Organic Drug Distribution Quiz
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Questions and Answers

What is the main challenge a drug faces after oral administration?

  • Passing through the gastrointestinal mucosa (correct)
  • Surviving in the acidic stomach
  • Avoiding metabolic destruction
  • Reaching the site of action

    • Which factor does not affect the ability of a drug to dissolve after oral administration?

  • Nature of the crystal form
  • Purity of the drug (correct)
  • Chemical structure of the drug
  • Type of tablet matrix

    • What determines if a drug will dissolve quickly or slowly after oral administration?

  • Physical characteristics of the drug (correct)
  • Ambient temperature during administration
  • Tablet color
  • Time of day when administered

    • What must a drug do to reach its desired target?

    <p>Undergo chemical modification</p> Signup and view all the answers

    Where is the site of action for a drug usually located?

    <p>On or in a cell</p> Signup and view all the answers

    What happens to drugs that do not dissolve well after oral administration?

    <p>They may not reach their desired target effectively</p> Signup and view all the answers

    What impact can gastrointestinal enzymes have on a drug molecule?

    <p>Accelerate its degradation</p> Signup and view all the answers

    Why might a new drug be considered for an alternate route of administration?

    <p>Low oral bioavailability</p> Signup and view all the answers

    Which drug is mentioned as a treatment for ulcerative colitis in the text?

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

    Why is mesalamine ineffective when taken orally?

    <p>It is metabolized to inactive forms before reaching the colon</p> Signup and view all the answers

    In what form is chloramphenicol mentioned to be water soluble enough to interact with taste receptors?

    <p>Dimeric form</p> Signup and view all the answers

    What alternative route of drug administration is NOT mentioned in the text?

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

    What are the main barriers involved in the distribution or partitioning of drugs in the gastrointestinal tract?

    <p>The aqueous environment of the gastrointestinal tract and the lipid bilayer cell membrane of the mucosal cells</p> Signup and view all the answers

    Why would parenteral administration be preferred in some cases?

    <p>When patients are unable to take drugs orally due to illness</p> Signup and view all the answers

    What is a disadvantage of intravenous administration of drugs?

    <p>Deposition in tissue depots and liver</p> Signup and view all the answers

    Why might some drugs be unsuitable for oral administration?

    <p>Because they are metabolized in the liver</p> Signup and view all the answers

    What can be a consequence of subcutaneous and intramuscular injections?

    <p>Deposition in tissue depots</p> Signup and view all the answers

    Where does intravenous administration place the drug within the body?

    <p>Directly into the circulatory system</p> Signup and view all the answers

    Why does protein binding limit the amount of drug available for interaction with specific receptor sites?

    <p>Proteins sequester the drug and reduce its availability</p> Signup and view all the answers

    What effect can the protein-bound form of a drug, like suramin, have on the duration of action in the body?

    <p>Prolongs the duration of action</p> Signup and view all the answers

    How can drug-protein binding lead to clinically significant drug interactions?

    <p>By displacing drugs from their protein-binding sites</p> Signup and view all the answers

    What impact can displacing warfarin from its albumin-binding sites have on prothrombin time?

    <p>Increased prothrombin time</p> Signup and view all the answers

    What is the role of tissue depots in drug distribution?

    <p>Tissue depots concentrate lipophilic drugs</p> Signup and view all the answers

    How does the lipophilicity of a drug relate to its concentration in tissue depots?

    <p>Lipophilic drugs accumulate in tissue depots</p> Signup and view all the answers

    Why does the concentration of thiopental rapidly decrease below its effective concentration after administration?

    <p>It redistributes into body fat.</p> Signup and view all the answers

    How does structural changes in the barbiturate series affect duration of action and CNS depression?

    <p>Decrease duration of action but increase CNS depression.</p> Signup and view all the answers

    What happens to the remaining thiopental that diffuses out of tissue depots into systemic circulation?

    <p>It is metabolized in the liver.</p> Signup and view all the answers

    Which type of barbiturates have the slowest onset of action and longest duration of action?

