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Questions and Answers
What is the primary function of a drug?
What is the primary function of a drug?
Which of the following is a source of naturally derived drugs?
Which of the following is a source of naturally derived drugs?
What is the term for a drug's brand name?
What is the term for a drug's brand name?
What is the purpose of a placebo?
What is the purpose of a placebo?
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What is the main goal of Phase I clinical trials?
What is the main goal of Phase I clinical trials?
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What is the purpose of pharmacovigilance?
What is the purpose of pharmacovigilance?
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What is the difference between single-blind and double-blind studies?
What is the difference between single-blind and double-blind studies?
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Which phase of clinical trials typically involves the largest number of patients?
Which phase of clinical trials typically involves the largest number of patients?
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What is the primary factor that affects the rate of drug absorption in the gastrointestinal tract?
What is the primary factor that affects the rate of drug absorption in the gastrointestinal tract?
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What happens to the absorption of a drug when the gastric emptying rate is slow?
What happens to the absorption of a drug when the gastric emptying rate is slow?
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Which of the following is a transmembrane transporter protein that is involved in drug absorption?
Which of the following is a transmembrane transporter protein that is involved in drug absorption?
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What is the role of P-glycoprotein in drug absorption?
What is the role of P-glycoprotein in drug absorption?
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What is the effect of pH on drug absorption?
What is the effect of pH on drug absorption?
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What is the clinical significance of a drug's pKa?
What is the clinical significance of a drug's pKa?
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Based on the information provided, how would you enhance the elimination of aspirin from the body in case of poisoning?
Based on the information provided, how would you enhance the elimination of aspirin from the body in case of poisoning?
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What is bioavailability of a drug?
What is bioavailability of a drug?
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Which of the following is NOT a mechanism of drug absorption from the GI tract?
Which of the following is NOT a mechanism of drug absorption from the GI tract?
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Which of the following is an example of active transport?
Which of the following is an example of active transport?
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What is the main difference between facilitated diffusion and active transport?
What is the main difference between facilitated diffusion and active transport?
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What is the role of carrier proteins in drug absorption?
What is the role of carrier proteins in drug absorption?
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Why does blood flow to the absorption site influence drug absorption?
Why does blood flow to the absorption site influence drug absorption?
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Which of the following is NOT a factor that influences drug absorption by passive diffusion?
Which of the following is NOT a factor that influences drug absorption by passive diffusion?
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Why is the surface area of the small intestine important for drug absorption?
Why is the surface area of the small intestine important for drug absorption?
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Why is epinephrine administered intramuscularly (IM) rather than subcutaneously (SC) during shock?
Why is epinephrine administered intramuscularly (IM) rather than subcutaneously (SC) during shock?
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What factor can influence the dissolution of drug particles into molecules?
What factor can influence the dissolution of drug particles into molecules?
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Which factor is least likely to affect drug stability in the gastrointestinal tract (GIT)?
Which factor is least likely to affect drug stability in the gastrointestinal tract (GIT)?
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What is the primary site for first-pass metabolism of drugs?
What is the primary site for first-pass metabolism of drugs?
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Which condition would most likely reduce hepatic first-pass metabolism?
Which condition would most likely reduce hepatic first-pass metabolism?
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Which of the following routes of administration is primarily used for topical effects?
Which of the following routes of administration is primarily used for topical effects?
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Which of the following factors does NOT affect drug absorption in the gastrointestinal tract?
Which of the following factors does NOT affect drug absorption in the gastrointestinal tract?
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What term describes the metabolism of drugs in a single passage through the liver before reaching systemic circulation?
What term describes the metabolism of drugs in a single passage through the liver before reaching systemic circulation?
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Which of the following drugs is known for being extensively metabolized during the first-pass effect?
Which of the following drugs is known for being extensively metabolized during the first-pass effect?
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What is the primary focus of pharmacokinetics?
What is the primary focus of pharmacokinetics?
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Which factor significantly influences drug ionization and absorption?
Which factor significantly influences drug ionization and absorption?
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What is bioavailability?
What is bioavailability?
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Which of the following routes of administration has the highest bioavailability?
Which of the following routes of administration has the highest bioavailability?
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What is the role of p-glycoprotein in pharmacology?
What is the role of p-glycoprotein in pharmacology?
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Which of these factors does NOT affect drug bioavailability?
Which of these factors does NOT affect drug bioavailability?
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What is the primary difference between pharmacokinetics and pharmacodynamics?
