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GENERAL
PHARMACOLOGY
1) HISTORY OF MEDICINE
2) INTRODUCTION TO PHARMACOLOGY
3) PHARMACOKINETIC
•ABSORPTON
•DISTRIBUTION
•BIOTRANSFORMATION
•ELIMINATION
•CLINICAL PHARMACOKINETIC
4) PHARMACODYNAMIC
5) DRUG INTERACTIONS
6) FACTORS THAT MODIFY DRUG ACTIONS
7) CLINICAL PHARMACOLOGY
8) DRUG TOXICOLOGY
9) PHARMACOGENETIC
10)
HISTORY OF MEDICINE
• As old as the history of human being
• As old as the age of pain an sufferings
• So, PAIN and sufferings were the first sensed alarm reactions that
drew the attention of human being.
Thus, surge was focused on how to combat with these
leading symptoms
By experience, the analgesic power of certain plants was
explored accidentally first
• HISTORICAL DEVELOPMENT
a) PRE-EXPERIMENTAL PERIOD (might be up to 1789)
b) EXPERIMENTAL PERIOD
• PRE-XPERIMENTAL PERIOD:
Depends on experience rather than experimentation
Mostly uses trial and error method
Under strict influence of religious and traditional beliefs
No experimentation at all
No questioning by what, why and how
Curative potential of plants was discovered accidentally

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The reason of illnesses was widely believed to be due to bad
spirits which were dismissed from body by magicians
SO, magicians were the first medical men who were also the
religious leader who were conducting ritual ceremonies
Belief in the curative powers of plants and certain
substances was exclusively depending upon traditional
knowledge which was empirical rather than subject to
critical examination
The effects of Opium, Belladonnae, Rauwolfia, Digitalis,
Curare etc. were discovered by experience accidentally and
were used empirically
• EXPERIMENTAL PERIOD:
Questioning with what, how and why
Not under religious and traditional false beliefs
Depending on experimental results
Reached by revolution in the brain cortex
• CHRONOLOGICAL BACKGROUND
First informations on opium and other curative plants appear in
the Sumerian and Egyptian manuscripts or tablets
First documental knowledge on drugs are deduced from EBERS
PAPYRUS written in 1550 B.C.
1sth
. Century A.C.: DIOSCORIDES assembled that far known
drugs in a book which is considered the first PHARMACOPEA
2nd
. Century A.C.: CLAUDIUS GALEN (129-200 A.C.)
He says: “All is found, is in part be experience and in part
theory. Neither experience nor theory alone apt to
discover all”
He described the ways to prepare drug forms from plants, eg.
powder, tincture, decoction, extract etc. which are called
GALENIC PREPARATIONS.
MIDDLE AGE:
Orientation to polypharmacy. A pharmaceutical form
possessing more than 100 active principle in it is called
THERIACA or TRIACA
Development in chemistry and synthesis of new
substances increased therapeutic facilities. Thus, new
substances were introduced into the therapy.
- John Rudolph Glauber (1604-1688): Na sulphate
-Aureolus Theophrastus Bombastus (PARACELSUS)
from Hochenheim (1493-1541): Iron and Arsenic
- He rejected irrational medicaments of
medieval medicine

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- He prescribed chemically defined
substances with success only
The influence of magic and religion (i.e. church) were
crushed down.
Experimental results and rationalism became the leading
approach for the treatment.
Johan Jacob Wepfer (1620-1695) was the first to
verify th pharmacologic and toxic actions of drugs by
animal experimentation
Serturner isolated morphine from opium milk
Emil Fisher synthesized barbital, a hypnotic
Paul Ehrlich by trying more than 500 bacteria dyes
and 606 newly synthesized chemicals on animals,
discovered the first useful chemotherapeutics
Oswald Schmiedeberg (1838-1921)
-Insisted on -structure activity relationship
-drug receptors
-selective toxicology
-With his students: T. Frazer from Scothland
Langley from England
P, Ehrlich from Germany
J. Clark from England
Was the first a) to propose receptor theories
b) to apply law of mass action to
drug-receptor interaction
-Published the first journal of pharmacology
John Abel, a student of O. Schmiedeberg, was the first to
publish J Pharmacol Exp Ther in USA
Pharmacology developed within physiology as
pharmacodynamic by experimentation of drugs on animals
The first pharmacologists were in fact physiologists
-Rudolph Bucheim (1846) in Dorpat Medical Faculty
was appointed as pharmacology lecturer for the fist time.
He investigated certain effects of atropine and ergot
alkaloids.
-Claud Bernard investigated the effects of curare and
morphine
O. Schmiedeberg was appointed as the director of
pharmacology department in Strasburg for the first time.
-Otto Loewi and Guddum improved biological essay
methods and developed comparative pharmacology
-Most recently gene cloning technology was developed

