Food and Drug Disposition

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Questions and Answers

What are the three main things that food can affect in the body in relation to drugs?

Drug absorption, metabolism, distribution, and excretion.

Which of these options are correct? (Select all that apply)

Food-drugs interactions can:

  • Result in therapeutic failure. (correct)
  • Contribute to morbidity. (correct)
  • Adversely affect patient care. (correct)
  • Reduce or increase the effect of the drug. (correct)
  • Prolong treatment time or hospitalization. (correct)
  • Increase toxicity. (correct)

Food affects drug absorption, metabolism, distribution, and excretion.

True (A)

Drugs can affect food absorption, metabolism, distribution, and excretion.

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

Drug's side effects can impact food intake and nutrient absorption.

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

What can occur when drugs are combined with certain types of food?

<p>Unhealthy effects.</p> Signup and view all the answers

Do food-drug interactions mainly occur with pharmacokinetics or pharmacodynamics?

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

Most food-drug interactions occur at the stage of absorption and then metabolism.

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

There are very few food-drug interactions with pharmacodynamics.

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

Where do most food-drug interactions with pharmacodynamics occur?

<p>Competing sites, such as transport and receptor bindings.</p> Signup and view all the answers

What can happen when someone consumes excessive potassium while taking ACE inhibitors?

<p>Hyperkalaemia.</p> Signup and view all the answers

A fatty meal can increase the absorption of Acitretin.

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

Alendronic acid is best absorbed with food or milk.

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

A fatty meal increases the solubility of Albendazole.

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

Ampicillin is best absorbed without food.

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

Atovaquone is best absorbed with a fatty meal.

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

Azithromycin capsules should be taken with food.

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

Captopril has no dietary restrictions.

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

A consistent meal routine helps maintain a steady level of Carbamazepine in the body.

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

Food can affect both the rate and extent of drug absorption.

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

What are the five categories of drug-food interactions that are related to absorption?

<p>Reduced (extent), delayed (rate), increased (extent), accelerated (rate), and no effect.</p> Signup and view all the answers

Delayed absorption of a drug is usually due to a slower gastric emptying rate and/or increased gastric pH.

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

Delayed absorption usually results in a decreased Cmax and a shorter Tmax.

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

Delayed absorption will always affect overall all extent of absorption (AUC).

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

Decreased absorption refers to an increase in the extent of gastrointestinal medicine absorption.

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

Diabetes mellitus and inflammatory bowel diseases can affect drug bioavailability.

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

In certain cases, patients with diabetes mellitus may experience delayed gastric emptying due to autonomic neuropathy.

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

Aspirin is best taken 2 hours after meals with a full glass of water.

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

Food slows down the absorption of Isoniazid.

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

Isoniazid should be taken 1 hour before or 2 hours after meals.

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

Increased intestinal drug uptake results from delayed gastric emptying and increased secretion of bile salts.

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

Accelerated drug uptake is caused by the up-regulation of carrier-mediated transport systems in response to high-protein meals.

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

Fatty foods and low-fiber foods speed up stomach emptying.

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

Griseofulvin and oltipraz show increased absorption and bioavailability after a high-fat meal.

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

Ascorbic acid inhibits iron absorption.

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

Carbonated drinks and acid juices slow down drug dissolution in the stomach.

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

Tetracyclines are best absorbed with food containing calcium, magnesium, or aluminium.

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

The physical and chemical characteristics of a drug can influence its absorption.

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

Fluconazole and itraconazole belong to different chemical classes.

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

Itraconazole displays increased absorption in the presence of food.

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

Meals can influence the chiral inversion of ibuprofen.

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

The size of the meal does not affect drug absorption.

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

High-fat content in meals can increase bioavailability of lipophilic drugs.

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

A high fiber content enhances the bioavailability of certain medications.

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

Grapefruit juice can increase the Cmax of felodipine.

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

Calcium in milk and milk products increase absorption of certain antibiotics.

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

Orange juice can enhance iron absorption.

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

Taking medications with soda or high acid fruit juice can potentially cause excess stomach acidity.

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

Fatty foods can decrease the absorption of griseofulvin.

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

Dietary components significantly influence certain medications' metabolism.

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

Malnutrition contributes to altered hepatic metabolism.