    <p>Those with more polar side chains.</p> Signup and view all the answers

    What effect do structural changes favoring partitioning into lipid tissue stores have?

    <p>Decrease duration of action and CNS depression.</p> Signup and view all the answers

    Why do barbiturates with more polar side chains enter and leave the CNS more slowly?

    <p>They have more difficulty diffusing across tissue depots.</p> Signup and view all the answers

    What factors contribute to a drug's ability to dissolve after oral administration?

    <p>Particle size, crystal form, and tablet coating</p> Signup and view all the answers

    Why is it important for a drug to dissolve quickly after oral administration?

    <p>To reach the site of action rapidly</p> Signup and view all the answers

    What can chemical modification of a drug help achieve?

    <p>Facilitate reaching the desired target</p> Signup and view all the answers

    How do varying the physical characteristics of a drug affect its dissolution after oral administration?

    <p>Speeds up the dissolution process</p> Signup and view all the answers

    Why must a drug avoid significant metabolic destruction before reaching the site of action?

    <p>To ensure its therapeutic effectiveness</p> Signup and view all the answers

    What role do tissue depots play in a drug's distribution within the body?

    <p>They store and release the drug over time</p> Signup and view all the answers

    What obstacle is common to both intravenous administration and subcutaneous/intramuscular injections according to the text?

    <p>Reaching tissue depots and the liver</p> Signup and view all the answers

    Which type of drug administration may be preferable for patients who are unable to accept drugs orally due to illness?

    <p>Parenteral administration</p> Signup and view all the answers

    What makes oral administration of some drugs not possible due to rapid and complete metabolism in the liver?

    <p>First-pass effect</p> Signup and view all the answers

    Which factor contributes to the rapid distribution of drugs throughout the body in intravenous administration?

    <p>Direct entry into the circulatory system</p> Signup and view all the answers

    Why is it mentioned that intramuscular injections show slow distribution of drugs into systemic circulation?

    <p>Diffusion from the site of injection</p> Signup and view all the answers

    What is a possible therapeutic advantage of bypassing the intestinal barrier using parenteral dosage forms?

    <p>Patients unable to accept oral drugs</p> Signup and view all the answers

    Why is acitretin recommended for a woman who wants to become pregnant?

    <p>It has a shorter half-life.</p> Signup and view all the answers

    What is the role of esterases in the activation of succinate esters to methylprednisolone?

    <p>They catalyze the hydrolysis to form methylprednisolone.</p> Signup and view all the answers

    What can be inferred about the biodistribution of etretinate and acitretin based on their respective terminal half-lives?

    <p>Etretinate has a longer half-life than acitretin.</p> Signup and view all the answers

    How does protein binding affect the availability of drugs in the systemic circulation?

    <p>It limits the amount of free drug in circulation.</p> Signup and view all the answers

    Why might prodrugs like methylprednisolone sodium succinate be preferred in drug design?

    <p>To increase water solubility.</p> Signup and view all the answers

    What distinguishes the terminal half-lives of etretinate and acitretin?

    <p>Their rate of metabolism in the body.</p> Signup and view all the answers

    What is the purpose of adding the palmitic acid moiety to chloramphenicol?

    <p>To mask the intense bitter taste of the drug</p> Signup and view all the answers

    What is a characteristic of most prodrugs mentioned in the text?

    <p>They are inactive in their native form</p> Signup and view all the answers

    Why is enalapril mentioned as an example of a prodrug in the text?

    <p>It is metabolized into an active inhibitor of angiotensin-converting enzyme (ACE)</p> Signup and view all the answers

    What happens to prodrugs like Olsalazine and chloramphenicol palmitate once they are inside the body?

    <p>They are cleaved to smaller compounds, including the active drug</p> Signup and view all the answers

    Why does a drug, unless intended for local action, need to pass through the gastrointestinal mucosal barrier?

    <p>To enter venous circulation and reach specific receptor sites</p> Signup and view all the answers

    How does the initial ester linkage of chloramphenicol palmitate affect drug solubility?

