Pharmacology Basics Quiz

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Questions and Answers

What is one of the primary reasons for switching a patient's medication form?

  • To improve patient adherence and ease of use (correct)
  • To match the brand name with the generic name
  • To reduce the cost of the medication
  • To increase the dosing frequency

Which of the following statements is true about modified or extended-release drugs?

  • They should always be taken with food to improve absorption.
  • They can be crushed for easier administration.
  • They have a higher risk of causing adverse effects than immediate-release drugs.
  • They allow for a more constant drug level in the bloodstream. (correct)

What must be considered when assessing renal dosing for a drug?

  • The type of oral solution the patient prefers
  • The patient’s age only
  • The patient's body mass index (BMI)
  • The patient's creatinine clearance (CrCl) or estimated glomerular filtration rate (eGFR) (correct)

What is a key counseling point for patients using transdermal medications?

<p>The application site should be rotated to prevent irritation. (B)</p> Signup and view all the answers

What lab test result is most relevant for calculating a Child-Pugh score?

<p>Serum bilirubin level (C)</p> Signup and view all the answers

Which term defines the process of how a drug is absorbed, distributed, metabolized, and excreted in the body?

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

In the context of drug distribution, which factor is most likely to affect the distribution of a drug within the body?

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

What is the term used to describe a drug that becomes active only after metabolization?

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

Which concept describes the difference in therapeutic effect between two drugs that are chemically identical?

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

What process primarily occurs in the liver and alters drug structure?

<p>First pass metabolism (C)</p> Signup and view all the answers

Which of the following is a common factor affecting drug absorption?

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

In terms of pharmacokinetics, which parameter is best described as the time taken for the concentration of a drug in the blood to decrease by half?

<p>Half-life (B)</p> Signup and view all the answers

What is the primary factor that facilitates drug absorption in the gastrointestinal tract?

<p>Ionization of the drug (B)</p> Signup and view all the answers

Which of the following is NOT a factor that can affect drug elimination in the body?

<p>Patient's mood (B)</p> Signup and view all the answers

What is the primary concern when prescribing an extended-release medication to a patient?

<p>Potential for crushing or altering the dosage form (D)</p> Signup and view all the answers

Which of the following is NOT a characteristic of a 'do not crush' medication?

<p>The medication is designed to be palatable for patients (E)</p> Signup and view all the answers

A patient with a Child-Pugh score of 8 is being considered for a new medication. What is the appropriate clinical action?

<p>Avoid the use of the medication or consider alternatives. (F)</p> Signup and view all the answers

Which of the following is NOT a key counseling point for patients using transdermal medications?

<p>Apply the patch to a hairy area of skin (C), Dispose of used patches properly (F)</p> Signup and view all the answers

Which of these statements accurately describes the impact of the first-pass effect on drug bioavailability?

<p>The first-pass effect reduces drug bioavailability as the drug is metabolized before entering systemic circulation. (A)</p> Signup and view all the answers

What factor plays a significant role in determining the rate and extent of drug distribution throughout the body?

<p>The drug's affinity for specific protein binding sites. (D)</p> Signup and view all the answers

Consider a drug with a narrow therapeutic index. What is a key implication of this characteristic?

<p>A small change in dose can significantly alter the therapeutic effect, potentially leading to toxicity. (A)</p> Signup and view all the answers

Which of the following routes of administration is associated with the fastest onset of action?

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

Which of the following factors is most likely to increase the bioavailability of an orally administered drug?

<p>Rapid gastric emptying. (A)</p> Signup and view all the answers

What is the primary function of Phase II metabolism reactions?

<p>To convert the drug into a more polar and excretable form. (B)</p> Signup and view all the answers

Which of these statements accurately describes the concept of bioequivalence?

<p>Two drugs have the same rate and extent of drug absorption into the systemic circulation. (A)</p> Signup and view all the answers

What is the relationship between a drug's half-life and its steady-state concentration?

<p>Steady-state concentration is directly proportional to half-life, meaning a longer half-life results in a higher steady-state concentration. (B)</p> Signup and view all the answers

What is the primary reason the FDA allows generic drugs to differ from brand-name drugs?

<p>Generic drugs may have different inactive ingredients but must demonstrate bioequivalence. (C)</p> Signup and view all the answers

A patient with hepatic impairment and a Child-Pugh score of 10 needs a medication dosage adjustment. What general recommendation is most appropriate?

