alpha-dendrotoxin

CHM 357a - TOPICS IN BIOCHEMISTRY:

PHARMACOLOGY

Syllabus
Fall 2007
Last Modified 9 Sept 2007

A. Theory and Practice of Pharmacology - Designing the Magic Bullet

  1. Drug Uptake
  2. Distribution and Partition
  3. Metabolism and Modification
    1. Utilization
    2. Inactivation, Elimination and Excretion
      1. Phase I: Modification - General Classes/Unique Pathways
      2. Phase II: Conjugation - GeneralClasses/Unique Pathways
  4. Duration (Pharmacokinetics)
    1. Kinetics and kinetic order
    2. Induction and Inhibition: Synergistic and Antagonistic Effects
  5. Mode of Action
    1. Enzyme Inhibitors, Activators and Allosteric Effectors
    2. Receptor Agonists and Antagonists
    3. DNA Binding/Modification
    4. Membrane Permeability
    5. Morphological Effectors

B. Example Systems
  1. Neuropharmacology
    1. Drugs Affecting the Peripheral Nervous ystem
    2. Drugs Affecting the Central Nervous System
    3. Drug Use and Abuse; Addiction, Recreation and Regulation
  2. Drugs Affecting Hormonal Systems
    1. Steroids and Adrenocorticoids
    2. Epinephrine, Histamine and Insulin
    3. Other
  3. Chemotherapeutic Drugs
    1. Antibiotics
    2. Immune-suppressive and Immune-activating drugs
    3. Antineoplastic agents

C. Drug Design (The Search for the Magic Bullet)
  1. Regulatory Approval
  2. Traditional Screening
    1. Screening compounds: (Try the pink stuff);
    2. Screening applications: (The pink stuff has to cure something.)
  3. Quantitative Structural/Activity Relationships(QSAR)
    1. Assumptions
    2. QSAR Techniques
      1. Topliss Tree
      2. Linear Regression
      3. Simplex
    3. Failings
  4. Rational Drug Design
  5. Computer-Aided Drug Design
  6. Irrational Drug Design

    7. Course Objectives - The objectives are to understand the principles of pharmacology, toxicology and drug design. The background required for this includes organic chemistry, cell biology, animal physiology and biochemistry. If you haven't had all of these subjects, don't despair! Although we will use information and concepts from all of these disciplines, occasional referral to appropriate texts on these subjects will probably be necessary for all of us. However, you should know the general structures and composition of common cellular components, including membranes, proteins and polynucleotides, and the general structures and properties of their component compounds (amino acids, carbohydrates, nucleic acids, and phospholipids). You also should know the names and structures of common chemical groups, such as amines, carboxylic acids, amides, ketones, nitriles and hydroxyls, and common reactions like hydrolyses, esterifications, oxidations and reductions. If you don't feel comfortable with these terms I strongly recommend that you study the appropriate cell physiology, biochemistry and/or organic chemistry text.
    Readings - The text for the course is "Smith and Williams' Introduction to the Principles of Drug Design and Action, 3rd Ed.," H.J. Smith ed., Harwood Acad. Publ. (1998). Introductory readings will be also provided, and there will be other readings from articles or other outside material.  Each week new readings will be available as links from this page or on reserve in the science library.  Reading this material is required. There are other good introductory texts available, including  "Basic and Clinical Pharmacology, 9th Edition",  B. Katzung, Lange Med. Books/McGraw Hill Press (2004).
    Classes - Classes will be in Bass 204, from 7:00 to 10:00 pm on Wednesday (and other times as necessary.)  Attendance is expected but is not mandatory.
    Oral presentation - A presentation (~30 minutes) of a particular topic (pharmacology of a particular compound, drug interaction, epidemiological program, metabolic path, etc.) that interests you. Three weeks before your presentation you should discuss your topic with me. Two weeks before your presentation you should give me links to, or electronic copies of, 2-3 articles, with at least one being a review or an article having a particularly good description of your topic. At least one week before your presentation I will make the articles available as links from this site. (30pts)
    Participation - Participation is good stuff. (15pts)
    Tests - There will be two take-home tests, covering the readings and class presentations. (30pts)
    Drug Design - Using software for chemical and enzyme modeling, you will identify a promising site for drug binding on a particular enzyme (my choice). You will then design a compound to bind to that site and estimate its affinity for the site by modeling its binding. Finally, you will submit a short report, indicating why you chose the binding site you proposed, and the factors you considered for the drug you designed. Evaluation will be based on your description of the factors you considered in chosing the drug binding site and of the methods used in designing and testing your proposed drug (25pts).

    Appointments - My office is Sabin-Reed 331
    email: dbickar@email.smith.edu
    tel: 585-3837 (I do Phone-Mail poorly.)
    office hours; Mon. 1:00 - 2:30 and Tues. 10:30 - 11:50
    or by appointment.

    Presentation Schedule
    Date Presentations Additional Readings, Deadlines
    Sept. 12 (me)  
    Sept. 19 (me) Ch 1.1 - 1.3
    Sept. 26 Kate Whitesell
    		Chiral, CEChiral, Sepracor Ch 1.4 - 1.6 Ppt
    Oct. 3
    		Elizabeth Liao
    		Angiogenesis, Angio Ang, An, A, Ch 2 Ppt,
    Oct. 10 me
    		"Smart Drugs"  Test
    Oct 17 Sarah Wardlaw
    		Opi, Opio, Opioid Ch 11 Ppt
    Oct. 24 me
    		 antibio cipro antimic Ch 11
    Oct. 31 me
    		 Ch 5
    Nov. 7 Mary Rose Stevens

    PEG Link, PEG-Pic, PEG, Ch 5 Ppt

    Nov. 14 Kashfi Qadri
    		BB1, BB2, BB3, BB4, Ppt
    Nov. 21 THANKSGIVING

    THANKSGIVING
    Nov. 28 Jillian Flynn
    		rit ADHD MP (Test due) Menace of Everyday Life
    Dec. 5
    		Aileen Novero
    Dec 12 Jen Tyson
    		 Arsenic Old Lace FDA Required Testing
    New Drug


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