CENTRO ESCOLAR UNIVERSITY
SCHOOL OF PHARMACY
Manila * Makati * Malolos
PHARM. CHEM. 1
PRINCIPLES OF MEDICFINAL CHEMISTRY 1
4 units ( 3 lec 1 lab)
Course Number
Course Title
Credit Unit/s
CEU Vision / Mission
Science and Virtue
Vision
CEU is the University of first choice – the leading higher education
institution fostering excellence in the pursuit of knowledge while
engendering personal integrity and social responsibility
Mission
Centro Escolar Expected Graduate Attributes (CEEGA)
Graduates
Attributes
Philosophy
 Enhance the development of higher education in the Philippines
through its exemplar academic programs and practices, leadership
in professional organizations, and participation in academic
consortia; and
 Contribute to the promotion of human health and well-being through
high-quality programs in health professional education, research,
and community service.
CORE VALUES
Reflective and
Creative Thinker




Thinks critically and creatively
Open-minded
Solves problems systematically
Loves art and shows artistic sensibility
Caring and
Trustworthy
Citizen


Values people and acts in unity with others
Commits to social justice and principles of sustainability and respect
for diversity
Practices good stewardship and accountability
Manifests social responsibility by helping improve conditions of
those who have less in life or circumstance


Proficient
Communicator


Articulates ideas clearly for varied purposes and audiences of
diverse culture.
Listens attentively, engages in meaningful exchange and shares
knowledge, values, attitudes and intentions
Utilizes effectively appropriate media and information technologies


Initiates, innovates better ways of doing things
Promotes quality and productivity

A - Accountability, integrity and trustworthiness
L - Lifelong learning as individuals and as an organization
E - Excellence in all endeavors




V - Valuing others, caring for them and empowering them
U - Unity, teamwork and loyalty
Skills, Knowledge, Attitudes that Escolarian Graduates Possess
Learns and works independently as well as collaboratively
Translates knowledge generated from research and other sources
to improve quality of life
Creates new ideas to better understand society
Evaluates own thinking, behavior and spirituality for self-growth
Lifelong Learner
CEU is committed to:
 Provide a rich and stimulating academic environment in order to
promote creative and scholarly academic pursuits among its faculty
and equip students with the knowledge, skills, sound moral values,
and an appreciation of arts and culture that will prepare them to
become productive and innovative professionals with a commitment
to nation building in the context of one world.
Lec: 3 Hrs./Wk
Lab: 3 Hrs./Wk
Hours Per Week
Competent and
Productive
Professional
S - Social responsibility as citizens of the Filipino nation and
of the world
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School Vision / Mission
Vision
To become the top provider of professionally competent pharmacist.
Mission
Guided and inspired by the University’s maxim “ CIENCIA Y VIRTUD” the
School of Pharmacy is committed to provide its students the necessary
knowledge, skills, values and competencies, so they will be professionally
competent, legally qualified, morally upright, population and patient-oriented
and globally competitive pharmacists.
School Objectives
The CEU School of Pharmacy is committed to the pursuance of the university’s philosophy of
cultivating the student’s mind, spirit and body for service of God, country and family. The
school is committed to the development of graduates who:
1.
manifest a sense of national identity, cultural consciousness, moral integrity,
and spiritual vigor;
2.
possess the required knowledge, skills values and competencies in the
practice of pharmacy;
3.
are committed to safeguard the integrity of the pharmacy profession in order
to provide leadership for the nation;
4.
possess the research skill needed to advance knowledge for the improvement
of the quality of life; and
5.
respond effectively to changing societal needs and conditions.
Program Outcomes
The graduates of the Bachelor of Science in Pharmacy program must be able to:
1. Demonstrate a working knowledge of concepts and principles to focus on patientcentered pharmacy practice;
2. Use problem solving skills to prevent or resolve problems within the practice of
Pharmacy;
3. Demonstrate effective interpersonal and communication skills in providing
pharmaceutical care and patient counselling;
4. Design pharmaceutical care services program with the integration of innovative
business/ entrepreneurial strategies;
5. Effectively utilize information and communication technology and demonstrate the
ability to retrieve and analyse data to assist in drug information provision, patient care
and safety;
6. Evaluate scientific papers on research that lead to the development of drugs for
prevention, diagnosis, mitigation and treatment of diseases of man;
7. Practice the profession consistent with ethical, legal, social, economic standards of
the pharmacy profession.
