Pharmacokinetics: Absorption, Distribution, Metabolism

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Questions and Answers

A medication administered via the sublingual route has a high bioavailability because it:

  • Undergoes extensive metabolism in the highly acidic environment of the stomach.
  • Is rapidly absorbed in the large intestine due to its extensive surface area.
  • Bypasses the liver, avoiding first-pass metabolism. (correct)
  • Has a low affinity for plasma proteins, resulting in a higher concentration of free drug.

A drug that is highly water-soluble will readily distribute into adipose tissue.

False (B)

What is bioavailability?

Bioavailability refers to the fraction of an administered dose of drug that reaches the systemic circulation unchanged.

The first pass effect, which reduces bioavailability, primarily occurs in the ______.

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

If a patient with low albumin levels is given a highly protein-bound drug, what is the likely effect?

<p>Increased risk of drug toxicity due to a higher concentration of free drug. (D)</p> Signup and view all the answers

During which phase of clinical trials are controlled studies used to treat disease in a small number of patients, establishing the potential of the drug to improve patient outcomes and short-term risks.

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

Crushing an enteric-coated tablet is an acceptable way to speed up drug absorption in the stomach.

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

Match the clinical trial stages with their primary focus:

<p>Preclinical = Animal testing and identification of promising drugs Phase 1 = Establish biological effects, safe dosages, and pharmacokinetics in healthy volunteers Phase 2 = Controlled studies to treat disease in a small number of patients</p> Signup and view all the answers

In Phase 3 clinical trials, a new medication is primarily compared to what?

<p>Standard therapy to evaluate risk vs. benefit (A)</p> Signup and view all the answers

Generic drugs always have the exact same inactive ingredients as their brand-name counterparts.

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

What is the term for the expression of how much drug is needed to produce a biological response?

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

________ are drugs that occupy receptors without stimulating them, preventing other molecules from producing a response.

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

Abrupt withdrawal of some antagonist drugs can lead to rebound effects due to which receptor process?

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

What does the acronym 'ICanPresCribE A Drug' stand for in the context of prescribing?

<p>Indication, Contraindications, Precautions, Cost/Compliance, Efficacy, Adverse effects, Dose/Duration/Direction (A)</p> Signup and view all the answers

According to the WHO prescribing model, what is the first step a practitioner should take?

<p>Define the patient's problem (D)</p> Signup and view all the answers

Match the following FDA responsibilities with their descriptions:

<p>Standardization of nomenclature = Creating uniform and consistent drug naming conventions Approval of new indications = Reviewing and approving new uses for existing medications Surveillance of adverse drug events = Monitoring and tracking negative effects associated with medications Regulation of medical devices = Ensuring the safety and effectiveness of various medical devices</p> Signup and view all the answers

Flashcards

Absorption

Process of drug uptake from the site of administration into the bloodstream.

Biological Availability

The proportion of a drug that enters circulation when introduced and is available for action.

First Pass Metabolism

Initial metabolism of a drug in the liver before it reaches systemic circulation.

Distribution

The dispersion of absorbed drugs throughout body fluids to target tissues.

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Protein Binding

The reversible attachment of drugs to plasma proteins, affecting their availability.

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Tissue Distribution

Movement of drugs into different tissues, affected by lipid solubility and blood flow.

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Phase 1 Trials

Initial phase of clinical trials focused on biological effects and safety in a small group of healthy subjects.

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Phase 2 Trials

Clinical trials that assess the efficacy and short-term risks of a drug with a small patient population.

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Phase 3 Clinical Trials

Comparative trials assessing new drugs against standard therapies for risk vs benefit.

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Drug Response Curve

Graph showing the relationship between drug concentration and biological response.

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Graded Responses

Measurable drug effects (e.g., blood pressure, heart rate).

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Quantal Responses

Binary drug effects that may or may not occur (e.g., rash, seizure).

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Potency

Amount of drug needed to produce a biological response; more potent drugs need lower doses.

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Therapeutic Index

Ratio comparing the lethal dose and therapeutic dose of a drug.

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Antagonists

Drugs that block receptors without stimulating them, preventing responses from agonists.

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FDA Role

Regulates drug approval, labeling, and monitors adverse effects and uses of drugs.

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Study Notes

Absorption

  • Oral administration: First pass through the liver
  • Small intestine: Less acidic environment, higher bioavailability than stomach
  • Sublingual: Bypasses the liver, high bioavailability
  • Bioavailability: The usable amount of a drug

Distribution

  • Movement of absorbed drug throughout the body to target tissues
  • Adequate blood supply is needed
  • Drugs distributed to areas with high blood flow first
  • Properties affecting distribution include water or lipid solubility, molecular size, acid vs. base environment, and protein binding

Metabolism

  • Phase 1: Non-synthetic reactions
  • Phase 2: Synthetic or conjugation reactions
  • Cytochrome P450: Organized into numbered families
  • CYP1, CYP2, CYP3
  • Metabolism and half-life affected by age, pregnancy, liver disease, time of day, environment, diet, alcohol, drug interactions

Excretion

  • Removal of drugs from the body by the kidneys, lungs, gastrointestinal tract, sweat, and saliva
  • Enterohepatic cycling: Drug is excreted in the bile, reabsorbed from intestines, and then excreted again in the bile
  • Renal processes: Passive glomerular filtration, active tubular secretion, tubular reabsorption

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