Pharmacology Course Overview
39 Questions
0 Views

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

Which of the following classes of drugs are included in the course?

  • Antibiotics
  • Hormonal agents
  • Antivirals
  • All of the above (correct)

    • Antihistamines are classified solely as anti-ulcer medications.

    False

    Which of the following statements is true about 2nd Generation fluoroquinolones?

  • They are only effective against anaerobic bacteria.
  • They have fewer side effects compared to nalidixic acid. (correct)
  • They are less effective against UTIs.
  • They induce high bacterial resistance.

    • Selective chemotherapeutic agents cannot be recommended based on the pathophysiology of diseases.

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

    3rd Generation fluoroquinolones are primarily used for skin infections.

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

    What are the potential side effects of Trovafloxacin?

    <p>Liver toxicity and pancreatitis.</p> Signup and view all the answers

    Name one type of drug that the course covers related to endocrine disorders.

    <p>Steroidal hormones</p> Signup and view all the answers

    2nd Generation fluoroquinolones are known for their broad-spectrum antibacterial activity and reduced ability to induce __________.

    <p>bacterial resistance</p> Signup and view all the answers

    Match the following fluoroquinolones with their primary uses:

    <p>Norfloxacin = UTI and resistant infections Ciprofloxacin = Broad-spectrum antibiotic Sparfloxacin = Lower respiratory infections Trovafloxacin = Life-threatening infections in hospitals</p> Signup and view all the answers

    Which of the following is a biochemical target for anti-infective agents?

    <p>Inhibition of nucleic acid synthesis</p> Signup and view all the answers

    Nitrofuran derivatives are effective for treating urinary tract infections.

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

    What is the role of the nitro group in nitrofuran derivatives?

    <p>The nitro group is essential for the activity of the drug and is involved in the production of reactive oxygen species that damage DNA.</p> Signup and view all the answers

    ___ is a medicinal dye that should be dissolved in alcohol.

    <p>Crystal violet</p> Signup and view all the answers

    Match the following antimicrobial agents to their descriptions:

    <p>Nitrofuran = Used for urinary tract infections Quinolones = Inhibition of nucleic acid synthesis Alcohols = Common disinfectant agents Phenols = Used as antiseptics and disinfectants</p> Signup and view all the answers

    Which of the following compounds is NOT included in the classification of antimicrobial agents?

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

    All antibacterial targets are aimed at inhibiting protein synthesis.

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

    What is the primary use of Nifuroxazide?

    <p>It is used for treating colitis and diarrhea.</p> Signup and view all the answers

    The conversion of pyruvic acid to __________ is blocked by nitrofuran derivatives.

    <p>acetyl CoA</p> Signup and view all the answers

    Which position of the nitrofuran derivative is essential for its activity?

    <p>5-position</p> Signup and view all the answers

    What is the mechanism of action of Quinolones in Gram-negative bacteria?

    <p>Inhibition of DNA gyrase enzyme</p> Signup and view all the answers

    Nalidixic acid is effective against Gram-positive bacteria.

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

    What effect does the fluorine substitution at position 6 have on fluoroquinolones?

    <p>Increases activity</p> Signup and view all the answers

    The introduction of a cyclopropyl substituent at position 1 enhances __________ activity.

    <p>broad-spectrum</p> Signup and view all the answers

    Match each modification of nalidixic acid with its effect:

    <p>Fluoro at position 6 = Increases activity Fluoro at position 8 = Causes phototoxicity Amino at position 5 = Prevents phototoxicity N-piperazine substitution = Prevents CNS side effects</p> Signup and view all the answers

    Which property is improved by piperazine substitution in Quinolones?

    <p>Better pharmacokinetic properties</p> Signup and view all the answers

    Enoxacin is a broad-spectrum antibiotic effective against both Gram-negative and Gram-positive bacteria.

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

    What is the primary application of nalidixic acid?