COURSE DESCRIPTION:
The course covers the chemistry and pharmacy of inorganic and organic compounds with emphasis on their properties, identification and confirmatory tests, uses and official preparations in USP
and NF. It also includes the concepts of chemical reactions related to qualitative analysis of inorganic compounds. It also provides an introduction on Medicinal Chemistry covering Drug Discovery
and design, general concept of drug metabolism and an overview of anti-infective agents
Pre-Requisite/s: Chem. 121 (Organic Chemistry)
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LECTURE
Course Objectives:
At the end of the course, the students should be able to:
1. Cognitive :
1.1. Understand the concepts and principles of inorganic and organic chemistry to medicinal and pharmaceutical chemistry.
1.2. Apply these concepts and principles in qualitative methods of analyzing and identifying ions and their compounds.
2. Psychomotor:
2.1. Acquire necessary laboratory techniques and skills in identifying, confirming and preparing inorganic medicinals
2.2. Correlate the physicochemical structure of the drug with drug action, biological activity and restate the different metabolic pathways for drugs.
3. Affective:
3.1. Appreciate the pharmacist’s social and professional responsibilities in helping restore or maintain the health of men and animals, and of the high moral and ethical standards that are
required of the Pharmacy profession.
Course Plan:
Suggested Teaching/
Program
Learning
Time
Assessment
Assessment
Specific Objectives
Course Content
Resources
Outcomes
Methodologies /
Allotment
Tasks
Tools
Strategies
A. INTRODUCTION TO MEDICINAL
At the end of the unit, the student should
Collaborative Learning
6 hrs.
Books
Assignment
Quizzes
CHEMISTRY
PO1
be able to:
Diagram
Unit Test
1. Compare and contrast inorganic from 1. Inorganic chemistry vs. Organic
Discussion
Journals
organic medicinal chemistry.
chemistry
Group
Participation in
2. Restate the early-discovered
2. Origins of medicinal chemistry
Video Presentation
Website
Dynamics
Class
inorganic and organic medicines.
3. Sources of Drugs
Sample of
Written report
3. Describe the sources, classification
4. Classification of Drugs
Drugs
and naming of drugs.
5. Drug Nomenclature
At the end of the unit, the students should B. INTRODUCTION TO INORGANIC
Collaborative Learning
8 hrs.
Books
Diagram
Quizzes
MEDICINAL CHEMISTRY
PO1
be able to:
Seatwork
PO2
1. Describe elements of different groups
Discussion
Journals
Scavenger Hunt
Unit Test
UNIT I: THE PERIODIC TABLE
in the periodic table.
2. Illustrate and justify important
1. Periodic classification of elements
Mnemonics
Websites
Familiarity on
Participation in
chemical reactions.
2. General aspects and group
the Periodic
Class
3. Acquire the skills in identifying ions
properties of each specific class of
Periodic
Trends
and compounds important as an
elements.
Table of
inorganic medicinal agent.
Elements
UNIT II: MAJOR INTRA AND
At the end of the unit, the student should
Collaborative Learning
6 hrs
Books
Assignment
Quizzes
EXTRA-CELLULAR
be able to:
Seatwork
Diagram
ELECTROLYTES
1. Enumerate the ions in intra and extraDiscussion
Journals
Unit Test
cellular fluids.
Group
2. Discuss the functions of these ions in
1. Major physiological ions
Mnemonics
Websites
Dynamics
Participation in
maintaining physiological acid-base
2. Physiological acid-base balance
Class
balance.
3. Electrolytes used for:
3. Identify commercially available
a. Replacement therapy
PRELIM
preparations used for electrolyteb. Acid-base therapy
EXAMINATION
imbalance.
c. Combination therapy
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Program
Outcomes
PO1
PO2
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PO2
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Specific Objectives
At the end of the unit, the student should
be able to:
1. Restate the definition of
gastrointestinal agents, acidifying
agents, antacids, protectives,
adsorbents and saline cathartics.
