Kimia Medisinal

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 NOMOR KODE/SKS : PAF 473 / 3 SKS
(48 x 50 menit)

DESKRIPSI SINGKAT

: Kuliah membahas sifat-sifat fisika dan kimia dari

senyawa-senyawa yang aktif secara biologi, antaraksi
dengan makromolekul dan memberikan efek fisiologi atau
biokimia sehingga dapat digunakan sebagai obat.

TUJUAN INSTRUKSIONAL UMUM

: Memperkenalkan prinsip-prinsip dan meningkatkan

pemahaman konsep-konsep penting berkaitan dengan
hubungan struktur dan aktifitas dan tempat kerja obat.
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 GENERAL OUTLINE

I Introduction
Overview of lecture, quizzes and
examinations, textbook.
Discussion of assumed prerequisites
Review and discussion of important
background principles
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II. Physico-Chemical Principles of Drug Action
Solvation and the structure of water
Solubility
Partition coefficients
Surface activity and drug effects
Streochemical aspects of drug action
Electronic structure and drug action
Chemical bonding and biological activity
Quantum chemical aspects of drug action
Quantitative structure activity relationships (QSAR)

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III. Receptor-Effector Theories

Receptor concept
Nature of receptors
Terminology of pharmacological binding
Classical theories of concentration response
Molecular models of receptor function

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IV. Methods of Receptor Characterization

Principles of the methods

Indirect methods of receptor
characterization
Direct methods of receptor
characterization
Data treatment

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V. Drugs Acting on
Neurotransmitters and Their
Receptors
A. Review of neuroanatomy and
neurophysiology
B. Acetylcholine and the cholinergic receptors
C. Norepinephrine and the adrenergic receptors
D. Dopamin and the dopaminergic receptor
E. Serotonin and the serotonic receptors
F. Histamine and the histaminergic receptors
G. Amino acid neurotrasmitters and related drug
effects
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VI. Drugs Acting as Hormones,
Neurohormones, and on Associated
Receptors

Steroid hormones and receptors

Amino acid hormones and receptors
Peptide and Protein Hormones,
Neurohormones, and Receptors
Enkephalins, Endorphins, Opiates, and
Opiate Analogs
Prostaglandins and Thromboxane

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VII. Non-Messenger Targets for Drug
Action.

A. Exitable Membranes
B. Cell-wall synthesis inhibitors
C. Enzymes as targets for drug action
D. Vitamins and co-enzymes
E. Nucleic acid as targets for drug action

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VIII. Drug Distribution, Metabolism,
and Excretion

A. Drug distribution
B. Drug metabolism
C. Drug Excretion

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IX.
Principles of Drug
Design
A. Analog synthesis vs. rational design
B. Discovery of lead compounds
C. Pharmacophore identification
D. Pro-drugs and soft drugs

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X. Conclusion and Evaluations

A. Concluding remarks
B. Final examination
C. Student evaluations of Course and
Lecturer

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 TEXT BOOK and REFERENCE
MATERIALS

Text for Special Lecture

Thomas Nogrady, Medicinal Chemistry: A Biochemical
Approach, 1988, Oxford University Press
Supplemental Texts
William O. Foye, Editor, Principles of Medicinal
Chemistry, 2nd Edition, 1981, Philadelphia, Lea and
Febiger
C. R. Ganellin and S.M. Roberts Editor. Medicinal
Chemistry, The Role of Organic Chemistry in Drug
Research. Academic Press, London. 1993
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Fig.7.1 Stimulation of the sympathetic nervous system due to f r i g h
t lead to preparation of the system for fight or flight: increase in
heart rate, dilation of bronchi, dilation of pupils, constriction of
peripheral blood vessels (pallor), etc (From B. L.A.T Booklet Action
of Drugs, Centre of health and Medical Education, London).
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