    <p>It decreases the drug's water solubility, allowing it to be formulated as a suspension</p> Signup and view all the answers

    How does protein binding affect the amount of drug available for interaction with specific receptor sites?

    <p>Limits the amount available</p> Signup and view all the answers

    What is the significance of a drug remaining in the body in protein-bound form for an extended period?

    <p>It prolongs toxic effects</p> Signup and view all the answers

    How can drug-protein binding lead to clinically significant drug interactions?

    <p>By displacing one drug from the binding site on albumin</p> Signup and view all the answers

    Why may a patient require a significant time for a drug's concentration to fall below toxic levels after experiencing serious adverse reactions?

    <p>Due to prolonged protein binding of the drug</p> Signup and view all the answers

    Which factor can lead to an increased prothrombin time and potential hemorrhage due to drug interactions?

    <p>Increased effective concentration of warfarin</p> Signup and view all the answers

    In which type of tissue depots are lipophilic drugs more likely to concentrate?

    <p>Inert tissue depots</p> Signup and view all the answers

    Why is acitretin recommended for a woman who would like to become pregnant?

    <p>It has a shorter half-life compared to etretinate.</p> Signup and view all the answers

    What is the purpose of using prodrug design?

    <p>To extend the biological half-life of the active drug.</p> Signup and view all the answers

    What effect does protein binding have on drugs once they enter the systemic circulation?

    <p>Delays the clearance of drugs from the body.</p> Signup and view all the answers

    How does the terminal half-life of etretinate compare to that of acitretin?

    <p>Etretinate has a shorter half-life than acitretin.</p> Signup and view all the answers

    What is significant about the biodistribution of prodrugs like methylprednisolone sodium succinate?

    <p>They alter the distribution and biological half-life of the active drug.</p> Signup and view all the answers

    Why are succinate esters used in drug design, specifically for methylprednisolone sodium succinate?

    <p>To enhance water solubility of the drug.</p> Signup and view all the answers

    How does protein binding affect a drug’s biodistribution according to the text?

    <p>Limits access to certain body compartments</p> Signup and view all the answers

    What is the role of the albumin–drug complex in drug distribution as mentioned in the text?

    <p>Acts as a reservoir for free drug</p> Signup and view all the answers

    How does protein binding impact a drug’s duration of action in the body?

    <p>Prolongs the duration of action</p> Signup and view all the answers

    Why might drugs bound to proteins like albumin be retained in maternal circulation and not cross the placental barrier?

    <p>Prevention of fetal exposure to drugs</p> Signup and view all the answers

    How does protein binding impact a drug’s effective solubility?

    <p>Reduces drug solubility</p> Signup and view all the answers

    What effect does the large size of the drug–protein complex have on renal excretion of the drug?

    <p>Prevents rapid excretion through glomerular membranes</p> Signup and view all the answers

    Why is palmitic acid moiety added as an ester to chloramphenicol?

    <p>To mask the intense bitter taste</p> Signup and view all the answers

    What is a common feature of most prodrugs mentioned in the text?

    <p>They are inactive in their native form</p> Signup and view all the answers

    Why is enalapril mentioned as an example of a prodrug?

    <p>To demonstrate its enhanced oral absorption</p> Signup and view all the answers

    What is the main purpose of converting chloramphenicol into chloramphenicol palmitate?

    <p>To enhance its interaction with taste receptors</p> Signup and view all the answers

    How do prodrugs like olsalazine and chloramphenicol palmitate become active drugs?

    <p>By being cleaved to smaller compounds</p> Signup and view all the answers

    Why do most prodrugs need to be metabolized to their active agents?

    <p>To convert them from inactive to active forms</p> Signup and view all the answers

    How does the presence of protein-bound drug in the body for an extended period affect the occurrence of serious adverse reactions?

    <p>Delays the occurrence of serious adverse reactions</p> Signup and view all the answers

    What can result from one drug displacing another from the binding site on albumin due to drug-protein binding phenomenon?