<p>Reduce the dose of the medication, as hepatic metabolism is significantly compromised. (C)</p> Signup and view all the answers

Which of the following is a typical pharmacokinetic change observed in geriatric patients that influences medication dosing?

<p>Reduced hepatic blood flow, leading to decreased drug metabolism. (C)</p> Signup and view all the answers

What process is least likely involved in drug elimination from the body?

<p>Drug deposition in adipose tissue (C)</p> Signup and view all the answers

A physician is considering prescribing a modified-release drug to a patient. What is a primary concern that should be considered?

<p>The rate of drug release may be inconsistent or unpredictable, resulting in fluctuations in drug levels. (B)</p> Signup and view all the answers

Which process best describes the movement of a drug from the bloodstream into tissue?

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

What primary effect does a drug's first pass metabolism have on its bioavailability?

<p>It decreases the drug’s bioavailability. (D)</p> Signup and view all the answers

What does a steep slope on a dose-response curve of a drug indicate?

<p>A small change in dose leads to large changes in response. (D)</p> Signup and view all the answers

What is the main benefit of administering a drug through the intravenous route?

<p>It bypasses the first-pass effect. (C)</p> Signup and view all the answers

What would be the most likely effect on the absorption of an acidic drug (such as aspirin) when administered with an antacid?

<p>Decreased absorption due to formation of a less absorbable salt. (B)</p> Signup and view all the answers

Which phase of drug metabolism primarily involves oxidation, reduction, or hydrolysis?

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

Which process is most likely to cause a drug to be reabsorbed from the renal tubules back into the bloodstream?

<p>Passive diffusion of lipophilic molecules (D)</p> Signup and view all the answers

If a drug has a half-life of 4 hours, how long will it take for the drug concentration to reach 25% of the original concentration?

<p>8 hours (A)</p> Signup and view all the answers

What factor may cause a need to switch a medication from an oral form to a transdermal form?

<p>Patient's difficulty in swallowing (A)</p> Signup and view all the answers

When considering a medication that should not be crushed, which of the following is a potential reason?

<p>The medication contains enteric coating (C)</p> Signup and view all the answers

What change in drug elimination might be expected in a patient with renal impairment?

<p>Decreased drug elimination rate (D)</p> Signup and view all the answers

Which aspect should be considered for prescribing medications to the geriatric population?

<p>Higher likelihood of drug-drug interactions (C)</p> Signup and view all the answers

Which of the following is a downside of using modified or extended-release formulations?

<p>Increased risk of dose dumping (A)</p> Signup and view all the answers

What is meant by the term 'therapeutic window' in pharmacology?

<p>The range between the minimum effective dose and the minimum toxic dose (A)</p> Signup and view all the answers

Which factor is likely to have the least effect on drug absorption?

<p>The patient’s age and weight (B)</p> Signup and view all the answers

Which process best describes the movement of a drug from its site of administration into the bloodstream?

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

What is the primary role of drug metabolism in pharmacokinetics?

<p>To facilitate drug elimination from the body (C)</p> Signup and view all the answers

Which of the following statements is true regarding 'first-pass effect'?

<p>It reduces the bioavailability of orally administered drugs (D)</p> Signup and view all the answers

What does a steep slope on a dose-response curve indicate?

<p>A small increase in dose yields a large increase in effect (D)</p> Signup and view all the answers

Which is NOT a characteristic of pharmaceutical equivalence?

<p>Identical inactive ingredients (C)</p> Signup and view all the answers

How does ionization of a drug molecule affect its distribution in the body?

<p>Influences the binding of the drug to plasma proteins (A)</p> Signup and view all the answers

A patient presents with severe nausea and vomiting, making oral medications difficult. Which of the following dosage forms would be most appropriate in this situation?

<p>Intravenous injection (C), Transdermal patch (D)</p> Signup and view all the answers

A patient with severe renal impairment is prescribed a medication that is primarily eliminated by the kidneys. What pharmacokinetic parameter would be most important to consider when determining a safe and effective dosage for this patient?

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

Which of the following scenarios is most likely to necessitate a change in the dosage form of a medication being used?

