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Questions and Answers
What is a reason sublingual and buccal routes of administration avoid the first pass effect?
What is a reason sublingual and buccal routes of administration avoid the first pass effect?
Which of the following is NOT a suitable candidate for oral delivery?
Which of the following is NOT a suitable candidate for oral delivery?
Which of the following routes of administration are suitable for patients who cannot swallow?
Which of the following routes of administration are suitable for patients who cannot swallow?
Which of the following is NOT a disadvantage of oral administration?
Which of the following is NOT a disadvantage of oral administration?
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What is a common reason why drugs are not suitable for oral administration?
What is a common reason why drugs are not suitable for oral administration?
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What is a significant advantage of sublingual and buccal routes of administration?
What is a significant advantage of sublingual and buccal routes of administration?
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What is a potential disadvantage of rectal administration?
What is a potential disadvantage of rectal administration?
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Which of the following drug administration routes is considered the most suitable for irritant drugs like anticancer drugs?
Which of the following drug administration routes is considered the most suitable for irritant drugs like anticancer drugs?
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What is the primary advantage of intravenous (IV) drug administration over other routes?
What is the primary advantage of intravenous (IV) drug administration over other routes?
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Which of the following is an example of a sublingual drug?
Which of the following is an example of a sublingual drug?
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Which of the following is NOT a disadvantage of intravenous (IV) drug administration?
Which of the following is NOT a disadvantage of intravenous (IV) drug administration?
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According to the provided text, what is a key advantage of intramuscular (IM) drug administration over oral administration?
According to the provided text, what is a key advantage of intramuscular (IM) drug administration over oral administration?
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Which of the following drug administration routes is most suitable for a patient experiencing severe vomiting?
Which of the following drug administration routes is most suitable for a patient experiencing severe vomiting?
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Which of the following routes of administration is considered unsuitable for children?
Which of the following routes of administration is considered unsuitable for children?
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Which route of administration is best suited for drugs that are inactivated in the gut and liver?
Which route of administration is best suited for drugs that are inactivated in the gut and liver?
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Which of the following is NOT a major advantage of rectal administration?
Which of the following is NOT a major advantage of rectal administration?
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Which route of administration is best suited for patients experiencing vomiting or seizures?
Which route of administration is best suited for patients experiencing vomiting or seizures?
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Which factor limits the use of oral administration for certain drugs?
Which factor limits the use of oral administration for certain drugs?
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Which of these is a DISADVANTAGE of rectal administration?
Which of these is a DISADVANTAGE of rectal administration?
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Why is sublingual administration considered an advantageous route?
Why is sublingual administration considered an advantageous route?
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Which factor is NOT a concern for parenteral drug administration?
Which factor is NOT a concern for parenteral drug administration?
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What factor is primarily influenced by the excipients in a drug formulation?
What factor is primarily influenced by the excipients in a drug formulation?
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Which dosage form is expected to have the highest rate of absorption?
Which dosage form is expected to have the highest rate of absorption?
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Which characteristic of a drug best indicates its ability to cross biological membranes?
Which characteristic of a drug best indicates its ability to cross biological membranes?
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What is a disadvantage of the intravenous (IV) route of drug administration compared to other methods?
What is a disadvantage of the intravenous (IV) route of drug administration compared to other methods?
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Which route of drug administration is noted for allowing self-administration?
Which route of drug administration is noted for allowing self-administration?
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What is the role of enteric coating in specially formulated oral drugs?
What is the role of enteric coating in specially formulated oral drugs?
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Which of the following drugs is least likely to be well absorbed due to high polarity?
Which of the following drugs is least likely to be well absorbed due to high polarity?
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What is a primary benefit of using transdermal/topical drug delivery?
What is a primary benefit of using transdermal/topical drug delivery?
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How does the absorption of subcutaneous drugs differ from that of intramuscular drugs?
How does the absorption of subcutaneous drugs differ from that of intramuscular drugs?
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What primarily affects the dissolution rate and absorption of a drug in the gastrointestinal tract?
What primarily affects the dissolution rate and absorption of a drug in the gastrointestinal tract?
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Which type of dosage form is expected to have slower absorption compared to others, all else being equal?
Which type of dosage form is expected to have slower absorption compared to others, all else being equal?
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What major downside does the inhalation route have when compared to others?
What major downside does the inhalation route have when compared to others?
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What is the significance of bioequivalence studies for generic drugs?
What is the significance of bioequivalence studies for generic drugs?
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Which method allows for a faster absorption than oral administration but is slower than IV?
Which method allows for a faster absorption than oral administration but is slower than IV?
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What is a significant risk associated with the use of transdermal patches?
What is a significant risk associated with the use of transdermal patches?
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What factor can affect the absorption rate of subcutaneous drugs?
What factor can affect the absorption rate of subcutaneous drugs?
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What is a significant disadvantage of using anaesthetic gases like sevoflurane?
What is a significant disadvantage of using anaesthetic gases like sevoflurane?
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Which of the following routes is specifically used for spinal anaesthesia?
Which of the following routes is specifically used for spinal anaesthesia?
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What does drug permeation refer to?
What does drug permeation refer to?
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What characteristic of the blood-brain barrier affects drug entry?
What characteristic of the blood-brain barrier affects drug entry?
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Which type of membrane allows both non-polar and polar molecules to pass through due to its porosity?
