Podcast
Questions and Answers
A patient with impaired renal function is prescribed a drug primarily eliminated through the kidneys. Which adjustment to the drug regimen would be LEAST appropriate to prevent drug accumulation and adverse effects?
A patient with impaired renal function is prescribed a drug primarily eliminated through the kidneys. Which adjustment to the drug regimen would be LEAST appropriate to prevent drug accumulation and adverse effects?
Competition between two drugs for the same anionic transporter in the proximal tubules of the kidney would most likely result in what outcome?
Competition between two drugs for the same anionic transporter in the proximal tubules of the kidney would most likely result in what outcome?
A drug is metabolized into more polar compounds via phase I and phase II reactions, what is the primary purpose of this biotransformation regarding renal excretion?
A drug is metabolized into more polar compounds via phase I and phase II reactions, what is the primary purpose of this biotransformation regarding renal excretion?
A drug is primarily cleared through both the kidney and the bile. If a patient experiences complete renal failure, what compensatory change in the body is most likely to occur to maintain drug clearance?
A drug is primarily cleared through both the kidney and the bile. If a patient experiences complete renal failure, what compensatory change in the body is most likely to occur to maintain drug clearance?
Signup and view all the answers
Premature infants and neonates have an incompletely developed tubular secretory mechanism. How does this physiological immaturity affect drug clearance and drug half-life in this population?
Premature infants and neonates have an incompletely developed tubular secretory mechanism. How does this physiological immaturity affect drug clearance and drug half-life in this population?
Signup and view all the answers
Why is rectal administration advantageous when a drug induces vomiting upon oral administration?
Why is rectal administration advantageous when a drug induces vomiting upon oral administration?
Signup and view all the answers
A patient requires immediate and localized treatment for cryptococcal meningitis. Which route of administration is MOST suitable?
A patient requires immediate and localized treatment for cryptococcal meningitis. Which route of administration is MOST suitable?
Signup and view all the answers
What is the PRIMARY reason that a significant portion of drugs administered rectally bypasses first-pass metabolism?
What is the PRIMARY reason that a significant portion of drugs administered rectally bypasses first-pass metabolism?
Signup and view all the answers
Why might transdermal drug delivery be considered advantageous over other routes for certain medications?
Why might transdermal drug delivery be considered advantageous over other routes for certain medications?
Signup and view all the answers
A patient with severe asthma is prescribed both albuterol and fluticasone via oral inhalation. What is the MOST LIKELY reason for prescribing these two drugs in combination?
A patient with severe asthma is prescribed both albuterol and fluticasone via oral inhalation. What is the MOST LIKELY reason for prescribing these two drugs in combination?
Signup and view all the answers
A researcher is developing a new topical cream containing a novel anti-inflammatory drug. What is the PRIMARY advantage of using topical administration for this drug?
A researcher is developing a new topical cream containing a novel anti-inflammatory drug. What is the PRIMARY advantage of using topical administration for this drug?
Signup and view all the answers
A patient is prescribed nitroglycerin via a transdermal patch. What is the MOST important consideration regarding the application site to ensure optimal drug absorption?
A patient is prescribed nitroglycerin via a transdermal patch. What is the MOST important consideration regarding the application site to ensure optimal drug absorption?
Signup and view all the answers
Why might nasal inhalation be preferred over oral administration for certain drugs targeting the respiratory system?
Why might nasal inhalation be preferred over oral administration for certain drugs targeting the respiratory system?
Signup and view all the answers
A drug's elimination half-life is significantly shorter than the desired duration of action. Which extended-release formulation strategy would least effectively maintain therapeutic drug levels?
A drug's elimination half-life is significantly shorter than the desired duration of action. Which extended-release formulation strategy would least effectively maintain therapeutic drug levels?
Signup and view all the answers
A patient with dysphagia requires medication that is usually administered orally. Which route of administration would be least appropriate, considering the patient's condition?
A patient with dysphagia requires medication that is usually administered orally. Which route of administration would be least appropriate, considering the patient's condition?
Signup and view all the answers
A new drug is developed that is highly susceptible to inactivation in the acidic environment of the stomach. Which formulation strategy would be most effective in ensuring its absorption?
A new drug is developed that is highly susceptible to inactivation in the acidic environment of the stomach. Which formulation strategy would be most effective in ensuring its absorption?
Signup and view all the answers
A drug is known to undergo significant first-pass metabolism, resulting in very low bioavailability when administered orally. Which alternative route of administration would be the least effective in improving the drug's bioavailability?