<p>Patient reports difficulty swallowing capsules (C)</p> Signup and view all the answers

A patient presents with hepatic impairment and a Child-Pugh score of 7. What general recommendation for dosage adjustments should be considered for medications that are primarily metabolized by the liver?

<p>Decrease the dosage by 25% (D)</p> Signup and view all the answers

Which of the following is a potential disadvantage of using modified or extended-release formulations?

<p>Increased risk of drug interactions (B)</p> Signup and view all the answers

What does the term 'bioavailability' refer to in pharmacology?

<p>The extent and rate at which the active ingredient is absorbed and becomes available at the site of action. (C)</p> Signup and view all the answers

Which statement best describes the first-pass effect?

<p>It is the process where the liver metabolizes a drug before it reaches systemic circulation. (C)</p> Signup and view all the answers

What is a primary consequence of a drug possessing a narrow therapeutic index?

<p>It requires more frequent dosing adjustments based on therapeutic monitoring. (C)</p> Signup and view all the answers

Which factors primarily influence drug absorption in the gastrointestinal tract?

<p>Molecular weight and hydrophobicity. (A)</p> Signup and view all the answers

What is the significance of the angle of the slope in a dose-response curve?

<p>It shows the potency of the drug and the steepness of the response to increasing doses. (A)</p> Signup and view all the answers

Which of the following best defines pharmacodynamics?

<p>The relationship between drug concentration and its effect on the body. (B)</p> Signup and view all the answers

In the context of drug metabolism, what is primarily involved in Phase II reactions?

<p>Conjugation reactions that make drugs more water-soluble. (C)</p> Signup and view all the answers

What does the term 'therapeutic window' imply about a drug?

<p>The range of drug dosage that produces a therapeutic effect without causing toxicity. (A)</p> Signup and view all the answers

Which characteristic is associated with passive transport across a cell membrane?

<p>Movement occurs down a concentration gradient. (D)</p> Signup and view all the answers

What primary factor determines the rate of absorption across cell membranes?

<p>The surface area available for absorption and concentration gradient. (D)</p> Signup and view all the answers

The ratio of ionized to unionized drug molecules at a specific site is most likely to impact which pharmacokinetic process?

<p>Absorption and distribution. (C)</p> Signup and view all the answers

A drug that relies on a protein carrier for transport is most likely using which process?

<p>Either active or facilitated diffusion. (D)</p> Signup and view all the answers

Which of these is a distinguishing characteristic of active transport compared to facilitated diffusion?

<p>Only active transport requires energy (D)</p> Signup and view all the answers

Which of the following best describes how a vasodilator could alter drug absorption?

<p>By altering gastrointestinal perfusion, affecting the rate of drug absorption into the bloodstream (B)</p> Signup and view all the answers

A drug administered intravenously has a bioavailability of 100%. What does this mean in the context of drug absorption?

<p>The total amount of the drug administered reaches systemic circulation without any loss due to absorption or first-pass effects. (A)</p> Signup and view all the answers

How does the first-pass effect primarily influence a drug's bioavailability?

<p>It reduces the amount of active drug that reaches systemic circulation due to liver metabolism. (D)</p> Signup and view all the answers

If a drug has 80% bioavailability when administered transdermally, what percentage of a 100mg dose will reach systemic circulation?

<p>80mg (D)</p> Signup and view all the answers

Which of the following medications is MOST likely to be affected by chelation with calcium?

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

What is the most accurate definition of the 'first-pass effect'?

<p>The initial metabolism of a drug by the liver before reaching systemic circulation. (B)</p> Signup and view all the answers

What does the therapeutic index of a drug reflect?

<p>The range of doses that produce a therapeutic effect without unacceptable adverse events. (C)</p> Signup and view all the answers

Which of the following best describes the term 'drug distribution' in pharmacology?

<p>The movement of a drug from the bloodstream to various body tissues and compartments. (D)</p> Signup and view all the answers

Which route of drug administration bypasses the gastrointestinal tract?

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

What is the primary function of plasma proteins in drug distribution?

<p>To bind to drugs, potentially decreasing their activity. (D)</p> Signup and view all the answers

Which of the following factors is most likely to decrease the percentage of a drug bound to plasma proteins?

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

What is a significant factor influencing the absorption of a drug?

<p>The number and type of membranes the drug must cross. (B)</p> Signup and view all the answers

According to the information provided, if two drugs have the same efficacy, which characteristic of a dose response curve would indicate one drug may be safer than another?

