Podcast
Questions and Answers
Which of the following factors is NOT a primary determinant of passive drug diffusion across cell membranes?
Which of the following factors is NOT a primary determinant of passive drug diffusion across cell membranes?
- Lipid solubility of the drug
- Presence of hydrophilic channels
- Concentration gradient of the drug
- Blood flow to the target organ (correct)
What is the primary reason why water-soluble drugs need hydrophilic channels to cross cell membranes?
What is the primary reason why water-soluble drugs need hydrophilic channels to cross cell membranes?
- To bypass the lipophilic core of the cell membrane (correct)
- To bind to specific transmembrane proteins
- To create a pathway for active transport
- To increase the concentration gradient of the drug
Which of the following statements accurately describes the difference between active transport and facilitated diffusion?
Which of the following statements accurately describes the difference between active transport and facilitated diffusion?
- Active transport requires energy, while facilitated diffusion does not
- Active transport utilizes specific carrier proteins, while facilitated diffusion does not
- Both A and B are correct (correct)
- Active transport can move drugs against their concentration gradient, while facilitated diffusion cannot
Why is the passive transport of drugs from the bloodstream to the interstitium of most organs primarily limited by blood flow?
Why is the passive transport of drugs from the bloodstream to the interstitium of most organs primarily limited by blood flow?
What is the primary reason oral administration of drugs often requires higher doses compared to intravenous administration?
What is the primary reason oral administration of drugs often requires higher doses compared to intravenous administration?
Which of the following statements best describes the blood-brain barrier?
Which of the following statements best describes the blood-brain barrier?
Which route of administration is considered impractical for rapid therapeutic effects in the perioperative setting?
Which route of administration is considered impractical for rapid therapeutic effects in the perioperative setting?
What is the primary mechanism by which hydrophilic drugs enter the CNS?
What is the primary mechanism by which hydrophilic drugs enter the CNS?
What characteristic primarily affects the ability of a drug to passively cross cell membranes?
What characteristic primarily affects the ability of a drug to passively cross cell membranes?
What advantages does sublingual administration offer over oral administration?
What advantages does sublingual administration offer over oral administration?
Which of the following is NOT a characteristic of active transport?
Which of the following is NOT a characteristic of active transport?
What is a key factor limiting the practical application of transcutaneous administration of drugs?
What is a key factor limiting the practical application of transcutaneous administration of drugs?
What is the primary factor determining the rate of absorption of intramuscularly administered drugs?
What is the primary factor determining the rate of absorption of intramuscularly administered drugs?
Which of the following drugs is specifically mentioned in the text as suitable for sublingual administration?
Which of the following drugs is specifically mentioned in the text as suitable for sublingual administration?
Which of the following administration routes is most likely to result in the fastest onset of action for a lipophilic drug?
Which of the following administration routes is most likely to result in the fastest onset of action for a lipophilic drug?
What is a major limitation for the use of electric current to enhance drug absorption through the skin?
What is a major limitation for the use of electric current to enhance drug absorption through the skin?
Which of the following is a reason why subcutaneous injection of certain drugs can be unpredictable?
Which of the following is a reason why subcutaneous injection of certain drugs can be unpredictable?
Which route of administration bypasses the limitations of drug absorption and distribution?
Which route of administration bypasses the limitations of drug absorption and distribution?
Why is inhalation an extremely desirable route of drug administration?
Why is inhalation an extremely desirable route of drug administration?
Which of the following is NOT a limitation of epidural and perineural administration of local anesthetics?
Which of the following is NOT a limitation of epidural and perineural administration of local anesthetics?
What is a major challenge with the administration of certain drugs, like heparin and insulin, subcutaneously?
What is a major challenge with the administration of certain drugs, like heparin and insulin, subcutaneously?
What is the primary factor that determines the rate of absorption of an orally administered drug?
What is the primary factor that determines the rate of absorption of an orally administered drug?
What is the likely consequence of a rapid increase in plasma concentration of a drug with a low therapeutic index?
What is the likely consequence of a rapid increase in plasma concentration of a drug with a low therapeutic index?
Which of the following routes of administration typically has the fastest absorption rate?
Which of the following routes of administration typically has the fastest absorption rate?
What is the main reason why oral administration is not commonly used in anesthesia practice?
What is the main reason why oral administration is not commonly used in anesthesia practice?
What is the therapeutic index of a drug?
What is the therapeutic index of a drug?
Which of the following is NOT a factor that can influence the rate of absorption of a drug?
Which of the following is NOT a factor that can influence the rate of absorption of a drug?
What is the significance of maintaining a plasma concentration above the minimum effective plasma concentration?
What is the significance of maintaining a plasma concentration above the minimum effective plasma concentration?
Which of the following statements about bioavailability is TRUE?
Which of the following statements about bioavailability is TRUE?
What does the provided text state about lipophilic drugs and their movement across capillary walls?
What does the provided text state about lipophilic drugs and their movement across capillary walls?
What is the primary factor limiting the rate of active transport or facilitated diffusion of drugs?
What is the primary factor limiting the rate of active transport or facilitated diffusion of drugs?
What is a notable characteristic of the P-glycoprotein (P-gp) transporter system?
What is a notable characteristic of the P-glycoprotein (P-gp) transporter system?
