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What type of antagonist affects a drug's efficacy by reducing it?
Which pharmacokinetic property describes the process of removing a drug from the body?
What must happen to drug concentration for drugs to maintain the same effect in the presence of an antagonist?
Which term describes what the drug does to the body?
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Agonists interact with receptors to:
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What is the significance of 'affinity' regarding drug-receptor interactions?
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Which type of drug binds and inactivates active targets?
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What types of changes do drug-receptor interactions typically cause?
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What type of chemical interactions allow for drug-receptor binding?
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Which describes drugs in the context of pharmacology?
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What is the primary function of P-glycoprotein in the context of drug transport?
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What is the primary purpose of the lock and key theory in drug-receptor binding?
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Which of the following is NOT a factor influencing the distribution of a drug from plasma to the interstitum?
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Which pharmacokinetic property is specifically responsible for the entry of a drug into circulation?
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Enteric-coated drugs primarily serve what purpose?
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What does bioavailability measure regarding a drug?
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Which route of drug administration has the highest bioavailability?
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First-pass metabolism primarily occurs in which organ?
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In which category of drug absorption is sublingual administration classified?
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Which of the following mechanisms of absorption involves the active transport of substances into cells?
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What distinguishes extended-release oral preparations from other forms?
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In the context of drug absorption, what is the role of blood flow?
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Which of the following routes provides rapid absorption while avoiding first-pass metabolism?
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Drugs with high first-pass metabolism require which of the following regarding dosing?
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Which area of high P-glycoprotein expression would limit drug absorption?
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What two barriers are primarily presented by the human body for drug absorption?
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Which drug administration route is characterized by its ability to provide rapid onset and maximum control?
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What role do cardiac output and local blood flow play in drug distribution?
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Which factor does NOT influence drug absorption?
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Which of the following statements about drug distribution is true?
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Study Notes
Pharmacology Basics
- Pharmacology studies drug-receptor interactions and the body's effects on drug movement, known as pharmacokinetics.
- Drugs interact with macromolecular receptors, leading to biochemical and physiological changes.
- Pharmacodynamics explores what drugs do to the body, while pharmacokinetics examines what the body does to drugs.
Drug-Receptor Interactions
- Antagonists: Inhibit target activation or inactivation.
- Competitive Antagonists: Bind to the same site as the agonist, reducing drug potency.
- Noncompetitive Antagonists: Bind to alternative sites, affecting drug efficacy.
- Inverse Agonists: Bind and deactivate active targets.
- Partial Agonists: Activate targets partially without full activation.
- Full Agonists: Fully activate their targets.
- Effects of drug binding lead to receptor conformational changes that enhance binding and modify activity.
Pharmacokinetics
- Absorption, Distribution, Metabolism, and Elimination (ADME) are the four key properties of pharmacokinetics affecting onset, intensity, and duration of drug action.
- Increased drug concentration may be necessary to achieve the same effects in the presence of antagonists.
- Bioavailability reflects the rate and extent to which a drug reaches systemic circulation, critical for dosages in non-intravenous administration.
- First-Pass Metabolism: Drug metabolism by the liver or GI tract before entering systemic circulation, influencing bioavailability.
- Drug absorption mechanisms include passive diffusion, facilitated diffusion, active transport, and endocytosis.
Factors Influencing Drug Absorption
- Obstacles: Integument and mucous membranes hinder drug absorption.
- Influencing factors: Blood flow, surface area, contact time, and P-glycoprotein expression impact absorption.
- P-glycoprotein, a transmembrane transporter, pumps drugs out of cells, limiting absorption in high-expressing areas.
Distribution
- After leaving the bloodstream, drugs enter interstitial spaces and tissues.
- Drug distribution is affected by cardiac output, local blood flow, capillary permeability, tissue volume, and the degree of drug binding to plasma and tissue proteins.
Routes of Drug Administration
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Enteral:
- Oral: Complex, affected by gastric pH; examples include enteric-coated (protect from stomach acid) and extended-release (slower absorption).
- Sublingual: Directly enters bloodstream, bypassing stomach acid.
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Parenteral: Direct systemic circulation; highest bioavailability, especially via intravenous administration.
- IV: Rapid effect and maximum control.
- IM: Variable absorption; e.g., epipens.
- SC: Slow absorption via diffusion; e.g., insulin.
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Other:
- Inhalation: Rapid absorption, avoids first-pass metabolism.
- Intrathecal/Intraventricular: Bypasses the blood-brain barrier directly into CSF.
- Transdermal: Varying absorption rates; e.g., nicotine patches.
- Rectal: Useful for patients who cannot take oral medications (vomiting).
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Description
Explore the essential concepts of pharmacology related to drug-receptor interactions, including the definitions and roles of antagonists, competitive antagonists, and noncompetitive antagonists. This quiz will test your understanding of how these interactions influence drug potency and efficacy.