<p>A wider therapeutic window. (B)</p> Signup and view all the answers

If a drug has a high apparent volume of distribution (Vd), what does that indicate?

<p>The drug is extensively distributed into tissues. (D)</p> Signup and view all the answers

Which of these options is a factor which affects the extent of a drug's distribution?

<p>Drug solubility (hydrophilic vs lipophilic) (A)</p> Signup and view all the answers

What does the term 'variability' refer to in the context of dose-response relationships?

<p>The range of responses to a particular dose in a population. (B)</p> Signup and view all the answers

What effect does drug binding to plasma proteins have on the drug's activity?

<p>Inactivates the drug, preventing it from binding to receptors. (B)</p> Signup and view all the answers

Which of the following is a key factor affecting the rate of drug distribution after absorption?

<p>The rate and amount of blood flow to an area. (B)</p> Signup and view all the answers

If a drug is administered via the sublingual route, what characteristic makes it a suitable method of administration?

<p>It bypasses the digestive system and enters the bloodstream quickly. (B)</p> Signup and view all the answers

What is the clinical relevance of the 'apparent volume of distribution'?

<p>It helps estimate the necessary drug dosage. (D)</p> Signup and view all the answers

Which of the following is an example of 'enteral' administration of a drug?

<p>Oral ingestion. (C)</p> Signup and view all the answers

What is the primary function of metabolic reactions in the body regarding a drug?

<p>To facilitate the elimination of the drug from the body. (B)</p> Signup and view all the answers

What is a key characteristic of a Phase II metabolic reaction?

<p>It involves the conjugation of drug metabolites, typically leading to inactive forms. (A)</p> Signup and view all the answers

If a drug is metabolized into an active form with affinity for the parent drug receptor, what is this metabolite best described as?

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

In terms of drug metabolism, what is the most important effect of chemical reactions in the liver?

<p>They enhance the drug's water solubility to facilitate elimination. (B)</p> Signup and view all the answers

A patient has a polymorphism that causes them to be a poor metabolizer of a particular drug; how would this most likely affect its concentration-time curve (AUC)?

<p>AUC will increase, reflecting a higher concentration of the parent drug. (D)</p> Signup and view all the answers

What is the most likely outcome of enzyme induction on a drug's effect?

<p>Decreased effectiveness of the drug therapy. (C)</p> Signup and view all the answers

If a drug is an enzyme inhibitor, what is the most likely effect this will have on a drug metabolized by that enzyme?

<p>An increased concentration of the drug in plasma. (B)</p> Signup and view all the answers

Consider a patient with extremely functional CYP2D6 when considering codeine, a prodrug requiring this enzyme for activation. What would be the appropriate adjustment for a dose of codeine in this patient?

<p>Decrease the dose to account for faster activation of the drug. (D)</p> Signup and view all the answers

What is a characteristic of competitive inhibitors?

<p>They can be displaced by higher concentrations of an agonist. (B)</p> Signup and view all the answers

Which of the following describes a consequence of P450 enzyme inhibition?

<p>Increased risk of drug toxicity. (C)</p> Signup and view all the answers

What role does drug metabolism play in excretion?

<p>It alters drugs into charged, hydrophilic metabolites for easier elimination. (D)</p> Signup and view all the answers

Which mechanism is NOT involved in renal drug excretion?

<p>Active absorption from the bloodstream (D)</p> Signup and view all the answers

What condition primarily affects glomerular filtration?

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

What type of excretion involves the bile instead of urine?

<p>Hepato/Biliary excretion (D)</p> Signup and view all the answers

Which statement correctly describes noncompetitive inhibitors?

<p>They bind to an alternative site and cannot be displaced by the agonist. (D)</p> Signup and view all the answers

Which factor does NOT influence the renal excretion process?

<p>Mood of the patient (C)</p> Signup and view all the answers

Flashcards

Pharmacology

The study of how drugs interact with living organisms, including their absorption, distribution, metabolism, excretion, and effects.

Drug

Any substance that can alter a biological function when administered to a living organism.

Biopharmaceutics

The study of how the physical and chemical properties of a drug affect its absorption, distribution, metabolism, and excretion. It focuses on how drugs are formulated and how they behave in the body.

Absorption

The process by which a drug enters the bloodstream.

