Pharmacokinetics L1

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Questions and Answers

What is Pharmacokinetics?

It is the study of what your body does to the drug

What does your body do to the drug?

It absorbs, distributes, metabolizes and excretes the drug.

In the ADME principle, which step involves the movement of a drug from the site of administration into the bloodstream?

  • Absorption (correct)
  • Distribution
  • Metabolism
  • Excretion

In the ADME principle, which step involves the movement of the drug from the bloodstream into tissues and organs?

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

In the ADME principle, which step involves the conversion of a drug into a different chemical form?

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

In the ADME principle, which step refers to the process of removing a drug or its metabolites from the body?

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

Which of the following correctly identifies the two broad categories of factors that influence pharmacokinetics?

<p>Patient factors and drug factors (C)</p> Signup and view all the answers

List the specific patient factors that influence pharmacokinetics?

<p>Membrane, cell, tissue barriers and pH environment</p> Signup and view all the answers

List the specific drug factors that influence pharmacokinetics

<p>Molecular size, solubility, ionization, chemical reaction</p> Signup and view all the answers

Drug movement depends on ________ (I.e. solubility, ionization, molecular size) and ______ (membranes, transporters, tissue specific barriers like the BBB)

<p>Chemical properties; biological barriers</p> Signup and view all the answers

Which of the following best describes a key determinant of drug movement across a biological membrane?

<p>The drug’s lipophilicity and presence of transporters (C)</p> Signup and view all the answers

Which of the following drug characteristics would MOST likely facilitate passive diffusion across a lipid bilayer?

<p>Lipophilicity and non-ionized state (D)</p> Signup and view all the answers

Which of the following best describes the role of ATP-binding cassette sub-family B member (ABCB) transporters, such as P-glycoproteins, in pharmacokinetics?

<p>They actively transport drugs out of cells, often contributing to drug resistance. (B)</p> Signup and view all the answers

In active transport, carrier proteins aren’t required.

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

How do metabolic inhibitors affect active transport mechanisms in drug movement?

<p>They reduce ATP production, preventing energy-dependent drug transport. (B)</p> Signup and view all the answers

How do hydrophilic and lipophilic media within cells influence drug pharmacokinetics?

<p>Lipophilic drugs easily diffuse through lipid membranes, while hydrophilic drugs may require transport mechanisms. (A)</p> Signup and view all the answers

Tissues that are more protected make it harder for a drug to move within the body. List examples of these tissues

<p>Blood brain barrier, eye, testicles, placental, mammary gland, prostate, synovial fluids</p> Signup and view all the answers

Match the correcting term to it’s function/description

<p>Chelation = Binding to metal ions Tautomerization = Conversion between isomers Conjugation = Combination with endogenous substance Photodegredation = Degradation by absorption of photons</p> Signup and view all the answers

Which of the following statements is TRUE regarding the order of drug processes?

<p>First-order kinetics occurs when the rate of drug movement depends on both a constant and drug concentration (B)</p> Signup and view all the answers

Which of the following best describes the two components that determine the rate of drug movement?

<p>A constant reflecting the rate of process and the amount of drug available (B)</p> Signup and view all the answers

What is a defining characteristic of zero-order kinetics in drug movement?

<p>The drug elimination rate increases proportionally with concentration. (B)</p> Signup and view all the answers

What happens when drug transporters become saturated?

<p>Drug elimination or absorption plateaus, leading to zero-order kinetics. (C)</p> Signup and view all the answers

What does the ionization of a drug depend on?

<p>The drug’s pKa and the pH of the surrounding environment (C)</p> Signup and view all the answers

When does a weak acid or weak base become "trapped" in a compartment?

<p>When the drug is in an environment where it remains in its ionized form (B)</p> Signup and view all the answers

When does ion trapping occur?

<p>It occurs when a drug becomes ionized in a specific pH environment, thus making it unable to cross biological membranes</p> Signup and view all the answers

Membranes are more permeable to ionized forms of drugs than nonionized

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

What happens when the pKa of a drug equals the pH of the surrounding medium?

<p>The drug exists in an equilibrium where it is 50% ionized and 50% non-ionized. (C)</p> Signup and view all the answers

Flashcards

Pharmacokinetics

The study of how the body affects a drug.

Absorption

The process by which a drug moves from the site of administration into the bloodstream.

Distribution

The process by which a drug moves from the bloodstream into tissues and organs.

Metabolism

The process by which a drug is converted into a different chemical form, often to make it easier for the body to eliminate.

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Excretion

The process of removing a drug or its metabolites from the body.

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Patient Factors

Factors related to the patient's body, such as their age, weight, and health conditions.

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Drug Factors

Factors related to the drug itself, such as its chemical properties, dosage form, and route of administration.

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Patient Factors (Specific)

These factors include the body's membranes, cells, tissue barriers, and the pH environment of different body compartments.

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Drug Factors (Specific)

These factors include the drug's molecular size, solubility, ionization, and chemical reactivity.

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Drug Transport Across Membranes

Drugs move across membranes by two main mechanisms: passive transport (diffusion) and active transport (carrier-mediated).

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Drug Solubility

The ability of a drug to dissolve in water or lipids determines how easily it crosses membranes.

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Drug Ionization

Ionization is the process of a drug gaining or losing a charge. Charged drugs have difficulty crossing membranes.

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Blood-Brain Barrier (BBB)

The blood-brain barrier (BBB) protects the brain from harmful substances. Only drugs with specific properties can cross it.

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Drug Chemical Transformations

Chemical reactions that drugs undergo in the body, altering their structure and affecting their activity, stability, absorption, metabolism, and elimination.

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Study Notes

Drug Movement Mechanisms

  • Drug movement relies on chemical properties (solubility, ionization, size) and biological barriers (membranes, transporters, blood-brain barrier).
  • Key mechanisms include passive transport (diffusion) and active transport (carrier-mediated).

Drug Transformations

  • Drugs undergo various chemical transformations:
    • Chelation (binding to metal ions)
    • Hydrolysis (water-mediated splitting)
    • Oxidation (electron transfer)
    • Tautomerization (isomer conversion)
    • Photodegradation (light-induced breakdown)
    • Conjugation (attachment to endogenous molecules)
  • These transformations affect drug stability, absorption, metabolism, and elimination.

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