A drug is known to undergo significant first-pass metabolism, resulting in very low bioavailability when administered orally. Which alternative route of administration would be the least effective in improving the drug's bioavailability?
Signup and view all the answers
A patient requires a medication that needs to reach the systemic circulation as rapidly as possible. Considering the typical absorption rates associated with different routes, which route would be the least suitable?
A patient requires a medication that needs to reach the systemic circulation as rapidly as possible. Considering the typical absorption rates associated with different routes, which route would be the least suitable?
Signup and view all the answers
Which statement regarding the impact of the route of administration on drug bioavailability is least accurate?
Which statement regarding the impact of the route of administration on drug bioavailability is least accurate?
Signup and view all the answers
A drug is being developed that must precisely target intracellular receptors within the central nervous system to exert its therapeutic effect. Which factor related to pharmacokinetics is least crucial for the drug's success?
A drug is being developed that must precisely target intracellular receptors within the central nervous system to exert its therapeutic effect. Which factor related to pharmacokinetics is least crucial for the drug's success?
Signup and view all the answers
Which factor most significantly contributes to the extended duration of action seen with extended-release (ER) oral medications?
Which factor most significantly contributes to the extended duration of action seen with extended-release (ER) oral medications?
Signup and view all the answers
A patient requires immediate and complete drug bioavailability. Which route of administration is most suitable to achieve this?
A patient requires immediate and complete drug bioavailability. Which route of administration is most suitable to achieve this?
Signup and view all the answers
Why are some drugs administered via inhalation for rapid delivery?
Why are some drugs administered via inhalation for rapid delivery?
Signup and view all the answers
Which characteristic of intravenous (IV) administration makes it particularly useful for drugs like rocuronium?
Which characteristic of intravenous (IV) administration makes it particularly useful for drugs like rocuronium?
Signup and view all the answers
For a drug that causes significant gastric irritation, which formulation strategy would be most appropriate?
For a drug that causes significant gastric irritation, which formulation strategy would be most appropriate?
Signup and view all the answers
Why are depot preparations, such as haloperidol decanoate, administered intramuscularly?
Why are depot preparations, such as haloperidol decanoate, administered intramuscularly?
Signup and view all the answers
A patient requires long-term treatment with a drug, but has poor adherence to oral medications. Which route of administration might be most suitable to improve compliance?
A patient requires long-term treatment with a drug, but has poor adherence to oral medications. Which route of administration might be most suitable to improve compliance?
Signup and view all the answers
Why is subcutaneous (SC) administration preferred over intravenous (IV) administration for certain drugs like heparin?
Why is subcutaneous (SC) administration preferred over intravenous (IV) administration for certain drugs like heparin?
Signup and view all the answers
A patient with poorly controlled diabetes develops a non-healing ulcer on their foot. Applying a topical antibiotic ointment to the ulcer would result in what regarding drug absorption, assuming the medication is typically administered topically for local effect?
A patient with poorly controlled diabetes develops a non-healing ulcer on their foot. Applying a topical antibiotic ointment to the ulcer would result in what regarding drug absorption, assuming the medication is typically administered topically for local effect?
Signup and view all the answers
A new drug is developed that is intended to act locally within the synovial fluid of the knee joint to treat arthritis. Considering the routes of administration, which route would be MOST appropriate to achieve the desired therapeutic effect?
A new drug is developed that is intended to act locally within the synovial fluid of the knee joint to treat arthritis. Considering the routes of administration, which route would be MOST appropriate to achieve the desired therapeutic effect?
Signup and view all the answers
A medication is administered via inhalation for the treatment of asthma. What BEST describes the intended primary site of action for this drug?
A medication is administered via inhalation for the treatment of asthma. What BEST describes the intended primary site of action for this drug?
Signup and view all the answers
A patient is prescribed nitroglycerin to be administered sublingually during an angina attack. What is the MOST important reason for choosing this route of administration compared to swallowing a nitroglycerin tablet?
A patient is prescribed nitroglycerin to be administered sublingually during an angina attack. What is the MOST important reason for choosing this route of administration compared to swallowing a nitroglycerin tablet?
Signup and view all the answers
Consider varying routes of drug administration. What BEST explains why intravenous administration does NOT require absorption?
Consider varying routes of drug administration. What BEST explains why intravenous administration does NOT require absorption?