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Distribution

The process by which a drug is transported from the bloodstream to the tissues and organs.

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Metabolism

The process by which a drug is broken down into inactive metabolites by enzymes in the liver and other organs.

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Excretion

The process by which a drug is eliminated from the body, mainly through the kidneys in urine, but also through feces, sweat, and breath.

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Pharmacodynamics

The study of the biochemical and physiological effects of drugs and their mechanisms of action.

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Generic vs. Brand-name Drugs: FDA Regulations

The FDA allows generic drugs to have the same active ingredient as brand-name drugs, but they may have different inactive ingredients, which can affect the drug's appearance, taste, and how it's absorbed. This leads to slight variations in bioavailability, the rate and extent to which the drug enters the bloodstream.

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Transdermal Drug Forms - Advantages & Disadvantages

Drugs delivered through the skin, like patches or lotions, offer a sustained release and avoid the digestive system, but can be affected by skin conditions like dryness, and may irritate the skin.

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Liver Disease & Drug Metabolism

If a patient's liver function declines, the body may not be able to process medications efficiently, potentially leading to drug accumulation and an increased risk of side effects. Doctors may need to adjust dosages based on the severity of liver damage.

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Do Not Crush Medications

Some medications, especially those with a narrow therapeutic window, can be deadly or cause significant harm if they are crushed and taken orally instead of being absorbed as intended by the medication's formulation.

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Prescribing Drugs for Geriatric Patients

Geriatric patients often experience changes in metabolism and excretion, leading to a higher risk of drug accumulation and adverse events. Prescribers need to be cautious, monitor for adverse effects, consider lower dosages, and choose age-appropriate formulations.

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Dose-Response Curve

The relationship between the amount of drug administered and the intensity of the effect it produces.

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Therapeutic Index

The ratio of the dose that produces a toxic effect to the dose that produces a therapeutic effect.

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Angle of the Slope (Dose-Response Curve)

The steepness of the dose-response curve, which reflects how quickly the drug's effect increases as the dose increases.

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Drug Metabolism

The process by which a drug is broken down into inactive metabolites, mainly by enzymes in the liver.

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Prodrug

A drug that is inactive when administered but becomes active after metabolism.

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Half-Life

The time it takes for the plasma concentration of a drug to decrease by half.

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Drug Excretion

The process by which a drug is eliminated from the body, primarily through the kidneys.

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Steady-State Drug Concentration

The concentration of a drug in the blood when the rate of drug administration equals the rate of drug elimination.

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Do Not Crush Medications: Why?

A drug labeled "do not crush" should never be crushed or broken down before administering. This is because crushing these medications can alter their release mechanism, potentially leading to dangerous overdose or ineffective treatment.

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Transdermal Drug Forms: Pros and Cons

Transdermal medications deliver drugs through the skin, providing sustained release and bypassing the digestive system. However, factors like skin dryness and irritation can affect absorption, and some patients may experience skin reactions.

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Liver Disease and Drug Metabolism

Hepatic disease can affect the liver's ability to metabolize drugs, potentially leading to drug accumulation and increased risk of side effects. Physicians might adjust dosages based on the severity of liver damage.

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Prescribing for Geriatrics: Special Considerations

Geriatric patients often experience changes in metabolism and excretion. This increases the risk of drug accumulation and adverse events. Prescribers should be cautious, monitor for side effects, consider lower doses, and choose age-appropriate formulations.

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Angle of the Slope in a Dose-Response Curve

The steepness of the dose-response curve. A steep slope means the drug's effect increases rapidly as the dose increases.

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Drug Absorption

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

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Drug Distribution

The process by which a drug is transported from the bloodstream to the tissues and organs. It is affected by factors like blood flow, tissue permeability, and protein binding.

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Pharmacokinetics

The study of what the body does to a drug, including how it's absorbed, distributed, metabolized, and excreted.

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Therapeutic window

The range of drug doses that produce therapeutic effects without causing significant toxicity.

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Therapeutic Index (TI)

The ratio of the dose that produces a toxic effect to the dose that produces a therapeutic effect. A higher TI suggests a safer drug as there's a wider gap between the effective and toxic doses.

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Bioavailability

The fraction of an administered drug dose that reaches the systemic circulation, relative to an intravenous (IV) injection, which represents 100% bioavailability. It reflects how efficiently a drug is absorbed and becomes available at its site of action.