What is the primary difference between pharmacokinetics and pharmacodynamics?
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Which edition of 'Lippincott's Illustrated Reviews: Pharmacology' is required for this course?
Which edition of 'Lippincott's Illustrated Reviews: Pharmacology' is required for this course?
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Flashcards
Pharmacokinetics
Pharmacokinetics
The study of how a drug's concentration changes over time in the body. It involves absorption, distribution, metabolism, and excretion.
Pharmacodynamics
Pharmacodynamics
The study of how a drug interacts with its target and produces its effects. It focuses on the drug's mechanism of action.
Drug Absorption
Drug Absorption
The movement of a drug from its administration site into the bloodstream.
Drug Ionization
Drug Ionization
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P-Glycoprotein
P-Glycoprotein
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Bioavailability
Bioavailability
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Factors Affecting Bioavailability
Factors Affecting Bioavailability
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Parenteral Routes of Administration
Parenteral Routes of Administration
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Placebo
Placebo
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Pharmacokinetics (PhK)
Pharmacokinetics (PhK)
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Placebo Effects
Placebo Effects
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Phase I Clinical Trial
Phase I Clinical Trial
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Phase II Clinical Trial
Phase II Clinical Trial
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Phase III Clinical Trial
Phase III Clinical Trial
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Post-Marketing Pharmacovigilance
Post-Marketing Pharmacovigilance
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Drug Distribution
Drug Distribution
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Drug Metabolism
Drug Metabolism
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Drug Excretion
Drug Excretion
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Passive Diffusion
Passive Diffusion
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Facilitated Diffusion
Facilitated Diffusion
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Active Transport
Active Transport
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Effect of pH on Drug Absorption
Effect of pH on Drug Absorption
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First-Pass Effect
First-Pass Effect
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Parenteral Routes
Parenteral Routes
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Enteral Routes
Enteral Routes
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Drug Dissolution
Drug Dissolution
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pKa
pKa
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Contact Time
Contact Time
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Gastric Emptying
Gastric Emptying
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Kidney Drug Elimination
Kidney Drug Elimination
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Study Notes
Course Information
- Course: BMS161 (1): General Pharmacology
- Professor: Ahmed Nour Eldin Hassan
- Assistant Professor: Nevien Fekry Abdalla
- Lecturer: Mai Ebeid
- Faculty: Medicine
- Semester: Spring 2024
Course Description
- Course Title: Foundations of Pharmacology
- Practical Course
- Emphasizes practical skills like finding knowledge and calculating doses.
- Includes discussions and free reading sessions.
- Covers areas including pharmacokinetics, pharmacodynamics, cholinergic nervous system, adrenergic nervous system, general chemotherapy, and principles of cancer chemotherapy.
- Includes learning resources based on specific textbooks/reviews
Learning Resources
- Required: Lippincott's Illustrated reviews: Pharmacology (7th edition)
- Optional:
- Basic and Clinical Pharmacology (15th edition) by Bertram G. Katzung, Suzan B. Masters, and Anthony J. Trevor
- Rang and Dale's Pharmacology (8th edition) by H.P. Rang, M.M. Dale, J.M. Ritter, R.J. Flower, and G. Henderson
Pharmacokinetic-1 Absorption Intended Learning Objectives
- Explain the difference between pharmacokinetics and pharmacodynamics.
- Understand the clinical significance of drug pKa & pH of medium in drug ionization, lipid solubility, absorption, and excretion.
- Summarize the role of P-glycoprotein in affecting serum drug levels.
- Compare different routes of drug administration.
- Define drug bioavailability.
- List factors affecting bioavailability.
- Predict the effect of liver diseases on drug pharmacokinetics.
Drug Information
- Drug Definition: A chemical substance for treatment, diagnosis, prevention, or to suppress a physiological process (e.g., ovulation suppression).
- Chemical Name (Generic)
- Nonproprietary Name (Brand name)
- Examples: Paracetamol (Acetaminophen), Panadol®, Abimol®, Pyral®
Sources of Drugs
- Natural sources: Plants (atropine, morphine, peppermint), Animals (insulin), Microorganisms (penicillin), Minerals (iron, calcium).
- Semi-synthetic: In-between natural and synthetic
- Synthetic:
- Chemical synthesis (e.g., aspirin)
- Biological synthesis using Recombinant DNA technology (e.g., human insulin, Erythropoietin).