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

Grapefruit juice inhibits the activity of CYP3A4 enzymes, affecting the metabolism of many medications.

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

Garlic inhibits the activity of CYP2C19 enzymes.

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

Broccoli induces the activity of CYP2C9 enzymes.

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

Piperine present in black pepper enhances the bioavailability of certain drugs.

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

Piperine inhibits the activity of hepatic and intestinal aryl hydrocarbon hydroxylase and UDP-glucuronyl transferase.

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

Piperine's effect on the ultrastructure of intestinal brush border decreases drug absorption.

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

Piperine has been shown to decrease the oral bioavailability of phenytoin in normal and epileptic patients.

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

Dietary changes can significantly alter drug excretion.

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

Changes in urine pH caused by food can significantly affect drug excretion rates.

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

A drug in unionized state can diffuse more easily out of the urine back into the blood.

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

Antacids can increase the excretion rate of acidic drugs.

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

Warfarin's effect can be directly antagonized by ingesting foods rich in vitamin K.

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

Avocado intake has been reported to cause warfarin antagonism.

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

Potassium-rich foods like bananas and spinach can potentially lead to hyperkalaemia when taken with diuretic drugs.

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

Certain food components compete with levodopa for transporters.

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

Corticosteroids can increase appetite.

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

Antidepressants often increase appetite.

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

Laxatives can cause nutrient loss.

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

Antacids are known to increase nutrient absorption.

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

Cancer drugs often cause nausea and vomiting.

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

Amoxicillin is a common antibiotic that can cause diarrhoea.

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

Reduced gastric emptying often leads to a decreased Tmax.

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

Increased blood flow to the GI tract can lead to increased AUC and Cmax for some drugs.

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

Increased gastric pH can create an environment that favors the absorption of acidic drugs.

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

Food ingredients can alter solubility of drugs, particularly lipophilic drugs.

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

Inhibition of GI enzymes or transporter activity can lead to decreased drug metabolism and uptake.

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

Inhibition of GI enzymes or transporter activity can result in lower AUC and Cmax for some drugs.

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

Flashcards

Food-drug interactions

Effects of food on drug absorption, metabolism, distribution, and excretion, or vice versa. These interactions can alter drug effectiveness, increase toxicity, or negatively impact patient care.

Pharmacokinetic interactions

Interactions primarily affecting how the body absorbs, distributes, metabolizes, and eliminates drugs.

Pharmacodynamic interactions

Interactions primarily affecting how drugs affect the body's systems and functions.

Absorption interactions (reduced)

Taking food reduces drug absorption rate, a slower gastric emptying rate, and/or increased gastric pH resulting from consuming food.

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Absorption interactions (delayed)

Food ingestion slows down the time it takes for medicine to be absorbed.

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Absorption interactions (increased)

Food can sometimes lead to increased intestinal absorption of drugs, possibly because of factors like higher fat content, higher bile secretion, or increased transport activity.

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Cmax

Maximum drug concentration in blood.

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tmax

Time taken to reach maximum drug concentration in blood.

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AUC

Area Under the Curve, representing the total drug exposure.

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Bioavailability

The percentage of administered drug that reaches the systemic circulation in an active form.

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Gastric emptying

Rate at which stomach contents are moved into the small intestine

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CYP450 enzymes

Liver enzymes that metabolize many drugs.

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Grapefruit juice

A food that can significantly alter the metabolism of some drugs.

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Vitamin K-rich foods

Foods like certain leafy green vegetables that can affect the blood-thinning effects of warfarin.

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Cytochrome P450 enzyme inhibitors

Substances that reduce the activity of cytochrome P450 enzymes

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Cytochrome P450 enzyme inducers

Substances that increase the activity of cytochrome P450 enzymes

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Piperine

A compound found in black pepper that can affect drug absorption

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Food-induced malabsorption

Certain foods can slow down the absorption of some drugs into the body

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Study Notes

Food and Drug Disposition

  • This lecture covers the effects of nutrition on drug pharmacokinetics and pharmacodynamics, as well as the effect of drugs on food.
  • Food-drug interactions can reduce or increase the effect of a drug, leading to therapeutic failure, increased toxicity, and adverse effects on patient care.
  • These interactions can also prolong treatment time or hospitalisation.
  • Food impacts drug absorption, metabolism, distribution, and excretion.
  • Drugs can also impact food absorption, metabolism, distribution, and excretion, as well as affect food intake and nutrient absorption.
  • Food-drug interactions can occur at the level of pharmacokinetics (majority of interactions) and pharmacodynamics (few interactions).
  • Pharmacokinetic interactions often occur during absorption or metabolism.
  • Pharmacodynamic interactions mostly occur at competing sites.
  • Several specific examples of drugs and how they interact with food are provided. Relevant dietary recommendations are included in the summary tables for different drug classes