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First-Pass Metabolism

The process by which a drug absorbed from the gastrointestinal tract enters the portal vein and passes through the liver before reaching the systemic circulation. This first pass through the liver can significantly metabolize and reduce the amount of drug available to reach its target.

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Drug Absorption: How pH Affects It

Changes in the pH of the stomach or intestines can affect how well a drug is absorbed. Medications like antacids, H2 blockers, and proton pump inhibitors can alter the pH environment, influencing drug absorption.

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Drug Absorption: How Motility Affects It

Factors like laxatives, anticholinergics, and metoclopramide can change the rate and duration of how a drug moves through your gastrointestinal tract, ultimately affecting its absorption.

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Drug Absorption: How Perfusion Affects It

Drugs that increase blood flow to the gastrointestinal tract can enhance absorption. This is because more blood carries the drug from the gut to the systemic circulation.

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What is drug distribution?

The movement of a drug from the bloodstream to different body compartments.

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What factors influence drug distribution?

Factors that affect how well a drug is absorbed, including its ability to pass through cell membranes, blood flow to the absorption site, and how much it binds to proteins.

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What are plasma proteins?

Proteins in the blood that bind to drugs, preventing them from reaching target tissues and exerting their effects.

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What is the apparent volume of distribution (Vd)?

A measure of how much a drug distributes into tissues compared to the bloodstream.

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What does a high Vd mean?

A high Vd suggests a drug is extensively distributed into tissues, while a low Vd indicates it stays mostly in the bloodstream.

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What does a low Vd mean?

A high Vd suggests a drug is extensively distributed into tissues, while a low Vd indicates it stays mostly in the bloodstream.

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How does the binding of drugs to plasma proteins affect their activity?

This affects the amount of free drug that's able to cause an effect.

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How can the amount of bound drug change?

Conditions like malnutrition or liver disease affect protein production which can change how much drug is bound to protein, changing how much free drug is active.

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Competitive Inhibitor

A type of drug inhibitor that binds to the same site as the agonist, reducing the agonist's effect. It can be overcome by increasing the concentration of the agonist.

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Noncompetitive Inhibitor

A type of drug inhibitor that binds to a different site on the enzyme or receptor than the agonist, reducing the agonist's effect. It cannot be overcome by increasing the concentration of the agonist.

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Renal Excretion

A primary site of drug excretion, responsible for filtering blood and producing urine. It utilizes various mechanisms like glomerular filtration, active secretion, and passive reabsorption.

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Nephron

The functional unit of the kidney responsible for urine formation. It consists of a glomerulus, renal tubule, and collecting duct.

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Glomerular Filtration

One of the three key transport mechanisms in renal excretion. It's a non-selective process where 'free' drugs (not bound to proteins) smaller than a certain size are filtered from the blood into the nephron.

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Tubular Secretion

This process allows drugs to be transported from the blood across the tubular epithelium into the urine. It works against the concentration gradient and requires energy.

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Phase I Metabolism

A phase in drug metabolism that adds a functional group (like a handle) to the drug molecule. This prepares the drug for further modifications in phase II.

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Phase II Metabolism

A phase in drug metabolism where a drug is conjugated to a larger, water-soluble molecule. This enhances excretion.

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Polymorphisms

Variations in drug metabolism due to genetic factors. For example, some people are 'slow metabolizers' meaning they break down drugs slower, while others are 'fast metabolizers'.

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Enzyme Induction

When a substance speeds up the rate of drug metabolism. This can lead to decreased drug effectiveness or the need for higher drug doses.

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Enzyme Inhibition

When a substance slows down the rate of drug metabolism, potentially prolonging the drug's effects or increasing the risk of adverse reactions.

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Active Metabolite

When a drug is metabolized to a form that still has affinity for the original drug's receptor, leading to continued drug activity.

