INTRODUCTION TO

PHARMACOLOGY
«PHR339»
Asst. Prof. Dr. Tambay Taşkın
2023-24 Fall Semester
INTRODUCTION
AND GENERAL
DEFINITIONS
INTRODUCTION
AND GENERAL
DEFINITIONS
In this section, the meaning
of pharmacology, its
definition, basic concepts
and how it emerged as a
science will be given in
detail.
SYLLABUS
I. Basic principles V. Drug Biotransformation
II. Introduction
VI. Pharmacogenomics
III. Drug Receptors &
Pharmacodynamics VII.Toxicology
IV. Pharmacokinetics &
Pharmacodynamics VIII.Special Topics
1. Actions of the body on the
drug
2. The Actions of a drug on the
body
LEARNING
OBJECTIVES OF THIS
COURSE
 Pharmacology
 Definitions what is
Drug
 Historic Perspectives
 Early Written Records
 Pharmacology as a
Seperate Scientific
Discipline
LEARNING
OBJECTIVES OF THIS
COURSE
 Major Milestones in
Drug Discovery
PHARMACOLOGY
AND ITS MEANING
Pharmacon = drug or active
ingredient of drugs
Logos = information
Combining the two terms
Pharmacon+Logos=
«Drug information»
WHAT IS DRUG?
Medicines are chemical, herbal,
biological substances or combinations
thereof used in the diagnosis, treatment
and prevention of diseases.
Substances that can act at the chemical
(molecular) level in living systems.
Drugs affect physiological functions in
a unique way.
PHARMACOLOGY
 It is the science that studies
the interaction of various
chemical, herbal or biological
substances (drugs or other)
with living systems
PHARMACOLOGY
 Examines the effects of drugs
on the biologic systems
«Pharmacodynamics»
 And also the actions of
biologic systems on the drugs
«Pharmacokinetics»
PHARMACOLOGY
…is a science that acts as a bridge
between biology and medicinal therapy!
HISTORY
In ancient times, the only
remedy for humanity in the
fight against diseases was
plants found in nature...
The word "DRUG" is taken
from the French word
‘Drogue’, which means
Dried Herb
HISTORY
The Ebers Papyrus, also known as Papyrus
Ebers, is an Egyptian medical papyrus of
herbal knowledge dating to c. 1550
Among the oldest and most important
medical papyri of Ancient Egypt, it was
purchased at Luxor in the winter of 1873–
1874 by the German Egyptologist Georg
Ebers.
It is currently kept at the Leipzig University
Library in Germany..
CHINESE
MATERIA
MEDICA
Chinese Materia Medica
(1100 B.C.) (Wu Shi Er Bing
Fang, contains 52
prescriptions)
Shennong Herbal (~100
B.C., 365 drugs) and Tang
Herbal (659 A.D., 850
drugs) are records of
natural remedies
SUMERİANS
AND EGYPTIANS
Sumerian and Egyptian
records contain records of
opium and other medicinal
plants.
ANCIENT GREEK
It has become widespread that nature is the
best healer rather than superstitions.
Hippocrates books:
Chest diseases: Take barley soup, vinegar
and honey to remove phlegm.
M.S. In the 1st century, Dioscorides
collected the known drugs in a book and
prepared the first pharmacopoeia (Materia
Medica).
AL BIRUNI
Biruni wrote a pharmacopoeia, the
"Kitab al-saydala fi al-tibb" (Book on
the Pharmacopoeia of Medicine).
It lists synonyms for drug names in
Syriac, Persian, Greek, Baluchi, Afghan,
Kurdi, and some Indian languages
He used a hydrostatic balance to
determine the density and purity of
metals and precious stones
MEDICAL RECORDS
The first Western pharmacological treatise, a listing of herbal
plants used in classical medicine, was made in the 1st century AD
by the Greek physician Dioscorides.
The medical discipline of pharmacology derives from the medieval
apothecaries, who both prepared and prescribed drugs.
THE DEVELOPMENT OF
PHARMACOLOGY AS A SEPARATE
SCIENTIFIC DISCIPLINE
Pharmacology was firmly established in the later 19th
century by the German Oswald Schmeiderberg (1838–
1921).
He defined its purpose, wrote a textbook of pharmacology,
helped to found the first pharmacological journal, and,
most importantly, headed a school at Strasbourg that
became the nucleus from which independent departments
of pharmacology were established in universities
throughout the world.
TRENDS TOWARD
PHARMACOLOGY
Trend towards pharmacology
originates from clinical urgencies
Physicians have been successful in
clinical diagnosis but was inadequate
in the treatment of diseases
«Syphilis» in last century is an
example
As a result, the need to increase
treatment success has fueled the
inclination towards pharmacology
PHARMACOTHERAPY

Microorganism causing
syphilis affected the
European population for
centuries
Physicians have not found a
cure for it for centuries.
IF IT WAS FOUND
140 YEARS AGO!
We might not have seen this
painting of Van Gogh!
NO CURE UNTIL 20TH CENTURY

Syphilis swept across Europe in short order.