2. Illustrate the mechanism of action of
gastrointestinal agents.
3. Justify the importance of
gastrointestinal agents as remedies
for GIT disorders.
Classify commercially available
products in the market
At the end of the unit, the student should
be able to:
1. Relay the definition of topical agents,
protective agents, antimicrobials and
astringents.
2. Categorize commercially available
preparations according to types of topical
agents.
At the end of the unit, the student should
be able to:
1. Illustrate and discuss the stages in
drug discovery, drug design and drug
development.
2. Discuss what are lead compound and
give examples.
Restate the principles of drug
discovery and present a timeline how
a drug was discovered.
Course Content
UNIT III: GASTROINTESTINAL
AGENTS
1.
2.
3.
4.
Acidifying agents
Antacids
Protectives and Adsorbents
Saline Cathartics
UNIT IV: TOPICAL AGENTS
1. Protective Agents
2. Antimicrobials
3. Astringents
Suggested Teaching/
Learning
Methodologies /
Strategies
Collaborative Learning
Time
Allotment
Resources
6 hrs.
Books
Assignment
Quizzes
Discussion
Journals
Diagram
Seatwork
Case Analysis
Clinical
Cases
available
online
Sample of GI
Drugs
Unit Test
Case and
Written Report
Participation in
Class
Books
Assignment
Quizzes
Discussion
Journals
Diagram
Unit Test
Mnemonics
Clinical
Cases
available
online
Written report
Participation in
Class
Collaborative Learning
UNIT I: PRINCIPLES OF DRUG
DISCOVERY
1. Drug discovery – finding a lead
compound
2. Drug design
3. Drug development
Assessment
Tools
4 hrs.
Case Analysis
INTRODUCTION TO ORGANIC
MEDICINAL CHEMISTRY
Assessment
Tasks
Presentation of
a topical
formulation
Books
Group
Dynamics
Assignment
Quizzes
Discussion
Journals
Diagram
Unit Test
Video Presentation
Interactive
web
exercises
available
online
Group
Dynamics
Participation in
Class
Collaborative Learning
4 hrs.
Role Play
(portraying
different
significant
events in drug
discovery)
Written report
MIDTERM
EXAMINATION
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Program
Outcomes
PO1
Specific Objectives
Course Content
At the end of the unit, the student should
be able to:
UNIT II: DRUG-RECEPTOR
INTERACTION
1. Enumerate and classify the
pharmacological receptors and its
importance.
1. Physico-chemical properties of drugs
2. Discuss important physico-chemical
properties and structural features of
drugs and relate it to drug action and
biological response.
3. Intermolecular Forces of attraction
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Discussion
Journals
Unit Test
Mnemonics
Interactive
web
exercises
available
online
Play
(Portraying
different types
of bond)
8 hrs.
Collaborative Learning
1. Identify the type of reactions a certain
drug would undergo.
1. Review of organic reactions
Demonstration on the
metabolic fate of the
drug
3. General pathways of drug
metabolism
4. Factors affecting drug metabolism
Quizzes
Journals
Group
Dynamics
Unit Test
Books
Assignment
1. Terminologies
Discussion
4. Retell mechanism of action and
therapeutic application of antiinfectives and anti-malarials
Assignment
Audio – Visual
Presentation
1. Locate the different functional groups
present in the drug molecule relevant
to its biologic activity.
3. Rationalize Structural Activity
Relationship
Books
Sample cases
and Drug
interactions
Collaborative Learning
5. Properties
6. Mechanism of action and therapeutic
application
Participation in
Class
Quizzes
6 hrs.
Journals
2. Chemical Classification
4. Preparation and synthesis
Written report
Interactive
web
exercises
available
online
UNIT IV: ANTI-INFECTIVE AGENTS &
ANTIMALARIALS
2. Classify organic medicinals and their
uses based on their structures.
Participation in
Class
8 hrs.