Signup and view all the answers
A drug molecule has a very high molecular weight. What is the MOST likely impact of this characteristic on its ability to cross cell membranes?
A drug molecule has a very high molecular weight. What is the MOST likely impact of this characteristic on its ability to cross cell membranes?
Signup and view all the answers
A weak acid drug is administered orally. Where in the body is this drug MOST likely to be absorbed?
A weak acid drug is administered orally. Where in the body is this drug MOST likely to be absorbed?
Signup and view all the answers
A research team is developing a new topical medication designed to deliver a drug for systemic absorption and effect. Which characteristic of the drug would be MOST favorable for effective absorption through the skin?
A research team is developing a new topical medication designed to deliver a drug for systemic absorption and effect. Which characteristic of the drug would be MOST favorable for effective absorption through the skin?
Signup and view all the answers
A drug administered intravenously exhibits a significantly shorter duration of action compared to the same drug administered orally. Which of the following factors would MOST likely explain this difference, assuming both routes achieve similar peak plasma concentrations?
A drug administered intravenously exhibits a significantly shorter duration of action compared to the same drug administered orally. Which of the following factors would MOST likely explain this difference, assuming both routes achieve similar peak plasma concentrations?
Signup and view all the answers
A novel drug is found to be a substrate for P-glycoprotein. If a patient is also taking a P-glycoprotein inhibitor, what is the MOST likely effect on the novel drug's oral bioavailability and tissue distribution?
A novel drug is found to be a substrate for P-glycoprotein. If a patient is also taking a P-glycoprotein inhibitor, what is the MOST likely effect on the novel drug's oral bioavailability and tissue distribution?
Signup and view all the answers
A patient with severe diarrhea is prescribed an oral medication. How will this condition MOST likely affect the drug's absorption, and what physiological mechanism is primarily responsible?
A patient with severe diarrhea is prescribed an oral medication. How will this condition MOST likely affect the drug's absorption, and what physiological mechanism is primarily responsible?
Signup and view all the answers
A weak acid drug with a pKa of 4.5 is administered orally. Where in the gastrointestinal tract will the drug be MOST readily absorbed, and what physicochemical property dictates this?
A weak acid drug with a pKa of 4.5 is administered orally. Where in the gastrointestinal tract will the drug be MOST readily absorbed, and what physicochemical property dictates this?
Signup and view all the answers
A drug that is a weak base is administered intravenously to a patient experiencing hyperventilation. How is the distribution of the drug likely to be affected, and what is the underlying mechanism?
A drug that is a weak base is administered intravenously to a patient experiencing hyperventilation. How is the distribution of the drug likely to be affected, and what is the underlying mechanism?
Signup and view all the answers
During the development of a new tablet formulation, it is observed that increasing the compression force during manufacturing significantly slows down the drug's dissolution rate. What is the MOST probable reason for this?
During the development of a new tablet formulation, it is observed that increasing the compression force during manufacturing significantly slows down the drug's dissolution rate. What is the MOST probable reason for this?
Signup and view all the answers
A drug is known to be absorbed via carrier-mediated transport in the small intestine. If an overdose of a structurally similar compound is ingested, what is the MOST likely effect on the absorption of the drug, and why?
A drug is known to be absorbed via carrier-mediated transport in the small intestine. If an overdose of a structurally similar compound is ingested, what is the MOST likely effect on the absorption of the drug, and why?
Signup and view all the answers
A research team is developing a new drug that needs to cross the blood-brain barrier (BBB). Considering the properties that facilitate drug entry into the brain, which of the following characteristics would be MOST favorable for this drug?
A research team is developing a new drug that needs to cross the blood-brain barrier (BBB). Considering the properties that facilitate drug entry into the brain, which of the following characteristics would be MOST favorable for this drug?
Signup and view all the answers
Flashcards
Pharmacokinetics
Pharmacokinetics
Quantitative measurement of drug processes: absorption, distribution, metabolism, and elimination.
Absorption
Absorption
Entry of the drug into plasma from the administration site.
Distribution
Distribution
Reversible movement of a drug from the bloodstream to tissues.