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By this way, pharmacology became an independent discipline
in medicine.
COCLUSION: Cordial respect to those who did their best
for human being.
INTRODUCTION TO PHARMACOLOGY
• PARMACOLOGY = Pharmacon + Logos
Drug Scıence
= Drug Science
= The science that deals with the interaction of living
systems with chemicals (endogenous or exogenous)
• SUBDIVISION OF PHARMACOLOGY:
1) MEDICAL PHARMACOLOGY:
Deals with materials used to prevent, diagnose and treat diseases.
2) PHARMACOTHERAPY:
Employment of drugs for the prevention and treatment of
diseases.
Its scope: -Indications
-Contraindications
-Drug interactions
-Rational therapy design (art of therapy planning)
-Good prescribing
THERAPY: i) Radical (full healing)
ii) Symptomatic(treatment of symptoms only)
iii)Prophylactic (eg. contraception, vaccine)
3) CLINICAL PHARMACOLOGY:
Deals with: -the discovery and development of new drug molecules
-evaluation of these on healthy and diseased human being
after enough experimentation on animals
-should not be mixed with pharmacotherapy and
art of prescription writings
4) CHEMOTHEREAPY:
Deals with the treatment of infectious and neoplastic disorders
5) PHARMACOKINETIC:
Deals with how the body handles a drug.
Its scope: - Absorption
- Distribution
- Biotransformation (metabolism)
- Elimination

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6) PHARMACODYNAMIC:
-Deals with how drug handles the body
-Deals with the biochemical and physiological effects
(beneficial or toxic) of drugs and their mechanism of action
in human being.
7) PHARMACOGENETIC:
Deals with:- the influence of genetic on the mode of drug actions
(eg. metabolism)
- and biological variations of drug responses
8) BIOPHARMACEUTIC:
Deals with: - the production of drug forms
- and the relationship between the pharmacokinetic of
these forms and their effects
9) PHARMACOGNOSIA:
Deals with plants possessing active principles
Eg. Digitalis purpurea
Atropa belladonnae
Papaver somniferum
10) IMMUNOPHARMACOLOGY
Deals with drugs that can bring about an effect by acting on immune
System: - Immunosuppressive agents used in organ transplantation
and in autoimmune disorders
- Immunomodulators like immunostimulants used in
immune deficiencies
11) TOXİCOLOGY:
Deals with undesirable or adverse effects of chemicals in
biological systems.
Drug Effects
Desirable Undesirable
(therapeutic)
Non-deleterious Deleterious
(side effects) (toxic effects)
-Pharmacologic
-Pathologic
-Genotoxic
(nitrogen mustard)
Liver: Acetaminophene
Lung: Paraquat (herbesite)
Phototoxicity: Sulfonamides, tetracyclines

