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Questions et Réponses
What are the two main processes of transfer of drugs across cell barriers?
What are the two main processes of transfer of drugs across cell barriers?
- Osmosis and pinocytosis
- Passive diffusion and active transport (correct)
- Facilitated diffusion and endocytosis
- Bulk flow and filtration
What are the main features of lipid diffusion of drugs across membranes?
What are the main features of lipid diffusion of drugs across membranes?
- Independent of drug charge and polarity
- Independent of drug size and lipid solubility
- Dependent on drug charge and polarity
- Dependent on drug size and lipid solubility (correct)
What are the main features of aqueous diffusion of drugs across membranes?
What are the main features of aqueous diffusion of drugs across membranes?
- Independent of drug charge and polarity
- Independent of drug size and lipid solubility
- Dependent on drug charge and polarity (correct)
- Dependent on drug size and lipid solubility
Which of the following is true about drug administration?
Which of the following is true about drug administration?
What does bioavailability (F) provide a quantitative measure of?
What does bioavailability (F) provide a quantitative measure of?
Which factor does not affect drug absorption?
Which factor does not affect drug absorption?
How is bioavailability (F) calculated?
How is bioavailability (F) calculated?
What does a bioavailability of 100% indicate?
What does a bioavailability of 100% indicate?
In the equation for calculating bioavailability, what does AUC represent?
In the equation for calculating bioavailability, what does AUC represent?
What does a lower oral bioavailability percentage indicate?
What does a lower oral bioavailability percentage indicate?
If the AUC for a drug given orally is 200 (mg/L) x h and the AUC for the same drug given intravenously is 300 (mg/L) x h, what is the bioavailability?
If the AUC for a drug given orally is 200 (mg/L) x h and the AUC for the same drug given intravenously is 300 (mg/L) x h, what is the bioavailability?
If a dose of a drug given orally yields an AUC of (50 mcg/ml)x min while the same dose given IV yields an AUC of 100 (mcg/ml) x min, what is the oral bioavailability?
If a dose of a drug given orally yields an AUC of (50 mcg/ml)x min while the same dose given IV yields an AUC of 100 (mcg/ml) x min, what is the oral bioavailability?
Which process facilitates drug movement across membranes through intercellular pores?
Which process facilitates drug movement across membranes through intercellular pores?
What theory explains drug concentration in specific compartments depending on pH?
What theory explains drug concentration in specific compartments depending on pH?
Which drug illustrates the ion trapping mechanism with a pKa of 3?
Which drug illustrates the ion trapping mechanism with a pKa of 3?
In which step of ion trapping does passive reabsorption of lipid-soluble, unionized drug molecules occur?
In which step of ion trapping does passive reabsorption of lipid-soluble, unionized drug molecules occur?
Which drug administration route involves absorption through the lungs?
Which drug administration route involves absorption through the lungs?
What factor affecting drug absorption via the oral route is discussed in the text?
What factor affecting drug absorption via the oral route is discussed in the text?
Which drug administration route involves absorption through the skin?
Which drug administration route involves absorption through the skin?
Which process involves the movement of drug molecules from an area of low concentration to an area of high concentration?
Which process involves the movement of drug molecules from an area of low concentration to an area of high concentration?
Which drug administration route involves absorption through the mucous membranes under the tongue?
Which drug administration route involves absorption through the mucous membranes under the tongue?
Which drug administration route involves absorption through the rectum?
Which drug administration route involves absorption through the rectum?
Which type of drug transport is based solely on molecular size and is passive and non-selective?
Which type of drug transport is based solely on molecular size and is passive and non-selective?
Which theory explains drug concentration in specific compartments depending on the difference between pH and pKa?
Which theory explains drug concentration in specific compartments depending on the difference between pH and pKa?
Which route of drug administration involves placing the drug under the tongue?
Which route of drug administration involves placing the drug under the tongue?
What is the most important site for passive drug absorption due to its high surface area and high blood flow?
What is the most important site for passive drug absorption due to its high surface area and high blood flow?
Which factor may affect the process of absorption of drugs administered orally?
Which factor may affect the process of absorption of drugs administered orally?
What does a delay in gastric emptying do to the rate and extent of drug absorption?