    <p>Short-term therapy for uncomplicated urinary tract infections</p> Signup and view all the answers

    Resistance to nalidixic acid often develops __________.

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

    Which of the following statements is true regarding the effects of fluorine at position 8?

    <p>It is responsible for phototoxicity</p> Signup and view all the answers

    Which of the following is NOT a type of antimicrobial agent?

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

    Gram-negative bacteria have a thicker cell wall than Gram-positive bacteria.

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

    What is the primary purpose of antibiotics?

    <p>To inhibit the life processes of microorganisms.</p> Signup and view all the answers

    The cell membrane and cell wall of bacteria protect them from ______.

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

    Match the following types of antimicrobial agents with their characteristics:

    <p>Antiseptic = Used on living tissues Disinfectant = Used on non-living surfaces Preservative = Prevents spoilage of food Antibiotic = Inhibits bacterial life processes</p> Signup and view all the answers

    What is the primary classification of antimicrobials according to mechanism of action?

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

    Synthetic antibacterial agents are considered antibiotics.

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

    What are the two main classifications of antimicrobials based on spectrum of activity?

    <p>Broad spectrum and narrow spectrum.</p> Signup and view all the answers

    Gram-positive bacteria typically have a ______ cell wall compared to Gram-negative bacteria.

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

    Which of the following agents is used to prevent microbial spoilage in food?

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

    Study Notes

    Course Information

    • Course Title: Medicinal Chemistry I (PC508)
    • Lecture: 1
    • Topic: Anti-Infective Drug
    • Department: Pharmaceutical Chemistry

    Course Specifications

    • Aims: Covers different classes of antibiotics, antimicrobials (natural and synthetic), chemotherapeutic agents (including antivirals, antifungals, and antiparasitic), anticancer therapies, steroidal hormones and related drugs, endocrine-related drugs (Diabetes, thyroid, calcium regulating agents), antihistamines (H1, H2 blockers), and anti-ulcer PPIs.

    Course Learning Objectives (CLOs)

    • Define principles of physicochemical properties on bioavailability and biological activities of antimicrobial and anticancer drugs.
    • Identify pharmacological properties (mechanisms of action, uses, adverse reactions, and interactions with other agents) of studied agents.
    • Interpret information about tumor cells and their hallmarks in cancer development.
    • Analyze representative drugs from various classes.
    • Apply pharmacopeial methods in detecting the purity of natural and synthetic materials.
    • Utilize synthetic laboratory materials and glassware safely.
    • Select chemotherapeutic and hormonal agents based on etiology and pathophysiology of infections/diseases.
    • Recommend the proper active drug based on its pharmacological properties.
    • Justify drug interactions and adverse effects of different chemotherapeutic classes and hormones.
    • Develop teamwork capabilities.

    Content Outline

    • Introduction
    • Antimicrobial agents (Antibacterial, Antifungal, Antiviral)
    • Anticancer agents
    • Antihistaminic
    • Antidiabetic

    Medicinal Chemistry

    • Multifaceted discipline encompassing synthetic organic chemistry, natural products chemistry, enzymology, chemical biology, structural biology, and computational methods.
    • Aimed at the discovery and development of new therapeutic agents/drugs.

    Bacterial Cell Structure

    • No defined nucleus, no organelles, different biochemistry.
    • Cell membrane and cell wall protect from lysis.
    • Gram-negative bacteria have a thin cell wall and an additional outer membrane made of lipopolysaccharides.

    Antimicrobial Agents

    • Antibiotics: Chemical compounds produced by living microorganisms to defend against other microorganisms by inhibiting their life process.
    • Synthetic antibacterial agents: Fully synthetic compounds that act against bacteria but are not antibiotics.

    Classification of Antimicrobials

    • Based on mechanism of action (inhibiting cell wall, protein synthesis, etc.)
    • Based on spectrum of activity (broad or narrow; Gram-negative, Gram-positive, or both).
    • Based on chemical classification (β-lactams, non-β-lactam antibiotics).

