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What is the primary function of Verapamil in the context of pharmacology?
What is the primary function of Verapamil in the context of pharmacology?
Which of the following drugs is an immune suppressive used in kidney and liver transplant patients?
Which of the following drugs is an immune suppressive used in kidney and liver transplant patients?
What is the primary consequence of Cytochrome P450 3A4 inhibition in clinical pharmacology?
What is the primary consequence of Cytochrome P450 3A4 inhibition in clinical pharmacology?
What is the role of transporters in drug interactions, according to Han (2011)?
What is the role of transporters in drug interactions, according to Han (2011)?
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Which of the following is a CP2C8 substrate?
Which of the following is a CP2C8 substrate?
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What is the primary mechanism of action of dietary nutraceuticals in enhancing anticancer drug activity, according to Khan et al. (2015)?
What is the primary mechanism of action of dietary nutraceuticals in enhancing anticancer drug activity, according to Khan et al. (2015)?
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Which enzyme is primarily responsible for metabolizing warfarin to 7-hydroxy warfarin?
Which enzyme is primarily responsible for metabolizing warfarin to 7-hydroxy warfarin?
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What is the effect of carbamazepine on warfarin metabolism?
What is the effect of carbamazepine on warfarin metabolism?
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What is the effect of grapefruit juice on intestinal drug metabolism?
What is the effect of grapefruit juice on intestinal drug metabolism?
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What percentage of variation in oral clearance of Cyclosporin A is accounted for by P-Glycoprotein (Pgp)?
What percentage of variation in oral clearance of Cyclosporin A is accounted for by P-Glycoprotein (Pgp)?
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What is the effect of St John's Wort on P-gp?
What is the effect of St John's Wort on P-gp?
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Which of the following is an example of an extrinsic factor that can impact drug efficacy?
Which of the following is an example of an extrinsic factor that can impact drug efficacy?
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What happens to gemfibrozil upon phase II metabolism?
What happens to gemfibrozil upon phase II metabolism?
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What is the term for the exchange of DNA with neighbours?
What is the term for the exchange of DNA with neighbours?
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What is the effect of amiodarone on warfarin metabolism?
What is the effect of amiodarone on warfarin metabolism?
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What is the name of the protein that pumps drugs back into the G.I. tract?
What is the name of the protein that pumps drugs back into the G.I. tract?
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What is the term for the process by which one allele has an advantage over another?
What is the term for the process by which one allele has an advantage over another?
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What is an example of a 'consumer drug' that can interact with pharmaceutical drugs?
What is an example of a 'consumer drug' that can interact with pharmaceutical drugs?
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What is the primary focus of the 2003 study mentioned in the text?
What is the primary focus of the 2003 study mentioned in the text?
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Which study found that prospective genetic screening decreases the incidence of abacavir hypersensitivity reactions?
Which study found that prospective genetic screening decreases the incidence of abacavir hypersensitivity reactions?
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What is the topic of the 2010 review by Sivasubramanian et al.?
What is the topic of the 2010 review by Sivasubramanian et al.?
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What is the role of HLA B∗5701 status according to the 2013 study by The UK Collaborative HIV Cohort Study Steering Committee?
What is the role of HLA B∗5701 status according to the 2013 study by The UK Collaborative HIV Cohort Study Steering Committee?
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What is the topic of the 2013 review by Yoshida et al.?
What is the topic of the 2013 review by Yoshida et al.?
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Which study discussed the importance of cancer drug resistance in the context of cancer treatment?
Which study discussed the importance of cancer drug resistance in the context of cancer treatment?
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Humans are exposed to fewer than 100 different chemicals every day.
Humans are exposed to fewer than 100 different chemicals every day.
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P-Glycoprotein (Pgp) is a drug transporter that pumps drugs into the G.I. tract.
P-Glycoprotein (Pgp) is a drug transporter that pumps drugs into the G.I. tract.
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Intrinsic factors that can impact drug efficacy include environmental factors such as grapefruit juice.
Intrinsic factors that can impact drug efficacy include environmental factors such as grapefruit juice.
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Random Drift is a process where one allele has an advantage over another.
Random Drift is a process where one allele has an advantage over another.
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Warfarin is an example of a 'perpetrator' drug in terms of drug-drug interactions.
Warfarin is an example of a 'perpetrator' drug in terms of drug-drug interactions.
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The primary focus of the lecture is to explain the rationale behind steps that can be taken to increase the risk of adverse effects or loss of efficacy in a drug.
The primary focus of the lecture is to explain the rationale behind steps that can be taken to increase the risk of adverse effects or loss of efficacy in a drug.
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Warfarin is primarily metabolized by CYP3A4.
Warfarin is primarily metabolized by CYP3A4.
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Fluvoxamine is a substrate of CYP2C9.
Fluvoxamine is a substrate of CYP2C9.
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Carbamazepine increases the effect of warfarin by inhibiting CYP2C9.