Which type of membrane allows both non-polar and polar molecules to pass through due to its porosity?
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What is a key factor in the bioavailability of inhaled anesthetics?
What is a key factor in the bioavailability of inhaled anesthetics?
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Which drugs are commonly administered intraperitoneally?
Which drugs are commonly administered intraperitoneally?
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Which types of compounds can be effectively reabsorbed in renal tubules?
Which types of compounds can be effectively reabsorbed in renal tubules?
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Study Notes
Pharmacokinetics I
- Pharmacokinetics is the study of how the body processes drugs.
- The principles of ADME: Absorption, Distribution, Metabolism, and Excretion.
- Absorption: How a drug enters the body.
- Distribution: How a drug moves throughout the body.
- Metabolism: How a drug is broken down.
- Excretion: How a drug leaves the body.
- ADME/LADME: Absorption, Distribution, Metabolism, and Excretion (also Liberation and Dosage form).
Drug Administration Routes
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Local: Applied directly to the area of need.
- Examples: topical application (skin, eyes, nasal), rectal, inhalation.
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Systemic: Enters the bloodstream and exerts effects throughout the body.
- Examples: oral, sublingual, buccal/cheek, rectal, inhalation. parenteral (injection - IV, IM, subcutaneous, transdermal).
-
Parenteral routes: Involves skin puncture.
- Examples: Intravenous (IV), Intramuscular (IM), Subcutaneous (SC), etc.
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Enteral routes: The drug enters the body through the digestive system.
- Examples: oral, sublingual, buccal,rectal, gastric feeding.
Drug Permeation
- Movement of drug molecules across biological membranes.
- Key for ADME process.
- Factors like lipid solubility, degree of ionization, and concentration gradients influence permeation.
- Drug permeation occurs via pathways like diffusion through lipid bilayers, aqueous channels, and carrier-mediated transport.
Drug Absorption
- Process of drug movement from administration site into systemic circulation.
- Crucial in pharmacokinetic study.
- Important factors influencing oral absorption: drug stability in the GI tract, dosage form, lipophilicity, particle size, degree of ionization, gastric emptying, intestinal motility, first-pass metabolism, disease state.
- Factors affecting absorption in the small intestine: large surface area of villi and microvilli, and active secretion.
Drug Interactions
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Drug-drug: These occur when multiple drugs interact. E.g. proton pump inhibitors raise stomach pH, reducing some drug absorption.
- Colestyramine binds to other drugs like warfarin, affecting their absorption.
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Drug-disease: Conditions that alter absorption. E.g. Crohn's disease or ulcerative colitis affects drug absorption; and some stomach conditions also impact drug absorption.
Routes of Drug Permeation
- Sublingual/Buccal: Absorption occurs via passive diffusion; limited by molecular weight of the drug through oral mucosa.
- Intramuscular (IM): Absorption into system occurs via slow process depending on muscle blood flow. Absorbed faster from deltoid than gluteal muscle.
- Subcutaneous (SC): Passive diffusion to capillary wall - Lipophilic/lipid solvable drugs travel through capillary membranes directly. Other water solvable drugs diffuse through membrane pores.
- Rectal: Highly vascularized for passive diffusion, but absorption can be erratic - some drugs pass through the superior rectal vein, which is still subjected to first pass metabolism and absorption in the liver.
- Transdermal: Drugs pass through intercellular and intracellular routes across the skin; The skin's stratum corneum (outermost layer) is a crucial factor.
- Inhalation: Drugs in aerosols or gases can be given systemically or locally..
- Intra-arterial: For thrombolytic drugs, chemotherapy or certain types of chemo, and spinal anesthesia.
- Intra-thecal: Used for central nervous system (CNS) infections or anesthesia.
- Intra-peritoneal: For continuous ambulatory peritoneal dialysis (CAPD) or animal experiments.
- Intra-articular: Injected directly into joints, often for rheumatoid arthritis treatment.
Special Formulations
- Enteric coated: Protects drugs from stomach acid and releases them in the small intestine, suitable in cases where the drug is not stable in the acidic conditions of the stomach.
- Sustained-release: Provides continuous drug delivery over an extended period.
Degree of Ionization (pH & pKa)
- Drugs are weak acids/bases, existing as ionized or unionized forms.
- Ionization impacts the drug's ability to cross membranes. Ionized forms of drugs typically do not pass through membranes as efficiently as non-ionized (uncharged) forms; which can affect absorption.
- The pH of various body parts (e.g., stomach, small intestine, blood) influences ionization.
- The Handerson-Hasselbalch equation relates pH, pKa, and the relative concentrations of ionized and unionized forms.
Other Factors Affecting Absorption
- Factors like gastric emptying rate, intestinal motility, and presence of food influence drug absorption.
- Drug interactions (drug-drug or drug-disease interactions) can also play a role, impacting absorption.
- Drug stability in the gastrointestinal tract and physicochemical properties such as lipophilicity, particle size, and form are influential factors.
- The environment in the small intestine tends to remain consistent throughout the day., which tends to affect drug absorption.
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Description
Test your understanding of the basic principles of pharmacokinetics, including the ADME process: Absorption, Distribution, Metabolism, and Excretion. Explore various drug administration routes, such as local and systemic options, and learn about parenteral and enteral methods. This quiz is designed to reinforce your knowledge in pharmacology.