Drug Journey from Discovery to Market
- Animal Study: Pharmacologic profile, organ actions, safety tests, acute/chronic toxicity, reproductive, carcinogenic, mutagenic, addiction liability.
- Clinical Study (3-7 years)
- Phase I: Small number of healthy volunteers (non-blind), determines clinical dose range in humans.
- Phase II: Small number of patients (single-blind), evaluates safety and efficacy compared to current drugs.
- Phase III: Large number of patients (double-blind), confirms previous findings.
- Post-Marketing Pharmacovigilance: Ongoing monitoring for adverse effects.
Single vs. Double-Blind technique
- Placebo: inert substance to gauge patient reactions unrelated to the drug's effects.
- Placebo effects: reactions not caused by the drug.
- Single-blind: patients unaware of the treatment, physician knows.
- Double-blind: patients and physician unaware of the treatment.
Division of General Pharmacology
- Pharmacodynamics: mechanism of drug action on the body (e.g., biochemical, physiological effects, side effects).
- Pharmacokinetics: What the body does to the drug (processes of absorption, distribution, metabolism (biotransformation), and excretion (ADME).
Pharmacokinetic Principles
- Absorption: Transfer of drug from administration site to bloodstream.
- Distribution: Movement of drug to various parts of the body (blood, target sites)
- Metabolism: Chemical alteration of drug by the body (e.g., liver).
- Excretion: Removal of drug or its metabolites from the body.
- Not specifically designed; but, we study effective dose kinetics (blood, distribution, elimination)
Absorption Mechanisms
- Passive diffusion, With concentration gradient, No ATP, No carrier
- Facilitated diffusion, With concentration gradient, Carrier, NO ATP
- Active transport, With or against concentration gradient, ATP, Carrier
- Endocytosis, (as in vitamin B12).
- Exocytosis, (as in neurotransmitter release).
Carrier Transport System
- Characteristics: Saturable, Limited absorption
- Competition: Endogenous substrate vs. drugs for the same carrier (e.g., L-Dopa for amino acid carriers to the brain).
Factors Influencing Absorption
- Effect of pH on drug absorption (ionized vs. unionized forms).
- Blood flow to the absorption site (blood flow in and out, e.g., intestinal flow).
- Total surface area available for absorption (intestine > stomach).
- Contact time at the absorption surface.
- Expression of P-glycoprotein (drug transport protein).
P-Glycoprotein
- Genetic variability involved.
- Associated with multidrug resistance (e.g., in cancer cells)
pKa and pH effects on drug absorption
- pKa: pH where 50% of drug is ionized (charged) and 50% unionized (uncharged).
- Change in local pH affecting the relative amounts of ionized/unionized forms, hindering/helping drug movement.
- Ionized forms are hydrophilic (water-soluble), cannot easily cross membranes.
- Unionized forms are lipophilic (fat-soluble), can easily cross membranes/enter the body.
Clinical Significance of pKa
- GIT: Aspirin (weak acid) absorption influenced by stomach pH.
- Kidney: Alkaline urine used in aspirin overdose to enhance excretion, increase ionization, inhibit tubular reabsorption.
Bioavailability
- Definition: Percentage of administered drug reaching systemic circulation, exerting biological effects.
- Calculation: AUC (area under the concentration-time curve) after non-IV administration / AUC after IV administration x 100.
- Factors impacting bioavailability: disintegration, dissolution, drug properties, pKa, gut pH. Factors from GIT, e.g., enzymes, food, presence of diseases, etc.
First-Pass Metabolism
- Definition: Drug metabolism occurring in the liver, gut wall, or lungs before systemic circulation.
- Factors affecting first pass metabolism -Reduction in portal blood flow -Inhibition of hepatic metabolizing enzymes
- Resulting Effects
- ↑ Bioavailability.
- Locations of metabolism (liver, intestines, lungs).
- Example drugs: nitroglycerin, propranolol, nicotine impacting first pass metabolism.
Routes of Administration
- Enteral (GI tract): oral (most common).
- Parenteral (outside of GI tract): intravenous, intramuscular, subcutaneous, intradermal, intrathecal, epidural, intra-arterial, inhalation, etc.
- Topical (skin/tissue): for direct local impact.
Prescription
- Rational professional prescription is critical.
- Rationale for professional/prescription treatment.
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Description
Test your knowledge in the foundations of pharmacology with this quiz designed for BMS161. Explore key concepts in pharmacokinetics, pharmacodynamics, and chemotherapy principles. This quiz is aligned with the required readings and practical skills emphasized in the course.