Flockhart Table and P450 Drug Interactions

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Questions and Answers

Which of the following substances is known to interact with multiple medications according to the Flockhart Table?

  • Omeprazole
  • Troglitazone
  • St. John's Wort (correct)
  • Phenobarbital

Which medication is indicated to interact with oxcarbazepine according to the content?

  • Phenytoin (correct)
  • Pioglitazone
  • Tobacco
  • Rifabutin

Which of the following is not listed as having an interaction with the medications mentioned?

  • Citalopram (correct)
  • Omeprazole
  • Rifampin
  • St. John's Wort

Which substance is commonly associated with inducing liver enzymes and is known for its interactions?

<p>Rifampin (B)</p> Signup and view all the answers

Which of the following medications is noted for having several drug-drug interactions?

<p>Phenobarbital (B)</p> Signup and view all the answers

Which medication is a substrate of CYP1A2?

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

Which of the following medications is NOT a substrate of CYP2D6?

<p>Hydrocodone (D)</p> Signup and view all the answers

Which drug is identified as a substrate of CYP3A4?

<p>Aprepitant (C)</p> Signup and view all the answers

Which of the following is TRUE about atorvastatin?

<p>It is an inhibitor of HMG CoA reductase. (A)</p> Signup and view all the answers

What is the role of inhibitors in drug metabolism?

<p>They compete with substrates for enzyme binding. (D)</p> Signup and view all the answers

Which of the following medications does NOT inhibit HMG CoA reductase?

<p>Risperidone (C)</p> Signup and view all the answers

Which of these drugs is a CYP2C9 substrate?

<p>Nortriptyline (B)</p> Signup and view all the answers

Which of the following defines a strong inhibitor?

<p>Causes a &gt; 5-fold increase in plasma AUC values. (B)</p> Signup and view all the answers

What constitutes a moderate inhibitor?

<p>An increase in plasma AUC by more than 2-fold. (B)</p> Signup and view all the answers

Which drug is commonly known for its interactions with CYP2C19?

<p>Nisoldipine (B)</p> Signup and view all the answers

Which medication is NOT a substrate of CYP2B6?

<p>Cilostazol (B)</p> Signup and view all the answers

Which of these drugs is NOT listed as a substrate?

<p>aspirin (B)</p> Signup and view all the answers

Which of the following is a known CYP3A4 substrate?

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

Which of the following describes a weak inhibitor?

<p>An increase in plasma AUC of 1.5-fold. (C)</p> Signup and view all the answers

Which medication is an example of a CYP2C8 substrate?

<p>Perhexiline (B)</p> Signup and view all the answers

What can be a consequence of using a strong inhibitor with a substrate?

<p>The response to the medication may become ineffective. (B)</p> Signup and view all the answers

What is the expected plasma AUC increase for a moderate inhibitor?

<p>More than 2-fold. (C)</p> Signup and view all the answers

Which enzyme is mentioned as part of the substrate-related information?

<p>2B6 (A)</p> Signup and view all the answers

Which drug is known to induce the enzyme CYP2B6?

<p>Phenobarbital (C)</p> Signup and view all the answers

Which of the following substances acts as an inducer for multiple cytochrome P450 enzymes?

<p>St. John's Wort (B)</p> Signup and view all the answers

What is the role of inducers in drug metabolism?

<p>They enhance enzyme activity. (D)</p> Signup and view all the answers

Which food item is listed as an inducer for the enzyme CYP1A2?

<p>Broccoli (A)</p> Signup and view all the answers

Which drug is NOT an inducer of CYP2C9?

<p>Phenobarbital (C)</p> Signup and view all the answers

Which of the following is associated with the induction of CYP3A4?

<p>Barbiturates (C)</p> Signup and view all the answers

Which drug is known to be a substrate of the 2D6 enzyme?

<p>Propranolol (C)</p> Signup and view all the answers

What is a common characteristic of drugs like efavirenz and nevirapine?

<p>They are known inducers. (D)</p> Signup and view all the answers

Which medication is a substrate of the 3A4 enzyme?

<p>Dexamethasone (B), Tamoxifen (C)</p> Signup and view all the answers

What is a common substrate of the 2C9 enzyme?

<p>Finasteride (A)</p> Signup and view all the answers

Which of the following medications is listed as an inducer of CYP2D6?

<p>Dexamethasone (D)</p> Signup and view all the answers

Which drug is associated with the 2B6 enzyme?

<p>Domperidone (A)</p> Signup and view all the answers

Which of the following drugs is not metabolized by the 2E1 enzyme?

<p>Romidepsin (C)</p> Signup and view all the answers

Identify a substrate for the 2C19 enzyme from the options below.

<p>Tamoxifen (B)</p> Signup and view all the answers

Which drug is a well-known substrate of the 2C8 enzyme?