Metabolism
Metabolism
Signup and view all the flashcards
Elimination/Excretion
Elimination/Excretion
Signup and view all the flashcards
Enteral Administration
Enteral Administration
Signup and view all the flashcards
Sublingual Administration
Sublingual Administration
Signup and view all the flashcards
Enteric-coated Preparations
Enteric-coated Preparations
Signup and view all the flashcards
Transdermal Administration
Transdermal Administration
Signup and view all the flashcards
Intrathecal Administration
Intrathecal Administration
Signup and view all the flashcards
Rectal Administration
Rectal Administration
Signup and view all the flashcards
Oral Inhalations
Oral Inhalations
Signup and view all the flashcards
Nasal Inhalations
Nasal Inhalations
Signup and view all the flashcards
Pulmonary Epithelium
Pulmonary Epithelium
Signup and view all the flashcards
Erratic Rectal Absorption
Erratic Rectal Absorption
Signup and view all the flashcards
Topical Administration
Topical Administration
Signup and view all the flashcards
Parenteral administration
Parenteral administration
Signup and view all the flashcards
Intravenous (IV)
Intravenous (IV)
Signup and view all the flashcards
Intramuscular (IM)
Intramuscular (IM)
Signup and view all the flashcards
Subcutaneous (SC)
Subcutaneous (SC)
Signup and view all the flashcards
Extended release (ER/XR)
Extended release (ER/XR)
Signup and view all the flashcards
High bioavailability
High bioavailability
Signup and view all the flashcards
Inhalation
Inhalation
Signup and view all the flashcards
P-glycoprotein (P-gp)
P-glycoprotein (P-gp)
Signup and view all the flashcards
Drug Clearance by the Kidney
Drug Clearance by the Kidney
Signup and view all the flashcards
Proximal Tubules
Proximal Tubules
Signup and view all the flashcards
Distal Tubular Reabsorption
Distal Tubular Reabsorption
Signup and view all the flashcards
Renal Dysfunction Risks
Renal Dysfunction Risks
Signup and view all the flashcards
Carrier-Mediated Transport
Carrier-Mediated Transport
Signup and view all the flashcards
Saturable Transport
Saturable Transport
Signup and view all the flashcards
Effect of pH on Drug Absorption
Effect of pH on Drug Absorption
Signup and view all the flashcards
Endocytosis
Endocytosis
Signup and view all the flashcards
Exocytosis
Exocytosis
Signup and view all the flashcards
Blood Flow to Absorption Site
Blood Flow to Absorption Site
Signup and view all the flashcards
Total Surface Area for Absorption
Total Surface Area for Absorption
Signup and view all the flashcards
Contact Time at Absorption Surface
Contact Time at Absorption Surface
Signup and view all the flashcards
Extravascular Administration
Extravascular Administration
Signup and view all the flashcards
Local Effects
Local Effects
Signup and view all the flashcards
Systemic Effects
Systemic Effects
Signup and view all the flashcards
Transdermal Absorption
Transdermal Absorption
Signup and view all the flashcards
Factors Affecting Absorption
Factors Affecting Absorption
Signup and view all the flashcards
Lipid Solubility and Absorption
Lipid Solubility and Absorption
Signup and view all the flashcards
Types of Drug Administration
Types of Drug Administration
Signup and view all the flashcards
Absorption Process in Extravascular Administration
Absorption Process in Extravascular Administration
Signup and view all the flashcards
Study Notes
Pharmacokinetics
- Pharmacokinetics is the quantitative measurement of drug action
- Absorption: Drug entry into plasma, either directly or indirectly
- Distribution: Drug reversibly leaves the bloodstream and distributes into interstitial and intracellular fluids
- Metabolism: Biotransformation of drugs by the liver or other tissues
- Elimination/Excretion: Drug and metabolites are eliminated from the body (urine, bile, or feces)
- It includes the rate processes for drug movement into, within, and out of the body
- Pharmacodynamics: Describes the effects the drug has on the human body, including adverse effects
Route of Drug Administration
- Determined by the therapeutic objective (rapid onset, long-term treatment, local site)
- Major routes are enteral, parenteral, and topical
A. Enteral
- Oral administration (safest, most common, and economical)
- Oral drugs can be overcome with activated charcoal
- Enteric-coated preparations protect the drug from stomach acid, delivering it to the less acidic intestine
- Useful for acid-unstable drugs (Omeprazole) and stomach-irritating drugs (aspirin)
- Extended-release preparations (ER or XR): Slower absorption and prolonged duration of action
2. Sublingual/Buccal
- Buccal similar to sublingual
- Advantages include ease of administration, rapid absorption, and bypassing the harsh GI environment.
