Introduction to Pharmacology - Pharmacokinetics 1

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Questions and Answers

What is the name of the first step in the process of pharmacokinetics?

Absorption

What is the abbreviation for the four main processes of pharmacokinetics?

ADME

The higher the molecular weight (MW) of a drug, the greater its absorption.

False (B)

A non-ionized drug is typically more water-soluble than a lipid-soluble drug.

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

Which of the following is NOT a drug property that affects its absorption?

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

What is the name of the pH-dependent constant that represents the degree of ionization of a drug?

<p>pKa</p> Signup and view all the answers

Aspirin is a weak acid with a pKa of 3.5. This means that in the acidic environment of the stomach, it will be primarily non-ionized.

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

What is a potential consequence of aspirin's high absorption in the gastric mucosa?

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

Which of the following strategies is NOT typically used to prolong the action of a drug?

<p>Administering the drug as a suppository (B)</p> Signup and view all the answers

Which of the following is NOT a benefit of using long-acting drug formulations?

<p>Increased frequency of administration (C)</p> Signup and view all the answers

What is the term used to describe the movement of a drug from the site of administration into the bloodstream?

<p>Absorption</p> Signup and view all the answers

What is the name of the process by which the body breaks down drugs into inactive metabolites?

<p>Metabolism</p> Signup and view all the answers

What is the primary organ responsible for drug excretion?

<p>Kidney</p> Signup and view all the answers

What is the name of the study that examines the effects of drugs on the body?

<p>Pharmacodynamics</p> Signup and view all the answers

Match the following steps in pharmacokinetics with their descriptions:

<p>Absorption = The process by which a drug is eliminated from the body. Distribution = The movement of a drug from the bloodstream to various tissues and organs. Metabolism = The process by which a drug is broken down into inactive metabolites Excretion = The movement of a drug from the site of administration into the bloodstream.</p> Signup and view all the answers

What does the term 'vehicle' refer to in the context of drug formulation?

<p>The inactive ingredient that carries the active drug.</p> Signup and view all the answers

Aqueous creams are generally more absorbable than oily ointments.

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

Sustained-release formulations are designed to provide a rapid, short-acting effect.

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

Long-acting drug formulations can help improve patient compliance by reducing the frequency of administration.

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

Flashcards

Pharmacokinetics

The study of how drugs move through the body, including absorption, distribution, metabolism, and excretion.

Drug Absorption

The process of a drug moving from its administration site into the bloodstream.

Factors Affecting Drug Absorption

Factors that influence a drug's rate and extent of absorption, including drug properties, formulation, and patient characteristics.

Drug Properties

Characteristics of a drug that affect its absorption, such as molecular weight, lipophilicity, and solubility.

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Drug Formulation

The way a drug is prepared for administration, including its dosage form, excipients, and release mechanisms.

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Molecular Weight and Absorption

The molecular weight of a drug influences its absorption, with smaller molecules being absorbed more readily.

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Lipophilicity and Absorption

The ability of a drug to dissolve in fats or lipids, which affects its ability to cross cell membranes.

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Solubility and Absorption

The ability of a drug to dissolve in a solvent, especially water, which is important for absorption.

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Drug Ionization and Absorption

The degree to which a drug is ionized (charged) or non-ionized (uncharged), which affects its ability to cross cell membranes.

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pKa (Dissociation Constant)

The pH at which a drug is 50% ionized and 50% non-ionized, which is important for determining its absorption.

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Ionization of Acidic and Basic Drugs

Acidic drugs have a higher ionization in basic environments, while basic drugs have a higher ionization in acidic environments.

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Aspirin Trap

The pH difference between the acidic stomach and the basic intestine creates a 'trap' for acidic drugs like aspirin.

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Clinical Significance of pKa in Kidney

Modifying the pH of urine can affect drug excretion, either by increasing or decreasing the drug's ionization.

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Alkalinization of Urine

Alkalinizing urine helps excrete acidic drugs like aspirin.

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Acidification of Urine

Acidifying urine helps excrete basic drugs like amphetamines.

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Vehicle in Drug Formulation

The inactive ingredients that help formulate a drug, such as fillers, binders, and disintegrants.

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Tablet Formulation

A solid dosage form that disintegrates and dissolves in the body, releasing the active drug.

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Slow Release Tablets

Tablets that are designed to release the drug gradually over a longer period of time.

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Sustained Release Capsules (Spansules)

Capsules that contain granules or beads that slowly release the drug, providing a prolonged effect.

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Long Acting Drugs

Drugs designed to have a longer duration of action, often requiring less frequent administration.

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Lower Peak Levels with Long-Acting Drugs

The peak level of a drug in the body is lower with long-acting formulations due to their gradual release.

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Good Compliance with Long-Acting Drugs

Long-acting drugs promote better adherence to medication schedules.

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Reduced Adverse Effects with Long-Acting Drugs

By extending the duration of drug action, long-acting formulations can reduce the frequency of adverse effects.

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Prolonging Drug Action

Strategies to prolong the action of a drug, such as increasing its molecular weight, using an oily preparation, or employing sustained-release formulations.

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Vasoconstrictors in Local Anesthetics

Adding a vasoconstrictor to local anesthetics can slow their absorption and prolong their effect.

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Study Notes

Introduction to Pharmacology - Pharmacokinetic 1

  • Topics covered include pharmacology introduction, pharmacokinetics, drug absorption, factors affecting drug absorption, drug properties and drug formulation.
  • Pharmacokinetics is a quantitative study of drug movement within the body.
  • It encompasses absorption, distribution, metabolism, and excretion (ADME).
  • Pharmacodynamics deals with how a drug affects the body, while pharmacokinetics deals with how the body affects the drug.
  • Drugs move from the site of administration to the blood, then to the target site through different mechanisms.
  • The body may also process the drug, leading to secondary metabolites that can be beneficial or harmful.

Drug Properties Affecting Absorption

  • Molecular weight (MW): Lower molecular weight (MW) leads to increased absorption, higher MW leads to decreased absorption.
  • Example: procaine penicillin has a low MW so it's absorbed better.

Factors Affecting Drug Absorption

  • Drug factors: Drug properties (e.g., MW, solubility) and drug formulation (e.g., vehicle, formulation type).
  • Patient factors: These factors are not explicitly listed but could include, for example, physiological conditions, age, gender, etc

Drug Solubility

  • Non-ionized drugs are lipid-soluble and readily diffuse.
  • Ionized drugs are water-soluble and do not diffuse easily.
  • Ionization depends on the pH of the solution and the pKa of the drug.

pKa

  • pKa is the pH of the medium at which 50% of the drug is ionized and 50% is non-ionized.
  • Acidic drugs are better absorbed in the stomach (low pH), while basic drugs are better absorbed in the intestines (high pH).

Clinical Significance of pKa

  • Gastrointestinal Tract (GIT): Aspirin (weak acid, pKa 3.5) is non-ionized in the stomach, enabling it to cross cell membranes, get trapped in gastric mucosa cells, and potentially cause peptic ulceration.
  • Kidney: Drug ionization affects renal excretion. Altering urine pH (alkalinization or acidification) can change the ionization state of a drug, impacting its excretion.

Drug Formulation

  • Drugs are often combined with a vehicle.
  • Aqueous vehicles (like creams) are more easily absorbed than oily vehicles (like ointments).
  • Formulation types include tablets, capsules, and others. Preparation affects the drug's dissolution and absorption.

Slow Release/Sustained Release

  • Slow-release (sustained release/spansules) preparations minimize frequent administrations, lower peak drug concentrations, thus potentially reducing adverse effects and improving patient compliance.

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