At the end of the unit, the student should
be able to:
3. Structural-activity relationship (SAR)
Assessment
Tools
Quizzes
Demonstration of
intermolecular forces of
attraction
2. Sites of drug biotransformation
Assessment
Tasks
Assignment
4. Structure activity relationship
5. Metabolic pathways of common
drugs
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Resources
Books
UNIT III: CHEMICAL ASPECTS OF
DRUG METABOLISM
3. Identify the functional groups in drug
molecule.
PO1
Collaborative Learning
At the end of the unit, the student should
be able to:
2. Predict the product of drug
biotransformation.
Time
Allotment
2. Structural features of drugs/
stereochemistry
3. Predict the type of forces of drugreceptor interactions.
PO1
Suggested Teaching/
Learning
Methodologies /
Strategies
Audio – Visual
Presentation (mode of
action)
Interactive
web
exercises
available
online
Unit Test
Group
Dynamics
Participation in
Class
SAR Analysis
FINAL
EXAMINATION
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LABORATORY
Program
Outcomes
PO1
PO2
Specific Objectives
At the end of the exercise, the student
should be able to:
1. Separate the cations systematically
into five (5) groups by solubility or
reactivity.
2. Identify and confirm the cations of
each group by using confirmatory
reagents.
Course Content
EXERCISE NO. 1
Separation of Cations into Analytical
Groups
Suggested Teaching/
Learning
Methodologies /
Strategies
Pre-lab and post-lab
discussion
Time
Allotment
9 hrs.
Give
examples
on
common
chemical
reactions
Discussion on general
guidelines
and
behavior
inside
laboratory room
Resources
Reagents
containing
cations
At the end of the exercise, the student
should be able to:
1. Describe
and
distinguish
the
reactions and solubilities of different
anions
EXERCISE NO. 2
Comparative reactions of the anions with
silver nitrate and barium chloride
Pre-lab and post-lab
discussion
Common
chemical
reaction
Glass wares
Correct
schematic
diagram on
pp. 20 and 21
Apparatus
9 hrs.
Rationalize the reaction
behind the experiment
Reagents
containing
anions
Confirmator
y reagents
Apparatus
Glass wares
Manual
PO1
PO2
At the end of the exercise, the student
should be able to:
EXERCISE NO. 3
Pre-lab and post-lab
discussion
Identification Tests of the Anions
1.
Conduct and perform identification
tests for each anion
Rationalize the reaction
behind the experiment
6 hrs.
Identify the
group
precipitating
reagent
Confirmator
y reagents
Manual
PO1
PO2
Assessment
Tasks
Reagents
containing
anions
Confirmator
y reagents
Submission of
completed
worksheet
Identify the
group
precipitating
reagent
Apparatus
Practical
examination
Quiz
Worksheet
Skills using
rubrics
Identify the
unknown cation
Practical
examination
Quiz
Common
chemical
reaction
Worksheet
Submission of
completed
worksheet
Identify
confirmatory
reagents
Identify the
unknown anion
Common
chemical
reaction
Worksheet
Submission of
completed
worksheet
Identify the
unknown anion
Manual
Glass wares
Assessment
Tools
Skills using
rubrics
Practical
examination
Quiz
Skills using
rubrics
PERIODIC
EXAMINATION
Page 6 of 10
Program
Outcomes
Specific Objectives
PO1
At the end of the exercise, the student
should be able to:
Course Content
EXERCISE NO. 4
Suggested Teaching/
Learning
Methodologies /
Strategies
Pre-lab and post-lab
discussion
Time
Allotment
3 hrs.
PO1
At the end of the exercise, the student
should be able to:
Pre-lab and post-lab
discussion
Preparation of Ferrous Sulfate Syrup
1. Prepare Ferrous sulfate syrup
2. Conduct identification tests for the
solution prepared
PO1
At the end of the exercise, the student
should be able to:
Pre-lab and post-lab
discussion
Skills using
rubrics
Write the
chemical
reactions
involved
Quiz
Manual
Submission
of completed
worksheet
Skills using
rubrics
Reagents
Product
Preparation
Practical
examination
Write the
chemical
reactions
involved
Quiz
Submission
of completed
worksheet
Product
Preparation
Skills using
rubrics
Write the
chemical
reactions
involved
Quiz
Submission
of completed
worksheet
Skills using
rubrics
Reagents
3 hrs.