Objectives

  • Students will be able to describe the impact of nutrition on drug pharmacokinetics.
  • Students will be able to describe the impact of nutrition on drug pharmacodynamics.
  • Students will be able to describe the effect of drugs on food pharmacokinetics.

Food-drug Interactions

  • Food can affect absorption (rate and extent) of drugs.
  • Absorption interactions are classified as: reduced extent, delayed rate, increased extent, accelerated rate, and no effect.
  • Delayed absorption typically results from slower gastric emptying or increased gastric pH from food ingestion, leading to reduced Cmax and prolonged tmax, but not impacting overall AUC.
  • Decreased absorption can be due to disease states (e.g. diabetes, inflammatory bowel disease) affecting drug bioavailability.
  • Increased/accelerated absorption, associated with delayed gastric emptying, increased secretion of bile salts, or upregulation of carrier systems (particularly with high-protein meals), leads to increased drug dissolution rates.
  • Certain foods reduce drug absorption rates and increase others.

Effects of Food on Drug Absorption

  • Food can influence the rate and extent of drug absorption from the gastrointestinal tract.
  • Examples of foods that reduce drug absorption include food with aspirin (take 2 hours after meals with a full glass of water) and isoniazid (consume 1 hour before or 2 hours after a meal.)
  • Certain foods increase drug absorption, e.g., fatty foods increasing absorption of griseofulvin.

Factors Affecting Drug Absorption

  • Drug characteristics (e.g., pKa, solubility, and formulation).

  • Meal characteristics (size and composition, high-fat content, fiber content).

  • Timing of drug and meal intake.

  • Grapefruit juice can increase the drug concentration (Cmax) of certain drugs by up to 99%.

  • Calcium found in dairy products reduces the absorption of certain antibiotics such as Tetracycline.

  • Ascorbic acid (e.g., found in orange juice) enhances iron absorption.

  • Drugs should not be taken with sodas or high-acid fruits due to potential disruption of drug absorption (stomach acidity dissolving drugs).

Effects of Food on Drug Metabolism

  • Various dietary compounds affect drug metabolism.

  • Cruciferous vegetables, charcoal-broiled beef, and certain proteins are examples of substances impacting metabolism.

  • Malnutrition can alter hepatic metabolism and reduce elimination of conjugates.

  • Cytochrome P450 enzymes play a central role in drug metabolism.

  • Garlic can inhibit CYP2C19, leading to potentially increased levels of omeprazole and diazepam.

  • Broccoli can induce CYP2C9, affecting drugs like warfarin and tolbutamide.

  • Black pepper (piperine) can enhance the bioavailability of several drugs by inhibiting hepatic and intestinal enzymes.

Food Effects on Drug Excretion

  • Urine pH changes due to food can influence excretion of acid and bases.
  • Unionised drugs are more readily reabsorbed from urine into the blood, prolonging drug action.
  • Acidic urine enhances the effect of acidic drugs.
  • Antacids alter urine pH, affecting drug excretion.

Pharmacodynamic Interactions

  • Food can directly antagonise (for example, vitamin K-rich food can counteract warfarin).
  • Potassium-rich foods can increase potassium in blood when taken with diuretics (e.g. hyperkalemia).
  • Some food components compete with drugs (e.g., levodopa) for specific transporters.

Effects of Drugs on Food

  • Drugs can impact appetite (corticosteroids or antidepressants).
  • Drugs can change nutrient absorption, metabolism or excretion (laxatives, antacids).
  • Drugs can cause side effects like nausea/vomiting or diarrhea.

Summary Examples

  • Several examples summarized how food can alter drug PK and PD effects, with emphasis on absorption, metabolism, and excretion.

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