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Serotonin Antagonists & Antifibrinolytic Agents
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Serotonin Antagonists & Antifibrinolytic Agents

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Questions and Answers

What is the main clinical use of Ondansetron (Zofran®)?

  • Treatment of postoperative hypotension
  • Treatment of severe hepatic impairment
  • Prevention of postoperative headache
  • Prevention of chemotherapy-induced nausea and vomiting (correct)

    • Which enzyme is inhibited by aprotinin at high concentrations?

  • Plasmin
  • Thrombin
  • Protein C
  • Kallikrein (correct)

    • How is Ondansetron metabolized in the body?

  • Excretion only through the liver
  • Metabolized by several CYP 450 enzyme systems (correct)
  • Primarily excreted through the kidney
  • Mainly metabolized via plasma carbonyl reductase enzyme

    • What is the role of lysine analogs in hyperfibrinolysis?

    <p>Inhibit fibrinolysis</p> Signup and view all the answers

    What is the main effect of aprotinin use in cardio-pulmonary bypass (CPB)?

    <p>Reduced need for blood transfusions</p> Signup and view all the answers

    Which drug interaction is contraindicated with Ondansetron due to the risk of hypotension?

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

    What is Dolasetron (Anzemet®) mainly used for?

    <p>Prevention of chemotherapy-induced nausea and vomiting</p> Signup and view all the answers

    Which adverse reaction is specifically associated with aprotinin derived from bovine origin?

    <p>Anaphylactic shock</p> Signup and view all the answers

    How is Dolasetron metabolized in the body?

    <p>Metabolized by plasma carbonyl reductase enzyme</p> Signup and view all the answers

    What mechanism of action does tranexamic acid (Cyklokapron®) have?

    <p>Inhibition of plasmin</p> Signup and view all the answers

    How does aminocaproic acid (Amicar®) prevent excessive bleeding?

    <p>By inhibiting lysine binding sites on plasminogen</p> Signup and view all the answers

    What is the route of elimination for Ondansetron?

    <p>~5% excreted in the kidney</p> Signup and view all the answers

    What is the main site of action for selective 5-HT3 receptor antagonists to exert their anti-emetic effects?

    <p>Centrally in the chemoreceptor trigger zone</p> Signup and view all the answers

    Which of the following is true regarding the metabolism of selective 5-HT3 receptor antagonists?

    <p>Dolasetron is not metabolized by liver CYP450 enzymes.</p> Signup and view all the answers

    What is the main reason to avoid using selective 5-HT3 receptor antagonists in patients with congenital long QT syndrome?

    <p>They can cause dose-dependent QT prolongation.</p> Signup and view all the answers

    Which of the following adverse effects is NOT commonly associated with selective 5-HT3 receptor antagonists?

    <p>QT prolongation</p> Signup and view all the answers

    What is a unique feature of dolasetron among the selective 5-HT3 receptor antagonists?

    <p>It does not require hepatic metabolism.</p> Signup and view all the answers

    What precaution should be taken when administering selective 5-HT3 receptor antagonists to patients with electrolyte abnormalities?

    <p>Monitor ECG for QT prolongation.</p> Signup and view all the answers

    What is the primary route of elimination for Aminocaproic Acid?

    <p>Renal excretion</p> Signup and view all the answers

    Why is caution advised when using Aminocaproic Acid in renal failure patients?

    <p>It may accumulate in the body due to impaired elimination</p> Signup and view all the answers

    What effect does Aminocaproic Acid have on fibrin degradation?

    <p>It inhibits fibrin degradation</p> Signup and view all the answers

    In which condition should Aminocaproic Acid not be used without concomitant heparin?

    <p>Disseminated intravascular coagulation (DIC)</p> Signup and view all the answers

    What adverse effects may result from the rapid intravenous administration of Aminocaproic Acid?

    <p>Hypotension, bradycardia, and/or arrhythmia</p> Signup and view all the answers

    What distinguishes the impact of Aminocaproic Acid on clotting or thrombosis?

    <p>Presence of disseminated intravascular coagulation (DIC)</p> Signup and view all the answers

    Which adverse effect of Tranexamic Acid is believed to be caused by blocking GABA receptors in the frontal cortex?

    <p>Convulsions/Seizures</p> Signup and view all the answers

    What potential thrombotic complication is associated with Tranexamic Acid administration?

    <p>Deep vein thrombosis (DVT)</p> Signup and view all the answers

    Why should Tranexamic Acid not be used in patients with acquired defective color vision?