<p>Nateglinide (D)</p> Signup and view all the answers

Which of the following drugs is metabolized by the 3A4, 5, or 7 enzymes?

<p>Nevirapine (C)</p> Signup and view all the answers

Which medication has no relationship with the 2D6 enzyme?

<p>Eplerenone (B)</p> Signup and view all the answers

Which of these drugs is NOT a substrate of the 2C9 enzyme?

<p>Romidepsin (B)</p> Signup and view all the answers

Which of the following drugs is a substrate for P450 2D6?

<p>Tamoxifen (A), Citalopram (D)</p> Signup and view all the answers

Which type of drug increases the enzyme's ability to metabolize substrates?

<p>Activators (A)</p> Signup and view all the answers

Which of the following is NOT a substrate for P450 1A2?

<p>Propranolol (D)</p> Signup and view all the answers

What can prescribers anticipate by knowing the dominant cytochrome P450 isoform of a drug?

<p>Possible metabolic interactions with other drugs. (B)</p> Signup and view all the answers

Which of the following statements about substrates is true?

<p>They are metabolized by enzymes. (B)</p> Signup and view all the answers

Which drug class is a known inhibitor of P450 2C19?

<p>Proton Pump Inhibitors (D)</p> Signup and view all the answers

Which substrate is associated with the drug class of anti-epileptics?

<p>Phenytoin (B), Valproic acid (D)</p> Signup and view all the answers

What is a common characteristic of substrates in the context of drug interactions?

<p>They are metabolized by the enzyme. (B)</p> Signup and view all the answers

Which drug is shown to be a substrate for cytochrome P450 3A4?

<p>Ketamine (B)</p> Signup and view all the answers

What is the main function of drug activators in metabolism?

<p>They increase the enzyme's metabolic capabilities. (C)</p> Signup and view all the answers

Which P450 isoform is involved in metabolizing antidepressants such as fluoxetine?

<p>2D6 (B)</p> Signup and view all the answers

Which of the following drugs would be considered an inhibitor for cytochrome P450 2C8?

<p>Amodiaquine (C)</p> Signup and view all the answers

Which drug is explicitly listed as a substrate for the P450 1A2 isoform?

<p>Caffeine (B)</p> Signup and view all the answers

What would be the likely outcome if a drug that inhibits P450 2C9 is taken alongside a 2C9 substrate?

<p>Reduced metabolism of the substrate drug. (D)</p> Signup and view all the answers

Flashcards

What are substrates?

Drugs that are broken down by a specific cytochrome P450 enzyme.

What are inhibitors?

Drugs that block or prevent a cytochrome P450 enzyme from breaking down other drugs.

What are activators?

Drugs that increase the activity of a cytochrome P450 enzyme, making it break down other drugs faster.

What is the Flockhart Tableâ„¢?

The Flockhart Tableâ„¢ is a reference tool that lists drugs based on their interaction with specific cytochrome P450 enzymes.

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What are CYP enzymes?

Cytochrome P450 (CYP) enzymes are a group of proteins found in the liver that play a crucial role in metabolizing drugs. They are also involved in breaking down many other substances in the body.

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Which CYP enzyme is most important for drug interactions?

CYP3A4 is a major cytochrome P450 enzyme responsible for metabolizing a wide variety of drugs, accounting for up to 50% of drug metabolism.

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Why is understanding CYP enzymes important for prescribers?

Knowing which CYP enzyme is primarily involved in a drug's metabolism allows prescribers to anticipate potential drug interactions.

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What happens when two drugs inhibit the same CYP enzyme?

Drugs that inhibit the same CYP enzyme can compete for metabolism, leading to higher levels of one or both drugs in the body. This could result in increased side effects or toxicity.

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What happens when two drugs activate the same CYP enzyme?

Drugs that activate the same CYP enzyme can accelerate the metabolism of other drugs, leading to lower levels of those drugs in the body. This could result in decreased effectiveness.

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How can the Flockhart Tableâ„¢ help predict drug interactions?

The Flockhart Tableâ„¢ provides lists of inhibitors and activators for each CYP enzyme, allowing prescribers to identify potential drug interactions based on a drug's known CYP substrate.

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Which drug classes are frequently impacted by CYP interactions?

Antidepressants, antipsychotics, anti-epileptics, and beta blockers are drug classes often involved in significant drug interactions.

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Why is CYP3A4 so important when considering drug interactions?

Drugs metabolized by CYP3A4 represent a significant portion of commonly prescribed medications, making it crucial to understand potential interactions involving this enzyme.

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What is the overall significance of the Flockhart Tableâ„¢?

The Flockhart Tableâ„¢ provides crucial information for prescribers to enhance the safety and effectiveness of drug therapy.

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Why is understanding drug interactions crucial?

Drug interactions can significantly impact the effectiveness and safety of medications. Understanding how drugs are metabolized by CYP enzymes is crucial for preventing adverse outcomes.