By the end of 1495, it had reached France, Switzerland, and
Germany.
By 1497, it took hold in England and Scotland.
By 1500, the epidemic had Scandinavia, Hungary, Greece, Poland,
and Russia in its grip.
SYPHYLIS
During the 1400s and 1500s, European explorers sailed the globe.
These explorers brought syphilis with them to India, Africa, the
Near East, China, Japan, and the Pacific islands.
TREATMENT OF SYPHILISIS- NEO
SALVARSAN
1909 Paul Ehrlich «German Scientist»
HUG THE SNAKE!
RATHER THAN FALLING INTO SEA!
Arsenic - the "poison of kings" and the "saviour of syphilis
Neurotoxic
Hepatotoxic
MAJOR MILESTONES IN DRUG
DISCOVERY
The smallpox vaccine was the first contagious disease vaccine. In 1796,
a British doctor, Edward Jenner
In the early 1800s, morphine was isolated from opium by a German
pharmacist’s assistant, Friedrich Wilhelm Adam Serturner.
The compound diethyl ether was first synthesized by a Prussian
botanist, Valerius Cordus.
Before its breakthrough discovery as an anesthetic in 1846, surgical
operations occurred with little to no pain relief
MAJOR MILESTONES IN DRUG
DISCOVERY
In 1897, Aspirin was first derived from acetylsalicylic acid by a
German chemist at Friedrich Bayer and Co., Felix Hoffman, to
alleviate his father’s rheumatism after reading the medical
benefits of salicin reported in The Lancet.
PHARMACOLOGICAL
ACHIEVEMENTS
Wide use of Neosalvarsan led to a decline of syphilis as a public health
problem by the 1920s, and syphilis continued to decline as effective
sulfa drugs replaced arsenicals in the 1930s and antibiotics such as
penicillin when they became available in the 1940s.o decline as
effective sulfa drugs replaced arsenicals in the 1930s and antibiotics
such as penicillin when they became available in the 1940s.
NEW DISCOVERIES
In the 20th century, and particularly in the years since World War
II, pharmacological research has developed a vast array of new
drugs, including antibiotics, such as penicillin, and many
hormonal drugs, such as insulin and cortisone.
SULPHONAMIDES
In early 1931 Gerhard Domagk immediately tested the compound
in mice that were having bacterial infection, and found that it was
effective against Gram-positive bacteria
He designated a code for the compound D 4145 (D for Domagk)
He induced infection at the belly (peritonitis) of mice using
clinical specimens (isolates) of Streptococcus pyogenes.
PRONTOSIL – FIRST SULPHA
DRUG
In the first experiment, he infected 26 mice by injecting the
bacteria, and he injected a single dose of Prontosil to 12 of the
infected mice, while the rest 14 were simply kept infected (as
controls) without Prontosil treatment.
All the Prontosil-injected mice survived, meaning they were cured
of the streptococcal infection, whereas the untreated 14 mice all
died by the fourth day of experiment.
PRONTOSIL – FIRST
SULPHA DRUG
There were several more experimental tests, and
a clinical trial in which a boy was cured of
streptococcal infection in 1933.
In February 1935, Domagk reported his
experiments in the journal Deutsche
Medizinische Wochenschrift as "Ein Beitrag zur
Chemotherapie der bakteriellen Infektionen" ("A
contribution to the chemotherapy of bacterial
infections").
MAJOR MILESTONES IN DRUG
DISCOVERY
In 1921, a Canadian surgeon named Frederick Grant Banting and his
assistant Charles Best discovered a method of removing insulin from a
dog’s pancreas.
The recovered insulin showed an important proof of concept by keeping
another dog with severe diabetes alive for 70 days only after running
out of insulin.
While the first genetically engineered synthetic “human” insulin was
produced by E. coli in 1978, Eli Lilly and Company became the first to
offer the commercially available name-brand biosynthetic human
insulin, Humulin, in 1982.
MAJOR MILESTONES IN DRUG
DISCOVERY
In the 1940s, two Yale pharmacologists, Alfred Gilman and Louis
Goodman, researched the effects of mustard agents on lymphoma
and found that they significantly reduced tumor masses for a few
weeks after treatment.
Unfortunately, while mustard gas has been proven to kill
cancerous cells in various studies, it also substantially damages
healthy ones.
PENICILLIN
Penicillin: An accidental
discovery changed the course
of medicine
Sir Alexander Fleming, a
Scottish researcher, is credited
with the discovery of penicillin
in 1928.
PENICILLIN
Often described as a careless lab
technician, Fleming returned from a
two-week vacation to find that a mold
had developed on an accidentally
contaminated staphylococcus culture
plate.
Upon examination of the mold, he
noticed that the culture prevented the
growth of staphylococci.
PENICILLIN