Carbamazepine increases the effect of warfarin by inhibiting CYP2C9.
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Grapefruit juice induces intestinal CYP3A4.
Grapefruit juice induces intestinal CYP3A4.
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Gemfibrozil becomes a potent inhibitor of CYP2C9 upon phase II metabolism.
Gemfibrozil becomes a potent inhibitor of CYP2C9 upon phase II metabolism.
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St. John's Wort is an inhibitor of P-gp.
St. John's Wort is an inhibitor of P-gp.
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Tacrolimus is used to treat kidney and liver transplant patients and is a CP2C8 substrate
Tacrolimus is used to treat kidney and liver transplant patients and is a CP2C8 substrate
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Verapamil is a P-gp inhibitor that can increase the bioavailability of certain drugs
Verapamil is a P-gp inhibitor that can increase the bioavailability of certain drugs
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Cytochrome P450 3A4 inhibition always leads to decreased drug efficacy
Cytochrome P450 3A4 inhibition always leads to decreased drug efficacy
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Rosiglitazone is a CP2C8 substrate that can also inhibit P-gp
Rosiglitazone is a CP2C8 substrate that can also inhibit P-gp
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Paclitaxel is a CP2C8 substrate that can be affected by the activity of P-gp
Paclitaxel is a CP2C8 substrate that can be affected by the activity of P-gp
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Dietary nutraceuticals can always enhance the activity of anticancer drugs
Dietary nutraceuticals can always enhance the activity of anticancer drugs
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The study by Holohan et al. (2013) discusses the role of HLA B∗5701 status in disease progression.
The study by Holohan et al. (2013) discusses the role of HLA B∗5701 status in disease progression.
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The 2003 study evaluated the toxicological relevance of CYP3A4 inhibition.
The 2003 study evaluated the toxicological relevance of CYP3A4 inhibition.
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The review by Sivasubramanian et al. (2010) focuses on the treatment of HIV using Abacavir/Lamivudine combination.
The review by Sivasubramanian et al. (2010) focuses on the treatment of HIV using Abacavir/Lamivudine combination.
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The study by Rauch et al. (2006) found that prospective genetic screening increases the incidence of abacavir hypersensitivity reactions.
The study by Rauch et al. (2006) found that prospective genetic screening increases the incidence of abacavir hypersensitivity reactions.
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The study by The UK Collaborative HIV Cohort Study Steering Committee (2013) found that HLA B∗5701 status has no impact on disease progression.
The study by The UK Collaborative HIV Cohort Study Steering Committee (2013) found that HLA B∗5701 status has no impact on disease progression.
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The review by Yoshida et al. (2013) focuses on the role of transporters in drug interactions and genetic polymorphisms.
The review by Yoshida et al. (2013) focuses on the role of transporters in drug interactions and genetic polymorphisms.
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Study Notes
Factors Affecting Drug Efficacy
- Drug interactions can occur with pharmaceuticals, consumer drugs, foodstuffs, and environmental chemicals, leading to adverse effects or loss of efficacy
- Intrinsic factors, such as genetics, can impact drug interactions and efficacy
- Extrinsic factors, such as environmental chemicals, can also affect drug interactions and efficacy
Cellular Effects
- Changes in metabolism enzymes can affect drug interactions and efficacy
- Tissue effects, such as inflammation, can also impact drug interactions and efficacy
Environmental Factors
- Humans are exposed to thousands of chemicals daily, which can interact with biological systems
- Pharmaceutical interactions can occur between different drugs, leading to adverse effects or loss of efficacy
- Induction, inhibition, and food-drug interactions can all impact drug efficacy
Intrinsic Factors: Genetics
- Genetic mutations, errors in DNA copying, and genetic drift can all impact drug interactions and efficacy
- Genetic variations can affect drug transporters, such as P-glycoprotein (Pgp), which pumps drugs out of the body
- Genetic variations can also affect drug-metabolizing enzymes, such as CYP2C9, which can impact warfarin metabolism
Drug Transporters
- P-glycoprotein (Pgp) is a drug transporter that pumps drugs out of the body
- Pgp can affect the oral clearance of drugs, such as Cyclosporin A
- Inducers of Pgp, such as St. John's Wort, can decrease drug efficacy
- Inhibitors of Pgp, such as grapefruit juice, can increase drug efficacy
Warfarin Metabolism
- Warfarin has a narrow therapeutic window and is metabolized by multiple enzymes, including CYP2C9
- Substrates for CYP2C9, such as fluvoxamine, can interact with warfarin
- Inhibitors of CYP2C9, such as gemfibrozil, can increase warfarin's effect
- Inducers of CYP4A4 and CYP1A2, such as carbamazepine and clozapine, can decrease warfarin's effect
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Description
This quiz covers the factors that influence a drug's effectiveness in the body. Learn about intrinsic and extrinsic factors affecting drug interaction and how to minimize adverse effects and loss of efficacy. Test your knowledge of pharmacology!