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Study Notes

Definitions

  • ADME: Absorption, Distribution, Metabolism, Excretion
  • Pharmacokinetics: The study of how drugs are absorbed, distributed, metabolized, and excreted in the body.
  • Pharmacodynamics: The study of the effects of drugs on the body and how the body responds to them.
  • Therapeutic Window: The range of drug concentrations that produce the desired effect without causing significant adverse effects; a narrow window means a small difference between the therapeutic and toxic doses while a wide window indicates a larger range.
  • Bioavailability: The fraction of administered drug that reaches the systemic circulation in an active form.
  • Bioequivalence: When two different formulations of the same drug have similar bioavailability and similar rates of absorption.
  • Drug: A substance used to treat, prevent, or diagnose a disease or condition.
  • Pharmacology: The study of drugs, their effects, and their uses.
  • Drug Biopharmaceutics: The study of how the physical and chemical properties of a drug affect its rate and extent of absorption.

Drug Dosing

  • Drug dosage forms/Drug Databases: Different ways a drug can be given (e.g., tablets, capsules, suspensions), and databases or websites used to look up drug information. This includes oral solutions, suspensions, elixirs and transdermal preparations.
  • Drug Dosing in Special Populations: Dosage adjustments tailored to specific groups of patients (e.g., elderly, pregnant women), including those with renal or hepatic disease.

Absorption, Distribution, Metabolism, Excretion (ADME)

  • Absorption: The process of taking in a drug. Factors affecting include:
    • Site of absorption in the GI tract (primary site is the small intestine).
    • Diffusion and transporter-mediated processes.
    • Particle size and ionization.
    • First-pass effect: The metabolism of a drug in the liver before it reaches the systemic circulation, reducing the bioavailability.
    • OTC medications may affect absorption.
    • Tissue permeability, and ionization.
  • Distribution: The movement of a drug throughout the body. Factors affecting include:
    • Tissue permeability, and ionization.
  • Metabolism: The process of breaking down a drug. Major enzymatic reactions include Phase I (e.g., oxidation, reduction, hydrolysis) and Phase II (conjugation) processes. These processes occur primarily within the liver. This includes the formation of active or inactive metabolites.
  • Excretion: The removal of a drug from the body. Important factors include renal excretion (filtration, secretion, reabsorption), biliary excretion, and other routes.

Dose-Response Relationships

  • Dose-response curve: A graph showing the relationship between the dose of a drug and its effect.
  • Therapeutic index: A measure of the safety of a drug. TI is quantified using ED50 and TD50 (effective dose and toxic dose).
  • Slope of the dose-response curve: Represents the magnitude of effect change per dose change also indicating the slope sensitivity. The angle of the slope corresponds to the rate of effect change as the dose increases.

Administration Routes

  • Various routes influence: onset, intensity, duration of a drug's effect. The comparison and contrast of different routes (e.g., oral, intravenous, intramuscular, subcutaneous, inhalational, transdermal) are crucial.

Other Key Concepts

  • Half-life: The time it takes for the concentration of a drug in the body to be reduced by half.
  • Drug interactions: The effects of one drug on another that alters drug metabolism or absorption.
  • Pharmaceutical equivalence/bioequivalence: The relative similarity of different formulations of the same drug in terms of activity; Bioequivalence relates specifically to absorption.
  • Therapeutic equivalence: When two different formulations of the same drug have the same therapeutic effect in a certain patient population.
  • Generic drugs: Drugs that contain the same active ingredients as brand-name drugs, but are made by different companies. (FDA approval implies similar bioavailability and absorption)
  • Adverse drug events (ADEs): Harmful effects of a drug.
  • Prescribing cascades: The pattern of prescribing drugs in response to another drug's adverse events.
  • Renal Disease and Hepatic Disease: These conditions can alter drug metabolism, elimination, and require dosage adjustments. This is relevant when considering dosages for special populations, such as those with hepatic disease or renal disease.
  • Child-Pugh score: A clinical assessment to evaluate liver function and severity of liver disease.
  • eGFR (estimated glomerular filtration rate): Estimate of kidney function.
  • CrCl (creatinine clearance): A measure of kidney function.

Patient counseling and considerations

  • Important factors to consider when counseling patients on dosage forms, routes of administration, and adverse effects of drugs.
  • Identifying medications that might need modification or avoidance for patients based on clinical evaluation and characteristics (renal disease, hepatic disease, geriatrics).
  • Consider conditions (e.g., geriatrics, hepatic/renal disease) and their impact on dosing and prescribing; this includes dosage and regimen adjustments for special populations.
  • Pharmaceutical Equivalence/Bioequivalence and FDA: FDA approval for generic equivalents implies similarity to the active ingredients of brand-name drugs with respect to bioavailability and rate of absorption.

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