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How can pharmacokinetic knowledge be used to improve patient care?

By using the Flockhart Tableâ„¢ and considering the CYP enzymes involved in a drug's metabolism, prescribers can make informed decisions to minimize potential drug interactions and optimize patient care.

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Cytochrome P450 (CYP) Enzymes

A group of enzymes responsible for metabolizing a variety of drugs and other substances in the liver.

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CYP3A4

A specific enzyme belonging to the Cytochrome P450 family, involved in the metabolism of various drugs.

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Drug-Drug Interaction (DDI)

The phenomenon where one drug affects the metabolism of another drug.

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Inducer

A drug that can increase the activity of another drug, leading to higher levels in the body.

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Inhibitor

A drug that can decrease the activity of another drug, leading to lower levels in the body.

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CYP3A4 Substrate

A drug that is metabolized by the CYP3A4 enzyme.

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Flockhart Table

A list of drugs that are known to be metabolized by specific CYP enzymes.

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Pharmacokinetics

The study of how drugs are absorbed, distributed, metabolized, and excreted.

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Metabolism

The process by which drugs are broken down into smaller molecules.

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Excretion

The process by which drugs are removed from the body.

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CYP2D6

An enzyme that plays a role in the metabolism of many medications, including anti-depressants, anti-psychotics, and some anti-rejection drugs.

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Induction

A type of drug interaction where one drug increases the activity of another.

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Enhanced Effect

When a drug's activity is increased due to its interaction with another drug.

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Reduced Effectiveness

When a drug's activity is decreased due to its interaction with another drug.

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Adverse Drug Reaction (ADR)

A type of drug interaction where a dangerous or unexpected reaction occurs.

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What is St. John's Wort?

St. John's Wort is a natural herbal remedy that can interact with various drugs, potentially altering their effectiveness or increasing side effects.

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What is Rifampin?

Rifampin is a strong antibiotic that can interact with numerous drugs, significantly impacting their effectiveness and potentially leading to adverse reactions.

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What is Phenytoin?

Phenytoin is an anticonvulsant drug that can interact with other medications, potentially causing dangerous side effects.

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What is Omeprazole?

Omeprazole is a medication used to treat heartburn and acid reflux. It can interact with other drugs affecting their absorption or effectiveness.

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How does Tobacco use affect medications?

Tobacco use can interact with numerous medications, potentially altering their effectiveness and causing severe side effects.

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CYP enzyme

An enzyme that plays a role in the metabolism of many drugs.

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CYP substrate

A drug that is broken down (metabolized) by a CYP enzyme.

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CYP inhibitor

A drug that blocks the activity of a CYP enzyme, preventing it from metabolizing other drugs.

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AUC (Area under the Curve)

The amount of a drug in the blood over time.

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Strong CYP inhibitor

A strong CYP inhibitor causes a more than 5-fold increase in the AUC of a substrate drug.

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Moderate CYP inhibitor

A moderate CYP inhibitor causes a 2 to 5-fold increase in the AUC of a substrate drug.

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Weak CYP inhibitor

A weak CYP inhibitor causes a 1.25 to 2-fold increase in the AUC of a substrate drug.

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Clearance

The rate at which a drug is removed from the body.

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Enzyme Inducer

Drugs that increase the activity of a specific enzyme, leading to faster breakdown of other medications.

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Rifampin

An enzyme inducer that can increase the metabolism of drugs like warfarin and theophylline.

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Carbamazepine

A potent enzyme inducer used to treat epilepsy and bipolar disorder. It can affect the effectiveness of several drugs.

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Efavirenz

This anti-HIV drug can induce the metabolism of other drugs.

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Dexamethasone

An anti-inflammatory drug that can induce the breakdown of other drugs.

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Decreased Drug Levels

Enzyme induction can lead to this: drugs are eliminated from the body faster, potentially reducing their effectiveness.

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Drug Interactions

Enzyme inducers can affect drug levels and effectiveness. This is important to consider when prescribing drugs and monitoring their effectiveness.

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Study Notes

Flockhart Table

  • The Flockhart Table is a tool for understanding drug interactions.
  • It's helpful in clinical prescribing when knowing how drugs are metabolized is crucial.
  • The table categorizes drugs by their cytochrome P450 isoform.
  • A drug can function as a substrate (metabolized by the enzyme), inhibitor (prevents enzyme activity), or activator (increases enzyme activity).
  • Recognizing these roles helps predict potential interactions between medications.

P450 Drug Interaction Table

  • This table details various drug interactions based on the particular cytochrome P450 enzyme (e.g., 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4,5,7).

  • The table shows which drugs act as substrates, inhibitors, or activators for particular enzymes.

  • This information helps anticipate potential drug interactions based on how each medication metabolizes.

  • The table contains specific examples of drugs grouped by the enzyme they affect.

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