    Bacterial Cell Structure and Antibacterial Agents

    • Diagram showing their interactions.

    Antiseptics, Disinfectants, and Preservatives

    • Antiseptics are for living tissues.
    • Disinfectants are for nonliving objects.
    • Preservatives hinder microbial spoilage.

    Biochemical Targets for Anti-Infective Agents

    • Inhibition of nucleic acid synthesis
    • Inhibition of bacterial cell wall synthesis
    • Alteration of cell membrane permeability/inhibition of active transport
    • Inhibition of protein synthesis

    Classification of Antimicrobials(chemical classes)

    • Alcohols, Phenols, Aldehydes, Acids, Halogen-containing compounds, Oxidizing agents, Mercury compounds, Silver salts, Medicinal dyes, Cationic surfactants, Nitrofuran derivatives, Esters of p-hydroxybenzoic acid (Parabens), Oxazolidinones (linezolid), Nalidixic acid & Quinolones

    Nitrofuran Derivatives

    • Nitro group reduction to hydroxyl amine then to amino group.
    • Production of reactive oxygen species (ROS), leading to DNA and protein destruction.
    • Blocking pyruvic acid to acetyl CoA conversion
    • Energy transfer inhibition.
    • Uses: Urinary tract infections resistant to antibiotics.
    • Structure-activity relationship (SAR) crucial to drug design
    • Synthesis of Nitrofuran derivatives

    Nalidixic acid and Quinolones

    • Mechanism of action (MOA): Inhibition of DNA gyrase (Gram-negative) and topoisomerase IV (Gram-positive).
    • Role in DNA replication.
    • History of Derivatives
    • Applications

    2nd Generation Fluoroquinolones

    • Used for UTI and infections resistant to other antibacterial agents.
    • Advantages over first-generation: Excellent and broad antibacterial activity, fewer side effects, and lower ability to induce bacterial resistance.
    • Examples: Norfloxacin (Noroxin), Ciprofloxacin (Ciprobay)

    3rd Generation Fluoroquinolone

    • Used for lower respiratory infections (bronchitis) and bacterial gastroenteritis.
    • Lower photosensitivity than other di-fluoro derivatives because of amino group counteracting the 8-fluoro substituent.
    • Example: Sparfloxacin

    4th Generation Fluoroquinolone

    • Reports of liver toxicity and pancreatitis, limited use in patients with life-threatening infections.
    • Active against anaerobic bacteria.
    • Example: Trovafloxacin (Trovan)

    Metabolism of Fluoroquinolones

    • 7-methyl group converted into a 7-OH/ 7-COOH alcoholic group.
    • 7-OH group is pharmacologically more active.
    • 7-COOH group is pharmacologically inactive.

    Incompatibilities of Quinolones

    • Chelation of polyvalent metal ions (Ca, Mg, Al, Fe) forms less water-soluble complexes.
    • Contraindicated with antacids, hematinics, tonics, or dairy products.
    • Not given to children less than 18 years old.
    • CYP450 inhibitors.

    Exercises

    • Questions related to topics covered in lecture.

    Arrangement according to phototoxicity.

    • Ranking order of fluoroquinolone drugs based on phototoxicity.

    Oral bioavailability of some Fluoroquinolones

    • Correlation with lipophilicity.

    Studying That Suits You

    Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

    Quiz Team

    Related Documents

    Medicinal Chemistry I Lecture 1 - Anti-Infective Drug PDF

    Description

    This quiz covers essential aspects of pharmacology, including the classification and functions of various drug types, particularly focusing on antihistamines, fluoroquinolones, and anticancer therapies. It also addresses side effects and the relationship between drug properties and bioavailability. Test your understanding of key objectives and concepts from the course.

    More Like This

    Use Quizgecko on...
    Browser
    Open
    Browser
    Browser