What does a delay in gastric emptying do to the rate and extent of drug absorption?
Which route of drug administration involves placing the drug between the cheek and gum?
Which route of drug administration involves placing the drug between the cheek and gum?
What is the primary method of absorption for drugs administered through the sublingual route?
What is the primary method of absorption for drugs administered through the sublingual route?
Which route of administration involves drug delivery to the intestine and is affected by gastric emptying?
Which route of administration involves drug delivery to the intestine and is affected by gastric emptying?
What can delay in gastric emptying potentially do to the pH of the stomach and drug permeation behavior?
What can delay in gastric emptying potentially do to the pH of the stomach and drug permeation behavior?
What does enteral administration of a drug involve?
What does enteral administration of a drug involve?
Which route of administration bypasses the harsh gastrointestinal (GI) environment and avoids the first-pass effect?
Which route of administration bypasses the harsh gastrointestinal (GI) environment and avoids the first-pass effect?
What is the main site for drug absorption in the body?
What is the main site for drug absorption in the body?
What is a disadvantage of oral drug administration?
What is a disadvantage of oral drug administration?
Which type of transport is mediated by a protein carrier, does not require energy, and is structurally selective for the drug?
Which type of transport is mediated by a protein carrier, does not require energy, and is structurally selective for the drug?
What type of transport moves drugs against a concentration gradient and is driven by ATP hydrolysis?
What type of transport moves drugs against a concentration gradient and is driven by ATP hydrolysis?
What type of transport involves cell membrane engulfing of drugs and transportation into the cell by vesicle formation?
What type of transport involves cell membrane engulfing of drugs and transportation into the cell by vesicle formation?
Which process is used to secrete substances out of the cell through vesicle formation?
Which process is used to secrete substances out of the cell through vesicle formation?
What is the molecular weight range of drugs that can cross membranes by lipid diffusion?
What is the molecular weight range of drugs that can cross membranes by lipid diffusion?
Which type of transport is dependent on channel number, concentration gradient, water solubility, and molecular size of the drug?
Which type of transport is dependent on channel number, concentration gradient, water solubility, and molecular size of the drug?
What type of transport process is driven by ATP hydrolysis and can be primary or secondary?
What type of transport process is driven by ATP hydrolysis and can be primary or secondary?
Which type of transport involves the movement of fluids and solutes across cell barriers?
Which type of transport involves the movement of fluids and solutes across cell barriers?
What type of transport involves the movement of drugs through gaps between cells?
What type of transport involves the movement of drugs through gaps between cells?
Which type of transport is mediated by influx transporters increasing drug absorption and efflux transporters decreasing it?
Which type of transport is mediated by influx transporters increasing drug absorption and efflux transporters decreasing it?
What type of transport is used for substances too large to pass through the plasma cell membrane or transport proteins?
What type of transport is used for substances too large to pass through the plasma cell membrane or transport proteins?
Which type of transport involves the movement of drugs across cells?
Which type of transport involves the movement of drugs across cells?
Which drug administration route is primarily suitable for lipophilic drugs and bypasses first-pass effect?
Which drug administration route is primarily suitable for lipophilic drugs and bypasses first-pass effect?
Which drug administration route may cause pain if the drug is irritating and is unsuitable for large volumes?
Which drug administration route may cause pain if the drug is irritating and is unsuitable for large volumes?
Which route of administration achieves systemic effects with immediate drug availability in systemic circulation, suitable for emergency situations?
Which route of administration achieves systemic effects with immediate drug availability in systemic circulation, suitable for emergency situations?
Which drug administration route achieves local effect with locally high drug concentration and delayed systemic absorption?
Which drug administration route achieves local effect with locally high drug concentration and delayed systemic absorption?
Which route of administration is suitable for drugs with slow-release properties?
Which route of administration is suitable for drugs with slow-release properties?
Which drug administration route achieves rapid, direct systemic absorption, bypassing first-pass effect and stomach acid destruction?
Which drug administration route achieves rapid, direct systemic absorption, bypassing first-pass effect and stomach acid destruction?
Which drug administration route is primarily suitable for local effects on the skin, but absorption can be variable and unsuitable for certain drugs?
