonvulsants (e.g. carbamazepine, phenobarbital, or phenytoin) decrease irinotecan and its metabolites' plasma concentrations.
    • Ketoconazole treatment results in a significant decrease in glutamine metabolite AUC and a marked increase in SN-38 AUC.

    Doxorubicin

    • Doxorubicin is an antibiotic anthracycline derivative used as an antineoplastic drug.
    • Doxorubicin inhibits DNA and RNA synthesis, acting specifically during the S-phase of the cell cycle.
    • Doxorubicin can cause free radical formation, leading to DNA strand breakage.
    • Doxorubicin is used to treat various solid tumors, including breast, bronchial, soft tissue sarcoma, osteosarcoma, gynecological, bladder, testicular, thyroid, Ewing's sarcoma, nephroblastoma, neuroblastoma, and others.
    • Doxorubicin is administered intravenously, typically over 3-10 minutes, but prolonged infusions (48-96 hours) may be used in specific cases.
    • Doxorubicin is widely distributed with a volume of 700-1100 l/m², but it crosses the cerebrospinal fluid minimally.
    • Doxorubicin exhibits high concentrations in ascites.
    • Doxorubicin's half-life is around 17 hours, while its metabolite doxorubicinol has a half life of 30-50 hours.
    • Inhibitors of CYP3A4, CYP2D6, and P-glycoprotein (e.g. verapamil) can increase doxorubicin's concentration and clinical effects.
    • Inducers of CYP3A4 (e.g. phenobarbital, phenytoin) and P-glycoprotein decrease doxorubicin's concentration.
    • Ciclosporin and doxorubicin co-administration elevates doxorubicin's concentration.
    • Doxorubicin increases the toxicity of other antineoplastic therapies, and vice versa.
    • Concurrent use of doxorubicin with trastuzumab increases the risk of cardiac dysfunction (cardiotoxicity).
    • Prior administration of paclitaxel increases the plasma concentrations of doxorubicin and its metabolites.
    • Doxorubicin may potentiate hepatotoxicity caused by 6-mercaptopurine.
    • Doxorubicin is contraindicated in patients with hypersensitivity, pre-existing bone marrow suppression, liver impairment, severe heart failure, recent myocardial infarction, acute myocardial disease of inflammatory origin, severe arrhythmias, pregnant or breastfeeding women.
    • Common side effects of doxorubicin include myelosuppression, cardiomyopathy, gastrointestinal disorders (mucosal inflammation/stomatitis, vomiting, nausea, diarrhea, decreased appetite), secondary malignancies (e.g., secondary AML), extravasation, tissue necrosis, alopecia, fever, pain, and swelling at the intravenous site.

    Bortezomib

    • Bortezomib is a dipeptide boronic acid derivative and a proteasome inhibitor.
    • Bortezomib reversibly binds to the chymotrypsin-like subunit of the 26S proteasome.
    • This binding inhibits the proteasome and prevents degradation of various pro-apoptotic factors.

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    Description

    This quiz provides an overview of the pharmacology and metabolism of two important oncology drugs: Irinotecan and Doxorubicin. It covers their mechanisms of action, metabolism, and implications for drug interactions. Test your knowledge of these critical chemotherapeutic agents.

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