Glass wares
Rationalize the reaction
behind the experiment
Apparatus
Manual
EXERCISE NO. 7
Pre-lab and post-lab
discussion
Preparation of Magnesium Hydroxide
1. Prepare magnesium hydroxide using
magnesium oxide and water and
2. Conduct identification tests for the
solution prepared
Submission
of completed
worksheet
Product
Preparation
Apparatus
1. Prepare Ammonium bromide from
potassium bromide and ammonium
sulfate and
2. Conduct identification tests for the
solution prepared
At the end of the exercise, the student
should be able to:
Quiz
Glass wares
Preparation of Ammonium Bromide
PO1
Write the
chemical
reactions
involved
Rationalize the reaction
behind the experiment
EXERCISE NO. 6
3 hrs.
Assessment
Tools
Practical
examination
Manual
3 hrs.
Assessment
Tasks
Product
Preparation
Apparatus
Rationalize the reaction
behind the experiment
EXERCISE NO. 5
Reagents
Glass wares
Preparation of Strong Iodine Solution
1. Prepare strong iodine solution by
simple solution process and
2. Conduct identification tests for the
solution prepared
Resources
Reagents
Glass wares
Rationalize the reaction
behind the experiment
Apparatus
Manual
Worksheet
Practical
examination
Worksheet
Worksheet
Practical
examination
Worksheet
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Program
Outcomes
PO1
Specific Objectives
At the end of the exercise, the student
should be able to:
Course Content
EXERCISE NO. 8
Suggested Teaching/
Learning
Methodologies /
Strategies
Pre-lab and post-lab
discussion
Time
Allotment
3 hrs.
Preparation of Plaster of Paris
1. Prepare Plaster of Paris and
2. Conduct identification tests for the
mixture prepared
Resources
Reagents
Glass
wares
Rationalize the reaction
behind the experiment
Apparatus
Manual
PO1
At the end of the exercise, the student
should be able to:
1. Prepare oral rehydration solution
2. Know the importance and indication of
oral rehydration therapy
3. Determine the ions present in the
preparation
EXERCISE NO. 9
Preparation of Oral Rehydration Salt
Solution
Pre-lab and post-lab
discussion
3 hrs.
Reagents
Glass
wares
Rationalize the reaction
behind the experiment
Apparatus
Manual
Assessment
Tasks
Product
Preparation
State the
chemical
reaction
during
chemical
testing
Assessment
Tools
Practical
examination
Quiz
Worksheet
Skills using
rubrics
Product
Preparation
Practical
examination
State the
chemical
reaction
during
chemical
testing
Quiz
Worksheet
Skills using
rubrics
Submission
of completed
worksheet
PO1
At the end of the exercise, the student
should be able to:
EXERCISE NO. 10
Pre-lab and post-lab
discussion
Preparation of Burrow’s Solution
1. Prepare Burrow’s solution using glacial
acetic acid, aluminum subacetate
solution and purified water and
2. Conduct identification tests for the
mixture prepared
Rationalize the reaction
behind the experiment
3 hrs.
Reagents
Glass
wares
Apparatus
Manual
Product
Preparation
State the
chemical
reaction
during
chemical
testing
Practical
examination
Quiz
Worksheet
Skills using
rubrics
Submission
of completed
worksheet
Page 8 of 10
Program
Outcomes
PO1
PO2
Specific Objectives
At the end of the exercise, the student
should be able to:
1. Familiarize and identify the different
ions present in some commercially
available preparations and
2. Conduct identification tests for the
mixture prepared
Course Content
EXERCISE NO. 11
Suggested Teaching/
Learning
Methodologies /
Strategies
Pre-lab and post-lab
discussion
Analysis of the ions found in preparations
containing Inorganic Medicinal
Substances
Time
Allotment
9 hrs.