    <p>Prevents measuring an important endpoint</p> Signup and view all the answers

    What is the major concern when administering Tranexamic Acid rapidly intravenously?

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

    Which condition should be avoided when considering the use of Tranexamic Acid?

    <p>Subarachnoid hemorrhage</p> Signup and view all the answers

    What potential rare complication has been reported following prolonged administration of Tranexamic Acid?

    <p>Skeletal muscle weakness with necrosis</p> Signup and view all the answers

    What is a common adverse effect associated with selective 5-HT3 receptor antagonists?

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

    Which enzyme system is responsible for the metabolism of most selective 5-HT3 receptor antagonists?

    <p>Cytochrome P450</p> Signup and view all the answers

    What effect can 5-HT3 antagonists have on the QT interval?

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

    Which 5-HT3 antagonist has the shortest serum half-life among the listed options?

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

    What is a serious potential complication associated with the prolonged use of 5-HT3 antagonists?

    <p>Serotonin syndrome</p> Signup and view all the answers

    What is a key recommendation for using 5-HT3 antagonists in patients with congenital long QT syndrome?

    <p>Close ECG monitoring</p> Signup and view all the answers

    Where are 5-HT3 receptors predominantly located in the central nervous system?

    <p>Solitary tract nucleus (STN)</p> Signup and view all the answers

    What type of receptors are ALL 5-HT receptors, except 5-HT3 receptors?

    <p>G protein-coupled receptors</p> Signup and view all the answers

    Which 5-HT receptor subtype is NOT linked to G proteins and instead functions as a ligand-gated ion channel?

    <p>5-HT3</p> Signup and view all the answers

    What is the primary basis for the anti-emetic property of 5-HT3 receptor antagonists?

    <p>Blockade of 5-HT3 receptors in the central nervous system</p> Signup and view all the answers

    Which selective 5-HT3 receptor antagonist is considered superior to others in the management of acute/delayed emesis?

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

    What is the mechanism of action of aprotinin?

    <p>Inhibits serine protease enzymes</p> Signup and view all the answers

    Why is aprotinin still available as an investigational drug despite its increased risk of death compared to other agents?

    <p>It enhances red blood cell transfusions</p> Signup and view all the answers

    Which enzymes are inhibited by aprotinin among the following?

    <p>Trypsin and elastase</p> Signup and view all the answers

    What is the main effect of aprotinin on fibrinolysis?

    <p>Inhibits fibrinolysis</p> Signup and view all the answers

    How does aprotinin impact inflammatory responses?

    <p>Reduces inflammatory mediators</p> Signup and view all the answers

    What is the source of aprotinin?

    <p>Bovine lung tissue</p> Signup and view all the answers

    What is a unique feature of benzyl alcohol in Aminocaproic Acid injection product?

    <p>Causes muscle weakness</p> Signup and view all the answers

    What is the primary concern when administering Aminocaproic Acid to premature neonates?

    <p>Gasping Syndrome</p> Signup and view all the answers

    Which adverse reaction is commonly associated with prolonged administration of Aminocaproic Acid?

    <p>Skeletal muscle weakness</p> Signup and view all the answers

    What is a distinguishing factor between the oral and IV forms of Tranexamic Acid?

    <p>Use in menstrual bleeding treatment</p> Signup and view all the answers

    In what manner does Tranexamic Acid act as an inhibitor?

    <p>Inhibits lysine binding sites</p> Signup and view all the answers

    What is the main route of elimination for Aminocaproic Acid?

    <p>Renal excretion</p> Signup and view all the answers

    What is a contraindication for using Tranexamic Acid (Cyklokapron®)?

    <p>Patients with acquired defective color vision</p> Signup and view all the answers

    Why should rapid intravenous administration of Tranexamic Acid (Cyklokapron®) be avoided?

    <p>To avoid hypotension</p> Signup and view all the answers

    What is a rare adverse effect that may be caused by Tranexamic Acid (Cyklokapron®) blocking GABA receptors in the frontal cortex?

    <p>Convulsions/seizures</p> Signup and view all the answers

    What is the suspected mechanism behind the risk of convulsions/seizures with Tranexamic Acid (Cyklokapron®) at higher doses?

    <p>Blocking GABA receptors in the frontal cortex</p> Signup and view all the answers

    What adverse effect of Tranexamic Acid (Cyklokapron®) should prompt immediate referral to an ophthalmologist?

