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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 Universitys 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 universitys philosophy of
cultivating the students 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 pharmacists 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
PO7

PO1
PO2

PO5
PO6

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

PO6

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

PO5

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

Page 7 of 10

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 Burrows Solution


1. Prepare Burrows 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 & Wilkins, 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. Foyes Principles of Medicinal Chemistry, 6 ed, Philadelphia: Lippincott Williams & Wilkins, USA, 2008.
th

Gennaro, Alfonso R. Remington: The Science and Practice of Pharmacy. 20 ed. Pennsylvania: Mack Publishing Company. 2000.
th

Svehla, G. Vogels 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

Page 10 of 10

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