Rationalize the reaction
behind the experiment
Resources
Reagents
Glass
wares
Apparatus
Manual
Assessment
Tasks
Product
Preparation
Assessment
Tools
Practical
examination
Quiz
State the
chemical
reaction
during
chemical
testing
Worksheet
Skills using
rubrics
Grading Scheme:
Cut off: 70%
Class Participation: recitation, unit tests, quizzes, projects, reports, assignments, etc.) weight of 2.00
Comprehensive / Summative Examination (first, second and third) – weight of 1.00
Books:
Textbook
th
Block, John H. and Beale, Jr., John M., Organic Medicinal and Pharmaceutical Chemistry, 12 ed. Philadelphia: Lippincott Williams & Wilkin’s, 2011.
Manual
Limuaco, Olivia M. et al. Laboratory Exercises in Chemistry and Pharmacy of Medicinals 1, School of Pharmacy Centro Escolar University, 2011.
References:
th
Lemke, Thomas L. et al. Foye’s Principles of Medicinal Chemistry, 6 ed, Philadelphia: Lippincott Williams & Wilkin’s, USA, 2008.
th
Gennaro, Alfonso R. Remington: The Science and Practice of Pharmacy. 20 ed. Pennsylvania: Mack Publishing Company. 2000.
th
Svehla, G. Vogel’s Qualitative Inorganic Analysis. 7 ed. England: Longman Group Limited. 1996.
nd
Cairns, Donald. Essentials of Pharmaceutical Chemistry. 2 ed. London: Pharmaceutical Press. 2003.
rd
Patrick. Graham L. An Introduction to Medicinal Chemistry. 3 ed. New York: Oxford University Press Inc.2005.
Lednicer, Daniel. Strategies for Organic Drug Synthesis and Design. New York. 1998.
rd
Krogssgaard-Larsen, Povl, et al. Textbook of Drug Design and Discovery. 3 ed. London: Taylor and Francis. 2002.
Page 9 of 10
th
McMurry, John, Organic Chemistry, 7 ed. USA: Thomson Brooks/Cole. 2008.
Holtsclaw, Henry F., William R. Robinson, Jerome D. Odom. General Chemistry with Qualitative Analysis. Lexington, Massachusetts: D. C. Heath 2001
Taylor, John B. Modern Medicinal Chemistry, New York: Ellis Horwood, 1993.
United States Pharmacopoeia Convention, Inc. The United States Pharmacopoeia XXVII and the National Formulary XXII. Rockville, MD: USP Convention Inc., 2003.
th
Whitten, Kenneth W., Raymond E. Davis, M. Larry Peck, General Chemistry with Qualitative Analysis. 5 edition. Saunders College Publishing, 1996.
Electronic References:
Drug Discovery and Development: Understanding the R & D Process www.innovation.org, February 2007.
Baille, Thomas A., MacCoss, Malcolm, Organic Chemistry in Drug Discovery www.sciencemag.org March 2004.
Molegro, ApS., Introduction to Drug Discovery, www.molegro.com, 2005
www.photobucket.com
www.cellbiologyolm.stevegalik.org/node/74
www.hotoshelter.com
www.sciencephoto.com
www.tutorbene.com
www.webmineral.com
http://kohyizhescienceeportfolio.wordpress.com
http://www.dartmouth.edu
http://whqlibdoc.who.int/hq/2006/WHO_FCH_CAH_06.1.pdf
Oral Rehydration Salts: Production of the New ORS [page 3]
World Health Organization 2006
Printed by the WHO Document Production Services, Geneva, Switzerland
Prepared by:
ROSA DS. IBARRA, MS Pharmacy
PENUEL P. DAVID, MS Pharmacy, Pursuing Ph. D Pharmacy
RACQUEL C. CRUZ, MS Pharmacy, Pursuing Ph. D Pharmacy
LEELAND ANTHONY L. DELA LUNA, Pursuing MS Pharmacy
JAN DOMINIQUE R. LAPIG, Pursuing MS Pharmacy
ANJELLIE T. MANANSALA, Pursuing MS Pharmacy
THEA RUTH FRANCES GONZALES, Pursuing Master in Education Management
RICARDO ARELLANO, JR. , Pursuing MS Pharmacy
Date:
Approved by:
APRIL 28, 2015
DR. CECILIA D. SANTIAGO
DEAN, SCHOOL OF PHARMACY
Date:
APRIL 28, 2015
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