Which drug administration route is primarily suitable for local effects on the skin, but absorption can be variable and unsuitable for certain drugs?
Which route of administration achieves systemic effects primarily by lipid diffusion through the alveolar membrane, but may cause allergic reactions in some patients?
Which route of administration achieves systemic effects primarily by lipid diffusion through the alveolar membrane, but may cause allergic reactions in some patients?
Which drug administration route is used to localize drug effects at specific sites?
Which drug administration route is used to localize drug effects at specific sites?
Which route of administration is primarily used for moderate volumes and may affect certain lab tests?
Which route of administration is primarily used for moderate volumes and may affect certain lab tests?
Which drug administration route is primarily used for systemic or local effects, primarily by lipid diffusion, but may irritate the rectal mucosa?
Which drug administration route is primarily used for systemic or local effects, primarily by lipid diffusion, but may irritate the rectal mucosa?
Which route of administration is suitable for achieving local effects on the skin but may have variable absorption and be unsuitable for certain drugs?
Which route of administration is suitable for achieving local effects on the skin but may have variable absorption and be unsuitable for certain drugs?
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Notes d'étude
Drug Transfer Across Cell Membranes
- Lipid solubility of drugs allows them to cross the phospholipid bilayer of cell membranes.
- Drugs with a molecular weight between 100 and 1500 D can cross membranes by lipid diffusion.
- Aqueous diffusion of drugs occurs through aquaporin protein channels, dependent on channel number, concentration gradient, water solubility, and molecular size of the drug.
- Facilitated diffusion is mediated by a protein carrier, does not require energy, and is structurally selective for the drug.
- Active transport, an energy-dependent process driven by ATP hydrolysis, moves drugs against a concentration gradient and is saturable.
- Active transport can be primary (directly ATP-driven) or secondary (derived from ionic concentration differences).
- Carrier-mediated processes include active transport and facilitated diffusion, with influx transporters increasing drug absorption and efflux transporters decreasing it.
- Endocytosis involves cell membrane engulfing of drugs, which are transported into the cell by vesicle formation and may be receptor-mediated.
- Exocytosis is used to secrete substances out of the cell through vesicle formation, exemplified by insulin transport from pancreatic cells.
- Some drugs are too large to pass through the plasma cell membrane or transport proteins and enter cells by endocytosis, such as hormones, growth factors, and antibodies.
- Bulk flow transport of drugs across cell barriers occurs through the movement of fluids and solutes, contributing to drug transfer.
- The movement of drugs across cell membranes can occur through transcellular movement (across cells) or paracellular movement (through gaps between cells), impacting drug absorption and distribution.
Routes of Drug Administration and Absorption
- Nitroglycerin has rapid, direct systemic absorption, bypassing first-pass effect and stomach acid destruction
- Rectal administration may be used for systemic or local effects, primarily by lipid diffusion, but drugs may irritate rectal mucosa
- Topical application is suitable for local effects on the skin, but absorption can be variable and unsuitable for certain drugs
- Transdermal administration, primarily by lipid diffusion, bypasses first-pass effect, ideal for lipophilic drugs, but some patients may be allergic to patches
- Pulmonary administration as gases achieves systemic effects, primarily by lipid diffusion through the alveolar membrane, but requires sophisticated equipment
- Pulmonary administration as aerosols achieves local effect, primarily by lipid diffusion through the alveolar membrane, with locally high drug concentration and delayed systemic absorption
- Intravenous administration achieves systemic effects, with immediate drug availability in systemic circulation, suitable for emergency situations, but strict aseptic techniques are needed
- Intramuscular administration, depending on drug diluents, is suitable for moderate volumes, but may affect certain lab tests and be painful
- Subcutaneous administration, depending on drug diluents, is suitable for slow-release drugs, but may cause pain if drug is irritating and is unsuitable for large volumes
- Special parenteral routes, such as intrathecal, intraarterial, intracardiac, intrapleural, and intraperitoneal, are used to localize drug effects at specific sites
- Learning objectives include drug absorption, factors affecting it, bioavailability, routes of administration, speed and magnitude of drug effect, and AUC calculation
- Drug absorption into the systemic circulation is necessary for drugs to exert their effects, except for IV or cutaneous administration
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