Which type of transporter is responsible for the transport of endogenous opioids into the brain?
Which type of transporter is responsible for the transport of endogenous opioids into the brain?
What does the text suggest about intravenous (IV) administration of drugs?
What does the text suggest about intravenous (IV) administration of drugs?
Why does loperamide, a lipophilic µ-opioid agonist used for diarrhea, have limited bioavailability?
Why does loperamide, a lipophilic µ-opioid agonist used for diarrhea, have limited bioavailability?
What is a common characteristic of both facilitated diffusion and active transport of drugs?
What is a common characteristic of both facilitated diffusion and active transport of drugs?
Why are there limited research findings on the impact of transporter proteins on individual drug responses?
Why are there limited research findings on the impact of transporter proteins on individual drug responses?
Flashcards
Drug Absorption
Drug Absorption
The process by which drugs move from administration site to bloodstream.
Lipophilic Drugs
Lipophilic Drugs
Drugs that can easily pass cell membranes due to their fat-loving nature.
Hydrophilic Drugs
Hydrophilic Drugs
Drugs that require water channels to move across membranes.
Passive Diffusion
Passive Diffusion
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Active Transport
Active Transport
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Facilitated Diffusion
Facilitated Diffusion
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Blood-Brain Barrier
Blood-Brain Barrier
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Transmembrane Proteins
Transmembrane Proteins
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Saturable processes
Saturable processes
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Lipophilic compounds
Lipophilic compounds
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P-glycoprotein (P-gp)
P-glycoprotein (P-gp)
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Bioavailability
Bioavailability
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OATP (Organic Anion Transporter Peptides)
OATP (Organic Anion Transporter Peptides)
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Intravenous (IV) administration
Intravenous (IV) administration
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Concentration gradient
Concentration gradient
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Therapeutic Index
Therapeutic Index
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Plasma Concentration
Plasma Concentration
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Minimum Effective Concentration
Minimum Effective Concentration
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Oral Administration
Oral Administration
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Gastric Emptying
Gastric Emptying
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Intravenous Administration
Intravenous Administration
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Pulmonary Endothelium
Pulmonary Endothelium
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Intramuscular Injection
Intramuscular Injection
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Subcutaneous Administration
Subcutaneous Administration
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Intrathecal Injection
Intrathecal Injection
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Epidural Injection
Epidural Injection
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Inhalational Administration
Inhalational Administration
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First-Pass Metabolism
First-Pass Metabolism
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Sublingual Administration
Sublingual Administration
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Transcutaneous Administration
Transcutaneous Administration
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Subcutaneous Injection
Subcutaneous Injection
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Nasal Drug Absorption
Nasal Drug Absorption
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Metabolically Active Intestinal Mucosa
Metabolically Active Intestinal Mucosa
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Study Notes
Drug Absorption and Routes of Administration
- Drugs must cross cell membranes to reach their site of action. Lipid-soluble drugs passively diffuse across lipid bilayers.
- Water-soluble drugs require hydrophilic channels in membranes for passive diffusion.
- CNS drug entry is often limited by the blood-brain barrier. Active transport mechanisms move drugs across the blood-brain barrier against concentration gradients.
- Active transport and facilitated diffusion are saturable processes, limited by the number of carrier proteins.
- Lipophilic drugs, while not needing transporters to enter tissues, may be removed by ATP-dependent transporters like P-gp.
- Organic anion polypeptide transporters (OATPs) transport endogenous opioids and some drugs into the brain.
- Intravenous (IV) administration provides immediate, 100% bioavailability, but rapid overshoot may occur with drugs having low therapeutic indices.
- Bioavailability is the rate and extent to which a drug reaches the systemic circulation unchanged.
Oral Administration
- Oral administration is safe and convenient, but bioavailability is variable and often less than 100%.
- Gastric emptying and intestinal surface area influence absorption rates.
- First-pass metabolism in the liver significantly reduces bioavailability for many orally administered drugs.
- Oral administration is typically less desirable for rapid effects in a clinical setting because of inconsistent rates of bioavailability and variable times to reach peak concentration.
- Sublingual administration bypasses first-pass metabolism and can rapidly achieve high plasma concentrations.
Transcutaneous Administration
- Some lipophilic drugs can penetrate intact skin.
- Transcutaneous patches provide sustained drug delivery for conditions like maintenance therapy, but they take a longer time to reach therapeutic levels compared to other routes.
- Using electricity to enhance transdermal drug absorption has been explored but remains limited in practical applications.
Intramuscular and Subcutaneous Administration
- Intramuscular (IM) absorption is usually rapid and complete due to high muscle blood flow.
- Subcutaneous (SC) absorption is more variable due to varying subcutaneous blood flow. This leads to variable absorption rates and times to onset of action when compared to IM.
Intrathecal, Epidural, and Perineural Injection
- Intrathecal injection directly delivers drugs to the spinal cord, avoiding absorption and distribution limitations.
- Epidural and perineural injections require drug absorption through the dura or nerve sheath, respectively.
Inhalational Administration
- Inhalational administration of drugs is highly effective due to the lung's large surface area and high blood flow.
- Newer technologies enable rapid and predictable aerosolization of drugs, achieving comparable pharmacokinetic effects to intravenous administration.
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