    <p>Retinal venous and arterial occlusions</p> Signup and view all the answers

    Why should Tranexamic Acid (Cyklokapron®) not be administered undiluted?

    <p>To reduce the risk of thrombosis</p> Signup and view all the answers

    Where are 5-HT3 receptors predominantly located?

    <p>Central nervous system</p> Signup and view all the answers

    What is the primary basis for the anti-emetic property of 5-HT3 receptor antagonists?

    <p>Antagonism of 5-HT3 receptors</p> Signup and view all the answers

    Which neurotransmitter is primarily affected by selective 5-HT3 receptor antagonists?

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

    What is the main route of elimination for selective 5-HT3 receptor antagonists?

    <p>Renal excretion</p> Signup and view all the answers

    Which area has the highest concentration of 5-HT3 receptor subtype in the central nervous system?

    <p>Solitary tract nucleus (STN)</p> Signup and view all the answers

    What type of receptor is the 5-HT3 receptor subtype?

    <p>Ligand-gated ion channel</p> Signup and view all the answers

    What is the primary mechanism of action of aprotinin?

    <p>Inhibiting fibrinolysis</p> Signup and view all the answers

    Why is aprotinin still available as an investigational drug despite an increased risk of death compared to other agents?

    <p>Because of its ability to reduce the need for red blood cell transfusions</p> Signup and view all the answers

    Which enzyme is NOT inhibited by aprotinin?

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

    What is the source of aprotinin?

    <p>Derived from bovine lung tissue</p> Signup and view all the answers

    Which of the following is a characteristic effect of aprotinin on thrombin?

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

    How does aprotinin affect inflammatory responses?

    <p>Suppresses inflammatory responses</p> Signup and view all the answers

    Which enzyme is aprotinin primarily known to inhibit at low concentrations?

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

    What is the primary use of lysine analogs in the context of surgical procedures?

    <p>To inhibit clot formation</p> Signup and view all the answers

    In which surgical procedure is the use of aprotinin particularly beneficial in reducing the need for allogeneic blood transfusions?

    <p>Coronary artery bypass grafting (CABG)</p> Signup and view all the answers

    What is the mechanism of action of aminocaproic acid (Amicar®) in the context of fibrinolysis?

    <p>Inhibition of plasminogen activation</p> Signup and view all the answers

    What is a potential adverse effect specifically associated with aprotinin being derived from bovine origin?

    <p>Anaphylactic shock</p> Signup and view all the answers

    Which FDA-approved product is a lysine analog used as an antifibrinolytic agent?

    <p>Tranexamic Acid (Cyklokapron®)</p> Signup and view all the answers

    Which selective 5-HT3 receptor antagonist is indicated only for women with severe diarrhea-predominant irritable bowel syndrome?

    <p>Dolasetron (Anzemet®)</p> Signup and view all the answers

    Which of the selective 5-HT3 receptor antagonists is available in both oral and intravenous dosage forms?

    <p>Ondansetron (Zofran®)</p> Signup and view all the answers

    Which selective 5-HT3 receptor antagonist is specifically contraindicated for the prevention/treatment of nausea/vomiting?

    <p>Dolasetron (Anzemet®)</p> Signup and view all the answers

    Which selective 5-HT3 receptor antagonist is solely available in an intravenous dosage form?

    <p>Palonosetron (Aloxi®)</p> Signup and view all the answers

    Which selective 5-HT3 receptor antagonist selectively binds to and inhibits 5-HT3 receptors to prevent nausea/vomiting?

    <p>Ondansetron (Zofran®)</p> Signup and view all the answers

    What adverse effect has been rarely reported with Tranexamic Acid (Cyklokapron®) administration?

    <p>Skeletal muscle weakness</p> Signup and view all the answers

    Which complication is associated with rapid intravenous administration of Tranexamic Acid (Cyklokapron®)?

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

    In which patients should Tranexamic Acid (Cyklokapron®) not be used according to the text?

    <p>Patients with acquired defective color vision</p> Signup and view all the answers

    What adverse reaction may occur due to the rapid intravenous administration of Tranexamic Acid (Cyklokapron®)?

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

    Why should Tranexamic Acid (Cyklokapron®) not be administered with Factor IX Complex concentrates or Anti-Inhibitor Coagulant concentrates?

    <p>To prevent an increased risk of thrombosis</p> Signup and view all the answers

    What visual defect has been rarely reported with Tranexamic Acid (Cyklokapron®) use?

    <p>Color vision changes</p> Signup and view all the answers

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