A mold, later identified as Penicillium

notatum (now classified as P.
chrysogenum), had inhibited the growth of
the bacteria.
He at first called the substance “mould
juice” and then “penicillin,” after the mold
that produced it.
DEVELOPMENT OF DRUGS
Pharmacology is presently involved in the development of more
effective versions of these and a vast array of other drugs through
chemical synthesis in the laboratory.
Pharmacology also seeks more efficient and effective ways of
administering drugs through clinical research on large numbers of
patients.
STRUCTURE AND ACTIVITY
During the early 20th century, pharmacologists became aware
that a relation exists between the chemical structure of a
compound and the effects it produces in the body.
Since that time, increasing emphasis has been placed on this
aspect of pharmacology, and studies routinely describe the
changes in drug action resulting from small changes in the
chemical structure of the drug.
DRUG DEVELOPMENT
Important basic pharmacological research is carried out in the
research laboratories of pharmaceutical and chemical companies.
After 1930 this area of pharmacological research underwent a vast
and rapid expansion in the world
ANIMAL EXPERIMENTS ARE MANDATORY FOR THE
DEVELOPMENT OF NEW DRUGS

The work of pharmacologists in industry deals also with the

exhaustive tests that must be made before promising
new drugs can be introduced into medical use.
Detailed observations of a drug’s effects on all systems and organs
of laboratory animals are necessary before the physician can
accurately predict both the effects of the drug on patients and
their potential toxicity to humans in general.
THALIDOMIDE DISASTER
1959
THALIDOMIDE DISASTER
Shows the lack of proper animal toxicity tests
In the late 1950s and early 1960s, the use of thalidomide in 46
countries by women who were pregnant or who subsequently
became pregnant resulted in the "biggest man-made medical
disaster ever," with more than 10,000 children born with a range
of severe deformities, such as phocomelia, as well as thousands of
miscarriages.
TESTING OF DRUGS
The pharmacologist does not himself test the effects of drugs in
patients; this is done only after exhaustive tests on animals and is
usually conducted by physicians to determine the clinical
effectiveness of new drugs.
Constant testing is also required for the routine control and
standardization of drug products and their potency and purity.
FOUNDATION OF
PHARMACOLOGY
IN TURKEY
Ord. Prof. Dr. Paul Pulewka is the
pioneer of pharmacology and
pharmacodynamic control in our
country
He completed his medical
education in Munich and earned
a doctorate degree in both
pharmacology and toxicology.
PHARMACOLOGY IN TURKEY
He had to leave Germany because his wife was Jewish.
The Pulewkas took the train to Turkey in October 1935.
He first established Pharmacology Laboratories at the
Ministry of Health Central Institute of Hygiene (established
in 1928) in Ankara.
PHARMACOLOGISTS OF ANKARA
REFIK SAYDAM
Prof. Dr. Şükrü
Kaymakçalan
Prof. Dr. Orhan Altınkurt
Prof. Dr. Firuz Baykal
DIVISION OF
PHARMACOLOGY
 Pharmacodynamics
 pharmacokinetics
 Clinical Pharmacology
 Pharmacotherapy
 Toxicology
 biopharmaceutical
PHARMACODYNAMICS
Examines what drugs do to our
body or organs
CARDIAC FAILURE
This disease occurs
after the heart muscles
cannot contract
adequately for various
reasons.
PHARMACODYNAMICS

Studying cardiotonic drugs

directly on the heart is a
subject matter of
pharmacodynamics….
It is a good example of what
drugs do in the body
ÖZGÜNLÜK
IN VITRO ILEUM AND
ACETHYLCHOLINE… 1 milyon litrelik su tankı

Let's weigh 111 g of

acetylcholine into this 1
million liter tank and throw it
(10-6 mol/L)
pipette 400 µl and add to the
isolated organ bath shown in
the movie
There will be a powerfull
smooth muscle contraction
SPECIFICITY
Biology has to be specific
If it had been needed 10,000 times
more acetylcholine to contract the
same ileum
We needed to consume 10 thousand
times more energy
In other words, it can be explained by
the availability of specific substances
in biologic systems binding with tiny
amounts to their specific receptors
leading to an amplified response.
Less energy, lots of work!
SELECTIVITY
It is essential that drugs be selective
BACTERIA HAS A CELL WALL… HUMAN CELLS
HAVE NONE
For example, penicillin kills bacteria but cannot have
any effects on human cells
Penicillin prevents the formation of thick cell wall…
As soon as the bacterium loses the thick cell wall
that protects it against its own high osmotic
pressure, it explodes and vanishes suddenly.
Human cells do not need a protective cell wall since
their osmotic pressure is less than that of bacteria
Penicillin destroys the thick cell wall