    <p>Increased hemorrhage risk</p> Signup and view all the answers

    How does the lipophilicity of a drug relate to its concentration in tissue depots according to the text?

    <p>The more lipophilic the drug, the more it concentrates in tissue depots</p> Signup and view all the answers

    What role do tissue depots play in drug distribution within the body?

    <p>Serve as storage locations for drugs</p> Signup and view all the answers

    How can displaced warfarin from its albumin-binding sites affect prothrombin time?

    <p>Increased prothrombin time</p> Signup and view all the answers

    Why do structural changes in the barbiturate series favoring partitioning into lipid tissue stores decrease duration of action?

    <p>Increased central nervous system (CNS) depression</p> Signup and view all the answers

    Why are barbiturates with slow onset of action and long duration of action said to contain more polar side chains?

    <p>To slow down entry and exit from the CNS</p> Signup and view all the answers

    What happens to the remaining thiopental that diffuses out of tissue depots into systemic circulation?

    <p>It is metabolized in the liver</p> Signup and view all the answers

    Why do barbiturates with more polar side chains enter and leave the central nervous system (CNS) more slowly?

    <p>To increase diffusion out of tissue depots</p> Signup and view all the answers

    How does protein binding affect drug availability for interaction with receptors?

    <p>It decreases the amount of free drug available</p> Signup and view all the answers

    What role do structural changes in barbiturate series that favor partitioning into lipid tissue stores play in CNS depression?

    <p>They increase CNS depression</p> Signup and view all the answers

    Chemical modification is not used to facilitate a drug reaching its desired target.

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

    Drugs administered orally always remain in solution as they pass through the gastrointestinal tract.

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

    Protein binding does not affect the distribution of drugs in the body.

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

    Dosage form and physical characteristics of a drug do not impact its dissolution rate after oral administration.

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

    A drug can easily reach its desired target without passing through various barriers in the body.

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

    The ability of a drug to dissolve after oral administration is solely determined by its chemical structure.

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

    Olsalazine is a monomer of the pharmacologically active mesalamine.

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

    Chloramphenicol is water insoluble enough to produce a pleasant taste when in contact with taste receptors on the tongue.

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

    Drugs that survive in the intestinal tract are more likely to be considered for oral administration than alternative routes.

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

    Metabolic degradation of drugs by intestinal bacteria can sometimes be advantageous.

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

    Parenteral administration is always preferred over oral administration for new drugs.

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

    Chloramphenicol palmitate is less water soluble than chloramphenicol.

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

    Parenterally administered drugs can easily cross the blood-brain barrier.

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

    Intraspinal routes deliver drugs directly into the brain.

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

    Methylprednisolone acetate is more water-soluble than methylprednisolone.

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

    The prodrug approach does not affect the solubility characteristics of a drug.

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

    The blood-brain barrier is composed of loosely joined epithelial cells.

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

    Injecting a drug directly into specific organs or areas of the body cannot bypass the BBB.

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

    Subcutaneous and intramuscular injections result in rapid distribution of the drug throughout the body.

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

    Intravenous administration causes the drug to be rapidly distributed throughout the body.

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

    The first-pass effect refers to drugs being metabolized in tissues other than the liver before reaching systemic circulation.

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

    Parenteral dosage forms are only used for patients who cannot tolerate oral drug administration.

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

    Drugs distributed via intravenous administration may end up in tissue depots and the liver.

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

    Protein binding can lead to clinically significant drug-drug interactions when one drug displaces another from the binding site on hemoglobin.

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

    The lipophilicity of a drug does not affect its concentration in tissue depots.

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

    The more lipophilic a drug is, the less likely it will concentrate in tissue depots.

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

    Suramin, a trypanocide drug, remains in the body in the protein-bound form for up to 3 months with a half-life of 50 days.

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

    Drugs bound to proteins like albumin are easily transported across the placental barrier.

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

    Neutral fat accounts for a small percentage of body weight and has minimal importance as a tissue depot for drugs.

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

    The lipophilicity of a drug does not impact its concentration in tissue depots.

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

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