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There is no strict limit between drugs, nutrients and poisons
DRUG
NUTRIENT POISON
Eg. - Water
- Vitamines
- d-Tubocurarine
• DRUG
The main concern of pharmacology.
Definitions: 1) Drugs are active chemical principles used in medicine
2) WHO: Drug is a compound used to change the
physiological functions or pathophysiological condi-
ditions for the benefit of human being.
3) MORE GENERAL: Any substance that bring about
changes in biological functions through its chemical
action.
4) OR: Drug is any small molecule that alter body
functions by interaction at the molecular level.
• Drug actions are mediated by 3 ways:
1) By acting on somatic or psychic processes or
functions.
2) By correction of deficiencies
3) By toxic action on pathogenic microorganism
• Drug effects: - Should be -selective
-temporary
-dose-related (controllable)
- And show close relationship with bioavailability
• HOW ARE DRUGS RESPONSES PRODUCED?
By interaction with active binding sites called RECEPTORS
- Inert binding sites (plasma & tissue proteins) do not
bring about a biological response
- Drug may be agonist or antagonist for the receptors
- Interaction wit receptors may be covalent, electrostatic..
- For best fitting, drug size, shape, electrical charges and
atomic composition are important
- Majority of drug size fall in 100 to 1000
-Small molecules are more selective in its action
-Large molecules move more slowly (mw 1000)

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Influence of physical nature of drugs
Physical state: -solid (aspirin)
-liquid(nicotine, ethanol) -Determine
-Gas route of
-Vaporizable liquid forms administration
Chemical structure: Protein, lipid, carbohydrate
To be weak acid or weak base
Primary amine : R-NH2
Secondary amine: R2-NH
Tertiary amine : R3-N
Quaternary : R4-N+
Isomeric forms: (+)d, (-)l, dl
Drug-body interactions: -PHARMACOKINETIC
-PHARMACOYNAMIC
• SOURCES OF DRUGS: 1) NATURAL
- Plants
- Animals
- Bacteria, fungi
- Inorganic compounds
2) SEMISYNTHETIC
3) Synthetic
4) DNA recombinant technology
DRUGS FROM PANTS:
- Active principles are found in roots, leaves and seeds in
2 forms: 1) Glycoside
2) Alkaloid
TO BE ALKALOİD TO BE GLYCOSIDE
-Must be of plant origin -Must be of plant origin
-Has a nitrogen atom in a -aglycone-O-carbohydrate
heterocyclic ring system linkage
-Has bitter taste -Genin (aglycone) is the avtive
-Base form is not soluble in component
water but in alcohol -eg. Digital glycosides
-Salt form is soluble in water
-eg. Morphine, curare, atropine
Pharmaceutical forms obtained from plans:
(GALENIC PREPARATIONS)
1) POWDERS
2) EXTRACTS: -Obtained by incubation in solvents
- May be soft, semisolid or dry

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3) INFUSIONS: -Obtained by incubation in hot water
-eg. Tea
- Must be prepared freshly
4) DECOCTIONS: -Obtained by boiling in water
-eg. Lindon blossom
5) TINCTURES: -Obtained by treatment with alcohol
-eg. Digital tincture
DRUGS FROM ANIMALS
-Hormones like heparin, insulin
-Plasma or serum from blood
-Gonadotrophines from urine of pregnant women
DRUGS FROM MICROORGANISMS:
-Antibiotics
-Streptokinase, streptodorinase
INORGANIC METALS:
-Iodine
-Lithium
-Radioactive elements: 131
I, 198
Au, 60
Co
SEMISYNTHETIC DRUGS
-Semisynthetic penicillins from 6-aminopenicillnic
acid
-Semisynthetic cephalosporins from 7-amino
cephalosporinic acid
-LSD from natural lysergic acid
DRUGS BY DNA RECOMBINANT TECHNOLOGY
Cells from animals or human that
produce active principle
Isolation of DNA
Release of DNA fragments
By endonuclease
Transfer to E-coli
by plasmids
(Gene cloning)
A new E-coli form
that synthesize the
the new substance

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• CRITERIA FOR DRUG CLASSIFICATION
1) Chemical structure: - Cholinester
- Organophosphates
- Catecholamines
2) Locus of action: - Heart glycosides
- Autonomic drugs
3) Purpose of medication: - Antihypertensive
- Diuretic
- Antiemetic
- Analgesic
4) Name of plant: - Opium alkaloids
- Digital glycosides Papaver somniferum
- Belladonnae alkaloids
• DRUG NAMES: 1) General or generic name given by WHO
3) Trade name given by the DRUG FIRMS
4) Chemical name which is LONG, COMPLEX AND
NOT USED CURRENTLY
Papaver somniferum

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