- Useful for drug rapid absorption
B. Parenteral
- Introduces drug directly into the systemic circulation
- Used for drugs poorly absorbed in the GI tract (e.g., Heparin)
- Useful for drugs unstable in the GI tract (e.g. Insulin), for unconscious patients or when rapid action is needed
1. Intravenous (IV)
- Most common parenteral route
- Useful for drugs not absorbed orally, such as neuromuscular blockers (e.g., rocuronium)
- Administered as a bolus (full amount of drug delivered immediately) or infusion (infused over a longer period)
- Lower peak plasma concentrations and increased duration of circulating drug levels
2. Intramuscular (IM)
- Can be in aqueous solutions or specialized depot preparations
- Depot preparations absorb slowly
3. Subcutaneous (SC)
- Minimizes hemolysis and thrombosis risks
- Provide constant, slow, and sustained effects
- Should not be used with drugs causing tissue irritation
C. Others
- Inhalations: Rapid delivery across the respiratory tract and pulmonary epithelium.
- Intrathecal/Intraventricular: Direct introduction into the cerebrospinal fluid (e.g., intrathecal amphotericin B)
- Topical: Used for local effects (e.g., creams for fungal infections)
- Transdermal: Achieves systemic effects through skin application (e.g., patches)
- Rectal: Minimizes liver biotransformation, useful for vomiting patients or unconscious patients.
5. Rectal
- 50% of rectal drainage bypasses the portal circulation, minimizing liver biotransformation.
- Useful when drug causes vomiting, or if the patient is unconscious.
Extravascular Administration
- Drugs administered extravascularly can be divided into two categories: local and systemic effects
- Local effects: often applied topically (e.g., eye drops, dermal preparations)
- Systemic effects: Facilitates absorption into the circulatory system (e.g., tablets)
Absorption
- Intravascular administration directly enters the bloodstream
- Extravascular administration: drug moves from the site of administration to the systemic circulation
- Mechanisms: Passive diffusion (most common), facilitated diffusion, active transport, endocytosis
Factors Affecting Absorption
- pH: Affects absorption of weak acids and bases
- Solubility: Lipophilic drugs absorb better than highly hydrophilic drugs.
- Surface area: Larger surface area facilitates greater absorption (e.g., intestine).
- Contact time: Longer contact time at the absorption site facilitates greater absorption
- Blood flow: Higher blood flow to the absorption site (e.g., intestine) increases absorption.
- Chemical instability: Some drugs, such as penicillin G, are unstable in the pH of the gastric contents, and some are degraded by the enzymes in the tract
Bioavailability
- The extent to which a drug is absorbed into the systemic circulation.
- It is calculated using the area under the plasma concentration-time curve (AUC).
- Poorly soluble drugs have a lower bioavailability
Factors Affecting Bioavailability
- First-pass metabolism: some drugs are metabolized by the liver when swallowed (before entering systemic circulation)
- Solubility of the drug
- Chemical instability
Distribution
- Movement of drugs from the systemic circulation to various tissues and organs
- Factors: Blood flow, capillary permeability, drug's binding to plasma proteins, and relative lipophilicity of the drug
- Compartments: Plasma, extracellular fluid (interstitial and intracellular), and total body water
Clearance
- Removal of drugs from the body.
- Important organs: kidneys, liver (bile), gut (feces), lungs, and skin.
Renal Elimination
- Glomerular filtration: Drugs enter the kidney to form a glomerular capillary plexus.
- Proximal tubular secretion: Drugs leave the glomerular filtrate (that were not transferred) and are secreted through the efferent arterioles which form a capillary plexus surrounding the tubular lumen.
- Factors to consider: Anions (weak acids) move in one transport system, and cations (weak bases) move in another.
Altered Metabolism
- Enzyme induction: Speeds up drug metabolism resulting in decreased drug concentration, half-life, and increased clearance
- Enzyme inhibition: slows down drug metabolism resulting in increased drug concentration, half-life, and decreased clearance.
- Factors like barbiturates, alcohol, some herbal substances and some foods inhibit/induce metabolic enzymes.
Zero and First Order Kinetics
- First-order kinetics: Constant percentage of drug removed per unit time, and rate of elimination is proportional to the drug concentration
- Zero-order kinetics: Constant amount of drug removed per unit time, and higher concentration decreases the elimination rate.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
Description
Explore factors affecting renal drug elimination, including renal impairment, drug competition, biotransformation, and compensatory mechanisms, in this quiz. Evaluate how these processes influence drug accumulation, clearance, and half-life, emphasizing dose adjustments needed in special populations like neonates.