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Questions and Answers

What is the primary elimination route of Studentamine?

  • Hepatic metabolism (correct)
  • Renal excretion
  • Lymphatic elimination
  • Biliary excretion

    • What is the impact of genetic mutation on Studentamine metabolism?

  • Moderate effect due to CYP3A4 metabolism
  • Significant effect due to high CYP2D6 metabolism
  • Minimal effect due to low CYP2D6 metabolism (correct)
  • No effect on metabolism

    • Which of the following is likely to affect Studentamine's metabolism?

  • Orange juice
  • Cranberry juice
  • Pineapple juice
  • Grapefruit juice (correct)

    • What is the impact of renal function on Studentamine elimination?

    <p>Renal function has a minimal effect on elimination</p> Signup and view all the answers

    What is the likely effect of age on Studentamine's anticoagulant properties?

    <p>Significant effect on clotting cascade</p> Signup and view all the answers

    What is the primary factor determining Studentamine's hepatic clearance?

    <p>Fraction unbound</p> Signup and view all the answers

    What is the role of CYP1A2 in the body?

    <p>It plays a role in detoxification and activation of carcinogens, and is also a drug metabolizing enzyme</p> Signup and view all the answers

    Which of the following is a characteristic of CYP1A2 substrates?

    <p>They have a low hepatic extraction ratio</p> Signup and view all the answers

    What is the effect of smoking on CYP1A2 activity?

    <p>It induces CYP1A2 activity</p> Signup and view all the answers

    What is the difference in CYP1A2 activity between South Asians and Europeans?

    <p>South Asians have a lower CYP1A2 activity</p> Signup and view all the answers

    What is the reason for the variability in warfarin response?

    <p>It is due to multifactorial interactions between PK and PD factors</p> Signup and view all the answers

    Why are warfarin drug interactions clinically significant?

    <p>Because warfarin has a narrow therapeutic range</p> Signup and view all the answers

    What is the effect of vitamin K rich foods on warfarin response?

    <p>They decrease the effect of warfarin</p> Signup and view all the answers

    What is the importance of monitoring INR when starting or ceasing medicines for patients on warfarin?

    <p>It is necessary to monitor INR to detect changes in warfarin response</p> Signup and view all the answers

    Study Notes

    Variability in Response to Medicines

    • Ethnic differences in drug response are significant, particularly with regards to CYP1A2 activity.

    CYP1A2 Importance and Substrates

    • CYP1A2 is an important drug metabolizing enzyme, responsible for metabolizing theophylline and olanzapine.
    • It plays a role in detoxification and activation of carcinogens.
    • CYP1A2 substrates, inducers, and inhibitors can alter intrinsic clearance, which is crucial for drugs with low hepatic extraction ratio.

    Effect of Diet and Lifestyle on CYP1A2 Activity

    • CYP1A2 activity is lower in South Asians.
    • Smoking induces CYP1A2 activity, while the oral contraceptive pill inhibits it.

    Ethnic Differences in CYP1A2

    • South Asians have significantly lower CYP1A2 activity than Europeans.
    • Oral contraceptive use inhibits CYP1A2 activity, while smoking induces it.
    • There are ethnic differences in CYP1A2 inducers.

    Warfarin - Variability in INR

    • Warfarin has a very narrow safety margin, and its response is highly variable between individuals.
    • Determinants of warfarin response include age, organ function, genetic influences, dietary influences, concomitant medicines, and other factors.

    Warfarin Drug Interactions

    • Warfarin drug interactions are clinically significant due to its narrow therapeutic range and low extraction ratio in the liver.
    • Hepatic metabolism by CYP2C9 is important for warfarin.
    • Warfarin drug interactions can affect pharmacokinetics of warfarin, vitamin K, and blood clotting mechanisms.

    Studentamine (New Anticoagulant)

    • Studentamine is predominantly metabolized in the liver, with 10% renally cleared.
    • It has a low extraction ratio, making hepatic clearance mainly determined by fraction unbound.
    • Genetic mutation is not significant, as only 7% of CYP2D6 is metabolized.
    • Grapefruit and pomelo juice can affect Studentamine metabolism through CYP3A4 inhibition.
    • Ethnic differences may not be significant due to low CYP1A2 involvement.
    • Age may affect Studentamine metabolism, as it is an anticoagulant.

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