Pharmacology: Drug Absorption and Distribution

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Questions and Answers

Which factor has the greatest impact on the rate of drug absorption when comparing different administration routes?

  • The solubility of the drug
  • The thickness of tissue
  • The blood supply at the site of administration (correct)
  • The formulation of the drug

How does a drug's solubility affect its absorption?

  • Higher solubility allows it to cross the plasma membrane easily. (correct)
  • Lower solubility results in a faster absorption.
  • Solubility has no effect on absorption.
  • Drugs must be solid to be absorbed.

What is the primary benefit of intravascular drug administration?

  • It is always less expensive than oral administration.
  • It requires less precise dosing.
  • It provides a longer duration of action.
  • It bypasses absorption barriers. (correct)

Which of the following descriptions best explains why absorption is faster through the small intestine compared to the skin?

<p>There is only a single layer of epithelial cells in the small intestine. (D)</p> Signup and view all the answers

Which condition could potentially slow down the absorption rate of a drug in a subcutaneous injection?

<p>Presence of cardiovascular disease (D)</p> Signup and view all the answers

Which type of drugs can pass through the plasma membrane via simple diffusion?

<p>Lipid-soluble drugs (D)</p> Signup and view all the answers

What primarily affects the pharmacological action of a drug after entering systemic circulation?

<p>The proportion of unbound drug in circulation (D)</p> Signup and view all the answers

Which barrier provides protection to the CNS from harmful substances?

<p>Blood-brain barrier (A)</p> Signup and view all the answers

What factor does NOT affect the distribution of a drug within the body?

<p>Age of the patient (B)</p> Signup and view all the answers

Which of the following describes how water-soluble drugs typically cross plasma membranes?

<p>Through facilitated diffusion or active transport (B)</p> Signup and view all the answers

What type of tissues are drugs likely to distribute to more slowly?

<p>Poorly perfused tissues like adipose tissue (D)</p> Signup and view all the answers

What factor can limit drug distribution across the placental barrier?

<p>Molecular weight of the drug (C)</p> Signup and view all the answers

The permeability of which type of tissue barriers can significantly influence drug absorption?

<p>Brain tissue barriers (B)</p> Signup and view all the answers

What is primarily responsible for the irreversible loss of a drug from the plasma?

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

Which of the following factors can influence the process of renal excretion of drugs?

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

Which route is primarily used by the body for the excretion of volatile substances?

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

What percentage of the original drug dose ultimately reaches systemic circulation after absorption and metabolism?

<p>20% (D)</p> Signup and view all the answers

Which factor does NOT play a role in the reabsorption of lipid-soluble drugs in the kidneys?

<p>Drug volume in plasma (D)</p> Signup and view all the answers

What term describes the range of drug concentration offering therapeutic effects while minimizing toxicity?

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

Which of the following is a primary site for drug excretion from the body?

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

How does the solubility of a drug primarily affect its absorption?

<p>Lipid soluble drugs are absorbed more rapidly than water-soluble drugs. (A)</p> Signup and view all the answers

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Study Notes

Drug Absorption

  • Drugs are absorbed from the site of administration into the bloodstream.
  • The rate of absorption depends on various factors, including:
    • Drug solubility (lipid-soluble drugs are absorbed faster)
    • Route of administration – oral vs. intravenous
    • Tissue surface area and thickness
    • Blood supply at the site of administration
  • Example:
    • A patient takes a 100mg dose of a drug
    • 80 mg of the dose is absorbed from the small intestine and reaches the liver via the hepatic portal vein → 20 mg was not absorbed from the small intestine
    • The liver then metabolises the remaining 80 mg → 60 mg is irreversibly lost (eliminated)
    • Only 20 % of the original dose reaches the systemic circulation
    • The amount of drug that reaches systemic circulation is known as the BIOAVAILABILITY of the drug

Drug Distribution

  • The drug is distributed to various body compartments after reaching the systemic circulation.
  • Distribution depends on:
    • Drug solubility
    • Cardiovascular functioning
    • Perfusion of the area
    • Degree of blood flow
    • The permeability of the capillaries
    • pH of the area
    • Binding of drug to plasma proteins
  • Barriers to drug distribution:
    • Blood-brain barrier
    • Placental barrier
  • Intravascular administration:
    • Intravenous and intra-arterial routes bypass absorption
    • Drugs are immediately distributed around the body.
    • Medication (tablet) taken orally must disintegrate, dissolve, and be absorbed from the small intestine into the hepatic portal system before entering the systemic circulation.

Drug Elimination

  • The pharmacological effects of a drug continue until it is removed from the body.
  • Elimination is the irreversible loss of the drug from the plasma, which occurs through metabolism and excretion.
  • The liver is the primary site of elimination due to metabolism.
  • Excretion is the irreversible loss of the drug from the body:
    • Kidneys excrete most drugs and their metabolites
    • Drugs can be eliminated in bile and removed from the body in faeces
    • Lungs are the primary route for excretion of volatile substances like inhalation anaesthetics
    • Other routes include intestine, salivary, sweat and mammary glands

Renal Excretion

  • Kidneys are the main site of drug excretion from the body.
  • Free unbound drug can be filtered from the blood into the renal filtrate.
  • Lipid-soluble drugs may be reabsorbed from the renal filtrate back into systemic circulation.
  • Water-soluble drugs can also be secreted from the blood into the filtrate.
  • The process of excretion is dependent on:
    • Urinary pH
    • Renal function
    • Cardiovascular function

Pharmacokinetics - How the Body Affects the Drug

  • Pharmacokinetics describes how the body absorbs, distributes, metabolizes, and excretes drugs.
  • It is essential for understanding how a drug will act within the body and for determining the most appropriate dosage.

Rational Drug Use: Dosage Regime Development

  • The therapeutic range is the concentration of a drug that has a high probability of producing the desired therapeutic effect with a low probability of toxic effects.

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